JP5318094B2 - 凝固因子阻害剤としてのジペプチド類似体 - Google Patents

凝固因子阻害剤としてのジペプチド類似体 Download PDF

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Publication number
JP5318094B2
JP5318094B2 JP2010512311A JP2010512311A JP5318094B2 JP 5318094 B2 JP5318094 B2 JP 5318094B2 JP 2010512311 A JP2010512311 A JP 2010512311A JP 2010512311 A JP2010512311 A JP 2010512311A JP 5318094 B2 JP5318094 B2 JP 5318094B2
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methyl
substituted
ylmethyl
alkyl
nhco
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JP2010529991A5 (enExample
JP2010529991A (ja
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ドナルド・ジェイ・ピー・ピント
ミミ・エル・クワン
レオン・エム・スミス・ザ・セカンド
マイケル・ジェイ・オーワット
ポール・ジェイ・ギリガン
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Bristol Myers Squibb Co
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (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)
  • Animal Behavior & Ethology (AREA)
  • Cardiology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
JP2010512311A 2007-06-13 2008-06-11 凝固因子阻害剤としてのジペプチド類似体 Expired - Fee Related JP5318094B2 (ja)

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 (3)

Publication Number Publication Date
JP2010529991A JP2010529991A (ja) 2010-09-02
JP2010529991A5 JP2010529991A5 (enExample) 2010-11-04
JP5318094B2 true JP5318094B2 (ja) 2013-10-16

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JP2010512311A Expired - Fee Related JP5318094B2 (ja) 2007-06-13 2008-06-11 凝固因子阻害剤としてのジペプチド類似体

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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
ATE543811T1 (de) * 2008-03-13 2012-02-15 Bristol Myers Squibb Co Pyridazinderivate als faktor-xia-inhibitoren
BRPI0912871A2 (pt) * 2008-05-19 2015-10-20 Actelion Pharmaceuticals Ltd novas tetraidroisoquinolinas como agentes antimaláricos.
CN102405220B (zh) * 2009-04-22 2015-05-27 埃科特莱茵药品有限公司 噻唑衍生物及其作为p2y12受体拮抗剂的用途
KR101843542B1 (ko) 2010-02-11 2018-03-30 브리스톨-마이어스 스큅 컴퍼니 인자 ＸＩａ 억제제로서의 마크로사이클
GB2494851A (en) * 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
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
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
EP2766347B1 (en) * 2011-10-14 2016-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
JP6033317B2 (ja) 2011-10-14 2016-11-30 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テトラヒドロイソキノリン化合物
UY34393A (es) 2011-10-14 2013-04-30 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor xia
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
WO2014014050A1 (ja) * 2012-07-19 2014-01-23 大日本住友製薬株式会社 １－（シクロアルキルカルボニル）プロリン誘導体
BR112015002081A2 (pt) 2012-08-03 2017-07-04 Bristol Myers Squibb Co di-hidropiridona p1 como inibidores de fator xia
EA025392B1 (ru) 2012-08-03 2016-12-30 Бристол-Маерс Сквибб Компани Дигидропиридон р1 в качестве ингибиторов фактора xia
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014059202A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EA032092B1 (ru) 2012-10-12 2019-04-30 Бристол-Майерс Сквибб Компани Кристаллические формы ингибитора фактора xia
EP2978751B1 (en) 2013-03-25 2018-12-05 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
US20160257668A1 (en) * 2013-10-07 2016-09-08 Merck Sharp & Dohme Corp. Factor XIa Inhibitors
NO2760821T3 (enExample) 2014-01-31 2018-03-10
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
EP3104702B1 (en) 2014-02-11 2022-08-10 Merck Sharp & Dohme LLC Factor xia inhibitors
EP3104703B1 (en) 2014-02-11 2020-11-18 Merck Sharp & Dohme Corp. Factor xia inhibitors
EP3134408B1 (en) 2014-04-22 2020-08-12 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
CN106413710A (zh) * 2014-05-28 2017-02-15 默沙东公司 因子XIa抑制剂
US9975874B2 (en) 2014-07-28 2018-05-22 Merck Sharp & Dohme Corp. Factor XIa inhibitors
EP3180317B1 (en) 2014-07-28 2021-04-14 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
WO2016118403A1 (en) * 2015-01-20 2016-07-28 Merck Sharp & Dohme Corp. Factor xia inhibitors
US10239845B2 (en) 2015-02-02 2019-03-26 Forma Therapeutics, Inc. 3-aryl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors
US10183934B2 (en) 2015-02-02 2019-01-22 Forma Therapeutics, Inc. Bicyclic [4,6,0] hydroxamic acids as HDAC inhibitors
CN108026083B (zh) 2015-06-19 2021-08-27 百时美施贵宝公司 作为因子xia抑制剂的二酰胺大环
JP6629958B2 (ja) 2015-07-29 2020-01-15 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤
EP3868753B1 (en) 2015-07-29 2022-12-21 Bristol-Myers Squibb Company Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group
EP3371162B1 (en) 2015-10-29 2022-01-26 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
MA43128A (fr) 2015-10-29 2018-09-05 Merck Sharp & Dohme Inhibiteurs du facteur xia
EP3472131B1 (en) 2016-06-17 2020-02-19 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
US10143681B2 (en) 2016-08-22 2018-12-04 Merck Sharp & Dohme Corp. Factor XIa inhibitors
CN109996541A (zh) * 2016-09-07 2019-07-09 普利安特治疗公司 N-酰基氨基酸化合物及其使用方法
TW201835078A (zh) 2017-02-28 2018-10-01 美商萊築理公司 αvβ6整合蛋白之抑制劑
AU2018227417B2 (en) 2017-02-28 2021-12-23 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
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
EP4086254B1 (en) 2018-08-29 2024-12-18 Morphic Therapeutic, Inc. Integrin inhibitors
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
US12209141B2 (en) * 2018-10-29 2025-01-28 Shanghai Synergy Pharmaceutical Sciences, Ltd. 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
US20220194939A1 (en) * 2019-04-17 2022-06-23 Colorado Research Partners, Llc Novel compounds and methods of use treating fructose-related disorders or diseases
JP2022552048A (ja) * 2019-08-21 2022-12-15 カルビスタ・ファーマシューティカルズ・リミテッド 酵素阻害剤
CN115066417B (zh) * 2019-12-31 2025-05-02 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
CN116615425A (zh) * 2020-09-17 2023-08-18 诺华股份有限公司 作为Sppl2a抑制剂的化合物和组合物
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
WO2022122035A1 (zh) * 2020-12-11 2022-06-16 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
WO2022164735A1 (en) * 2021-01-28 2022-08-04 Merck Sharp & Dohme Llc Factor xia inhibitors
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

Family Cites Families (25)

* 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
HU201032B (en) * 1986-03-14 1990-09-28 Syntex Inc Process for production of izoxasoles hindering transglumatinase and medical 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
BR9916733A (pt) * 1999-01-02 2001-09-25 Aventis Pharma Gmbh Derivados de arilalcanoìla, processos para sua preparação, seu uso e composições farmacêuticas que os contêm
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
US7144899B2 (en) 2001-02-09 2006-12-05 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
WO2004103270A2 (en) * 2003-04-02 2004-12-02 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
US7453002B2 (en) * 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US7429604B2 (en) * 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
CN101137412B (zh) * 2005-01-13 2012-11-07 布里斯托尔-迈尔斯·斯奎布公司 用作凝血因子XIa抑制剂的取代的二芳基化合物
US8466295B2 (en) * 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
US8163749B2 (en) * 2005-12-14 2012-04-24 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
NZ568595A (en) * 2005-12-14 2010-04-30 Bristol Myers Squibb Co Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor Xla inhibitors
MX2009010297A (es) * 2007-03-26 2009-10-12 Astellas Pharma Inc Derivado de ornitina.

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US8367709B2 (en) 2013-02-05
CN101784516B (zh) 2014-07-02
MX2009012847A (es) 2009-12-08
US20100173899A1 (en) 2010-07-08
EP2152664A1 (en) 2010-02-17
AR067329A1 (es) 2009-10-07
AU2008266228A1 (en) 2008-12-24
KR20100037600A (ko) 2010-04-09
TW200848024A (en) 2008-12-16
WO2008157162A1 (en) 2008-12-24
CN101784516A (zh) 2010-07-21
JP2010529991A (ja) 2010-09-02
CL2008001724A1 (es) 2008-08-08
PE20091002A1 (es) 2009-07-15

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