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1. WO2012130153 - QUINOLINONE DERIVATIVES AND USE THEREOF AS MEDICAMENT AGAINST SCHIZOPHRENIA

Publication Number WO/2012/130153
Publication Date 04.10.2012
International Application No. PCT/CN2012/073281
International Filing Date 30.03.2012
IPC
C07D 413/14 2006.1
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
A61K 31/4709 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
435having six-membered rings with one nitrogen as the only ring hetero atom
47Quinolines; Isoquinolines
4709Non-condensed quinolines containing further heterocyclic rings
A61P 25/04 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
04Centrally acting analgesics, e.g. opioids
A61P 25/18 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
18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
A61P 25/22 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
22Anxiolytics
A61P 25/24 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
24Antidepressants
CPC
C07D 413/14
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
Applicants
  • 江苏恒谊药业有限公司 JIANGSU HENGYI PHARMACEUTICAL CO. LTD [CN]/[CN] (AllExceptUS)
  • 上海医药工业研究院 SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY [CN]/[CN] (AllExceptUS)
  • 李建其 LI, Jianqi [CN]/[CN] (UsOnly)
  • 辜顺林 GU, Shunlin [CN]/[CN] (UsOnly)
  • 蔡王平 CAI, Wangping [CN]/[CN] (UsOnly)
Inventors
  • 李建其 LI, Jianqi
  • 辜顺林 GU, Shunlin
  • 蔡王平 CAI, Wangping
Agents
  • 中原信达知识产权代理有限责任公司 CHINA SINDA INTELLECTUAL PROPERTY LTD.
Priority Data
201110079904.431.03.2011CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) QUINOLINONE DERIVATIVES AND USE THEREOF AS MEDICAMENT AGAINST SCHIZOPHRENIA
(FR) DÉRIVÉS DE QUINOLINONE ET LEUR UTILISATION COMME MÉDICAMENT CONTRE LA SCHIZOPHRÉNIE
(ZH) 喹啉酮衍生物及其作为抗精神分裂症药物的应用
Abstract
(EN) Disclosed are quinolinone derivatives and use thereof as a medicament against schizophrenia. The quinolinone derivatives of the present invention have a high affinity to dopamine d2 receptors, not only showing a relatively strong antagonist activity, but also exhibiting partial activation of d2 receptors. The compounds have good oral absorption and exhibit low acute toxicity (LD50 > 1500 mg/kg, a single gavage in mice) that is equivalent to aripiprazole and ziprasidone and far lower than risperidone, thus having the potential to be developed into a novel medicament against schizophrenia. The general structure is as follows:
(FR) L'invention concerne des dérivés de quinolinone et leur utilisation comme médicament contre la schizophrénie. Les dérivés de quinolinone de la présente invention ont une affinité élevée pour les récepteurs d2 de la dopamine, lesquels présentent non seulement une activité antagoniste relativement puissante, mais encore manifestant une activation partielle de récepteurs d2. Les composés ont une bonne absorption par voie orale et présentent une faible toxicité aiguë (DL50 > 1 500 mg/kg, un simple gavage chez les souris) qui est équivalente à l'aripiprazole et à la ziprasidone et de loin inférieure à la rispéridone, ayant ainsi le potentiel d'être élaborés sous la forme d'un nouveau médicament contre la schizophrénie. La structure générale est la suivante :
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