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1. (WO2018086547) 2-SUBSTITUTED AROMATIC RING-PYRIMIDINE DERIVATIVE, AND PREPARATION AND APPLICATION THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/086547 International Application No.: PCT/CN2017/110030
Publication Date: 17.05.2018 International Filing Date: 08.11.2017
IPC:
C07D 401/14 (2006.01) ,A61K 31/506 (2006.01) ,A61P 35/00 (2006.01)
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
14
containing three or more hetero rings
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
506
not condensed and containing further 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: ZHEJIANG UNIVERSITY[CN/CN]; No.38, Zheda Road, Xihu District Hangzhou, Zhejiang 310027, CN
SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES[CN/CN]; 555 ZuChongZhi Rd, Pudong New Area Shanghai 201203, CN
Inventors: LIU, Tao; CN
LI, Jia; CN
HU, Yongzhou; CN
ZHOU, Yubo; CN
DONG, Xiaowu; CN
GAO, Anhui; CN
SONG, Pinrao; CN
WANG, Peipei; CN
TONG, Lexian; CN
HU, Xiaobei; CN
SU, Mingbo; CN
Agent: HANGZHOU QIUSHI PATENT OFFICE CO.,LTD.; Hangli ZHAO/Room 215 Huanghongnian Science and Technology Complex Building, No.147, Yugu Road, Xihu District Hangzhou, Zhejiang 310013, CN
Priority Data:
201610988060.810.11.2016CN
Title (EN) 2-SUBSTITUTED AROMATIC RING-PYRIMIDINE DERIVATIVE, AND PREPARATION AND APPLICATION THEREOF
(FR) DÉRIVÉ DU CYCLE PYRIMIDINE AROMATIQUE À SUBSTITUTION EN POSITION 2, PRÉPARATION ET APPLICATION ASSOCIÉES
(ZH) 2-取代芳环-嘧啶类衍生物及制备和应用
Abstract:
(EN) Provided are a 2-substituted aromatic ring-pyrimidine derivative represented by general formula (I), and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof. N-substituted pyridine-2-aminopyrimidine obtained by structure-based virtual screening is used as a lead compound, and then a series of novel small-molecular Chk1 inhibitors are designed and synthesized. The compounds are then subjected to Chk1 kinase inhibitory activity assay at molecular level. The assay proves that the compound has strong anticancer performance, has Chk1 kinase inhibitory activity, has prospect as a Chk1 inhibitor, and can be applied to medicines for therapy of human or animal cell proliferation related solid tumors or leukaemia.
(FR) L'invention concerne un dérivé de cycle-pyrimidine aromatique à substitution en position 2 représenté par la formule générale (I), et un isomère optique de celui-ci, ou un sel ou un solvate pharmaceutiquement acceptable de celui-ci. La pyridine-2-aminopyrimidine N-substituée obtenue par criblage virtuel à base de structure est utilisée en tant que composé tête de série, puis une série de nouveaux inhibiteurs de Chk1 de petites molécules sont conçus et synthétisés. Les composés sont ensuite soumis à un dosage d'activité inhibitrice de kinase Chk1 à un niveau moléculaire. Le dosage prouve que le composé a une forte performance anticancéreuse, a une activité inhibitrice de kinase Chk1, a une perspective en tant qu'inhibiteur de Chk1, et peut être appliqué à des médicaments pour la thérapie de tumeurs solides ou de leucémie solides associées à la prolifération de cellules humaines ou animales.
(ZH) 提供如下通式I所示的2-取代芳环-嘧啶类衍生物及其光学异构体或其药学上可接受的盐或溶剂合物。以通过基于结构的虚拟筛选得到的N-取代吡啶-2-氨基嘧啶为先导化合物,设计并合成了一系列全新的小分子Chk1抑制剂,并对该类化合物进行了分子水平的Chk1激酶抑制活性测试,证实所述化合物抗癌作用强,具有Chk1激酶抑制活性,是有前景的Chk1抑制剂,可应用于治疗人或动物细胞增殖性相关的实体瘤或血癌的药物。
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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)