BR0210504A - Derivados de naftil-indol substituidos, atuantes como inibidores do inibidor tipo 1 (pai-1) do ativador de plasminogênio - Google Patents

Derivados de naftil-indol substituidos, atuantes como inibidores do inibidor tipo 1 (pai-1) do ativador de plasminogênio

Info

Publication number
BR0210504A
BR0210504A BR0210504-7A BR0210504A BR0210504A BR 0210504 A BR0210504 A BR 0210504A BR 0210504 A BR0210504 A BR 0210504A BR 0210504 A BR0210504 A BR 0210504A
Authority
BR
Brazil
Prior art keywords
hydrogen
optionally substituted
alkyl
inhibitors
alkanoyl
Prior art date
Application number
BR0210504-7A
Other languages
English (en)
Inventor
Scott Christian Mayer
Eric Gould Gundersen
Hassan Mahmoud Elokdah
David Leroy Crandall
Original Assignee
Wyeth Corp
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.)
Filing date
Publication date
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of BR0210504A publication Critical patent/BR0210504A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/04—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
    • A61P9/06—Antiarrhythmics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms

Abstract

"DERIVADOS DE NAFTIL-INDOL SUBSTITUìDOS, ATUANTES COMO INIBIDORES DO INIBIDOR TIPO 1 (PAI-1) DO ATIVADOR DE PLASMINOGêNIO". A presente invenção refere-se a compostos inibidores de PAI-1 de Fórmula (I): em que: R~ 1~, R~ 2~, R~ 3~ e R~ 4~ são cada um hidrogênio, alquila, alcanoíla, halogênio, OH, e arila opcionalmente substituída por R~ 8~, perfluoroalquila, alcóxi, amino, alquilamino, dialquilamino, perfluoroalcóxi; R~ 5~ é hidrogênio, alquila, perfluoroalquila, arila opcionalmente substituída por R~ 8~, alcanoíla, aroíla opcionalmente substituída por R~ 8~; R~ 6~ é hidrogênio, alquila, alquilarila, benzila opcionalmente substituída. por R~ 8~, alcanoíla, aroíla opcionalmente substituída por R~ 8~; R~ 7~ é hidrogênio, alquila, alquilarila, arila opcionalmente substituída por R~ 8~; n é um número inteiro de 0-6; A é COOH ou um ácido mímico, tal como tetrazol, SO~ 3~H, PO~ 3~H~ 2~, ácido tetrónico, etc. R~ 8~ é hidrogênio, alquila, cicloalquila, alcanoíla, halogênio, OH, perfluoroalquila, alcóxi, amino, alquilamino, dialquilamino, perfluoroalcóxi; ou um sal farmaceuticamente aceitável dos mesmos; assim como composições farmacêuticas e métodos de tratamento usando esses compostos.
BR0210504-7A 2001-06-20 2002-06-18 Derivados de naftil-indol substituidos, atuantes como inibidores do inibidor tipo 1 (pai-1) do ativador de plasminogênio BR0210504A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29965101P 2001-06-20 2001-06-20
PCT/US2002/021113 WO2003000684A1 (en) 2001-06-20 2002-06-18 Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (pai-1)

Publications (1)

Publication Number Publication Date
BR0210504A true BR0210504A (pt) 2004-05-18

Family

ID=23155676

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0210504-7A BR0210504A (pt) 2001-06-20 2002-06-18 Derivados de naftil-indol substituidos, atuantes como inibidores do inibidor tipo 1 (pai-1) do ativador de plasminogênio

Country Status (25)

Country Link
US (4) US6800654B2 (pt)
EP (1) EP1397356B1 (pt)
JP (1) JP4520144B2 (pt)
KR (1) KR20040007744A (pt)
CN (1) CN1280288C (pt)
AR (1) AR036101A1 (pt)
AT (1) ATE431346T1 (pt)
AU (1) AU2002316533B2 (pt)
BR (1) BR0210504A (pt)
CA (1) CA2448798C (pt)
CO (1) CO5540286A2 (pt)
DE (1) DE60232328D1 (pt)
EA (1) EA009696B1 (pt)
EC (1) ECSP034904A (pt)
ES (1) ES2325733T3 (pt)
HU (1) HUP0400233A3 (pt)
IL (1) IL159449A0 (pt)
MX (1) MXPA03011522A (pt)
NO (2) NO326316B1 (pt)
NZ (1) NZ530312A (pt)
PL (1) PL367525A1 (pt)
TW (1) TWI224101B (pt)
UA (1) UA78708C2 (pt)
WO (1) WO2003000684A1 (pt)
ZA (1) ZA200400380B (pt)

Families Citing this family (43)

* 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)
ES2290318T3 (es) * 2001-06-20 2008-02-16 Wyeth Derivados sustituidos de acido indolico como inhibidores del inhibidor del activador del plasminogeno-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)
UA80453C2 (en) * 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
CN1726191A (zh) * 2002-12-10 2006-01-25 惠氏公司 用作纤溶酶原激活物抑制剂－1(pai－1)的抑制剂的取代的吲哚氧代－乙酰氨基乙酸衍生物
CA2509170A1 (en) * 2002-12-10 2004-06-24 Wyeth Substituted 3-alkyl and 3-arylalkyl 1h-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
JP2006510673A (ja) * 2002-12-10 2006-03-30 ワイス プラスミノゲンアクティベータインヒビター１（ｐａｉ−１）のインヒビターとしての、アリール、アリールオキシ、および、アルキルオキシ置換１ｈ−インドール−３−イルグリオキシル酸誘導体
CN1726190A (zh) 2002-12-10 2006-01-25 惠氏公司 作为纤溶酶原激活物抑制剂－1(pai－1)的抑制剂的取代3－羰基－1h－吲哚－1－基乙酸衍生物
JP4390460B2 (ja) * 2003-02-21 2009-12-24 株式会社静岡カフェイン工業所 オキサゾール誘導体
US7534894B2 (en) * 2003-09-25 2009-05-19 Wyeth Biphenyloxy-acids
US7163954B2 (en) * 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7332521B2 (en) * 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7411083B2 (en) 2003-09-25 2008-08-12 Wyeth Substituted acetic acid derivatives
US7420083B2 (en) * 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7141592B2 (en) * 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US7342039B2 (en) * 2003-09-25 2008-03-11 Wyeth Substituted indole oximes
US7268159B2 (en) * 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7442805B2 (en) * 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7446201B2 (en) * 2003-09-25 2008-11-04 Wyeth Substituted heteroaryl benzofuran acids
US7351726B2 (en) * 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7265148B2 (en) * 2003-09-25 2007-09-04 Wyeth Substituted pyrrole-indoles
US7582773B2 (en) * 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7115815B2 (en) * 2003-10-31 2006-10-03 Adc Telecommunications, Inc. Cable utilizing varying lay length mechanisms to minimize alien crosstalk
US7605172B2 (en) * 2004-08-23 2009-10-20 Wyeth Thiazolo-naphthyl acids
MX2007002177A (es) * 2004-08-23 2007-04-02 Wyeth Corp Acidos de pirrolo-naftilo como inhibidores 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
CN101111491A (zh) * 2005-01-27 2008-01-23 惠氏公司 用于制备被取代的萘基吲哚衍生物的方法和化合物
WO2007022321A2 (en) * 2005-08-17 2007-02-22 Wyeth Substituted indoles and use thereof
MX2008011015A (es) * 2006-02-27 2008-11-14 Wyeth Corp Inhibidores de pai-1 para tratamiento de afecciones musculares.
JP5207972B2 (ja) 2006-10-12 2013-06-12 株式会社医薬分子設計研究所 カルボン酸誘導体
WO2008044731A1 (fr) 2006-10-12 2008-04-17 Institute Of Medicinal Molecular Design. Inc. Dérivé d'acide n-phényloxamidique
US9120744B2 (en) * 2007-04-16 2015-09-01 The Regents Of The University Of Michigan Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism
US8759327B2 (en) 2007-04-16 2014-06-24 The Regents Of The University Of Michigan Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism
EP2172458A4 (en) 2007-06-27 2011-11-16 Kowa Co pyrazolone
CA2703494A1 (en) 2007-10-23 2009-04-30 Institute Of Medicinal Molecular Design, Inc. Inhibitor of pai-1 production
CN102137837A (zh) 2008-04-11 2011-07-27 株式会社医药分子设计研究所 Pai-1抑制剂
US8633245B2 (en) * 2008-04-11 2014-01-21 Institute Of Medicinal Molecular Design, Inc. PAI-1 inhibitor
HUE053325T2 (hu) 2012-10-31 2021-06-28 Univ Michigan Regents Plazminogén aktivátor-1 gátlók és ezek alkalmazási eljárásai
CA3008686C (en) 2015-12-18 2023-03-14 Talengen International Limited Method for preventing and treating diabetic nephropathy
CN106890324A (zh) * 2015-12-18 2017-06-27 深圳瑞健生命科学研究院有限公司 一种预防和治疗糖尿病肾病的方法
TWI763680B (zh) 2016-12-15 2022-05-11 大陸商深圳瑞健生命科學硏究院有限公司 纖溶酶原在製備藥物中的用途
JP7291119B2 (ja) 2017-07-27 2023-06-14 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン プラスミノーゲン活性化因子阻害剤－１（ｐａｉ－１）阻害剤および使用方法
CN114057623B (zh) * 2021-12-07 2023-07-21 湖南第一师范学院 一种n-萘基吲哚衍生物及其合成方法

Family Cites Families (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US4519909A (en) * 1977-07-11 1985-05-28 Akzona Incorporated Microporous products
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
US4859538A (en) * 1986-11-20 1989-08-22 Ribi Hans O Novel lipid-protein compositions and articles and methods for their preparation
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
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
US6756388B1 (en) 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
CA2134192A1 (en) 1993-11-12 1995-05-13 Michael L. Denney 5, 6-bicyclic glycoprotein iib/iiia antagonists
DE4338770A1 (de) 1993-11-12 1995-05-18 Matthias Dr Lehr Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶
US5521213A (en) 1994-08-29 1996-05-28 Merck Frosst Canada, Inc. Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
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
KR100430059B1 (ko) 1995-04-10 2004-09-24 후지사와 야꾸힝 고교 가부시키가이샤 cGMP-PDE억제제로서의인돌유도체
US5728724A (en) 1995-08-17 1998-03-17 Eli Lilly And Company Benzothiophene compounds
WO1997009308A1 (en) 1995-09-01 1997-03-13 Eli Lilly And Company Indolyl neuropeptide y receptor antagonists
DE19543639A1 (de) 1995-11-23 1997-05-28 Merck Patent Gmbh Endothelin-Rezeptor-Antagonisten
GB9609641D0 (en) 1996-05-09 1996-07-10 Pfizer Ltd Compounds useful in therapy
EP0934307B1 (en) 1996-06-19 2011-04-27 Aventis Pharma 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
CA2207141A1 (en) * 1996-07-15 1998-01-15 David Thompson Berg Benzothiophene compounds, and uses and formulations thereof
US5859044A (en) * 1996-07-31 1999-01-12 Pfizer Inc. β-adrenergic agonists
WO1998008818A1 (en) 1996-08-26 1998-03-05 Genetics Institute, Inc. Inhibitors of phospholipase enzymes
DE19753522A1 (de) 1997-12-03 1999-06-10 Boehringer Ingelheim Pharma Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel
KR20010041346A (ko) 1998-02-25 2001-05-15 브루스 엠. 에이센, 토마스 제이 데스로저 포스포리파제 ａ2 억제제
KR20010041344A (ko) 1998-02-25 2001-05-15 브루스 엠. 에이센, 토마스 제이 데스로저 포스포리파제 효소의 억제제
CN1299347A (zh) 1998-02-25 2001-06-13 遗传研究所有限公司 磷脂酶抑制剂
SE9800836D0 (sv) 1998-03-13 1998-03-13 Astra Ab New Compounds
US6214991B1 (en) 1998-03-31 2001-04-10 The Institute For Pharmaceutical Discovery, Inc. Substituted indolealkanoic acids
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
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
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
BR9911779A (pt) 1998-05-12 2001-02-06 American Home Prod Benzotiofenos, benzofuranos e indóis úteis no tratamento de resistência à insulina e hiperglicemia
AU3791799A (en) 1998-05-12 1999-11-29 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
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
WO2000031045A1 (fr) * 1998-11-20 2000-06-02 Torii Pharmaceutical Co., Ltd. Derives de naphtalene
TNSN99224A1 (fr) 1998-12-01 2005-11-10 Inst For Pharm Discovery Inc Methodes de reduction des niveaux de glucose et triglyceride en serum et pour suppression de l'antigenese utilisant les acides la indolealkanoique
AU2097100A (en) * 1998-12-16 2000-07-03 Boehringer Ingelheim Pharma Kg Substituted aryl and heteroaryl derivatives, their production and their use as medicines
GB9827882D0 (en) 1998-12-17 1999-02-10 Smithkline Beecham Plc Novel compounds
WO2000044743A1 (fr) 1999-01-28 2000-08-03 Nippon Shinyaku Co., Ltd. Derives d'amides et compositions de medicaments
GB9902459D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
SK15522001A3 (sk) 1999-04-28 2002-06-04 Aventis Pharma Deutschland Gmbh Deriváty kyselín s tromi arylovými zvyškami ako ligandy receptorov PPAR a farmaceutické kompozície, ktoré ich obsahujú
HUP0201291A3 (en) 1999-04-28 2002-11-28 Sanofi Aventis Deutschland Di-aryl acid derivatives as ppar receptor ligands and pharmaceutical compositions containing them
GB9919413D0 (en) * 1999-08-18 1999-10-20 Zeneca Ltd Chemical compounds
GB9919411D0 (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
DE10031281A1 (de) * 2000-06-27 2002-01-10 Creavis Tech & Innovation Gmbh Polyelektrolytbeschichteter, stoffdurchlässiger Verbundwerkstoff, Verfahren zu dessen Herstellung und die Verwendung des Verbundwerkstoffes
HUP0302477A2 (hu) 2000-10-10 2003-12-29 Smithkline Beecham Corp. Szubsztituált indolszármazékok, ezeket tartalmazó gyógyszerkészítmények és ezek alkalmazása PPAR-gamma kötő szerként
US6951848B2 (en) 2001-03-12 2005-10-04 Millennium Pharmaceuticals, Inc., Functionalized heterocycles as modulators of chemokine receptor function and methods of use therefor
US6808908B2 (en) * 2001-05-30 2004-10-26 Porex Technologies Corporation Functionalized porous substrate for binding chemical and biological moieties
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
US7291639B2 (en) * 2001-06-20 2007-11-06 Wyeth Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
ES2290318T3 (es) * 2001-06-20 2008-02-16 Wyeth Derivados sustituidos de acido indolico como inhibidores del inhibidor del activador del plasminogeno-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)
TWI240723B (en) * 2001-06-20 2005-10-01 Wyeth Corp Substituted naphthyl benzofuran derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
US7456025B2 (en) * 2001-08-28 2008-11-25 Porex Corporation Sintered polymer membrane for analyte detection device
KR100810468B1 (ko) * 2001-10-10 2008-03-07 씨제이제일제당 (주) 사이클로옥시게나제-2의 저해제로서 선택성이 뛰어난1ｈ-인돌 유도체
CN1915991B (zh) 2002-02-12 2010-05-26 威斯康星校友研究基金会 用于ah受体作为配体的吲哚噻唑化合物的合成
CA2509170A1 (en) * 2002-12-10 2004-06-24 Wyeth Substituted 3-alkyl and 3-arylalkyl 1h-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
CN1726191A (zh) * 2002-12-10 2006-01-25 惠氏公司 用作纤溶酶原激活物抑制剂－1(pai－1)的抑制剂的取代的吲哚氧代－乙酰氨基乙酸衍生物
UA80453C2 (en) * 2002-12-10 2007-09-25 Derivatives of substituted dyhydropyranoindol-3,4-dion as inhibitors of plasminogen activator inhibitor-1 (pai-1)
CN1726190A (zh) * 2002-12-10 2006-01-25 惠氏公司 作为纤溶酶原激活物抑制剂－1(pai－1)的抑制剂的取代3－羰基－1h－吲哚－1－基乙酸衍生物
JP2006510673A (ja) * 2002-12-10 2006-03-30 ワイス プラスミノゲンアクティベータインヒビター１（ｐａｉ−１）のインヒビターとしての、アリール、アリールオキシ、および、アルキルオキシ置換１ｈ−インドール−３−イルグリオキシル酸誘導体
US7141592B2 (en) * 2003-09-25 2006-11-28 Wyeth Substituted oxadiazolidinediones
US20050215626A1 (en) * 2003-09-25 2005-09-29 Wyeth Substituted benzofuran oximes
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
US7582773B2 (en) * 2003-09-25 2009-09-01 Wyeth Substituted phenyl indoles
US7268159B2 (en) * 2003-09-25 2007-09-11 Wyeth Substituted indoles
US7442805B2 (en) * 2003-09-25 2008-10-28 Wyeth Substituted sulfonamide-indoles
US7351726B2 (en) * 2003-09-25 2008-04-01 Wyeth Substituted oxadiazolidinediones
US7420083B2 (en) * 2003-09-25 2008-09-02 Wyeth Substituted aryloximes
US7332521B2 (en) * 2003-09-25 2008-02-19 Wyeth Substituted indoles
US7163954B2 (en) * 2003-09-25 2007-01-16 Wyeth Substituted naphthyl benzothiophene acids
US7342039B2 (en) * 2003-09-25 2008-03-11 Wyeth Substituted indole oximes

Also Published As

Publication number Publication date
MXPA03011522A (es) 2004-03-19
EP1397356B1 (en) 2009-05-13
KR20040007744A (ko) 2004-01-24
US7351730B2 (en) 2008-04-01
JP2004534825A (ja) 2004-11-18
NZ530312A (en) 2005-05-27
NO20084390L (no) 2003-12-17
PL367525A1 (en) 2005-02-21
IL159449A0 (en) 2004-06-01
ATE431346T1 (de) 2009-05-15
TWI224101B (en) 2004-11-21
US20080182883A1 (en) 2008-07-31
ZA200400380B (en) 2006-06-28
ES2325733T3 (es) 2009-09-15
EA009696B1 (ru) 2008-02-28
CO5540286A2 (es) 2005-07-29
US6800654B2 (en) 2004-10-05
AU2002316533B2 (en) 2007-10-18
EP1397356A1 (en) 2004-03-17
UA78708C2 (en) 2007-04-25
US20040266733A1 (en) 2004-12-30
CA2448798A1 (en) 2003-01-03
NO326316B1 (no) 2008-11-10
CN1280288C (zh) 2006-10-18
HUP0400233A3 (en) 2008-10-28
ECSP034904A (es) 2004-01-28
DE60232328D1 (de) 2009-06-25
US20060014725A1 (en) 2006-01-19
US20030032626A1 (en) 2003-02-13
US7629377B2 (en) 2009-12-08
WO2003000684A1 (en) 2003-01-03
CN1549814A (zh) 2004-11-24
HUP0400233A2 (hu) 2004-08-30
JP4520144B2 (ja) 2010-08-04
CA2448798C (en) 2010-07-20
EA200400054A1 (ru) 2004-04-29
AR036101A1 (es) 2004-08-11
NO20035635D0 (no) 2003-12-17
US6939886B2 (en) 2005-09-06

Similar Documents

Publication Publication Date Title
BR0210504A (pt) Derivados de naftil-indol substituidos, atuantes como inibidores do inibidor tipo 1 (pai-1) do ativador de plasminogênio
ATE253545T1 (de) Biarylessigsäure-derivate und ihre verwendung als cox-2 inhibitoren
TR200201506T2 (tr) Terapötik maddeler olarak kinaz inhibitörleri
TR199902606T2 (xx) Farnesil transferaz� engelleyici kinazolinonlar.
DE60217114D1 (de) Verbrückte bizyklische serinproteaseinhibitoren
BR0312999A (pt) Compostos, composições farmacêticas, método para aumentar a cognição, de tratamento, de inibição da atividade de enzima pde4 em um paciente
MY141661A (en) 17b-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
TR200201505T2 (tr) Terapötik maddeler olarak pirazolopirimidinler
CY1107852T1 (el) Νεες χρησεις αμινοξικων αντισπασμωδικων για τη θεραπευτικη αγωγη της ημικρανιας
ATE273305T1 (de) Thrombin-inhibitoren
NO20071042L (no) 5-substituerte 2-fenylaminobenzamider som MEK-inhibitorer
TNSN03144A1 (en) Pyrrolopyrimidines as protein kinase inhibitors
BR9809062A (pt) Inibidores da metaloproteinase, composições farmacêuticas comtendo os mesmos e seus usos farmacêuticos
BRPI0406721A (pt) Compostos condensados de furano
EA200300982A1 (ru) Гетероциклические производные для лечения рака и других пролиферативных заболеваний
BR0313969A (pt) Inibidores de oxitocina
ATE239741T1 (de) Derivate der phosphonsäure zur inhibierung von carboxypeptidase b
NO20022977L (no) Substituerte homopiperidinylbenzimidazolanaloger som fundiske relaksanter
DE69812028D1 (de) Creatine Derivate für Asthma
BR0313000A (pt) Compostos, composição farmacêutica e método para efetuar a inibição da enzima pde4, realçar a cognição e/ou tratar a psicose em um paciente
DK1451182T3 (da) Dimere forbindelser og deres anvendelse som antivirale midler
ATE229538T1 (de) 22r-hydroxycholesta-8,14-diene derivate zur hemmung der meiose
BRPI0416703A (pt) derivados de cicloalquila de 3-hidróxi-4-piridinonas
BR0307266A (pt) Compostos que inibem a atividade do fator xa
EA200200682A1 (ru) Новые соединения n-бензилпиперазина, способ их получения и фармацевтические композиции, их содержащие

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 9A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2108 DE 31/05/2011.