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
Authority
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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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

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

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US6221914B1 (en) 1997-11-10 2001-04-24 Array Biopharma Inc. Sulfonamide bridging compounds that inhibit tryptase activity
EP1030844A1 (fr) * 1997-11-10 2000-08-30 Array Biopharma Inc. Composes inhibant l'activite de la tryptase
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
JP2002509923A (ja) 1998-03-31 2002-04-02 ワーナー−ランバート・カンパニー Ｘａ因子およびトロンビンのようなセリンプロテアーゼ阻害剤としてのキノキサリノン
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
CA2320730A1 (fr) * 1998-12-23 2000-07-06 Renhua Li Inhibiteurs du facteur xa ou de la thrombine
IL143906A0 (en) 1998-12-24 2002-04-21 Aventis Pharmaceuticals Produs 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
CA2382751A1 (fr) * 1999-05-24 2000-11-30 Cor Therapeutics, Inc. Inhibiteurs du facteur xa
WO2001012600A1 (fr) * 1999-08-12 2001-02-22 Cor Therapeutics, Inc. INHIBITEURS DU FACTEUR Xa
MXPA02001735A (es) * 1999-08-26 2002-08-06 Aventis Pharm Prod Inc (aminoiminometil o aminometil) dihidrobenzofuranos y benzopiranos sustituidos.
GB9924155D0 (en) * 1999-10-12 1999-12-15 Rhone Poulenc Rorer Pharma Chemical compounds
DE60036568T2 (de) * 1999-11-10 2008-06-26 Sanofi-Aventis Deutschland Gmbh N-acylpyrrolidin-2-ylalkylbenzamidin-derivate als inhibitoren von 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
JP2004510762A (ja) * 2000-10-02 2004-04-08 メルク　エンド　カムパニー　インコーポレーテッド プレニル−蛋白質トランスフェラーゼの阻害剤
EP1383748A2 (fr) 2000-12-22 2004-01-28 Axys Pharmaceuticals, Inc. Composes et compositions en tant qu'inhibiteurs de cathepsine
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
JP2005504078A (ja) 2001-09-14 2005-02-10 アベンティス・ファーマスーティカルズ・インコーポレイテツド カテプシン阻害剤としての新規化合物および組成物
EP1446392A1 (fr) 2001-11-14 2004-08-18 Aventis Pharmaceuticals, Inc. Nouveaux composes et compositions jouant le role d'inhibiteurs de cathepsine s
BR0308232A (pt) 2002-03-07 2004-12-28 Hoffmann La Roche Inibidores de cinase p38 de piridina e pirimidina bicìclicas
DK1569912T3 (en) 2002-12-03 2015-06-29 Pharmacyclics Inc 2- (2-hydroxybiphenyl-3-yl) -1h-benzoimidazole-5-carboxamidine derivatives as factor VIIa inhibitors.
JP4897221B2 (ja) * 2002-12-20 2012-03-14 チバ ホールディング インコーポレーテッド アミン類の合成及びその合成のための中間体
TW200508197A (en) * 2003-03-31 2005-03-01 Ucb Sa Indolone-acetamide derivatives, processes for preparing them and their uses
CN100372851C (zh) 2003-05-05 2008-03-05 弗·哈夫曼-拉罗切有限公司 具有crf活性的稠合的嘧啶衍生物
JP4130219B2 (ja) 2004-11-29 2008-08-06 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 治療用のピラゾロ［３，４−ｂ］ピリジンおよびインダゾール
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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.
AU2006311101A1 (en) * 2005-11-11 2007-05-18 F. Hoffmann-La Roche Ag Carbocyclic fused cyclic amines as inhibitors of the coagulation factor Xa
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
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
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
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
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
LT2864323T (lt) 2012-06-15 2017-07-25 Janssen Sciences Ireland Uc 1,3-dihidro-2h-benzimidazol-2-ono dariniai, turintys heterociklų pakaitų, kaip antivirusiniai agentai prieš respiratorinį sincitinį virusą
WO2019036562A1 (fr) * 2017-08-18 2019-02-21 Saint Louis University Agonistes inverses d'err

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

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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued