TW201008930A - Heterocyclic compounds as factor IXa inhibitors - Google Patents

Heterocyclic compounds as factor IXa inhibitors Download PDF

Info

Publication number
TW201008930A
TW201008930A TW098116429A TW98116429A TW201008930A TW 201008930 A TW201008930 A TW 201008930A TW 098116429 A TW098116429 A TW 098116429A TW 98116429 A TW98116429 A TW 98116429A TW 201008930 A TW201008930 A TW 201008930A
Authority
TW
Taiwan
Prior art keywords
group
compound
alkyl
aryl
phenyl
Prior art date
Application number
TW098116429A
Other languages
English (en)
Chinese (zh)
Inventor
Martin C Clasby
William J Greenlee
Samuel Chackalamannil
Yan Xia
Xiao-Bang Gao
Mariappan V Chelliah
Keith A Eagen
Henry Vaccaro
Tin-Yau Chan
Brian A Mckittrick
Li Yuan Wang
Haiyan Pu
Original Assignee
Schering Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41066042&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW201008930(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of TW201008930A publication Critical patent/TW201008930A/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18—One oxygen or sulfur atom
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW098116429A 2008-05-19 2009-05-18 Heterocyclic compounds as factor IXa inhibitors TW201008930A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US5431008P 2008-05-19 2008-05-19

Publications (1)

Publication Number Publication Date
TW201008930A true TW201008930A (en) 2010-03-01

Family

ID=41066042

Family Applications (1)

Application Number Title Priority Date Filing Date
TW098116429A TW201008930A (en) 2008-05-19 2009-05-18 Heterocyclic compounds as factor IXa inhibitors

Country Status (11)

Country Link
US (1) US8148363B2 (enExample)
EP (2) EP2300435A2 (enExample)
JP (1) JP5504259B2 (enExample)
CN (1) CN102099340A (enExample)
AR (1) AR071823A1 (enExample)
CA (1) CA2724430A1 (enExample)
CL (1) CL2009001214A1 (enExample)
MX (1) MX2010012635A (enExample)
PE (1) PE20091972A1 (enExample)
TW (1) TW201008930A (enExample)
WO (1) WO2009143039A2 (enExample)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA33451B1 (fr) * 2009-06-26 2012-07-03 Novartis Ag Dérivés d'imidazolidin-2-one 1,3-disubstitués en tant qu'inhibiteurs de cyp 17
US8242284B1 (en) * 2009-09-21 2012-08-14 The United States Of America As Represented By The United States Department Of Energy Anti-cancer agents based on 6-trifluoromethoxybenzimidazole derivatives and method of making
JP6155187B2 (ja) * 2010-03-30 2017-06-28 ヴァーセオン コーポレイション トロンビンの阻害剤としての多置換芳香族化合物
ES2626601T3 (es) * 2010-06-28 2017-07-25 Bayer Intellectual Property Gmbh Compuestos heterocíclicos como pesticidas
WO2012003405A1 (en) 2010-06-30 2012-01-05 Ironwood Pharmaceuticals, Inc. Sgc stimulators
NZ609955A (en) 2010-11-09 2015-05-29 Ironwood Pharmaceuticals Inc Sgc stimulators
EA023064B1 (ru) 2011-04-28 2016-04-29 Новартис Аг ИНГИБИТОРЫ 17α-ГИДРОКСИЛАЗЫ/C-ЛИАЗЫ
EP2729150B1 (en) 2011-07-08 2016-09-14 Merck Sharp & Dohme Corp. Factor ixa inhibitors
ES2882807T3 (es) 2011-09-16 2021-12-02 Novartis Ag Heterociclil carboxamidas N-sustituidas
CN104066731B (zh) 2011-12-27 2016-06-15 铁木医药有限公司 可用作sgc刺激剂的2-苄基、3-(嘧啶-2-基)取代的吡唑类
CN102660253B (zh) * 2012-03-07 2014-05-21 泰山医学院 一种吡唑啉衍生物类Ni2+荧光探针及其应用
US9914727B2 (en) 2012-12-19 2018-03-13 Merck Sharp & Dohme Corp. Factor IXa inhibitors
US9695198B2 (en) 2012-12-19 2017-07-04 Merck Sharp & Dohme Corp. Factor IXa inhibitors
EP2934538B1 (en) * 2012-12-19 2021-03-31 Merck Sharp & Dohme Corp. Factor ixa inhibitors
ES2791749T3 (es) 2013-03-15 2020-11-05 Verseon Corp Halogenopirazoles como inhibidores de la trombina
WO2014145986A1 (en) 2013-03-15 2014-09-18 Verseon, Inc. Multisubstituted aromatic compounds as serine protease inhibitors
WO2015160636A1 (en) 2014-04-16 2015-10-22 Merck Sharp & Dohme Corp. Factor ixa inhibitors
US10266526B2 (en) * 2014-09-10 2019-04-23 Epizyme, Inc. Substituted 1,2,3-triazoles as SMYD inhibitors for treating cancer
WO2016044645A1 (en) * 2014-09-17 2016-03-24 Elmaleh David R Anticoagulant derivatives for cardiovascular imaging
KR20170048410A (ko) 2014-09-17 2017-05-08 베르선 코포레이션 세린 프로테아제 저해제로서의 피라졸릴-치환된 피리돈 화합물
US10314820B2 (en) 2014-12-04 2019-06-11 Procomcure Biotech Gmbh Imidazole-based heterocyclic compounds
WO2016087616A1 (en) * 2014-12-04 2016-06-09 Procomcure Biotech Gmbh Imidazole-based antimicrobial agents
WO2016133793A1 (en) * 2015-02-16 2016-08-25 Merck Sharp & Dohme Corp. FACTOR IXa INHIBITORS
AU2016224974B2 (en) 2015-02-27 2019-09-26 Verseon Corporation Substituted pyrazole compounds as serine protease inhibitors
KR20180132783A (ko) * 2016-04-07 2018-12-12 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 단백질 조절제로서 유용한 헤테로사이클릭 아미드
CN113549110B (zh) * 2016-04-07 2024-08-16 葛兰素史密斯克莱知识产权发展有限公司 用作蛋白质调节剂的杂环酰胺
EP3541381B1 (en) * 2016-11-18 2022-12-28 Merck Sharp & Dohme LLC Inhibitors of factor xiia
WO2018175670A1 (en) 2017-03-22 2018-09-27 The Research Foundation For The State University Of New York Matrix metalloproteinase-9 hemopexin domain inhibitors and methods of treatment using same
WO2019204447A1 (en) 2018-04-17 2019-10-24 The Regents Of The University Of Michigan Inhibitors of platelet function and methods for use of the same
CN112457308B (zh) * 2019-09-09 2024-01-02 上海长森药业有限公司 新型三环芳香杂环化合物，及其制备方法、药物组合物和应用
EP4143183B1 (en) 2020-04-29 2025-10-22 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
WO2022028572A1 (en) 2020-08-06 2022-02-10 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
WO2022081573A1 (en) * 2020-10-12 2022-04-21 University Of Tennessee Research Foundation Transient receptor potential canonical 3 inhibitors and methods of use thereof
CN116547279A (zh) * 2020-10-13 2023-08-04 加舒布鲁姆生物公司 杂环glp-1激动剂
CN114149371B (zh) * 2021-11-26 2023-08-22 首都医科大学 四取代吡唑类化合物及其应用
CN114478511B (zh) * 2022-02-24 2023-06-20 中国药科大学 苯并恶唑类化合物及其制备方法、药物组合物和应用

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0028489B1 (en) 1979-11-05 1983-10-05 Beecham Group Plc Enzyme derivatives, and their preparation
IL106197A (en) 1992-07-30 1999-11-30 Cor Therapeutics Inc Agagonists for the rhombin receptors and pharmaceutical preparations containing them
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
US6063847A (en) 1997-11-25 2000-05-16 Schering Corporation Thrombin receptor antagonists
PT1094816E (pt) 1998-07-06 2009-03-10 Bristol Myers Squibb Co Sulfonamidas bifenílicas duplamente antagonistas receptores de angiotensina e endotelina
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
AU6690001A (en) 2000-06-15 2001-12-24 Schering Corp Thrombin receptor antagonists
US7235567B2 (en) 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
KR100960170B1 (ko) 2001-10-18 2010-05-26 쉐링 코포레이션 트롬빈 수용체 길항제로서의 힘바신 동족체
JP5039268B2 (ja) * 2001-10-26 2012-10-03 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 ベンゾイミダゾールおよび類縁体および蛋白キナーゼ阻害剤としてのその使用
JP4558331B2 (ja) 2002-04-16 2010-10-06 シェーリング コーポレイション 三環式トロンビンレセプターアンタゴニスト
WO2005030128A2 (en) * 2003-09-23 2005-04-07 Merck & Co., Inc. Pyrazole modulators of metabotropic glutamate receptors
JP2008505905A (ja) * 2004-07-07 2008-02-28 メルク　エンド　カムパニー　インコーポレーテッド ピラゾールアミド誘導体、こうした化合物を含有する組成物および使用方法
CA2574147A1 (en) * 2004-07-22 2006-02-09 Linda Brockunier Substituted pyrazoles, compositions containing such compounds and methods of use
US8710038B2 (en) * 2004-09-17 2014-04-29 Exelixis, Inc. Pyrazole kinase modulators and methods of use
US20070197532A1 (en) * 2005-11-18 2007-08-23 Cao Sheldon X Glucokinase activators
US7968683B1 (en) * 2008-05-07 2011-06-28 Schering Corporation Factor IXa crystals, related complexes and methods
CA2724294A1 (en) * 2008-05-16 2009-11-19 Schering Corporation Glucagon receptor antagonists, compositions, and methods for their use

Also Published As

Publication number Publication date
EP2805939B1 (en) 2018-06-27
CA2724430A1 (en) 2009-11-26
JP2011520967A (ja) 2011-07-21
CL2009001214A1 (es) 2010-12-31
EP2805939A1 (en) 2014-11-26
CN102099340A (zh) 2011-06-15
US8148363B2 (en) 2012-04-03
PE20091972A1 (es) 2010-01-15
WO2009143039A2 (en) 2009-11-26
WO2009143039A3 (en) 2010-07-08
MX2010012635A (es) 2010-12-06
AR071823A1 (es) 2010-07-14
US20110065682A1 (en) 2011-03-17
EP2300435A2 (en) 2011-03-30
JP5504259B2 (ja) 2014-05-28

Similar Documents

Publication Publication Date Title
TWI393716B (zh) 作為ｉｘａ因子抑制劑之雜環化合物
JP5504259B2 (ja) 第ｉｘａ因子阻害剤としての複素環式化合物
TWI804933B (zh) 用作cdk7激酶抑制劑的化合物及其應用
KR101813830B1 (ko) 친전자성 작용기를 갖는 헤테로아릴 피리돈 및 아자-피리돈 화합물
JP5752232B2 (ja) プロテインキナーゼ阻害剤としての置換ピロロトリアジン化合物
US20040132732A1 (en) Quinazolinones and derivatives thereof as factor Xa inhibitors
TW200900058A (en) N-(heteroaryl)-1-heteroaryl-1H-indole-2-carboxamide derivatives, their preparation and their therapeutic application
CN111646995B (zh) 4-氨基-嘧啶并氮杂环-苯基脲类衍生物及其制备方法和用途
TW202115065A (zh) Kras突變蛋白抑制劑
TW200906825A (en) Inhibitors of protein kinases
TW200825087A (en) Certain chemical entities, compositions and methods
TW200803863A (en) Method for inhibiting protein kinases
TW200920370A (en) Heterocyclic amide compounds as protein kinase inhibitors
TW200804276A (en) 5-lipoxygenase-activating protein (FLAP) inhibitors
TW200900403A (en) Pyrimidinone derivatives and methods of use thereof
TW201213324A (en) Fused heterocyclic compounds
CN111053768A (zh) 用于治疗黑素瘤的药物组合
WO2014082578A1 (zh) 杂芳基炔烃化合物及其应用
KR20220113771A (ko) 마크로사이클릭 구조를 갖는 불소-함유 헤테로사이클릭 유도체 및 이의 용도
US9724331B2 (en) Use of maleimide derivatives for preventing and treating leukemia
PH12016500495B1 (en) Compositions for the treatment of hypertension and/or fibrosis
US8426432B2 (en) Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties
WO2023078451A1 (zh) 用作cdk7激酶抑制剂的化合物及其应用
TW593314B (en) Benzisoxazolyl-pyrazole compounds, intermediates therefor, processes for making the same, and pharmaceutical composition useful as a factor XA inhibitor comprising the same
CN113354630B (zh) 一种5,6-二氢苯并[h]喹唑啉类化合物及其应用