KR20180117156A - 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 - Google Patents

인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 Download PDF

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Publication number
KR20180117156A
KR20180117156A KR1020187027820A KR20187027820A KR20180117156A KR 20180117156 A KR20180117156 A KR 20180117156A KR 1020187027820 A KR1020187027820 A KR 1020187027820A KR 20187027820 A KR20187027820 A KR 20187027820A KR 20180117156 A KR20180117156 A KR 20180117156A
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KR
South Korea
Prior art keywords
alkyl
independently selected
nhco
pharmaceutically acceptable
thrombosis
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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.)
Ceased
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KR1020187027820A
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English (en)
Korean (ko)
Inventor
준 시
윌리엄 알. 유잉
도널드 제이.피. 핀토
Original Assignee
브리스톨-마이어스 스큅 컴퍼니
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Application filed by 브리스톨-마이어스 스큅 컴퍼니 filed Critical 브리스톨-마이어스 스큅 컴퍼니
Publication of KR20180117156A publication Critical patent/KR20180117156A/ko
Ceased legal-status Critical Current

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Classifications

    • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020187027820A 2016-03-02 2017-03-01 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 Ceased KR20180117156A (ko)

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 (1)

Publication Number Publication Date
KR20180117156A true KR20180117156A (ko) 2018-10-26

Family

ID=58361087

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020187027820A Ceased KR20180117156A (ko) 2016-03-02 2017-03-01 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클

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
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
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
JP7700218B2 (ja) 2020-09-17 2025-06-30 浙江海正薬業股▲ふん▼有限公司 ピペラジン誘導体、その製造方法、およびその使用
KR20230110544A (ko) * 2020-11-19 2023-07-24 머크 샤프 앤드 돔 엘엘씨 혈장 칼리크레인 억제제

Family Cites Families (21)

* 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.
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
CN104744461A (zh) 2001-09-21 2015-07-01 百时美施贵宝公司 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂
US20040180855A1 (en) 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
NZ602266A (en) 2010-02-11 2014-05-30 Bristol Myers Squibb Co Macrocycles as factor xia inhibitors
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
AU2013296259A1 (en) 2012-08-03 2015-03-19 Bristol-Myers Squibb Company Dihydropyridone P1 as factor XIa inhibitors
US9376444B2 (en) * 2012-08-03 2016-06-28 Bristol-Myers Squibb Company Dihydropyridone P1 as factor XIa inhibitors
SG10201908467RA (en) 2014-01-31 2019-10-30 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (https=) 2014-01-31 2018-03-10
EP3134408B1 (en) * 2014-04-22 2020-08-12 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
ES2714283T3 (es) 2014-09-04 2019-05-28 Bristol Myers Squibb Co Macrociclos de diamida que son inhibidores de FXIa
NO2721243T3 (https=) 2014-10-01 2018-10-20
ES2762987T3 (es) 2015-06-19 2020-05-26 Bristol Myers Squibb Co Macrociclos de diamida como inhibidores del factor XIA
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
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

Also Published As

Publication number Publication date
WO2017151746A1 (en) 2017-09-08
EP3423458A1 (en) 2019-01-09
CN109195973A (zh) 2019-01-11
JP2019507167A (ja) 2019-03-14
US20190062343A1 (en) 2019-02-28
US10752641B2 (en) 2020-08-25

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