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PE20091002A1 - Analogos dipeptidos como inhibidores del factor de coagulacion - Google Patents

Analogos dipeptidos como inhibidores del factor de coagulacion

Info

Publication number
PE20091002A1
PE20091002A1 PE2008001000A PE2008001000A PE20091002A1 PE 20091002 A1 PE20091002 A1 PE 20091002A1 PE 2008001000 A PE2008001000 A PE 2008001000A PE 2008001000 A PE2008001000 A PE 2008001000A PE 20091002 A1 PE20091002 A1 PE 20091002A1
Authority
PE
Peru
Prior art keywords
phenyl
chloro
compound
dipeptided
analogs
Prior art date
Application number
PE2008001000A
Other languages
English (en)
Inventor
Mimi L Quan
Ii Leon M Smith
Michael J Orwat
Paul J Gilligan
Donald J P Pinto
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 PE20091002A1 publication Critical patent/PE20091002A1/es

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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)
  • Cardiology (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)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (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)
  • Pyridine Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDO A UN COMPUESTO DE FORMULAS (I), (II), (III) DONDE A ES UN CARBOCICLO C3-C10 SUSTITUIDO CON 0-3 R1, HETEROCICLO DE 5-10 MIEMBROS; L1 ES -CH(R5)CH2C(O)NH-, -C(R5)=CHC(O)NH-, -C(R5)=C(R5)C(O)NH-, ENTRE OTROS; L2 ES -NHNHC(O)CH2-, -CH(R5)CH2NHC(O)-, ENTRE OTROS; M ES DE PREFERENCIA FENILO, CICLOHEXILO, PIRIMIDINILO, FURANILO, TIENILO, ENTRE OTROS; R1 ES =O, F, CL, ENTRE OTROS; R5 ES H, F, CF3, ENTRE OTROS; R11 ES HALOALQUILO C1-C4, METILO, NEOPENTILO, -CH2CONME, ENTRE OTROS; R12 ES H, F, ALQUILO C1-C4. SON COMPUESTOS PREFERIDOS: OXIDO DE (S,E)-4-(3-(4-CARBOXIFENILAMINO)-2-(3-(5-CLORO-2-(1H-TETRAZOL-1-IL)FENIL)ACRILAMINO)-3-OXOPROPIL)PIRIDINA; ACIDO (S,E)-4-(2-(3-CLORO-2-FLUORO-6-(1H-TETRAZOL-1-IL)FENIL)ACRILAMIDO)-3-(PIRIDIN-4-IL)PROPANAMIDO)BENZOICO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A UN PROCESO DE PREPARACION. DICHO COMPUESTO ES INHIBIDOR DEL FACTOR XIa Y/O CALICREINA PLASMATICA Y ES UTIL EN EL TRATAMIENTO O PROFILAXIS DE ENFERMEDADES TROMBOTICAS
PE2008001000A 2007-06-13 2008-06-11 Analogos dipeptidos como inhibidores del factor de coagulacion PE20091002A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US94379107P 2007-06-13 2007-06-13
US4951608P 2008-05-01 2008-05-01

Publications (1)

Publication Number Publication Date
PE20091002A1 true PE20091002A1 (es) 2009-07-15

Family

ID=39714076

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001000A PE20091002A1 (es) 2007-06-13 2008-06-11 Analogos dipeptidos como inhibidores del factor de coagulacion

Country Status (12)

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

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7632858B2 (en) 2002-11-15 2009-12-15 Bristol-Myers Squibb Company Open chain prolyl urea-related modulators of androgen receptor function
CN102026996B (zh) * 2008-03-13 2015-01-07 百时美施贵宝公司 作为凝血因子xia抑制剂的哒嗪衍生物
US20110281869A1 (en) * 2008-05-19 2011-11-17 Hamed Aissaoui Tetrahydroisoquinolines as antimalarial agents
US8664203B2 (en) * 2009-04-22 2014-03-04 Actelion Pharmaceuticals Ltd. Thiazole derivatives and their use as P2Y12 receptor antagonists
AU2011215898B2 (en) 2010-02-11 2016-08-11 Bristol-Myers Squibb Company 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
EP2766347B1 (en) 2011-10-14 2016-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
ES2625256T3 (es) 2011-10-14 2017-07-19 Bristol-Myers Squibb Company Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIA
ES2572908T3 (es) 2011-10-14 2016-06-03 Bristol-Myers Squibb Company 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
JP6220786B2 (ja) * 2012-07-19 2017-10-25 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
AU2013296259A1 (en) 2012-08-03 2015-03-19 Bristol-Myers Squibb Company Dihydropyridone P1 as factor XIa inhibitors
PT2882734T (pt) 2012-08-03 2016-12-09 Bristol Myers Squibb Co Di-hidropiridona pi como inibidores do fator xia
PE20150639A1 (es) 2012-10-12 2015-05-11 Bristol Myers Squibb Co Formas cristalinas de inhibidor del factor xia
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9738655B2 (en) 2013-03-25 2017-08-22 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors
WO2015054087A1 (en) * 2013-10-07 2015-04-16 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
PE20210470A1 (es) 2014-01-31 2021-03-08 Bristol Myers Squibb Co Macrociclos con grupos p2' heterociclicos como inhibidores del factor xia
NO2760821T3 (es) 2014-01-31 2018-03-10
US9676723B2 (en) 2014-02-11 2017-06-13 Merck Sharp & Dohme Corp Factor XIa inhibitors
US9944643B2 (en) 2014-02-11 2018-04-17 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US10093683B2 (en) 2014-04-22 2018-10-09 Merck Sharp & Dohme Corp. Factor XIa inhibitors
JP2017517512A (ja) * 2014-05-28 2017-06-29 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． 第ｘｉａ因子インヒビター
WO2016015593A1 (en) 2014-07-28 2016-02-04 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
WO2016018702A1 (en) 2014-07-28 2016-02-04 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
US10081623B2 (en) 2014-09-04 2018-09-25 Bristol-Myers Squibb Company Diamide macrocycles that are FXIa inhibitors
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
CN107106548A (zh) * 2015-01-20 2017-08-29 默沙东公司 因子XIa抑制剂
JP6668362B2 (ja) 2015-02-02 2020-03-18 フォーマ セラピューティクス，インコーポレイテッド Ｈｄａｃ阻害薬としての３−アルキル−４−アミド−二環式［４，５，０］ヒドロキサム酸
US10183934B2 (en) 2015-02-02 2019-01-22 Forma Therapeutics, Inc. Bicyclic [4,6,0] hydroxamic acids as HDAC inhibitors
EP3310777B1 (en) 2015-06-19 2019-10-09 Bristol-Myers Squibb Company Diamide macrocycles as factor xia inhibitors
EP3868753B1 (en) 2015-07-29 2022-12-21 Bristol-Myers Squibb Company Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group
ES2803659T3 (es) 2015-07-29 2021-01-28 Bristol Myers Squibb Co Inhibidores macrocíclicos del factor xia que contienen restos alquilo o cicloalquilo p2’
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
EP3368036B1 (en) * 2015-10-29 2022-07-20 Merck Sharp & Dohme LLC Macrocyclic pyridine-n-oxide derivatives as factor xia inhibitors
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
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
WO2018049068A1 (en) * 2016-09-07 2018-03-15 Pliant Therapeutics, Inc. N-acyl amino acid compounds and methods of use
EP4147698A1 (en) 2017-02-28 2023-03-15 Morphic Therapeutic, Inc. Inhibitors of (alpha-v)(beta-6) integrin
EP4159727A1 (en) 2017-02-28 2023-04-05 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
TW202035400A (zh) 2018-08-29 2020-10-01 美商莫菲克醫療股份有限公司 抑制αvβ6整合素
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
CN113195515B (zh) * 2018-10-29 2024-11-15 丽珠医药集团股份有限公司 新的二肽类化合物及其用途
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
JP7515481B2 (ja) 2018-12-19 2024-07-12 レオ ファーマ アクティーゼルスカブ Ｉｌ－１７の小分子調節物質としてのアミノ酸アニリド
CN114007602A (zh) * 2019-04-17 2022-02-01 科罗拉多研究合作伙伴有限责任公司 治疗果糖相关病症或疾病的新型化合物和使用方法
WO2021032933A1 (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
GEP20257771B (en) * 2020-09-17 2025-06-10 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
EP4284367A4 (en) * 2021-01-28 2024-11-27 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
CA2358581C (en) * 1999-01-02 2010-02-02 Aventis Pharma Deutschland Gmbh Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them
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
JP2005504003A (ja) * 2001-02-09 2005-02-10 メルク　エンド　カムパニー　インコーポレーテッド トロンビン阻害剤
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
US7217794B2 (en) * 2003-04-02 2007-05-15 Daiamed, Inc. Compounds and methods for treatment of thrombosis
WO2005040355A2 (en) * 2003-10-24 2005-05-06 Exelixis, Inc. Tao kinase modulators and methods 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
EP1841504B1 (en) 2005-01-13 2014-11-19 Bristol-Myers Squibb Company Substituted biaryl compounds as factor xia inhibitors
KR20080087817A (ko) * 2005-12-14 2008-10-01 브리스톨-마이어스 스큅 컴퍼니 인자 ｘｉａ 억제제로서 아릴프로피온아미드,아릴아크릴아미드, 아릴프로핀아미드 또는 아릴메틸우레아유사체
KR20080080173A (ko) 2005-12-14 2008-09-02 브리스톨-마이어스 스큅 컴퍼니 세린 프로테아제 억제제로서 유용한 6-원 헤테로사이클
US8466295B2 (en) 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
CA2681861A1 (en) * 2007-03-26 2008-10-16 Astellas Pharma Inc. Ornithine derivative

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EP2152664A1 (en) 2010-02-17
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JP5318094B2 (ja) 2013-10-16
US20100173899A1 (en) 2010-07-08
US8367709B2 (en) 2013-02-05
AR067329A1 (es) 2009-10-07
CL2008001724A1 (es) 2008-08-08
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MX2009012847A (es) 2009-12-08
CN101784516A (zh) 2010-07-21

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