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1. WO2022001881 - TRICYCLIC PYRIMIDINONE COMPOUND, PREPARATION METHOD THEREFOR, AND COMPOSITION AND USE THEREOF

Publication Number WO/2022/001881
Publication Date 06.01.2022
International Application No. PCT/CN2021/102420
International Filing Date 25.06.2021
IPC
C07D 487/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 487/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
12in which the condensed system contains three hetero rings
A61K 31/522 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
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
522having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/519 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
519ortho- or peri-condensed with heterocyclic rings
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
Applicants
  • 上海纽思克生物科技有限公司 NEUSCO BIOTECH LIMITED [CN]/[CN]
Inventors
  • 顾正华 GU, Zhenghua
  • 王冬琴 WANG, Dongqin
  • 胡有洪 HU, Youhong
Agents
  • 北京坦路来专利代理有限公司 BEIJING TANLULAI PATENT AGENT LTD
Priority Data
202010608551.130.06.2020CN
202010952714.811.09.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) TRICYCLIC PYRIMIDINONE COMPOUND, PREPARATION METHOD THEREFOR, AND COMPOSITION AND USE THEREOF
(FR) COMPOSÉ DE PYRIMIDINONE TRICYCLIQUE, SON PROCÉDÉ DE PRÉPARATION ET SA COMPOSITION AINSI QUE SON UTILISATION
(ZH) 三环嘧啶酮类化合物、其制备方法、其组合物和用途
Abstract
(EN) A tricyclic pyrimidinone compound as shown in formula (I) or a tautomer, a mesomer, a raceme, an enantiomer, or a diastereoisomer thereof, or a form of a mixture thereof, or a pharmaceutically acceptable salt thereof, wherein same has the structure as shown in formula (I), is a completely new Lp-PLA2 inhibitor, and can be used for treating neurodegenerative-related diseases, such as Alzheimer’s disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis, etc.
(FR) L'invention concerne un composé de pyrimidinone tricyclique tel que représenté dans la formule (I) ou un tautomère, un mésomère, un racémique, un énantiomère ou un diastéréoisomère associé, ou une forme d'un mélange associé, ou un sel pharmaceutiquement acceptable associé. Ledit composé a la structure telle que représentée dans la formule (I), est un inhibiteur complètement nouveau de Lp-PLA2, et peut être utilisé pour traiter des maladies neurodégénératives, telles que la maladie d'Alzheimer (MA), le glaucome, la dégénérescence maculaire liée à l'âge (DMLA) ou les maladies cardiovasculaires comme l'athérosclérose, etc.
(ZH) 一种式(I)所示的三环嘧啶酮类化合物或其互变异构体、内消旋体、外消旋体、对映异构体、非对映异构体、或其混合物形式、或其药学上可接受的盐,具有式(I)所示的结构,是一种全新的Lp-PLA2抑制剂,可用于治疗神经退行性相关疾病,如阿尔茨海默病(AD)、青光眼、年龄相关的黄斑变性(AMD),或者包括动脉粥样硬化等心血管疾病。
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