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 & 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

    • 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)
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
PE20121048A1 (es) * 2009-06-26 2012-08-25 Novartis Ag Derivados de imidazolidin-2-ona 1,3-disustituida como inhibidores de cyp17
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
SG10201502484SA (en) * 2010-03-30 2015-05-28 Verseon Corp Multisubstituted aromatic compounds as inhibitors of thrombin
CN103119036B (zh) * 2010-06-28 2018-05-08 拜耳知识产权有限责任公司 作为杀虫剂的杂环化合物
TWI532737B (zh) 2010-06-30 2016-05-11 艾諾屋製藥公司 可溶性鳥苷酸環化酶（ｓＧＣ）刺激物
JP5878546B2 (ja) 2010-11-09 2016-03-08 アイアンウッド ファーマシューティカルズ インコーポレイテッド ｓＧＣ刺激剤
MX359399B (es) 2011-04-28 2018-09-27 Novartis Ag Inhibidores de 17alfa-hidroxilasa/c17-20-liasa.
EP2729150B1 (en) 2011-07-08 2016-09-14 Merck Sharp & Dohme Corp. Factor ixa inhibitors
JP6165733B2 (ja) 2011-09-16 2017-07-19 ノバルティス アーゲー Ｎ−置換ヘテロシクリルカルボキサミド類
CA2861804C (en) 2011-12-27 2021-10-26 Ironwood Pharmaceuticals, Inc. 2-benzyl,3(pyrimidin-2-yl)substituted pyrazoles useful as sgc stimulators
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
WO2014120346A1 (en) * 2012-12-19 2014-08-07 Merck Sharp & Dohme Corp. Factor ixa inhibitors
EP2934536B1 (en) 2012-12-19 2017-09-27 Merck Sharp & Dohme Corp. FACTOR IXa INHIBITORS
WO2014099695A1 (en) * 2012-12-19 2014-06-26 Merck Sharp & Dohme Corp. Factor ixa inhibitors
DK2968297T3 (en) * 2013-03-15 2019-01-07 Verseon Inc MULTI-SUBSTITUTED AROMATIC COMPOUNDS AS SERINE PROTEASE INHIBITORS
WO2014149139A2 (en) 2013-03-15 2014-09-25 Verseon, Inc. Halogenopyrazoles as inhibitors of thrombin
WO2015160636A1 (en) 2014-04-16 2015-10-22 Merck Sharp & Dohme Corp. Factor ixa inhibitors
AU2015315174B2 (en) * 2014-09-10 2019-12-12 Epizyme, Inc. Smyd inhibitors
US10300154B2 (en) 2014-09-17 2019-05-28 David R Elmaleh Anticoagulant derivatives for cardiovascular imaging
JP2017528486A (ja) 2014-09-17 2017-09-28 ヴァーセオン コーポレイション セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物
WO2016087615A1 (en) 2014-12-04 2016-06-09 Procomcure Biotech Gmbh Novel imidazole-based heterocyclic compounds
ES2859674T3 (es) 2014-12-04 2021-10-04 Procomcure Biotech Gmbh Agentes antimicrobianos a base de imidazol
WO2016133793A1 (en) * 2015-02-16 2016-08-25 Merck Sharp & Dohme Corp. FACTOR IXa INHIBITORS
ES2931460T3 (es) 2015-02-27 2022-12-29 Verseon Int Corporation Compuestos de pirazol sustituido como inhibidores de serina proteasa
SG10201900628RA (en) 2016-04-07 2019-02-27 Glaxosmithkline Ip Dev Ltd Heterocyclic amides useful as protein modulators
WO2017175156A1 (en) * 2016-04-07 2017-10-12 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides useful as protein modulators
WO2018093716A1 (en) * 2016-11-18 2018-05-24 Merck Sharp & Dohme Corp. FACTOR XIIa INHIBITORS
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
HUE062236T2 (hu) * 2018-04-17 2023-10-28 Univ Michigan Regents Vérlemezke funkció inhibitorok és eljárás azok alkalmazására
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
WO2021219019A1 (en) 2020-04-29 2021-11-04 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
PE20231181A1 (es) 2020-08-06 2023-08-11 Gasherbrum Bio Inc Agonistas del glp-1 heterociclicos
WO2022081573A1 (en) * 2020-10-12 2022-04-21 University Of Tennessee Research Foundation Transient receptor potential canonical 3 inhibitors and methods of use thereof
JP2023546055A (ja) * 2020-10-13 2023-11-01 ガシャーブラム・バイオ・インコーポレイテッド ヘテロ環ｇｌｐ－１アゴニスト
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
ID26984A (id) 1998-07-06 2001-02-22 Bristol Myers Squibb Co Senyawa-senyawa sulfonamida sebagai antagonis reseptor angiotensin endotelin ganda
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
US7235567B2 (en) 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
KR100604742B1 (ko) 2000-06-15 2006-07-26 쉐링 코포레이션 트롬빈 수용체 길항제
CA2463628A1 (en) 2001-10-18 2003-04-24 Schering Corporation Himbacine analogues as thrombin receptor antagonists
IL161576A0 (en) * 2001-10-26 2004-09-27 Aventis Pharma Inc Benzimidazoles and analogues and their use as protein kinases inhibitors
EP1982984B1 (en) 2002-04-16 2013-02-13 Merck Sharp & Dohme Corp. Manufacture of tricyclic thrombin receptor antagonists and pharmaceutical compositions comprising them
US20060281803A1 (en) * 2003-09-23 2006-12-14 Lindsley Craig W Pyrazole modulators of metabotropic glutamate receptors
DE602005017895D1 (de) * 2004-07-07 2010-01-07 Merck & Co Inc Pyrazolamid-derivate, diese verbindungen enthaltende zusammensetzungen und anwendungsverfahren
AU2005269792B9 (en) * 2004-07-22 2008-11-27 Merck Sharp & Dohme Corp. Substituted pyrazoles, compositions containing such compounds and methods of use
WO2006033943A2 (en) * 2004-09-17 2006-03-30 Exelixis, Inc Pyrazole kinase modulators and methods of use
WO2007061923A2 (en) * 2005-11-18 2007-05-31 Takeda San Diego, Inc. Glucokinase activators
US7968683B1 (en) * 2008-05-07 2011-06-28 Schering Corporation Factor IXa crystals, related complexes and methods
US8623818B2 (en) * 2008-05-16 2014-01-07 Merck Sharp & Dohme Corp. Glucagon receptor antagonists, compositions, and methods for their use

Also Published As

Publication number Publication date
CL2009001214A1 (es) 2010-12-31
MX2010012635A (es) 2010-12-06
EP2805939A1 (en) 2014-11-26
WO2009143039A3 (en) 2010-07-08
US8148363B2 (en) 2012-04-03
AR071823A1 (es) 2010-07-14
PE20091972A1 (es) 2010-01-15
WO2009143039A2 (en) 2009-11-26
TW201008930A (en) 2010-03-01
US20110065682A1 (en) 2011-03-17
EP2805939B1 (en) 2018-06-27
JP5504259B2 (ja) 2014-05-28
EP2300435A2 (en) 2011-03-30
CN102099340A (zh) 2011-06-15
JP2011520967A (ja) 2011-07-21

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20140515

FZDE Discontinued

Effective date: 20160519