JP6101343B2 - 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピリダジン誘導体 - Google Patents

血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピリダジン誘導体 Download PDF

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JP6101343B2
JP6101343B2 JP2015509093A JP2015509093A JP6101343B2 JP 6101343 B2 JP6101343 B2 JP 6101343B2 JP 2015509093 A JP2015509093 A JP 2015509093A JP 2015509093 A JP2015509093 A JP 2015509093A JP 6101343 B2 JP6101343 B2 JP 6101343B2
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エルドン・スコット・プリーストリー
ショシャナ・エル・ポージー
フランソワ・トランブレイ
アラン・マーテル
アンヌ・マリニエ
アール・マイケル・ローレンス
マイケル・エム・ミラー
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Bristol Myers Squibb Co
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • 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
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/33Heterocyclic compounds
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    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • 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
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    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
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    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C

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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2015509093A 2012-04-26 2013-04-24 血小板凝集を治療するためのプロテアーゼ活性化受容体4(par4)阻害剤としてのイミダゾチアジアゾールおよびイミダゾピリダジン誘導体 Active JP6101343B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261638567P 2012-04-26 2012-04-26
US61/638,567 2012-04-26
PCT/US2013/037884 WO2013163241A1 (en) 2012-04-26 2013-04-24 Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation

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JP2015514806A JP2015514806A (ja) 2015-05-21
JP2015514806A5 JP2015514806A5 (https=) 2016-03-17
JP6101343B2 true JP6101343B2 (ja) 2017-03-22

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US (1) US9518064B2 (https=)
EP (1) EP2855489B1 (https=)
JP (1) JP6101343B2 (https=)
KR (1) KR20150003766A (https=)
CN (1) CN104640869B (https=)
AU (1) AU2013251680A1 (https=)
BR (1) BR112014026651A8 (https=)
CA (1) CA2871599A1 (https=)
EA (1) EA201491954A1 (https=)
ES (1) ES2617879T3 (https=)
IL (1) IL235141A0 (https=)
MX (1) MX2014012741A (https=)
SG (1) SG11201406733QA (https=)
WO (1) WO2013163241A1 (https=)

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SI2841437T1 (sl) 2012-04-26 2017-09-29 Bristol-Myers Squibb Company Derivati imidazotiadiazola in imidazopirazina kot proteazno aktivirani receptor 4 (PAR4) inhibitorji za zdravljenje agregacije trombocitov
SG11201406759YA (en) * 2012-04-26 2014-11-27 Bristol Myers Squibb Co Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
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CN109689664B (zh) * 2016-07-14 2022-04-15 百时美施贵宝公司 作为par4抑制剂的三环杂芳基取代的喹啉和氮杂喹啉化合物
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CN111094300B (zh) * 2018-01-31 2022-09-16 江苏恒瑞医药股份有限公司 苯并杂芳基类衍生物、其制备方法及其在医药上的应用
CN110218218B (zh) * 2018-03-01 2022-04-08 江苏恒瑞医药股份有限公司 苯并呋喃类衍生物、其制备方法及其在医药上的应用
CN112074522B (zh) * 2018-05-16 2022-08-26 深圳信立泰药业股份有限公司 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物
WO2019218955A1 (zh) * 2018-05-16 2019-11-21 深圳信立泰药业股份有限公司 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物
CN110627817B (zh) * 2018-06-25 2022-03-29 中国药科大学 咪唑并环类par4拮抗剂及其医药用途
CN111349105B (zh) * 2018-12-24 2023-04-07 江苏恒瑞医药股份有限公司 苯并呋喃类衍生物、其制备方法及其在医药上的应用
CN109651126A (zh) * 2019-01-17 2019-04-19 杭州师范大学 一种四苯乙烯基羧酸有机配体及其配合物的制备方法
CN113150005B (zh) * 2021-04-09 2022-08-30 中国药科大学 喹喔啉类化合物、制备方法及其在医药上的应用

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US9518064B2 (en) 2016-12-13
BR112014026651A2 (pt) 2017-06-27
BR112014026651A8 (pt) 2018-01-16
CN104640869A (zh) 2015-05-20
AU2013251680A1 (en) 2014-11-13
WO2013163241A1 (en) 2013-10-31
EP2855489A1 (en) 2015-04-08
KR20150003766A (ko) 2015-01-09
JP2015514806A (ja) 2015-05-21
CA2871599A1 (en) 2013-10-31
ES2617879T3 (es) 2017-06-20
SG11201406733QA (en) 2014-11-27
EP2855489B1 (en) 2017-01-04
CN104640869B (zh) 2017-12-12
EA201491954A1 (ru) 2015-01-30

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