OA11379A - Combination of an aldose reductase inhibitor and aglycogen phosphrylase inhibitor. - Google Patents

Combination of an aldose reductase inhibitor and aglycogen phosphrylase inhibitor. Download PDF

Info

Publication number: OA11379A
Authority: OA; OAPI
Prior art keywords: amide; chloro; indole; hydroxy; oxo
Prior art date: 1997-11-21

Application number

OA1200000137A

Other languages

English (en)

Inventor

Dennis Jay Hoover

Bernard Hulin

Banavara Lakshman Mylari

Judith Lee Treadway

Original Assignee

Pfizer Prod 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.)

1997-11-21

Filing date

2000-05-12

Publication date

2004-01-28

2000-05-12 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

2004-01-28 Publication of OA11379A publication Critical patent/OA11379A/en

Links

239000003288 aldose reductase inhibitor Substances 0.000 title claims abstract description 45
239000003112 inhibitor Substances 0.000 title claims abstract description 19
229940118148 Aldose reductase inhibitor Drugs 0.000 title claims description 34
MNQZXJOMYWMBOU-UHFFFAOYSA-N glyceraldehyde Chemical compound OCC(O)C=O MNQZXJOMYWMBOU-UHFFFAOYSA-N 0.000 title claims description 16
238000000034 method Methods 0.000 claims abstract description 104
NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims abstract description 90
108010046163 Glycogen Phosphorylase Proteins 0.000 claims abstract description 73
102000007390 Glycogen Phosphorylase Human genes 0.000 claims abstract description 73
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-1 2-hydrOxy-ethyl Chemical group 0.000 claims description 195
239000002253 acid Substances 0.000 claims description 72
FUQOTYRCMBZFOL-UHFFFAOYSA-N 5-chloro-1H-indole-2-carboxylic acid Chemical group ClC1=CC=C2NC(C(=O)O)=CC2=C1 FUQOTYRCMBZFOL-UHFFFAOYSA-N 0.000 claims description 55
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 38
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241000124008 Mammalia Species 0.000 claims description 17
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 description 16
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125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 12
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125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 5
RIIVBOIBIOLLPO-UHFFFAOYSA-N 2-phthalazin-1-ylacetic acid Chemical compound C1=CC=C2C(CC(=O)O)=NN=CC2=C1 RIIVBOIBIOLLPO-UHFFFAOYSA-N 0.000 claims description 5
239000003937 drug carrier Substances 0.000 claims description 5
LFVXINNUOAXXAV-NSHDSACASA-N (2S)-2-amino-1-(3-hydroxyazetidin-1-yl)-3-phenylpropan-1-one Chemical compound C([C@H](N)C(=O)N1CC(O)C1)C1=CC=CC=C1 LFVXINNUOAXXAV-NSHDSACASA-N 0.000 claims description 4
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230000002301 combined effect Effects 0.000 claims description 3
SGPGESCZOCHFCL-UHFFFAOYSA-N Tilisolol hydrochloride Chemical compound [Cl-].C1=CC=C2C(=O)N(C)C=C(OCC(O)C[NH2+]C(C)(C)C)C2=C1 SGPGESCZOCHFCL-UHFFFAOYSA-N 0.000 claims 5
TWKHGKCRNDRGFY-UHFFFAOYSA-N 2-amino-1-(1,1-dioxo-1,3-thiazolidin-3-yl)ethanone Chemical compound NCC(=O)N1CCS(=O)(=O)C1 TWKHGKCRNDRGFY-UHFFFAOYSA-N 0.000 claims 2
XBNPCJMXDNUUNN-ZDUSSCGKSA-N (2s)-2-amino-3-(4-fluorophenyl)-1-(4-hydroxypiperidin-1-yl)propan-1-one Chemical compound C([C@H](N)C(=O)N1CCC(O)CC1)C1=CC=C(F)C=C1 XBNPCJMXDNUUNN-ZDUSSCGKSA-N 0.000 claims 1
AVGBKIPAXGXJQH-SYDPRGILSA-N 2-amino-1-[(3S,4R)-3,4-dihydroxypyrrolidin-1-yl]ethanone Chemical compound NCC(=O)N1C[C@H](O)[C@H](O)C1 AVGBKIPAXGXJQH-SYDPRGILSA-N 0.000 claims 1
FTMFRKISBMECSW-SLFFLAALSA-N 5-chloro-n-[(2s)-1-[(3r,4s)-3,4-dihydroxypyrrolidin-1-yl]-1-oxo-3-phenylpropan-2-yl]-1h-indole-2-carboxamide Chemical compound C1[C@@H](O)[C@@H](O)CN1C(=O)[C@@H](NC(=O)C=1NC2=CC=C(Cl)C=C2C=1)CC1=CC=CC=C1 FTMFRKISBMECSW-SLFFLAALSA-N 0.000 claims 1
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239000000203 mixture Substances 0.000 abstract description 47
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125000000217 alkyl group Chemical group 0.000 description 169
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125000005843 halogen group Chemical group 0.000 description 52
PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 50
239000000543 intermediate Substances 0.000 description 50
230000000694 effects Effects 0.000 description 49
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YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 42
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OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 41
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125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 36
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 33
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 33
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WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 30
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BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 24
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JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
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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
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Classifications

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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
- 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
- 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
- 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

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Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Chemical Kinetics & Catalysis (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Diabetes (AREA)
Obesity (AREA)
Hematology (AREA)
Epidemiology (AREA)
Cardiology (AREA)
Heart & Thoracic Surgery (AREA)
Endocrinology (AREA)
Emergency Medicine (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Child & Adolescent Psychology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Superheterodyne Receivers (AREA)
Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Indole Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Noise Elimination (AREA)
Enzymes And Modification Thereof (AREA)

OA1200000137A 1997-11-21 2000-05-12 Combination of an aldose reductase inhibitor and aglycogen phosphrylase inhibitor. OA11379A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US6636597P	1997-11-21	1997-11-21

Publications (1)

Publication Number	Publication Date
OA11379A true OA11379A (en)	2004-01-28

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ID=22069038

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA1200000137A OA11379A (en)	1997-11-21	2000-05-12	Combination of an aldose reductase inhibitor and aglycogen phosphrylase inhibitor.

Country Status (38)

Country	Link
EP (1)	EP1032424B9 (fr)
JP (1)	JP2002504478A (fr)
KR (2)	KR20010032304A (fr)
CN (1)	CN1279617A (fr)
AP (1)	AP911A (fr)
AR (1)	AR016423A1 (fr)
AT (1)	ATE205403T1 (fr)
AU (1)	AU733304B2 (fr)
BG (1)	BG104435A (fr)
BR (1)	BR9814698A (fr)
CA (1)	CA2310069A1 (fr)
DE (1)	DE69801680T2 (fr)
DK (1)	DK1032424T3 (fr)
DZ (1)	DZ2656A1 (fr)
EA (1)	EA002365B1 (fr)
ES (1)	ES2161548T3 (fr)
GR (1)	GR3037071T3 (fr)
GT (1)	GT199800166A (fr)
HR (1)	HRP20000327A2 (fr)
HU (1)	HUP0100272A3 (fr)
ID (1)	ID24524A (fr)
IL (1)	IL135713A0 (fr)
IS (1)	IS5453A (fr)
MA (1)	MA26568A1 (fr)
NO (1)	NO20002164L (fr)
OA (1)	OA11379A (fr)
PA (1)	PA8462301A1 (fr)
PE (1)	PE135399A1 (fr)
PL (1)	PL340643A1 (fr)
PT (1)	PT1032424E (fr)
SK (1)	SK7222000A3 (fr)
TN (1)	TNSN98211A1 (fr)
TR (1)	TR200001451T2 (fr)
UA (1)	UA57811C2 (fr)
UY (1)	UY25258A1 (fr)
WO (1)	WO1999026659A1 (fr)
YU (1)	YU30700A (fr)
ZA (1)	ZA9810636B (fr)

Families Citing this family (45)

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Publication number	Priority date	Publication date	Assignee	Title
JP2002536410A (ja) *	1999-02-12	2002-10-29	ノボノルディスクアクティーゼルスカブ	肥満の治療又は予防もしくは食欲の調節を目的とした薬学的組成物の製造におけるピロリジン誘導体の使用
EP1741445B1 (fr)	2000-01-21	2013-08-14	Novartis AG	Combinaisons à base d'inhibiteurs de DPP-IV et d'antidiabetiques
CO5271699A1 (es) *	2000-01-24	2003-04-30	Pfizer Prod Inc	Procedimiento para el tratamiento de cardiomiopatia utilizando inhibidores de la glucogeno fosforilasa
US6570013B2 (en)	2000-02-16	2003-05-27	Pfizer Inc	Salts of zopolrestat
US6395767B2 (en)	2000-03-10	2002-05-28	Bristol-Myers Squibb Company	Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
IL144507A0 (en) *	2000-07-31	2002-05-23	Pfizer Prod Inc	Use of glycogen phosphorylase inhibitors to inhibit tumor growth
WO2002098429A1 (fr) *	2001-06-07	2002-12-12	Pfizer Products Inc.	Formes salines du zopolrestat, a savoir ethanolamine, diethanolamine ou triethanolamine
GB0205175D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
GB0205162D0 (en)	2002-03-06	2002-04-17	Astrazeneca Ab	Chemical compounds
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1998
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- 1998-11-02 PT PT81300054T patent/PT1032424E/pt unknown
- 1998-11-02 AU AU95558/98A patent/AU733304B2/en not_active Ceased
- 1998-11-02 EP EP98949193A patent/EP1032424B9/fr not_active Expired - Lifetime
- 1998-11-02 CN CN98811329A patent/CN1279617A/zh active Pending
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- 1998-11-02 WO PCT/IB1998/001752 patent/WO1999026659A1/fr not_active Ceased
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1999
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Also Published As

Publication number	Publication date
UA57811C2 (uk)	2003-07-15
DE69801680D1 (de)	2001-10-18
IS5453A (is)	2000-04-14
NO20002164D0 (no)	2000-04-27
EA002365B1 (ru)	2002-04-25
KR20010032300A (ko)	2001-04-16
HRP20000327A2 (en)	2001-02-28
GR3037071T3 (en)	2002-01-31
PE135399A1 (es)	2000-01-15
UY25258A1 (es)	2000-12-29
ATE205403T1 (de)	2001-09-15
AP9801401A0 (en)	1998-12-31
EP1032424A1 (fr)	2000-09-06
KR20010032304A (ko)	2001-04-16
PA8462301A1 (es)	2000-05-24
WO1999026659A1 (fr)	1999-06-03
DE69801680T2 (de)	2002-02-07
ID24524A (id)	2000-07-20
KR100661214B1 (ko)	2006-12-26
ZA9810636B (en)	2000-05-22
GT199800166A (es)	2000-04-19
TR200001451T2 (tr)	2002-06-21
SK7222000A3 (en)	2001-09-11
PL340643A1 (en)	2001-02-12
TNSN98211A1 (fr)	2005-03-15
EP1032424B9 (fr)	2004-10-06
AR016423A1 (es)	2001-07-04
MA26568A1 (fr)	2004-12-20
CN1279617A (zh)	2001-01-10
EA200000433A1 (ru)	2000-12-25
CA2310069A1 (fr)	1999-06-03
BG104435A (bg)	2001-01-31
HUP0100272A2 (hu)	2001-06-28
JP2002504478A (ja)	2002-02-12
HUP0100272A3 (en)	2002-11-28
EP1032424B1 (fr)	2001-09-12
IL135713A0 (en)	2001-05-20
DZ2656A1 (fr)	2003-03-22
BR9814698A (pt)	2000-10-03
DK1032424T3 (da)	2001-11-19
YU30700A (sh)	2002-12-10
AU733304B2 (en)	2001-05-10
ES2161548T3 (es)	2001-12-01
AU9555898A (en)	1999-06-15
NO20002164L (no)	2000-07-19
PT1032424E (pt)	2001-12-28
AP911A (en)	2000-12-07

Publication	Publication Date	Title
AU733304B2 (en)	2001-05-10	Combination of an aldose reductase inhibitor and a glycogen phosphorylase inhibitor
AU717547B2 (en)	2000-03-30	Method of reducing tissue damage associated with non-cardiac ischemia using glycogen phosphorylase inhibitors
AP624A (en)	1997-12-19	Substituted n-(indole-2-carbonyl)-b- alanimamides and derivatives as antidiabetic agents.
CA2279732A1 (fr)	2000-02-07	Methode pour inhiber la phosphorylase de glycogene humain
US6277877B1 (en)	2001-08-21	Substituted n-(indole-2-carbonyl)glycinamides and derivates as glycogen phosphorylase inhibitors
US6846820B2 (en)	2005-01-25	Substituted N-(indole-2-carbonyl) -amides and derivatives as glycogen phosphorylase inhibitors
JP2000500490A (ja)	2000-01-18	糖尿病治療用の４−ヒドロキシクマリン−３−カルボキシアミド
MXPA00005025A (en)	2001-05-07	Combination of an aldose reductase inhibitor and a glycogen phosphorylase inhibitor
CZ20001837A3 (cs)	2001-05-16	Kombinace inhibitoru aldosa reduktasy a inhibitoru glykogen fosforylasy