BR9916363A - Composto, composição farmacêutica e método paratratar ou prevenir um distúrbio tromboembólico - Google Patents

Composto, composição farmacêutica e método paratratar ou prevenir um distúrbio tromboembólico

Info

Publication number
BR9916363A
BR9916363A BR9916363-2A BR9916363A BR9916363A BR 9916363 A BR9916363 A BR 9916363A BR 9916363 A BR9916363 A BR 9916363A BR 9916363 A BR9916363 A BR 9916363A
Authority
BR
Brazil
Prior art keywords
compound
pharmaceutical composition
treat
prevent
compounds
Prior art date
Application number
BR9916363-2A
Other languages
English (en)
Inventor
Darin Arthur Allen
Jason M Hataye
Witold N Hruzewicz
Leksandr Kolesnikov
Richard Laurence Mackman
Roopa Rai
Effrey R Spencer
Erik J Verner
Wendy B Young
Williamdvorak Shrader
Original Assignee
Axys Pharm 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.)
Filing date
Publication date
Application filed by Axys Pharm Inc filed Critical Axys Pharm Inc
Publication of BR9916363A publication Critical patent/BR9916363A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 aromatic rings
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • 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
    • 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
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/20—Two benzimidazolyl-2 radicals linked together directly or via a hydrocarbon or substituted hydrocarbon radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

Landscapes

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

Abstract

"COMPOSTO, COMPOSIçãO FARMACêUTICA E MéTODOPARA TRATAR OU PREVENIR UM DISTúRBIOTROMBOEMBóLICO" A presente invenção fornece novoscompostos da Fórmula (I): A-B. suas formas pró-medicamentos, ouseus sais farmaceuticamente aceitáveis, em que A representa umaestrutura de anel heterocíclico bicíclico saturado, insaturado ouparcialmente insaturado, e B representa um grupo arila ou umheteroarila. Compostos preferidos da presente invençãocompreendem um núcleo de benzimidazol ou de indol. Oscompostos desta invenção são inibidores das serina proteases,Urocinase (uPA), Fator Xa (FXa),e/ou Fator VIIa (FVIIa), e têmutilidade como agentes anti-câncer e/ou como anticoagulantespara o tratamento ou prevenção de distúrbios tromboembólicos emmamíferos.
BR9916363-2A 1998-12-18 1999-12-17 Composto, composição farmacêutica e método paratratar ou prevenir um distúrbio tromboembólico BR9916363A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US11300798P 1998-12-18 1998-12-18
PCT/US1999/030302 WO2000035886A2 (en) 1998-12-18 1999-12-17 (hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors

Publications (1)

Publication Number Publication Date
BR9916363A true BR9916363A (pt) 2001-12-11

Family

ID=22347074

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9916363-2A BR9916363A (pt) 1998-12-18 1999-12-17 Composto, composição farmacêutica e método paratratar ou prevenir um distúrbio tromboembólico

Country Status (20)

Country Link
US (1) US6867200B1 (pt)
EP (1) EP1140859A2 (pt)
JP (1) JP2002532479A (pt)
KR (1) KR20010086119A (pt)
CN (1) CN1344256A (pt)
AU (1) AU779117B2 (pt)
BR (1) BR9916363A (pt)
CA (1) CA2355249A1 (pt)
CZ (1) CZ20012006A3 (pt)
EA (1) EA200100675A1 (pt)
EE (1) EE200100323A (pt)
HU (1) HUP0104987A3 (pt)
IL (1) IL143801A0 (pt)
NO (1) NO20012980L (pt)
NZ (1) NZ512375A (pt)
PL (1) PL349192A1 (pt)
SK (1) SK7972001A3 (pt)
TR (1) TR200102533T2 (pt)
UA (1) UA70976C2 (pt)
WO (1) WO2000035886A2 (pt)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60128475T2 (de) * 2000-07-25 2008-02-07 Merck & Co., Inc. N-substituierte indole mit anwendung in der behandlung von diabetes
US6465503B2 (en) * 2000-08-11 2002-10-15 Axys Pharmaceuticals, Inc. Selective urokinase inhibitors
WO2002062829A1 (fr) 2001-02-02 2002-08-15 Chugai Seiyaku Kabushiki Kaisha Derives de peptide
SE0100902D0 (sv) 2001-03-15 2001-03-15 Astrazeneca Ab Compounds
JP2004535411A (ja) 2001-05-25 2004-11-25 ブリストルーマイヤーズ スクイブ カンパニー マトリックスメタロプロテナーゼ及び／またはＴＮＦ−α転換酵素（ＴＡＣＥ）の阻害剤としてのヒダントイン及び関連複素環化合物
CA2452391A1 (en) * 2001-07-09 2003-01-23 Axys Pharmaceuticals, Inc. 2-[5-(5-carbamimidoyl-1h-heteroaryl)-6-hydroxybiphenyl-3-yl]-succinic acid derivatives as factor viia inhibitors
PL366799A1 (en) 2001-07-27 2005-02-07 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
WO2003015715A2 (en) * 2001-08-20 2003-02-27 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives as antithrombotic agents
SE0103710D0 (sv) 2001-11-07 2001-11-07 Astrazeneca Ab Compounds
EP1474400A1 (en) * 2002-02-13 2004-11-10 Axys Pharmaceuticals, Inc. 2-[5-(5-carbamimidoyl-1h-heteroaryl)] -6-hydroxybiphenyl-3-yl derivatives as factor viia inhibitors
US6867320B2 (en) 2002-02-21 2005-03-15 Asahi Kasei Pharma Corporation Substituted phenylalkanoic acid derivatives and use thereof
WO2003080545A2 (en) 2002-03-20 2003-10-02 Metabolex, Inc. Substituted phenylacetic acids
WO2004010996A1 (ja) * 2002-07-29 2004-02-05 Shizuoka Coffein Co., Ltd. 1,3アゾール誘導体及び同誘導体を含む血栓症治療のための医薬組成物
SE0202539D0 (sv) * 2002-08-27 2002-08-27 Astrazeneca Ab Compounds
JP4377815B2 (ja) 2002-08-29 2009-12-02 メルク エンド カムパニー インコーポレーテッド 抗糖尿病活性を有するインドール類
CN100513398C (zh) 2002-12-03 2009-07-15 Axys药物公司 作为因子viia抑制剂的2-(2-羟基联苯-3-基)-1h-苯并咪唑-5-甲脒衍生物
WO2004062661A1 (en) * 2003-01-08 2004-07-29 Axys Pharmaceuticals, Inc. 2-‘5-(5-carbamimidoyl-1h-heteroaryl)-6-hydroxybiphenyl-3-yl!- carboxylic acid derivatives as factor viia inhibitors
ES2295816T3 (es) 2003-01-14 2008-04-16 Arena Pharmaceuticals, Inc. Derivados arilo y heteroarilo 1,2,3-trisustituidos como moduladores del metabolismo, y profilaxis y tratamiento de transtornos relacionados con los mismos, tales como la diabetes y la hiperglucemia.
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US7199259B2 (en) 2003-06-20 2007-04-03 Metabolex, Inc. Resolution of α-(phenoxy)phenylacetic acid derivatives
AU2004265191A1 (en) 2003-08-14 2005-02-24 Asahi Kasei Pharma Corporation Substituted arylalkanoic acid derivative and use thereof
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
CA2567437A1 (en) 2004-05-25 2005-12-08 Metabolex, Inc. Substituted triazoles as modulators of ppar and methods of their preparation
US8729117B2 (en) 2004-06-02 2014-05-20 Pharmacyclics, Inc. Factor VIIa inhibitor
KR100977903B1 (ko) * 2004-06-02 2010-08-24 파마시클릭스, 인코포레이티드 Ⅶａ 인자 억제제
EP1751114A2 (en) * 2004-06-02 2007-02-14 Pharmacyclics, Inc. Factor viia inhibitor
US7648992B2 (en) 2004-07-05 2010-01-19 Astrazeneca Ab Hydantoin derivatives for the treatment of obstructive airway diseases
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US8048909B2 (en) * 2004-09-30 2011-11-01 Takeda Pharmaceutical Company Limited Proton pump inhibitors
SE0403085D0 (sv) 2004-12-17 2004-12-17 Astrazeneca Ab Novel componds
SE0403086D0 (sv) 2004-12-17 2004-12-17 Astrazeneca Ab Compounds
US7714131B2 (en) 2005-09-23 2010-05-11 Metabolex, Inc. Process for the stereoselective preparation of (−)-halofenate and derivatives thereof
AU2006311914C1 (en) * 2005-11-03 2013-10-24 Chembridge Corporation Heterocyclic compounds as tyrosine kinase modulators
WO2007114213A1 (ja) 2006-03-30 2007-10-11 Asahi Kasei Pharma Corporation 置換二環式環状誘導体及びその用途
ES2422603T3 (es) 2007-05-31 2013-09-12 Shionogi & Co Compuestos oxiimino y el uso de estos
US20100215837A1 (en) * 2007-06-19 2010-08-26 Rhodri Evans Process for making an electrode, an electrode and a battery comprising the electrode
EP2586794A3 (en) 2007-10-16 2013-07-17 Pharmacyclics, Inc. Manufacture, Compositions and Uses of Coagulationfactor VIIA Modulator
JP5198560B2 (ja) 2008-04-28 2013-05-15 旭化成ファーマ株式会社 フェニルプロピオン酸誘導体及びその用途
EP2346820B1 (en) 2008-06-11 2013-02-13 Shionogi & Co., Ltd. Oxycarbamoyl compounds and the use thereof
AR072297A1 (es) 2008-06-27 2010-08-18 Novartis Ag Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona.
CN101654427B (zh) * 2008-08-19 2012-12-05 信谊药厂 抗凝化合物、组合物及其用途
KR101354418B1 (ko) * 2009-07-30 2014-01-23 단국대학교 산학협력단 형광 탐지자 및 이의 제조 방법
WO2012040279A1 (en) 2010-09-22 2012-03-29 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
TWI501967B (zh) 2010-12-16 2015-10-01 Janssen R&D Ireland 作為呼吸道融合病毒抗病毒劑之氮雜吲哚類
TWI527814B (zh) 2010-12-16 2016-04-01 健生科學愛爾蘭無限公司 作為呼吸道融合病毒抗病毒劑之氮雜苯并咪唑類
TWI515187B (zh) 2010-12-16 2016-01-01 健生科學愛爾蘭無限公司 作為呼吸道融合病毒抗病毒劑之吲哚類
TWI541241B (zh) * 2010-12-16 2016-07-11 健生科學愛爾蘭無限公司 作為呼吸道融合病毒抗病毒劑之咪唑并吡啶類
CN103561573A (zh) * 2011-04-26 2014-02-05 印第安纳大学研究与技术公司 酪氨酸磷酸酶及其在调节参与结核分枝杆菌之病理学的酶的活性中的用途
PT2864323T (pt) 2012-06-15 2017-07-14 Janssen Sciences Ireland Uc Derivados de 1,3-di-hidro-2h-benzimidazol-2-ona substituídos com heterociclos como agentes antivirais do vírus sincicial respiratório
EP2977374A1 (en) 2014-07-21 2016-01-27 Université de Strasbourg Molecules presenting dual emission properties
AU2015324313B2 (en) * 2014-09-30 2018-11-15 Transitions Optical, Inc. Ultraviolet light absorbers
NZ734220A (en) 2015-01-06 2022-01-28 Arena Pharm Inc Methods of treating conditions related to the s1p1 receptor
PE20180572A1 (es) 2015-06-18 2018-04-04 Cephalon Inc Derivados de piperidina 1,4-sustituidos
ES2849951T3 (es) 2015-06-18 2021-08-24 89Bio Ltd Derivados de piperidina 4-bencil y 4-benzoil sustituidos
MA42807A (fr) 2015-06-22 2018-07-25 Arena Pharm Inc Sel l-arginine cristallin d'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclo-penta[b]indol-3-yl)acétique (composé 1) pour une utilisation dans des troubles associés au récepteur de s1p1
TW201718581A (zh) 2015-10-19 2017-06-01 英塞特公司 作為免疫調節劑之雜環化合物
KR102547771B1 (ko) * 2015-11-09 2023-06-26 고려대학교 산학협력단 4-치환된-2-(5-치환된-1h-인돌-2-일)페놀 유도체, 그 제조방법 및 이를 포함하는 세포 증식 및 전이 억제용 약학 조성물
ES2928856T3 (es) 2015-11-19 2022-11-23 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
UA126113C2 (uk) 2015-12-22 2022-08-17 Інсайт Корпорейшн Гетероциклічні сполуки як імуномодулятори
WO2017192961A1 (en) * 2016-05-06 2017-11-09 Incyte Corporation Heterocyclic compounds as immunomodulators
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
CN105884673B (zh) * 2016-06-03 2018-05-11 温州大学 一种吲哚衍生物的合成方法
WO2017222976A1 (en) 2016-06-20 2017-12-28 Incyte Corporation Heterocyclic compounds as immunomodulators
US10071079B2 (en) 2016-06-29 2018-09-11 Bristol-Myers Squibb Company [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
WO2018013789A1 (en) 2016-07-14 2018-01-18 Incyte Corporation Heterocyclic compounds as immunomodulators
CA3031675A1 (en) 2016-07-30 2018-02-08 Bristol-Myers Squibb Company Dimethoxyphenyl substituted indole compounds as tlr7, tlr8 or tlr9 inhibitors
MA46045A (fr) 2016-08-29 2021-04-28 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
KR102519535B1 (ko) 2016-09-09 2023-04-06 브리스톨-마이어스 스큅 컴퍼니 피리딜 치환된 인돌 화합물
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
BR112019012957A2 (pt) 2016-12-22 2019-11-26 Incyte Corp derivados de tetra-hidroimidazo[4,5-c]piridina como indutores de internalização de pd-l1
US20180179179A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Heterocyclic compounds as immunomodulators
AU2017382870B2 (en) 2016-12-22 2022-03-24 Incyte Corporation Benzooxazole derivatives as immunomodulators
KR20190116416A (ko) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. 원발 담즙성 담관염을 치료하기 위한 화합물 및 방법
US11130756B2 (en) 2017-08-04 2021-09-28 Bristol-Myers Squibb Company [1,2,4]Triazolo[4,3-A]pyridinyl substituted indole compounds
KR102651947B1 (ko) 2017-08-04 2024-03-26 브리스톨-마이어스 스큅 컴퍼니 Tlr7/8/9의 억제제로서 유용한 치환된 인돌 화합물
JP7265554B2 (ja) 2017-11-14 2023-04-26 ブリストル－マイヤーズ スクイブ カンパニー 置換インドール化合物
CN111819176B (zh) 2017-12-18 2023-12-15 百时美施贵宝公司 4-氮杂吲哚化合物
AU2018390543A1 (en) 2017-12-19 2020-08-06 Bristol-Myers Squibb Company 6-azaindole compounds
WO2019126113A1 (en) 2017-12-19 2019-06-27 Bristol-Myers Squibb Company Substituted indole compounds useful as tlr inhibitors
MX2020005515A (es) 2017-12-19 2020-09-03 Bristol Myers Squibb Co Compuestos de indol sustituidos con amida, utiles como inhibidores de receptores de tipo toll (tlr).
AU2018390544A1 (en) 2017-12-20 2020-08-06 Bristol-Myers Squibb Company Diazaindole compounds
CA3085942A1 (en) 2017-12-20 2019-06-27 Bristol-Myers Squibb Company Aryl and heteroaryl substituted indole compounds
CA3086431A1 (en) 2017-12-20 2019-06-27 Bristol-Myers Squibb Company Amino indole compounds useful as tlr inhibitors
SI3774791T1 (sl) 2018-03-30 2023-04-28 Incyte Corporation Heterociklične spojine kot imunomodulatorji
DK3790877T3 (da) 2018-05-11 2023-04-24 Incyte Corp Tetrahydro-imidazo[4,5-c]pyridinderivater som pd-l1-immunmodulatorer
ES2963696T3 (es) 2018-10-24 2024-04-01 Bristol Myers Squibb Co Compuestos diméricos de indol sustituidos
CA3150434A1 (en) 2019-08-09 2021-02-18 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
BR112022005826A2 (pt) 2019-09-30 2022-06-21 Incyte Corp Compostos de pirido[3,2-d]pirimidina como imunomoduladores
MX2022005651A (es) 2019-11-11 2022-07-27 Incyte Corp Sales y formas cristalinas de un inhibidor de la proteina de muerte celular programada 1 (pd-1)/ligando de muerte celular programada 1 (pd-l1).
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
JP2023548859A (ja) 2020-11-06 2023-11-21 インサイト・コーポレイション Ｐｄ－１／ｐｄ－ｌ１阻害剤ならびにその塩及び結晶形態を作製するためのプロセス
CN117430525A (zh) * 2023-03-01 2024-01-23 中化学科学技术研究有限公司 席夫碱配体及其制备方法和应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3224512A1 (de) 1982-07-01 1984-01-05 Dr. Karl Thomae Gmbh, 7950 Biberach Neue imidazolderivate, ihre herstellung und diese verbindungen enthaltende arzneimittel
JPS63166588A (ja) * 1986-12-27 1988-07-09 Kanzaki Paper Mfg Co Ltd クロメノ化合物およびクロメノ化合物を用いた感熱記録体
JP2869561B2 (ja) * 1989-05-22 1999-03-10 大塚製薬株式会社 血小板粘着抑制剤
US6255091B1 (en) * 1995-04-28 2001-07-03 Axys Pharmaceuticals, Inc. Potentiating metal mediated serine protease inhibitors with cobalt or zinc ions
WO1999026933A1 (en) 1997-11-26 1999-06-03 Axys Pharmaceuticals, Inc. Substituted amidinoaryl derivatives and their use as anticoagulants
US6150379A (en) 1997-11-26 2000-11-21 Axys Pharmaceuticals, Inc. Compounds and compositions as anticoagulants

Also Published As

Publication number Publication date
UA70976C2 (uk) 2004-11-15
EE200100323A (et) 2002-08-15
EP1140859A2 (en) 2001-10-10
WO2000035886A2 (en) 2000-06-22
US6867200B1 (en) 2005-03-15
CA2355249A1 (en) 2000-06-22
CZ20012006A3 (cs) 2002-03-13
HUP0104987A3 (en) 2002-09-30
NO20012980L (no) 2001-08-01
HUP0104987A2 (hu) 2002-07-29
EA200100675A1 (ru) 2001-12-24
KR20010086119A (ko) 2001-09-07
SK7972001A3 (en) 2002-06-04
IL143801A0 (en) 2002-04-21
AU2711500A (en) 2000-07-03
JP2002532479A (ja) 2002-10-02
NO20012980D0 (no) 2001-06-15
NZ512375A (en) 2003-11-28
CN1344256A (zh) 2002-04-10
AU779117B2 (en) 2005-01-06
PL349192A1 (en) 2002-07-01
TR200102533T2 (tr) 2006-06-21
WO2000035886A3 (en) 2000-10-26

Similar Documents

Publication Publication Date Title
BR9916363A (pt) Composto, composição farmacêutica e método paratratar ou prevenir um distúrbio tromboembólico
DE60132975D1 (de) Neue substanzen und verbindungen als protease-inhibitoren
TR200001279T2 (tr) Poli (ADP-riboz) polimeraz ("PARP") inhibitörleri, nevral ve kardiyovasküler doku hasarının tedavisi için yöntemler ve farmasötik bileşimler.
NO990433L (no) Nye forbindelser og blandinger for behandling av sykdommer i forbindelse med tryptase-aktivitet
NO20060974L (no) Pyridazinderivater og deres anvendelse som terapeutiske midler
DE60324183D1 (en) Aryl-, aryloxy- und alkyloxysubstituierte 1h-indol-3-yl-glyoxylsäurederivateals inhibitoren des plasminogenaktivatorinhibitors-1 (pai-1)
BR0009167A (pt) Inibidores de enzima impdh
GEP20022676B (en) 4-Phenyl-Pyridine Derivatives, Method for Their Production and Their Use for Treatment of Disorders Caused by Antagonist of NK-1 Receptors
EE200100487A (et) Uudsed ühendid ja kompositsioonid proteaasiinhibiitoritena
TR200201505T2 (tr) Terapötik maddeler olarak pirazolopirimidinler
ECSP045115A (es) INDOL-2-CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
BR9810841A (pt) Inibidores de metaloprotease alicìclicos
BR0007424A (pt) Composto, composição farmacêutica, método para o tratamento de depressão em um paciente necessitando do mesmo, e, processo para a preparação de um composto
NO20014529D0 (no) Tetrahydropyranderivater og deres anvendelse som terapautiske midler
ES2136252T3 (es) Tratamiento de enfermedades causadas por trastornos de la glandula sebacea mediante el uso de inhibidores de acil coa colesterol acil transferasa.
ID24228A (id) (+)norcisaprida yang berguna untuk gangguan tertular 5-ht3 dan 5-ht4
DK1458393T3 (da) Substituerede diketopiperaziner som oxytocinantagonister
NO20050279D0 (no) Ny fremgangsmate
ATE342264T1 (de) Indolderivate und deren verwendung als gnrh antagonisten
DK1226819T3 (da) Inhibitor for 20-HETE-producerende enzym
SE0002353D0 (sv) New use
ATE293602T1 (de) 2-aminopyridine als inhibitoren von cyclooxygenase-2
DE69910706D1 (de) Medikament zur Behandlung von Glaukoma und ischämischer Retinopathie
DK1343523T3 (da) Anvendelse af aktiveret faktor VII til behandling af thrombolytisk terapi-inducerede alvorlige blödninger
BR0211847A (pt) Composto ou um derivado farmaceuticamente aceitável do mesmo, formulação farmacêutica, uso do composto ou do derivado, métodos para tratar uma condição onde a inibição de trombina é requerida, e para tratar uma condição onde a terapia anticoagulante é indicada, e, processo para a preparação de um composto

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A E 8A ANUIDADES.

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 PUBLICADO NA RPI 1962 DE 12/08/2008.