CN107106548A - 因子XIa抑制剂 - Google Patents

因子XIa抑制剂 Download PDF

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Publication number
CN107106548A
CN107106548A CN201680006558.8A CN201680006558A CN107106548A CN 107106548 A CN107106548 A CN 107106548A CN 201680006558 A CN201680006558 A CN 201680006558A CN 107106548 A CN107106548 A CN 107106548A
Authority
CN
China
Prior art keywords
dihydro
halogen
mmol
phenyl
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
CN201680006558.8A
Other languages
English (en)
Chinese (zh)
Inventor
E.默茨
刘卫国
S.D.埃蒙森
A.阿利
高颖多
S.F.尼拉姆卡维尔
苏崇修
R.莫宁卡
孙万莺
A.赫鲁扎
L.L.布罗库尼尔
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.)
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme LLC
Publication of CN107106548A publication Critical patent/CN107106548A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • 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
    • C07D401/10—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 linked by a carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201680006558.8A 2015-01-20 2016-01-15 因子XIa抑制剂 Pending CN107106548A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562105385P 2015-01-20 2015-01-20
US62/105385 2015-01-20
PCT/US2016/013507 WO2016118403A1 (en) 2015-01-20 2016-01-15 Factor xia inhibitors

Publications (1)

Publication Number Publication Date
CN107106548A true CN107106548A (zh) 2017-08-29

Family

ID=56417605

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680006558.8A Pending CN107106548A (zh) 2015-01-20 2016-01-15 因子XIa抑制剂

Country Status (11)

Country Link
US (1) US10123995B2 (enExample)
EP (1) EP3247354B1 (enExample)
JP (1) JP2018502137A (enExample)
KR (1) KR20170103962A (enExample)
CN (1) CN107106548A (enExample)
AU (1) AU2016209623B2 (enExample)
BR (1) BR112017015431A2 (enExample)
CA (1) CA2973202A1 (enExample)
MX (1) MX2017009445A (enExample)
RU (1) RU2712268C2 (enExample)
WO (1) WO2016118403A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021121396A1 (zh) * 2019-12-20 2021-06-24 成都康弘药业集团股份有限公司 作为血浆激肽释放酶抑制剂的三环类化合物及其用途

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9975874B2 (en) 2014-07-28 2018-05-22 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US10081617B2 (en) 2015-04-16 2018-09-25 Merck Sharp & Dohme Corp. Factor XIa inhibitors
EP3383847B1 (en) * 2015-12-02 2022-08-24 Merck Sharp & Dohme LLC FACTOR XIa INHIBITORS
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
JP6839208B2 (ja) * 2016-10-12 2021-03-03 常州市派騰電子技術服務有限公司Ｃｈａｎｇｚｈｏｕ Ｐａｔｅｎｔ Ｅｌｅｃｔｒｏｎｉｃ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏ．， Ｌｔｄ． 電子タバコの吸口、カートリッジ及び電子タバコ

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101341124A (zh) * 2005-12-14 2009-01-07 布里斯托尔-迈尔斯斯奎布公司 可用作丝氨酸蛋白酶抑制剂的6元杂环
CN101784516A (zh) * 2007-06-13 2010-07-21 百时美施贵宝公司 作为凝血因子抑制剂的二肽类似物
JP2014511359A (ja) * 2011-01-24 2014-05-15 エフ．ホフマン−ラ ロシュ アーゲー 新しいアリール−ベンゾシクロアルキルアミド誘導体
WO2014081618A1 (en) * 2012-11-20 2014-05-30 Merck Sharp & Dohme Corp. Thrombin inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7829584B2 (en) * 2006-03-21 2010-11-09 Janssen Pharmaceutica Nv Pyridines and pyridine N-oxides as modulators of thrombin
PE20091825A1 (es) * 2008-04-04 2009-12-04 Merck & Co Inc Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3
US8828983B2 (en) * 2010-02-11 2014-09-09 Bristol-Myers Squibb Company Macrocycles as factor XIa inhibitors
KR20140052034A (ko) 2011-08-19 2014-05-02 머크 샤프 앤드 돔 코포레이션 신장 외수질 칼륨 채널의 억제제
US20150225404A1 (en) * 2012-08-30 2015-08-13 Nippon Shinyaku Co., Ltd. Pyridine derivative and medicine
KR20170005871A (ko) * 2014-05-28 2017-01-16 머크 샤프 앤드 돔 코포레이션 인자 XIa 억제제
US9975874B2 (en) 2014-07-28 2018-05-22 Merck Sharp & Dohme Corp. Factor XIa inhibitors
EP3180327B1 (en) 2014-07-28 2019-05-08 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
WO2016015593A1 (en) 2014-07-28 2016-02-04 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101341124A (zh) * 2005-12-14 2009-01-07 布里斯托尔-迈尔斯斯奎布公司 可用作丝氨酸蛋白酶抑制剂的6元杂环
US20090181983A1 (en) * 2005-12-14 2009-07-16 Bristol -Meyers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
CN101784516A (zh) * 2007-06-13 2010-07-21 百时美施贵宝公司 作为凝血因子抑制剂的二肽类似物
JP2014511359A (ja) * 2011-01-24 2014-05-15 エフ．ホフマン−ラ ロシュ アーゲー 新しいアリール−ベンゾシクロアルキルアミド誘導体
WO2014081618A1 (en) * 2012-11-20 2014-05-30 Merck Sharp & Dohme Corp. Thrombin inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021121396A1 (zh) * 2019-12-20 2021-06-24 成都康弘药业集团股份有限公司 作为血浆激肽释放酶抑制剂的三环类化合物及其用途

Also Published As

Publication number Publication date
US20180000795A1 (en) 2018-01-04
EP3247354B1 (en) 2019-08-07
KR20170103962A (ko) 2017-09-13
RU2712268C2 (ru) 2020-01-28
EP3247354A4 (en) 2018-06-27
US10123995B2 (en) 2018-11-13
BR112017015431A2 (pt) 2018-01-16
JP2018502137A (ja) 2018-01-25
MX2017009445A (es) 2017-11-08
RU2017129275A (ru) 2019-02-21
CA2973202A1 (en) 2016-07-28
WO2016118403A1 (en) 2016-07-28
EP3247354A1 (en) 2017-11-29
RU2017129275A3 (enExample) 2019-07-26
AU2016209623B2 (en) 2019-11-14
AU2016209623A1 (en) 2017-07-13

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Application publication date: 20170829