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1. WO2020134921 - AMINO QUINAZOLINONE, AMINO ISOQUINOLONE DERIVATIVES AND APPLICATION THEREOF

Publication Number WO/2020/134921
Publication Date 02.07.2020
International Application No. PCT/CN2019/122973
International Filing Date 04.12.2019
IPC
C07D 239/95 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
C07D 401/12 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
12linked by a chain containing hetero atoms as chain links
C07D 403/12 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
12linked by a chain containing hetero atoms as chain links
C07D 417/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 413/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
C07D 473/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
CPC
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 13/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
12of the kidneys
A61P 17/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
06Antipsoriatics
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 19/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
Applicants
  • 浙江大学 ZHEJIANG UNIVERSITY [CN]/[CN]
  • 中国科学院上海药物研究所 SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES [CN]/[CN]
Inventors
  • 盛荣 SHENG, Rong
  • 李佳 LI, Jia
  • 顾东炎 GU, Dongyan
  • 周宇波 ZHOU, Yubo
  • 危俊 WEI, Jun
  • 张梦梦 ZHANG, Mengmeng
  • 胡永洲 HU, Yongzhou
  • 张凯祥 ZHANG, Kaixiang
  • 刘婕妤 LIU, Jieyu
  • 阚伟娟 KAN, Weijuan
Agents
  • 杭州求是专利事务所有限公司 HANGZHOU QIUSHI PATENT OFFICE CO.,LTD.
Priority Data
201811593915.225.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) AMINO QUINAZOLINONE, AMINO ISOQUINOLONE DERIVATIVES AND APPLICATION THEREOF
(FR) AMINO QUINAZOLINONE, DÉRIVÉS D'AMINOISOQUINOLONE ET UTILISATION ASSOCIÉE
(ZH) 氨基喹唑啉酮和氨基异喹啉酮衍生物及其应用
Abstract
(EN)
Provided by the present invention are an amino quinazolinone and amino isoquinolone derivatives. It is verified by numerous experiments that the compounds provided by the present invention have good inhibiting effects on PI3Kα and PI3Kγ, most of the compounds have prominent inhibiting effect on PI3Kα, and show strong growth inhibiting effect on PIK3CA mutant tumor cells such as human breast cancer cell strain (MCF7). Therefore, the amino quinazolinone and amino isoquinolone derivatives according to the present invention can be applied in the preparation of anti-tumor and anti-inflammatory medicines, and can be used as PI3Kα inhibitors in the preparation of medicines for treatment of human or animal cell proliferation related tumors, the medicines comprising the derivatives any one or more of pharmaceutically acceptable salts and solvates thereof as well as pharmaceutically acceptable carriers. Formulas a and b for the compounds of the present invention are shown as below:
(FR)
La présente invention concerne un amino quinazolinone et des dérivés d'aminoisoquinolone. De nombreuses expériences montrent que les composés fournis par la présente invention ont de bons effets inhibiteurs sur PI3Kα et PI3Kγ, la plupart des composés ayant un effet inhibiteur important sur PI3Kα, et présentent un effet inhibiteur de croissance puissant sur des cellules tumorales mutantes PIK3CA telles que la souche de cellules du cancer du sein humain (MCF7). Par conséquent, l'amino quinazolinone et les dérivés d'aminoisoquinolone selon la présente invention peuvent être utilisés dans la préparation de médicaments anti-tumoraux et anti-inflammatoires, et peuvent être utilisés en tant qu'inhibiteurs de PI3Kα dans la préparation de médicaments pour le traitement de tumeurs associées à la prolifération de cellules humaines ou animales, des médicaments comprenant les dérivés, l'un quelconque ou plusieurs de leurs sels et solvates pharmaceutiquement acceptables, ainsi que des véhicules pharmaceutiquement acceptables. Les formules a et b pour les composés selon la présente invention sont présentées ci-dessous :
(ZH)
本发明提供一种氨基喹唑啉酮和氨基异喹啉酮类衍生物,本发明经通过多次实验证实,所合成的化合物均具有优良的PI3Kα,PI3Kγ的抑制作用,其中大部分化合物对PI3Kα有显著的抑制作用,对PIK3CA突变的人乳腺癌细胞细胞株(MCF7)等肿瘤细胞株显示出强效的抑制生长作用。因此,本发明所述氨基喹唑啉酮和氨基异喹啉酮类衍生物可在制备抗肿瘤和抗炎药物中的应用,可作为PI3Kα抑制剂应用于治疗人或动物细胞增殖性相关的肿瘤的药物,所述药物包括衍生物及其药学上可接受的盐、溶剂合物中的任意一种或任意多种与药学上可接受的载体。本发明化合物通式a和b结构
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