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1. WO2022007810 - TRICYCLIC PYRIMIDINONE COMPOUND, PREPARATION METHOD THEREFOR, AND COMPOSITION AND USE THEREOF

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Publication Number WO/2022/007810
Publication Date 13.01.2022
International Application No. PCT/CN2021/104826
International Filing Date 06.07.2021
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 498/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
498Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
C07D 513/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
12in which the condensed system contains three hetero rings
C07D 471/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
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
CPC
A61K 31/519
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
519ortho- or peri-condensed with heterocyclic rings
A61K 31/5383
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
5383ortho- or peri-condensed with heterocyclic ring systems
A61P 13/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
08of the prostate
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 27/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
A61P 27/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27Drugs for disorders of the senses
02Ophthalmic agents
06Antiglaucoma agents or miotics
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
202010661516.610.07.2020CN
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 COMPOSITION ET UTILISATION DE CELUI-CI
(ZH) 三环嘧啶酮类化合物、其制备方法、其组合物和用途
front page image
Abstract
(EN) A tricyclic pyrimidinone compound as represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein the compound has a structure as represented by 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 comprising atherosclerosis.
(FR) L'invention concerne un composé de pyrimidinone tricyclique tel que représenté par la formule (I) ou un sel pharmaceutiquement acceptable de celui-ci, le composé ayant une structure telle que représentée par la formule (I), étant un nouvel inhibiteur de Lp-PLA2 complètement nouveau, et pouvant être utilisé pour traiter des maladies neurodégénératives, telles que la maladie d'Alzheimer (AD), le glaucome, la dégénérescence maculaire liée à l'âge (AMD), ou les maladies cardiovasculaires comprenant l'athérosclérose.
(ZH) 一种式（I）所示的三环嘧啶酮类化合物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的心血管疾病。
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