AU3645697A - Amidinoindoles, amidinoazoles, and analogs thereof as inhibitors of factor xa and of thrombin - Google Patents

Amidinoindoles, amidinoazoles, and analogs thereof as inhibitors of factor xa and of thrombin

Info

Publication number
AU3645697A
AU3645697A AU36456/97A AU3645697A AU3645697A AU 3645697 A AU3645697 A AU 3645697A AU 36456/97 A AU36456/97 A AU 36456/97A AU 3645697 A AU3645697 A AU 3645697A AU 3645697 A AU3645697 A AU 3645697A
Authority
AU
Australia
Prior art keywords
amidinoazoles
amidinoindoles
thrombin
analogs
inhibitors
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
AU36456/97A
Inventor
Celia Dominguez
Daniel Emmett Duffy
Qi n Han
Jeongsook Maria Park
Mimi Lifen Quan
Karen Anita Rossi
Ruth Richmond Wexler
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Pharma Co
Original Assignee
DuPont Merck Pharmaceutical Co
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 DuPont Merck Pharmaceutical Co filed Critical DuPont Merck Pharmaceutical Co
Publication of AU3645697A publication Critical patent/AU3645697A/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/58—Radicals substituted by nitrogen atoms
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D401/06—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 only aliphatic carbon atoms
    • 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
    • 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
    • C07D463/00—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D463/02—Preparation
    • C07D463/06—Preparation from compounds already containing the ring or condensed ring systems, e.g. by dehydrogenation of the ring, by introduction, elimination or modification of substituents
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU36456/97A 1996-07-08 1997-06-30 Amidinoindoles, amidinoazoles, and analogs thereof as inhibitors of factor xa and of thrombin Abandoned AU3645697A (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US67676696A 1996-07-08 1996-07-08
US08676766 1996-07-08
US4951997P 1997-06-13 1997-06-13
US60049519 1997-06-13
PCT/US1997/011325 WO1998001428A1 (en) 1996-07-08 1997-06-30 AMIDINOINDOLES, AMIDINOAZOLES, AND ANALOGS THEREOF AS INHIBITORS OF FACTOR Xa AND OF THROMBIN

Publications (1)

Publication Number Publication Date
AU3645697A true AU3645697A (en) 1998-02-02

Family

ID=26727252

Family Applications (1)

Application Number Title Priority Date Filing Date
AU36456/97A Abandoned AU3645697A (en) 1996-07-08 1997-06-30 Amidinoindoles, amidinoazoles, and analogs thereof as inhibitors of factor xa and of thrombin

Country Status (7)

Country Link
EP (1) EP0960102A1 (en)
JP (1) JP2002514162A (en)
AU (1) AU3645697A (en)
CA (1) CA2259573A1 (en)
IL (1) IL127873A0 (en)
NZ (1) NZ333696A (en)
WO (1) WO1998001428A1 (en)

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EP1030844A1 (en) * 1997-11-10 2000-08-30 Array Biopharma Inc. Compounds which inhibit tryptase activity
US6221914B1 (en) * 1997-11-10 2001-04-24 Array Biopharma Inc. Sulfonamide bridging compounds that inhibit tryptase activity
WO1999026932A1 (en) * 1997-11-26 1999-06-03 Axys Pharmaceuticals, Inc. By amidino group substituted heterocyclic derivatives and their use as anticoagulants
AU1608399A (en) * 1997-11-26 1999-06-15 Axys Pharmaceuticals, Inc. Substituted amidinoaryl derivatives and their use as anticoagulants
DE19753522A1 (en) * 1997-12-03 1999-06-10 Boehringer Ingelheim Pharma Substituted indoles, their preparation and their use as pharmaceuticals
JP2002509923A (en) * 1998-03-31 2002-04-02 ワーナー−ランバート・カンパニー Quinoxalinones as serine protease inhibitors such as factor Xa and thrombin
TWI248435B (en) * 1998-07-04 2006-02-01 Boehringer Ingelheim Pharma Benzimidazoles, the preparation thereof and their use as pharmaceutical compositions
US6248770B1 (en) 1998-07-09 2001-06-19 Boehringer Ingelheim Pharma Kg Benzimidazoles having antithrombotic activity
DE19845153A1 (en) * 1998-10-01 2000-04-06 Merck Patent Gmbh Imidazo [4,5] pyridin-4-one derivatives
US6362216B1 (en) 1998-10-27 2002-03-26 Array Biopharma Inc. Compounds which inhibit tryptase activity
CA2320730A1 (en) * 1998-12-23 2000-07-06 Renhua Li Thrombin or factor xa inhibitors
KR20010086461A (en) 1998-12-24 2001-09-12 오흘러 로스 제이. Substituted (aminoiminomethyl or aminomethyl)benzoheteroaryl compounds as factor XA inhibitors
TW200404789A (en) 1999-03-15 2004-04-01 Axys Pharm Inc Novel compounds and compositions as protease inhibitors
CA2374820A1 (en) * 1999-05-24 2000-11-30 Cor Therapeutics, Inc. Inhibitors of factor xa
AU6762400A (en) * 1999-08-12 2001-03-13 Cor Therapeutics, Inc. Inhibitors of factor xa
DE60024120T2 (en) * 1999-08-26 2006-07-27 Aventis Pharmaceuticals Inc. SUBSTITUTED (AMINOIMINOMETHYL OR AMINOMETHYL) DIHYDROBENZOFURANE AND BENOZOPYRANE
GB9924155D0 (en) * 1999-10-12 1999-12-15 Rhone Poulenc Rorer Pharma Chemical compounds
US7361663B2 (en) 1999-11-10 2008-04-22 Aventis Pharmaceuticals Inc. N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
MXPA02003802A (en) * 1999-11-10 2002-09-30 Aventis Pharma Gmbh N acylpyrrolidin 2 ylalkylbenzamidine derivatives as inhibitors of factor xa.
US6451832B2 (en) 1999-12-23 2002-09-17 Boehringer Ingelheim Pharma Kg Benzimidazoles with antithrombotic activity
AU2002211828A1 (en) * 2000-10-02 2002-04-15 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
JP2004523506A (en) 2000-12-22 2004-08-05 アクシス・ファーマシューティカルズ・インコーポレイテッド Novel compounds and compositions as cathepsin inhibitors
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
WO2003024924A1 (en) 2001-09-14 2003-03-27 Aventis Pharmaceuticals Inc. Novel compounds and compositions as cathepsin inhibitors
IL161950A0 (en) 2001-11-14 2005-11-20 Axys Pharm Inc Oligopeptides and compositions containing them as cathepsin s inhibitors
KR100714519B1 (en) 2002-03-07 2007-05-07 에프. 호프만-라 로슈 아게 Bicyclic pyridine and pyrimidine p38 kinase inhibitors
US7479502B2 (en) 2002-12-03 2009-01-20 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors
CN1729174B (en) * 2002-12-20 2015-10-21 西巴特殊化学品控股有限公司 The synthesis of amine and the intermediate for the synthesis of amine
TW200508197A (en) 2003-03-31 2005-03-01 Ucb Sa Indolone-acetamide derivatives, processes for preparing them and their uses
KR100767272B1 (en) 2003-05-05 2007-10-17 에프. 호프만-라 로슈 아게 Fused pyrimidine derivatives with crf activity
EP1828182B1 (en) 2004-11-29 2010-03-10 Warner-Lambert Company LLC Therapeutic pyrazolo[3,4-b]pyridines and indazoles
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
AR057455A1 (en) 2005-07-22 2007-12-05 Merck & Co Inc INHIBITORS OF HIV REVERSE TRANSCRIPTASE AND PHARMACEUTICAL COMPOSITION
NL2000291C2 (en) 2005-11-10 2009-02-17 Pfizer Prod Inc 1- (1- (2-ethoxyethyl) -3-ethyl-7- (4-methylpyridin-2-ylamino) -1 H -pyrazole (4,3-d) pyrimidin-5-yl) piperidine-4-carboxylic acid and salts thereof.
CN101304989A (en) * 2005-11-11 2008-11-12 弗·哈夫曼-拉罗切有限公司 Carbocyclic fused cyclic amines as inhibitors of the coagulation factor XA
TWI501967B (en) * 2010-12-16 2015-10-01 Janssen R&D Ireland Azaindoles as respiratory syncytial virus antiviral agents
TWI530495B (en) 2010-12-16 2016-04-21 健生科學愛爾蘭無限公司 Benzimidazole respiratory syncytial virus inhibitors
TWI527814B (en) 2010-12-16 2016-04-01 健生科學愛爾蘭無限公司 Azabenzimidazoles as respiratory syncytial virus antiviral agents
TWI541241B (en) 2010-12-16 2016-07-11 健生科學愛爾蘭無限公司 Imidazopyridines as respiratory syncytial virus antiviral agents
TWI515187B (en) 2010-12-16 2016-01-01 健生科學愛爾蘭無限公司 Indoles as respiratory syncytial virus antiviral agents
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Also Published As

Publication number Publication date
WO1998001428A1 (en) 1998-01-15
IL127873A0 (en) 1999-10-28
JP2002514162A (en) 2002-05-14
NZ333696A (en) 2000-06-23
CA2259573A1 (en) 1998-01-15
EP0960102A1 (en) 1999-12-01

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Legal Events

Date Code Title Description
MK5 Application lapsed section 142(2)(e) - patent request and compl. specification not accepted