[go: up one dir, main page]

BR9814340A - Derivados de indol como inibidores de fator xa - Google Patents

Derivados de indol como inibidores de fator xa

Info

Publication number
BR9814340A
BR9814340A BR9814340-9A BR9814340A BR9814340A BR 9814340 A BR9814340 A BR 9814340A BR 9814340 A BR9814340 A BR 9814340A BR 9814340 A BR9814340 A BR 9814340A
Authority
BR
Brazil
Prior art keywords
formula
factor
compounds
inhibitors
blood clotting
Prior art date
Application number
BR9814340-9A
Other languages
English (en)
Other versions
BR9814340B1 (pt
Inventor
Elizabeth Defossa
Uwe Heinelt
Otmar Klingler
Gerhard Zoller
Fahad Al-Obeidi
Armin Walser
Peter Wildgoose
Hans Matter
Original Assignee
Aventis Pharma Gmbh
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 Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Publication of BR9814340A publication Critical patent/BR9814340A/pt
Publication of BR9814340B1 publication Critical patent/BR9814340B1/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Patente de Invenção: <B>"DERIVADOS DE INDOL COMO INIBIDORES DE FATOR Xa"<D>. A presente invenção refere-se à inibição de proteínas de coagulação sang³ínea e, mais particularmente, aos derivados de indol da fórmula (I), nos quais R^ 1a^ , R^ 1b^, R^ 1c^, R^ 1d^, R^ 2^, R^ 3^, R^ 4^ e A são definidos como indicado nas reivindicações. Os compostos da fórmulas (I) são inibidores do fator Xa da enzima de coagulação sang³ínea. A invenção refere-se também aos processos para a preparação dos compostos da fórmula (I), a métodos para inibir a atividade do fator Xa e de inibição da coagulação sang³ínea, ao uso dos compostos da fórmula (I) no tratamento e profilaxia de doenças que podem ser curadas ou prevenidas pela inibição da atividade do fator Xa, tais como doenças tromboembólicas, e ao uso dos compostos da fórmula (I) na preparação de medicamentos a serem aplicados em tais doenças. A invenção refere-se adicionalmente a composições que contêm um composto da fórmula (I) em mistura ou, de outro modo, em associação com um carreador inerte, particularmente composições farmacêuticas que contêm um composto da fórmula (I) junto com substâncias carreadoras aceitáveis farmaceuticamente e/ou substâncias auxiliares.
BRPI9814340-9A 1997-12-24 1998-12-10 compostos derivados de indol, processo para a preparação dos mesmo e composição farmacêutica. BR9814340B1 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP97122901 1997-12-24
PCT/EP1998/008030 WO1999033800A1 (en) 1997-12-24 1998-12-10 Indole derivatives as inhibitors or factor xa

Publications (2)

Publication Number Publication Date
BR9814340A true BR9814340A (pt) 2000-10-03
BR9814340B1 BR9814340B1 (pt) 2010-07-13

Family

ID=8227884

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI9814340-9A BR9814340B1 (pt) 1997-12-24 1998-12-10 compostos derivados de indol, processo para a preparação dos mesmo e composição farmacêutica.

Country Status (28)

Country Link
US (1) US6337344B1 (pt)
EP (1) EP1042287B1 (pt)
JP (1) JP4589529B2 (pt)
KR (1) KR100608472B1 (pt)
CN (1) CN1220681C (pt)
AR (1) AR018031A1 (pt)
AT (1) ATE293599T1 (pt)
AU (1) AU743881B2 (pt)
BR (1) BR9814340B1 (pt)
CA (1) CA2316172C (pt)
CZ (1) CZ298827B6 (pt)
DE (1) DE69829879T2 (pt)
DK (1) DK1042287T3 (pt)
ES (1) ES2241194T3 (pt)
HU (1) HU227568B1 (pt)
ID (1) ID27044A (pt)
IL (1) IL136954A0 (pt)
MY (1) MY120064A (pt)
NO (1) NO316912B1 (pt)
NZ (1) NZ505370A (pt)
PL (1) PL195682B1 (pt)
PT (1) PT1042287E (pt)
RU (1) RU2225397C2 (pt)
SI (1) SI1042287T1 (pt)
TR (1) TR200001954T2 (pt)
TW (1) TWI241294B (pt)
WO (1) WO1999033800A1 (pt)
ZA (1) ZA9811759B (pt)

Families Citing this family (75)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9716657D0 (en) 1997-08-07 1997-10-15 Zeneca Ltd Chemical compounds
ID27044A (id) * 1997-12-24 2001-02-22 Aventis Pharma Gmbh Derivatif indole sebagai penghambat pada faktor xa
GB9803226D0 (en) 1998-02-17 1998-04-08 Zeneca Ltd Chemical compounds
DE19917504A1 (de) * 1999-04-17 2000-10-19 Dresden Arzneimittel Verwendung von Hydroxyindolen, die Inhibitoren der Phosphodiesterase 4 sind, zur Therapie chronisch obstruktiver Lungenerkrankungen
KR20010089753A (ko) 1999-01-02 2001-10-08 로버트 흐라이탁, 미쉘 베스트 아릴알카노일 유도체, 이의 제조방법, 이의 용도 및 이를함유하는 약제학적 조성물
KR20010101355A (ko) 1999-01-02 2001-11-14 로버트 흐라이탁, 미쉘 베스트 신규한 말론산 유도체, 이의 제조 방법, 이의 용도 및이를 함유하는 약제학적 조성물(인자 xa 활성 억제)
GB9902455D0 (en) * 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902459D0 (en) * 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902461D0 (en) * 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902452D0 (en) * 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
AR024158A1 (es) * 1999-06-01 2002-09-04 Smithkline Beecham Corp Compuestos antibacterianos
EP1095933A1 (en) 1999-10-30 2001-05-02 Aventis Pharma Deutschland GmbH Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them
GB0000625D0 (en) 2000-01-13 2000-03-01 Zeneca Ltd Chemical compounds
EP1127884A1 (en) 2000-02-26 2001-08-29 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them
GB0005366D0 (en) * 2000-03-06 2000-04-26 Xenova Ltd Pharmaceutical compounds
US6548517B2 (en) 2000-03-24 2003-04-15 Millennium Pharmaceuticals, Inc. Oxindole inhibitors of factor Xa
US6670388B1 (en) 2000-06-27 2003-12-30 Smithkline Beecham Corporation Fatty acid synthase inhibitors
WO2002026712A2 (en) * 2000-09-29 2002-04-04 Millennium Pharmaceuticals, Inc. Quaternary amines and related inhibitors of factor xa
NZ528752A (en) 2001-06-28 2006-06-30 Pfizer Prod Inc Triamide-substituted indoles, benzofuranes and benzothiophenes as inhibitors of microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (APO B) secretion
DE10147672A1 (de) 2001-09-27 2003-04-10 Bayer Ag Substituierte 2,5-Diamidoindole und ihre Verwendung
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
US7794965B2 (en) 2002-03-13 2010-09-14 Signum Biosciences, Inc. Method of identifying modulators of PP2A methylase
AU2003302238A1 (en) 2002-12-03 2004-06-23 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
US7317027B2 (en) * 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
EP1479680A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Azaindole derivatives as Factor Xa inhibitors
EP1479677A1 (en) * 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH New indole derivatives as factor xa inhibitors
WO2004108671A1 (en) * 2003-06-06 2004-12-16 Suven Life Sciences Limited Substituted indoles with serotonin receptor affinity, process for their preparation and pharmaceutical compositions containing them
SE0302035D0 (sv) * 2003-07-09 2003-07-09 Biolipox Ab New compound
CN102875441A (zh) * 2003-07-17 2013-01-16 普莱希科公司 Ppar活性化合物
US7348338B2 (en) * 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
US7186084B2 (en) * 2003-11-19 2007-03-06 General Electric Company Hot gas path component with mesh and dimpled cooling
EP1568698A1 (en) * 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
DE602005009209D1 (de) 2004-06-18 2008-10-02 Biolipox Ab Zur behandlung von entzündungen geeignete indole
EP1765775B1 (en) * 2004-06-18 2009-04-29 Biolipox AB Indoles useful in the treatment of inflammation
KR20070029809A (ko) * 2004-06-18 2007-03-14 바이올리폭스 에이비 염증치료에 유용한 인돌
CN1972926B (zh) * 2004-06-21 2011-02-16 霍夫曼-拉罗奇有限公司 作为组胺受体拮抗剂的吲哚衍生物
CA2577608A1 (en) * 2004-09-06 2006-03-16 F. Hoffmann-La Roche Ag 4-aminomethyl benzamidine derivatives and their use as factor viia inhibitors
AU2005299693B2 (en) 2004-10-26 2012-07-05 Janssen Pharmaceutica, N.V. Factor Xa compounds
GB0428173D0 (en) * 2004-12-23 2005-01-26 Astrazeneca Ab Compounds
FR2880625B1 (fr) * 2005-01-07 2007-03-09 Sanofi Aventis Sa Derives de n-(heteroaryl)-1h-indole-2-carboxamides, leur preparation et leur application en therapeutique
EP1841735B1 (en) 2005-01-19 2011-03-09 Biolipox AB Indoles useful in the treatment of inflammation
EP1838669A1 (en) * 2005-01-19 2007-10-03 Biolipox AB Indoles useful in the treatment of inflammation
JP2008527030A (ja) * 2005-01-19 2008-07-24 バイオリポックス エービー 炎症の治療に有用なインドール類
EP1844013A1 (en) * 2005-01-19 2007-10-17 Biolipox AB Indoles useful in the treatment of inflammation
US20090069384A1 (en) * 2005-01-19 2009-03-12 Biolipox Ab Thienopyrroles useful in the treatment of inflammation
US20090048285A1 (en) * 2005-01-19 2009-02-19 Benjamin Pelcman Pyrrolopyridines Useful in the Treatment of Inflammation
EP1843734A4 (en) * 2005-02-03 2008-09-10 Signum Biosciences Inc COMPOSITIONS AND METHOD FOR INTENSIFYING COGNITIVE FUNCTIONS
US7923041B2 (en) 2005-02-03 2011-04-12 Signum Biosciences, Inc. Compositions and methods for enhancing cognitive function
EP1747779A1 (en) 2005-07-28 2007-01-31 Laboratorios Del Dr. Esteve, S.A. Tetrahydro-b-carbolin-sulfonamide derivatives as 5-HT6 ligands
EP1943245A2 (en) * 2005-09-07 2008-07-16 Plexxikon, Inc. 1,3-disubstituted indole derivatives for use as ppar modulators
US7977359B2 (en) 2005-11-04 2011-07-12 Amira Pharmaceuticals, Inc. 5-lipdxygenase-activating protein (FLAP) inhibitors
GB2431927B (en) * 2005-11-04 2010-03-17 Amira Pharmaceuticals Inc 5-Lipoxygenase-activating protein (FLAP) inhibitors
CN101316838B (zh) * 2005-11-30 2013-01-30 霍夫曼-拉罗奇有限公司 用作h3调节剂的1,1-二氧代-硫代吗啉基吲哚基甲酮衍生物
WO2008016883A2 (en) * 2006-07-31 2008-02-07 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
RU2446157C2 (ru) * 2006-09-13 2012-03-27 Санофи-Авентис Изосериновые производные для применения в качестве ингибиторов фактора свертывания крови ixa
EP2079466B1 (en) * 2006-09-29 2014-01-15 GlaxoSmithKline LLC Substituted indole compounds
MX2009004898A (es) 2006-11-09 2009-05-19 Hoffmann La Roche Derivados de indol y de benzofurano-2-carboxamida.
US8524917B2 (en) * 2007-01-11 2013-09-03 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
PE20090159A1 (es) * 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
CN101778850A (zh) * 2007-08-10 2010-07-14 H.隆德贝克有限公司 杂芳基酰胺类似物
US9486441B2 (en) 2008-04-21 2016-11-08 Signum Biosciences, Inc. Compounds, compositions and methods for making the same
CN101654427B (zh) * 2008-08-19 2012-12-05 信谊药厂 抗凝化合物、组合物及其用途
US8546431B2 (en) 2008-10-01 2013-10-01 Panmira Pharmaceuticals, Llc 5-lipoxygenase-activating protein (FLAP) inhibitors
WO2011044134A1 (en) 2009-10-05 2011-04-14 Albany Molecular Research, Inc. Epiminocycloalkyl(b)indole derivatives as serotonin sub-type 6 (5-ht6) modulators and uses thereof
MX2012006913A (es) 2009-12-18 2012-08-23 Activesite Pharmaceuticals Inc Profarmacos de inhibidores de calicreina plasmatica.
US9206123B2 (en) 2009-12-18 2015-12-08 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
US9067949B2 (en) 2011-01-19 2015-06-30 Albany Molecular Research, Inc. Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-HT6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia
US9353113B2 (en) 2011-03-18 2016-05-31 Ono Pharmaceutical Co., Ltd. Tetrahydrocarboline derivative
US8691861B2 (en) 2011-04-13 2014-04-08 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
US20190016680A1 (en) 2016-01-14 2019-01-17 Beth Israel Deaconess Medical Center, Inc. Mast-cell modulators and uses thereof
ES2910787T3 (es) 2016-05-12 2022-05-13 Univ Michigan Regents Inhibidores de ASH1L y métodos de tratamiento con los mismos
CN111542318A (zh) * 2017-11-10 2020-08-14 密歇根大学董事会 Ash1l降解剂及用其进行治疗的方法
US12478610B2 (en) 2020-05-11 2025-11-25 Orit MALKA Compositions of tryptophol derivatives and 4-ethyl-phenol derivatives, and methods of using same
WO2023068700A1 (ko) * 2021-10-20 2023-04-27 동국대학교 와이즈캠퍼스 산학협력단 두룸아마이드 a를 포함하는 혈소판 응집 예방, 개선 또는 치료용 조성물

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US997638A (en) * 1910-08-13 1911-07-11 Eugene Rynearson Pavement-breaking machine.
US4529724A (en) * 1983-10-11 1985-07-16 Mcneilab, Inc. 6H-indolo[2,1-c][1,4]benzodiazepines and 12-oxo derivatives useful as antihypertensives
DD235866B1 (de) 1985-03-29 1988-12-28 Univ Leipzig Verfahren zur herstellung von n alpha (2-naphthyl)-sulfonylaminoacylierten amidinophenylalanisamiden
EP0639573A1 (de) * 1993-08-03 1995-02-22 Hoechst Aktiengesellschaft Benzokondensierte 5-Ringheterocyclen, Verfahren zu ihrer Herstellung, ihre Verwendung als Medikament, ihre Verwendung als Diagnostikum, sowie sie enthaltendes Medikament
DE69532754T2 (de) 1994-04-26 2005-03-10 Aventis Pharmaceuticals, Inc. Faktor xa inhibitoren
US5612363A (en) * 1995-06-02 1997-03-18 Berlex Laboratories, Inc. N,N-di(aryl) cyclic urea derivatives as anti-coagulants
DE19530996A1 (de) 1995-08-23 1997-02-27 Boehringer Mannheim Gmbh Cyclische Guanidine, Verfahren zu ihrer Herstellung und Arzneimittel
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
AU2056197A (en) * 1996-02-22 1997-09-10 Du Pont Merck Pharmaceutical Company, The M-amidino phenyl analogs as factor xa inhibitors
US6200969B1 (en) * 1996-09-12 2001-03-13 Idun Pharmaceuticals, Inc. Inhibition of apoptosis using interleukin-1β-converting enzyme (ICE)/CED-3 family inhibitors
US6184244B1 (en) * 1996-12-16 2001-02-06 Idun Pharmaceuticals, Inc. C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US5886191A (en) * 1997-08-18 1999-03-23 Dupont Pharmaceuticals Company Amidinoindoles, amidinoazoles, and analogs thereof
ID27044A (id) * 1997-12-24 2001-02-22 Aventis Pharma Gmbh Derivatif indole sebagai penghambat pada faktor xa

Also Published As

Publication number Publication date
CN1220681C (zh) 2005-09-28
PT1042287E (pt) 2005-08-31
HU227568B1 (en) 2011-08-29
CZ20002310A3 (cs) 2000-10-11
NO20003057D0 (no) 2000-06-14
SI1042287T1 (en) 2005-10-31
CN1283186A (zh) 2001-02-07
AU743881B2 (en) 2002-02-07
CA2316172C (en) 2010-02-02
DK1042287T3 (da) 2005-08-15
EP1042287A1 (en) 2000-10-11
US6337344B1 (en) 2002-01-08
ZA9811759B (en) 1999-07-28
EP1042287B1 (en) 2005-04-20
HUP0100723A3 (en) 2002-12-28
DE69829879D1 (de) 2005-05-25
KR100608472B1 (ko) 2006-08-09
PL195682B1 (pl) 2007-10-31
HK1033795A1 (en) 2001-09-21
ATE293599T1 (de) 2005-05-15
RU2225397C2 (ru) 2004-03-10
TR200001954T2 (tr) 2000-12-21
WO1999033800A1 (en) 1999-07-08
AR018031A1 (es) 2001-10-31
HUP0100723A2 (hu) 2001-08-28
NO20003057L (no) 2000-08-18
PL341400A1 (en) 2001-04-09
JP4589529B2 (ja) 2010-12-01
DE69829879T2 (de) 2006-03-02
IL136954A0 (en) 2001-06-14
KR20010033573A (ko) 2001-04-25
MY120064A (en) 2005-08-30
NO316912B1 (no) 2004-06-21
NZ505370A (en) 2002-06-28
CA2316172A1 (en) 1999-07-08
ID27044A (id) 2001-02-22
BR9814340B1 (pt) 2010-07-13
ES2241194T3 (es) 2005-10-16
AU2052899A (en) 1999-07-19
TWI241294B (en) 2005-10-11
CZ298827B6 (cs) 2008-02-20
JP2001527066A (ja) 2001-12-25

Similar Documents

Publication Publication Date Title
BR9814340A (pt) Derivados de indol como inibidores de fator xa
BR9916732A (pt) Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa)
BR0108694A (pt) Derivados de ácido malÈnico, processo para preparação dos mesmos, uso dos mesmos como inibidor de atividade do fator xa e composições farmacêuticas que contêm os mesmos
BR9810592A (pt) Composto, processos para preparar um composto, para tratar ou prevenir doenças do sistema endócrino e para a fabricação de um medicamento, composição farmacêutica, e, uso de um composto
BR9806060A (pt) Composto, composição farmacêutica e processos para tratar um paciente sofrendo de um estado doentio, para inibir o fator xa, e, para inibir a formação de trombina.
BR9916980A (pt) Derivados bicìclicos substituìdos úteis como agentes anticancerìgenos
BR9908275A (pt) Inibidores de enzimas fosfolipase
RU95110938A (ru) Производные 1-(2-оксоацетил)пиперидин-2-карбоновых кислот, фармацевтическая композиция, способ лечения, способ получения
BR9800228A (pt) Compostos de peridilfurano e piridiltiofeno
BR9911488A (pt) Composto, uso do mesmo, composição farmacêutica, e, processos para tratamento ou de profilaxia de doenças inflamatórias, e para a preparação de um composto
BR0007589A (pt) Inibidores da proliferação de células
BR9812095A (pt) Compostos de indol como inibidores de cox-2
BR9910573A (pt) Compostos antipicornavirais, preparação e uso dos mesmos
BR9911013A (pt) Derivados de pirazol como inibidores da p-38 map quinase
BR0010520A (pt) Novos compostos farmaceuticamente ativos
BR9912612A (pt) Composto de maleimida dissubstituìdo e seu usofarmacêutico
BR9713921A (pt) Composto, composição farmacêutica, processo para tógico capaz de ser modulado através da inibição do fator xa
BR9916669A (pt) Uso de derivados de ácidos 4-biarilbutìricos e 5-biarilpentanóicos substituìdos como inibidores de metaloproteases de matriz para o tratamento de doenças respiratórias
BR9712707A (pt) Derivados de ácido 4-bifenil-4-hidroxibutìrico substituìdo com inibidores de metaloprotease de matriz
BR0309014A (pt) ácido(2-((2-alcóxi)-fenil)-ciclopent-1-enil)carbo e heterocìclico aromático e derivados
BR9916733A (pt) Derivados de arilalcanoìla, processos para sua preparação, seu uso e composições farmacêuticas que os contêm
NO983444D0 (no) Benzo(c)kinolizin derivater, deres fremstilling og anvendelse som 5&lt;alfa&gt;-reduktaseinhibitorer
DK0966462T3 (da) Heterocykliske forbindelser, der er egnede som oxidosqualencyklaseinhibitorer
BR0013306A (pt) Processos úteis na sìntese de compostos antipicornavirais
NO992009L (no) Nye trans-3,4-kromanderivater som kan anvendes ved forhindring eller behandling av °strogenrelaterte sykdommer eller syndromer

Legal Events

Date Code Title Description
B25D Requested change of name of applicant approved

Owner name: SANOFI-AVENTIS DEUTSCHLAND GMBH (DE)

Free format text: ALTERADO DE: AVENTIS PHARMA DEUTSCHLAND GMBH

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 13/07/2010, OBSERVADAS AS CONDICOES LEGAIS.

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 16A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2284 DE 14-10-2014 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.