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1. WO2017128036 - QUINAZOLINONE PARP-1 INHIBITOR AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Publication Number WO/2017/128036
Publication Date 03.08.2017
International Application No. PCT/CN2016/072135
International Filing Date 26.01.2016
IPC
C07D 403/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
C07D 239/96 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
95with hetero atoms directly attached in positions 2 and 4
96Two oxygen atoms
C07D 401/10 2006.01
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
10linked by a carbon chain containing aromatic rings
A61K 31/517 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
517ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/541 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
54having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
541Non-condensed thiazines containing further heterocyclic rings
A61K 31/5377 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
535having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
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
A61K 31/5377
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541
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
54having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
541Non-condensed thiazines containing further heterocyclic rings
C07D 239/96
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
95with hetero atoms directly attached in positions 2 and 4
96Two oxygen atoms
C07D 401/10
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
10linked by a carbon chain containing aromatic rings
C07D 403/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
Applicants
  • 中国医学科学院药物研究所 INSTITUTE OF MATARIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES [CN]/[CN]
  • 北京科莱博医药开发有限责任公司 BEIJNG COLLAB PHARMA CO., LTD [CN]/[CN]
Inventors
  • 徐柏玲 XU, Bailing
  • 陈晓光 CHEN, Xiaoguang
  • 姚海平 YAO, Haiping
  • 季鸣 JI, Ming
  • 金晶 JIN, Jing
  • 周洁 ZHOU, Jie
  • 王珂 WANG, Ke
  • 赵大龙 ZHAO, Dalong
Agents
  • 北京三高永信知识产权代理有限责任公司 BEIJING SAN GAO YONG XIN INTELLECTUAL PROPERTY AGENCY CO., LTD.
Priority Data
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) QUINAZOLINONE PARP-1 INHIBITOR AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
(FR) INHIBITEUR DE PARP-1 À BASE DE QUINAZOLINONE ET SON PROCÉDÉ DE PRÉPARATION, COMPOSITION PHARMACEUTIQUE ET UTILISATION ASSOCIÉES
(ZH) 喹唑啉酮类PARP-1抑制剂及其制备方法、药物组合物和用途
Abstract
(EN)
Disclosed are a new class of quinazoline-2,4 (1H, 3H)-diketone PARP-1 inhibitors, and a preparation method and pharmaceutical composition and a use thereof. In particular, the present invention relates to a quinazoline-2,4 (1H, 3H)-diketone derivative as shown in general formula I and a stereoisomer thereof, pharmaceutically acceptable salts thereof, and a preparation method thereof, a composition comprising one or more of such compounds, and a use of such compounds in the preparation of drugs for preventing and/or treating tumours.
(FR)
La présente invention concerne une nouvelle classe d'inhibiteurs de PARP-1 à base de quinazoline-2,4(1H,3H)-dicétone, et leur procédé de préparation et une composition pharmaceutique et une utilisation associées. En particulier, la présente invention concerne un dérivé de quinazoline-2,4(1H,3H)-dicétone tel que représenté par la formule générale I et un stéréoisomère de celui-ci, des sels pharmaceutiquement acceptables de celui-ci, et son procédé de préparation, une composition comprenant un ou plusieurs de ces composés, et une utilisation de ces composés dans la préparation de médicaments pour la prévention et/ou le traitement de tumeurs.
(ZH)
本发明公开了一类新的喹唑啉-2,4(1H,3H)-二酮类PARP-1抑制剂、及其制法和药物组合物与用途。具体而言,本发明涉及通式I所示的喹唑啉-2,4(1H,3H)-二酮类衍生物及其立体异构体、其可药用盐,及其制备方法,含有一个或多个该类化合物的组合物,和该类化合物在制备、预防和/或治疗肿瘤药物中的用途。
Also published as
Latest bibliographic data on file with the International Bureau