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

Info

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
Authority
JP
Japan
Prior art keywords
substituted
independently
alkyl
chloro
phenyl
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.)
Active
Application number
JP2017565810A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018517753A (ja
JP2018517753A5 (enExample
Inventor
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
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 JP2018517753A publication Critical patent/JP2018517753A/ja
Publication of JP2018517753A5 publication Critical patent/JP2018517753A5/ja
Application granted granted Critical
Publication of JP6742348B2 publication Critical patent/JP6742348B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D403/14—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 three or more hetero 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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

Landscapes

  • 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

Family

ID=56204067

Family Applications (1)

Application Number Title Priority Date Filing Date
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)

Country Link
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
NO2760821T3 (enExample) 2014-01-31 2018-03-10
KR20240017118A (ko) 2014-01-31 2024-02-06 브리스톨-마이어스 스큅 컴퍼니 인자 XIa 억제제로서의 헤테로시클릭 P2' 기를 갖는 마크로사이클
JP6742348B2 (ja) 2015-06-19 2020-08-19 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ジアミド大員環
US10676477B2 (en) 2015-07-29 2020-06-09 Bristol-Myers Squibb Company Factor XIa macrocycle 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
WO2017151746A1 (en) 2016-03-02 2017-09-08 Bristol-Myers Squibb Company Diamide macrocycles having factor xia inhibiting activity
CA3123324A1 (en) * 2018-12-17 2020-06-25 Bayer Aktiengesellschaft Substituted oxopyridine derivatives for the treatment and/or prophylaxis of thrombotic or thromboembolic disorders and/or thrombotic or thromboembolic complications
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

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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.
WO2000077027A2 (en) 1999-06-14 2000-12-21 Tularik Limited Serine protease inhibitors
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
EP1427415B1 (en) 2001-09-21 2009-08-12 Brystol-Myers Squibb Company 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
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
JP5236293B2 (ja) 2005-01-13 2013-07-17 ブリストル−マイヤーズ スクイブ カンパニー Ｘｉａ因子阻害剤としての置換ビアリール化合物
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
EP1981854B1 (en) 2005-12-14 2011-06-01 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
US8466295B2 (en) 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
AU2006325746A1 (en) 2005-12-14 2007-06-21 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
EP2102189B1 (en) 2006-12-15 2015-07-29 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors
KR101571654B1 (ko) 2007-02-28 2015-11-25 레오 파마 에이/에스 신규한 포스포디에스테라제 억제제
EP2152664B1 (en) 2007-06-13 2014-09-03 Bristol-Myers Squibb Company Dipeptide analogs as coagulation factor inhibitors
EP2265601B1 (en) 2008-03-13 2012-02-01 Bristol-Myers Squibb Company Pyridazine derivatives as factor xia inhibitors
FR2944014A1 (fr) 2009-04-06 2010-10-08 Univ Grenoble 1 Peptides cycliques a activite antiparasitaire
CA2789622C (en) 2010-02-11 2018-04-03 Bristol-Myers Squibb Company Macrocycles as factor xia inhibitors
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
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
SI2766346T1 (sl) 2011-10-14 2017-05-31 Bristol-Myers Squibb Company Substituirane tetrahidroizokinolinske spojine kot faktor xia inhibitorji
LT2882734T (lt) 2012-08-03 2016-12-12 Bristol-Myers Squibb Company Dihidropiridonai, kaip xia faktoriaus slopikliai
PT2880026T (pt) * 2012-08-03 2017-05-03 Bristol Myers Squibb Co Dihidropiridona p1 como inibidores de fator xia
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2906551B1 (en) 2012-10-12 2018-02-28 Bristol-Myers Squibb Company Crystalline forms of a factor xia inhibitor
EP2978751B1 (en) 2013-03-25 2018-12-05 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
US9809545B2 (en) * 2013-03-27 2017-11-07 Merck Sharp & Dohme Corp. Factor XIa inhibitors
NO2760821T3 (enExample) 2014-01-31 2018-03-10
KR20240017118A (ko) 2014-01-31 2024-02-06 브리스톨-마이어스 스큅 컴퍼니 인자 XIa 억제제로서의 헤테로시클릭 P2' 기를 갖는 마크로사이클
EP3189047B1 (en) 2014-09-04 2018-12-26 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
NO2721243T3 (enExample) 2014-10-01 2018-10-20
JP6742348B2 (ja) 2015-06-19 2020-08-19 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ジアミド大員環
US10676477B2 (en) 2015-07-29 2020-06-09 Bristol-Myers Squibb Company Factor XIa macrocycle 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
CN108137549B (zh) 2015-08-05 2021-07-20 百时美施贵宝公司 取代的甘氨酸衍生的fxia抑制剂
WO2017151746A1 (en) 2016-03-02 2017-09-08 Bristol-Myers Squibb Company Diamide macrocycles having factor xia inhibiting activity

Also Published As

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

Similar Documents

Publication Publication Date Title
US10899743B2 (en) Substituted glycine derived FXIA inhibitors
JP6937734B2 (ja) 第ｘｉａ因子阻害剤としてのピリミジノン
JP6082462B2 (ja) 第ｘｉａ因子阻害剤としてのジヒドロピリドンｐ１
JP6033319B2 (ja) 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
JP6464176B2 (ja) 芳香族ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
CA2937738C (en) Macrocyclic factor xia inhibitors condensed with heterocycles
JP6082463B2 (ja) 第ｘｉａ因子阻害剤としてのジヒドロピリドンｐ１
US10160750B2 (en) Diamide macrocycles as factor XIa inhibitors
JP6629958B2 (ja) 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
JP2017525744A (ja) Ｆｘｉａ阻害剤であるジアミドマクロ環
JP6816103B2 (ja) 非芳香族性Ｐ２’基を担持する新規大員環の第ＸＩａ因子阻害剤
HK40053570A (en) Pyrimidinones as factor xia inhibitors
BR112017006702B1 (pt) Pirimidinonas inibidoras de fator xia, composição farmacêutica e seu uso

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190517

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190517

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20200312

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20200324

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200624

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20200630

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20200728

R150 Certificate of patent or registration of utility model

Ref document number: 6742348

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250