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1. WO2020207352 - TRIAZINE BENZIMIDAZOLE COMPOUNDS AND MEDICAL USE THEREOF

Publication Number WO/2020/207352
Publication Date 15.10.2020
International Application No. PCT/CN2020/083270
International Filing Date 03.04.2020
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • 四川科伦博泰生物医药股份有限公司 SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 陈寿军 CHEN, Shoujun
  • 宋帅 SONG, Shuai
  • 蒋小玲 JIANG, Xiaoling
  • 唐祖建 TANG, Zujian
  • 田强 TIAN, Qiang
  • 宋宏梅 SONG, Hongmei
  • 薛彤彤 XUE, Tongtong
  • 王晶翼 WANG, Jingyi
Agents
  • 中国国际贸易促进委员会专利商标事务所 CCPIT PATENT AND TRADEMARK LAW OFFICE
Priority Data
201910289078.211.04.2019CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) TRIAZINE BENZIMIDAZOLE COMPOUNDS AND MEDICAL USE THEREOF
(FR) COMPOSÉS DE BENZIMIDAZOLE TRIAZINE ET LEUR UTILISATION MÉDICALE
(ZH) 三嗪酮并咪唑类化合物及其医药用途
Abstract
(EN)
The present invention relates to the field of medicine, and in particular, to a compound as represented by formula I, pharmaceutically acceptable salts or esters, solvates, stereoisomers, tautomers, prodrugs, any crystalline form, metabolites thereof or a mixture thereof. The present invention further relates to a medical use of the compound as represented by formula I, pharmaceutically acceptable salts or esters, solvates, stereoisomers, tautomers, prodrugs, any crystalline form, metabolites thereof or the mixture thereof. The compound in the present invention has a strong inhibition effect on the activity of deubiquitinating enzyme USP7, has good pharmacokinetics property, and can be used to prevent or treat the cancer disease.
(FR)
La présente invention se rapporte au domaine de la médecine et, concerne en particulier, un composé tel que représenté par la formule I, des sels ou des esters pharmaceutiquement acceptables, des solvates, des stéréoisomères, des tautomères, des promédicaments, toute forme cristalline, des métabolites de ceux-ci ou un mélange de ceux-ci. La présente invention concerne en outre une utilisation médicale du composé tel que représenté par la formule I, des sels ou esters pharmaceutiquement acceptables, des solvates, des stéréoisomères, des tautomères, des promédicaments, toute forme cristalline, des métabolites de ceux-ci ou un mélange de ceux-ci. Le composé selon la présente invention a un fort effet d'inhibition sur l'activité de l'enzyme de désubiquitination USP7, a une bonne propriété pharmacocinétique, et peut être utilisé pour prévenir ou traiter une maladie cancéreuse.
(ZH)
本发明属于医药领域,具体涉及式I所示的化合物、其可药用盐、酯、溶剂化物、立体异构体、互变异构体、前药、任意晶型、代谢物或它们的混合物。本发明还涉及式I所示的化合物、其可药用盐、酯、溶剂化物、立体异构体、互变异构体、前药、任意晶型、代谢物或它们的混合物的医药用途。本发明化合物对去泛素化酶USP7的活性具有较强抑制作用,具有良好的药代动力学性质,能用于预防或治疗癌症疾病。
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