BG107812A - Комбинация на гамк агонист и инхибитори на алдозна редуктаза - Google Patents

Комбинация на гамк агонист и инхибитори на алдозна редуктаза Download PDF

Info

Publication number: BG107812A
Authority: BG; Bulgaria
Prior art keywords: prodrug; pharmaceutically acceptable; gaba agonist; acceptable salt; pharmaceutical composition
Prior art date: 2000-11-30

Application number

BG107812A

Other languages

Bulgarian (bg)

English (en)

Inventor

Banavara L. Mylari

Original Assignee

Pfizer Products Inc.

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2000-11-30

Filing date

2003-05-13

Publication date

2004-02-27

2003-05-13 Application filed by Pfizer Products Inc. filed Critical Pfizer Products Inc.

2004-02-27 Publication of BG107812A publication Critical patent/BG107812A/bg

Links

239000003477 4 aminobutyric acid receptor stimulating agent Substances 0.000 title claims abstract description 76
239000003288 aldose reductase inhibitor Substances 0.000 title claims description 14
229940090865 aldose reductase inhibitors used in diabetes Drugs 0.000 title description 9
229940002612 prodrug Drugs 0.000 claims abstract description 89
239000000651 prodrug Substances 0.000 claims abstract description 89
150000003839 salts Chemical class 0.000 claims abstract description 61
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 42
208000002249 Diabetes Complications Diseases 0.000 claims abstract description 10
206010012655 Diabetic complications Diseases 0.000 claims abstract description 10
241000124008 Mammalia Species 0.000 claims abstract description 10
206010012601 diabetes mellitus Diseases 0.000 claims abstract description 8
208000032131 Diabetic Neuropathies Diseases 0.000 claims abstract description 6
208000032781 Diabetic cardiomyopathy Diseases 0.000 claims abstract description 6
206010012689 Diabetic retinopathy Diseases 0.000 claims abstract description 6
208000002177 Cataract Diseases 0.000 claims abstract description 4
208000025865 Ulcer Diseases 0.000 claims abstract 2
231100000397 ulcer Toxicity 0.000 claims abstract 2
UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims description 37
150000001875 compounds Chemical class 0.000 claims description 34
AYXYPKUFHZROOJ-ZETCQYMHSA-N pregabalin Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims description 20
229960001233 pregabalin Drugs 0.000 claims description 19
ZJQHPWUVQPJPQT-UHFFFAOYSA-N muscimol Chemical group NCC1=CC(=O)NO1 ZJQHPWUVQPJPQT-UHFFFAOYSA-N 0.000 claims description 18
229960002870 gabapentin Drugs 0.000 claims description 17
CXOFVDLJLONNDW-UHFFFAOYSA-N Phenytoin Chemical compound N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 CXOFVDLJLONNDW-UHFFFAOYSA-N 0.000 claims description 14
-1 zenastat Chemical compound 0.000 claims description 14
PBJUNZJWGZTSKL-MRXNPFEDSA-N tiagabine Chemical compound C1=CSC(C(=CCCN2C[C@@H](CCC2)C(O)=O)C2=C(C=CS2)C)=C1C PBJUNZJWGZTSKL-MRXNPFEDSA-N 0.000 claims description 13
PYZRQGJRPPTADH-UHFFFAOYSA-N lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 claims description 11
229960002036 phenytoin Drugs 0.000 claims description 11
229960001918 tiagabine Drugs 0.000 claims description 10
KPYSYYIEGFHWSV-UHFFFAOYSA-N Baclofen Chemical compound OC(=O)CC(CN)C1=CC=C(Cl)C=C1 KPYSYYIEGFHWSV-UHFFFAOYSA-N 0.000 claims description 9
229960000794 baclofen Drugs 0.000 claims description 9
239000003085 diluting agent Substances 0.000 claims description 9
FTALBRSUTCGOEG-UHFFFAOYSA-N Riluzole Chemical compound C1=C(OC(F)(F)F)C=C2SC(N)=NC2=C1 FTALBRSUTCGOEG-UHFFFAOYSA-N 0.000 claims description 8
KJADKKWYZYXHBB-XBWDGYHZSA-N Topiramic acid Chemical compound C1O[C@@]2(COS(N)(=O)=O)OC(C)(C)O[C@H]2[C@@H]2OC(C)(C)O[C@@H]21 KJADKKWYZYXHBB-XBWDGYHZSA-N 0.000 claims description 8
NIJJYAXOARWZEE-UHFFFAOYSA-N di-n-propyl-acetic acid Natural products CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 claims description 8
229960001848 lamotrigine Drugs 0.000 claims description 8
239000000546 pharmaceutical excipient Substances 0.000 claims description 8
229960004181 riluzole Drugs 0.000 claims description 8
MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 claims description 8
229960000604 valproic acid Drugs 0.000 claims description 8
FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 claims description 7
229960000623 carbamazepine Drugs 0.000 claims description 7
239000003937 drug carrier Substances 0.000 claims description 7
229960004394 topiramate Drugs 0.000 claims description 7
PJDFLNIOAUIZSL-UHFFFAOYSA-N vigabatrin Chemical compound C=CC(N)CCC(O)=O PJDFLNIOAUIZSL-UHFFFAOYSA-N 0.000 claims description 7
229960005318 vigabatrin Drugs 0.000 claims description 6
229940118148 Aldose reductase inhibitor Drugs 0.000 claims description 5
208000007342 Diabetic Nephropathies Diseases 0.000 claims description 5
208000033679 diabetic kidney disease Diseases 0.000 claims description 5
239000003814 drug Substances 0.000 claims description 5
230000000144 pharmacologic effect Effects 0.000 claims description 5
BUYWFAJWTSIACV-UHFFFAOYSA-N 2-[3-oxo-4-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)methyl]-1,4-benzothiazin-2-yl]acetic acid Chemical compound FC1=CC(F)=C2SC(CN3C4=CC=CC=C4SC(C3=O)CC(=O)O)=NC2=C1F BUYWFAJWTSIACV-UHFFFAOYSA-N 0.000 claims description 4
BMHZAHGTGIZZCT-LJQANCHMSA-N (4r)-2-[(4-bromo-2-fluorophenyl)methyl]-6-fluorospiro[isoquinoline-4,3'-pyrrolidine]-1,2',3,5'-tetrone Chemical compound C1([C@]2(C(NC(=O)C2)=O)C2=O)=CC(F)=CC=C1C(=O)N2CC1=CC=C(Br)C=C1F BMHZAHGTGIZZCT-LJQANCHMSA-N 0.000 claims description 3
CHNUOJQWGUIOLD-NFZZJPOKSA-N epalrestat Chemical compound C=1C=CC=CC=1\C=C(/C)\C=C1/SC(=S)N(CC(O)=O)C1=O CHNUOJQWGUIOLD-NFZZJPOKSA-N 0.000 claims description 3
229950010170 epalrestat Drugs 0.000 claims description 3
CHNUOJQWGUIOLD-UHFFFAOYSA-N epalrestate Natural products C=1C=CC=CC=1C=C(C)C=C1SC(=S)N(CC(O)=O)C1=O CHNUOJQWGUIOLD-UHFFFAOYSA-N 0.000 claims description 3
MNQZXJOMYWMBOU-UHFFFAOYSA-N glyceraldehyde Chemical compound OCC(O)C=O MNQZXJOMYWMBOU-UHFFFAOYSA-N 0.000 claims description 3
229950002259 minalrestat Drugs 0.000 claims description 3
BCSVCWVQNOXFGL-UHFFFAOYSA-N 3,4-dihydro-4-oxo-3-((5-trifluoromethyl-2-benzothiazolyl)methyl)-1-phthalazine acetic acid Chemical compound O=C1C2=CC=CC=C2C(CC(=O)O)=NN1CC1=NC2=CC(C(F)(F)F)=CC=C2S1 BCSVCWVQNOXFGL-UHFFFAOYSA-N 0.000 claims description 2
RCKMWOKWVGPNJF-UHFFFAOYSA-N diethylcarbamazine Chemical compound CCN(CC)C(=O)N1CCN(C)CC1 RCKMWOKWVGPNJF-UHFFFAOYSA-N 0.000 claims 4
229960003974 diethylcarbamazine Drugs 0.000 claims 4
238000004519 manufacturing process Methods 0.000 claims 1
229960002752 progabide Drugs 0.000 claims 1
IBALRBWGSVJPAP-HEHNFIMWSA-N progabide Chemical compound C=1C(F)=CC=C(O)C=1C(=N/CCCC(=O)N)/C1=CC=C(Cl)C=C1 IBALRBWGSVJPAP-HEHNFIMWSA-N 0.000 claims 1
229950005346 zopolrestat Drugs 0.000 claims 1
238000000034 method Methods 0.000 abstract description 38
206010054044 Diabetic microangiopathy Diseases 0.000 abstract description 5
201000009101 diabetic angiopathy Diseases 0.000 abstract description 5
108091007065 BIRCs Proteins 0.000 description 31
102100027670 Islet amyloid polypeptide Human genes 0.000 description 31
239000002253 acid Substances 0.000 description 15
BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 14
239000002775 capsule Substances 0.000 description 13
239000003826 tablet Substances 0.000 description 13
229960003692 gamma aminobutyric acid Drugs 0.000 description 12
125000002887 hydroxy group Chemical group [H]O* 0.000 description 11
241000713321 Intracisternal A-particles Species 0.000 description 10
239000000203 mixture Substances 0.000 description 8
239000002552 dosage form Substances 0.000 description 5
239000000243 solution Substances 0.000 description 5
FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 4
FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 4
102000005915 GABA Receptors Human genes 0.000 description 4
108010005551 GABA Receptors Proteins 0.000 description 4
125000003277 amino group Chemical group 0.000 description 4
125000002091 cationic group Chemical group 0.000 description 4
210000003169 central nervous system Anatomy 0.000 description 4
201000010099 disease Diseases 0.000 description 4
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
230000000694 effects Effects 0.000 description 4
239000012458 free base Substances 0.000 description 4
150000002500 ions Chemical class 0.000 description 4
102000005962 receptors Human genes 0.000 description 4
108020003175 receptors Proteins 0.000 description 4
239000000600 sorbitol Substances 0.000 description 4
239000000126 substance Substances 0.000 description 4
KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 4
102000016912 Aldehyde Reductase Human genes 0.000 description 3
108010053754 Aldehyde reductase Proteins 0.000 description 3
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 3
PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
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 3
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
229910019142 PO4 Inorganic materials 0.000 description 3
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
239000004480 active ingredient Substances 0.000 description 3
150000001412 amines Chemical class 0.000 description 3
239000007864 aqueous solution Substances 0.000 description 3
239000000460 chlorine Substances 0.000 description 3
229940064790 dilantin Drugs 0.000 description 3
238000009472 formulation Methods 0.000 description 3
229940084457 gabitril Drugs 0.000 description 3
239000008103 glucose Substances 0.000 description 3
150000004677 hydrates Chemical class 0.000 description 3
230000002401 inhibitory effect Effects 0.000 description 3
230000005764 inhibitory process Effects 0.000 description 3
229940072170 lamictal Drugs 0.000 description 3
229940072228 neurontin Drugs 0.000 description 3
NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 3
239000010452 phosphate Substances 0.000 description 3
229920006254 polymer film Polymers 0.000 description 3
239000011734 sodium Substances 0.000 description 3
229910052708 sodium Inorganic materials 0.000 description 3
LKBFFDOJUKLQNY-UHFFFAOYSA-N 2-[3-[(4-bromo-2-fluorophenyl)methyl]-4-oxo-1-phthalazinyl]acetic acid Chemical compound O=C1C2=CC=CC=C2C(CC(=O)O)=NN1CC1=CC=C(Br)C=C1F LKBFFDOJUKLQNY-UHFFFAOYSA-N 0.000 description 2
108010060511 4-Aminobutyrate Transaminase Proteins 0.000 description 2
102100035923 4-aminobutyrate aminotransferase, mitochondrial Human genes 0.000 description 2
QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 description 2
OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
206010007749 Cataract diabetic Diseases 0.000 description 2
ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 2
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 2
229940122240 IAP agonist Drugs 0.000 description 2
FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 2
GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 description 2
JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 2
WQDUMFSSJAZKTM-UHFFFAOYSA-N Sodium methoxide Chemical compound [Na+].[O-]C WQDUMFSSJAZKTM-UHFFFAOYSA-N 0.000 description 2
229920002472 Starch Polymers 0.000 description 2
QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 2
239000000654 additive Substances 0.000 description 2
230000000996 additive effect Effects 0.000 description 2
239000000556 agonist Substances 0.000 description 2
239000002249 anxiolytic agent Substances 0.000 description 2
230000000949 anxiolytic effect Effects 0.000 description 2
229940005530 anxiolytics Drugs 0.000 description 2
239000002585 base Substances 0.000 description 2
JUHORIMYRDESRB-UHFFFAOYSA-N benzathine Chemical compound C=1C=CC=CC=1CNCCNCC1=CC=CC=C1 JUHORIMYRDESRB-UHFFFAOYSA-N 0.000 description 2
WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 2
230000037396 body weight Effects 0.000 description 2
229910052791 calcium Inorganic materials 0.000 description 2
239000011575 calcium Substances 0.000 description 2
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
150000001732 carboxylic acid derivatives Chemical class 0.000 description 2
210000004027 cell Anatomy 0.000 description 2
OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 description 2
229960001231 choline Drugs 0.000 description 2
238000013270 controlled release Methods 0.000 description 2
239000006184 cosolvent Substances 0.000 description 2
201000007025 diabetic cataract Diseases 0.000 description 2
ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 2
229940043237 diethanolamine Drugs 0.000 description 2
229940079593 drug Drugs 0.000 description 2
FBPFZTCFMRRESA-GUCUJZIJSA-N galactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-GUCUJZIJSA-N 0.000 description 2
238000001727 in vivo Methods 0.000 description 2
239000007788 liquid Substances 0.000 description 2
229910052749 magnesium Inorganic materials 0.000 description 2
239000011777 magnesium Substances 0.000 description 2
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
239000000463 material Substances 0.000 description 2
238000004806 packaging method and process Methods 0.000 description 2
239000006187 pill Substances 0.000 description 2
229960005141 piperazine Drugs 0.000 description 2
239000002244 precipitate Substances 0.000 description 2
238000002360 preparation method Methods 0.000 description 2
239000011343 solid material Substances 0.000 description 2
239000012453 solvate Substances 0.000 description 2
239000002904 solvent Substances 0.000 description 2
239000008107 starch Substances 0.000 description 2
235000019698 starch Nutrition 0.000 description 2
239000011885 synergistic combination Substances 0.000 description 2
238000003419 tautomerization reaction Methods 0.000 description 2
RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 2
230000001225 therapeutic effect Effects 0.000 description 2
JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical class CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 2
SXONDGSPUVNZLO-UHFFFAOYSA-N zenarestat Chemical compound O=C1N(CC(=O)O)C2=CC(Cl)=CC=C2C(=O)N1CC1=CC=C(Br)C=C1F SXONDGSPUVNZLO-UHFFFAOYSA-N 0.000 description 2
OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 description 1
DGCTZGDPGOMMNB-UHFFFAOYSA-N 2-[3-oxo-2,8-di(propan-2-yl)-1,4-benzoxazin-4-yl]acetic acid Chemical compound C1=CC=C2N(CC(O)=O)C(=O)C(C(C)C)OC2=C1C(C)C DGCTZGDPGOMMNB-UHFFFAOYSA-N 0.000 description 1
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
239000004135 Bone phosphate Substances 0.000 description 1
201000006474 Brain Ischemia Diseases 0.000 description 1
BUELMBFSPQNFIS-UHFFFAOYSA-N C=1(C=CC2=CCC=CC12)O Chemical compound C=1(C=CC2=CCC=CC12)O BUELMBFSPQNFIS-UHFFFAOYSA-N 0.000 description 1
206010008120 Cerebral ischaemia Diseases 0.000 description 1
241000283153 Cetacea Species 0.000 description 1
KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
208000008960 Diabetic foot Diseases 0.000 description 1
102000004190 Enzymes Human genes 0.000 description 1
108090000790 Enzymes Proteins 0.000 description 1
PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
208000003790 Foot Ulcer Diseases 0.000 description 1
102000003688 G-Protein-Coupled Receptors Human genes 0.000 description 1
108090000045 G-Protein-Coupled Receptors Proteins 0.000 description 1
102000056764 GABAA-rho receptor Human genes 0.000 description 1
108700010345 GABAA-rho receptor Proteins 0.000 description 1
208000027472 Galactosemias Diseases 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
239000004705 High-molecular-weight polyethylene Substances 0.000 description 1
208000023105 Huntington disease Diseases 0.000 description 1
102000004310 Ion Channels Human genes 0.000 description 1
208000005230 Leg Ulcer Diseases 0.000 description 1
240000007472 Leucaena leucocephala Species 0.000 description 1
235000010643 Leucaena leucocephala Nutrition 0.000 description 1
240000003183 Manihot esculenta Species 0.000 description 1
235000016735 Manihot esculenta subsp esculenta Nutrition 0.000 description 1
CERQOIWHTDAKMF-UHFFFAOYSA-M Methacrylate Chemical compound CC(=C)C([O-])=O CERQOIWHTDAKMF-UHFFFAOYSA-M 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
102000004316 Oxidoreductases Human genes 0.000 description 1
108090000854 Oxidoreductases Proteins 0.000 description 1
208000018737 Parkinson disease Diseases 0.000 description 1
235000019483 Peanut oil Nutrition 0.000 description 1
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
KNAHARQHSZJURB-UHFFFAOYSA-N Propylthiouracile Chemical compound CCCC1=CC(=O)NC(=S)N1 KNAHARQHSZJURB-UHFFFAOYSA-N 0.000 description 1
244000000231 Sesamum indicum Species 0.000 description 1
KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
244000061456 Solanum tuberosum Species 0.000 description 1
235000002595 Solanum tuberosum Nutrition 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
206010043118 Tardive Dyskinesia Diseases 0.000 description 1
238000009825 accumulation Methods 0.000 description 1
150000007513 acids Chemical class 0.000 description 1
230000009471 action Effects 0.000 description 1
150000001323 aldoses Chemical class 0.000 description 1
229910052783 alkali metal Inorganic materials 0.000 description 1
229910052784 alkaline earth metal Inorganic materials 0.000 description 1
230000003281 allosteric effect Effects 0.000 description 1
WQZGKKKJIJFFOK-PHYPRBDBSA-N alpha-D-galactose Chemical compound OC[C@H]1O[C@H](O)[C@H](O)[C@@H](O)[C@H]1O WQZGKKKJIJFFOK-PHYPRBDBSA-N 0.000 description 1
AZDRQVAHHNSJOQ-UHFFFAOYSA-N alumane Chemical class [AlH3] AZDRQVAHHNSJOQ-UHFFFAOYSA-N 0.000 description 1
150000001413 amino acids Chemical class 0.000 description 1
150000003863 ammonium salts Chemical class 0.000 description 1
238000004458 analytical method Methods 0.000 description 1
230000002921 anti-spasmodic effect Effects 0.000 description 1
239000000935 antidepressant agent Substances 0.000 description 1
229940005513 antidepressants Drugs 0.000 description 1
239000000164 antipsychotic agent Substances 0.000 description 1
229940005529 antipsychotics Drugs 0.000 description 1
239000012736 aqueous medium Substances 0.000 description 1
239000007900 aqueous suspension Substances 0.000 description 1
230000001174 ascending effect Effects 0.000 description 1
230000003906 autonomic nervous system functioning Effects 0.000 description 1
230000004888 barrier function Effects 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
230000008238 biochemical pathway Effects 0.000 description 1
230000033228 biological regulation Effects 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
210000004556 brain Anatomy 0.000 description 1
229910000019 calcium carbonate Inorganic materials 0.000 description 1
239000001506 calcium phosphate Substances 0.000 description 1
229910000389 calcium phosphate Inorganic materials 0.000 description 1
235000011010 calcium phosphates Nutrition 0.000 description 1
150000001735 carboxylic acids Chemical class 0.000 description 1
230000015556 catabolic process Effects 0.000 description 1
206010008118 cerebral infarction Diseases 0.000 description 1
229910052801 chlorine Inorganic materials 0.000 description 1
125000001309 chloro group Chemical group Cl* 0.000 description 1
239000000812 cholinergic antagonist Substances 0.000 description 1
239000003086 colorant Substances 0.000 description 1
230000001276 controlling effect Effects 0.000 description 1
210000000695 crystalline len Anatomy 0.000 description 1
230000007812 deficiency Effects 0.000 description 1
238000011161 development Methods 0.000 description 1
HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 description 1
239000007884 disintegrant Substances 0.000 description 1
239000003995 emulsifying agent Substances 0.000 description 1
230000002255 enzymatic effect Effects 0.000 description 1
206010015037 epilepsy Diseases 0.000 description 1
HHFAWKCIHAUFRX-UHFFFAOYSA-N ethoxide Chemical compound CC[O-] HHFAWKCIHAUFRX-UHFFFAOYSA-N 0.000 description 1
SLFUXNFVAANERW-UHFFFAOYSA-N ethyl hexanoate;potassium Chemical compound [K].CCCCCC(=O)OCC SLFUXNFVAANERW-UHFFFAOYSA-N 0.000 description 1
229940012017 ethylenediamine Drugs 0.000 description 1
WAAPEIZFCHNLKK-PELKAZGASA-N fidarestat Chemical compound C([C@@H](OC1=CC=C(F)C=C11)C(=O)N)[C@@]21NC(=O)NC2=O WAAPEIZFCHNLKK-PELKAZGASA-N 0.000 description 1
229950007256 fidarestat Drugs 0.000 description 1
239000000945 filler Substances 0.000 description 1
239000000796 flavoring agent Substances 0.000 description 1
125000001153 fluoro group Chemical group F* 0.000 description 1
125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 description 1
239000011888 foil Substances 0.000 description 1
235000013355 food flavoring agent Nutrition 0.000 description 1
235000003599 food sweetener Nutrition 0.000 description 1
229930182830 galactose Natural products 0.000 description 1
229940065734 gamma-aminobutyrate Drugs 0.000 description 1
239000008273 gelatin Substances 0.000 description 1
229920000159 gelatin Polymers 0.000 description 1
239000007903 gelatin capsule Substances 0.000 description 1
235000019322 gelatine Nutrition 0.000 description 1
235000011852 gelatine desserts Nutrition 0.000 description 1
229910052739 hydrogen Inorganic materials 0.000 description 1
239000001257 hydrogen Substances 0.000 description 1
125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 description 1
150000004806 hydroxypyridines Chemical class 0.000 description 1
239000003112 inhibitor Substances 0.000 description 1
238000007918 intramuscular administration Methods 0.000 description 1
238000007912 intraperitoneal administration Methods 0.000 description 1
238000001990 intravenous administration Methods 0.000 description 1
210000003734 kidney Anatomy 0.000 description 1
239000008101 lactose Substances 0.000 description 1
239000004973 liquid crystal related substance Substances 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
235000019359 magnesium stearate Nutrition 0.000 description 1
229960003194 meglumine Drugs 0.000 description 1
AXLHVTKGDPVANO-UHFFFAOYSA-N methyl 2-amino-3-[(2-methylpropan-2-yl)oxycarbonylamino]propanoate Chemical compound COC(=O)C(N)CNC(=O)OC(C)(C)C AXLHVTKGDPVANO-UHFFFAOYSA-N 0.000 description 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
238000002156 mixing Methods 0.000 description 1
238000012986 modification Methods 0.000 description 1
230000004048 modification Effects 0.000 description 1
230000003562 morphometric effect Effects 0.000 description 1
238000013425 morphometry Methods 0.000 description 1
210000003205 muscle Anatomy 0.000 description 1
239000002636 mycotoxin Substances 0.000 description 1
208000010125 myocardial infarction Diseases 0.000 description 1
GZCNKQPANHRSAJ-UHFFFAOYSA-N n-[3,5-dimethyl-4-(nitromethylsulfonyl)phenyl]-2-(2-methylphenyl)acetamide Chemical compound CC1=CC=CC=C1CC(=O)NC1=CC(C)=C(S(=O)(=O)C[N+]([O-])=O)C(C)=C1 GZCNKQPANHRSAJ-UHFFFAOYSA-N 0.000 description 1
210000005036 nerve Anatomy 0.000 description 1
230000007830 nerve conduction Effects 0.000 description 1
210000000653 nervous system Anatomy 0.000 description 1
210000002569 neuron Anatomy 0.000 description 1
239000002858 neurotransmitter agent Substances 0.000 description 1
238000012856 packing Methods 0.000 description 1
238000007911 parenteral administration Methods 0.000 description 1
239000000312 peanut oil Substances 0.000 description 1
210000000578 peripheral nerve Anatomy 0.000 description 1
230000035790 physiological processes and functions Effects 0.000 description 1
230000010287 polarization Effects 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
229920005862 polyol Polymers 0.000 description 1
150000003077 polyols Chemical class 0.000 description 1
229920001451 polypropylene glycol Polymers 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
229950010884 ponalrestat Drugs 0.000 description 1
229910052700 potassium Inorganic materials 0.000 description 1
239000011591 potassium Substances 0.000 description 1
BDAWXSQJJCIFIK-UHFFFAOYSA-N potassium methoxide Chemical compound [K+].[O-]C BDAWXSQJJCIFIK-UHFFFAOYSA-N 0.000 description 1
239000000843 powder Substances 0.000 description 1
239000002243 precursor Substances 0.000 description 1
238000003825 pressing Methods 0.000 description 1
230000003518 presynaptic effect Effects 0.000 description 1
210000005215 presynaptic neuron Anatomy 0.000 description 1
MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
229960004919 procaine Drugs 0.000 description 1
UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 description 1
230000009467 reduction Effects 0.000 description 1
230000001105 regulatory effect Effects 0.000 description 1
229940125723 sedative agent Drugs 0.000 description 1
239000000932 sedative agent Substances 0.000 description 1
230000035945 sensitivity Effects 0.000 description 1
239000008159 sesame oil Substances 0.000 description 1
235000011803 sesame oil Nutrition 0.000 description 1
150000004760 silicates Chemical class 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
239000001509 sodium citrate Substances 0.000 description 1
NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
229910000104 sodium hydride Inorganic materials 0.000 description 1
239000012312 sodium hydride Substances 0.000 description 1
235000019333 sodium laurylsulphate Nutrition 0.000 description 1
FNXKBSAUKFCXIK-UHFFFAOYSA-M sodium;hydrogen carbonate;8-hydroxy-7-iodoquinoline-5-sulfonic acid Chemical class [Na+].OC([O-])=O.C1=CN=C2C(O)=C(I)C=C(S(O)(=O)=O)C2=C1 FNXKBSAUKFCXIK-UHFFFAOYSA-M 0.000 description 1
239000008247 solid mixture Substances 0.000 description 1
241000894007 species Species 0.000 description 1
ZVGYIXBHESYHCE-UHFFFAOYSA-N spiro[6H-quinoline-5,4'-imidazolidine] Chemical compound N1=CC=CC2=C1C=CCC21NCNC1 ZVGYIXBHESYHCE-UHFFFAOYSA-N 0.000 description 1
238000012289 standard assay Methods 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
238000007920 subcutaneous administration Methods 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
239000000725 suspension Substances 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
210000000225 synapse Anatomy 0.000 description 1
230000005062 synaptic transmission Effects 0.000 description 1
238000003786 synthesis reaction Methods 0.000 description 1
239000007916 tablet composition Substances 0.000 description 1
239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
235000012222 talc Nutrition 0.000 description 1
229940090016 tegretol Drugs 0.000 description 1
229940124597 therapeutic agent Drugs 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
238000004448 titration Methods 0.000 description 1
229960003069 tolrestat Drugs 0.000 description 1
LUBHDINQXIHVLS-UHFFFAOYSA-N tolrestat Chemical compound OC(=O)CN(C)C(=S)C1=CC=CC2=C(C(F)(F)F)C(OC)=CC=C21 LUBHDINQXIHVLS-UHFFFAOYSA-N 0.000 description 1
229940035305 topamax Drugs 0.000 description 1
QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
229960000281 trometamol Drugs 0.000 description 1
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
238000005303 weighing Methods 0.000 description 1
229950006343 zenarestat Drugs 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/12—Ophthalmic agents for cataracts
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Landscapes

Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Chemical & Material Sciences (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Epidemiology (AREA)
General Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Chemical Kinetics & Catalysis (AREA)
Biomedical Technology (AREA)
Cardiology (AREA)
Diabetes (AREA)
Hospice & Palliative Care (AREA)
Heart & Thoracic Surgery (AREA)
Ophthalmology & Optometry (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Emergency Medicine (AREA)
Endocrinology (AREA)
Obesity (AREA)
Psychiatry (AREA)
Hematology (AREA)
Urology & Nephrology (AREA)
Physical Education & Sports Medicine (AREA)
Vascular Medicine (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

BG107812A 2000-11-30 2003-05-13 Комбинация на гамк агонист и инхибитори на алдозна редуктаза BG107812A (bg)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US25044800P	2000-11-30	2000-11-30
PCT/IB2001/002214 WO2002043763A2 (fr)	2000-11-30	2001-11-19	Combinaison de gaba-agonistes et d'inhibiteurs d'aldose-réductase

Publications (1)

Publication Number	Publication Date
BG107812A true BG107812A (bg)	2004-02-27

Family

ID=22947799

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
BG107812A BG107812A (bg)	2000-11-30	2003-05-13	Комбинация на гамк агонист и инхибитори на алдозна редуктаза

Country Status (34)

Country	Link
US (1)	US6720348B2 (fr)
EP (1)	EP1337272A2 (fr)
JP (1)	JP2004514700A (fr)
KR (1)	KR20030059287A (fr)
CN (1)	CN1477976A (fr)
AP (1)	AP2001002359A0 (fr)
AR (1)	AR031432A1 (fr)
AU (1)	AU2002215160A1 (fr)
BG (1)	BG107812A (fr)
BR (1)	BR0115776A (fr)
CA (1)	CA2430309A1 (fr)
CR (1)	CR6962A (fr)
CZ (1)	CZ20031387A3 (fr)
DO (1)	DOP2001000294A (fr)
EA (1)	EA200300433A1 (fr)
EC (1)	ECSP034629A (fr)
EE (1)	EE200300249A (fr)
HR (1)	HRP20030419A2 (fr)
HU (1)	HUP0302555A3 (fr)
IL (1)	IL155710A0 (fr)
IS (1)	IS6787A (fr)
MA (1)	MA26965A1 (fr)
MX (1)	MXPA03004871A (fr)
NO (1)	NO20032387D0 (fr)
OA (1)	OA12413A (fr)
PA (1)	PA8534201A1 (fr)
PE (1)	PE20020598A1 (fr)
PL (1)	PL365378A1 (fr)
SK (1)	SK6092003A3 (fr)
SV (1)	SV2003000752A (fr)
TN (1)	TNSN01170A1 (fr)
UY (1)	UY27044A1 (fr)
WO (1)	WO2002043763A2 (fr)
ZA (1)	ZA200303340B (fr)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
KR100491282B1 (ko)	1996-07-24	2005-05-24	워너-램버트 캄파니 엘엘씨	통증 치료용 이소부틸가바 및 그의 유도체
US6696407B1 (en) *	1997-03-21	2004-02-24	The Regents Of The University Of California	Huntington's disease treatment comprising administering aldose reductase inhibitors to increase striatal CNTF
US20030162754A1 (en) *	2001-12-17	2003-08-28	Tufts University	Use of GABA and GABAB agonists
AU2003243603A1 (en) *	2002-06-13	2003-12-31	Board Of Regents, The University Of Texas System	Methods and compositions involving aldose reductase inhibitors
PT1572173E (pt) *	2002-12-13	2010-05-10	Warner Lambert Co	Ligando alfa-2-delta para tratar sintomas do tracto urinário inferior
US20080318908A1 (en) *	2002-12-17	2008-12-25	Trustees Of Tufts College	Use of gaba and gabab agonists
ES2288641T3 (es) *	2002-12-20	2008-01-16	Dynogen Pharmaceuticals Inc.	Metodo para tratar trastornos indoloros de la vejiga usando moduladores de canales del calcio de la subunidad alfa2-delta.
DE602004003172T2 (de) *	2003-03-21	2007-09-27	Dynogen Pharmaceuticals Inc., Waltham	Verfahren zur behandlung von erkrankungen der unteren harnwege mit antimuskarinika und mit modulatoren der alpha-2-delta untereinheit des kalziumkanals
KR20050036195A (ko) *	2003-10-15	2005-04-20	고재영	신규한 망막병증 치료제 조성물
US20110092566A1 (en) *	2004-11-19	2011-04-21	Srivastava Satish K	Treatment of cancer with aldose reductase inhibitors
EP2314289A1 (fr) *	2005-10-31	2011-04-27	Braincells, Inc.	Modulation de la neurogenese dont la médiation est assurée par récepteur gaba
JP2009533368A (ja)	2006-04-11	2009-09-17	ノバルティスアクチエンゲゼルシャフト	有機化合物
WO2008077597A1 (fr) *	2006-12-22	2008-07-03	Novartis Ag	Dérives de 1-aminométhyl- l- phényl- cyclohexane comme inhibiteurs de ddp-iv
US8273746B2 (en)	2007-03-23	2012-09-25	The Board Of Regents Of The University Of Texas System	Methods involving aldose reductase inhibitors
US20090270490A1 (en) *	2008-04-24	2009-10-29	The Board Of Regents Of The University Of Texas System	Methods involving aldose reductase inhibition
EP2116618A1 (fr)	2008-05-09	2009-11-11	Agency for Science, Technology And Research	Diagnostic et traitement de la maladie de Kawasaki
EP2309858A4 (fr)	2008-07-31	2011-09-14	Dekel Pharmaceuticals Ltd	Compositions et procédés de traitement de troubles inflammatoires
PL2326632T3 (pl) *	2008-09-06	2017-10-31	Bionevia Pharmaceuticals Inc	Nowy kokryształ choliny i epalrestatu
WO2012088525A2 (fr)	2010-12-23	2012-06-28	The Board Of Regents Of The University Of Texas System	Méthodes de traitement de copd
US8652527B1 (en)	2013-03-13	2014-02-18	Upsher-Smith Laboratories, Inc	Extended-release topiramate capsules
US9101545B2 (en)	2013-03-15	2015-08-11	Upsher-Smith Laboratories, Inc.	Extended-release topiramate capsules
CN107847548B (zh) *	2015-05-18	2022-06-14	贝思以色列女会吏医学中心公司	P物质、肥大细胞脱颗粒抑制剂和周围神经病
JP7171611B2 (ja) *	2017-04-21	2022-11-15	スティーブン・ホフマン	網膜症を治療するための組成物及び方法
GB2571696B (en)	2017-10-09	2020-05-27	Compass Pathways Ltd	Large scale method for the preparation of Psilocybin and formulations of Psilocybin so produced
US12459965B2 (en)	2017-10-09	2025-11-04	Compass Pathfinder Limited	Preparation of psilocybin, different polymorphic forms, intermediates, formulations and their use
US12433904B2 (en)	2019-04-17	2025-10-07	Compass Pathfinder Limited	Methods for treating anxiety disorders, headache disorders, and eating disorders with psilocybin
CN116235853B (zh) *	2022-12-28	2025-11-04	中国农业大学	一种植物生长调节剂及其在促进植物生长、提高植物产量和增强植物抗逆性中的应用

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
CH449645A (de)	1963-07-09	1968-01-15	Ciba Geigy	Verfahren zur Herstellung neuer Aminosäuren
CH427803A (de)	1963-12-06	1967-01-15	Geigy Ag J R	Verfahren zur Herstellung eines neuen Isoxazolderivates
DE2460891C2 (de) *	1974-12-21	1982-09-23	Gödecke AG, 1000 Berlin	1-Aminomethyl-1-cycloalkanessigsäuren und deren Ester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel
US3960927A (en)	1975-03-18	1976-06-01	Richardson-Merrell Inc.	Olefinic derivatives of amino acids
FR2319338A1 (fr)	1975-08-01	1977-02-25	Synthelabo	Nouveaux derives de a- phenyl benzylideniques des acides amines, leur preparation et les medicaments qui en contiennent
US4130714A (en)	1977-05-23	1978-12-19	Pfizer Inc.	Hydantoin therapeutic agents
IE47592B1 (en) *	1977-12-29	1984-05-02	Ici Ltd	Enzyme inhibitory phthalazin-4-ylacetic acid derivatives, pharmaceutical compositions thereof,and process for their manufacture
JPS5625169A (en)	1979-06-01	1981-03-10	Wellcome Found	Triazine derivative
JPS5745185A (en)	1980-07-21	1982-03-13	Eisai Co Ltd	Hydantoin derivative and its preparation
JPS5740478A (en) *	1980-08-22	1982-03-06	Ono Pharmaceut Co Ltd	Rhodanine derivative, its preparation and aldose reductase inhibitor containing rhodanine derivative
US4791126A (en)	1980-08-22	1988-12-13	Ono Pharmaceutical Co., Ltd.	Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredients
FR2492258A1 (fr)	1980-10-17	1982-04-23	Pharmindustrie	Nouveau medicament a base d'amino-2 trifluoromethoxy-6 benzothiazole
CA1176269A (fr)	1981-03-02	1984-10-16	Kazimir Sestanj	Derives de n-naphtoylglycine
US4436745A (en)	1982-04-15	1984-03-13	Alcon Laboratories, Inc.	Method of inhibiting aldose reductase activity
US4438272A (en)	1982-04-15	1984-03-20	Alcon Laboratories, Inc.	Spiro-(fluoren-9,4'-imidazolidine)-2',5'-diones
US4513006A (en)	1983-09-26	1985-04-23	Mcneil Lab., Inc.	Anticonvulsant sulfamate derivatives
US5066659A (en)	1984-10-30	1991-11-19	Pfizer Inc.	Spiro-heteroazalones for treatment of diabetic complications
DK288385D0 (da) *	1985-06-26	1985-06-26	Novo Industri As	Aminosyrederivater
GB8524663D0 (en)	1985-10-07	1985-11-13	Fujisawa Pharmaceutical Co	Quinazoline derivatives
US4939140A (en) *	1985-11-07	1990-07-03	Pfizer Inc.	Heterocyclic oxophthalazinyl acetic acids
AU602641B2 (en)	1986-04-17	1990-10-18	Senju Pharmaceutical Co., Ltd.	Thiolactam-N-acetic acid derivatives, their production and use
EP0264586B1 (fr)	1986-08-28	1991-04-03	Sanwa Kagaku Kenkyusho Co., Ltd.	Dérivés de l'hydantoine pour le traîtement de complications du diabète
US4771052A (en) *	1987-02-05	1988-09-13	Hoechst-Roussel Pharmaceuticals, Inc.	Tetrahydropyrido[3',4':4,5]pyrrolo[2,3-c]quinolines and their use as hypotensive agents
GB8801037D0 (en)	1988-01-18	1988-02-17	Plessey Co Ltd	Improvements relating to fuel supply systems
US5252572A (en) *	1988-02-03	1993-10-12	Chinoin Gyogyszer- Es Vegyeszeti Termekek Gyara Rt.	Pyridopyrimidine derivatives, pharmaceutical compositions containing them and process for preparing same
US4996204A (en) *	1989-05-11	1991-02-26	Pfizer Inc.	Pyrido[2,3-d]pyridazinones as aldose reductase inhibitors
US4980357A (en)	1990-03-01	1990-12-25	Pfizer Inc.	Azolidinedione derivatives
US5037831A (en)	1990-05-21	1991-08-06	American Home Products Corporation	Spiro-isoquinoline-pyrrolidines and analogs thereof useful as aldose reductase inhibitors
US5236945A (en) *	1990-06-11	1993-08-17	Pfizer Inc.	1H-indazole-3-acetic acids as aldose reductase inhibitors
GB9016978D0 (en)	1990-08-02	1990-09-19	Ici Plc	Acetamide derivatives
US6197819B1 (en) *	1990-11-27	2001-03-06	Northwestern University	Gamma amino butyric acid analogs and optical isomers
KR950703539A (ko) *	1992-09-28	1995-09-20	알렌 제이. 스피겔	당뇨병 합병증 치료용 치환된 피리미딘(substituted pyrimidines for control or diabetic complications)
FR2774908B1 (fr) *	1998-02-17	2000-06-23	Centre Nat Rech Scient	Utilisation d'inhibiteur de la liberation du glutamate dans le traitement de l'ischemie retinienne
GB0001662D0 (en) *	1999-02-06	2000-03-15	Zeneca Ltd	Pharmaceutical compositions
US6350769B1 (en) *	1999-02-24	2002-02-26	The Regents Of The University Of California	Gaba alpha receptors mediate inhibition of T cell responses
ATE264311T1 (de) *	1999-04-01	2004-04-15	Pfizer Prod Inc	Verbindungen zur behandlung und vorsorge bei diabetes
AU782344C (en) *	1999-04-08	2006-08-17	Ortho-Mcneil Pharmaceutical, Inc.	Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders

2001
- 2001-11-19 CN CNA018195954A patent/CN1477976A/zh active Pending
- 2001-11-19 AU AU2002215160A patent/AU2002215160A1/en not_active Abandoned
- 2001-11-19 EE EEP200300249A patent/EE200300249A/xx unknown
- 2001-11-19 CZ CZ20031387A patent/CZ20031387A3/cs unknown
- 2001-11-19 AP APAP/P/2001/002359A patent/AP2001002359A0/en unknown
- 2001-11-19 EA EA200300433A patent/EA200300433A1/ru unknown
- 2001-11-19 WO PCT/IB2001/002214 patent/WO2002043763A2/fr not_active Ceased
- 2001-11-19 KR KR10-2003-7007221A patent/KR20030059287A/ko not_active Ceased
- 2001-11-19 JP JP2002545733A patent/JP2004514700A/ja not_active Withdrawn
- 2001-11-19 SK SK609-2003A patent/SK6092003A3/sk not_active Application Discontinuation
- 2001-11-19 MX MXPA03004871A patent/MXPA03004871A/es unknown
- 2001-11-19 CA CA002430309A patent/CA2430309A1/fr not_active Abandoned
- 2001-11-19 IL IL15571001A patent/IL155710A0/xx unknown
- 2001-11-19 EP EP01983740A patent/EP1337272A2/fr not_active Withdrawn
- 2001-11-19 PL PL01365378A patent/PL365378A1/xx not_active Application Discontinuation
- 2001-11-19 HU HU0302555A patent/HUP0302555A3/hu unknown
- 2001-11-19 HR HR20030419A patent/HRP20030419A2/hr not_active Application Discontinuation
- 2001-11-19 BR BR0115776-0A patent/BR0115776A/pt not_active IP Right Cessation
- 2001-11-19 OA OA1200300138A patent/OA12413A/en unknown
- 2001-11-26 DO DO2001000294A patent/DOP2001000294A/es unknown
- 2001-11-27 PE PE2001001187A patent/PE20020598A1/es not_active Application Discontinuation
- 2001-11-28 UY UY27044A patent/UY27044A1/es not_active Application Discontinuation
- 2001-11-28 AR ARP010105542A patent/AR031432A1/es not_active Application Discontinuation
- 2001-11-29 TN TNTNSN01170A patent/TNSN01170A1/fr unknown
- 2001-11-29 US US09/997,039 patent/US6720348B2/en not_active Expired - Fee Related
- 2001-11-30 PA PA20018534201A patent/PA8534201A1/es unknown
- 2001-11-30 SV SV2001000752A patent/SV2003000752A/es unknown
2003
- 2003-04-14 IS IS6787A patent/IS6787A/is unknown
- 2003-04-24 CR CR6962A patent/CR6962A/es not_active Application Discontinuation
- 2003-04-30 ZA ZA200303340A patent/ZA200303340B/en unknown
- 2003-05-13 BG BG107812A patent/BG107812A/bg unknown
- 2003-05-20 MA MA27166A patent/MA26965A1/fr unknown
- 2003-05-27 NO NO20032387A patent/NO20032387D0/no not_active Application Discontinuation
- 2003-05-28 EC EC2003004629A patent/ECSP034629A/es unknown

Also Published As

Publication number	Publication date
JP2004514700A (ja)	2004-05-20
HUP0302555A2 (hu)	2003-11-28
HUP0302555A3 (en)	2005-06-28
WO2002043763A3 (fr)	2003-03-13
UY27044A1 (es)	2002-07-31
OA12413A (en)	2004-09-30
US20020077319A1 (en)	2002-06-20
TNSN01170A1 (fr)	2005-11-10
BR0115776A (pt)	2004-01-13
SV2003000752A (es)	2003-01-13
KR20030059287A (ko)	2003-07-07
CZ20031387A3 (cs)	2004-04-14
AP2001002359A0 (en)	2001-12-31
PA8534201A1 (es)	2002-10-24
PL365378A1 (en)	2005-01-10
NO20032387L (no)	2003-05-27
AR031432A1 (es)	2003-09-24
HRP20030419A2 (en)	2004-08-31
US6720348B2 (en)	2004-04-13
ECSP034629A (es)	2003-07-25
ZA200303340B (en)	2004-04-30
CA2430309A1 (fr)	2002-06-06
AU2002215160A1 (en)	2002-06-11
EE200300249A (et)	2003-10-15
CN1477976A (zh)	2004-02-25
EP1337272A2 (fr)	2003-08-27
DOP2001000294A (es)	2002-08-30
WO2002043763A2 (fr)	2002-06-06
CR6962A (es)	2004-02-02
NO20032387D0 (no)	2003-05-27
IL155710A0 (en)	2003-11-23
MXPA03004871A (es)	2003-08-19
EA200300433A1 (ru)	2003-10-30
MA26965A1 (fr)	2004-12-20
IS6787A (is)	2003-04-14
SK6092003A3 (en)	2004-07-07
PE20020598A1 (es)	2002-07-08

Publication	Publication Date	Title
BG107812A (bg)	2004-02-27	Комбинация на гамк агонист и инхибитори на алдозна редуктаза
JP5980840B2 (ja)	2016-08-31	インスリン感受性を増すための組成物および方法
US6413965B1 (en)	2002-07-02	Compositions and treatment for diabetic complications
JP2001163805A (ja)	2001-06-19	糖尿病性合併症治療用のアルドース還元酵素阻害剤と抗高血圧剤の組合せ
AU5030399A (en)	2000-02-01	Agents with an antidepressive effect
CZ20031399A3 (cs)	2004-04-14	Farmaceutický prostředek, kterým je směs agonistů gama-aminomáselné kyseliny a inhibitorů sorbitoldehydrogenázy
US6380200B1 (en)	2002-04-30	Combination of aldose reductase inhibitors and selective serotonin reuptake inhibitors for the treatment of diabetic complications
JP2009539996A (ja)	2009-11-19	腎機能障害を持つ個体における利尿改善方法
JP3010153B2 (ja)	2000-02-14	糖尿病性心筋症の予防または逆転におけるアルドースレダクターゼ阻害
US6426341B1 (en)	2002-07-30	Treatment for diabetic complications
AU2006311574A1 (en)	2007-05-18	Use of cicletanine and other furopyridines for treatment of hypertension
HK1059382A (en)	2004-07-02	Combination of gaba agonists and aldose reductase inhibitors
KR950703958A (ko)	1995-11-17	Hiv 감염증을 치료하기 위한,다른 비뉴클레오사이드 역 전사효소 억제제와 혼합된 bhap 화합물의 용도(use of bhap compounds in combination with other non-nucleoside reverse transcriptase inhibitors for the treatment of hiv infection)
AU598366B2 (en)	1990-06-21	Use of aldose reductase inhibitors to enhance insulin sensitivity in diabetes
MXPA00006504A (en)	2002-07-25	Compositions and treatment for diabetic complications
JPH0344321A (ja)	1991-02-26	抗高血圧症および抗うっ血性心不全用の医薬組成物
HK1233527A1 (en)	2018-02-02	Composition and methods for increasing insulin sensitivity