CAS: 351003-34-4; 4-(Difluoromethoxy)Benzene-1-Sulfonyl Chloride

专利信息

专利号:US-2022220095-A1
优先权日:2019-04-26
标 题 :N-((HETEROARYL)METHYL)-1-TOSYL-1H-PYRAZOLE-3-CARBOXAMIDE DERIVATIVES AS Kv3 POTASSIUM CHANNEL ACTIVATORS FOR TREATING NEUROLOGICAL AND PSYCHIATRIC DISORDERS
发明人：SAMS ANETTE GRAVEN; RASMUSSEN LARS KYHN; YU WANWAN
权利人:H LUNDBECK AS
摘要:The present invention provides N-(heteroaryl)methyl)-1-tosyl-1H-pyrazole-3-carboxamide derivatives of the structure Formula (I), which activate the Kv3 potassium channels. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and to the compounds and pharmaceutical compositions thereof for use in methods of medical treatment of disorders responsive to the activation of Kv3 potassium channels, such as e.g. neurological or psychiatric disorders for example epilepsy, schizophrenia, cognitive impairment associated with schizophrenia (CIAS), autism spectrum disorder, bipolar disorder, ADHD, anxiety-related disorders, depression, cognitive dysfunction, Alzheimer's disease, Fragile X syndrome, chronic pain, hearing loss, sleep and circadian disorders, and sleep disruption. Exemplary compounds are e.g.: •4-methyl-N-((5-methylpyrazin-2-yl)methyl)-1-tosyl-1H-pyrazole-3-carboxamide (example 1; compound 32), •N-((1-methyl-1H-pyrazol-4-yl)methyl)-1-tosyl-1H-pyrazole-3-carboxamide (example 2; compound 62) •1-((4-(difluoro methoxy)phenypsulfonyl)-N-((5-methylpyrazin-2-yl)methyl)-1H-pyrazole-3-carboxamide (example 3; compound 65) The present description discloses the synthesis of exemplary compounds as well as relevant biological activity data (e.g. pages 24 to 47; examples 1 to 3; table 1; compounds 1 to 86).