JP2019507167A - 第xia因子阻害活性を有するジアミド大員環 - Google Patents

第xia因子阻害活性を有するジアミド大員環 Download PDF

Info

Publication number
JP2019507167A
JP2019507167A JP2018545880A JP2018545880A JP2019507167A JP 2019507167 A JP2019507167 A JP 2019507167A JP 2018545880 A JP2018545880 A JP 2018545880A JP 2018545880 A JP2018545880 A JP 2018545880A JP 2019507167 A JP2019507167 A JP 2019507167A
Authority
JP
Japan
Prior art keywords
alkyl
nhco
independently selected
pharmaceutically acceptable
independently
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.)
Pending
Application number
JP2018545880A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019507167A5 (enExample
Inventor
シ・ジュン
ウィリアム・アール・ユーイング
ドナルド・ジェイ・ピー・ピント
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 JP2019507167A publication Critical patent/JP2019507167A/ja
Publication of JP2019507167A5 publication Critical patent/JP2019507167A5/ja
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2018545880A 2016-03-02 2017-03-01 第xia因子阻害活性を有するジアミド大員環 Pending JP2019507167A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662302220P 2016-03-02 2016-03-02
US62/302,220 2016-03-02
PCT/US2017/020161 WO2017151746A1 (en) 2016-03-02 2017-03-01 Diamide macrocycles having factor xia inhibiting activity

Publications (2)

Publication Number Publication Date
JP2019507167A true JP2019507167A (ja) 2019-03-14
JP2019507167A5 JP2019507167A5 (enExample) 2020-04-02

Family

ID=58361087

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018545880A Pending JP2019507167A (ja) 2016-03-02 2017-03-01 第xia因子阻害活性を有するジアミド大員環

Country Status (6)

Country Link
US (1) US10752641B2 (enExample)
EP (1) EP3423458A1 (enExample)
JP (1) JP2019507167A (enExample)
KR (1) KR20180117156A (enExample)
CN (1) CN109195973A (enExample)
WO (1) WO2017151746A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023551150A (ja) * 2020-11-19 2023-12-07 メルク・シャープ・アンド・ドーム・エルエルシー 血漿カリクレイン阻害剤

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
CN107922393A (zh) 2015-07-29 2018-04-17 百时美施贵宝公司 携带非芳族p2,基团的因子xia新大环
CN107849026B (zh) 2015-07-29 2021-01-01 百时美施贵宝公司 携带烷基或环烷基p2′部分的因子xia大环抑制剂
US20230373972A1 (en) 2020-09-17 2023-11-23 Zhejiang Hisun Pharmaceutical Co., Ltd. Piperazine derivative, preparation method therefor and use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013519678A (ja) * 2010-02-11 2013-05-30 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マクロ環
JP2015524443A (ja) * 2012-08-03 2015-08-24 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ヒドロピリドンp1
WO2015164308A1 (en) * 2014-04-22 2015-10-29 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0028489B1 (en) 1979-11-05 1983-10-05 Beecham Group Plc Enzyme derivatives, and their preparation
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.
WO2000076970A2 (en) 1999-06-14 2000-12-21 Eli Lilly And Company 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
GEP20074098B (en) 2001-09-21 2007-05-10 Bristol Myers Squibb Co 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
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
US9409908B2 (en) 2012-08-03 2016-08-09 Bristol-Myers Squibb Company Dihydropyridone p1 as factor XIa inhibitors
NO2760821T3 (enExample) 2014-01-31 2018-03-10
ES2687498T3 (es) 2014-01-31 2018-10-25 Bristol-Myers Squibb Company Macrociclos con grupos P2¿ heterocíclicos como inhibidores del factor XIa
ES2714283T3 (es) * 2014-09-04 2019-05-28 Bristol Myers Squibb Co Macrociclos de diamida que son inhibidores de FXIa
NO2721243T3 (enExample) 2014-10-01 2018-10-20
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
CN107922393A (zh) 2015-07-29 2018-04-17 百时美施贵宝公司 携带非芳族p2,基团的因子xia新大环
CN107849026B (zh) 2015-07-29 2021-01-01 百时美施贵宝公司 携带烷基或环烷基p2′部分的因子xia大环抑制剂

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013519678A (ja) * 2010-02-11 2013-05-30 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マクロ環
JP2015524443A (ja) * 2012-08-03 2015-08-24 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ヒドロピリドンp1
WO2015164308A1 (en) * 2014-04-22 2015-10-29 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023551150A (ja) * 2020-11-19 2023-12-07 メルク・シャープ・アンド・ドーム・エルエルシー 血漿カリクレイン阻害剤
JP7787890B2 (ja) 2020-11-19 2025-12-17 メルク・シャープ・アンド・ドーム・エルエルシー 血漿カリクレイン阻害剤

Also Published As

Publication number Publication date
WO2017151746A1 (en) 2017-09-08
US10752641B2 (en) 2020-08-25
US20190062343A1 (en) 2019-02-28
CN109195973A (zh) 2019-01-11
KR20180117156A (ko) 2018-10-26
EP3423458A1 (en) 2019-01-09

Similar Documents

Publication Publication Date Title
JP7317905B2 (ja) 第xia因子阻害剤としてのピリミジノン
JP6526796B2 (ja) Fxia阻害剤であるジアミドマクロ環
JP6082462B2 (ja) 第xia因子阻害剤としてのジヒドロピリドンp1
JP5841547B2 (ja) 第xia因子阻害剤としてのマクロ環
US9403774B2 (en) Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9315519B2 (en) Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
JP2018522046A (ja) 新規な置換グリシン誘導のfxia阻害剤
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
JP6742348B2 (ja) 第xia因子阻害剤としてのジアミド大員環
JP2019507167A (ja) 第xia因子阻害活性を有するジアミド大員環
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
US20190144393A1 (en) Factor xia macrocycles with novel p1 groups
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: 20200221

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200221

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20210128

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210202

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20210430

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210701

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20211124