CA2724430A1 - Heterocyclic compounds as factor ixa inhibitors - Google Patents

Heterocyclic compounds as factor ixa inhibitors Download PDF

Info

Publication number
CA2724430A1
CA2724430A1 CA2724430A CA2724430A CA2724430A1 CA 2724430 A1 CA2724430 A1 CA 2724430A1 CA 2724430 A CA2724430 A CA 2724430A CA 2724430 A CA2724430 A CA 2724430A CA 2724430 A1 CA2724430 A1 CA 2724430A1
Authority
CA
Canada
Prior art keywords
compound
alkyl
aryl
group
phenyl
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
CA2724430A
Other languages
English (en)
French (fr)
Inventor
Martin C. Clasby
William J. Greenlee
Samuel Chackalamannil
Yan Xia
Xiaobang Gao
Mariappan V. Chelliah
Keith A. Eagen
Henry Vaccaro
Tin-Yau Chan
Brian Mckittrick
Li Yuan Wang
Haiyan Pu
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.)
Merck Sharp and Dohme LLC
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=CA2724430(A1) "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 CA2724430A1 publication Critical patent/CA2724430A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • C07D231/18One oxygen or sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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)
CA2724430A 2008-05-19 2009-05-18 Heterocyclic compounds as factor ixa inhibitors Abandoned CA2724430A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5431008P 2008-05-19 2008-05-19
US61/054,310 2008-05-19
PCT/US2009/044291 WO2009143039A2 (en) 2008-05-19 2009-05-18 Heterocyclic compounds as factor ixa inhibitors

Publications (1)

Publication Number Publication Date
CA2724430A1 true CA2724430A1 (en) 2009-11-26

Family

ID=41066042

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2724430A Abandoned CA2724430A1 (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
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
TW201008930A (en) 2010-03-01

Similar Documents

Publication Publication Date Title
EP2805939B1 (en) Heterocyclic compounds as factor IXA inhibitors.
US8609676B2 (en) 4, 5, 6-trisubstituted pyrimidine derivatives as factor IXa inhibitors
CN108602776B (zh) 用作irak抑制剂的杂芳基化合物及其用途
CA2927392C (en) Dna-pk inhibitors
CA2958262C (en) 1-cyano-pyrrolidine derivatives as deubiquitinase inhibitors (dub) and use thereof
CN108290879B (zh) 用作irak抑制剂的杂芳基化合物及其用途
CA2937739C (en) Macrocycles with heterocyclic p2' groups as factor xia inhibitors
AU2021200884A1 (en) MK2 inhibitors and uses thereof
US20040209863A1 (en) Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors
NO319816B1 (no) Nitrogenholdige heterocykler,anvendelse av disse for fremstilling av medikamenter samt farmasoytiske preparater.
AU2015295405A1 (en) Compounds active towards bromodomains
BRPI0620010A2 (pt) compostos ánalogos de arilpropionamida, arilacrilamida, arilpropinamida, ou arilmetiluréia, processo para sua preparação, composição farmacêutica e uso dos mesmos
CA2694284A1 (en) Heterocyclic compounds useful as raf kinase inhibitors
CA2679807A1 (en) Piperidine derivatives and methods of use thereof
CA3122623C (en) Halo-allylamine compounds and use thereof
CA2963607A1 (en) Heparan sulfate biosynthesis inhibitors for the treatment of diseases
CA2849194A1 (en) Imidazopyridazine compounds
CA2983668A1 (en) Pyrazole derivatives useful as 5-lipoxygenase activating protein (flap) inhibitors
JP2008543972A (ja) 血栓症状の治療に有用なp2y1受容体のn−結合複素環式アンタゴニスト
JP2021524469A (ja) Nrf2アクチベーターとしてのインダン
CN101341129B (zh) 作为因子xia抑制剂的芳基丙酰胺,芳基丙烯酰胺,芳基丙炔酰胺,或芳基甲基脲类似物
EP4282862A1 (en) Flavivirus inhibitors
HK1246287A1 (zh) 用作irak抑制剂的哒嗪酮类大环化合物及其用途
HK1137013A (en) Compounds useful as protein kinase inhibitors

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20140515

FZDE Discontinued

Effective date: 20160519