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IL127873A0 - 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
IL127873A0
IL127873A0 IL12787397A IL12787397A IL127873A0 IL 127873 A0 IL127873 A0 IL 127873A0 IL 12787397 A IL12787397 A IL 12787397A IL 12787397 A IL12787397 A IL 12787397A IL 127873 A0 IL127873 A0 IL 127873A0
Authority
IL
Israel
Prior art keywords
amidinoazoles
amidinoindoles
thrombin
analogs
inhibitors
Prior art date
Application number
IL12787397A
Original Assignee
Du Pont Pharm 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 Du Pont Pharm Co filed Critical Du Pont Pharm Co
Publication of IL127873A0 publication Critical patent/IL127873A0/en

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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
IL12787397A 1996-07-08 1997-06-30 Amidinoindoles amidinoazoles and analogs thereof as inhibitors of factor xa and of thrombin IL127873A0 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US67676696A 1996-07-08 1996-07-08
US4951997P 1997-06-13 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
IL127873A0 true IL127873A0 (en) 1999-10-28

Family

ID=26727252

Family Applications (1)

Application Number Title Priority Date Filing Date
IL12787397A IL127873A0 (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)

Families Citing this family (45)

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US6221914B1 (en) 1997-11-10 2001-04-24 Array Biopharma Inc. Sulfonamide bridging compounds that inhibit tryptase activity
AU1208999A (en) * 1997-11-10 1999-05-31 Array Biopharma, Inc. Compounds which inhibit tryptase activity
AU1608399A (en) * 1997-11-26 1999-06-15 Axys Pharmaceuticals, Inc. Substituted amidinoaryl derivatives and their use as anticoagulants
WO1999026932A1 (en) * 1997-11-26 1999-06-03 Axys Pharmaceuticals, Inc. By amidino group substituted heterocyclic 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
KR20010042298A (en) * 1998-03-31 2001-05-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 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
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
CA2358047A1 (en) 1998-12-24 2000-07-06 Francis A. Volz Substituted (aminoiminomethyl or aminomethyl)benzoheteroaryl compounds
TW200404789A (en) 1999-03-15 2004-04-01 Axys Pharm Inc Novel compounds and compositions as protease inhibitors
WO2000071512A1 (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
EP1222182B1 (en) * 1999-08-26 2005-11-16 Aventis Pharmaceuticals Inc. Substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benozopyrans
GB9924155D0 (en) * 1999-10-12 1999-12-15 Rhone Poulenc Rorer Pharma Chemical compounds
CA2390858C (en) * 1999-11-10 2010-02-02 Aventis Pharma Deutschland Gmbh N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor xa
US7361663B2 (en) 1999-11-10 2008-04-22 Aventis Pharmaceuticals Inc. 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
CA2424222A1 (en) * 2000-10-02 2002-04-11 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
CA2433520A1 (en) 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
PL369312A1 (en) 2001-09-14 2005-04-18 Aventis Pharmaceuticals Inc. Novel compounds and compositions as cathepsin inhibitors
CA2467391A1 (en) 2001-11-14 2003-05-22 Aventis Pharmaceuticals Inc. Oligopeptides and compositions containing them as cathepsin s inhibitors
EP1485390B1 (en) 2002-03-07 2008-10-08 F. Hoffman-la Roche AG Bicyclic pyridine and pyrimidine p38 kinase inhibitors
ES2543588T3 (en) 2002-12-03 2015-08-20 Pharmacyclics Llc 2- (2-Hydroxybiphenyl-3-yl) -1H-benzoimidazol-5-carboxamidine derivatives as inhibitors of factor VIIa
EP2666772B1 (en) * 2002-12-20 2017-03-01 Basf Se Synthesis of amines and intermediates for the synthesis thereof
TW200508197A (en) * 2003-03-31 2005-03-01 Ucb Sa Indolone-acetamide derivatives, processes for preparing them and their uses
EP1622910A1 (en) 2003-05-05 2006-02-08 F. Hoffmann-La Roche Ag Fused pyrimidine derivatives with crf activity
ATE460415T1 (en) 2004-11-29 2010-03-15 Warner Lambert Co THERAPEUTIC PYRAZOLOA3,4-BUPYRIDINES 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.
BRPI0618523A2 (en) * 2005-11-11 2011-09-06 Hoffmann La Roche carbocyclically fused cyclic amine compounds, pharmaceutical compositions and uses thereof
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
TWI530495B (en) 2010-12-16 2016-04-21 健生科學愛爾蘭無限公司 Benzimidazole respiratory syncytial virus inhibitors
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
TWI501967B (en) 2010-12-16 2015-10-01 Janssen R&D Ireland Azaindoles as respiratory syncytial virus antiviral agents
CN103649079B (en) 2010-12-22 2016-11-16 Abbvie公司 Hepatitis c inhibitor and application thereof
CN103376329A (en) * 2012-04-19 2013-10-30 蓬莱诺康药业有限公司 Characterization method of stypticity of hemocoagulase atrox for injection and effective components thereof
DK2864323T3 (en) 2012-06-15 2017-08-14 Janssen Sciences Ireland Uc 1,3-DIHYDRO-2H-BENZIMIDAZOLE-2 UNDERIVATIVES SUBSTITUTED BY HETEROCYCLES AS ANTIVIRUS AGENTS AGAINST RESPIRATORY SYNCYTIAL VIRUS
WO2019036562A1 (en) * 2017-08-18 2019-02-21 Saint Louis University Err inverse agonists
EP4165034A1 (en) 2020-06-11 2023-04-19 Janssen Sciences Ireland Unlimited Company Hemi (l)-tartrate forms of 3-({5-chloro-1-[3-(methylsulfonyl)propyl]-1h-indol-2 yl} methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2h-imidazo[4,5-c]pyridin-2-one and pharmaceutical compositions comprising the same

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Also Published As

Publication number Publication date
EP0960102A1 (en) 1999-12-01
CA2259573A1 (en) 1998-01-15
WO1998001428A1 (en) 1998-01-15
AU3645697A (en) 1998-02-02
NZ333696A (en) 2000-06-23
JP2002514162A (en) 2002-05-14

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