JP2002514162A - Ｘａ因子阻害薬およびトロンビン阻害薬としてのアミジノインドール類、アミジノアゾール類、およびそれらの類似体 - Google Patents

Ｘａ因子阻害薬およびトロンビン阻害薬としてのアミジノインドール類、アミジノアゾール類、およびそれらの類似体

Info

Publication number
JP2002514162A
JP2002514162A JP50524998A JP50524998A JP2002514162A JP 2002514162 A JP2002514162 A JP 2002514162A JP 50524998 A JP50524998 A JP 50524998A JP 50524998 A JP50524998 A JP 50524998A JP 2002514162 A JP2002514162 A JP 2002514162A
Authority
JP
Japan
Prior art keywords
methyl
substituted
phenyl
alkyl
compound
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.)
Pending
Application number
JP50524998A
Other languages
English (en)
Japanese (ja)
Inventor
ドミンゲス，セリア
ハン，キ．
ダフィー，ダニエル，エメット．
パク，ジョオンスク，マリア．
クアン，ミミ，ライフェン．
ロッシ，カレン，アニータ．
ヴェクスラー，ルース，リッチモンド．
Original Assignee
デュポン ファーマシューティカルズ カンパニー
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 デュポン ファーマシューティカルズ カンパニー filed Critical デュポン ファーマシューティカルズ カンパニー
Publication of JP2002514162A publication Critical patent/JP2002514162A/ja
Pending 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP50524998A 1996-07-08 1997-06-30 Ｘａ因子阻害薬およびトロンビン阻害薬としてのアミジノインドール類、アミジノアゾール類、およびそれらの類似体 Pending JP2002514162A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US67676696A 1996-07-08 1996-07-08
US4951997P 1997-06-13 1997-06-13
US60/049,519 1997-06-13
US08/676,766 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
JP2002514162A true JP2002514162A (ja) 2002-05-14

Family

ID=26727252

Family Applications (1)

Application Number Title Priority Date Filing Date
JP50524998A Pending JP2002514162A (ja) 1996-07-08 1997-06-30 Ｘａ因子阻害薬およびトロンビン阻害薬としてのアミジノインドール類、アミジノアゾール類、およびそれらの類似体

Country Status (7)

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

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006522041A (ja) * 2003-03-31 2006-09-28 ユ セ ベ ソシエテ アノニム インドロンアセトアミド誘導体、その調製方法及びその使用
JP2009514926A (ja) * 2005-11-11 2009-04-09 エフ．ホフマン−ラ ロシュ アーゲー 凝固因子Ｘａの阻害剤としての炭素環式縮合環アミン
JP2011168608A (ja) * 2002-12-20 2011-09-01 Ciba Holding Inc アミン類の合成及びその合成のための中間体
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

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (de) * 1997-12-03 1999-06-10 Boehringer Ingelheim Pharma Substituierte Indole, ihre Herstellung und ihre Verwendung als Arzneimittel
WO1999050254A1 (en) 1998-03-31 1999-10-07 Warner-Lambert Company 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 (de) * 1998-10-01 2000-04-06 Merck Patent Gmbh Imidazo[4,5]-pyridin-4-on-derivate
US6362216B1 (en) 1998-10-27 2002-03-26 Array Biopharma Inc. Compounds which inhibit tryptase activity
WO2000039102A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
ID30516A (id) * 1998-12-24 2001-12-13 Aventis Pharm Prod Inc Senyawa-senyawa (aminoiminometil atau aminometil) benzoheteroaril tersubstitusi
TW200404789A (en) 1999-03-15 2004-04-01 Axys Pharm Inc Novel compounds and compositions as protease inhibitors
JP2003500387A (ja) * 1999-05-24 2003-01-07 シーオーアール セラピューティクス インコーポレイテッド Ｘａ因子の阻害剤
US6534535B1 (en) * 1999-08-12 2003-03-18 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
GB9924155D0 (en) * 1999-10-12 1999-12-15 Rhone Poulenc Rorer Pharma Chemical compounds
CA2383257C (en) * 1999-08-26 2010-09-28 Christopher J. Burns Substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benozopyrans
EP1263726B1 (en) * 1999-11-10 2007-09-26 Sanofi-Aventis 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
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
US7064123B1 (en) 2000-12-22 2006-06-20 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
RS19504A (xx) 2001-09-14 2007-02-05 Aventis Pharmaceuticals Inc., Nova jedinjenja i kompozicije kao inhibitori katepsina
HUP0401906A3 (en) 2001-11-14 2008-07-28 Aventis Pharma Inc Novel cathepsin s inhibitors, process for their preparation and pharmaceutical compositions containing them
CA2477721A1 (en) 2002-03-07 2003-09-12 F. Hoffmann-La Roche Ag Bicyclic pyridine and pyrimidine p38 kinase inhibitors
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
RU2328497C2 (ru) 2003-05-05 2008-07-10 Ф.Хоффманн-Ля Рош Аг Конденсированные производные пиримидина и лекарственное средство, обладающее активностью в отношении crf
DK1828182T3 (da) 2004-11-29 2010-05-10 Warner Lambert Co Terapeutiske pyrazol[3,4-B]pyridiner og indazoler
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.
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
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
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
EP2655362A1 (en) 2010-12-22 2013-10-30 Abbvie Inc. Hepatitis c inhibitors and uses thereof
KR102092612B1 (ko) 2012-06-15 2020-03-25 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 호흡기 합포체 바이러스의 항바이러스제로서의 헤테로사이클로 치환된 1,3-디하이드로-2h-벤즈이미다졸-2-온 유도체
US11795162B2 (en) * 2017-08-18 2023-10-24 Saint Louis University Modulators of the estrogen-related receptor

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA928276B (en) * 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011168608A (ja) * 2002-12-20 2011-09-01 Ciba Holding Inc アミン類の合成及びその合成のための中間体
JP2006522041A (ja) * 2003-03-31 2006-09-28 ユ セ ベ ソシエテ アノニム インドロンアセトアミド誘導体、その調製方法及びその使用
JP2009514926A (ja) * 2005-11-11 2009-04-09 エフ．ホフマン−ラ ロシュ アーゲー 凝固因子Ｘａの阻害剤としての炭素環式縮合環アミン
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

Also Published As

Publication number Publication date
AU3645697A (en) 1998-02-02
EP0960102A1 (en) 1999-12-01
IL127873A0 (en) 1999-10-28
CA2259573A1 (en) 1998-01-15
WO1998001428A1 (en) 1998-01-15
NZ333696A (en) 2000-06-23

Similar Documents

Publication Publication Date Title
JP2002514162A (ja) Ｘａ因子阻害薬およびトロンビン阻害薬としてのアミジノインドール類、アミジノアゾール類、およびそれらの類似体
US6043257A (en) Amidinoindoles, amidinoazoles, and analogs thereof
US6369227B1 (en) Thrombin or factor Xa inhibitors
EP1175419B1 (en) Aryl sulfonyls as factor xa inhibitors
US6716841B2 (en) Nitrogen containing heterobicycles as factor Xa inhibitors
US6436985B2 (en) Disubstituted pyrazolines and triazolines as factor Xa inhibitors
JP2001515887A (ja) Ｘａ因子の阻害剤としての、ベンゾイミダゾリノン類、ベンゾオキサゾリノン類、ベンゾピペラジノン類、インダノン類、およびそれらの誘導体
US6790845B2 (en) Fused heterocyclic inhibitors of factor Xa
US6730689B2 (en) N-[4-(1H-imidazol-1-yl)-2-fluorophenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as factor Xa inhibitors
US6586418B2 (en) Thrombin or factor Xa inhibitors
US6747158B2 (en) Efficient process for the preparation of a factor Xa inhibitor
US20040038980A1 (en) Imidazo-heterobicycles as factor xa inhibitors
US20030096804A1 (en) Bicyclic inhibitors of factor Xa
MXPA99000375A (en) Amidinoindoles, amidinoazoles and analogues of them as inhibitors of the factor xa and the tromb