Heteroaromatic NMDA receptor modulators and uses thereof

An individual and carrier technology, applied in medical preparations containing active ingredients, drug combinations, organic chemistry, etc., can solve problems such as unclear functions

Pending Publication Date: 2021-03-16
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The GluN3 subunit has also been identified, but its function is unclear

Method used

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  • Heteroaromatic NMDA receptor modulators and uses thereof
  • Heteroaromatic NMDA receptor modulators and uses thereof
  • Heteroaromatic NMDA receptor modulators and uses thereof

Examples

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example

[0050] Example 1-5-(3-chloro-4-fluorophenyl)-7-cyclopropyl-3-(2-(3-fluoro-3-methylazidine-1-yl)-2-oxo Preparation of ethyl)-3,7-dihydro-4H-pyrrole[2,3-d]pyrimidin-4-one (compound 1)

[0051]

[0052] Step-1: Preparation of 4,6-dichloro-5-(2,2-diethoxyethyl)pyrimidine (2):

[0053] Ammonium chloride was added to a solution of 2-(4,6-dichloropyrimidin-5-yl)acetaldehyde (1,5 g, 26.17 mmol) in ethanol (250 mL), and the reaction mixture was refluxed for 20 hours. The reaction mixture was concentrated; the residue was diluted with water (50 mL) and extracted with ethyl acetate (2 x 100 mL). The combined organic layers were dried over anhydrous sodium sulfate, filtered and concentrated to give the title compound 4,6-dichloro-5-(2,2-diethoxyethyl)pyrimidine (2 , 6.9 g, crude product). Calculated (M+H): 265.04; Found (M+H): 265.

[0054] Step-2: Preparation of 4-chloro-7-cyclopropyl-7H-pyrrole[2,3-d]pyrimidine (3):

[0055]Add cyclopropylamine (2 mL, 28.62 mmol) to 4,6-dichloro...

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Abstract

Provided are 5-(3-chloro-4-fluorophenyl)-7-cyclopropyl-3-(2-(3-fluoro-3-methylazetidin-1-yl)-2-oxoethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one and pharmaceutically acceptable salts thereof, andtheir uses in the treatment of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system.

Description

[0001] Related applications [0002] This application claims the benefit of priority to U.S. Provisional Application No. 62 / 714,100, filed August 3, 2018, the entire contents of which are incorporated herein by reference. Background technique [0003] Neurological disorders are the leading cause of human disability as measured by the global burden of disease. Even major diseases of the nervous system for which health authorities have approved their treatments (including psychiatric disorders such as schizophrenia, neurological disorders such as Alzheimer's disease, and neurological disorders such as Attention Deficit and Hyperactivity Disorder) developmental disorders) are poorly managed due to the limited efficacy of approved treatments and severe side effects, resulting in a significant burden of unmet medical need. In addition, there are many major rare neurological disorders for which there are no approved treatments, such as neurodevelopmental abnormalities on the autis...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): C07D487/04A61P25/18
CPCC07D487/04A61P25/18A61K31/519A61P25/28
InventorR·A·沃克曼D·R·安德森S·马勒基亚尼T·皮瑟G·F·基尼S·C·雷瑟
OwnerNOVARTIS AG