CN102099340A - 作为因子ixa抑制剂的杂环化合物 - Google Patents

作为因子ixa抑制剂的杂环化合物 Download PDF

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Publication number
CN102099340A
CN102099340A CN200980128238XA CN200980128238A CN102099340A CN 102099340 A CN102099340 A CN 102099340A CN 200980128238X A CN200980128238X A CN 200980128238XA CN 200980128238 A CN200980128238 A CN 200980128238A CN 102099340 A CN102099340 A CN 102099340A
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CN
China
Prior art keywords
alkyl
compound
aryl
group
phenyl
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Pending
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CN200980128238XA
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English (en)
Chinese (zh)
Inventor
M.C.克拉斯比
W.J.格林李
S.查卡拉曼尼尔
Y.夏
X.高
M.V.彻利亚
K.A.伊根
H.瓦卡罗
T.陈
B.麦基崔克
L.Y.王
H.普
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Merck Sharp and Dohme LLC
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Schering Corp
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Application filed by Schering Corp filed Critical Schering Corp
Publication of CN102099340A publication Critical patent/CN102099340A/zh
Pending legal-status Critical Current

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    • 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

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  • 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)
CN200980128238XA 2008-05-19 2009-05-18 作为因子ixa抑制剂的杂环化合物 Pending CN102099340A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5431008P 2008-05-19 2008-05-19
US61/054310 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
CN102099340A true CN102099340A (zh) 2011-06-15

Family

ID=41066042

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980128238XA Pending CN102099340A (zh) 2008-05-19 2009-05-18 作为因子ixa抑制剂的杂环化合物

Country Status (11)

Country Link
US (1) US8148363B2 (enExample)
EP (2) EP2805939B1 (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)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110179795A (zh) * 2013-03-15 2019-08-30 维颂公司 作为丝氨酸蛋白酶抑制剂的多取代芳族化合物的制药用途
CN113015725A (zh) * 2018-04-17 2021-06-22 密歇根大学董事会 血小板功能抑制剂及其使用方法
CN114149371A (zh) * 2021-11-26 2022-03-08 首都医科大学 四取代吡唑类化合物及其应用
CN116547279A (zh) * 2020-10-13 2023-08-04 加舒布鲁姆生物公司 杂环glp-1激动剂

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5456891B2 (ja) * 2009-06-26 2014-04-02 ノバルティス アーゲー Cyp17阻害剤としての1,3−二置換イミダゾリジン−2−オン誘導体
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
RU2639876C2 (ru) 2010-03-30 2017-12-25 Версеон Корпорейшн Мультизамещенные ароматические соединения в качестве ингибиторов тромбина
PH12012502551A1 (en) * 2010-06-28 2017-08-23 Bayer Ip Gmbh Heterocyclic compounds as agents for pest control
UY33476A (es) 2010-06-30 2012-02-29 Ironwood Pharmaceuticals Inc Estimuladores de sgc
RU2016101964A (ru) 2010-11-09 2018-11-21 Айронвуд Фармасьютикалз, Инк. СТИМУЛЯТОРЫ sGC
AU2012249421B9 (en) 2011-04-28 2015-10-22 Novartis Ag 17alpha-hydroxylase/C17,20-lyase inhibitors
WO2013009527A2 (en) 2011-07-08 2013-01-17 Merck Sharp & Dohme Corp. Factor ixa inhibitors
ES2882807T3 (es) 2011-09-16 2021-12-02 Novartis Ag Heterociclil carboxamidas N-sustituidas
EP3112363A1 (en) 2011-12-27 2017-01-04 Ironwood Pharmaceuticals, Inc. 2-[1-[(2-fluorophenyl)methyl]-5-(3-isoxazolyl)-1h-pyrazol-3-yl]-pyrimidine derivatives and related compounds as soluble guanylate cyclase (sgc) stimulators for the treatment of pulmonary hypertension
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
WO2014099695A1 (en) * 2012-12-19 2014-06-26 Merck Sharp & Dohme Corp. Factor ixa inhibitors
EP2934538B1 (en) 2012-12-19 2021-03-31 Merck Sharp & Dohme Corp. Factor ixa inhibitors
US9695198B2 (en) 2012-12-19 2017-07-04 Merck Sharp & Dohme Corp. Factor IXa inhibitors
US9951025B2 (en) 2013-03-15 2018-04-24 Verseon Corporation Halogenopyrazoles as inhibitors of thrombin
US9969724B2 (en) 2014-04-16 2018-05-15 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
US10189810B2 (en) 2014-09-17 2019-01-29 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
HRP20210484T1 (hr) 2014-12-04 2021-06-25 Procomcure Biotech Gmbh Antimikrobna sredstva koja se temelje na imidazolu
WO2016087615A1 (en) 2014-12-04 2016-06-09 Procomcure Biotech Gmbh Novel imidazole-based heterocyclic compounds
EP3258929B1 (en) 2015-02-16 2022-04-27 Merck Sharp & Dohme Corp. Factor ixa inhibitors
SI3261639T1 (sl) 2015-02-27 2023-01-31 Verseon International Corporation Substituirane pirazolne spojine kot zaviralci serinskih proteaz
WO2017175156A1 (en) * 2016-04-07 2017-10-12 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides useful as protein modulators
JOP20170083B1 (ar) * 2016-04-07 2022-03-14 Glaxosmithkline Ip Dev Ltd أميدات هتيروسيكلية مفيدة كمعدلات بروتين
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
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
WO2022081573A1 (en) * 2020-10-12 2022-04-21 University Of Tennessee Research Foundation Transient receptor potential canonical 3 inhibitors and methods of use thereof
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
ES2318899T3 (es) 1998-07-06 2009-05-01 Bristol-Myers Squibb Company Bifenil sulfonamidas como antagonistas duales de los receptores de angiotensina y endotelina.
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
TWI302913B (en) 2000-06-15 2008-11-11 Schering Corp Thrombin receptor antagonists
JP4307260B2 (ja) 2001-10-18 2009-08-05 シェーリング コーポレイション トロンビンレセプタアンタゴニストとしてのヒンバシン類似物
MXPA04003954A (es) * 2001-10-26 2004-11-29 Aventis Pharma Inc Bencimidazoles.
PT1495018E (pt) 2002-04-16 2008-02-19 Schering Corp Antagonistas tricíclicos de receptores de trombina
JP2007506741A (ja) * 2003-09-23 2007-03-22 メルク エンド カムパニー インコーポレーテッド 向代謝性グルタミン酸受容体のピラゾール系調節剤
CN1980665A (zh) * 2004-07-07 2007-06-13 默克公司 吡唑酰胺衍生物,包含这些化合物的组合物和使用方法
US7625938B2 (en) * 2004-07-22 2009-12-01 Merck & Co., Inc. Substituted pyrazoles, compositions containing such compounds and methods of use
AU2005287170B2 (en) * 2004-09-17 2012-03-29 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
WO2009140342A1 (en) * 2008-05-16 2009-11-19 Schering Corporation Glucagon receptor antagonists, compositions, and methods for their use

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110179795A (zh) * 2013-03-15 2019-08-30 维颂公司 作为丝氨酸蛋白酶抑制剂的多取代芳族化合物的制药用途
CN113015725A (zh) * 2018-04-17 2021-06-22 密歇根大学董事会 血小板功能抑制剂及其使用方法
CN113015725B (zh) * 2018-04-17 2024-08-13 密歇根大学董事会 血小板功能抑制剂及其使用方法
US12269805B2 (en) 2018-04-17 2025-04-08 The Regents Of The University Of Michigan Inhibitors of platelet function and methods for use of the same
CN116547279A (zh) * 2020-10-13 2023-08-04 加舒布鲁姆生物公司 杂环glp-1激动剂
CN114149371A (zh) * 2021-11-26 2022-03-08 首都医科大学 四取代吡唑类化合物及其应用
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

Also Published As

Publication number Publication date
AR071823A1 (es) 2010-07-14
TW201008930A (en) 2010-03-01
CL2009001214A1 (es) 2010-12-31
WO2009143039A2 (en) 2009-11-26
JP5504259B2 (ja) 2014-05-28
EP2805939A1 (en) 2014-11-26
EP2805939B1 (en) 2018-06-27
US8148363B2 (en) 2012-04-03
JP2011520967A (ja) 2011-07-21
US20110065682A1 (en) 2011-03-17
CA2724430A1 (en) 2009-11-26
MX2010012635A (es) 2010-12-06
WO2009143039A3 (en) 2010-07-08
EP2300435A2 (en) 2011-03-30
PE20091972A1 (es) 2010-01-15

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