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1. WO2018086446 - SUBSTITUTED QUINAZOLINE COMPOUND HAVING BLOOD-BRAIN BARRIER PENETRATION CAPABILITY

Publication Number WO/2018/086446
Publication Date 17.05.2018
International Application No. PCT/CN2017/106616
International Filing Date 17.10.2017
IPC
C07D 405/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14containing three or more hetero rings
C07D 401/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61K 31/517 2006.1
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
517ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 25/28 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
CPC
A61K 31/517
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
517ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
04specific for metastasis
C07B 2200/07
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
07Optical isomers
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic 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
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • 威尚(上海)生物医药有限公司 WEISHANG (SHANGHAI) BIO-PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 钟卫 ZHONG, Wei
Agents
  • 上海汉声知识产权代理有限公司 SHANGHAI HANGSOME INTELLECTUAL PROPERTY LTD.
Priority Data
201610982608.808.11.2016CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) SUBSTITUTED QUINAZOLINE COMPOUND HAVING BLOOD-BRAIN BARRIER PENETRATION CAPABILITY
(FR) COMPOSÉ QUINAZOLINE SUBSTITUÉ AYANT UNE CAPACITÉ DE PÉNÉTRATION DE BARRIÈRE HÉMATO-ENCÉPHALIQUE
(ZH) 具有穿过血脑屏障能力的取代的喹唑啉化合物
Abstract
(EN) Disclosed is a substituted quinazoline compound having blood-brain barrier penetration capability. The structural formula of the compound is as represented by formula (I). The substituted quinazoline compound of the present invention, and a derivative and a pharmaceutical salt thereof have unexpected blood-brain barrier penetration capability, and pharmaceutical characteristics which enable them to serve as protein kinase inhibitors. They are particularly used for medical situations mediated by some activated and mutated forms of an epidermal growth factor receptor, and can be used for treating or preventing disorders associated with abnormal protein kinase activity, such as cancer, brain metastasis, meningeal metastasis, and central nervous diseases.
(FR) L'invention concerne un composé quinazoline substitué ayant une capacité de pénétration de barrière hémato-encéphalique. La formule structurelle du composé est telle que représentée dans la formule (I). Le composé quinazoline substitué de la présente invention, et un dérivé et un sel pharmaceutique de celui-ci ont une capacité de pénétration de barrière hémato-encéphalique inattendue, et des caractéristiques pharmaceutiques qui leur permettent de servir d'inhibiteurs de protéine kinase. Ils sont particulièrement utilisés pour des situations médicales induites par certaines formes activées et mutées d'un récepteur du facteur de croissance épidermique, et peut être utilisée pour traiter ou prévenir des troubles associés à une activité anormale des protéines kinases, tels que le cancer, les métastases cérébrales, les métastases méningées et les maladies du système nerveux central.
(ZH) 本发明公开了一种具有穿过血脑屏障能力的取代的喹唑啉化合物;该化合物的结构式如式(I)所示。本发明的喹唑啉化合物、衍生物及其药学盐具有预料之外的具有穿过血脑屏障的能力,并能作为蛋白激酶抑制剂的药物特性,尤其是针对通过表皮生长因子受体的某些活化突变形式介导的医疗状况,并且可用于治疗或预防异常蛋白激酶活性相关的紊乱,例如癌症、癌症脑转移,癌症脑膜转移和神经中枢疾病等。
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