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1. (WO2017092523) FUSED PYRIMIDINE COMPOUND, COMPOSITION COMPRISING SAME AND USE OF SAME
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/092523 International Application No.: PCT/CN2016/103368
Publication Date: 08.06.2017 International Filing Date: 26.10.2016
IPC:
C07D 495/04 (2006.01) ,A61K 31/519 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
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
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
深圳市塔吉瑞生物医药有限公司 SHENZHEN TARGETRX, INC. [CN/CN]; 中国广东省深圳市 南山区科苑路15号科兴科学园A栋1单元301 Room 301, Unit 1, Building A, Kexing Science Park No.15 of Keyuan Road, Nanshan District Shenzhen, Guangdong 518057, CN
Inventors:
王义汉 WANG, Yihan; CN
李焕银 LI, Huanyin; CN
Agent:
北京市柳沈律师事务所 LIU, SHEN & ASSOCIATES; 中国北京市 海淀区彩和坊路10号1号楼10层 10th Floor, Building 1 10 Caihefang Road, Haidian District Beijing 100080, CN
Priority Data:
201510872331.902.12.2015CN
Title (EN) FUSED PYRIMIDINE COMPOUND, COMPOSITION COMPRISING SAME AND USE OF SAME
(FR) COMPOSÉ DE PYRIMIDINE CONDENSÉE, COMPOSITION LE COMPRENANT ET SON UTILISATION
(ZH) 一种稠合嘧啶化合物及包含该化合物的组合物及其用途
Abstract:
(EN) The present invention discloses a fused pyrimidine compound as shown in formula (I), and preparation and use of same. In particular, the present invention discloses a fused pyrimidine compound as shown in formula (I), or a crystal form, a pharmaceutically acceptable salt, a prodrug, a stereoisomer, an isotopic variant, a hydrate or solvate thereof, and a pharmaceutical composition comprising same and use of same. The fused pyrimidine compound and the composition comprising the compound disclosed in the present invention exhibit an excellent inhibitory effect against protein kinases, and have improved pharmacokinetic parameter characteristics, which allow increased drug concentration of the compounds in an animal body and enhance drug efficacy and safety.
(FR) La présente invention concerne un composé de pyrimidine condensée représenté par la formule (I), sa préparation et son utilisation. En particulier, la présente invention concerne un composé de pyrimidine condensée représenté par la formule (I) ou une forme cristalline, un sel pharmaceutiquement acceptable, un promédicament, un stéréoisomère, un variant isotopique, un hydrate ou un solvate de celui-ci, ainsi qu'une composition pharmaceutique le comprenant et son utilisation. Le composé de pyrimidine condensée et la composition comprenant le composé décrit dans la présente invention présentent un excellent effet d'inhibition contre les protéine kinases, et présentent des caractéristiques de paramètres pharmacocinétiques améliorées, qui permettent une plus grande concentration médicamenteuse de ces composés dans le corps d'un animal et améliorent l'efficacité et la tolérance des médicaments. FORMULE (I)
(ZH) 本发明公开了如式(I)所示的稠合嘧啶化合物,以及它们的制备和用途。具体地,本发明公开了如式(I)所示的稠合嘧啶化合物,或其多晶型、药学上可接受的盐、前药、立体异构体、同位素变体、水合物或溶剂合物,以及含有它们的药物组合物及其用途。本发明公开的稠合嘧啶化合物及包含该化合物的组合物对蛋白激酶具有优异的抑制性,同时具有更好的药代动力学参数特性,能够提高化合物在动物体内的药物浓度,以提高药物疗效和安全性。
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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, JP, KE, KG, 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 Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
Also published as:
CN108137614