CN101784516B - 作为凝血因子抑制剂的二肽类似物 - Google Patents

作为凝血因子抑制剂的二肽类似物 Download PDF

Info

Publication number
CN101784516B
CN101784516B CN200880103481.1A CN200880103481A CN101784516B CN 101784516 B CN101784516 B CN 101784516B CN 200880103481 A CN200880103481 A CN 200880103481A CN 101784516 B CN101784516 B CN 101784516B
Authority
CN
China
Prior art keywords
methyl
independently
turn
phenyl
ylmethyl
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.)
Expired - Fee Related
Application number
CN200880103481.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN101784516A (zh
Inventor
唐纳德·J·p·平托
米米·L·匡
利昂·M·史密斯二世
迈克尔·J·奥瓦特
保罗·J·吉利根
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.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN101784516A publication Critical patent/CN101784516A/zh
Application granted granted Critical
Publication of CN101784516B publication Critical patent/CN101784516B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • 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
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Cardiology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
CN200880103481.1A 2007-06-13 2008-06-11 作为凝血因子抑制剂的二肽类似物 Expired - Fee Related CN101784516B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US94379107P 2007-06-13 2007-06-13
US60/943,791 2007-06-13
US4951608P 2008-05-01 2008-05-01
US61/049,516 2008-05-01
PCT/US2008/066506 WO2008157162A1 (en) 2007-06-13 2008-06-11 Dipeptide analogs as coagulation factor inhibitors

Publications (2)

Publication Number Publication Date
CN101784516A CN101784516A (zh) 2010-07-21
CN101784516B true CN101784516B (zh) 2014-07-02

Family

ID=39714076

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200880103481.1A Expired - Fee Related CN101784516B (zh) 2007-06-13 2008-06-11 作为凝血因子抑制剂的二肽类似物

Country Status (12)

Country Link
US (1) US8367709B2 (enExample)
EP (1) EP2152664B1 (enExample)
JP (1) JP5318094B2 (enExample)
KR (1) KR20100037600A (enExample)
CN (1) CN101784516B (enExample)
AR (1) AR067329A1 (enExample)
AU (1) AU2008266228A1 (enExample)
CL (1) CL2008001724A1 (enExample)
MX (1) MX2009012847A (enExample)
PE (1) PE20091002A1 (enExample)
TW (1) TW200848024A (enExample)
WO (1) WO2008157162A1 (enExample)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003302084A1 (en) 2002-11-15 2004-06-15 Bristol-Myers Squibb Company Open chain prolyl urea-related modulators of androgen receptor function
JP5537442B2 (ja) * 2008-03-13 2014-07-02 ブリストル−マイヤーズ スクイブ カンパニー 第ｘｉａ因子阻害剤としてのピリダジン誘導体
WO2009141782A1 (en) * 2008-05-19 2009-11-26 Actelion Pharmaceuticals Ltd Tetrahydroisoquinolines as antimalarial agents
EP2421859B1 (en) * 2009-04-22 2014-04-09 Actelion Pharmaceuticals Ltd. Thiazole derivatives and their use as p2y12 receptor antagonists
PH12012501589A1 (en) 2010-02-11 2012-10-22 Bristol Myers Squibb Co Macrocycles as factor xia inhibitors
GB2494851A (en) * 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
TW201319068A (zh) 2011-08-05 2013-05-16 必治妥美雅史谷比公司 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑
TW201311689A (zh) 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
HRP20170784T8 (hr) 2011-10-14 2018-05-18 Bristol-Myers Squibb Company Supstituirani spojevi tetrahidroizohinolina kao inhbitori xia faktora
WO2013056034A1 (en) 2011-10-14 2013-04-18 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2899183B1 (en) 2011-10-14 2018-09-19 Bristol-Myers Squibb Company Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors
JP2015083542A (ja) * 2012-02-08 2015-04-30 大日本住友製薬株式会社 ３位置換プロリン誘導体
GB201209138D0 (en) * 2012-05-24 2012-07-04 Ono Pharmaceutical Co Compounds
CA2881566A1 (en) * 2012-07-19 2014-01-23 Yohei Ikuma 1-(cycloalkyl-carbonyl)proline derivative
WO2014022766A1 (en) 2012-08-03 2014-02-06 Bristol-Myers Squibb Company Dihydropyridone p1 as factor xia inhibitors
CN104507924B (zh) 2012-08-03 2018-01-23 百时美施贵宝公司 二氢吡啶酮p1作为凝血因子xia抑制剂
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
HRP20180465T1 (hr) 2012-10-12 2018-05-04 Bristol-Myers Squibb Company Kristalni oblici inhibitora faktora xia
JP6479763B2 (ja) 2013-03-25 2019-03-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン
US20160257668A1 (en) * 2013-10-07 2016-09-08 Merck Sharp & Dohme Corp. Factor XIa Inhibitors
UY35971A (es) 2014-01-31 2015-07-31 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Macrociclos con grupos p2? aromáticos como inhibidores del factor xia
NO2760821T3 (enExample) 2014-01-31 2018-03-10
EP3104703B1 (en) 2014-02-11 2020-11-18 Merck Sharp & Dohme Corp. Factor xia inhibitors
US9676723B2 (en) 2014-02-11 2017-06-13 Merck Sharp & Dohme Corp Factor XIa inhibitors
US10093683B2 (en) 2014-04-22 2018-10-09 Merck Sharp & Dohme Corp. Factor XIa inhibitors
RU2016150410A (ru) * 2014-05-28 2018-06-28 Мерк Шарп И Доум Корп. Ингибиторы фактора xia
EP3180317B1 (en) 2014-07-28 2021-04-14 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
US9975874B2 (en) 2014-07-28 2018-05-22 Merck Sharp & Dohme Corp. Factor XIa inhibitors
CN107074821B (zh) 2014-09-04 2020-05-22 百时美施贵宝公司 为fxia抑制剂的二酰胺大环化合物
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
CN105294669B (zh) * 2014-10-24 2019-01-22 山东凯森制药有限公司 一种第十因子抑制剂及其制备方法和应用
BR112017015431A2 (pt) * 2015-01-20 2018-01-16 Merck Sharp & Dohme composto, composição farmacêutica, métodos para inibir a formação de trombos no sangue ou tratar uma formação de trombos no sangue, para impedir a formação de trombos no sangue, para tratar tromboembolismo venoso e embolia pulmonar, para tratar trombose venosa profunda e para tratar ataque tromboembólico, e, uso de um composto
WO2016126726A1 (en) 2015-02-02 2016-08-11 Forma Therapeutics, Inc. Bicyclic [4,6,0] hydroxamic acids as hdac6 inhibitors
SG10202100916PA (en) 2015-02-02 2021-02-25 Valo Early Discovery Inc 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as hdac inhibitors
ES2762987T3 (es) 2015-06-19 2020-05-26 Bristol Myers Squibb Co Macrociclos de diamida como inhibidores del factor XIA
CN114874222B (zh) 2015-07-29 2025-06-06 百时美施贵宝公司 携带非芳族p2,基团的因子xia新大环
EP3328851B1 (en) 2015-07-29 2020-04-22 Bristol-Myers Squibb Company Factor xia macrocyclic inhibitors bearing alkyl or cycloalkyl p2' moieties
US10344039B2 (en) 2015-10-29 2019-07-09 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use
CN108430471B (zh) * 2015-10-29 2021-07-09 默沙东公司 因子XIa抑制剂
WO2017218950A1 (en) 2016-06-17 2017-12-21 Forma Therapeutics, Inc. 2-spiro-5- and 6-hydroxamic acid indanes as hdac inhibitors
IT201600074606A1 (it) * 2016-07-18 2018-01-18 Italfarmaco Spa New benzo-N-hydroxy amide compounds having antitumor activity
TW201808908A (zh) 2016-08-22 2018-03-16 美商默沙東藥廠 因子XIa抑制劑
TW201823208A (zh) 2016-09-07 2018-07-01 美商普萊恩醫療公司 N－醯基胺基酸化合物及其使用方法
CN116283977A (zh) 2017-02-28 2023-06-23 莫菲克医疗股份有限公司 αvβ6整合蛋白的抑制剂
EP3589285A4 (en) 2017-02-28 2020-08-12 Morphic Therapeutic, Inc. INHIBITORS OF INTEGRIN (ALPHA-V) (BETA-6)
TWI780281B (zh) * 2017-12-14 2022-10-11 丹麥商Ｎｍｄ藥品公司 用於治療神經肌肉病症的化合物
CN109928910B (zh) * 2017-12-19 2022-07-22 上海医药工业研究院 抗偏头痛药物阿莫曲坦的制备方法
SG11202101913PA (en) 2018-08-29 2021-03-30 Morphic Therapeutic Inc INHIBITING aV ß6 INTEGRIN
TW202028179A (zh) 2018-10-08 2020-08-01 美商普萊恩醫療公司 胺基酸化合物及使用方法
WO2020092139A1 (en) * 2018-10-29 2020-05-07 Huahai Us Inc. Novel dipeptide compounds and uses thereof
CN111138366B (zh) * 2018-11-06 2023-03-28 天津药物研究院有限公司 吡唑氨基甲酰类衍生物、及其制备方法和用途
NZ777871A (en) 2018-12-19 2024-11-29 Leo Pharma As Small molecule modulators of il-17
WO2020215022A1 (en) * 2019-04-17 2020-10-22 Colorado Research Partners, Llc Novel compounds and methods of use treating fructose-related disorders or diseases
CA3147564A1 (en) * 2019-08-21 2021-02-25 Kalvista Pharmaceuticals Limited Enzyme inhibitors
WO2021136390A1 (zh) * 2019-12-31 2021-07-08 上海京新生物医药有限公司 凝血因子XIa抑制剂
CN113943259A (zh) * 2020-07-17 2022-01-18 西安禾渼生物医药有限公司 一种氨基酸衍生物、其制备方法及应用
EP4214210B1 (en) * 2020-09-17 2025-04-09 Novartis AG Compounds and compositions as sppl2a inhibitors
CN112341398B (zh) * 2020-11-11 2022-05-03 湖北文理学院 具有生物活性的1,2,3-三氮唑取代的查尔酮衍生物、制备方法及其应用
CN117480164B (zh) * 2020-12-11 2024-07-05 上海领泰生物医药科技有限公司 凝血因子XIa抑制剂及其制备方法和应用
KR20230137378A (ko) * 2021-01-28 2023-10-04 머크 샤프 앤드 돔 엘엘씨 인자 xia 억제제
CN113636982A (zh) * 2021-04-28 2021-11-12 合肥工业大学 一种肉桂酸衍生物及其制备方法和用途
CN116655534A (zh) * 2023-06-07 2023-08-29 上海吉奉生物科技有限公司 一种Boc-3-（3-吡唑）- L -丙氨酸的合成方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007070826A1 (en) * 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1108819A (en) * 1964-07-31 1968-04-03 Rotta Research Lab Derivatives of 2-acylaminobicarboxylic acids and method for preparing same
DE3065190D1 (en) 1979-11-05 1983-11-10 Beecham Group Plc Enzyme derivatives, and their preparation
JPS611651A (ja) * 1984-06-12 1986-01-07 Toyama Chem Co Ltd Ｎ−アシル酸性アミノ酸ジアミド類およびその製造法並びにそれらを含有する抗潰瘍剤
IL81887A0 (en) * 1986-03-14 1987-10-20 Syntex Inc Dihydroisoxazole derivatives,their preparation and pharmaceutical compositions containing them
AU680870B2 (en) * 1993-04-28 1997-08-14 Astellas Pharma Inc. New heterocyclic compounds
JPH09169752A (ja) * 1995-02-14 1997-06-30 Mitsubishi Chem Corp 含酸素複素環誘導体
AR013079A1 (es) * 1997-05-06 2000-12-13 Smithkline Beecham Corp Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios
JP4191825B2 (ja) * 1998-09-10 2008-12-03 あすか製薬株式会社 ５−アミノイソキサゾール誘導体
CN1332723A (zh) * 1999-01-02 2002-01-23 阿文蒂斯药物德国有限公司 芳基链烷酰基衍生物、其制备方法、其用途和含有它们的药物组合物
US6362165B1 (en) * 1999-03-30 2002-03-26 Pharmacor Inc. Hydroxyphenyl derivatives with HIV integrase inhibitory properties
CA2321348A1 (en) * 2000-09-27 2002-03-27 Blaise Magloire N'zemba Aromatic derivatives with hiv integrase inhibitory properties
DE10063008A1 (de) * 2000-12-16 2002-06-20 Merck Patent Gmbh Carbonsäureamidderivate
WO2002064559A2 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
DE10124041A1 (de) * 2001-05-16 2002-11-21 Graffinity Pharm Design Gmbh Protease Inhibitoren
WO2004032834A2 (en) * 2002-10-04 2004-04-22 Merck & Co., Inc. Thrombin inhibitors
US20040180855A1 (en) 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
WO2004089297A2 (en) * 2003-04-02 2004-10-21 Suntory Pharmaceutical Research Laboratories, Llc Compounds and methods for treatment of thrombosis
US20070208166A1 (en) * 2003-10-24 2007-09-06 Exelixis, Inc. Tao Kinase Modulators And Method Of Use
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US7459564B2 (en) 2005-01-13 2008-12-02 Bristol-Myers Squibb Company Substituted biaryl compounds as factor XIa inhibitors
WO2007070818A1 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US8466295B2 (en) 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
JPWO2008123207A1 (ja) * 2007-03-26 2010-07-15 アステラス製薬株式会社 オルニチン誘導体

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007070826A1 (en) * 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors

Also Published As

Publication number Publication date
AU2008266228A1 (en) 2008-12-24
EP2152664A1 (en) 2010-02-17
AR067329A1 (es) 2009-10-07
EP2152664B1 (en) 2014-09-03
JP5318094B2 (ja) 2013-10-16
KR20100037600A (ko) 2010-04-09
JP2010529991A (ja) 2010-09-02
US8367709B2 (en) 2013-02-05
PE20091002A1 (es) 2009-07-15
US20100173899A1 (en) 2010-07-08
TW200848024A (en) 2008-12-16
CN101784516A (zh) 2010-07-21
CL2008001724A1 (es) 2008-08-08
WO2008157162A1 (en) 2008-12-24
MX2009012847A (es) 2009-12-08

Similar Documents

Publication Publication Date Title
CN101784516B (zh) 作为凝血因子抑制剂的二肽类似物
CN102026996B (zh) 作为凝血因子xia抑制剂的哒嗪衍生物
US10208021B2 (en) Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
CN106795161B (zh) 作为因子xia抑制剂的嘧啶酮
CN104507924B (zh) 二氢吡啶酮p1作为凝血因子xia抑制剂
CN105228996A (zh) 作为因子XIa抑制剂的含取代唑类的四氢异喹啉
CN101631784A (zh) 用作抗凝血药的二环内酰胺凝血因子viia抑制剂
CN107849026A (zh) 携带烷基或环烷基p2,部分的因子xia大环抑制剂
EP3328852B1 (en) Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group
CN101006063B (zh) 用作丝氨酸蛋白酶抑制剂的五元杂环类化合物
NZ624874B2 (en) Substituted tetrahydroisoquinoline compounds as factor xia inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20140702

Termination date: 20200611

CF01 Termination of patent right due to non-payment of annual fee