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1. (WO2017096648) PLK1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/096648 International Application No.: PCT/CN2015/098880
Publication Date: 15.06.2017 International Filing Date: 25.12.2015
IPC:
C07D 403/14 (2006.01) ,A61K 31/4178 (2006.01) ,A61K 31/497 (2006.01) ,A61K 31/4184 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
4178
not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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
4965
Non-condensed pyrazines
497
containing further heterocyclic 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
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
4184
condensed with carbocyclic rings, e.g. benzimidazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
深圳先进技术研究院 SHENZHEN INSTITUTES OF ADVANCED TECHNOLOGY [CN/CN]; 中国广东省深圳市 南山区西丽大学城学苑大道1068号 No.1068, Xueyuan Avenue, Xili University Town, Nanshan District Shenzhen, Guangdong 518055, CN
Inventors:
粟武 SU, Wu; CN
李红昌 LI, Hongchang; CN
房丽晶 FANG, Lijing; CN
刘科 LIU, Ke; CN
张建超 ZHANG, Jianchao; CN
潘正银 PAN, Zhengyin; CN
Agent:
北京三友知识产权代理有限公司 BEIJING SANYOU INTELLECTUAL PROPERTY AGENCY LTD.; 中国北京市 金融街35号国际企业大厦A座16层 16th Fl., Block A, Corporate Square, No.35 Jinrong Street Beijing 100033, CN
Priority Data:
201510916228.X10.12.2015CN
Title (EN) PLK1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
(FR) INHIBITEUR DE PLK1, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) PLK1抑制剂及其制备方法与应用
Abstract:
(EN) The present invention provides a PLK1 inhibitor and a preparation method and a use thereof. The PLK1 inhibitor is a compound of general formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the groups in formula (I) are as defined in the description. The PLK1 inhibitor of the present invention can specifically bind with high affinity to a DNA sequence, as shown by SEQ ID NO: 1, in the transcription promoter region of a PLK1 gene to inhibit the transcription of the PLK1 gene and thus inhibit the expression of a PLK1 protein, resulting in inhibition of growth of tumor cells or apoptosis of the cells. Moreover, the PLK1 inhibitor of the present invention can pass through cell membranes and nuclear membranes and resist hydrolysis by nucleases. Further, the PLK1 inhibitor of the present invention overcomes the problem of drug resistance facing small-molecule kinase inhibitors.
(FR) La présente invention concerne un inhibiteur de PLK1, son procédé de préparation et son utilisation. L'inhibiteur de PLK1 est un composé de formule générale (I) ou un stéréoisomère ou un sel pharmaceutiquement acceptable de celui-ci, les groupes de la formule (I) étant tels que définis dans la description. L'inhibiteur de PLK1 de la présente invention peut se lier spécifiquement avec une grande affinité à une séquence d'ADN telle que présentée dans SEQ ID NO : 1, dans la région de promoteur de transcription d'un gène PLK1 pour inhiber la transcription du gène PLK1 et ainsi inhiber l'expression d'une protéine PLK1, entraînant l'inhibition de la croissance des cellules tumorales ou l'apoptose des cellules. En outre, l'inhibiteur de PLK1 de la présente invention peut traverser les membranes cellulaires et les membranes nucléaires et résister à l'hydrolyse par les nucléases. L'inhibiteur de PLK1 de la présente invention résout en outre le problème de pharmacorésistance posé par les petites molécules inhibitrices de kinases.
(ZH) 本发明提供PLK1抑制剂及其制备方法与应用,所述PLK1抑制剂具有通式(I)所示的化合物、其立体异构体或药学上可接受的盐,式(I)中的各基团的定义与说明书相同。本发明所述PLK1抑制剂能够特异性高强度的结合于SEQ:NO:1所示的PLK1基因转录启动子区域中的DNA序列,抑制PLK1基因的转录,抑制PLK1蛋白的表达,造成肿瘤细胞生长抑制或凋亡,并且其能够穿过细胞膜和核膜及抵抗核酸酶水解,此外,其还克服了小分子激酶抑制剂的耐药性难题。
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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, 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, 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)