TW200808390A - Inhaler - Google Patents
Inhaler Download PDFInfo
- Publication number
- TW200808390A TW200808390A TW096112554A TW96112554A TW200808390A TW 200808390 A TW200808390 A TW 200808390A TW 096112554 A TW096112554 A TW 096112554A TW 96112554 A TW96112554 A TW 96112554A TW 200808390 A TW200808390 A TW 200808390A
- Authority
- TW
- Taiwan
- Prior art keywords
- inhaler
- amino
- capsule
- phenyl
- medicament
- Prior art date
Links
- 239000003814 drug Substances 0.000 claims abstract description 30
- 239000000126 substance Substances 0.000 claims abstract description 11
- 239000000203 mixture Substances 0.000 claims abstract description 9
- 238000009472 formulation Methods 0.000 claims abstract 2
- 239000002775 capsule Substances 0.000 claims description 40
- 239000002253 acid Substances 0.000 claims description 16
- 230000004913 activation Effects 0.000 claims description 10
- 229920003023 plastic Polymers 0.000 claims description 10
- 239000004033 plastic Substances 0.000 claims description 10
- 239000005557 antagonist Substances 0.000 claims description 9
- 229940079593 drug Drugs 0.000 claims description 9
- 239000000812 cholinergic antagonist Substances 0.000 claims description 7
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims description 5
- 239000013543 active substance Substances 0.000 claims description 5
- 239000003112 inhibitor Substances 0.000 claims description 4
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims description 3
- 239000000808 adrenergic beta-agonist Substances 0.000 claims description 2
- 230000003454 betamimetic effect Effects 0.000 claims description 2
- 239000002245 particle Substances 0.000 claims description 2
- 239000012780 transparent material Substances 0.000 claims description 2
- 229940127597 CGRP antagonist Drugs 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 239000000043 antiallergic agent Substances 0.000 claims 1
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims 1
- 239000011888 foil Substances 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 89
- -1 EGFR inhibitors Substances 0.000 description 87
- 150000003839 salts Chemical class 0.000 description 33
- 150000001875 compounds Chemical class 0.000 description 15
- GZUXJHMPEANEGY-UHFFFAOYSA-N methyl bromide Substances BrC GZUXJHMPEANEGY-UHFFFAOYSA-N 0.000 description 15
- 239000002585 base Substances 0.000 description 10
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 10
- 229940102396 methyl bromide Drugs 0.000 description 10
- 239000001257 hydrogen Substances 0.000 description 9
- 229910052739 hydrogen Inorganic materials 0.000 description 9
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 8
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 7
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 7
- 229940121647 egfr inhibitor Drugs 0.000 description 7
- 125000001207 fluorophenyl group Chemical group 0.000 description 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 7
- 239000012453 solvate Substances 0.000 description 7
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 description 6
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 5
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 5
- 125000003277 amino group Chemical group 0.000 description 5
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 5
- 239000003246 corticosteroid Substances 0.000 description 5
- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- MUBZPKHOEPUJKR-UHFFFAOYSA-M oxalate(1-) Chemical compound OC(=O)C([O-])=O MUBZPKHOEPUJKR-UHFFFAOYSA-M 0.000 description 5
- 239000000843 powder Substances 0.000 description 5
- 229910021653 sulphate ion Inorganic materials 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 description 4
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 4
- FEWJPZIEWOKRBE-JCYAYHJZSA-M L-tartrate(1-) Chemical compound OC(=O)[C@H](O)[C@@H](O)C([O-])=O FEWJPZIEWOKRBE-JCYAYHJZSA-M 0.000 description 4
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 4
- 150000002431 hydrogen Chemical class 0.000 description 4
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 4
- 210000000214 mouth Anatomy 0.000 description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 4
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-L 2-(carboxymethyl)-2-hydroxysuccinate Chemical compound [O-]C(=O)CC(O)(C(=O)O)CC([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-L 0.000 description 3
- CHRMMMLUWHPZAH-UHFFFAOYSA-N 7-methoxyquinazoline Chemical compound C1=NC=NC2=CC(OC)=CC=C21 CHRMMMLUWHPZAH-UHFFFAOYSA-N 0.000 description 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 3
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- 206010011469 Crying Diseases 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 3
- 229910019142 PO4 Inorganic materials 0.000 description 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 3
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical class OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 3
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 3
- 229930013930 alkaloid Natural products 0.000 description 3
- 150000001450 anions Chemical class 0.000 description 3
- 150000003842 bromide salts Chemical class 0.000 description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-M fumarate(1-) Chemical compound OC(=O)\C=C\C([O-])=O VZCYOOQTPOCHFL-OWOJBTEDSA-M 0.000 description 3
- 239000007789 gas Substances 0.000 description 3
- 150000004677 hydrates Chemical class 0.000 description 3
- 239000010452 phosphate Substances 0.000 description 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
- 235000021317 phosphate Nutrition 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- KDYFGRWQOYBRFD-UHFFFAOYSA-M succinate(1-) Chemical compound OC(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-M 0.000 description 3
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 3
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 2
- ULMFXAMQUGLVGA-LJQANCHMSA-N 3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methyl-n-[(2r)-4,4,4-trifluoro-2-methylbutyl]indole-5-carboxamide Chemical compound C=1C=C(CC=2C3=CC(=CC=C3N(C)C=2)C(=O)NC[C@H](C)CC(F)(F)F)C(OC)=CC=1C(=O)NS(=O)(=O)C1=CC=CC=C1C ULMFXAMQUGLVGA-LJQANCHMSA-N 0.000 description 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 description 2
- PYUGFOWNYMLROI-KPKJPENVSA-N 8-[(e)-2-[4-[4-(4-fluorophenyl)butoxy]phenyl]ethenyl]-2-(2h-tetrazol-5-yl)chromen-4-one Chemical compound C1=CC(F)=CC=C1CCCCOC(C=C1)=CC=C1\C=C\C1=CC=CC2=C1OC(C=1NN=NN=1)=CC2=O PYUGFOWNYMLROI-KPKJPENVSA-N 0.000 description 2
- NLHHRLWOUZZQLW-UHFFFAOYSA-N Acrylonitrile Chemical compound C=CC#N NLHHRLWOUZZQLW-UHFFFAOYSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- XTEGARKTQYYJKE-UHFFFAOYSA-M Chlorate Chemical compound [O-]Cl(=O)=O XTEGARKTQYYJKE-UHFFFAOYSA-M 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- 241000272186 Falco columbarius Species 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 2
- 229910002651 NO3 Inorganic materials 0.000 description 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 description 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-L Phosphate ion(2-) Chemical compound OP([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-L 0.000 description 2
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 2
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 2
- 235000011054 acetic acid Nutrition 0.000 description 2
- 150000003797 alkaloid derivatives Chemical class 0.000 description 2
- 150000001412 amines Chemical class 0.000 description 2
- RDOXTESZEPMUJZ-UHFFFAOYSA-N anisole Chemical compound COC1=CC=CC=C1 RDOXTESZEPMUJZ-UHFFFAOYSA-N 0.000 description 2
- 239000000739 antihistaminic agent Substances 0.000 description 2
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 description 2
- TXKAQZRUJUNDHI-UHFFFAOYSA-K bismuth tribromide Chemical compound Br[Bi](Br)Br TXKAQZRUJUNDHI-UHFFFAOYSA-K 0.000 description 2
- 150000001649 bromium compounds Chemical class 0.000 description 2
- FVGVORIVAWDBMI-UHFFFAOYSA-N bromomethane;2,2-diphenylpropanoic acid Chemical compound BrC.C=1C=CC=CC=1C(C(O)=O)(C)C1=CC=CC=C1 FVGVORIVAWDBMI-UHFFFAOYSA-N 0.000 description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- CFBUZOUXXHZCFB-OYOVHJISSA-N chembl511115 Chemical compound COC1=CC=C([C@@]2(CC[C@H](CC2)C(O)=O)C#N)C=C1OC1CCCC1 CFBUZOUXXHZCFB-OYOVHJISSA-N 0.000 description 2
- 125000001309 chloro group Chemical group Cl* 0.000 description 2
- 238000004140 cleaning Methods 0.000 description 2
- 229960001334 corticosteroids Drugs 0.000 description 2
- NZNMSOFKMUBTKW-UHFFFAOYSA-N cyclohexanecarboxylic acid Chemical compound OC(=O)C1CCCCC1 NZNMSOFKMUBTKW-UHFFFAOYSA-N 0.000 description 2
- 229960003957 dexamethasone Drugs 0.000 description 2
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 2
- 229960000520 diphenhydramine Drugs 0.000 description 2
- 239000003136 dopamine receptor stimulating agent Substances 0.000 description 2
- 229960003133 ergot alkaloid Drugs 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 description 2
- 150000003840 hydrochlorides Chemical class 0.000 description 2
- 229910052751 metal Inorganic materials 0.000 description 2
- 239000002184 metal Substances 0.000 description 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 2
- VMGAPWLDMVPYIA-HIDZBRGKSA-N n'-amino-n-iminomethanimidamide Chemical compound N\N=C\N=N VMGAPWLDMVPYIA-HIDZBRGKSA-N 0.000 description 2
- AZQWKYJCGOJGHM-UHFFFAOYSA-N para-benzoquinone Natural products O=C1C=CC(=O)C=C1 AZQWKYJCGOJGHM-UHFFFAOYSA-N 0.000 description 2
- 229950010765 pivalate Drugs 0.000 description 2
- IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 2
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 2
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 description 2
- BOLDJAUMGUJJKM-LSDHHAIUSA-N renifolin D Natural products CC(=C)[C@@H]1Cc2c(O)c(O)ccc2[C@H]1CC(=O)c3ccc(O)cc3O BOLDJAUMGUJJKM-LSDHHAIUSA-N 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 239000002689 soil Substances 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 229910001220 stainless steel Inorganic materials 0.000 description 2
- 239000010935 stainless steel Substances 0.000 description 2
- UBXAKNTVXQMEAG-UHFFFAOYSA-L strontium sulfate Chemical compound [Sr+2].[O-]S([O-])(=O)=O UBXAKNTVXQMEAG-UHFFFAOYSA-L 0.000 description 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 2
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 2
- 229940095064 tartrate Drugs 0.000 description 2
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 2
- 229920001169 thermoplastic Polymers 0.000 description 2
- 239000004416 thermosoftening plastic Substances 0.000 description 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 2
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 description 1
- XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 description 1
- MCKJPJYRCPANCC-XLXYOEISSA-N (8s,9s,10r,11s,13s,14s,17r)-11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-17-carboxylic acid Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(O)=O)[C@@H]4[C@@H]3CCC2=C1 MCKJPJYRCPANCC-XLXYOEISSA-N 0.000 description 1
- IATKKATWPOVYCC-VMXHOPILSA-N (8s,9s,10r,13s,14s)-10,13-dimethyl-2,3,6,7,8,9,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthrene Chemical compound C1CC2=CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CCC[C@@]1(C)CC2 IATKKATWPOVYCC-VMXHOPILSA-N 0.000 description 1
- NDAUXUAQIAJITI-LBPRGKRZSA-N (R)-salbutamol Chemical compound CC(C)(C)NC[C@H](O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-LBPRGKRZSA-N 0.000 description 1
- SILNNFMWIMZVEQ-UHFFFAOYSA-N 1,3-dihydrobenzimidazol-2-one Chemical compound C1=CC=C2NC(O)=NC2=C1 SILNNFMWIMZVEQ-UHFFFAOYSA-N 0.000 description 1
- VXNZUUAINFGPBY-UHFFFAOYSA-N 1-Butene Chemical compound CCC=C VXNZUUAINFGPBY-UHFFFAOYSA-N 0.000 description 1
- ZCJAYDKWZAWMPR-UHFFFAOYSA-N 1-chloro-2-fluorobenzene Chemical compound FC1=CC=CC=C1Cl ZCJAYDKWZAWMPR-UHFFFAOYSA-N 0.000 description 1
- VZHJIJZEOCBKRA-UHFFFAOYSA-N 1-chloro-3-fluorobenzene Chemical compound FC1=CC=CC(Cl)=C1 VZHJIJZEOCBKRA-UHFFFAOYSA-N 0.000 description 1
- 125000004343 1-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C([H])([H])[H] 0.000 description 1
- VGCZCJQRGDELDD-UHFFFAOYSA-N 2,2-dioxo-1,3,2-dioxathiepane-4,7-dione Chemical compound O=C1CCC(=O)OS(=O)(=O)O1 VGCZCJQRGDELDD-UHFFFAOYSA-N 0.000 description 1
- SNTWKPAKVQFCCF-UHFFFAOYSA-N 2,3-dihydro-1h-triazole Chemical compound N1NC=CN1 SNTWKPAKVQFCCF-UHFFFAOYSA-N 0.000 description 1
- IMSODMZESSGVBE-UHFFFAOYSA-N 2-Oxazoline Chemical compound C1CN=CO1 IMSODMZESSGVBE-UHFFFAOYSA-N 0.000 description 1
- MAGCRYYXZYUDSY-UHFFFAOYSA-N 2-fluoro-2,2-diphenylacetic acid Chemical compound C=1C=CC=CC=1C(F)(C(=O)O)C1=CC=CC=C1 MAGCRYYXZYUDSY-UHFFFAOYSA-N 0.000 description 1
- FWWOWPGPERBCNJ-UHFFFAOYSA-N 2-hydroxy-4-(2-hydroxyethoxy)-4-oxobutanoic acid Chemical compound OCCOC(=O)CC(O)C(O)=O FWWOWPGPERBCNJ-UHFFFAOYSA-N 0.000 description 1
- BWYJJZBRYSADRP-UHFFFAOYSA-N 2-methoxyquinazoline Chemical compound C1=CC=CC2=NC(OC)=NC=C21 BWYJJZBRYSADRP-UHFFFAOYSA-N 0.000 description 1
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 description 1
- DDYUBCCTNHWSQM-UHFFFAOYSA-N 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-(1,3-dioxoisoindol-2-yl)propanamide Chemical compound COC1=CC=C(C(CC(N)=O)N2C(C3=CC=CC=C3C2=O)=O)C=C1OC1CCCC1 DDYUBCCTNHWSQM-UHFFFAOYSA-N 0.000 description 1
- LIXBJWRFCNRAPA-NSHDSACASA-N 4-[(1r)-2-(tert-butylamino)-1-hydroxyethyl]-3-chlorophenol Chemical compound CC(C)(C)NC[C@H](O)C1=CC=C(O)C=C1Cl LIXBJWRFCNRAPA-NSHDSACASA-N 0.000 description 1
- LIXBJWRFCNRAPA-UHFFFAOYSA-N 4-[2-(tert-butylamino)-1-hydroxyethyl]-3-chlorophenol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C=C1Cl LIXBJWRFCNRAPA-UHFFFAOYSA-N 0.000 description 1
- LSLYOANBFKQKPT-DIFFPNOSSA-N 5-[(1r)-1-hydroxy-2-[[(2r)-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]benzene-1,3-diol Chemical compound C([C@@H](C)NC[C@H](O)C=1C=C(O)C=C(O)C=1)C1=CC=C(O)C=C1 LSLYOANBFKQKPT-DIFFPNOSSA-N 0.000 description 1
- DHSSDEDRBUKTQY-UHFFFAOYSA-N 6-prop-2-enyl-4,5,7,8-tetrahydrothiazolo[4,5-d]azepin-2-amine Chemical compound C1CN(CC=C)CCC2=C1N=C(N)S2 DHSSDEDRBUKTQY-UHFFFAOYSA-N 0.000 description 1
- XEKAWZARUWARND-UHFFFAOYSA-N 6h-oxazin-3-one Chemical compound O=C1NOCC=C1 XEKAWZARUWARND-UHFFFAOYSA-N 0.000 description 1
- MBUVEWMHONZEQD-UHFFFAOYSA-N Azeptin Chemical compound C1CN(C)CCCC1N1C(=O)C2=CC=CC=C2C(CC=2C=CC(Cl)=CC=2)=N1 MBUVEWMHONZEQD-UHFFFAOYSA-N 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 description 1
- QGBIFMJAQARMNQ-QISPFCDLSA-N C1([C@@H](F)C2)=CC(=O)CC[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3O[C@@H](CCC)O[C@@]3(SC)[C@@]2(C)C[C@@H]1O Chemical compound C1([C@@H](F)C2)=CC(=O)CC[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3O[C@@H](CCC)O[C@@]3(SC)[C@@]2(C)C[C@@H]1O QGBIFMJAQARMNQ-QISPFCDLSA-N 0.000 description 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 description 1
- 244000025254 Cannabis sativa Species 0.000 description 1
- ZKLPARSLTMPFCP-UHFFFAOYSA-N Cetirizine Chemical compound C1CN(CCOCC(=O)O)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-UHFFFAOYSA-N 0.000 description 1
- LUKZNWIVRBCLON-GXOBDPJESA-N Ciclesonide Chemical compound C1([C@H]2O[C@@]3([C@H](O2)C[C@@H]2[C@@]3(C[C@H](O)[C@@H]3[C@@]4(C)C=CC(=O)C=C4CC[C@H]32)C)C(=O)COC(=O)C(C)C)CCCCC1 LUKZNWIVRBCLON-GXOBDPJESA-N 0.000 description 1
- MHZGKXUYDGKKIU-UHFFFAOYSA-N Decylamine Chemical compound CCCCCCCCCCN MHZGKXUYDGKKIU-UHFFFAOYSA-N 0.000 description 1
- 101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 description 1
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 1
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 description 1
- 229930194542 Keto Natural products 0.000 description 1
- ZCVMWBYGMWKGHF-UHFFFAOYSA-N Ketotifene Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CC(=O)C2=C1C=CS2 ZCVMWBYGMWKGHF-UHFFFAOYSA-N 0.000 description 1
- 241000272168 Laridae Species 0.000 description 1
- OCJYIGYOJCODJL-UHFFFAOYSA-N Meclizine Chemical compound CC1=CC=CC(CN2CCN(CC2)C(C=2C=CC=CC=2)C=2C=CC(Cl)=CC=2)=C1 OCJYIGYOJCODJL-UHFFFAOYSA-N 0.000 description 1
- PVLJETXTTWAYEW-UHFFFAOYSA-N Mizolastine Chemical compound N=1C=CC(=O)NC=1N(C)C(CC1)CCN1C1=NC2=CC=CC=C2N1CC1=CC=C(F)C=C1 PVLJETXTTWAYEW-UHFFFAOYSA-N 0.000 description 1
- UCHDWCPVSPXUMX-TZIWLTJVSA-N Montelukast Chemical compound CC(C)(O)C1=CC=CC=C1CC[C@H](C=1C=C(\C=C\C=2N=C3C=C(Cl)C=CC3=CC=2)C=CC=1)SCC1(CC(O)=O)CC1 UCHDWCPVSPXUMX-TZIWLTJVSA-N 0.000 description 1
- IJHNSHDBIRRJRN-UHFFFAOYSA-N N,N-dimethyl-3-phenyl-3-(2-pyridinyl)-1-propanamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=CC=C1 IJHNSHDBIRRJRN-UHFFFAOYSA-N 0.000 description 1
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 1
- JAUOIFJMECXRGI-UHFFFAOYSA-N Neoclaritin Chemical compound C=1C(Cl)=CC=C2C=1CCC1=CC=CN=C1C2=C1CCNCC1 JAUOIFJMECXRGI-UHFFFAOYSA-N 0.000 description 1
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 241000233805 Phoenix Species 0.000 description 1
- YGYAWVDWMABLBF-UHFFFAOYSA-N Phosgene Chemical class ClC(Cl)=O YGYAWVDWMABLBF-UHFFFAOYSA-N 0.000 description 1
- VQDBNKDJNJQRDG-UHFFFAOYSA-N Pirbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=N1 VQDBNKDJNJQRDG-UHFFFAOYSA-N 0.000 description 1
- 101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 description 1
- 239000004952 Polyamide Substances 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 206010036790 Productive cough Diseases 0.000 description 1
- BPZSYCZIITTYBL-YJYMSZOUSA-N R-Formoterol Chemical compound C1=CC(OC)=CC=C1C[C@@H](C)NC[C@H](O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-YJYMSZOUSA-N 0.000 description 1
- BKRGVLQUQGGVSM-KBXCAEBGSA-N Revanil Chemical compound C1=CC(C=2[C@H](N(C)C[C@H](C=2)NC(=O)N(CC)CC)C2)=C3C2=CNC3=C1 BKRGVLQUQGGVSM-KBXCAEBGSA-N 0.000 description 1
- RUOGJYKOQBFJIG-UHFFFAOYSA-N SCH-351591 Chemical compound C12=CC=C(C(F)(F)F)N=C2C(OC)=CC=C1C(=O)NC1=C(Cl)C=[N+]([O-])C=C1Cl RUOGJYKOQBFJIG-UHFFFAOYSA-N 0.000 description 1
- VPMWDFRZSIMDKW-YJYMSZOUSA-N Salmefamol Chemical compound C1=CC(OC)=CC=C1C[C@@H](C)NC[C@H](O)C1=CC=C(O)C(CO)=C1 VPMWDFRZSIMDKW-YJYMSZOUSA-N 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical class O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 206010041235 Snoring Diseases 0.000 description 1
- 240000006394 Sorghum bicolor Species 0.000 description 1
- 235000011684 Sorghum saccharatum Nutrition 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 239000005864 Sulphur Substances 0.000 description 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 description 1
- JOAHPSVPXZTVEP-YXJHDRRASA-N Terguride Chemical compound C1=CC([C@H]2C[C@@H](CN(C)[C@@H]2C2)NC(=O)N(CC)CC)=C3C2=CNC3=C1 JOAHPSVPXZTVEP-YXJHDRRASA-N 0.000 description 1
- DHCOPPHTVOXDKU-UHFFFAOYSA-N Tofimilast Chemical compound C1CN2C(C=3SC=CC=3)=NN=C2C2=C1C(CC)=NN2C1CCCC1 DHCOPPHTVOXDKU-UHFFFAOYSA-N 0.000 description 1
- 241000270506 Tupinambis Species 0.000 description 1
- BZHJMEDXRYGGRV-UHFFFAOYSA-N Vinyl chloride Chemical compound ClC=C BZHJMEDXRYGGRV-UHFFFAOYSA-N 0.000 description 1
- YEEZWCHGZNKEEK-UHFFFAOYSA-N Zafirlukast Chemical compound COC1=CC(C(=O)NS(=O)(=O)C=2C(=CC=CC=2)C)=CC=C1CC(C1=C2)=CN(C)C1=CC=C2NC(=O)OC1CCCC1 YEEZWCHGZNKEEK-UHFFFAOYSA-N 0.000 description 1
- ANGKOCUUWGHLCE-HKUYNNGSSA-N [(3s)-1,1-dimethylpyrrolidin-1-ium-3-yl] (2r)-2-cyclopentyl-2-hydroxy-2-phenylacetate Chemical class C1[N+](C)(C)CC[C@@H]1OC(=O)[C@](O)(C=1C=CC=CC=1)C1CCCC1 ANGKOCUUWGHLCE-HKUYNNGSSA-N 0.000 description 1
- HOAKOHHSHOCDLI-TUFAYURCSA-N [(8s,9s,10r,11s,13s,14s,17r)-11-hydroxy-10,13-dimethyl-3-oxo-17-(2-sulfanylacetyl)-2,6,7,8,9,11,12,14,15,16-decahydro-1h-cyclopenta[a]phenanthren-17-yl] butanoate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)CS)(OC(=O)CCC)[C@@]1(C)C[C@@H]2O HOAKOHHSHOCDLI-TUFAYURCSA-N 0.000 description 1
- YPFLFUJKZDAXRA-UHFFFAOYSA-N [3-(carbamoylamino)-2-(2,4-dichlorobenzoyl)-1-benzofuran-6-yl] methanesulfonate Chemical compound O1C2=CC(OS(=O)(=O)C)=CC=C2C(NC(N)=O)=C1C(=O)C1=CC=C(Cl)C=C1Cl YPFLFUJKZDAXRA-UHFFFAOYSA-N 0.000 description 1
- WKHOPHIMYDJVSA-UHFFFAOYSA-N [3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(2-methylpropanoyloxy)phenyl] 2-methylpropanoate Chemical compound CC(C)C(=O)OC1=CC(OC(=O)C(C)C)=CC(C(O)CNC(C)(C)C)=C1 WKHOPHIMYDJVSA-UHFFFAOYSA-N 0.000 description 1
- RBXBKNSKYADFNQ-AHUNZLEGSA-H [Bi+3].[Bi+3].[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O Chemical compound [Bi+3].[Bi+3].[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O RBXBKNSKYADFNQ-AHUNZLEGSA-H 0.000 description 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 1
- NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 150000001340 alkali metals Chemical class 0.000 description 1
- 229940037003 alum Drugs 0.000 description 1
- 150000005018 aminopurines Chemical class 0.000 description 1
- 230000001387 anti-histamine Effects 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 229960001692 arformoterol Drugs 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 229960004574 azelastine Drugs 0.000 description 1
- 229960003060 bambuterol Drugs 0.000 description 1
- ANZXOIAKUNOVQU-UHFFFAOYSA-N bambuterol Chemical compound CN(C)C(=O)OC1=CC(OC(=O)N(C)C)=CC(C(O)CNC(C)(C)C)=C1 ANZXOIAKUNOVQU-UHFFFAOYSA-N 0.000 description 1
- 229960002526 bamipine Drugs 0.000 description 1
- VZSXTYKGYWISGQ-UHFFFAOYSA-N bamipine Chemical compound C1CN(C)CCC1N(C=1C=CC=CC=1)CC1=CC=CC=C1 VZSXTYKGYWISGQ-UHFFFAOYSA-N 0.000 description 1
- 229910052788 barium Inorganic materials 0.000 description 1
- HQYOWPDUMCBSLQ-UHFFFAOYSA-L barium(2+);2,3-dihydroxybutanedioate Chemical compound [Ba+2].[O-]C(=O)C(O)C(O)C([O-])=O HQYOWPDUMCBSLQ-UHFFFAOYSA-L 0.000 description 1
- 229940092705 beclomethasone Drugs 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 229960002537 betamethasone Drugs 0.000 description 1
- UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-DVTGEIKXSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229960004620 bitolterol Drugs 0.000 description 1
- FZGVEKPRDOIXJY-UHFFFAOYSA-N bitolterol Chemical compound C1=CC(C)=CC=C1C(=O)OC1=CC=C(C(O)CNC(C)(C)C)C=C1OC(=O)C1=CC=C(C)C=C1 FZGVEKPRDOIXJY-UHFFFAOYSA-N 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 description 1
- 229960002802 bromocriptine Drugs 0.000 description 1
- JBRBWHCVRGURBA-UHFFFAOYSA-N broxaterol Chemical compound CC(C)(C)NCC(O)C1=CC(Br)=NO1 JBRBWHCVRGURBA-UHFFFAOYSA-N 0.000 description 1
- 229950008847 broxaterol Drugs 0.000 description 1
- 229960004436 budesonide Drugs 0.000 description 1
- 239000001273 butane Substances 0.000 description 1
- 229950001167 butixocort Drugs 0.000 description 1
- MFSZEZNGBZWFNC-UHFFFAOYSA-N butylbismuth Chemical compound CCCC[Bi] MFSZEZNGBZWFNC-UHFFFAOYSA-N 0.000 description 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 1
- 150000007942 carboxylates Chemical class 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 229960001386 carbuterol Drugs 0.000 description 1
- KEMXXQOFIRIICG-UHFFFAOYSA-N carbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(NC(N)=O)=C1 KEMXXQOFIRIICG-UHFFFAOYSA-N 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 239000003518 caustics Substances 0.000 description 1
- 229960001803 cetirizine Drugs 0.000 description 1
- 150000001805 chlorine compounds Chemical class 0.000 description 1
- FZFAMSAMCHXGEF-UHFFFAOYSA-N chloro formate Chemical compound ClOC=O FZFAMSAMCHXGEF-UHFFFAOYSA-N 0.000 description 1
- 229960003728 ciclesonide Drugs 0.000 description 1
- 229950001653 cilomilast Drugs 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical class OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 1
- 229960002881 clemastine Drugs 0.000 description 1
- YNNUSGIPVFPVBX-NHCUHLMSSA-N clemastine Chemical compound CN1CCC[C@@H]1CCO[C@@](C)(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 YNNUSGIPVFPVBX-NHCUHLMSSA-N 0.000 description 1
- 229960001117 clenbuterol Drugs 0.000 description 1
- STJMRWALKKWQGH-UHFFFAOYSA-N clenbuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(Cl)=C1 STJMRWALKKWQGH-UHFFFAOYSA-N 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- VZFUCHSFHOYXIS-UHFFFAOYSA-N cycloheptane carboxylic acid Natural products OC(=O)C1CCCCCC1 VZFUCHSFHOYXIS-UHFFFAOYSA-N 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000001887 cyclopentyloxy group Chemical group C1(CCCC1)O* 0.000 description 1
- 230000001120 cytoprotective effect Effects 0.000 description 1
- 125000006612 decyloxy group Chemical group 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 229960001145 deflazacort Drugs 0.000 description 1
- FBHSPRKOSMHSIF-GRMWVWQJSA-N deflazacort Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(C)=N[C@@]3(C(=O)COC(=O)C)[C@@]1(C)C[C@@H]2O FBHSPRKOSMHSIF-GRMWVWQJSA-N 0.000 description 1
- 229940120124 dichloroacetate Drugs 0.000 description 1
- JXTHNDFMNIQAHM-UHFFFAOYSA-N dichloroacetic acid Chemical compound OC(=O)C(Cl)Cl JXTHNDFMNIQAHM-UHFFFAOYSA-N 0.000 description 1
- HESHRHUZIWVEAJ-JGRZULCMSA-N dihydroergotamine Chemical compound C([C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@@](C(N21)=O)(C)NC(=O)[C@H]1CN([C@H]2[C@@H](C3=CC=CC4=NC=C([C]34)C2)C1)C)C1=CC=CC=C1 HESHRHUZIWVEAJ-JGRZULCMSA-N 0.000 description 1
- 229960004704 dihydroergotamine Drugs 0.000 description 1
- MZDOIJOUFRQXHC-UHFFFAOYSA-N dimenhydrinate Chemical compound O=C1N(C)C(=O)N(C)C2=NC(Cl)=N[C]21.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 MZDOIJOUFRQXHC-UHFFFAOYSA-N 0.000 description 1
- 229960004993 dimenhydrinate Drugs 0.000 description 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 description 1
- 229960001992 dimetindene Drugs 0.000 description 1
- MVMQESMQSYOVGV-UHFFFAOYSA-N dimetindene Chemical compound CN(C)CCC=1CC2=CC=CC=C2C=1C(C)C1=CC=CC=N1 MVMQESMQSYOVGV-UHFFFAOYSA-N 0.000 description 1
- 229940052760 dopamine agonists Drugs 0.000 description 1
- 229960005178 doxylamine Drugs 0.000 description 1
- HCFDWZZGGLSKEP-UHFFFAOYSA-N doxylamine Chemical compound C=1C=CC=NC=1C(C)(OCCN(C)C)C1=CC=CC=C1 HCFDWZZGGLSKEP-UHFFFAOYSA-N 0.000 description 1
- 239000003640 drug residue Substances 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 229960001971 ebastine Drugs 0.000 description 1
- MJJALKDDGIKVBE-UHFFFAOYSA-N ebastine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(=O)CCCN1CCC(OC(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 MJJALKDDGIKVBE-UHFFFAOYSA-N 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960000325 emedastine Drugs 0.000 description 1
- KBUZBQVCBVDWKX-UHFFFAOYSA-N emedastine Chemical compound N=1C2=CC=CC=C2N(CCOCC)C=1N1CCCN(C)CC1 KBUZBQVCBVDWKX-UHFFFAOYSA-N 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 229960003449 epinastine Drugs 0.000 description 1
- WHWZLSFABNNENI-UHFFFAOYSA-N epinastine Chemical compound C1C2=CC=CC=C2C2CN=C(N)N2C2=CC=CC=C21 WHWZLSFABNNENI-UHFFFAOYSA-N 0.000 description 1
- OFKDAAIKGIBASY-VFGNJEKYSA-N ergotamine Chemical compound C([C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@@](C(N21)=O)(C)NC(=O)[C@H]1CN([C@H]2C(C3=CC=CC4=NC=C([C]34)C2)=C1)C)C1=CC=CC=C1 OFKDAAIKGIBASY-VFGNJEKYSA-N 0.000 description 1
- 229960004943 ergotamine Drugs 0.000 description 1
- XCGSFFUVFURLIX-UHFFFAOYSA-N ergotaminine Natural products C1=C(C=2C=CC=C3NC=C(C=23)C2)C2N(C)CC1C(=O)NC(C(N12)=O)(C)OC1(O)C1CCCN1C(=O)C2CC1=CC=CC=C1 XCGSFFUVFURLIX-UHFFFAOYSA-N 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- ZOOODBUHSVUZEM-UHFFFAOYSA-N ethoxymethanedithioic acid Chemical compound CCOC(S)=S ZOOODBUHSVUZEM-UHFFFAOYSA-N 0.000 description 1
- JTXYEERBIZXLJC-DCJXKKNWSA-N ethyl (8s,9s,10r,11s,13s,14s,17r)-11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6h-cyclopenta[a]phenanthrene-17-carboxylate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)OCC)(O)[C@@]1(C)C[C@@H]2O JTXYEERBIZXLJC-DCJXKKNWSA-N 0.000 description 1
- 229960001022 fenoterol Drugs 0.000 description 1
- 229960003592 fexofenadine Drugs 0.000 description 1
- 229960002714 fluticasone Drugs 0.000 description 1
- MGNNYOODZCAHBA-GQKYHHCASA-N fluticasone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(O)[C@@]2(C)C[C@@H]1O MGNNYOODZCAHBA-GQKYHHCASA-N 0.000 description 1
- 229960002848 formoterol Drugs 0.000 description 1
- BPZSYCZIITTYBL-UHFFFAOYSA-N formoterol Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-UHFFFAOYSA-N 0.000 description 1
- 238000002309 gasification Methods 0.000 description 1
- 208000014617 hemorrhoid Diseases 0.000 description 1
- 229960000708 hexoprenaline Drugs 0.000 description 1
- OXLZNBCNGJWPRV-UHFFFAOYSA-N hexoprenaline Chemical compound C=1C=C(O)C(O)=CC=1C(O)CNCCCCCCNCC(O)C1=CC=C(O)C(O)=C1 OXLZNBCNGJWPRV-UHFFFAOYSA-N 0.000 description 1
- 125000003707 hexyloxy group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])O* 0.000 description 1
- TWTMQRXNAZGSCE-UHFFFAOYSA-N hydron;[6-(methylamino)-1-(2-methylpropanoyloxy)-5,6,7,8-tetrahydronaphthalen-2-yl] 2-methylpropanoate;chloride Chemical compound Cl.C1=CC(OC(=O)C(C)C)=C(OC(=O)C(C)C)C2=C1CC(NC)CC2 TWTMQRXNAZGSCE-UHFFFAOYSA-N 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 229950002451 ibuterol Drugs 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000001746 injection moulding Methods 0.000 description 1
- 239000012212 insulator Substances 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- OEXHQOGQTVQTAT-JRNQLAHRSA-N ipratropium Chemical class O([C@H]1C[C@H]2CC[C@@H](C1)[N@@+]2(C)C(C)C)C(=O)C(CO)C1=CC=CC=C1 OEXHQOGQTVQTAT-JRNQLAHRSA-N 0.000 description 1
- 229910052742 iron Inorganic materials 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 229940039009 isoproterenol Drugs 0.000 description 1
- 125000000468 ketone group Chemical group 0.000 description 1
- 229960004958 ketotifen Drugs 0.000 description 1
- 229960001120 levocabastine Drugs 0.000 description 1
- ZCGOMHNNNFPNMX-KYTRFIICSA-N levocabastine Chemical compound C1([C@@]2(C(O)=O)CCN(C[C@H]2C)[C@@H]2CC[C@@](CC2)(C#N)C=2C=CC(F)=CC=2)=CC=CC=C1 ZCGOMHNNNFPNMX-KYTRFIICSA-N 0.000 description 1
- 229950008204 levosalbutamol Drugs 0.000 description 1
- 229950008462 lirimilast Drugs 0.000 description 1
- 229960003587 lisuride Drugs 0.000 description 1
- 229960003088 loratadine Drugs 0.000 description 1
- JCCNYMKQOSZNPW-UHFFFAOYSA-N loratadine Chemical compound C1CN(C(=O)OCC)CCC1=C1C2=NC=CC=C2CCC2=CC(Cl)=CC=C21 JCCNYMKQOSZNPW-UHFFFAOYSA-N 0.000 description 1
- 229960001798 loteprednol Drugs 0.000 description 1
- JSJCTEKTBOKRST-UHFFFAOYSA-N mabuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(C(F)(F)F)=C1 JSJCTEKTBOKRST-UHFFFAOYSA-N 0.000 description 1
- 229950004407 mabuterol Drugs 0.000 description 1
- 229920002521 macromolecule Polymers 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 229960001474 meclozine Drugs 0.000 description 1
- 229960003194 meglumine Drugs 0.000 description 1
- 229950001737 meluadrine Drugs 0.000 description 1
- LMOINURANNBYCM-UHFFFAOYSA-N metaproterenol Chemical compound CC(C)NCC(O)C1=CC(O)=CC(O)=C1 LMOINURANNBYCM-UHFFFAOYSA-N 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-M methanesulfonate group Chemical class CS(=O)(=O)[O-] AFVFQIVMOAPDHO-UHFFFAOYSA-M 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- UZKWTJUDCOPSNM-UHFFFAOYSA-N methoxybenzene Substances CCCCOC=C UZKWTJUDCOPSNM-UHFFFAOYSA-N 0.000 description 1
- JZMJDSHXVKJFKW-UHFFFAOYSA-M methyl sulfate(1-) Chemical compound COS([O-])(=O)=O JZMJDSHXVKJFKW-UHFFFAOYSA-M 0.000 description 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
- 244000005700 microbiome Species 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 229960001144 mizolastine Drugs 0.000 description 1
- YGAMIEYKXHAVBP-UHFFFAOYSA-N molecular hydrogen;hydrochloride Chemical compound Cl.[H][H] YGAMIEYKXHAVBP-UHFFFAOYSA-N 0.000 description 1
- 229960001664 mometasone Drugs 0.000 description 1
- QLIIKPVHVRXHRI-CXSFZGCWSA-N mometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)C[C@@H]2O QLIIKPVHVRXHRI-CXSFZGCWSA-N 0.000 description 1
- 229960005127 montelukast Drugs 0.000 description 1
- VSEAAEQOQBMPQF-UHFFFAOYSA-N morpholin-3-one Chemical compound O=C1COCCN1 VSEAAEQOQBMPQF-UHFFFAOYSA-N 0.000 description 1
- 210000002200 mouth mucosa Anatomy 0.000 description 1
- DPHDSIQHVGSITN-UHFFFAOYSA-N n-(3,5-dichloropyridin-4-yl)-2-[1-[(4-fluorophenyl)methyl]-5-hydroxyindol-3-yl]-2-oxoacetamide Chemical compound C1=C(C(=O)C(=O)NC=2C(=CN=CC=2Cl)Cl)C2=CC(O)=CC=C2N1CC1=CC=C(F)C=C1 DPHDSIQHVGSITN-UHFFFAOYSA-N 0.000 description 1
- HHRNQOGXBRYCHF-UHFFFAOYSA-N n-[2-hydroxy-5-[1-hydroxy-2-(propan-2-ylamino)ethyl]phenyl]methanesulfonamide Chemical compound CC(C)NCC(O)C1=CC=C(O)C(NS(C)(=O)=O)=C1 HHRNQOGXBRYCHF-UHFFFAOYSA-N 0.000 description 1
- 239000005445 natural material Substances 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
- 239000011664 nicotinic acid Substances 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 229960005419 nitrogen Drugs 0.000 description 1
- 229960002657 orciprenaline Drugs 0.000 description 1
- 150000002923 oximes Chemical class 0.000 description 1
- 125000005825 oxyethoxy group Chemical group [H]C([H])(O[*:1])C([H])([H])O[*:2] 0.000 description 1
- 150000002926 oxygen Chemical class 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 229960001972 panitumumab Drugs 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 229960001190 pheniramine Drugs 0.000 description 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 description 1
- ABOYDMHGKWRPFD-UHFFFAOYSA-N phenylmethanesulfonamide Chemical compound NS(=O)(=O)CC1=CC=CC=C1 ABOYDMHGKWRPFD-UHFFFAOYSA-N 0.000 description 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 description 1
- 229960005414 pirbuterol Drugs 0.000 description 1
- 229920002647 polyamide Polymers 0.000 description 1
- 239000004417 polycarbonate Substances 0.000 description 1
- 229920000515 polycarbonate Polymers 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920000098 polyolefin Polymers 0.000 description 1
- 229920001955 polyphenylene ether Polymers 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229960004583 pranlukast Drugs 0.000 description 1
- UAJUXJSXCLUTNU-UHFFFAOYSA-N pranlukast Chemical compound C=1C=C(OCCCCC=2C=CC=CC=2)C=CC=1C(=O)NC(C=1)=CC=C(C(C=2)=O)C=1OC=2C=1N=NNN=1 UAJUXJSXCLUTNU-UHFFFAOYSA-N 0.000 description 1
- 229960005205 prednisolone Drugs 0.000 description 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- 229960004618 prednisone Drugs 0.000 description 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 description 1
- 229960002288 procaterol Drugs 0.000 description 1
- FKNXQNWAXFXVNW-BLLLJJGKSA-N procaterol Chemical compound N1C(=O)C=CC2=C1C(O)=CC=C2[C@@H](O)[C@@H](NC(C)C)CC FKNXQNWAXFXVNW-BLLLJJGKSA-N 0.000 description 1
- 229960003910 promethazine Drugs 0.000 description 1
- SCUZVMOVTVSBLE-UHFFFAOYSA-N prop-2-enenitrile;styrene Chemical compound C=CC#N.C=CC1=CC=CC=C1 SCUZVMOVTVSBLE-UHFFFAOYSA-N 0.000 description 1
- 125000006308 propyl amino group Chemical group 0.000 description 1
- 239000003223 protective agent Substances 0.000 description 1
- 229960001457 rimiterol Drugs 0.000 description 1
- IYMMESGOJVNCKV-SKDRFNHKSA-N rimiterol Chemical compound C([C@@H]1[C@@H](O)C=2C=C(O)C(O)=CC=2)CCCN1 IYMMESGOJVNCKV-SKDRFNHKSA-N 0.000 description 1
- 229960001634 ritodrine Drugs 0.000 description 1
- IOVGROKTTNBUGK-SJCJKPOMSA-N ritodrine Chemical compound N([C@@H](C)[C@H](O)C=1C=CC(O)=CC=1)CCC1=CC=C(O)C=C1 IOVGROKTTNBUGK-SJCJKPOMSA-N 0.000 description 1
- HGEYJZMMUGWEOT-UHFFFAOYSA-N roxindole Chemical compound C12=CC(O)=CC=C2NC=C1CCCCN(CC=1)CCC=1C1=CC=CC=C1 HGEYJZMMUGWEOT-UHFFFAOYSA-N 0.000 description 1
- 239000005060 rubber Substances 0.000 description 1
- 229960002052 salbutamol Drugs 0.000 description 1
- 229950001879 salmefamol Drugs 0.000 description 1
- 239000000779 smoke Substances 0.000 description 1
- 229950010289 soterenol Drugs 0.000 description 1
- 210000003802 sputum Anatomy 0.000 description 1
- 208000024794 sputum Diseases 0.000 description 1
- PWEBUXCTKOWPCW-UHFFFAOYSA-N squaric acid Chemical compound OC1=C(O)C(=O)C1=O PWEBUXCTKOWPCW-UHFFFAOYSA-N 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 229910052712 strontium Inorganic materials 0.000 description 1
- 229920000638 styrene acrylonitrile Polymers 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 229960000195 terbutaline Drugs 0.000 description 1
- 229960004558 terguride Drugs 0.000 description 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000000383 tetramethylene group Chemical group [H]C([H])([*:1])C([H])([H])C([H])([H])C([H])([H])[*:2] 0.000 description 1
- 229960000278 theophylline Drugs 0.000 description 1
- 229950010302 tiaramide Drugs 0.000 description 1
- HTJXMOGUGMSZOG-UHFFFAOYSA-N tiaramide Chemical compound C1CN(CCO)CCN1C(=O)CN1C(=O)SC2=CC=C(Cl)C=C21 HTJXMOGUGMSZOG-UHFFFAOYSA-N 0.000 description 1
- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical class O([C@H]1C[C@@H]2[N+]([C@H](C1)[C@@H]1[C@H]2O1)(C)C)C(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 LERNTVKEWCAPOY-DZZGSBJMSA-N 0.000 description 1
- 229950003899 tofimilast Drugs 0.000 description 1
- OOGJQPCLVADCPB-HXUWFJFHSA-N tolterodine Chemical compound C1([C@@H](CCN(C(C)C)C(C)C)C=2C(=CC=C(C)C=2)O)=CC=CC=C1 OOGJQPCLVADCPB-HXUWFJFHSA-N 0.000 description 1
- 229960004045 tolterodine Drugs 0.000 description 1
- 229960000575 trastuzumab Drugs 0.000 description 1
- 229960005294 triamcinolone Drugs 0.000 description 1
- GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 description 1
- BDIAUFOIMFAIPU-UHFFFAOYSA-N valepotriate Natural products CC(C)CC(=O)OC1C=C(C(=COC2OC(=O)CC(C)C)COC(C)=O)C2C11CO1 BDIAUFOIMFAIPU-UHFFFAOYSA-N 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 238000011179 visual inspection Methods 0.000 description 1
- 239000012991 xanthate Substances 0.000 description 1
- 229960004764 zafirlukast Drugs 0.000 description 1
- XJBCFFLVLOPYBV-UHFFFAOYSA-N zinterol Chemical compound C=1C=C(O)C(NS(C)(=O)=O)=CC=1C(O)CNC(C)(C)CC1=CC=CC=C1 XJBCFFLVLOPYBV-UHFFFAOYSA-N 0.000 description 1
- 229950004209 zinterol Drugs 0.000 description 1
- XJSMBWUHHJFJFV-VTIMJTGVSA-N α-dihydroergocryptine Chemical compound C([C@H]1N(C)C2)C([C]34)=CN=C4C=CC=C3[C@H]1C[C@H]2C(=O)N[C@@]1(C(C)C)C(=O)N2[C@@H](CC(C)C)C(=O)N3CCC[C@H]3[C@]2(O)O1 XJSMBWUHHJFJFV-VTIMJTGVSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/0028—Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/0028—Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up
- A61M15/003—Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up using capsules, e.g. to be perforated or broken-up
- A61M15/0033—Details of the piercing or cutting means
- A61M15/0041—Details of the piercing or cutting means with movable piercing or cutting means
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
- A61M11/001—Particle size control
- A61M11/003—Particle size control by passing the aerosol trough sieves or filters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M2205/00—General characteristics of the apparatus
- A61M2205/27—General characteristics of the apparatus preventing use
- A61M2205/273—General characteristics of the apparatus preventing use preventing reuse, e.g. of disposables
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M2209/00—Ancillary equipment
- A61M2209/06—Packaging for specific medical equipment
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Biomedical Technology (AREA)
- Anesthesiology (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
200808390 九、發明說明： 【發明所屬之技術領域】 、本發明係關於一種用於投予可吸入物質、物質之調配物 或〜物之形式的藥劑之吸入器，其具有一包含偶接至接 口的用於承载物質之内腔之外殼。 【先前技術】 口口 911 047 A1揭不用於自囊吸入粉末狀藥劑之吸入 口口其包含一具有兩個窗口之下部部分及一板 提供囊固持哭及允遙Λ 工^ 口。另外，將一吸入腔室連接至該 ,、’、該腔室上提供_可相對於彈簣而移動的具有兩個尖 ，針聊之㈣。將接口管連接至吸^之上料分且將罩 盘可折疊地連接至下部部分、板及上部部分。 為了有效地吸入藥劑，串去 〜、者須使吸入益之接口舆口腔黏 …、口腔/咽腔）接觸。此證實為存在問題的 人'之口腔黏膜均含有可變大旦沾夂絲^ 為所有 大里的各種細鼬及其他微生物， :广些為致病的。因此，吸入器之接口在使用時受到污 乐。雖然建議患者（及因此吸入哭， · °。 使用者）在使用吸入哭 生:潔接口’但清潔處理因此將視患者之個人習慣、二 .、 +度之徹底性得以執行。此 物必須亦清潔吸入器之外殼的内部(尤其)以移除藥物 【發明内容】 =:因“等殘餘物在其以不規則時間間隔逸出且與適 虽劑同經傳遞之情況下可能導致劑量問題。入 本發明之欲解決問題為提供前文所提之類型之吸入器 H9615.doc 200808390 其對於患者而言易於操作。 根據本發明，藉由使外殼剛性連接至接口而解決該問 題。 由製造者向外殼或外殼之内腔供應精確計量之劑量的藥 - 劑且無需為了將藥物填充之囊插入外殼而以此項技術中已 知的方式將接口自外殼翻開。相反，將接口剛性連接至外 殼以使得吸入器之使用者無法打開外殼以藉由藥物來填充 ^ 内腔。此吸入器具有優勢在於其可由小數目之個別零件而 低廉地製造以用於單次使用且其僅包含絕對必要之組件 (即外殼及接口）。其作為單次使用吸入器之構造亦使得其 較易於操作，因為（尤其是）不存在對於規律清潔之需要且 ， · * 吸入器中之藥物殘餘物無法影響其使用。舉例而言，接口 \ 可採取無人體工學成形之簡單管形式且可夾至外殼。此 外，對於使用者或患者而言無需隨身攜帶吸入器且單獨地 攜帶待吸入之物質。 • 已知商標名稱為 HandiHaler®、Spinhaler⑧、Rotahaler®、 Aerolizer ⑧、Flowcaps®、Turbospin ⑧、AIR DPI®、 Orbital®、Directhaler®及 / 或描述於 DE 33 45 722、EP 0 • 591 136、DE 43 18 455、WO 91/02558、FR-A-2 146 • 202 、 US-A-4 069 819 、 EP 666085 、 EP 869079 、 US 3,991，761、WO 99/45987、WO 2Q0051672、Bell, J. Pharm. Sci. 60? 1559 (1971)； Cox? Brit. Med. J. 2? 634 (1969)中之吸入器。已知單劑量及多劑量粉劑吸入器，尤 其為 Spinhaler®、Rotahaler®、Aerolizer®、Inhalator®、 119615.doc 200808390
HandiHaler®、Diskhaler®、Diskus®、Accuhaler®、 Aerohaler®、Eclipse®、Turbohaler®、Turbuhaler®、 Easyhaler®、Novolizer®、Clickhaler ⑧、Pulvinal®、 Novolizer^、SkyeHaler®、Xcelovair ⑧、Pulvina®、 Taifirn^、MAGhaler®、Twisthaler®及 Jethaler®之單劑量及 多劑量粉劑吸入器。 下文所列之化合物可獨立地或組合地用於根據本發明之 裝置中。在下文所提之化合物中，W為藥理學上之活性物 質且係選自（例如）倍他米美類（betamimetics)、抗膽驗能 劑、皮質類固醇類、PDE4-抑制劑、LTD4-拮抗劑、EGFR 抑制劑、多巴胺（dopamine)促效劑、H1-抗組胺劑、PAF-拮 抗劑及PI3-激酶抑制劑。此外，W之雙重或三重組合可經 組合且用於根據本發明之裝置中。W之組合可為（例如）： -W表示與抗膽鹼能劑、皮質類固醇、PDE4-抑制劑；、 EGFR-抑制劑或LTD4-拮抗劑組合之倍他米美， -W表示與倍他米美、皮質類固醇、PDE4-抑制劑、 EGFR-抑制劑或LTD4-拮抗劑組合之抗膽驗能劑， -W表示與PDE4-抑制劑、EGFR-抑制劑或LTD4-拮抗劑組 合之皮質類固醇 - W表示與EGFR-抑制劑或LTD4-拮抗劑組合之PDE4-抑制劑 -W表示與LTD4-拮抗劑組合之EGFR-抑制劑。 用作倍他米美類之化合物較佳地為選自以下各物之化合 物：舒喘寧（albuterol)、阿福莫特羅（arformoterol)、班布 特羅（bambuterol)、比托特羅（bitolterol)、溴沙特羅 119615.doc 200808390
(broxaterol)、卡布特羅（carbuterol)、克倫特羅 (clenbuterol)、非諾特羅（fenoterol)、福莫特羅 (formoterol)、海索那林（hexoprenaline)、異 丁特羅 (ibuterol)、新呉丙腎上腺素、異丙腎上腺素、左沙丁胺醇 (levosalbutamol) > 馬布特羅（mabuterol)、美盧群 (meluadrine)、二羥苯基異丙氨基乙醇（metaproterenol)、 間經異丙腎上腺素（orciprenaline)、啤布特羅（pirbuterol)、 丙卡特羅（procaterol)、茶丙特羅（reproter〇i)、利米特羅 (rimiterol)、 利托君（ritodrine)、 甲氧苯舒喘寧 (salmefamol)、沙美特羅（salmeter〇1)、索特瑞醇 (soterenol)、磺醯特羅（sulph〇nter〇1)、特布他林 (terbutaline)、嘆拉米特（tiaramide)、托布特羅 (tolubuterol)、淨特羅（zinterol)、CHF-1035、HOKU-81、 KUL-1248 及 -3-(4-{6-[2-羥基-2-(4:羥基-3-羥甲基-苯基乙胺基]_己氧 基}-丁基）-苯甲基·石黃酿胺 -5-[2-(5.6-二乙'基-茚-2-基胺基）-1-羥基_乙基]-8-輕基-111-嘴琳-2-酮 _ 4-羥基1[2_{[M[3_(孓苯基乙氧基）丙基]磺醯基}乙 基]_胺'基}乙基]-2(3H)-苯幷噻唑軻 _ 1-(2-氟基-4-羥苯'基）-2-[4-(1-苯幷咪唑基)甲基·2_ 丁基 胺基]乙醇 -1-[3-(4-甲氡基苄基-胺基>冬羥笨基苯幷咪唑 (基>2-曱基丁基胺基]乙醇 119615.doc 200808390 1 [2H 5-羥基-3-側氧基-4Η-1，4-苯幷噁嗪基]-2_[3-(4- N’N-一曱私基苯基）_2_甲基-2-丙胺基]乙醇 -1-[2Η-5-羥基側氧基“Η·!，心苯幷噁嗪基]_2_[3_(4_ 甲氧苯基）-2-甲基-2-丙胺基]乙醇 -1-[2Η-5-羥基側氧基，‘苯幷噁嗪彳·基卜2_[3_(4_ 正丁氧基苯基甲基-2·丙胺基]乙醇 _ 1-[2Η-5-羥基-3-側氧基 _4Η·ΐ54_苯幷噁嗪_8•基]_2·{4·[3_
(‘甲氧苯基）-1，2,4-三唑-3-基]-2-甲基-2-丁基胺基}乙醇 -5-經基1(1-羥基-2-異丙胺基丁基）_2Η_Μ_苯幷噁 嗪-3-(4Η)-酮 -1-(4-胺基-3-氯-5-三氟甲基苯基）_2_第三τ基胺基）乙醇 • 6-羥基·8·{1_羥基_2_[2_(4_甲氧基苯基^山二甲基-乙 胺基]-乙基}-4Η-苯幷ρ〆]噁嗪_3_綱 6-羥基-8-{1-羥基_2-[2-(4-苯氧基-乙酸乙酯）n-二甲 基-乙胺基]-乙基}-4H-苯幷[M]噁嗪_3_酮 -6-經基-8-{l-經基_2_[2_(4_苯氧基_乙酸）〈，卜二曱基-乙 胺基]-乙基}-4H-笨幷tl，4]噁嗪_3_酮 -8-{2-[1，1-二甲基_2_(2 4 6_三甲基苯基）-乙胺基]小經 基-乙基}-6-經基，-笨幷^]嗔嗪_3_酮 -6-經基-8-{1-經基|[2_(4，基_苯基）_u_二甲基一乙胺 基]乙基}-4H-笨幷[14]噁嘻_3_酮 -6-經基經基-2_[2♦異丙基·苯基基-乙胺 基]-乙基}_4Η-笨幷U，4]噁嗪_3-酮 8-{2-[2-(4-乙基-苯基H山二甲基_乙胺基]小經基-乙 119615.doc 200808390 基}-6-羥基-4H-苯幷[1，4]噁嗪-3-酮 -8-{2-[2-(4-乙氧基-苯基二甲基_乙胺基]—^羥基-乙 基}-6-經基-4H-苯幷[l，4p惡嘻-3-酮 -4-(4-{2-[2-羥基-2-(6-羥基-3-侧氧基-3.4-二氫-2H-苯幷 [1，4]喔嘻冬基）-乙胺基]-2 -甲基-丙基}-苯氧基）_ 丁酸 -8-{2-[2-(3.4-二氟_苯基）-1,1-二甲基-乙胺基]·^羥基-乙 基}-6-羥基-4H-苯幷[1，4]噁療-3-酮 -1-(4-乙氧基-羰基胺基-3-氰基-5-氟苯基）-2-(第三丁基胺 基）乙醇 -2-羥基-5-(1-羥基-2-{2-[4-(2-羥基-2-苯基-乙胺基苯 、， , 基]-乙胺基}-乙基）-苯甲酸 -N-[2-經基-5-(1 “經基-2-{2-[4-(2-經基-2-苯基-乙胺基)一笨 基l·乙胺基}-乙基）-苯基]-甲醯胺 -8-羥基-,5-(1-經基-2-{2-[4-(6-甲氧基-聯二苯-3 -基胺 基）-本基]-乙胺基}-乙基）-1Η -啥4木-2 -酉同 -8-羥基-5-[1-羥基-2-(6-苯乙基胺基-己基胺基）-乙基]-1Η-喹琳-2-酮 -5-[2-(2-{4-[4_(2-胺基甲基-丙氧基）_苯基胺基]-笨 基卜乙胺棊）-1-羥基-乙基]-8-羥基-1H-喹啉-2-酮 -[3-(4-{6-[2-羥基4-(4-羥基-3-羥甲基-苯基）-乙胺基]•己 氧基}-丁基）-5-甲基-苯基]-脲 -4-(2-{6-[2-(2.6-二氯-苯曱氧基）-乙氧基]-己基胺基}-1_ 羥基-乙基）-2-羥曱基-酚 -3-(‘{6-[2-經基-2-(4-羥基-3-羥甲基-苯基）-乙胺基]-己氧 119615.doc •10- 200808390 基丁基）-苄基磺醯胺 ^(3-{7β[2-羥基-2-(4-羥基-3-羥甲基〜苯基）_乙胺基卜庚氧 基卜丙基；l·苄基磺醯胺 4 (2 {6-[4-(3-環戊烷磺醯基_苯基）_ 丁氧基]_己基胺 基卜1-羥基-乙基）-2-羥曱基-酚 - N-金剛烷_2-基_2_(3_{2-[2-羥基_2兴‘羥基羥甲基-苯 基）-乙胺基]-丙基}-苯基）_乙醯胺， 其視情況可為其外消旋體、對映異構物、非對映體之形式 且視情況可為其在藥理學上可接受的酸加成鹽、溶劑合物 或水·合物之形式。根據本發明，倍他米美類之酸加成鹽較 仫k自鹽酸鹽、氫溴酸鹽、氫蛾酸鹽、硫酸氫鹽、填酸氫 鹽、甲烧碍酸氫鹽、硝酸氫鹽、順丁烯二酸氫鹽、醋酸氫 鹽、榉棣酸氫鹽、反丁烯二酸氫鹽、酒石酸氫鹽、草酸氫 鹽、琥珀.酸氫鹽、苯甲酸氫鹽及對曱苯磺酸氫鹽。 所使'用之抗膽鹼能劑較佳為選自以下各物之化合物：噻 托鞍鹽，較佳為溴化鹽、氧托銨鹽，·較佳為溴φ鹽、氟托 叙鹽，’較佳為溴化鹽、異丙托錢鹽，較佳為漠化鹽、格隆 銨，較佳為溴化鹽、曲司銨（tr〇spium) 鹽 較彳·•為氣化鹽、托特羅,定（tolterodine)。在上文所提 之鹽中’陽離子為藥理學上之活性組份。就陰離子而言， 上文所提之鹽較佳地可含有氣化物、溴化物、碘化物、硫 酸根、磷酸根、甲烷磺醵根、硝酸根、順丁烯二酸根、酷 酸根、檸檬酸根、反丁烯二酸根、酒石酸根、草酸根、琥 ί白酸根、苯曱酸根或對曱苯磺酸根，而氯化物、溴化物、 119615.doc -11 - 200808390 /、匕物硫酸根、曱燒項酸根或對甲苯磺酸根較佳作為抗 衡離子。在所有鹽中，氯化物、溴化物、鐵化物及甲烷磺 酉欠根為尤其較佳的。 其他較佳抗膽鹼能劑選自具有式AC-1之鹽
其中X-表示具有單_負電荷之陰離子，較佳為選自以下各 物之陰離子·氟化物、氣化物、溴化物、埃化物、硫酸 根'磷酸根、甲烷磺酸根、硝酸根、順丁烯二酸根、醋酸 根、棒楝酸根、反丁烯二酸根、酒石酸根、草酸根、琥珀 酸根、苯甲酸根及對甲苯磺酸根，較佳為具有單一負電荷 之陰離子，尤其較佳為選自以下各物之陰離子：氟化粉、 氯化物、溴化物、甲烷磺酸根及對曱苯磺酸根，尤其較佳 為溴化物，其視情況可為其外消旋體、對映異構物或水合 物之形式。含有具有式之對映異構物的彼等醫藥 上之組合尤為重要
A C -1 - e n 其中X可具有上文所提之意義。其他較佳抗膽驗能劑選自 119615.doc -12-
X 200808390 具有式AC-2之鹽
AC-2 • 其中反表示甲基或乙基，且其中X—可具有上文所提之意 義。在一替代實施例中，具有式ac_2之化合物亦可以游離 _ 驗AC-2驗之形式存在。
A02鹼 其他指定化合物為： -托品醇（tropenol)2,2-二苯丙酸甲溴化物、 ' 艮宏品驗2,2-二苯丙酸甲溴化物、 -茛菪品鹼2-氟-2,2-二苯乙酸曱溴化物、 -托品醇2_氟_2,2_二苯乙酸甲潭化物； -托品醇3,3，，4,4，-四氟三苯乙醇酸曱溴化物、 -貧菪品鹼3,3，，4,4，-四氟三苯乙醇酸甲溴化物、 -托品醇4,4，-二氟三苯乙醇酸甲溴化物、 -茛菪品鹼4,4，-二氟三苯乙醇酸甲溴化物、 -托今醇3,3，_二氟三苯乙醇酸甲溴化物.、 ' k菪品驗，3，3’-二氟三苯乙醇酸曱溴化物； 119615.doc -13 - 200808390 / / . _托品醇9-羥基_苐_9_羧酸甲溴化物； -托品醇9-氟-第-9-羧酸.甲溴化物； -茛宕品鹼9-羥基-薙-9-羧酸甲溴化物； _ k宕品鹼9-氟-第羧酸甲溴化物； _托品醇％甲基-第冬羧酸甲溴化物； -k宕品鹼9-曱基-苐-9-羧酸甲溴化物；
缞丙基托品鹼（Cyclopr〇pyltr〇pine)三苯乙醇酸 物； 宍化 衣土托品鹼2,2-二苯丙酸甲溴化物； -環丙基牦品鹼9_羥基_二苯幷哌喃·9_羧酸甲演化物. _ ，丙基托品鹼9—T基-苐-9-羧酸甲涘化物； - 環丙基托品驗9·甲其 _ 丄 s 甲土 _一本幷哌喃羧酸甲溴化物； - 環丙基托品驗9 _ _其銥Λ仏^ ^ 匕暴·第-9-羧酸f溴化物； 環丙基托品鹼甲基4 4，_ — 一 ，一齓二本乙醇酸甲溴化物、 -托品醇9 -經基·-贫# κ上 一— 丞—本幷哌喃羧酸甲溴化物； - 良宏品驗9-經基·-贫丑 一本幷哌喃-9-羧酸甲溴化物； -#6品醇9 -甲基·-贫丑 ^ 本幷哌喃·、羧酸_甲溴化物； -艮菪品鹼9-甲基_ -贫私〆 ^ 一本幷哌喃羧酸-甲溴化物； 把口口醇9 -乙基-二！赶 本幷哌喃-9-羧酸〒溴化物； •托品醇9 -二氟甲其一 口 土~—本幷哌喃·9-羧酸甲溴化物； 艮石口口鹼9-羥甲基_ — 一本幷哌喃-9-羧酸甲溴化物， 上文所&之化合物— 、 替代甲漳# ^ "作本發明之範疇内之鹽.，其中 朁代甲溴化物而使用 Τ 之意義。 甲氧其中X可具有前文給予X- 319615.doc -34- 200808390 就皮質類固醇類而言，較佳使用選自以下各物之化合
物：倍氯米松 （beclomethasone)、 倍他米松 (betamethasone)、布地奈德(budesonide)、布替可特 (butixocort)、環索奈德（ciclesonide)、地夫可特 (deflazacort)、地塞米松（dexamethasone)、依替潑諾 (etiprednol)、氟尼縮松（flunisoiide)、氟替卡松 (fluticasone)、氯替潑諾（loteprednol)、莫美他松 (mometasone)、潑尼松龍（prednisolone)、發尼松 (prednisone)、羅氟奈德（rofiep^ide)、曲安西龍 (triamcinolone)、RPR-106541、NS-126、ST-26及 -(S)-氟甲基6,9-二氟-17-[(2-呋喃基羰基）氧基羥 基-16-曱基-3-側氧基-1,4-雄二烯-17-羰基磺酸鹽 -(S)-(2-側氧基-四氫-呋喃-3S-基）6,9-二氟-羥基一曱 基-3-側氧基‘17-丙醯氧基-i_，4-雄二烯羰基磺酸鹽、 -氰基.曱基6α，9α-二氟- ΐ1β'羥基]6心曱基_3_側氧 基-17«-(2,2,3,3-四甲基環-丙基羰基）氧基_Μ_雄二 烯-17β-羧酸鹽， 其視情況可為其外消旋體、對映異構物或非對映體之形式 且視情況可為其鹽及衍生物之形式、其溶劑合物及/或水 合物之形式。㈣類之任何μ包括對可能存在的其任何 鹽或衍生物、其溶劑合物或水合物之引用。崔類之可能的 鹽及衍生物之實例可么· 、』了為·鹼孟屬鹽（諸如鈉鹽或鉀鹽碏 苯甲酸鹽、磷酸鷗、蓉栖缺雜 ^ ^ 皿一、煙馱|、醋酸鹽、二氯醋酸鹽、丙 酸鹽、'—氣鱗酸_、於柄Μ 1 櫚fee鹽、特戊酸鹽或糠酸鹽。 119615.doc -15- 200808390 可使用之PDE4抑制劑較隹為選自以下各物之化合物：3 -丙基黃瞟呤（enprofyllin)、茶鹼、羅說司特（r〇flmnilast)、 ariflo(西洛司特（cilomilast))、托非司特（tofimilast)、普馬 芬丁（pumafentdn)、里拉司特（lirimilast)、阿羅非林 (arofyllin)、阿替唑侖（atiz〇rani)、D-4418、Bay-198004、 BY343 - CP-325.366 - D-4396 (Sch-351591) - AWD-12-281 (GW-842470) > NCS-613 - CDP-840 - D-4418 - PD- 168787、T-440、T-2585、V_11294A、C1-1018、CDC-801、CDC-3052、D-22888、YM-58997、Z-15370及 _ N-(3,5-二氯_1-侧氧基-吡啶基）二氟曱氧基環丙 基甲氧基苄醯胺 -㈠iH(4aR*，106S*)-9-乙氧基胃^义七如^⑽-六氫-^甲氧 基-2-曱基苯幷[s][i，6]啶二異丙基苄醯胺 -化)气+)-1-(4-溴苄基）-4_[(3_環戊氧基兴‘甲氧苯基卜2 ―比 咯啶酮 • 3-(環戊氧基-4-曱氧苯基）氰基-甲基·異 疏腺基]苯甲基）-2-°比洛II定酮 -順[4-氰基-4-(3-環戊氧基_心甲氧苯基）環己烷羧酸] -1甲氧羰基-4-氰基-4-(3-環丙基甲氧基-4-二氟甲氧基笨 基）壤己基-1 -酉同 -順[4-氰基-4-(3-環丙基甲氧基二氟甲氧基苯基）環己 基-1 -醇] -(RM+)-乙基[4-(3-環戊氧基曱氧苯基比咯啶亞基 醋酸鹽 119615.doc 16- 200808390 (s)()乙基[4 (3-環戊氧基_4_甲氧苯基）d比咯啶亞基
醋酸鹽 土 J _ 9-環戊基-5,6_二氫_7-乙基-3-(2-噻吩基）-9//-吡唑幷 [3.4-〇]-1，2,4-三唑[4.3-&]吡啶 • - 9-環戊基_5,6•二氫_7_乙基_3_(廣三丁基吡。坐幷 . [3.4-c]-l，2,4-三唑[4.3-a]吡啶 其視’丨月況可為其外消旋體、對映異構物或非對映體之形式 • '視情況可為其在藥理學上可接受的酸加成鹽之形式、^ 溶劑合物及/或水合物之形式。根據本發明，ρΜ4_抑制劑 之酸加成鹽較佳選自鹽酸鹽、氯演酸鹽、氯块酸鹽、硫= A鹽、磷酸氫鹽、甲糾酸氫鹽、石肖酸氫鹽、順丁稀二酸 .氫鹽、酷酸氫鹽、擰檬酸氫鹽、反丁稀二酸氮鹽、酒石酸 虱鹽、草酸氫鹽、琥珀酸氫鹽、苯甲酸氫鹽及對甲苯磺酸 氫鹽。 所使用之LTD4拮抗劑較佳為選自以下各物之化合物： • 孟魯司特(m〇ntelukast)、普侖司特（pranlukast)、紮魯司特 (zafirlukast) ^ MCC-847 (ZD-3523) ^ MN-Q01 . MEN-91507 (LM-1507)、VUF-5078、VUFU707、L-733321 及 _1-(((11)-(3-(2-(6,7-二氟-2-喹啉基）乙烯基）苯基）_3_(2_(2_ — 羥基―2*·丙基）苯基）硫基）-甲基環丙烷-乙酸、 -1-(((1(尺)-3(3-(2-(2,3-二氯-噻吩幷[3,2讣]吼啶_5_基）_(£> 乙烯基）苯基）-3-(2-(1-羥基-1-曱基乙基）苯基）丙基）硫基） 曱基）環，丙烷-乙酸 -1>[[2-(4-第三丁基-2-噻唑基）-5-苯幷呋喃基]氧甲基]苯 119615.doc -17- 200808390 基]-乙酸
其視情況可為复外、'A 一卜4旋體、對映異構物 且視情況可為其在藥理學冓”對映體之形式 及/或水人铷+ 了接又的I加成鹽、溶劑合物 自鹽酸趨、气、、自 月此專酉夂加成鹽較佳選 夏 虱〉臭酸鹽、氫班酸踏 ^ ^ 甲烷磺酸氫隨、硝… 义虱鹽、磷酸氫鹽、 臨 風鹽、順丁烯二酸氳鹽、醋酸氫鹽、 #棣酸氫鹽、及丁秘—放& 卜 一次氧鹽、酒石酸氫鹽、草廉氫鹽、
號珀酸氫鹽、苯甲醅备a 凰 本甲酉夂風鹽及對甲苯石黃酸氫鹽。LTD4·拮抗 劑視情況可能能夠形成之商 :次何生物思谓（例如）··鹼金屬. 麗（諸如納鹽或鉀鹽）、驗土金屬鹽、續苯甲酸鹽、鱗酸 -異煙酸鹽.、酷酸鹽、丙酸鹽、二氯鱗酸鹽、稼搁酸 鹽、特戊酸鹽或糠酸鹽。 了使：之EGFR·抑制劑較佳為選自以下各物之化合物： 西女昔早抗、曲妥珠單抗、ABX-EGF ' Mab ICR-62及 4-[(3-氯-4-氟苯基）胺基]_6_{[4_(嗎琳_心基）小側氧基_2_ 丁烯-1 -基]-胺基卜孓環丙基甲氧基_喹唑啉 -4-[(3'乳-4-氟苯基）胺基μ6_{[4-(Ν，Ν_二乙胺基卜卜側氧 基-2-丁烯-1_基]_胺基卜'環丙基甲氧基-喹唑啉 4-[(3-氯-4-氟苯基）胺基]-64[‘(]^，1二甲胺基）_卜侧氧 基-2-丁烯-1-基]胺基}_7-環丙基甲氧基_喹唑啉 -4-[(R)-(l -苯基_乙基）胺基μ6-{[4_(嗎啉基卜卜側氣 基-2-丁烯-1-基]胺基}_7_環戊氧基-喹唑啉 -4-[(3-氣-4-氟-苯基）胺基]，6-{[4-((r)冬甲基侧氧 基-嗎啉-4-基）-1-側氧基-2-丁烯基]胺基卜八環丙基曱 119615.doc -18- 200808390 氧基-啥。坐琳 4-[(3-乳-4-氟-苯基）胺基]_6_{[4_((κ)_6_甲基_2侧氧 基-嗎啉_4_基）_卜侧氧基_2_ 丁烯小基丨胺基卜厂[⑻-㈣氫 吱喃-3-基）氧基h喹唑啉 -扣[(3-氯氟-苯基）胺基]·6-{[‘((R)-2_甲氧基甲基·6_側 氧基-馬啉-4-基）_ 〗_側氧基丁烯基]胺基卜'環丙基 曱氧基-啥嗤琳 -4-[(3-氯_4_氟-苯基）胺基]_6_[2_((s)_6·曱基_2_側氧基嗎 琳基）-乙氧基]-7-曱氧基-喹唑| _ 4_[(3-氯-4-氟苯基）胺基]-6-({4_[N-(2-甲氧基-乙基）-N-甲 基-胺基]側氧基-2- 丁烯-1-基}胺基）環丙基甲氧 基-嗟ϋ坐琳 -4_[(3-氯-4-氟苯基）胺基]-6-{[4-(N，N-二曱胺基）-1-側氧 基-2-丁烯-1-基]胺基卜7_環戊氧基_喹唑啉 -4-[(R)-(l-苯基-乙基）胺基]一6-{[4-(Ν，Ν-雙-(2-甲氧基-乙 基）-胺基）-1-側氧基-2-丁烯-1-基]胺基}-7-環丙基甲氧 基-喧唑來 -4-[(R)-(l-苯基-乙基）胺基]乂2-曱氧基-乙基 乙基-胺基]-1-側氧基-2-丁烯-l-基}胺基）-7-環丙基甲氧 基-喧。坐琳 -4-[(R)-(l“苯基-乙基）胺基]-6_({4-[Ν-(2-曱氧基-乙基:)-Ν-甲基-胺基]-1-側氧基-2-丁烯-l-基 }胺基）-7-環丙基曱氧 基-邊嗤琳 -4-[(R)-(l-苯基-乙基）胺基]«{4-[N-(四氫吼喃-4-基)-N- 119615.doc -19· 200808390 甲基-胺基]-1-側氧基-2-丁烯^-基}胺基）_7_環丙基甲氧 基-喧唾琳 -4-[(3_氯冰氟苯基）胺基]_6][4_(N，N_二甲胺基）小側氧 基-2 - 丁烯-1-基]胺基}-7-((R)·四氫呋喃基氧基）_喹 。坐琳 -4·[(3'氯-4-氟苯基）胺基]-6- {[4-(N，N-二甲胺基）小側氧 基-2 - 丁稀-1-基]胺基}-7-((S)-四氫吱喃-3-基氧基）-喹 口坐琳 -4-[(3、氯-4-氟苯基）胺基]-6-({4-[N-(2-甲氧基-乙基）-N-甲 基-胺基;μΐ-側氧基-2-丁烯-l-基}胺基）-7-環戊氧基-喹 嗤琳 -4-[(3_氯-4-氟苯基）胺基]-6-{[4-(N-環丙基-N-曱基-胺 基）-1_側氧基-2-丁烯-1-基]胺基卜7-環戊氧基-喹唑啉 -4·[(3 -氯-4-氟苯基）胺基]-6〜{[4-(N，N-二曱胺基）小侧氧 基1 丁烯-1-基]胺基}-7-[(R)-(四氫呋喃-2-基）曱氧 基]-喹唾琳 -4-[(3·*氯-4-氟苯基）胺基] + {[4-(Ν，Ν-二甲胺基)小侧氧 土 丁細*基]胺基}> 7 - [ (S)-（四氫咬喃-2 -基）曱氧 基卜啥唾琳 -4-[(3-乙炔基-苯基）胺基甲氧基-乙氧基）_啥 。坐琳 _ 4-[(3**氯+氟苯基）胺基]-7-[3-(嗎啉-4-基）-丙氧 基]_6~[(乙烯基羰基）胺基]_喹唑啉 -4-[(R)-(^苯基—乙基）胺基羥基-苯基比咯幷 119615.doc -20- 200808390 [2,3-d]嘧啶 氯基4 [(3氣+氟苯基）胺基]-6-{[4-(N N-二甲胺 基Η-側氧基-2-丁烤小基]胺基卜7_乙氧基_喧啉 {[3氯4 (3氣-节氧基）_苯基]胺基卜6_(5_{[(2_甲烧續 醯基-乙基）胺基]曱基卜呋喃_2·基）喹唑啉 [(R) (1笨基乙基）胺基]_6-{[4_(⑻·6_甲基_2_側氧 基-嗎啉-‘基兴扣側氧基丁烯基]胺基卜甲氧基-喹 °坐琳 -叫3|心氟苯基）胺基]|{[心（嗎琳冰基)小側氧基| 丁稀+基]胺基卜7-[(四氫吱喃_2_基)甲氧基[喧唑啉 -‘[(3H I苯基）胺基]_6_({4_[ν，Νκ2_甲氧基-乙 基）-胺基]-1·•側氧基士丁稀+基}胺基)·7·[(四氫咬喃I 基）曱氧基]-喹唑啉 -心[(3-乙炔基-苯基）胺基]+ {[4-(5 ^二甲基1側氧基喝 啉-4-基）-1_側氧基丁烯基]胺基卜喹唑啉 -4-[(3n氟-苯基）胺基卜6私(2义二甲基^側氡基_嗎 啉基）-乙氧基]—7_甲氧基_喹唑啉 MO备4'氟-苯基）胺基]_6_[2_(2,2二甲基_6_側氧基：嗎 啉+基）-乙氧基]ι[(11Η四氫吱喃|基）甲氧略 唑啉 土 -心旧·氣_4_氟_苯基）胺基]_7_[2_(2,2_二曱基側氧基、嗎 琳-4-基）-乙氧基]_6_[(8)_(四氯咬喃_2_基）甲氧基]-啥唾啉 ΜΑ氯-4-氟_苯基）胺基]_6_{2普(2_側氧基_嗎淋_4 基）-哌啶-1-基]-乙氧基}_7_甲氧基_喹唑啉 119615.doc -21 - 200808390 -4-[(3-氯-4-氟-苯基)胺基]-6〜[κ(第三丁氧羰基）_哌啶―心 基氧基]-7-曱氧基-喹唑琳 -4-[(3-氯-4-氟-苯基）胺基]-6-(反胺基-環己基基氧 基）-7-曱氧基-喹唑啉 ^ _ 4-[(3-氯-4-氟-苯基）胺基]-6、（反曱烷磺醯胺基、環己 基-基氧基）-7-曱氧基-喹唑啉 、 - 4-[(3-氯-4-氟-苯基）胺基]-6-(四氫哌喃基氧基甲氧 基-噎唾琳 -4-[(3-氯-4-氟-苯基）胺基]_6_(1_甲基_哌啶_4_基氧基 曱氧基-喹唑啉 -4-[(3-氯-4-1 _苯基）胺基卜6，{1_ [(嗎淋|基）魏基卜辰 咬-4-基氧基}-7_甲氧基_喹唑啉 _ 4-[(3-氯_4_氟-苯基）胺基]_6_{1_[(甲氧基甲基）駿基卜呢 啶-4-基氧基卜7-甲氧基-喹唑琳 -4-[(3-氯-4-氟_苯基）胺基]_6·(哌啶_3_基氧基）_7_甲氧 基-啥嗤琳 -4-[(3-氯-4-氟-苯基）胺基(入乙醯胺基-乙基）·哌 咬-4-基氧基]_7_曱氧基_喹唑啉 -4-[(3-氯-4-氟-苯基）胺基]-6_(四氫哌喃_4_基氧基>7-乙氧 基-喹唑啉 -心[(3-氯-4‘氟-苯基）胺基}卜（（s)-四氫呋喃-3-基氧基 經基-啥唾琳 -4-[(3-氯-4-氟-苯基)胺基(四氪哌喃-4-基氧基）-7-(2- 曱氧基-乙氧基）_喹唑啉 119615.doc •22- 200808390 -4-[(3-氣-4-氟-苯基）胺基卜6-{反-4-[(二甲胺基）石黃:醯胺 基l·環己基· 1 -基氧基}-7-曱氧基-喹唑啉 -4-[(3-氯-4-氟-苯基）胺基]-6-{反-4_[(嗎啉_4_基）羰基胺 基l·環己基-1-基氧基}-7-曱氧基-喹唑啉 4 [(3 -氯-4-氟-本基）胺基]_6_{反-4-[(嗎嘛-4-基）續醯胺 基]-壤己基-1 -基氧基} -7-甲氧基-喧嗤琳 -4-[(3-氯-4-氟-苯基）胺基]冬（四氫旅喃冰基氧基）-7_(2一 乙酿胺基-乙氧基）-P奎嗤琳 -4-[(3 -氣_4_氟-苯基）胺基]-6-(四氫哌喃_4基氧基）_7_(2_ 曱烧石黃酿胺基-乙氧基)-啥。坐琳 -4-[(3-氣-4-氟-苯基）胺基]-6-{1-[(哌啶-1-基）羰基μ哌 啶-4-基氧基} -7-甲氧基-喹唑啉 -4-[(3-氯-4-氟-苯基）胺基]-6-(1-胺基羰基甲基_哌啶-4•基 氧基）-7-甲氧基-喹唑啉 _ 4>[(3-氣-4-氟_苯基）胺基]-6-(順[(四氫哌喃》4-基） 戴基]-Ν-曱基-胺基卜環己基-1-基氧基）_'曱氧基_啥嗤琳 -4-[(3-氣-4-氟-苯，基）胺基]-6-(順一4-{>^[(嗎啉-4-基）羰 基；1-N-甲基-胺基卜環己基小基氧基）_7·甲氧基_啥唾琳 -‘[(3-氯-4-氟-苯基）胺基]-6-(順-4>{N-[(嗎啉-4-基）磺醯 基]-Ν-甲基-胺基卜環己基-1-基氧基）_7/甲氧基_喧唾琳 -4-[(3-氣-4-氟_苯基）胺基]-6-(反_4_乙烷磺醯胺基_環已 基-1-基氧基）-7-甲氧基-喹唑啉 -4-[(3-氣-4-氟-苯基)胺基]-6-(1-曱.烷磺醯基-哌啶基氧 基）-7-乙氧基-喹唑啉 119615.doc -23- 200808390 -4-[(3-氯-4_氟-苯基）胺基]_6-(1-甲烷磺醯基_哌啶4_基氧 基）-7-(2-甲氧基-乙氧基）_喹唑啉 -4-[(3-氯-‘氟_苯基）胺基]-6 —[H2_甲氧基_乙醯基）_哌 啶-4-基氧基]-7-(2_甲氧基_乙氧基）_喹唑啉 -仁[(3-氯-4-氟-苯基）胺基;μ6_(順乙醯胺基-環己基_卜基 氧基）-7 -甲氧基_啥哇琳 -心阶乙炔基-苯基）胺基]_Μ1_(第三了氧獄基）旅咬冰
基氧基]-7-甲氧基-喹唑啉 -4-[(3-乙块基-苯基）胺基]冬（四氫口底„南_心基氧基卜η氧 基-啥唑琳 4.氯I氟-苯基）胺基]LMN_[(娘咬小基）幾 基]養甲基-胺基環己基_卜基氧基卜7_甲氧基♦坐琳 4-K3-氯-4-氟-苯基）胺基]_6_(順_4_{N俗甲基_㈣小 基m基]專甲基·胺基卜環己基+基氧基）_7_甲氧基啥 嗤琳 ^ 4-[(3-氯-4-氟_苯基）胺基]_6_{順· “ 基]-環己基-1-基氧基}-7-甲氧基_喹唑啉 4-[(3-氯-4-氟-苯基）胺基]-6-{1_[ K U-虱代吡咯啶 乙基哌啶-4-基氧基卜7_甲氧基·喹唑啉 土） 4-[(3-氯_4_氟-苯基）胺基]_6_{ w(嗎琳+ 咬-4-基氧基}·7·(2_甲氧基_乙氧基η唾琳/)厌基]-派 4-[(3-乙*夬基-苯基）胺基]_6_〇_乙酸基_〇辰咬_ 甲氧基-喹唑啉 土乳基）-7- 4-[(3-乙炔基-苯基）胺基]_6-(1-甲 辰疋基氧基）-7—甲 119615.doc -24- 200808390 氧基-啥嗤琳 -4- [(3 -乙快基-本基）胺基]-6-(1-曱烧續酿·基-旅咬-4 -基氧 基）-7-甲氧基-喹唑啉 -4-[(3-氯-4-氟-苯基）胺基]-6-(1-甲基-哌啶-4-基氧 基）-7(2-曱氧基-乙氧基）-喹唑啉 -4“[(3-氯-4-氟-苯基）胺基]-6-(1-異丙氧基羰基、哌啶-4-基 氧基）-7-甲氧基-啥嗤嘛 -4-[(3-氯-4-氣-苯基）胺基]- 6- (順-4 -曱胺基-環己基-1-基氧 基)-7 -甲氧基-啥嗤琳 - 4-[(3 -氯-4-氣-苯基）胺基]-6-{順-4 - [N - (2-曱氧基-乙酿 基）-N-曱基-胺基]-¾己基-1-基氧基} - 7 -曱氧基-啥π坐琳 -4-[(3-乙炔基-苯基）胺基]-6-(哌啶-4-基氧基）-7-甲氧 基-啥。坐琳 -4-[(3-乙快基-苯基）胺基]-6-[1-(2-曱乳基-乙酿基）-略°定_ 4-基氧基]-7-曱氧基-喹唑淋 -4 - [(3 -乙快基-苯基）胺基]-6 - {1 -[(嗎淋-4 -基）談基]-娘 啶-4-基氧基卜7-曱氧基-喹唑啉 -4- [(3 -氯-4 -氣-苯基）胺基]-6-{1-[(順-2,6-二曱基-嗎琳- 4· 基）羰基]-哌啶-4-基氧基}-7-甲氧基-喹唑啉 -4-[(3 -鼠-4-氣-苯基）胺基]-6-{1-[(2-甲基-嗎琳-4-基）幾 基]-哌啶-4-基氧基}-7-曱氧基-喹唑啉 -4-[(3 -氣-4-氟-苯基）胺基]-6-{l-[(S，S)-(2-氧-5-氮-雙環 [2,2，1]庚-5-基）羰基]-哌啶-4-基氧基}-7-甲氧基-喹唑啉 -4-[(3 -氣-4 -氣-苯基）胺基]-6-{1-[(Ν-曱基“N-2-曱氧基乙 119615.doc -25- 200808390 基-胺基）幾基]♦定_4-基氧基}_7_甲氧基+坐琳 4-[(3-氯-4-氟-苯基）胺基]—6_( U乙基-哌啶·4-基氧基 甲氧基-喹唑啉 ) 4-[(3·氯-4-氣-苯基）胺基]-Mw(2_甲氧基乙基)幾基卜派 啶基氧基}-7_甲氧基-喹唑f 4-[(3‘氯-本氟-苯基）胺基]-6‘{1‘『 U ίί3-甲乳基丙基-胺基）-羰 基]-哌啶-4-基氧基卜7-甲氧基-喹唑啉
4-[(3-氯-4_氟-苯基）胺基]_6_[順_4_(ν_甲烷磺醯基况甲 基-胺基）_環己基-1-基氧基]甲氧基_喹唑啉 4-[(3ϋ氟-苯基）胺基]冬[順供乙醯基·队甲基·胺 基）-環己基-1-基氧基]-7-甲氧基_喹唑啉 4-[(3-氯-4-氟-苯基）胺基]_6_(反甲胺基_環己基基氧 基）-7 -甲氧基-啥。坐琳 -M(3-氯-4-氟-苯基）胺基]_6•[反一4供甲烷磺酸基况甲 基-月女基）-環己基]-基氧基]-7-甲氧基_啥唾琳 -4-[(3-氣-4-氟-苯基）胺基；μ6_(反二曱胺基-環己基_^基 氧基）-7-甲氧基-啥。坐琳 •4-[(3-氯-4-氟_苯基）胺基.]_6-(反-4_{：^-[(嗎啉-4-基）羰 基]-Ν-曱基-胺基卜環己基基氧基）_7_甲氧基_喹唑啉 _ 4-[(3-氯-4-氟-苯基）胺基]_6-[2-(2,2-二曱基_6-側氧基·嗎 啉-4-基）-乙氧基]-7_[(8)_(四氫呋喃-2_基）甲氧基]_喹唑啉 -心[(3-氯-4-氟-苯基）胺基]_6_(1_甲烷磺醯基-哌啶基氣 基）-7-甲氧基·《啥。坐琳 -4-[(3-氯-4-氟_苯基）胺基]-6_(1_氰基_痕啶_4_基氧基η、 119615.doc -26- 200808390 曱氧基-喹唑啉 其視情況可為其外消旋體、對映異構物、非對映體之形式 且視情況可為其在藥理學上可接受的酸加成鹽、溶劑 或水合物之形式。根據本發明，此等酸加成鹽較佳選自鹽 酸鹽、氫溴酸鹽、氫碘酸鹽、硫酸氫鹽、磷酸氫鹽、曱烷 磺酸氫鹽、硝酸氫鹽、順丁烯二酸氫鹽、醋酸氫鹽、檸^ 酉欠氫鹽、反丁烯二酸氫鹽、酒石酸氫鹽、草酸氫鹽、琥珀 酸氫鹽、苯甲酸氫鹽及對甲苯磺酸氫鹽。 所使用之多巴胺促效劑較佺為選自以下各物之化合物： 溴麥角環肽（bromocriptin)、卡麥角林（caberg〇line) ' α•二 鼠麥角 争（alpha-dihydroergocryptine)、麥角乙腺 (lisuride)、培* 利特（perg〇Hde)、普拉克索（pramipexoi)、 /口处生多（roxindol)、羅匹尼洛（r〇pinir〇i)、他利克索 (talipexol)、特古利特（tergurid)及維歐贊（vi〇zan)，其視情 況可為其外消旋體、對映異構物、非對映體之形式且視情 況可為其在藥理學上可接受的酸加成鹽、溶劑合物或水合 物之形式。根據本發明，此等酸加成鹽較佳選自鹽駿鹽、 氫溴酸鹽、氫碘酸鹽、硫酸氫鹽、磷酸氫鹽、曱烷磺酸氫 鹽、瑞酸虱鹽、順丁浠二酸氫鹽、醋酸氫鹽、檸檬酸氫 鹽、反丁稀二酸氫鹽、酒石酸氫鹽、草酸氫鹽、號珀酸氫 鹽、苯甲酸氫鹽及對甲苯磺酸氫鹽。 可使用之H1抗組胺劑較佳為選自以下各物之化合物：依 匹斯汀（epinastine)、西替利嗪（cetirizine)、氮拉斯丁 (azelastine)、非索非那定（fexofenadine)、左卡巴斯汀 119615.doc -27- 200808390
(levocabastine)、洛拉他定（loratadine)、哺唆斯灯 (mizolastine)、酮替芬（ketotifen)、依美斯汀 (emedastine)、二甲茚定（dimetindene)、氯馬斯汀 (clemastine)、巴米品（bamipine)、塞克斯氯芬尼拉明 (cexchlorptieiiiramine)、芬尼拉明（pheniramine)、多西拉敏 (doxylamine)、氯齡沙、明（chlorophenoxamine)、茶苯海明 (dimenhydrinate)、苯海拉明（心口11611]1}^<11^11^116)、普魯米近 (promethazine)、依巴斯、;丁（ebastine)、地氯雷他定 (desloratidine)及美克洛唤（meclozine)，其視情況可為其外 消旋體、對映異構物、非對映體之形式且視情況可為其在 藥理學上可接受的酸加成鹽、溶劑合物或水合物之形式。 根據本發明，此等酸加成鹽較佳選自鹽酸鹽、氫溴酸鹽、 氫碘酸鹽、硫酸氫鹽、磷酸氫鹽、甲烷磺酸氫鹽、硝酸氫 鹽、順丁烯二酸氫鹽、醋酸氫鹽、檸檬酸氫鹽、反丁烯二 酸氫鹽、酒石酸氫鹽、草酸氫鹽、琥珀酸氫鹽、苯甲酸氫 鹽及對甲苯磺酸氫鹽。 亦可能使用如EP 1 003 478中所揭示之可吸入巨分子。 另外，該等化合物可來自麥角生物鹼衍生物、曲普坦 (triptans)、CGRP-抑制劑、鱗酸二酯酶-V抑制劑之基團， 其視情況可為其外消旋體、對映異構物、非對映體之形 式，視情況可為其在藥理學上可接受的酸加成鹽、溶劑合 物及/或水合物之形式。 麥角生物鹼衍生物之實例為二氫麥角胺及麥角胺。 對於吸入，合適物質包括含有上文所提之活性物質以及 119615.doc -28- 200808390 其鹽及酯以及此等活性物質、踐 物。 ' | 之組合物的醫藥組合 卓父佳地將外殼不可鬆 膠黏或溶接至接口，則，接至接口。若（例如）將外殼 。。$ 器之使用者無法在不破壞吸入 盗之情況下得到藥物。 外设適宜地包含用於吸入粉末 者經由接口吸氣或吸入時，妹由“入…口… 變得充有藥劑。 、、、由工乳入口進入内部之空氣 根據一特徵，用於分邱 ^ 、刀放粒子之組件與接口相關聯。該組 十士 及入刀佈。便利地將該組件與接口 或内腔之吸入通道形成兔 ”、、1體。可（例如）藉由射出成形而 件連同由塑膠製成之接口或亦由塑膠製成的外殼之 入通道。根據另-特徵，將組件建構為篩網或其類似 物0 塑膠較佳地為聚合物、熱塑性縮聚物、聚加合物、改質 天然物質或橡膠，或者此等塑膠之混合物。 尤其較佳的為聚烯烴、乙烯基氯聚合物、苯乙烯聚合 物、聚縮酸、聚醯胺、熱塑性聚醋及聚㈣，或者此等塑 t之混合物。此等塑膠之實例為聚乙烯、聚氯乙烯、聚甲 "聚鈿醛丙烯腈7丁二蝉/苯乙烯（ABS)、丙烯腈/苯乙 烯丙烯酉夂酉曰（ASA)、聚醯胺、聚碳酸醋、聚對苯二甲酸乙 聚對苯—甲酸丁二酯或聚苯醚。此種類之塑膠可 (例如）購自德國Nufringen之Ensinger公司。 為了省去藥物之額外封裝’其適宜地含於内腔中。根據 119615.doc -29- 200808390 另-實施例，藥劑含於插入内腔中之囊中。 之囊已證明為有價# Μ / ;祆载樂劑 響。為了進一！？ 其提供額外保護以不受環境影 藥劑或含有_之囊。 者向内腔填充 較佳地提供至少一針腳以刺穿囊
At τ ° & 提供兩個斜 腳，-針腳與囊之面對接口的區域相關 相對之區域相關聯。 針腳與 根據又一特徵，將針腳偶接至安裝於吸入器之囊 的啟動元件錢得t該元件受到啟料，針龍推入工囊及/ 或針腳被自囊抽出。若囊僅待在緊於使用吸入器之前打 Γ則在啟㈣使得針㈣穿囊之啟動元件尤其易於操 作。啟動元件可經調適以藉由按壓、拉動或移位而受到摔 作。為了輔助將針腳自囊抽出，啟動元件相對於囊腔室而 受到彈簧負載。 適宜地，在供應時針腳已刺穿吸人器中之囊。若在供應 時針腳已處於吸入器中之囊中，則藉由啟動元件藉由按壓 或拉動之啟動:而將針腳自囊㈣。此程序具有優勢在於， 藉由吸入器之使用者方面的相對較小之力之施加，確保針 腳已在囊中產生具有預定大小之孔且因此用於吸入之藥劑 的傳遞速率得到保證。此外，向囊中突起之針聊將囊緊固 於外殼之内腔中之一預定位置（亦即，囊腔室中）。 針腳較佳地由塑膠製成。由於吸入器僅使用一次且針腳 亦為如此，因此針腳並非絕對必要由不銹鋼製成。當然， 亦有可能使用由金屬（尤其為不銹鋼）製成之已知針腳。熟 119615.doc -30- 200808390 習此項技術者視強加於針腳之要求而將選擇適當材 判定其幾何形狀。 ' 或者，將囊可移除地配置有兩個隔開之開口 1等門口 位於囊腔室中之相應固持器上。因此，安裝可移針腳:非 必要。相反’吸入器之使用者可(例如)藉由吸入器之突然 移動而將囊自形成為（例如）柱之固持器釋放。 …、 為了使吸人器在無使用者方面之任何進—步動作的情況 下準備好使用，較佳以-方式將囊安裝於固持器上，在該 式中展藉由由吸人所造成之氣流而被放開且因此釋放物 質。 為了進行視覺檢驗，囊腔室由透明材料製成。由於囊妒 室不由其他組件環繞，因此使用者可立即觀察到（例如 於其中之所有藥劑是否已被吸入。 為了保護用於吸入之筚遂，丨另成λ抑π， 杲剎及吸入态不受環境影響，吸入 器具備氣密之外部封裝(特定言之為箱容器此種類之外 =裝為f知的。其他或料，可藉由可移除蓋而緊密密 :接口及/或空氣入口。由於此等措施，(例如)以最小之封 、成本而使吸人器之含有藥劑之内腔得到保護不受（詳言 之）將損害藥劑之影響（諸如濕氣）。 " 應瞭解’上文所述之特徵及仍待於後文解釋之特徵可不 ^所指^之料组合而錢，而亦可以其他組合使用。 發明之範疇僅由申請專利範圍界定。 【實施方式】 根據圖1之吸入器本質上由包含一用於容納可吸入藥劑 H9615.doc 200808390 之内腔的外殼i組成，其在一方面包含接 包含空氣入口 3。將用於分散待吸入之藥劑 ：面 配置於吸入通道4中接口 2之末端處。將㈣5 待由兩個可移地安裝於卜 Μ 、樂劑且 提供壓贿 至針腳8之啟動元件1〇上。 牙於連接 猎由裏把者將囊7置放於外殼！
之囊腔m且接著將外殼10定地連接至接 狀況下為管狀)’在此之後不可能移除囊7。 吸入器之使用者將其自其（尤其）保護藥劑不受環境影塑 之氣密封裝移除，且接著作用於啟動元件ig以將兩個針ς 8推入囊7。在釋放啟動元件1〇之後，其在壓縮彈簧9之效 應下返回至其原始位置。使用者將接口2置放於其口中用 於吸入且經由空氣入口3以箭頭u之方向將空氣吸進外殼! 中口此使知囊7振動，因此藥劑經排出且經由接口 2以箭 T 12之：向進入使用者之氣管。在吸入之後，使用者可： 棄吸入器，因為其意欲僅用於單次使用。 根據圖2，針腳8已由製造者推入囊7且因此為了使用吸 入器，須藉由啟動元件10而以箭頭13之方向將針腳8自囊7 抽出，以使囊7中之開口暢通從而允許排出藥劑。因此， 對於患者而言無需刺穿囊7且針腳8之直徑可適應於可吸入 粉末之所需傳遞速率而無需考慮將針腳7推入（例如）由塑膠 製成之囊7所需的力。經推入囊7之針腳7藉由製成囊之材 料的彈性能而密封囊，目此確保粉末狀藥劑無法自囊7漏 119615.doc * 32 - 200808390 出，且該等針腳7將囊7緊固於囊腔室6中。 在根據圖3之吸入器中，斜腳 卞腳8再次已由製造者推入囊 7。將啟動元件1〇安裝於外_ 1 μ 外成1上，使得為了將針腳8自囊7 移除以使囊7中之開口暢通，笮兹士 # γ 顶遇須猎由按壓而以箭頭14之方 向使啟動元件10操作。 【圖式簡單說明】 圖1為根據本發明之吸入器之示意圖，
圖2為根據圖1之吸入器在一替代實施例中之示意圖，及 圖3為根據圖1之吸入器在另一替代實施例中之示意圖。 【主要元件符號說明】 ' 1 外殼 2 接口 3 空氣入口 4 吸入通道 5 篩網 6 囊腔室 7 囊 8 針腳 9 壓縮彈簀 10 啟動元件 11 箭頭 12 箭頭 13 箭頭 14 箭頭 119615.doc -33 -
Claims (1)
- 200808390 十、申請專利範圍： 1 · 一種用於投予可吸入物質、物質之調配物或混合物之形 式的-藥劑之吸入器’其具有包含一用於承載該藥劑之 内腔之外殼（1)，其係偶接至一接口（2)，該吸入器之特 徵在於該外殼（1)係剛性地連接至該接口（2)。 、 2·如請求項！之吸入器，其特徵在於該外殼〇)經不可鬆開 地偶接至該接口（2)。 ^ 3.如請求項！或2之吸入器，其特徵在於該外殼⑴具有—用 於粉末狀藥劑之吸入之空氣入口（3)。 4·如請求項1或2之吸入器，其特徵在於一用於分散粒子之 組件與該接口（2)相結合。 5.如請求項之吸入器，其特徵在於該組件與該接口⑺ 或该内腔之一吸入通道（4)形成為一整體。 士 1求項4之吸入裔，其特徵在於該組件經建構為一篩 網（5)或其類似物。 士明求項1或2之吸入器，其特徵在於該藥劑係承載於該 内腔中。 " 士明求項1或2之吸入器，其特徵在於該藥劑係承載於一 插入於該内腔中之囊（7)中。 月求項1或2之吸入器，其特徵在於該内腔由製造者填 充有該藥劑或該含有該藥劑之囊（7)。 、 士明求項8之吸入器，其特徵在於提供至少一針腳0)以 刺穿該囊（7)。 11·如請族了石 "、1或2之吸入器，其特徵在於該針腳（8)偶接至一 119615.doc 200808390 啟動元件⑽，該啟動元件⑽以其啟動伴隨有 (8)經推入該囊（7)及/或該針腳（8)經拉出該囊Q)之方式而 女裝於該吸入器之一囊腔室（6)上。 而 12. 如請求項此吸人器，其特徵在於該啟動元件⑽ 於该囊腔室（6)係受到彈簧負載。 13. 如請求項!或2之吸入器，其特徵在於在供應 χ BS 你必吸 入裔中，該針腳（8)已被推入該囊（7)。 14·如明求項10之吸人器，其特徵在於該針腳⑻由-塑膠製 成 15. ::求項8之吸入器’其特徵在於該囊⑺經可鬆開地配 有兩個隔開之開口 ’該等開口位於該囊 應承载器上。 ；之相 16. 如請求項14之吸入器，其特徵在於該囊⑺以其藉由—由 吸入所產成之氣流而被放開且釋放該物質之― 固於該等承载器上。 緊 17·如請求項丨〗之入 / 在於该囊腔室（6)由一透明 材枓製成。 1 8·如明求項1或2之吸入器，盆特徼在於Α 八特铽在於其具備氣密之外部 封哀，特定言之為一箔容器。 19·如明求項i或2之吸入 ，、特欲在於该接口（2)及/或該 % 〇 (3)藉由一可移除蓋而經封閉。 2〇· : 求項1或2之吸入器，其特徵在於其係用於單次使 用0 劑 21.如請求項1或2之吸入器，其用於投予-粉末狀藥 I196I5.doc 200808390 2 2 ·如請求項21之吸入裔’其用於投予一含有一選自以下各 物之活性物質.的粉末狀藥劑：抗膽鹼能劑 (anticholinergics)、倍他米美類（betamimetics)、類固醇 類、構酸二酯酶-IV抑制劑、LTD4·拮抗劑、激酶 抑制劑、抗過敏性劑、麥角生物驗衍生物、 u、萌晋坦 (tHpeanes)、CGRP-拮抗劑、磷酸二酯酶- 種類之活性物質的組合。及此等 119615.doc
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE102006016903A DE102006016903A1 (de) | 2006-04-11 | 2006-04-11 | Inhalator |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW200808390A true TW200808390A (en) | 2008-02-16 |
Family
ID=38051941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW096112554A TW200808390A (en) | 2006-04-11 | 2007-04-10 | Inhaler |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US7870856B2 (zh) |
| EP (1) | EP2007458B1 (zh) |
| JP (1) | JP2009533114A (zh) |
| AR (1) | AR060501A1 (zh) |
| CA (1) | CA2648577A1 (zh) |
| CL (1) | CL2007001018A1 (zh) |
| DE (1) | DE102006016903A1 (zh) |
| PE (1) | PE20080354A1 (zh) |
| TW (1) | TW200808390A (zh) |
| UY (1) | UY30265A1 (zh) |
| WO (1) | WO2007116002A1 (zh) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102004012093A1 (de) * | 2004-03-05 | 2005-09-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pulverinhalator mit Merkanaldüse |
| AU2005303596B2 (en) * | 2004-11-10 | 2011-08-18 | Cipla Limited | Inhaler |
| DE102006016903A1 (de) | 2006-04-11 | 2007-10-25 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Inhalator |
| DE102006044752A1 (de) * | 2006-09-20 | 2008-04-10 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Kolbendosierer |
| CA2706018C (en) | 2007-11-30 | 2015-11-24 | Boehringer Ingelheim International Gmbh | 1, 5-dihydro-pyrazolo [3,4-d]pyrimidin-4-one derivatives and their use as pde9a modulators for the treatment of cns disorders |
| CA2709071C (en) | 2007-12-14 | 2016-11-15 | Labogroup S.A.S. | Delivering aerosolizable food products |
| WO2009103336A1 (de) * | 2008-02-20 | 2009-08-27 | Boehringer Ingelheim International Gmbh | Pulverinhalatoren |
| UA105362C2 (en) | 2008-04-02 | 2014-05-12 | Бьорингер Ингельхайм Интернациональ Гмбх | 1-heterocyclyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| NZ590788A (en) | 2008-09-08 | 2012-11-30 | Boehringer Ingelheim Int | Pyrazolopyrimidines and their use for the treatment of cns disorders |
| CA2757231A1 (en) | 2009-03-31 | 2010-10-07 | Boehringer Ingelheim International Gmbh | 1-heterocyclyl-1,5-dihydro-pyrazolo [3,4-d] pyrimidin-4-one derivatives and their use as pde9a modulators |
| AR077859A1 (es) * | 2009-08-12 | 2011-09-28 | Boehringer Ingelheim Int | Compuestos para el tratamiento de trastornos del snc |
| GEP20156217B (en) | 2010-08-12 | 2015-01-12 | Boehringer Ingelheim Int | 6-cycloalkyl-1, 5-dihydro-pyrazolo [3, 4-d] pyrimidin-4-one derivatives and their use as pde9a inhibitors |
| US8809345B2 (en) | 2011-02-15 | 2014-08-19 | Boehringer Ingelheim International Gmbh | 6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders |
| CA2841748C (en) | 2011-07-15 | 2021-06-15 | Nusirt Sciences, Inc. | Compositions and methods for modulating metabolic pathways |
| WO2013016784A1 (en) | 2011-08-04 | 2013-02-07 | Victor Esteve | Dry powder inhaler |
| EP2919772B1 (en) | 2012-11-13 | 2019-03-27 | NuSirt Sciences, Inc. | Pde5 inhibitors and leucine or a leucine metabolite for use in the treatment of diabetes |
| EP2945616B1 (en) | 2013-01-15 | 2018-11-28 | NuSirt Sciences, Inc. | Treating pulmonary conditions |
| KR20150130455A (ko) | 2013-03-15 | 2015-11-23 | 뉴서트 사이언시스, 인크. | 지질 수준을 감소시키는 류신 및 니코틴산 |
| CN105517608B (zh) | 2013-07-16 | 2019-05-31 | 维克托·史蒂夫 | 粉末吸入器 |
| US9272123B2 (en) * | 2013-12-16 | 2016-03-01 | Esther Gallant | Device and method for inserting lubricating capsule |
| AU2015222754B2 (en) | 2014-02-27 | 2020-06-25 | Nusirt Sciences Inc. | Compositions and methods for the reduction or prevention of hepatic steatosis |
| USD752734S1 (en) | 2014-03-10 | 2016-03-29 | Civitas Therapeutics, Inc. | Inhaler grip |
| USD752204S1 (en) | 2014-03-10 | 2016-03-22 | Civitas Therapeutics, Inc. | Indicator for an inhaler |
| USD755367S1 (en) | 2014-03-10 | 2016-05-03 | Civitas Therapeutics, Inc. | Indicator for an inhaler |
| US20160044961A1 (en) * | 2014-08-14 | 2016-02-18 | Tuanfang Liu | Electronic cigarette |
| DE102014017409B4 (de) * | 2014-11-26 | 2016-06-09 | Klaus Dieter Beller | Einzeldosis-Pulverinhalator und Verfahren zu dessen Herstellung |
| CN109922851B (zh) * | 2016-11-30 | 2022-05-27 | 菲利普莫里斯生产公司 | 具有经大小设定的腔的吸入器 |
| US20190076607A1 (en) * | 2017-09-13 | 2019-03-14 | Lupin Atlantis Holdings Sa | Inhaler and mesh for an inhaler |
| WO2019116061A1 (en) | 2017-12-13 | 2019-06-20 | Emphasys Importadora Exportadora E Distribuidora Ltda. | Dry powder inhaler |
| CN108323802A (zh) * | 2018-03-21 | 2018-07-27 | 深圳市凯神科技股份有限公司 | 香烟烟嘴 |
| JP2022554177A (ja) * | 2019-10-25 | 2022-12-28 | フィリップ・モーリス・プロダクツ・ソシエテ・アノニム | 開放遠位端を有する吸入器物品、および吸入器システム |
| JP7733645B2 (ja) * | 2019-10-25 | 2025-09-03 | フィリップ・モーリス・プロダクツ・ソシエテ・アノニム | 接線方向気流端要素を有する吸入器物品 |
| USD983354S1 (en) | 2020-12-21 | 2023-04-11 | Rpc Formatec Gmbh | Inhaler |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT941426B (it) | 1971-07-17 | 1973-03-01 | Isf Spa | Inalatore a camera di turbinio per sostanze medicamentose polveriformi |
| US4069819A (en) | 1973-04-13 | 1978-01-24 | Societa Farmaceutici S.P.A. | Inhalation device |
| GB1479283A (en) * | 1973-07-23 | 1977-07-13 | Bespak Industries Ltd | Inhaler for powdered medicament |
| IT1016489B (it) | 1974-03-18 | 1977-05-30 | Isf Spa | Inalatore |
| GB8314308D0 (en) | 1983-05-24 | 1983-06-29 | Matburn Holdings Ltd | Medical administration devices |
| DE3345722A1 (de) | 1983-12-17 | 1985-06-27 | Boehringer Ingelheim KG, 6507 Ingelheim | Inhalator |
| IT1228460B (it) * | 1989-02-23 | 1991-06-19 | Phidea S R L | Inalatore monouso con capsula pre-forata |
| IT1228459B (it) | 1989-02-23 | 1991-06-19 | Phidea S R L | Inalatore con svuotamento regolare e completo della capsula. |
| DE3927170A1 (de) | 1989-08-17 | 1991-02-21 | Boehringer Ingelheim Kg | Inhalator |
| DE4318455A1 (de) | 1993-06-03 | 1994-12-08 | Boehringer Ingelheim Kg | Kapselhalterung |
| PT101450B (pt) | 1994-02-02 | 1999-11-30 | Hovione Produtos Farmaceuticos | Novo dispositivo para inalacao |
| JP3372105B2 (ja) * | 1994-05-26 | 2003-01-27 | 株式会社日立ユニシアオートモティブ | 吸入式投薬器 |
| JP3388896B2 (ja) * | 1994-08-08 | 2003-03-24 | 株式会社日立ユニシアオートモティブ | 吸入式投薬器 |
| DE69839356T2 (de) * | 1997-01-30 | 2009-06-25 | Dott Ltd. Co., Yokohama | Trockenpulverinhalator für Kapseln |
| PT101988B (pt) | 1997-04-04 | 2004-02-27 | Hovione Farmaciencia Sa | Sistema de orientacao e posicionamento de um objecto |
| DE19733651A1 (de) | 1997-08-04 | 1999-02-18 | Boehringer Ingelheim Pharma | Wässrige Aerosolzubereitungen enthaltend biologisch aktive Markomoleküle und Verfahren zur Erzeugung entsprechender Aerosole |
| JP3488620B2 (ja) * | 1998-02-05 | 2004-01-19 | 株式会社日立ユニシアオートモティブ | 吸入式投薬器 |
| GB9805102D0 (en) | 1998-03-10 | 1998-05-06 | Ciba Geigy Ag | Device |
| PL206121B1 (pl) | 1999-03-03 | 2010-07-30 | Optinose Asoptinose As | Nosowe urządzenie do dostarczania substancji do nosowej części dróg oddechowych pacjenta |
| US20010029947A1 (en) | 1999-12-17 | 2001-10-18 | Steve Paboojian | Receptacles to facilitate the extraction of powders |
| US6443152B1 (en) * | 2001-01-12 | 2002-09-03 | Becton Dickinson And Company | Medicament respiratory delivery device |
| EP1238680B1 (en) * | 2001-03-05 | 2003-12-10 | Ivo Pera | Inhaling device for dispersing powdered medicaments contained in a capsule through the respiratory tract |
| ITMI20020078A1 (it) * | 2002-01-16 | 2003-07-16 | Fabrizio Niccolai | Dispositivo utilizzabile nel tratamento di affezzioni delle vie respiratorie |
| DE10244795A1 (de) | 2002-09-26 | 2004-04-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pulverinhalator |
| DE102004012093A1 (de) | 2004-03-05 | 2005-09-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pulverinhalator mit Merkanaldüse |
| GB0503738D0 (en) * | 2005-02-23 | 2005-03-30 | Optinose As | Powder delivery devices |
| DE102006016903A1 (de) | 2006-04-11 | 2007-10-25 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Inhalator |
| EP1844805A1 (de) | 2006-04-13 | 2007-10-17 | Boehringer Ingelheim Pharma GmbH & Co.KG | Inhalator |
| US20090235929A1 (en) | 2008-03-19 | 2009-09-24 | Marc Egen | Powder inhalers |
-
2006
- 2006-04-11 DE DE102006016903A patent/DE102006016903A1/de not_active Withdrawn
-
2007
- 2007-04-04 CA CA002648577A patent/CA2648577A1/en not_active Abandoned
- 2007-04-04 WO PCT/EP2007/053335 patent/WO2007116002A1/de not_active Ceased
- 2007-04-04 JP JP2009504700A patent/JP2009533114A/ja not_active Abandoned
- 2007-04-04 EP EP07727804.2A patent/EP2007458B1/de active Active
- 2007-04-09 PE PE2007000420A patent/PE20080354A1/es not_active Application Discontinuation
- 2007-04-10 CL CL2007001018A patent/CL2007001018A1/es unknown
- 2007-04-10 UY UY30265A patent/UY30265A1/es not_active Application Discontinuation
- 2007-04-10 US US11/733,399 patent/US7870856B2/en active Active
- 2007-04-10 TW TW096112554A patent/TW200808390A/zh unknown
- 2007-04-11 AR ARP070101528A patent/AR060501A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2007458B1 (de) | 2018-05-02 |
| JP2009533114A (ja) | 2009-09-17 |
| WO2007116002A1 (de) | 2007-10-18 |
| US20070240713A1 (en) | 2007-10-18 |
| CL2007001018A1 (es) | 2008-01-25 |
| EP2007458A1 (de) | 2008-12-31 |
| UY30265A1 (es) | 2007-11-30 |
| US7870856B2 (en) | 2011-01-18 |
| DE102006016903A1 (de) | 2007-10-25 |
| AR060501A1 (es) | 2008-06-25 |
| CA2648577A1 (en) | 2007-10-18 |
| PE20080354A1 (es) | 2008-05-14 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| TW200808390A (en) | Inhaler | |
| AU2008281704B2 (en) | Inhaler | |
| TW200803932A (en) | Atomiser | |
| TW201134508A (en) | Powder inhaler | |
| ES2734501T3 (es) | Boquilla para un inhalador | |
| CA2629358C (en) | Needle for puncturing powder capsules for inhalation | |
| TW200922644A (en) | Powder inhaler | |
| TW200846038A (en) | Dispensing device | |
| TW200906456A (en) | Dispensing device | |
| TW200930420A (en) | Dispensing device (cat) | |
| TW200911311A (en) | Inhaler | |
| TW200815059A (en) | Dosage aerosols for the application of pharmaceutical formulations | |
| TW200902101A (en) | Dispensing device | |
| TW200848099A (en) | Dispensing device | |
| TW200911218A (en) | Packaging material with desiccant | |
| TW200846039A (en) | Dispensing device | |
| TW200902102A (en) | Dispensing device | |
| TW200846041A (en) | Dispensing device | |
| TW200831146A (en) | Powder inhalers | |
| TW200803933A (en) | Package for multiple dose inhalators, having optimised emptying properties | |
| HK1144079B (zh) | 气雾吸入器 | |
| HK1144079A (zh) | 气雾吸入器 |