JP6742348B2 - 第xia因子阻害剤としてのジアミド大員環 - Google Patents

第xia因子阻害剤としてのジアミド大員環 Download PDF

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Publication number
JP6742348B2
JP6742348B2 JP2017565810A JP2017565810A JP6742348B2 JP 6742348 B2 JP6742348 B2 JP 6742348B2 JP 2017565810 A JP2017565810 A JP 2017565810A JP 2017565810 A JP2017565810 A JP 2017565810A JP 6742348 B2 JP6742348 B2 JP 6742348B2
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substituted
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alkyl
chloro
phenyl
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JP2018517753A (ja
JP2018517753A5 (enExample
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レオン・エム・スミス・ザ・セカンド
ドナルド・ジェイ・ピー・ピント
ジェイムズ・アール・コート
ウィリアム・アール・ユーイング
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2017565810A 2015-06-19 2016-06-16 第xia因子阻害剤としてのジアミド大員環 Active JP6742348B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562181875P 2015-06-19 2015-06-19
US62/181,875 2015-06-19
PCT/US2016/037823 WO2016205482A1 (en) 2015-06-19 2016-06-16 Diamide macrocycles as factor xia inhibitors

Publications (3)

Publication Number Publication Date
JP2018517753A JP2018517753A (ja) 2018-07-05
JP2018517753A5 JP2018517753A5 (enExample) 2019-06-20
JP6742348B2 true JP6742348B2 (ja) 2020-08-19

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JP2017565810A Active JP6742348B2 (ja) 2015-06-19 2016-06-16 第xia因子阻害剤としてのジアミド大員環

Country Status (6)

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US (1) US10160750B2 (enExample)
EP (1) EP3310777B1 (enExample)
JP (1) JP6742348B2 (enExample)
CN (1) CN108026083B (enExample)
ES (1) ES2762987T3 (enExample)
WO (1) WO2016205482A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
US10752641B2 (en) 2016-03-02 2020-08-25 Bristol-Myers Squibb Company Diamide macrocycles having factor XIa inhibiting activity
CN113166099A (zh) * 2018-12-17 2021-07-23 拜耳公司 用于治疗和/或预防血栓形成性或血栓栓塞性疾病和/或血栓形成性或血栓栓塞性并发症的取代的氧代吡啶衍生物
WO2021110076A1 (zh) * 2019-12-04 2021-06-10 深圳信立泰药业股份有限公司 草酰胺类衍生物、其制备方法及其在医药上的应用

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PE121699A1 (es) 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
ZA985247B (en) 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
AU5546000A (en) 1999-06-14 2001-01-02 Protherics Molecular Design Limited Compounds
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
AR035216A1 (es) 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
HRP20080382A2 (en) 2001-09-21 2008-12-31 Bristol-Myers Squibb Company A Delaware (Usa) Corporation LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR Xa INHIBITORS
US20040180855A1 (en) 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
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
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
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
WO2006089005A2 (en) 2005-02-17 2006-08-24 Bristol-Myers Squibb Company Combination of selective factor viia and/or xia and plasma kallikrein inhibitors
US8466295B2 (en) 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
NZ568595A (en) 2005-12-14 2010-04-30 Bristol Myers Squibb Co Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor Xla inhibitors
US8163749B2 (en) 2005-12-14 2012-04-24 Bristol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
PE20071132A1 (es) * 2005-12-23 2007-12-14 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
US8410155B2 (en) 2006-12-15 2013-04-02 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIA inhibitors
CA2676933C (en) 2007-02-28 2015-09-29 Leo Pharma A/S Novel phosphodiesterase inhibitors
MX2009012847A (es) 2007-06-13 2009-12-08 Bristol Myers Squibb Co Analogos dipeptidicos como inhibidores de factores de coagulacion.
ATE543811T1 (de) 2008-03-13 2012-02-15 Bristol Myers Squibb Co Pyridazinderivate als faktor-xia-inhibitoren
FR2944014A1 (fr) 2009-04-06 2010-10-08 Univ Grenoble 1 Peptides cycliques a activite antiparasitaire
KR101843542B1 (ko) 2010-02-11 2018-03-30 브리스톨-마이어스 스큅 컴퍼니 인자 XIa 억제제로서의 마크로사이클
EP2603080A4 (en) 2010-08-12 2014-01-22 Enanta Pharm Inc HEPATITIS C-VIRUS HEMMER
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
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
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
EP2766347B1 (en) 2011-10-14 2016-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
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
WO2014160592A2 (en) * 2013-03-27 2014-10-02 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
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
NO2721243T3 (enExample) 2014-10-01 2018-10-20
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
EP3868753B1 (en) 2015-07-29 2022-12-21 Bristol-Myers Squibb Company Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group
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
KR102697816B1 (ko) 2015-08-05 2024-08-21 브리스톨-마이어스 스큅 컴퍼니 신규 치환된 글리신 유도된 fxia 억제제
US10752641B2 (en) 2016-03-02 2020-08-25 Bristol-Myers Squibb Company Diamide macrocycles having factor XIa inhibiting activity

Also Published As

Publication number Publication date
JP2018517753A (ja) 2018-07-05
US10160750B2 (en) 2018-12-25
EP3310777A1 (en) 2018-04-25
CN108026083A (zh) 2018-05-11
EP3310777B1 (en) 2019-10-09
CN108026083B (zh) 2021-08-27
WO2016205482A1 (en) 2016-12-22
ES2762987T3 (es) 2020-05-26
US20180141932A1 (en) 2018-05-24

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