KR20150038372A - 인자 XIa 억제제로서의 디히드로피리돈 P1 - Google Patents

인자 XIa 억제제로서의 디히드로피리돈 P1 Download PDF

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KR20150038372A
KR20150038372A KR1020157004963A KR20157004963A KR20150038372A KR 20150038372 A KR20150038372 A KR 20150038372A KR 1020157004963 A KR1020157004963 A KR 1020157004963A KR 20157004963 A KR20157004963 A KR 20157004963A KR 20150038372 A KR20150038372 A KR 20150038372A
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alkyl
optionally substituted
independently selected
heterocycle
carbocycle
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Inventor
우 양
제임스 알. 코르테
폴 제이. 길리건
도날드 제이.피. 핀토 핀토
윌리엄 알. 유잉
앤드류 케이. 딜저
유펭 왕
티아난 팡
쿠마르 비. 파비세티
레온 엠. 스미쓰 2세
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브리스톨-마이어스 스큅 컴퍼니
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Publication of KR20150038372A publication Critical patent/KR20150038372A/ko
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged 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
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/16Halogenated acetic acids
    • C07C53/18Halogenated acetic acids containing fluorine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic radicals containing only nitrogen as ring hetero atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020157004963A 2012-08-03 2013-08-02 인자 XIa 억제제로서의 디히드로피리돈 P1 Withdrawn KR20150038372A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261679197P 2012-08-03 2012-08-03
US61/679,197 2012-08-03
US201361787081P 2013-03-15 2013-03-15
US61/787,081 2013-03-15
PCT/US2013/053416 WO2014022767A1 (en) 2012-08-03 2013-08-02 Dihydropyridone p1 as factor xia inhibitors

Publications (1)

Publication Number Publication Date
KR20150038372A true KR20150038372A (ko) 2015-04-08

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KR1020157004963A Withdrawn KR20150038372A (ko) 2012-08-03 2013-08-02 인자 XIa 억제제로서의 디히드로피리돈 P1

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US (2) US9409908B2 (enExample)
EP (1) EP2880026B1 (enExample)
JP (1) JP6082463B2 (enExample)
KR (1) KR20150038372A (enExample)
CN (2) CN108250199B (enExample)
AR (1) AR091981A1 (enExample)
AU (1) AU2013296259A1 (enExample)
BR (1) BR112015002081A2 (enExample)
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CY (1) CY1119004T1 (enExample)
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HU (1) HUE032622T2 (enExample)
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LT (1) LT2880026T (enExample)
MX (1) MX361759B (enExample)
PL (1) PL2880026T3 (enExample)
PT (1) PT2880026T (enExample)
RS (1) RS55975B1 (enExample)
SG (1) SG11201500271UA (enExample)
SI (1) SI2880026T1 (enExample)
SM (1) SMT201700240T1 (enExample)
TW (1) TW201410667A (enExample)
UY (1) UY34960A (enExample)
WO (1) WO2014022767A1 (enExample)

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KR20180033267A (ko) * 2015-07-29 2018-04-02 브리스톨-마이어스 스큅 컴퍼니 비-방향족 P2' 기를 갖는 인자 XIa 신규 마크로사이클

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CN110062757B (zh) * 2017-01-18 2022-03-04 广东东阳光药业有限公司 凝血因子XIa抑制剂及其用途
WO2019011166A1 (zh) * 2017-07-14 2019-01-17 四川科伦博泰生物医药股份有限公司 大环酰胺化合物及其药物组合物和用途
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WO2021013209A1 (zh) 2019-07-23 2021-01-28 南京明德新药研发有限公司 作为XIa因子抑制剂的大环衍生物
CN113004286B (zh) * 2019-12-20 2022-08-12 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
CN113004284B (zh) * 2019-12-20 2022-08-12 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四环类化合物及其用途
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20180033267A (ko) * 2015-07-29 2018-04-02 브리스톨-마이어스 스큅 컴퍼니 비-방향족 P2' 기를 갖는 인자 XIa 신규 마크로사이클

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US20150203492A1 (en) 2015-07-23
EA028581B1 (ru) 2017-12-29
US9951071B2 (en) 2018-04-24
CN104507924A (zh) 2015-04-08
CY1119004T1 (el) 2018-01-10
EA201590277A1 (ru) 2015-05-29
SMT201700240T1 (it) 2017-07-18
CN108250199B (zh) 2021-07-16
SG11201500271UA (en) 2015-03-30
WO2014022767A1 (en) 2014-02-06
LT2880026T (lt) 2017-04-25
RS55975B1 (sr) 2017-09-29
US20160340360A1 (en) 2016-11-24
US9409908B2 (en) 2016-08-09
TW201410667A (zh) 2014-03-16
AU2013296259A1 (en) 2015-03-19
PL2880026T3 (pl) 2017-08-31
CN104507924B (zh) 2018-01-23
UY34960A (es) 2014-01-31
JP6082463B2 (ja) 2017-02-15
MX361759B (es) 2018-12-17
EP2880026B1 (en) 2017-02-22
CA2880866A1 (en) 2014-02-06
JP2015528022A (ja) 2015-09-24
MX2015000892A (es) 2015-04-17
SI2880026T1 (sl) 2017-04-26
PT2880026T (pt) 2017-05-03
EP2880026A1 (en) 2015-06-10
ES2623175T3 (es) 2017-07-10
DK2880026T3 (en) 2017-06-06
HRP20170506T1 (hr) 2017-06-02
HUE032622T2 (en) 2017-10-30
BR112015002081A2 (pt) 2017-07-04
IL237011A0 (en) 2015-03-31
CN108250199A (zh) 2018-07-06
AR091981A1 (es) 2015-03-11

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