SK12622002A3 - Farmaceutická kompozícia na báze inhibítorov glykogén fosforylázy - Google Patents

Farmaceutická kompozícia na báze inhibítorov glykogén fosforylázy Download PDF

Info

Publication number: SK12622002A3
Authority: SK; Slovakia
Prior art keywords: alkyl; carbon atoms; composition; cellulose acetate; glycogen phosphorylase
Prior art date: 2000-03-16

Application number

SK1262-2002A

Other languages

English (en)

Slovak (sk)

Inventor

Dennis HOOVER

Ravi Mysore Shanker

Dwayne Thomas Friesen

Douglas Alan Lorenz

James Alan Schriver Nightingale

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.)

2000-03-16

Filing date

2001-03-16

Publication date

2004-02-03

2001-03-16 Application filed by Pfizer Products Inc. filed Critical Pfizer Products Inc.

2004-02-03 Publication of SK12622002A3 publication Critical patent/SK12622002A3/sk

Links

239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 15
102000007390 Glycogen Phosphorylase Human genes 0.000 title claims description 41
108010046163 Glycogen Phosphorylase Proteins 0.000 title claims description 41
239000003112 inhibitor Substances 0.000 title claims description 22
229920000642 polymer Polymers 0.000 claims abstract description 289
239000000203 mixture Substances 0.000 claims abstract description 253
239000006185 dispersion Substances 0.000 claims abstract description 54
ROJNYKZWTOHRNU-UHFFFAOYSA-N 2-chloro-4,5-difluoro-n-[[2-methoxy-5-(methylcarbamoylamino)phenyl]carbamoyl]benzamide Chemical compound CNC(=O)NC1=CC=C(OC)C(NC(=O)NC(=O)C=2C(=CC(F)=C(F)C=2)Cl)=C1 ROJNYKZWTOHRNU-UHFFFAOYSA-N 0.000 claims abstract description 41
239000006069 physical mixture Substances 0.000 claims abstract description 9
-1 1,2-oxazetidin-2-yl Chemical group 0.000 claims description 184
125000004432 carbon atom Chemical group C* 0.000 claims description 183
125000000217 alkyl group Chemical group 0.000 claims description 163
125000001424 substituent group Chemical group 0.000 claims description 72
229910052739 hydrogen Inorganic materials 0.000 claims description 69
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 64
150000001875 compounds Chemical class 0.000 claims description 62
239000001257 hydrogen Substances 0.000 claims description 60
238000000034 method Methods 0.000 claims description 56
229910052799 carbon Inorganic materials 0.000 claims description 55
239000002904 solvent Substances 0.000 claims description 55
229910052736 halogen Inorganic materials 0.000 claims description 53
229920002301 cellulose acetate Polymers 0.000 claims description 52
229910052757 nitrogen Inorganic materials 0.000 claims description 47
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 46
125000003545 alkoxy group Chemical group 0.000 claims description 44
150000002367 halogens Chemical class 0.000 claims description 40
150000002431 hydrogen Chemical class 0.000 claims description 40
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 38
IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 32
229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 30
235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 30
206010012601 diabetes mellitus Diseases 0.000 claims description 29
229940081735 acetylcellulose Drugs 0.000 claims description 28
235000010980 cellulose Nutrition 0.000 claims description 28
229920002678 cellulose Polymers 0.000 claims description 28
239000001913 cellulose Substances 0.000 claims description 28
239000001863 hydroxypropyl cellulose Substances 0.000 claims description 28
235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 28
229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 28
SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 26
125000004093 cyano group Chemical group *C#N 0.000 claims description 25
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 25
239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 24
238000000338 in vitro Methods 0.000 claims description 24
125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 23
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 23
229920000623 Cellulose acetate phthalate Polymers 0.000 claims description 23
229940081734 cellulose acetate phthalate Drugs 0.000 claims description 23
125000005843 halogen group Chemical group 0.000 claims description 22
125000004076 pyridyl group Chemical group 0.000 claims description 22
HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical group CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 claims description 21
GAMPNQJDUFQVQO-UHFFFAOYSA-N acetic acid;phthalic acid Chemical compound CC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O GAMPNQJDUFQVQO-UHFFFAOYSA-N 0.000 claims description 21
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 21
208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 20
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 19
230000002209 hydrophobic effect Effects 0.000 claims description 18
229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 claims description 18
239000007787 solid Substances 0.000 claims description 18
238000001694 spray drying Methods 0.000 claims description 18
125000005591 trimellitate group Chemical group 0.000 claims description 18
FUQOTYRCMBZFOL-UHFFFAOYSA-N 5-chloro-1H-indole-2-carboxylic acid Chemical compound ClC1=CC=C2NC(C(=O)O)=CC2=C1 FUQOTYRCMBZFOL-UHFFFAOYSA-N 0.000 claims description 17
239000000651 prodrug Substances 0.000 claims description 17
229940002612 prodrug Drugs 0.000 claims description 17
150000003839 salts Chemical class 0.000 claims description 17
125000000623 heterocyclic group Chemical group 0.000 claims description 16
229910052760 oxygen Inorganic materials 0.000 claims description 16
QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 15
IYKJEILNJZQJPU-UHFFFAOYSA-N acetic acid;butanedioic acid Chemical compound CC(O)=O.OC(=O)CCC(O)=O IYKJEILNJZQJPU-UHFFFAOYSA-N 0.000 claims description 15
125000003118 aryl group Chemical group 0.000 claims description 15
239000007864 aqueous solution Substances 0.000 claims description 14
229920000609 methyl cellulose Polymers 0.000 claims description 14
235000010981 methylcellulose Nutrition 0.000 claims description 14
239000001923 methylcellulose Substances 0.000 claims description 14
230000008569 process Effects 0.000 claims description 14
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 13
229920001479 Hydroxyethyl methyl cellulose Polymers 0.000 claims description 13
150000001408 amides Chemical class 0.000 claims description 13
150000001721 carbon Chemical group 0.000 claims description 13
229920006218 cellulose propionate Polymers 0.000 claims description 13
238000001727 in vivo Methods 0.000 claims description 13
125000000168 pyrrolyl group Chemical group 0.000 claims description 13
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 12
125000000753 cycloalkyl group Chemical group 0.000 claims description 12
125000001786 isothiazolyl group Chemical group 0.000 claims description 12
125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 12
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 12
125000000714 pyrimidinyl group Chemical group 0.000 claims description 12
KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 12
229910052717 sulfur Inorganic materials 0.000 claims description 12
229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 claims description 11
229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims description 11
125000002883 imidazolyl group Chemical group 0.000 claims description 11
125000003226 pyrazolyl group Chemical group 0.000 claims description 11
SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims description 11
208000002177 Cataract Diseases 0.000 claims description 10
208000031226 Hyperlipidaemia Diseases 0.000 claims description 10
206010020772 Hypertension Diseases 0.000 claims description 10
125000001153 fluoro group Chemical group F* 0.000 claims description 10
125000002541 furyl group Chemical group 0.000 claims description 10
125000005842 heteroatom Chemical group 0.000 claims description 10
125000000842 isoxazolyl group Chemical group 0.000 claims description 10
125000004043 oxo group Chemical group O=* 0.000 claims description 10
125000000335 thiazolyl group Chemical group 0.000 claims description 10
201000001320 Atherosclerosis Diseases 0.000 claims description 9
208000007342 Diabetic Nephropathies Diseases 0.000 claims description 9
208000032131 Diabetic Neuropathies Diseases 0.000 claims description 9
208000035150 Hypercholesterolemia Diseases 0.000 claims description 9
206010022489 Insulin Resistance Diseases 0.000 claims description 9
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 9
125000004429 atom Chemical group 0.000 claims description 9
208000033679 diabetic kidney disease Diseases 0.000 claims description 9
230000002708 enhancing effect Effects 0.000 claims description 9
201000001421 hyperglycemia Diseases 0.000 claims description 9
208000028867 ischemia Diseases 0.000 claims description 9
125000003373 pyrazinyl group Chemical group 0.000 claims description 9
125000002098 pyridazinyl group Chemical group 0.000 claims description 9
125000003363 1,3,5-triazinyl group Chemical group N1=C(N=CN=C1)* 0.000 claims description 8
206010012689 Diabetic retinopathy Diseases 0.000 claims description 8
241001465754 Metazoa Species 0.000 claims description 8
229910052731 fluorine Inorganic materials 0.000 claims description 8
125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 8
125000002757 morpholinyl group Chemical group 0.000 claims description 8
125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
125000004193 piperazinyl group Chemical group 0.000 claims description 8
125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims description 8
239000001856 Ethyl cellulose Substances 0.000 claims description 7
239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 7
229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 7
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 7
239000001768 carboxy methyl cellulose Substances 0.000 claims description 7
235000019325 ethyl cellulose Nutrition 0.000 claims description 7
229920001249 ethyl cellulose Polymers 0.000 claims description 7
125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 7
235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 7
125000002755 pyrazolinyl group Chemical group 0.000 claims description 7
125000006699 (C1-C3) hydroxyalkyl group Chemical group 0.000 claims description 6
125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 6
CGMMPMYKMDITEA-UHFFFAOYSA-N 2-ethylbenzoic acid Chemical compound CCC1=CC=CC=C1C(O)=O CGMMPMYKMDITEA-UHFFFAOYSA-N 0.000 claims description 6
125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims description 6
125000002971 oxazolyl group Chemical group 0.000 claims description 6
UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims description 6
125000003072 pyrazolidinyl group Chemical group 0.000 claims description 6
YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 6
229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 5
206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 5
PLEULVPCZZDBNB-UHFFFAOYSA-N acetic acid;butanedioic acid;phthalic acid Chemical compound CC(O)=O.OC(=O)CCC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O PLEULVPCZZDBNB-UHFFFAOYSA-N 0.000 claims description 5
FMTQGBMMIVVKSN-UHFFFAOYSA-N acetic acid;terephthalic acid Chemical compound CC(O)=O.OC(=O)C1=CC=C(C(O)=O)C=C1 FMTQGBMMIVVKSN-UHFFFAOYSA-N 0.000 claims description 5
239000011203 carbon fibre reinforced carbon Substances 0.000 claims description 5
235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 5
239000008112 carboxymethyl-cellulose Substances 0.000 claims description 5
125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 5
125000001041 indolyl group Chemical group 0.000 claims description 5
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 5
125000000719 pyrrolidinyl group Chemical group 0.000 claims description 5
125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 4
125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 4
VMJNTFXCTXAXTC-UHFFFAOYSA-N 2,2-difluoro-1,3-benzodioxole-5-carbonitrile Chemical group C1=C(C#N)C=C2OC(F)(F)OC2=C1 VMJNTFXCTXAXTC-UHFFFAOYSA-N 0.000 claims description 4
FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims description 4
125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 4
GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims description 4
ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 4
HCUARRIEZVDMPT-UHFFFAOYSA-N Indole-2-carboxylic acid Chemical compound C1=CC=C2NC(C(=O)O)=CC2=C1 HCUARRIEZVDMPT-UHFFFAOYSA-N 0.000 claims description 4
125000005118 N-alkylcarbamoyl group Chemical group 0.000 claims description 4
125000000676 alkoxyimino group Chemical group 0.000 claims description 4
VYGAQHDGEYQIJU-UHFFFAOYSA-N butanedioic acid;phthalic acid Chemical compound OC(=O)CCC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O VYGAQHDGEYQIJU-UHFFFAOYSA-N 0.000 claims description 4
VHEMBTYWURNBQQ-UHFFFAOYSA-N butanoic acid;phthalic acid Chemical compound CCCC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O VHEMBTYWURNBQQ-UHFFFAOYSA-N 0.000 claims description 4
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 4
125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims description 4
125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 4
239000011737 fluorine Substances 0.000 claims description 4
125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims description 4
125000001072 heteroaryl group Chemical group 0.000 claims description 4
125000002768 hydroxyalkyl group Chemical group 0.000 claims description 4
230000002401 inhibitory effect Effects 0.000 claims description 4
230000005764 inhibitory process Effects 0.000 claims description 4
125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 4
125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 4
125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 4
230000002441 reversible effect Effects 0.000 claims description 4
125000003107 substituted aryl group Chemical group 0.000 claims description 4
125000001544 thienyl group Chemical group 0.000 claims description 4
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 3
ZNNQGSGPVUYWOS-UHFFFAOYSA-N 2-(3-hydroxypropoxy)benzoic acid Chemical compound OCCCOC1=CC=CC=C1C(O)=O ZNNQGSGPVUYWOS-UHFFFAOYSA-N 0.000 claims description 3
OEXIDSNKGPWFGB-UHFFFAOYSA-N 2-ethyl-3-(3-hydroxypropyl)benzoic acid Chemical compound CCC1=C(CCCO)C=CC=C1C(O)=O OEXIDSNKGPWFGB-UHFFFAOYSA-N 0.000 claims description 3
RESGCFMULOVHHB-UHFFFAOYSA-N 2-ethylpyridine-3-carboxylic acid Chemical compound CCC1=NC=CC=C1C(O)=O RESGCFMULOVHHB-UHFFFAOYSA-N 0.000 claims description 3
NMGBFVPQUCLJGM-UHFFFAOYSA-N 3-ethylphthalic acid Chemical compound CCC1=CC=CC(C(O)=O)=C1C(O)=O NMGBFVPQUCLJGM-UHFFFAOYSA-N 0.000 claims description 3
125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims description 3
VFFMCGXIWQUAEL-UHFFFAOYSA-N 5-acetyl-1-ethyl-2-oxo-n-[3-(phenylcarbamoyl)phenyl]-3h-indole-3-carboxamide Chemical compound C12=CC(C(C)=O)=CC=C2N(CC)C(=O)C1C(=O)NC(C=1)=CC=CC=1C(=O)NC1=CC=CC=C1 VFFMCGXIWQUAEL-UHFFFAOYSA-N 0.000 claims description 3
VFTOHJFKIJLYKN-UHFFFAOYSA-N 7-nitro-9h-fluoren-2-ol Chemical group [O-][N+](=O)C1=CC=C2C3=CC=C(O)C=C3CC2=C1 VFTOHJFKIJLYKN-UHFFFAOYSA-N 0.000 claims description 3
FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 claims description 3
102000004190 Enzymes Human genes 0.000 claims description 3
108090000790 Enzymes Proteins 0.000 claims description 3
ZNPLZHBZUSCANM-UHFFFAOYSA-N acetic acid;benzene-1,3-dicarboxylic acid Chemical compound CC(O)=O.OC(=O)C1=CC=CC(C(O)=O)=C1 ZNPLZHBZUSCANM-UHFFFAOYSA-N 0.000 claims description 3
125000004183 alkoxy alkyl group Chemical group 0.000 claims description 3
125000004103 aminoalkyl group Chemical group 0.000 claims description 3
125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 3
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 3
229920003064 carboxyethyl cellulose Polymers 0.000 claims description 3
210000001035 gastrointestinal tract Anatomy 0.000 claims description 3
208000031225 myocardial ischemia Diseases 0.000 claims description 3
FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims description 3
125000003386 piperidinyl group Chemical group 0.000 claims description 3
125000005936 piperidyl group Chemical group 0.000 claims description 3
150000003254 radicals Chemical class 0.000 claims description 3
229960004889 salicylic acid Drugs 0.000 claims description 3
208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims description 3
229920002554 vinyl polymer Polymers 0.000 claims description 3
125000006526 (C1-C2) alkyl group Chemical group 0.000 claims description 2
125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 2
AVGBKIPAXGXJQH-SYDPRGILSA-N 2-amino-1-[(3S,4R)-3,4-dihydroxypyrrolidin-1-yl]ethanone Chemical group NCC(=O)N1C[C@H](O)[C@H](O)C1 AVGBKIPAXGXJQH-SYDPRGILSA-N 0.000 claims description 2
125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 2
INTNEELQXPKMNM-UHFFFAOYSA-N 3-ethylpyridine-2-carboxylic acid Chemical compound CCC1=CC=CN=C1C(O)=O INTNEELQXPKMNM-UHFFFAOYSA-N 0.000 claims description 2
125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims description 2
CVICEEPAFUYBJG-UHFFFAOYSA-N 5-chloro-2,2-difluoro-1,3-benzodioxole Chemical group C1=C(Cl)C=C2OC(F)(F)OC2=C1 CVICEEPAFUYBJG-UHFFFAOYSA-N 0.000 claims description 2
101100516572 Caenorhabditis elegans nhr-8 gene Proteins 0.000 claims description 2
208000032781 Diabetic cardiomyopathy Diseases 0.000 claims description 2
PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
LEHOTFFKMJEONL-UHFFFAOYSA-N Uric Acid Chemical compound N1C(=O)NC(=O)C2=C1NC(=O)N2 LEHOTFFKMJEONL-UHFFFAOYSA-N 0.000 claims description 2
125000002252 acyl group Chemical group 0.000 claims description 2
125000003342 alkenyl group Chemical group 0.000 claims description 2
125000005078 alkoxycarbonylalkyl group Chemical group 0.000 claims description 2
XKMRRTOUMJRJIA-UHFFFAOYSA-N ammonia nh3 Chemical compound N.N XKMRRTOUMJRJIA-UHFFFAOYSA-N 0.000 claims description 2
125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims description 2
125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
125000005111 carboxyalkoxy group Chemical group 0.000 claims description 2
125000004181 carboxyalkyl group Chemical group 0.000 claims description 2
150000003950 cyclic amides Chemical group 0.000 claims description 2
125000000000 cycloalkoxy group Chemical group 0.000 claims description 2
125000005112 cycloalkylalkoxy group Chemical group 0.000 claims description 2
229920013819 hydroxyethyl ethylcellulose Polymers 0.000 claims description 2
229960002900 methylcellulose Drugs 0.000 claims description 2
DOTMOQHOJINYBL-UHFFFAOYSA-N molecular nitrogen;molecular oxygen Chemical compound N#N.O=O DOTMOQHOJINYBL-UHFFFAOYSA-N 0.000 claims description 2
125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
125000006413 ring segment Chemical group 0.000 claims description 2
230000004614 tumor growth Effects 0.000 claims description 2
229920006163 vinyl copolymer Polymers 0.000 claims description 2
CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 10
MYTGFBZJLDLWQG-UHFFFAOYSA-N 5-chloro-1h-indole Chemical compound ClC1=CC=C2NC=CC2=C1 MYTGFBZJLDLWQG-UHFFFAOYSA-N 0.000 claims 6
XKGCPLIJAJPIOP-UHFFFAOYSA-N 2-chloro-6H-thieno[2,3-b]pyrrole-5-carboxamide Chemical compound ClC1=CC2=C(NC(=C2)C(=O)N)S1 XKGCPLIJAJPIOP-UHFFFAOYSA-N 0.000 claims 2
CRLYLKAPBMACHE-UHFFFAOYSA-N C(C=1C(C(=O)O)=CC=CC1)(=O)OC.C(C)(=O)O Chemical compound C(C=1C(C(=O)O)=CC=CC1)(=O)OC.C(C)(=O)O CRLYLKAPBMACHE-UHFFFAOYSA-N 0.000 claims 2
125000005988 1,1-dioxo-thiomorpholinyl group Chemical group 0.000 claims 1
125000005987 1-oxo-thiomorpholinyl group Chemical group 0.000 claims 1
JPXQQFCADYJMMN-UHFFFAOYSA-N 5-chloro-n-[2-(1,1-dioxo-1,3-thiazolidin-3-yl)-2-oxoethyl]-1h-indole-2-carboxamide Chemical compound C=1C2=CC(Cl)=CC=C2NC=1C(=O)NCC(=O)N1CCS(=O)(=O)C1 JPXQQFCADYJMMN-UHFFFAOYSA-N 0.000 claims 1
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Classifications

- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/43—Enzymes; Proenzymes; Derivatives thereof
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
- 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
- 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
- A61P3/06—Antihyperlipidemics
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- 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
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- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- 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
- A61P9/12—Antihypertensives

Landscapes

Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Medicinal Chemistry (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Epidemiology (AREA)
Diabetes (AREA)
Heart & Thoracic Surgery (AREA)
Obesity (AREA)
Cardiology (AREA)
Hematology (AREA)
Endocrinology (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Communicable Diseases (AREA)
Oncology (AREA)
Emergency Medicine (AREA)
Gastroenterology & Hepatology (AREA)
Immunology (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Indole Compounds (AREA)

SK1262-2002A 2000-03-16 2001-03-16 Farmaceutická kompozícia na báze inhibítorov glykogén fosforylázy SK12622002A3 (sk)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US18994200P	2000-03-16	2000-03-16
PCT/IB2001/000394 WO2001068055A1 (en)	2000-03-16	2001-03-16	Pharmaceutical compositions of glycogen phosphorylase inhibitors

Publications (1)

Publication Number	Publication Date
SK12622002A3 true SK12622002A3 (sk)	2004-02-03

Family

ID=22699402

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
SK1262-2002A SK12622002A3 (sk)	2000-03-16	2001-03-16	Farmaceutická kompozícia na báze inhibítorov glykogén fosforylázy

Country Status (32)

Country	Link
US (1)	US20010053778A1 (et)
EP (1)	EP1263414A1 (et)
JP (1)	JP2003526654A (et)
KR (1)	KR20020081445A (et)
CN (1)	CN1418089A (et)
AP (1)	AP2002002621A0 (et)
AR (1)	AR027656A1 (et)
AU (1)	AU2001242669A1 (et)
BG (1)	BG107037A (et)
BR (1)	BR0109189A (et)
CA (1)	CA2403241A1 (et)
CO (1)	CO5280087A1 (et)
CZ (1)	CZ20022955A3 (et)
EA (1)	EA200200858A1 (et)
EE (1)	EE200200530A (et)
HU (1)	HUP0204583A2 (et)
IL (1)	IL151320A0 (et)
IS (1)	IS6508A (et)
MA (1)	MA26882A1 (et)
MX (1)	MXPA02009097A (et)
NO (1)	NO20024386L (et)
OA (1)	OA12232A (et)
PA (1)	PA8513601A1 (et)
PE (1)	PE20011184A1 (et)
PL (1)	PL360780A1 (et)
SK (1)	SK12622002A3 (et)
SV (1)	SV2002000343A (et)
TN (1)	TNSN01040A1 (et)
TR (1)	TR200202184T2 (et)
WO (1)	WO2001068055A1 (et)
YU (1)	YU67202A (et)
ZA (1)	ZA200207290B (et)

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TR200201617T2 (tr) *	1999-12-23	2002-10-21	Pfizer Products Inc.	Kuvvetlendirilmiş ilaç konsantrasyonları sağlayan farmasötik kompozisyonlar
CO5271699A1 (es) *	2000-01-24	2003-04-30	Pfizer Prod Inc	Procedimiento para el tratamiento de cardiomiopatia utilizando inhibidores de la glucogeno fosforilasa
WO2002070478A1 (en)	2001-03-06	2002-09-12	Astrazeneca Ab	Indolone derivatives having vascular-damaging activity
CA2450957A1 (en)	2001-06-22	2003-01-03	Pfizer Products Inc.	Pharmaceutical compositions of dispersions of drugs and neutral polymers
JP2004534811A (ja) *	2001-06-22	2004-11-18	ファイザー・プロダクツ・インク	ポリマーと薬剤の集合体を含む医薬組成物
EP1269994A3 (en) *	2001-06-22	2003-02-12	Pfizer Products Inc.	Pharmaceutical compositions comprising drug and concentration-enhancing polymers
WO2003000238A1 (en) *	2001-06-22	2003-01-03	Pfizer Products Inc.	Pharmaceutical compositions of adsorbates of amorphous drug
BR0307344A (pt)	2002-02-01	2004-12-14	Pfizer Prod Inc	Composições farmacêuticas de dispersões amorfas de fármacos e materiais formadores de microfase lipofìlica
EP1469833B1 (en)	2002-02-01	2021-05-19	Bend Research, Inc.	Method for making homogeneous spray-dried solid amorphous drug dispersions utilizing modified spray-drying apparatus
PL371593A1 (en)	2002-02-01	2005-06-27	Pfizer Products Inc.	Method for making homogeneous spray-dried solid amorphous drug dispersions using pressure nozzles
GB0205166D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
GB0205162D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
GB0205165D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
GB0205170D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
GB0205175D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
GB0205176D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
US7405210B2 (en)	2003-05-21	2008-07-29	Osi Pharmaceuticals, Inc.	Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
BRPI0413277A (pt)	2003-08-04	2006-10-10	Pfizer Prod Inc	composições farmacêuticas de adsorvatos de medicamentos amorfos e materiais que formam microfases lipofìlicas
CL2004001884A1 (es)	2003-08-04	2005-06-03	Pfizer Prod Inc	Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros.
US7390503B1 (en)	2003-08-22	2008-06-24	Barr Laboratories, Inc.	Ondansetron orally disintegrating tablets
US8974823B2 (en) *	2003-12-31	2015-03-10	Bend Research, Inc.	Solid compositions of low-solubility drugs and poloxamers
ATE483708T1 (de)	2004-03-08	2010-10-15	Prosidion Ltd	Pyrrolopyridin-2-carbonsäurehydrazide als inhibitoren von glykogenphosphorylase
US20090298745A1 (en) *	2004-12-02	2009-12-03	Gerard Hugh Thomas	Treatment of Diabetes with Glycogen Phosphorylase Inhibitors
DE102005026755A1 (de) *	2005-06-09	2006-12-14	Basf Ag	Herstellung von festen Lösungen schwerlöslicher Wirkstoffe durch Kurzzeitüberhitzung und schnelle Trocknung
EP2888290B1 (en)	2012-08-24	2018-12-26	Dow Global Technologies LLC	Novel esterified cellulose ethers of high molecular weight and homogeneity
HUE057701T2 (hu)	2012-09-11	2022-05-28	Medivation Prostate Therapeutics Llc	Enzalutamid kiszerelési formái
JP6843616B2 (ja)	2013-07-19	2021-03-17	シガ・テクノロジーズ・インコーポレーテッド	アモルファステコビリマット調製
CN103709171B (zh) *	2014-01-20	2015-09-16	武汉大学	具有哒嗪并[3,4-b]吲哚骨架结构的衍生物及其合成方法
JP6796083B2 (ja)	2015-06-09	2020-12-02	カプスゲル・ベルギウム・ナムローゼ・フェンノートシャップＣａｐｓｕｇｅｌＢｅｌｇｉｕｍＮＶ	カプセル中の薬剤の噴霧乾燥ディスパーションからの迅速な溶解を達成するための製剤
CN112442022B (zh) *	2019-09-02	2022-05-20	承德医学院	苯并嗪-4-酮类化合物、其制备方法及医药用途
US11291701B1 (en) *	2021-02-04	2022-04-05	Seed Edibles	Orally disintegrating, sublingual and buccal formulations

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CA2224062C (en) *	1995-06-06	2001-09-04	Pfizer Limited	Substituted n-(indole-2-carbonyl)-glycinamides and derivatives as glycogen phosphorylase inhibitors
DK0832066T3 (da) *	1995-06-06	2001-11-19	Pfizer	Substituerede N-(indol-2-carbonyl)amider og derivater som glycogenphosphorylaseinhibitorer
PT901786E (pt) *	1997-08-11	2007-08-07	Pfizer Prod Inc	Disperções farmacêuticas sólidas com biodisponibilidade melhorada
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2001
- 2001-03-14 AR ARP010101185A patent/AR027656A1/es not_active Application Discontinuation
- 2001-03-14 PE PE2001000246A patent/PE20011184A1/es not_active Application Discontinuation
- 2001-03-14 US US09/805,828 patent/US20010053778A1/en not_active Abandoned
- 2001-03-15 SV SV2001000343A patent/SV2002000343A/es not_active Application Discontinuation
- 2001-03-15 TN TNTNSN01040A patent/TNSN01040A1/fr unknown
- 2001-03-16 CN CN01806619A patent/CN1418089A/zh active Pending
- 2001-03-16 CA CA002403241A patent/CA2403241A1/en not_active Abandoned
- 2001-03-16 AP APAP/P/2002/002621A patent/AP2002002621A0/en unknown
- 2001-03-16 OA OA1200200290A patent/OA12232A/en unknown
- 2001-03-16 PA PA20018513601A patent/PA8513601A1/es unknown
- 2001-03-16 AU AU2001242669A patent/AU2001242669A1/en not_active Abandoned
- 2001-03-16 CZ CZ20022955A patent/CZ20022955A3/cs unknown
- 2001-03-16 MX MXPA02009097A patent/MXPA02009097A/es unknown
- 2001-03-16 TR TR2002/02184T patent/TR200202184T2/xx unknown
- 2001-03-16 IL IL15132001A patent/IL151320A0/xx unknown
- 2001-03-16 PL PL36078001A patent/PL360780A1/xx not_active Application Discontinuation
- 2001-03-16 EP EP01915586A patent/EP1263414A1/en not_active Withdrawn
- 2001-03-16 JP JP2001566619A patent/JP2003526654A/ja active Pending
- 2001-03-16 EA EA200200858A patent/EA200200858A1/ru unknown
- 2001-03-16 BR BR0109189-1A patent/BR0109189A/pt not_active Application Discontinuation
- 2001-03-16 WO PCT/IB2001/000394 patent/WO2001068055A1/en not_active Ceased
- 2001-03-16 KR KR1020027012009A patent/KR20020081445A/ko not_active Ceased
- 2001-03-16 SK SK1262-2002A patent/SK12622002A3/sk unknown
- 2001-03-16 CO CO01021769A patent/CO5280087A1/es not_active Application Discontinuation
- 2001-03-16 HU HU0204583A patent/HUP0204583A2/hu unknown
- 2001-03-16 EE EEP200200530A patent/EE200200530A/et unknown
- 2001-03-16 YU YU67202A patent/YU67202A/sh unknown
2002
- 2002-08-16 IS IS6508A patent/IS6508A/is unknown
- 2002-08-26 BG BG107037A patent/BG107037A/bg unknown
- 2002-09-11 ZA ZA200207290A patent/ZA200207290B/xx unknown
- 2002-09-11 MA MA26810A patent/MA26882A1/fr unknown
- 2002-09-13 NO NO20024386A patent/NO20024386L/no not_active Application Discontinuation

Also Published As

Publication number	Publication date
CO5280087A1 (es)	2003-05-30
CA2403241A1 (en)	2001-09-20
TNSN01040A1 (fr)	2005-11-10
IS6508A (is)	2002-08-16
CZ20022955A3 (cs)	2003-09-17
ZA200207290B (en)	2003-09-11
AU2001242669A1 (en)	2001-09-24
IL151320A0 (en)	2003-04-10
EA200200858A1 (ru)	2003-02-27
MA26882A1 (fr)	2004-12-20
EP1263414A1 (en)	2002-12-11
MXPA02009097A (es)	2003-03-12
PA8513601A1 (es)	2004-08-31
PL360780A1 (en)	2004-09-20
OA12232A (en)	2006-05-10
AR027656A1 (es)	2003-04-09
EE200200530A (et)	2004-04-15
CN1418089A (zh)	2003-05-14
KR20020081445A (ko)	2002-10-26
NO20024386L (no)	2002-11-13
US20010053778A1 (en)	2001-12-20
YU67202A (sh)	2006-01-16
TR200202184T2 (tr)	2003-01-21
SV2002000343A (es)	2002-07-03
WO2001068055A1 (en)	2001-09-20
PE20011184A1 (es)	2001-11-15
NO20024386D0 (no)	2002-09-13
BR0109189A (pt)	2003-05-27
AP2002002621A0 (en)	2002-09-30
HUP0204583A2 (hu)	2003-04-28
BG107037A (bg)	2003-04-30
JP2003526654A (ja)	2003-09-09

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