CA2259573A1 - Amidinoindoles, amidinoazoles et leurs analogues agissant en tant qu'inhibiteurs du facteur xa et de la thrombine - Google Patents

Amidinoindoles, amidinoazoles et leurs analogues agissant en tant qu'inhibiteurs du facteur xa et de la thrombine Download PDF

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Publication number
CA2259573A1
CA2259573A1 CA002259573A CA2259573A CA2259573A1 CA 2259573 A1 CA2259573 A1 CA 2259573A1 CA 002259573 A CA002259573 A CA 002259573A CA 2259573 A CA2259573 A CA 2259573A CA 2259573 A1 CA2259573 A1 CA 2259573A1
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CA
Canada
Prior art keywords
phenyl
methyl
substituted
alkyl
amidinoindole
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
CA002259573A
Other languages
English (en)
Inventor
Ruth Richmond Wexler
Jeongsook Maria Park
Daniel Emmett Duffy
Mimi Lifen Quan
Qi Han
Karen Anita Rossi
Celia Dominguez
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
Individual
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 Individual filed Critical Individual
Publication of CA2259573A1 publication Critical patent/CA2259573A1/fr
Abandoned legal-status Critical Current

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    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente demande concerne des amidinoindoles, des amidinoazoles et leurs analogues répondant à la formule (I), où W, W?1¿, W?2¿ et W?3¿ sont choisis parmi CH et N, à condition que l'un des éléments W?1¿ et W?2¿ soit C(C(=NH)NH¿2?), que deux au plus des éléments W, W?1¿, W?2¿ et W?3¿ soient N, et que l'un des éléments J?a¿ et J?b¿ soit substitué par -(CH¿2?)¿n?-Z-A-B, et pouvant être utiles en tant qu'inhibiteurs du facteur Xa ou de la thrombine.
CA002259573A 1996-07-08 1997-06-30 Amidinoindoles, amidinoazoles et leurs analogues agissant en tant qu'inhibiteurs du facteur xa et de la thrombine Abandoned CA2259573A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US67676696A 1996-07-08 1996-07-08
US08/676,766 1996-07-08
US4951997P 1997-06-13 1997-06-13
US60/049,519 1997-06-13

Publications (1)

Publication Number Publication Date
CA2259573A1 true CA2259573A1 (fr) 1998-01-15

Family

ID=26727252

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002259573A Abandoned CA2259573A1 (fr) 1996-07-08 1997-06-30 Amidinoindoles, amidinoazoles et leurs analogues agissant en tant qu'inhibiteurs du facteur xa et de la thrombine

Country Status (7)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6492384B1 (en) 1998-10-01 2002-12-10 Merck Patent Gmbh Imidazo (4,5-C) pyridine-4-one derivatives with factor XA inhibiting effect

Families Citing this family (43)

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Publication number Priority date Publication date Assignee Title
AU1208999A (en) * 1997-11-10 1999-05-31 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 (fr) * 1997-11-26 1999-06-03 Axys Pharmaceuticals, Inc. Derives heterocycliques substitues par un groupe amidino et leur utilisation en tant qu'anticoagulants
WO1999026933A1 (fr) * 1997-11-26 1999-06-03 Axys Pharmaceuticals, Inc. Derives d'amidinoaryle substitue et leur utilisation comme anticoagulants
DE19753522A1 (de) * 1997-12-03 1999-06-10 Boehringer Ingelheim Pharma Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel
HUP0101470A3 (en) 1998-03-31 2002-09-30 Warner Lambert Co Quinoxalinones as serine protease inhibitors such as factor xa and thrombin and medicaments containing the compounds
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
US6362216B1 (en) 1998-10-27 2002-03-26 Array Biopharma Inc. Compounds which inhibit tryptase activity
EP1058549A4 (fr) * 1998-12-23 2003-11-12 Bristol Myers Squibb Pharma Co INHIBITEURS DU FACTEUR Xa OU DE LA THROMBINE
EE200100341A (et) * 1998-12-24 2002-12-16 Aventis Pharmaceuticals Products Inc. Asendatud (aminoiminometüül- või aminometüül)bensoheteroarüülühendid, nende kasutamine ja farmatseutiline kompositsioon
TW200404789A (en) 1999-03-15 2004-04-01 Axys Pharm Inc Novel compounds and compositions as protease inhibitors
EP1189879A1 (fr) * 1999-05-24 2002-03-27 Cor Therapeutics, Inc. Inhibiteurs du facteur xa
WO2001012600A1 (fr) * 1999-08-12 2001-02-22 Cor Therapeutics, Inc. INHIBITEURS DU FACTEUR Xa
GB9924155D0 (en) * 1999-10-12 1999-12-15 Rhone Poulenc Rorer Pharma Chemical compounds
DE60024120T2 (de) * 1999-08-26 2006-07-27 Aventis Pharmaceuticals Inc. Substituierte (aminoiminomethyl oder aminomethyl) dihydrobenzofurane und benozopyrane
US7361663B2 (en) 1999-11-10 2008-04-22 Aventis Pharmaceuticals Inc. N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
AU2155001A (en) * 1999-11-10 2001-06-06 Aventis Pharma Deutschland 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
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
IL156577A0 (en) 2000-12-22 2004-01-04 Axys Pharm Inc Selective cathepsin s inhibitors and pharmaceutical compositions containing the same
BR0212535A (pt) 2001-09-14 2004-10-19 Aventis Pharma Inc Compostos e composições como inibidores de catepsina
CN1324018C (zh) 2001-11-14 2007-07-04 安万特药物公司 作为组织蛋白酶s抑制剂的寡肽以及含有它们的组合物
CA2477721A1 (fr) 2002-03-07 2003-09-12 F. Hoffmann-La Roche Ag Pyridine et pyrimidine bicycliques, inhibitrices de la p38 kinase
PT1569912E (pt) 2002-12-03 2015-09-15 Pharmacyclics Llc Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia
CN1729174B (zh) * 2002-12-20 2015-10-21 西巴特殊化学品控股有限公司 胺的合成以及用于合成胺的中间体
TW200508197A (en) * 2003-03-31 2005-03-01 Ucb Sa Indolone-acetamide derivatives, processes for preparing them and their uses
CA2523261C (fr) 2003-05-05 2009-07-07 F. Hoffmann-La Roche Ag Derives de pyrimidine fusionnees a activite crf
WO2006056873A2 (fr) 2004-11-29 2006-06-01 Warner-Lambert Company Llc Pyrazolo[3,4-b] pyridines et indazoles therapeutiques
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
AR057455A1 (es) 2005-07-22 2007-12-05 Merck & Co Inc Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica
NL2000291C2 (nl) 2005-11-10 2009-02-17 Pfizer Prod Inc 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H- pyrazool(4,3-d)pyrimidine-5-yl)piperidine-4-carbonzuur en zouten daarvan.
WO2007054453A2 (fr) * 2005-11-11 2007-05-18 F. Hoffmann-La Roche Ag Nouvelles amines cycliques fusionnees a un carbocyclyle
TWI530495B (zh) 2010-12-16 2016-04-21 健生科學愛爾蘭無限公司 苯并咪唑呼吸道融合病毒抑制劑
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
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
WO2012087833A1 (fr) 2010-12-22 2012-06-28 Abbott Laboratories Inhibiteurs de l'hépatite c et leurs utilisations
CN103376329A (zh) * 2012-04-19 2013-10-30 蓬莱诺康药业有限公司 巴曲亭及其有效成份止血作用的表征方法
CN104540817B (zh) 2012-06-15 2017-03-01 爱尔兰詹森科学公司 作为呼吸道合胞病毒抗病毒剂的用杂环取代的1，3‑二氢‑2h‑苯并咪唑‑2‑酮衍生物
WO2019036562A1 (fr) * 2017-08-18 2019-02-21 Saint Louis University Agonistes inverses d'err

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ZA928276B (en) * 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6492384B1 (en) 1998-10-01 2002-12-10 Merck Patent Gmbh Imidazo (4,5-C) pyridine-4-one derivatives with factor XA inhibiting effect

Also Published As

Publication number Publication date
EP0960102A1 (fr) 1999-12-01
NZ333696A (en) 2000-06-23
JP2002514162A (ja) 2002-05-14
WO1998001428A1 (fr) 1998-01-15
AU3645697A (en) 1998-02-02
IL127873A0 (en) 1999-10-28

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued