JP6526796B2 - Ｆｘｉａ阻害剤であるジアミドマクロ環 - Google Patents

Ｆｘｉａ阻害剤であるジアミドマクロ環 Download PDF

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Publication number
JP6526796B2
JP6526796B2 JP2017512780A JP2017512780A JP6526796B2 JP 6526796 B2 JP6526796 B2 JP 6526796B2 JP 2017512780 A JP2017512780 A JP 2017512780A JP 2017512780 A JP2017512780 A JP 2017512780A JP 6526796 B2 JP6526796 B2 JP 6526796B2
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alkyl
methyl
dioxo
benzodiazacyclododecin
nhco
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JP2017525744A5 (OSRAM
JP2017525744A (ja
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シ・ジュン
ウィリアム・アール・ユーイング
ローラ・ニールセン
ジルン・フー
ミミ・エル・クワン
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Bristol Myers Squibb Co
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P9/10—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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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

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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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2017512780A 2014-09-04 2015-09-03 Ｆｘｉａ阻害剤であるジアミドマクロ環 Active JP6526796B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462045589P 2014-09-04 2014-09-04
US62/045,589 2014-09-04
PCT/US2015/048212 WO2016036893A1 (en) 2014-09-04 2015-09-03 Diamide macrocycles that are fxia inhibitors

Publications (3)

Publication Number Publication Date
JP2017525744A JP2017525744A (ja) 2017-09-07
JP2017525744A5 JP2017525744A5 (OSRAM) 2018-10-11
JP6526796B2 true JP6526796B2 (ja) 2019-06-05

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Country Status (6)

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US (1) US10081623B2 (OSRAM)
EP (1) EP3189047B1 (OSRAM)
JP (1) JP6526796B2 (OSRAM)
CN (1) CN107074821B (OSRAM)
ES (1) ES2714283T3 (OSRAM)
WO (1) WO2016036893A1 (OSRAM)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2019507167A (ja) 2016-03-02 2019-03-14 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因子阻害活性を有するジアミド大員環
EP3426674A4 (en) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
US11292801B2 (en) 2016-07-05 2022-04-05 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
TW201808908A (zh) 2016-08-22 2018-03-16 美商默沙東藥廠 因子XIa抑制劑
AU2017336523B2 (en) 2016-09-28 2022-07-21 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
CN112778273B (zh) * 2019-11-11 2022-08-23 江西济民可信集团有限公司 环酮并吡啶酮类化合物及其制备方法和用途
CN113135930B (zh) * 2020-01-17 2023-11-17 上海济煜医药科技有限公司 呋喃并吡啶酮咪唑化合物及其制备方法和用途
CN114085223B (zh) * 2020-08-25 2025-04-04 黄河科技学院 一类大环小分子pcsk9蛋白抑制剂

Family Cites Families (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1525186A (fr) 1967-03-29 1968-05-17 Roussel Uclaf Nouvelles pénicillines et procédé de préparation
DE4034829A1 (de) 1990-11-02 1992-05-07 Merck Patent Gmbh Cyclopeptide
JP3190431B2 (ja) 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
GB9206757D0 (en) 1992-03-27 1992-05-13 Ferring Bv Novel peptide receptor ligands
WO1996034010A2 (en) 1995-03-29 1996-10-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5624936A (en) 1995-03-29 1997-04-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2249617A1 (en) 1996-04-03 1997-10-09 S. Jane Desolms Inhibitors of farnesyl-protein transferase
US5869682A (en) 1996-04-03 1999-02-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
TW557297B (en) 1997-09-26 2003-10-11 Abbott Lab Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
RU2274642C2 (ru) 1998-03-19 2006-04-20 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы каспаз
ES2310039T3 (es) 1998-05-26 2008-12-16 Warner-Lambert Company Llc Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular.
US6307049B1 (en) 1998-09-30 2001-10-23 The Procter & Gamble Co. Heterocyclic 2-substituted ketoamides
AU3043100A (en) 1999-01-02 2000-07-24 Aventis Pharma Deutschland Gmbh Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor xa activity)
EP1016663A1 (en) 1999-01-02 2000-07-05 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity)
AU4111700A (en) 1999-04-09 2000-11-14 Basf Aktiengesellschaft Low-molecular inhibitors of complement proteases
EP1125925A1 (en) 2000-02-15 2001-08-22 Applied Research Systems ARS Holding N.V. Amine derivatives for the treatment of apoptosis
JP2004507456A (ja) 2000-05-11 2004-03-11 ブリストル−マイヤーズ　スクイブ　カンパニー 成長ホルモン分泌促進薬として有用なテトラヒドロイソキノリン類縁体
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
WO2003011222A2 (en) 2001-07-27 2003-02-13 Merck & Co., Inc. Thrombin inhibitors
US6951840B2 (en) 2001-08-31 2005-10-04 Eli Lilly And Company Lipoglycopeptide antibiotics
WO2003041641A2 (en) 2001-11-09 2003-05-22 Bristol-Myers Squibb Company Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
AU2002316317A1 (en) 2002-06-18 2003-12-31 The Scripps Research Institute Synthesis of diazonamide "a" core
US7138412B2 (en) 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
CN1832920A (zh) 2003-08-08 2006-09-13 特兰斯泰克制药公司 芳基和杂芳基化合物,组合物及其使用方法
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic 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
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US20100190688A1 (en) 2004-07-12 2010-07-29 Bin Chao Tetrapeptide analogs
US7459564B2 (en) 2005-01-13 2008-12-02 Bristol-Myers Squibb Company Substituted biaryl compounds as factor XIa inhibitors
US20060183771A1 (en) 2005-02-17 2006-08-17 Seiffert Dietmar A Novel combination of selective factor VIIa and/or factor XIa inhibitors and selective plasma kallikrein inhibitors
US20080214495A1 (en) * 2005-07-08 2008-09-04 Astrazeneca Ab Heterocyclic Sulfonamide Derivatives as Inhibitors of Factor Xa
US20070111947A1 (en) 2005-10-14 2007-05-17 Mcmurry Thomas J Fibrin targeted therapeutics
CA2627426A1 (en) 2005-11-11 2007-05-18 Markus Boehringer Carbocyclic fused cyclic amines as inhibitors of the coagulation factor xa
US8466295B2 (en) 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
WO2007070818A1 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
CA2633252A1 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
TW200745062A (en) * 2005-12-23 2007-12-16 Bristol Myers Squibb Co Macrocyclic factor VIIA inhibitors useful as anticoagulants
JP5342450B2 (ja) 2006-12-15 2013-11-13 ブリストル−マイヤーズ スクイブ カンパニー 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ
PE20081775A1 (es) 2006-12-20 2008-12-18 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
CN101784516B (zh) 2007-06-13 2014-07-02 百时美施贵宝公司 作为凝血因子抑制剂的二肽类似物
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
US8624040B2 (en) 2009-06-22 2014-01-07 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
US8513433B2 (en) 2009-07-02 2013-08-20 Angion Biomedica Corp. Small molecule inhibitors of PARP activity
WO2011017296A1 (en) 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
PH12012501589A1 (en) * 2010-02-11 2012-10-22 Bristol Myers Squibb Co Macrocycles as factor xia inhibitors
WO2013009527A2 (en) 2011-07-08 2013-01-17 Merck Sharp & Dohme Corp. Factor ixa 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
WO2013056034A1 (en) 2011-10-14 2013-04-18 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
HRP20170784T8 (hr) 2011-10-14 2018-05-18 Bristol-Myers Squibb Company Supstituirani spojevi tetrahidroizohinolina kao inhbitori xia faktora
EP2899183B1 (en) 2011-10-14 2018-09-19 Bristol-Myers Squibb Company Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors
JP6137193B2 (ja) 2011-12-21 2017-05-31 小野薬品工業株式会社 第ＸＩａ因子阻害剤としての新規ピリジノンおよびピリミジノン誘導体
GB2497806A (en) 2011-12-21 2013-06-26 Ono Pharmaceutical Co Pyridinone and pyrimidinone derivatives as factor XIa inhibitors
WO2013111107A1 (en) 2012-01-27 2013-08-01 Novartis Ag Aminopyridine derivatives as plasma kallikrein inhibitors
EP2807157A1 (en) 2012-01-27 2014-12-03 Novartis AG 5-membered heteroarylcarboxamide derivatives as plasma kallikrein 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
SI2847228T1 (sl) 2012-05-10 2018-11-30 Bayer Pharma Aktiengesellschaft Protitelesa zmožna vezave na faktor koagulacije XI in/ali njeno aktivirano obliko faktor XIa in njihove uporabe
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
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
WO2014022766A1 (en) 2012-08-03 2014-02-06 Bristol-Myers Squibb Company Dihydropyridone p1 as factor xia inhibitors
HRP20180465T1 (hr) 2012-10-12 2018-05-04 Bristol-Myers Squibb Company Kristalni oblici inhibitora faktora xia
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
US9708308B2 (en) 2012-12-19 2017-07-18 Merck Sharp Dohme Corp. Factor IXa inhibitors
GB201300304D0 (en) 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
GB2510407A (en) 2013-02-04 2014-08-06 Kalvista Pharmaceuticals Ltd Aqueous suspensions of kallikrein inhibitors for parenteral administration
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
TWI633089B (zh) 2013-03-28 2018-08-21 拜耳製藥股份有限公司 經取代的酮基吡啶衍生物
WO2015011087A1 (de) 2013-07-23 2015-01-29 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate und ihre verwendung als faktor xia / plasma
TW201605810A (zh) 2013-09-26 2016-02-16 拜耳製藥股份有限公司 經取代苯丙胺酸衍生物（二）
US20160237045A1 (en) 2013-09-26 2016-08-18 Bayer Pharma Aktiengesellschaft Substituted phenylalanine derivatives
US20160280699A1 (en) 2013-09-26 2016-09-29 Bayer Pharma Aktiengesellschaft Substituted phenylalanine derivatives
AR097754A1 (es) 2013-09-26 2016-04-13 Bayer Pharma AG Derivados sustituidos de fenilalanina
AR097755A1 (es) 2013-09-26 2016-04-13 Bayer Pharma AG Derivados sustituidos de fenilalanina como moduladores del factor xia
WO2015044167A1 (de) 2013-09-26 2015-04-02 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate als faktor xia modulatoren
EP3049408A1 (de) 2013-09-26 2016-08-03 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate
EP3049406A1 (de) 2013-09-26 2016-08-03 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate und ihre verwendung zur behandlung von thrombotischen / thromboembolischen erkrankungen
WO2015047973A1 (en) 2013-09-27 2015-04-02 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
US20160257668A1 (en) 2013-10-07 2016-09-08 Merck Sharp & Dohme Corp. Factor XIa Inhibitors
JP6337750B2 (ja) 2013-11-22 2018-06-06 小野薬品工業株式会社 化合物
AU2014378428A1 (en) 2014-01-14 2016-09-01 Sumitomo Dainippon Pharma Co., Ltd. Condensed 5-oxazolidinone derivative
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 (OSRAM) 2014-01-31 2018-03-10
JP6382997B2 (ja) 2014-02-07 2018-08-29 エクセセーラ ファーマシューティカルズ インコーポレイテッド 治療用化合物および組成物
US9676723B2 (en) 2014-02-11 2017-06-13 Merck Sharp & Dohme Corp Factor XIa inhibitors
WO2015123090A1 (en) 2014-02-11 2015-08-20 Merck Sharp & Dohme Corp. Factor xia inhibitors
EP3104703B1 (en) 2014-02-11 2020-11-18 Merck Sharp & Dohme Corp. Factor xia inhibitors
WO2015120777A1 (zh) 2014-02-14 2015-08-20 四川海思科制药有限公司 一种吡啶酮或嘧啶酮衍生物、及其制备方法和应用
DK3113772T3 (da) 2014-03-07 2020-12-07 Biocryst Pharm Inc Trifluormethylsubstituerede pyrazoler som inhibitorer af kallikrein fra humant plasma
US9969724B2 (en) 2014-04-16 2018-05-15 Merck Sharp & Dohme Corp. Factor IXa inhibitors
US9808445B2 (en) 2014-04-16 2017-11-07 Merck Sharp & Dohme Corp. Factor IXa inhibitors
KR20150136294A (ko) 2014-05-27 2015-12-07 주식회사 레고켐 바이오사이언스 인자 ＸＩａ 억제 활성을 가지는 신규한 화합물
RU2016150410A (ru) 2014-05-28 2018-06-28 Мерк Шарп И Доум Корп. Ингибиторы фактора xia
ES2712886T3 (es) 2014-09-24 2019-05-16 Bayer Pharma AG Derivados de piridobenzazepina y piridobenzazocina que inhiben el factor XIa
NO2721243T3 (OSRAM) 2014-10-01 2018-10-20
JP6610562B2 (ja) 2014-12-10 2019-11-27 小野薬品工業株式会社 ジヒドロインドリジノン誘導体

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CN107074821B (zh) 2020-05-22
CN107074821A (zh) 2017-08-18
US10081623B2 (en) 2018-09-25
WO2016036893A1 (en) 2016-03-10
US20170283403A1 (en) 2017-10-05
EP3189047A1 (en) 2017-07-12
ES2714283T3 (es) 2019-05-28
JP2017525744A (ja) 2017-09-07
EP3189047B1 (en) 2018-12-26

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