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1. (WO2018137639) HISTONE METHYLTRANSFERASE EZH2 INHIBITOR, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
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Pub. No.: WO/2018/137639 International Application No.: PCT/CN2018/073946
Publication Date: 02.08.2018 International Filing Date: 24.01.2018
IPC:
C07D 213/64 (2006.01) ,C07D 401/12 (2006.01) ,C07D 405/12 (2006.01) ,C07D 409/12 (2006.01) ,C07D 491/10 (2006.01) ,C07D 413/12 (2006.01) ,C07D 417/12 (2006.01) ,A61K 31/4412 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
62
Oxygen or sulfur atoms
63
One oxygen atom
64
attached in position 2 or 6
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
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
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02
in which the condensed system contains two hetero rings
10
Spiro-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4412
having oxo groups directly attached to the heterocyclic ring
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
恩瑞生物医药科技(上海)有限公司 ANCUREALL PHARMACEUTICAL (SHANGHAI) CO., LTD. [CN/CN]; 中国上海市 自由贸易试验区法拉第路249号7幢第二层西楼面 2nd Floor West Wing, Building 7 249 Faladi Road, Shanghai Pilot Free Trade Zone Shanghai 201210, CN
Inventors:
司聚同 SI, Jutong; CN
王贯 WANG, Guan; CN
姜美锋 JIANG, Meifeng; CN
杨志和 YANG, Zhihe; CN
周晨涛 ZHOU, Chentao; CN
Agent:
北京戈程知识产权代理有限公司 GE CHENG & CO., LTD.; 中国北京市 东城区东长安街1号东方广场东三办公楼19层1901 Level 19, Tower E3, The Towers, Oriental Plaza No.1, East Chang An Avenue, Docheng Beijing 100738, CN
Priority Data:
201710061026.025.01.2017CN
201710345609.616.05.2017CN
Title (EN) HISTONE METHYLTRANSFERASE EZH2 INHIBITOR, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
(FR) INHIBITEUR D'HISTONE MÉTHYLTRANSFÉRASE EZH2, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION PHARMACEUTIQUE
(ZH) 一种组蛋白甲基转移酶EZH2抑制剂、其制备方法及其医药用途
Abstract:
(EN) The invention relates to a histone methyltransferase EZH2 inhibitor, a preparation method and pharmaceutical use thereof. In particular, the invention relates to a compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and a use thereof as a histone methyltransferase EZH2 inhibitor for treating diseases associated with the histone methyltransferase EZH2, especially cancer. The definition of each substituents in the general formula (I) is same as the definition in the specification.
(FR) L'invention concerne un inhibiteur d'histone méthyltransférase EZH2, un procédé de préparation et une utilisation pharmaceutique de celui-ci. En particulier, l'invention concerne un composé représenté par la formule générale (I), son procédé de préparation, une composition pharmaceutique le contenant, et son utilisation en tant qu'inhibiteur d'histone méthyltransférase EZH2 pour traiter des maladies associées à l'histone méthyltransférase EZH2, en particulier le cancer. La définition de chaque substituant dans la formule générale (I) est la même que celle donnée dans la description.
(ZH) 本发明涉及一种组蛋白甲基转移酶EZH2抑制剂、其制备方法及其医药用途。特别地,本发明涉及通式(I)所示的化合物,其制备方法及含有其的药物组合物,以及其作为组蛋白甲基转移酶EZH2抑制剂,治疗与组蛋白甲基转移酶EZH2相关的疾病特别是癌症的用途。其中通式(I)中的各取代基的定义与说明书中的定义相同。
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)