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1. WO2020007234 - ALKYNYL(HETERO)AROMATIC COMPOUND FOR INHIBITING PROTEIN KINASE ACTIVITY

Publication Number WO/2020/007234
Publication Date 09.01.2020
International Application No. PCT/CN2019/093469
International Filing Date 28.06.2019
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
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
4985
Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
C07D 487/04 (2006.01)
A61K 31/4985 (2006.01)
A61K 31/519 (2006.01)
A61P 35/00 (2006.01)
CPC
A61K 31/4985
A61K 31/519
A61P 1/04
A61P 11/00
A61P 17/06
A61P 19/02
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A1栋301 Room 301, Building A1 Kexing Science Park, No.15 of Keyuan Road, Nanshan District Shenzhen, Guangdong 518057, CN
Inventors
  • 王义汉 WANG, Yihan; CN
  • 邢青峰 XING, Qingfeng; CN
Priority Data
201810707422.002.07.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) ALKYNYL(HETERO)AROMATIC COMPOUND FOR INHIBITING PROTEIN KINASE ACTIVITY
(FR) COMPOSÉ ALCYNYL(HÉTÉRO)AROMATIQUE POUR L'INHIBITION DE L'ACTIVITÉ DE PROTÉINE KINASE
(ZH) 用于抑制蛋白激酶活性的炔基(杂)芳环类化合物
Abstract
(EN)
Provided is an alkynyl(hetero)aromatic compound having an inhibitory effect to protein tyrosine kinase, a pharmaceutical composition comprising same, preparation and usage thereof. Specifically, disclosed is an alkynyl(hetero)aromatic compound as shown in formula (I), wherein rings A, R 1, R 2, R 3, R 4, R 5, L, and B are defined in the description, a pharmaceutically acceptable salt, a stereisomer, a solvate, a hydrate, a crystal form, a prodrug or an isotopic variant thereof. The compound can be used for treating and/or preventing protein tyrosine kinase-related diseases, such as anti-tumor.
(FR)
L'invention concerne un composé alcynyle(hétéro)aromatique ayant un effet inhibiteur vis-à-vis de la protéine tyrosine kinase, une composition pharmaceutique le comprenant, sa préparation et son utilisation. Plus particulièrement, l'invention concerne un composé alcynyle(hétéro)aromatique tel que représenté par la formule (I), dans laquelle les cycles A, R 1, R 2, R 3, R 4, R 5, L et B sont définis dans la description, un sel pharmaceutiquement acceptable, un stéréisomère, un solvate, un hydrate, une forme cristalline, un promédicament ou un variant isotopique de celui-ci. Le composé peut être utilisé pour le traitement et/ou la prévention de maladies liées à la protéine tyrosine kinase, telles que des anti-tumeurs.
(ZH)
提供一种对蛋白酪氨酸激酶具有抑制作用的炔基(杂)芳环类化合物,包含它们的药物组合物,以及它们的制备和用途。具体地,公开了式(I)所示的炔基(杂)芳环类化合物,其中环A、R 1、R 2、R 3、R 4、R 5、L和B如说明书中所定义,及其药学上可接受的盐、立体异构体、溶剂合物、水合物、晶型、前药或同位素变体。该类化合物可用于治疗和/或预防蛋白酪氨酸激酶相关性疾病,例如抗肿瘤。
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