BRPI0414462A - derivados de ácido 4-(fenil-etilidenoaminóxi-propóxi)-fenil-acético e compostos relacionados como inibidores de pai-1 para o tratamento de dano do sistema fibrinolìtico e de trombose - Google Patents

derivados de ácido 4-(fenil-etilidenoaminóxi-propóxi)-fenil-acético e compostos relacionados como inibidores de pai-1 para o tratamento de dano do sistema fibrinolìtico e de trombose

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Publication number
BRPI0414462A
BRPI0414462A BRPI0414462-7A BRPI0414462A BRPI0414462A BR PI0414462 A BRPI0414462 A BR PI0414462A BR PI0414462 A BRPI0414462 A BR PI0414462A BR PI0414462 A BRPI0414462 A BR PI0414462A
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Prior art keywords
aryl
heteroaryl
phenyl
pai
thrombosis
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BRPI0414462-7A
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English (en)
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Lisa Marie Havran
John Anthony Butera
Hassan Mahmoud Elokdah
Douglas John Jenkins
Eric Gould Gundersen
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Wyeth Corp
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Publication of BRPI0414462A publication Critical patent/BRPI0414462A/pt

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Abstract

"DERIVADOS DE áCIDO 4-(FENIL-ETILIDENOAMINóXI-PROPóXI)-FENIL-ACéTICO E COMPOSTOS RELACIONADOS COMO INIBIDORES DE PAI-1 PARA O TRATAMENTO DE DANO DO SISTEMA FIBRINOLìTICO E DE TROMBOSE". A presente invenção refere-se a oximas de arila substituída de fórmula (i) ou um sal farmaceuticamente aceitável ou forma de éster deste em que R~ 1~ é uma ligação direta a A, C~ 1~-C~ 4~ alquileno ou -O-C~ 1~-C~ 4~ alquileno; R~ 2~ e R~ 3~ são, independentemente, hidrogênio, halogênio, C~ 1~-C~ 4~ alquila, C~ 1~-C~ 3~ perfluoroalquila, -O-C~ 1~-C~ 3~ perfluoroalquila, C~ 1~-C~ 3~ alcóXi, -OH, -NH~ 2~, -NO~ 2~, -O(CH~ 2~)~ p~-arila, -O(CH~ 2~)~ p~-heteroarila, arila, heteroarila, -NH(CH~ 2~)~ p~-arila, -NH(CH~ 2~)~ p~-heteroarila, -NH(CO)-arila, -NH(CO)-heteroarila, -O(CO)-arila, -O(CO)-heteroarila, -NH(CO)-CH=CH-arila ou -NH(CO)-CH=CH-heteroarila; p é um número inteiro de 0 - 6; R~ 4~ é hidrogênio, C~ 1~-C~ 8~ alquila ou C~ 3~-C~ 6~ cicloalquila; A é COOH ou uma imitação de ácido; X é C~ 1~-C~ 8~ alquileno, C~ 3~-C~ 6~ cicloalquileno, -(CH~ 2~)~ m~O- ou -(CH~ 2~)~ m~NH-; m é um número inteiro de 1- 6; R~ 5~ e R~ 6~, São, independentemente, hidrogênio, halogênio, C~ 1~-C~ 6~ alquila, C~ 1~-C~ 6~ perfluoroalquila, -O-C~ 1~-C~ 6~ perfluoroalquila, C~ 1~-C~ 6~ alcóxi, -OH, -NH~ 2~, -NO~ 2~, -O(CH~ 2~)~ n~-arila, -O(CH~ 2~)~ n~-heteroarila, arila ou heteroarila; e n é um número inteiro de 0 - 6, em que C~ 1~-C~ 4~ alquileno, -O-C~ 1~-C~ 4~ alquileno, alquila, arila e heteroarila são cada qual opcionalmente substituídas por um ou mais substituintes. Os compostos presentes são inibidores de PAI-1 para o tratamento, por exemplo, de dano do sistema fibrinolítico, trombose ou doenças cardiovasculares.
BRPI0414462-7A 2003-09-25 2004-09-24 derivados de ácido 4-(fenil-etilidenoaminóxi-propóxi)-fenil-acético e compostos relacionados como inibidores de pai-1 para o tratamento de dano do sistema fibrinolìtico e de trombose BRPI0414462A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US50580103P 2003-09-25 2003-09-25
US10/948,611 US7420083B2 (en) 2003-09-25 2004-09-23 Substituted aryloximes
PCT/US2004/031460 WO2005030193A1 (en) 2003-09-25 2004-09-24 4-(phenyl-ethylideneaminoxy-propoxy) -phenyl-acetic acid derivatives and related compounds as pai-1 inhibitors for the treatment of impairment of the fibrinolytic system and of thrombosis

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Publication Number Publication Date
BRPI0414462A true BRPI0414462A (pt) 2006-11-21

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BRPI0414462-7A BRPI0414462A (pt) 2003-09-25 2004-09-24 derivados de ácido 4-(fenil-etilidenoaminóxi-propóxi)-fenil-acético e compostos relacionados como inibidores de pai-1 para o tratamento de dano do sistema fibrinolìtico e de trombose

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US (2) US7420083B2 (pt)
EP (1) EP1663189A1 (pt)
JP (1) JP2007506773A (pt)
AU (1) AU2004275824A1 (pt)
BR (1) BRPI0414462A (pt)
CA (1) CA2538259A1 (pt)
MX (1) MXPA06003247A (pt)
WO (1) WO2005030193A1 (pt)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI224101B (en) * 2001-06-20 2004-11-21 Wyeth Corp Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
ES2268480T3 (es) * 2002-12-10 2007-03-16 Wyeth Derivados del acido 3-alquilo- y 3-arilalquilo-1h-indol-1-il-acetico sustituidos como inhibidores del inhibidor del activador del plasminogeno-1 (pai-1).
BR0316574A (pt) * 2002-12-10 2005-10-04 Wyeth Corp Derivados de ácido acético 3-carbonil-1h-indol-1-il substituìdo como inibidores do inibidor-1 do ativador do plasminogênio (pai-1)
DE60324183D1 (en) * 2002-12-10 2008-11-27 Wyeth Corp Aryl-, aryloxy- und alkyloxysubstituierte 1h-indol-3-yl-glyoxylsäurederivateals inhibitoren des plasminogenaktivatorinhibitors-1 (pai-1)
UA80453C2 (en) * 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
AU2004220221A1 (en) * 2003-03-13 2004-09-23 Ono Pharmaceutical Co., Ltd. Imino ether derivative compounds and drugs containing the compounds as the active ingredient
US7446201B2 (en) * 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7342039B2 (en) * 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7141592B2 (en) * 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7332521B2 (en) * 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7442805B2 (en) * 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7163954B2 (en) * 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7351726B2 (en) * 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
US7582773B2 (en) * 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7268159B2 (en) * 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7265148B2 (en) * 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7420083B2 (en) * 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7534894B2 (en) * 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
BRPI0514549A (pt) * 2004-08-23 2008-06-17 Wyeth Corp ácidos de pirrol-naftila como inibidores de pai-1
CN101039936A (zh) * 2004-08-23 2007-09-19 惠氏公司 作为i-型纤溶酶原激活剂抑制剂(pai-1)调节剂用于治疗血栓形成和心血管疾病的唑基-萘基酸
US7605172B2 (en) 2004-08-23 2009-10-20 Wyeth Thiazolo-naphthyl acids
EP1919866A2 (en) * 2005-08-17 2008-05-14 Wyeth a Corporation of the State of Delaware Substituted indoles and use thereof
JP2009528290A (ja) * 2006-02-27 2009-08-06 ワイス 筋肉病の処置のためのpai−1阻害剤
EP2080751A4 (en) * 2006-10-12 2011-06-22 Inst Med Molecular Design Inc CARBOXYLIC ACID DERIVATIVE
EP2072498A4 (en) * 2006-10-12 2012-07-18 Inst Med Molecular Design Inc N-PHENYLOXAMIDE ACID DERIVATIVE
US8633245B2 (en) * 2008-04-11 2014-01-21 Institute Of Medicinal Molecular Design, Inc. PAI-1 inhibitor
WO2010011302A1 (en) * 2008-07-22 2010-01-28 Chdi, Inc. Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
EP2597670B1 (de) 2010-03-31 2016-03-30 EV Group E. Thallner GmbH Verfahren zum permanenten Verbinden zweier Metalloberflächen
KR101510975B1 (ko) * 2010-12-28 2015-04-10 카딜라 핼쓰캐어 리미티드 이상지질혈증의 치료에 적절한 헤테로시클릭 화합물
ES2629194T3 (es) 2011-08-30 2017-08-07 Chdi Foundation, Inc. Inhibidores de kinurenina-3-monoxigenasa, composiciones farmacéuticas y métodos de utilización del mismo
CN103827095A (zh) 2011-08-30 2014-05-28 Chdi基金会股份有限公司 犬尿氨酸-3-单加氧酶抑制剂、其药物组合物及其使用方法
UA120856C2 (uk) 2014-07-17 2020-02-25 Кхді Фаундейшн, Інк. Способи та композиції для лікування розладів, пов'язаних з віл
CN105541741A (zh) * 2016-01-14 2016-05-04 青岛友诚高新技术有限公司 一种具有治疗冠心病活性的化合物及其制备方法

Family Cites Families (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US678556A (en) * 1900-11-20 1901-07-16 George Froeba Lock.
US3026325A (en) 1959-01-26 1962-03-20 Upjohn Co 5-hydroxy-alpha-alkyltryptophans
US3476770A (en) 1967-04-14 1969-11-04 Parke Davis & Co 2-methyl-7-phenylindole-3-acetic acid compounds
GB1321433A (en) 1968-01-11 1973-06-27 Roussel Uclaf 1,2,3,6-tetrasubstituted indoles
US3557142A (en) 1968-02-20 1971-01-19 Sterling Drug Inc 4,5,6,7-tetrahydro-indole-lower-alkanoic acids and esters
FR2244499A1 (en) 1973-06-07 1975-04-18 Delalande Sa Indol-3-ylformaldoxime carbamates - for treating anxiety epilepsy, cardiac arrhythmias, asthma, intestinal spasm, peptic ulcer, cardiac insufficiency
DE3147276A1 (de) 1981-11-28 1983-06-09 Boehringer Mannheim Gmbh, 6800 Mannheim Verfahren zur herstellung von indolderivaten, deren verwendung als wertvolle zwischenprodukte und neue 4-hydroxyindole
FR2525474A1 (fr) 1982-04-26 1983-10-28 Roussel Uclaf Nouvelle forme pharmaceutique orale de clometacine
DE3531658A1 (de) 1985-09-05 1987-03-12 Boehringer Mannheim Gmbh Heterocyclisch substituierte indole, zwischenprodukte, verfahren zu ihrer herstellung und arzneimittel
US5164372A (en) 1989-04-28 1992-11-17 Fujisawa Pharmaceutical Company, Ltd. Peptide compounds having substance p antagonism, processes for preparation thereof and pharmaceutical composition comprising the same
IL95584A (en) 1989-09-07 1995-03-15 Abbott Lab Indole-, benzoporene- and benzothiophene compounds including lipoxygenase-inhibiting compounds and pharmaceutical compounds containing them
US5420289A (en) 1989-10-27 1995-05-30 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
DE4035961A1 (de) 1990-11-02 1992-05-07 Thomae Gmbh Dr K Cyclische iminoderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
US5151435A (en) 1991-04-08 1992-09-29 Merck & Co., Inc. Angiotensin ii antagonists incorporating an indole or dihydroindole
IL101785A0 (en) 1991-05-10 1992-12-30 Fujisawa Pharmaceutical Co Urea derivatives,processes for the preparation thereof and pharmaceutical compositions containing the same
GB9123396D0 (en) 1991-11-04 1991-12-18 Hoffmann La Roche A process for the manufacture of substituted maleimides
US5502187A (en) 1992-04-03 1996-03-26 The Upjohn Company Pharmaceutically active bicyclic-heterocyclic amines
IL105191A (en) * 1992-04-04 1998-08-16 Basf Ag Acids and aminooxymethylbenzoic acids and their preparation
US5612360A (en) 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
DE4242675A1 (de) 1992-12-17 1994-06-23 Basf Ag Neue Hydroxyiminoalkylindolcarbonsäure-Derivate, ihre Herstellung und Verwendung
ZA939516B (en) 1992-12-22 1994-06-06 Smithkline Beecham Corp Endothelin receptor antagonists
IL109568A0 (en) 1993-05-19 1994-08-26 Fujisawa Pharmaceutical Co Urea derivatives, pharmaceutical compositions containing the same and processes for the preparation thereof
JPH0741459A (ja) 1993-07-29 1995-02-10 Sumitomo Pharmaceut Co Ltd 新規エラスターゼ阻害剤
US5599663A (en) 1993-08-27 1997-02-04 Brighan & Women's Hospital Angiotensin IV and analogs as regulators of fibrinolysis
US6756388B1 (en) 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
DE4338770A1 (de) 1993-11-12 1995-05-18 Matthias Dr Lehr Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶
CA2134192A1 (en) 1993-11-12 1995-05-13 Michael L. Denney 5, 6-bicyclic glycoprotein iib/iiia antagonists
MX9603516A (es) 1994-03-10 1997-03-29 Bayer Ag Derivados de oxima y su uso como pesticidas.
GB9408577D0 (en) 1994-04-29 1994-06-22 Fujisawa Pharmaceutical Co New compound
US5521213A (en) 1994-08-29 1996-05-28 Merck Frosst Canada, Inc. Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
EP0779884B1 (de) * 1994-09-09 2000-05-03 Bayer Ag Imidsäurederivate und ihre verwendung als schädlingsbekämpfungsmittel
US5703096A (en) 1994-10-07 1997-12-30 Sankyo Company, Limited Oxime derivatives, their preparation and their therapeutic use
US5482960A (en) 1994-11-14 1996-01-09 Warner-Lambert Company Nonpeptide endothelin antagonists
US5552412A (en) 1995-01-09 1996-09-03 Pfizer Inc 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis
IL117208A0 (en) 1995-02-23 1996-06-18 Nissan Chemical Ind Ltd Indole type thiazolidines
DE69622031T2 (de) 1995-04-10 2002-12-12 Fujisawa Pharmaceutical Co INDOLDERIVATE ALS cGMP-PDE INHIBITOREN
US5728724A (en) 1995-08-17 1998-03-17 Eli Lilly And Company Benzothiophene compounds
DE19530199A1 (de) * 1995-08-17 1997-02-20 Bayer Ag Alkoxyacrylsäurethiolester
CA2203912A1 (en) 1995-09-01 1997-03-13 Dennis Michael Zimmerman Indolyl neuropeptide y receptor antagonists
US6221865B1 (en) 1995-11-06 2001-04-24 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
DE19543639A1 (de) 1995-11-23 1997-05-28 Merck Patent Gmbh Endothelin-Rezeptor-Antagonisten
ATE252074T1 (de) 1996-04-04 2003-11-15 Sankyo Co Phenylalkylcarbonsäure-derivate
JPH09323967A (ja) * 1996-04-04 1997-12-16 Sankyo Co Ltd フェニルアルキルカルボン酸誘導体
GB9609641D0 (en) 1996-05-09 1996-07-10 Pfizer Ltd Compounds useful in therapy
CA2258728C (en) 1996-06-19 2011-09-27 Rhone Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
CA2207083A1 (en) 1996-07-15 1998-01-15 Brian William Grinnell Benzothiophene compounds, and uses and formulations thereof
EP0822185A1 (en) 1996-07-31 1998-02-04 Pfizer Inc. B-3-adrenergic agonists as antidiabetic and antiobesity agents
AU717430B2 (en) 1996-08-26 2000-03-23 Genetics Institute, Llc Inhibitors of phospholipase enzymes
ATE546139T1 (de) 1997-05-07 2012-03-15 Univ Pittsburgh Isoprentransferase proteine inhibitoren
JPH11193272A (ja) 1997-10-01 1999-07-21 Sankyo Co Ltd フェニルアルキルカルボン酸誘導体を含有する医薬
DE19753522A1 (de) 1997-12-03 1999-06-10 Boehringer Ingelheim Pharma Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel
WO1999043651A2 (en) 1998-02-25 1999-09-02 Genetics Institute, Inc. Inhibitors of phospholipase enzymes
PL342516A1 (en) 1998-02-25 2001-06-18 Genetics Inst Phospholipase a2 inhibitors
EA003876B1 (ru) 1998-02-25 2003-10-30 Дженетикс Инститьют, Ллс Ингибиторы фосфолипазных ферментов
SE9800836D0 (sv) 1998-03-13 1998-03-13 Astra Ab New Compounds
FR2777886B1 (fr) 1998-04-27 2002-05-31 Adir Nouveaux derives benzothiopheniques, benzofuraniques et indoliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6232322B1 (en) 1998-05-12 2001-05-15 American Home Products Corporation Biphenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
US6251936B1 (en) 1998-05-12 2001-06-26 American Home Products Corporation Benzothiophenes, benzofurans, and indoles useful in the treatment of insulin resistance and hyperglycemia
US6166069A (en) 1998-05-12 2000-12-26 American Home Products Corporation Phenyl oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
US6110963A (en) 1998-05-12 2000-08-29 American Home Products Corporation Aryl-oxo-acetic acids useful in the treatment of insulin resistance and hyperglycemia
CA2353151A1 (en) 1998-12-16 2000-06-22 Boehringer Ingelheim Pharma Kg Substituted aryl and heteroaryl derivatives, the preparation thereof and their use as medicaments
AU2319100A (en) 1999-01-28 2000-08-18 Nippon Shinyaku Co. Ltd. Amide derivatives and drug compositions
JP2000344748A (ja) 1999-03-29 2000-12-12 Welfide Corp 3−芳香族置換プロピオン酸またはアクリル酸化合物
GB9919413D0 (en) 1999-08-18 1999-10-20 Zeneca Ltd Chemical compounds
FR2799756B1 (fr) 1999-10-15 2001-12-14 Adir Nouveaux derives benzothiopheniques, benzofuraniques et indoliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE19963178A1 (de) 1999-12-27 2001-07-05 Gruenenthal Gmbh Substituierte Indol-Mannichbasen
WO2002024633A1 (fr) * 2000-09-21 2002-03-28 Sankyo Company, Limited Derives d'acide phenylpropionique
EP1695716A2 (en) * 2000-12-26 2006-08-30 Sankyo Company, Limited Medicinal compositions containing diuretics and insulin sensitizers
FR2825706B1 (fr) 2001-06-06 2003-12-12 Pf Medicament Nouveaux derives de benzothienyle ou d'indole, leur preparation et leur utilisation comme inhibiteurs de proteines prenyl transferase
EP1397130B1 (en) 2001-06-20 2007-07-25 Wyeth Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
TWI240723B (en) 2001-06-20 2005-10-01 Wyeth Corp Substituted naphthyl benzofuran derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
TWI224101B (en) 2001-06-20 2004-11-21 Wyeth Corp Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
US7291639B2 (en) 2001-06-20 2007-11-06 Wyeth Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
KR100810468B1 (ko) 2001-10-10 2008-03-07 씨제이제일제당 (주) 사이클로옥시게나제-2의 저해제로서 선택성이 뛰어난1h-인돌 유도체
BR0316574A (pt) 2002-12-10 2005-10-04 Wyeth Corp Derivados de ácido acético 3-carbonil-1h-indol-1-il substituìdo como inibidores do inibidor-1 do ativador do plasminogênio (pai-1)
DE60324183D1 (en) 2002-12-10 2008-11-27 Wyeth Corp Aryl-, aryloxy- und alkyloxysubstituierte 1h-indol-3-yl-glyoxylsäurederivateals inhibitoren des plasminogenaktivatorinhibitors-1 (pai-1)
ES2268480T3 (es) 2002-12-10 2007-03-16 Wyeth Derivados del acido 3-alquilo- y 3-arilalquilo-1h-indol-1-il-acetico sustituidos como inhibidores del inhibidor del activador del plasminogeno-1 (pai-1).
MXPA05006287A (es) 2002-12-10 2005-09-08 Wyeth Corp Derivados de acido indoloxo-acetilaminoacetico sustituidos como inhibidores del inhibidor del activador de plasminogeno 1 (pai-1).
UA80453C2 (en) 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
AU2004220221A1 (en) * 2003-03-13 2004-09-23 Ono Pharmaceutical Co., Ltd. Imino ether derivative compounds and drugs containing the compounds as the active ingredient
US20050215626A1 (en) 2003-09-25 2005-09-29 Wyeth Substituted benzofuran oximes
US7582773B2 (en) 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7351726B2 (en) 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7342039B2 (en) 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7442805B2 (en) 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7332521B2 (en) 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7163954B2 (en) 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7141592B2 (en) 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7420083B2 (en) * 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7268159B2 (en) 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7265148B2 (en) 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7446201B2 (en) 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids

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EP1663189A1 (en) 2006-06-07
CA2538259A1 (en) 2005-04-07
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US20080293790A1 (en) 2008-11-27
US7420083B2 (en) 2008-09-02

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