KR20150038369A - 인자 XIa 억제제로서의 디히드로피리돈 P1 - Google Patents

인자 XIa 억제제로서의 디히드로피리돈 P1 Download PDF

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KR20150038369A
KR20150038369A KR20157004959A KR20157004959A KR20150038369A KR 20150038369 A KR20150038369 A KR 20150038369A KR 20157004959 A KR20157004959 A KR 20157004959A KR 20157004959 A KR20157004959 A KR 20157004959A KR 20150038369 A KR20150038369 A KR 20150038369A
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mmol
methyl
compounds
independently selected
oxo
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Inventor
우 양
제임스 알. 코르테
폴 제이. 길리건
도날드 제이.피. 핀토 핀토
윌리엄 알. 유잉
유펭 왕
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브리스톨-마이어스 스큅 컴퍼니
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Publication of KR20150038369A publication Critical patent/KR20150038369A/ko
Withdrawn legal-status Critical Current

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    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • 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
    • C07D401/06Heterocyclic 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 only aliphatic carbon atoms
    • 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
    • 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
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
KR20157004959A 2012-08-03 2013-08-02 인자 XIa 억제제로서의 디히드로피리돈 P1 Withdrawn KR20150038369A (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
US201361786992P 2013-03-15 2013-03-15
US61/786,992 2013-03-15
PCT/US2013/053414 WO2014022766A1 (en) 2012-08-03 2013-08-02 Dihydropyridone p1 as factor xia inhibitors

Publications (1)

Publication Number Publication Date
KR20150038369A true KR20150038369A (ko) 2015-04-08

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KR20157004959A Withdrawn KR20150038369A (ko) 2012-08-03 2013-08-02 인자 XIa 억제제로서의 디히드로피리돈 P1

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Country Link
US (2) US20140038969A1 (enExample)
EP (1) EP2882734B1 (enExample)
JP (1) JP6082462B2 (enExample)
KR (1) KR20150038369A (enExample)
AR (1) AR093759A1 (enExample)
AU (1) AU2013296258A1 (enExample)
BR (1) BR112015002293A2 (enExample)
CA (1) CA2880898A1 (enExample)
CY (1) CY1118450T1 (enExample)
DK (1) DK2882734T3 (enExample)
EA (1) EA025392B1 (enExample)
ES (1) ES2605824T3 (enExample)
HR (1) HRP20161378T1 (enExample)
HU (1) HUE031582T2 (enExample)
IL (1) IL237012A0 (enExample)
LT (1) LT2882734T (enExample)
MX (1) MX361370B (enExample)
PL (1) PL2882734T3 (enExample)
PT (1) PT2882734T (enExample)
RS (1) RS55581B1 (enExample)
SG (1) SG11201500270RA (enExample)
SI (1) SI2882734T1 (enExample)
SM (2) SMT201700003T1 (enExample)
TW (1) TW201410666A (enExample)
UY (1) UY34959A (enExample)
WO (1) WO2014022766A1 (enExample)

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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
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PL2766346T3 (pl) 2011-10-14 2017-09-29 Bristol-Myers Squibb Company Podstawione związki tetrahydroizochinoliny jako inhibitory czynnika XIA
IN2014CN02806A (enExample) 2011-10-14 2015-07-03 Bristol Myers Squibb Co
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
EA032092B1 (ru) 2012-10-12 2019-04-30 Бристол-Майерс Сквибб Компани Кристаллические формы ингибитора фактора xia
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
JP6479763B2 (ja) 2013-03-25 2019-03-06 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置換アゾール含有のテトラヒドロイソキノリン
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ES2687498T3 (es) * 2014-01-31 2018-10-25 Bristol-Myers Squibb Company Macrociclos con grupos P2¿ heterocíclicos como inhibidores del factor XIa
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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
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
CA2998902C (en) * 2015-10-29 2024-03-26 Merck Sharp & Dohme Corp. Macrocyclic compounds as factor xia inhibitors
WO2017074833A1 (en) 2015-10-29 2017-05-04 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
WO2017151746A1 (en) * 2016-03-02 2017-09-08 Bristol-Myers Squibb Company Diamide macrocycles having factor xia inhibiting activity
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
CN113677682B (zh) 2019-04-16 2023-05-30 华润生物医药有限公司 作为XIa因子抑制剂的大环衍生物
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

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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
IN2014CN02806A (enExample) 2011-10-14 2015-07-03 Bristol Myers Squibb Co
JP6033318B2 (ja) 2011-10-14 2016-11-30 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置換テトラヒドロイソキノリン化合物
PL2766346T3 (pl) 2011-10-14 2017-09-29 Bristol-Myers Squibb Company Podstawione związki tetrahydroizochinoliny jako inhibitory czynnika XIA
DK2794597T3 (en) 2011-12-21 2018-01-15 Ono Pharmaceutical Co PYRIDINON AND PYRIMIDINON DERIVATIVES AS FACTOR XIA INHIBITORS
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Publication number Publication date
TW201410666A (zh) 2014-03-16
PL2882734T3 (pl) 2017-05-31
EA025392B1 (ru) 2016-12-30
UY34959A (es) 2014-01-31
SG11201500270RA (en) 2015-03-30
CA2880898A1 (en) 2014-02-06
SI2882734T1 (sl) 2017-01-31
MX361370B (es) 2018-12-05
CN104520289A (zh) 2015-04-15
IL237012A0 (en) 2015-03-31
EP2882734A1 (en) 2015-06-17
SMT201700003B (it) 2017-03-08
CY1118450T1 (el) 2017-06-28
LT2882734T (lt) 2016-12-12
HRP20161378T1 (hr) 2016-12-02
EP2882734B1 (en) 2016-10-12
US20140038969A1 (en) 2014-02-06
MX2015000919A (es) 2015-09-21
WO2014022766A1 (en) 2014-02-06
ES2605824T3 (es) 2017-03-16
JP2015524443A (ja) 2015-08-24
BR112015002293A2 (pt) 2017-07-04
RS55581B1 (sr) 2017-06-30
PT2882734T (pt) 2016-12-09
EA201590284A1 (ru) 2015-05-29
AU2013296258A1 (en) 2015-03-19
SMT201700003T1 (it) 2017-03-08
DK2882734T3 (en) 2017-01-30
HUE031582T2 (en) 2017-07-28
US20150166550A1 (en) 2015-06-18
JP6082462B2 (ja) 2017-02-15
US9376444B2 (en) 2016-06-28
AR093759A1 (es) 2015-06-24

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