CN109195973A - 具有因子xia抑制活性的二酰胺大环类化合物 - Google Patents

具有因子xia抑制活性的二酰胺大环类化合物 Download PDF

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Publication number
CN109195973A
CN109195973A CN201780026984.2A CN201780026984A CN109195973A CN 109195973 A CN109195973 A CN 109195973A CN 201780026984 A CN201780026984 A CN 201780026984A CN 109195973 A CN109195973 A CN 109195973A
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CN
China
Prior art keywords
alkyl
independently selected
nhco
factor
pharmaceutically acceptable
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
CN201780026984.2A
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English (en)
Chinese (zh)
Inventor
史俊
W.R.欧文
D.J.P.平托
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
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Bristol Myers Squibb Co
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Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN109195973A publication Critical patent/CN109195973A/zh
Pending legal-status Critical Current

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    • 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
    • C07D498/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/537—Heterocyclic 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201780026984.2A 2016-03-02 2017-03-01 具有因子xia抑制活性的二酰胺大环类化合物 Pending CN109195973A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662302220P 2016-03-02 2016-03-02
US62/302220 2016-03-02
PCT/US2017/020161 WO2017151746A1 (en) 2016-03-02 2017-03-01 Diamide macrocycles having factor xia inhibiting activity

Publications (1)

Publication Number Publication Date
CN109195973A true CN109195973A (zh) 2019-01-11

Family

ID=58361087

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780026984.2A Pending CN109195973A (zh) 2016-03-02 2017-03-01 具有因子xia抑制活性的二酰胺大环类化合物

Country Status (6)

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

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016205482A1 (en) 2015-06-19 2016-12-22 Bristol-Myers Squibb Company Diamide macrocycles as factor xia inhibitors
US10287288B2 (en) 2015-07-29 2019-05-14 Bristol-Myers Squibb Factor XIa macrocyclic inhibitors bearing alkyl or cycloalkyl P2' moieties
ES2871111T3 (es) 2015-07-29 2021-10-28 Bristol Myers Squibb Co Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático
EP4215525A4 (en) 2020-09-17 2024-08-21 Zhejiang Hisun Pharmaceutical Co., Ltd. Piperazine derivative, preparation method therefor and use thereof
KR20230110544A (ko) * 2020-11-19 2023-07-24 머크 샤프 앤드 돔 엘엘씨 혈장 칼리크레인 억제제

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011100401A1 (en) * 2010-02-11 2011-08-18 Bristol-Myers Squibb Company Macrocycles as factor xia inhibitors
WO2014022766A1 (en) * 2012-08-03 2014-02-06 Bristol-Myers Squibb Company Dihydropyridone p1 as factor xia inhibitors
WO2015164308A1 (en) * 2014-04-22 2015-10-29 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
WO2016036893A1 (en) * 2014-09-04 2016-03-10 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3065190D1 (en) 1979-11-05 1983-11-10 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.
EP1192135A2 (en) 1999-06-14 2002-04-03 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
CA2461202C (en) 2001-09-21 2011-07-12 Donald Pinto 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
MX361759B (es) 2012-08-03 2018-12-17 Bristol Myers Squibb Co Compuestos macrocíclicos de dihidropiridona como inhibidores del factor xia y el uso de los mismos en el tratamiento de un trastorno tromboembólico.
CN116987080A (zh) 2014-01-31 2023-11-03 百时美施贵宝公司 作为因子xia抑制剂的具有杂环p2′基团的大环化合物
NO2760821T3 (https=) 2014-01-31 2018-03-10
NO2721243T3 (https=) 2014-10-01 2018-10-20
WO2016205482A1 (en) 2015-06-19 2016-12-22 Bristol-Myers Squibb Company Diamide macrocycles as factor xia inhibitors
US10287288B2 (en) 2015-07-29 2019-05-14 Bristol-Myers Squibb Factor XIa macrocyclic inhibitors bearing alkyl or cycloalkyl P2' moieties
ES2871111T3 (es) 2015-07-29 2021-10-28 Bristol Myers Squibb Co Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011100401A1 (en) * 2010-02-11 2011-08-18 Bristol-Myers Squibb Company Macrocycles as factor xia inhibitors
WO2014022766A1 (en) * 2012-08-03 2014-02-06 Bristol-Myers Squibb Company Dihydropyridone p1 as factor xia inhibitors
WO2015164308A1 (en) * 2014-04-22 2015-10-29 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
WO2016036893A1 (en) * 2014-09-04 2016-03-10 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors

Also Published As

Publication number Publication date
KR20180117156A (ko) 2018-10-26
US10752641B2 (en) 2020-08-25
JP2019507167A (ja) 2019-03-14
WO2017151746A1 (en) 2017-09-08
EP3423458A1 (en) 2019-01-09
US20190062343A1 (en) 2019-02-28

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Application publication date: 20190111