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NOVEL FUMARATE SALTS OF A HISTAMINE H3 RECEPTOR ANTAGONIST
专利权人:
SANOFI
发明人:
LANGEVIN, BEVERLY C
申请号:
NZ59721910
公开号:
NZ597219A
申请日:
2010.06.24
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
597219 Disclosed herein are fumerate salts of a compound of formula I selected from the group consisting of: 2-(cyclohexylmethyl)-N-{ 2-[(2S)-1-methylpyrrolidin-2-yl]ethyl} -1,2,3,4-tetrahydroisoquinoline-7-sulfonamide difumarate monohydrate 2-(cyclohexylmethyl)-N-{ 2-[(2S)-1-methylpyrrolidin-2-yl]ethyl} -1,2,3,4-tetrahydroisoquinoline-7-sulfonamide difumarate 2-(cyclohexylmethyl)-N-{ 2-[(2S)-1-methylpyrrolidin-2-yl]ethyl} -1,2,3,4-tetrahydroisoquinoline-7-sulfonamide monofumarate 2-(cyclohexylmethyl)-N-{ 2-[(2S)-1-methylpyrrolidin-2-yl]ethyl} -1,2,3,4-tetrahydroisoquinoline-7-sulfonamide hemifumarate 2-(cyclohexylmethyl)-N-{ 2-[(2S)-1-methylpyrrolidin-2-yl]ethyl} -1,2,3,4-tetrahydroisoquinoline-7-sulfonamide hemifumarate dehydrate and the use thereof in the treatment of a disease or disorder selected from the group consisting of obesity, diabetes?vigilance disorders?sleep disorders, narcolepsy Alzheimers disease, dementia, Parkinsons disease, attention-deficit hyperactivity disorder, memory disorders, learning disorders, epilepsy, schizophrenia, moderate cognitive disorders, depression, anxiety, sexual dysfunction, dizziness?and travel sickness. Also disclosed is a process for the manufacture of the 2-(cyclohexylmethyl)-N-{ 2-[(2S)-1-methylpyrrolidin-2-yl]ethyl} -1,2,3,4-tetrahydroisoquinoline-7-sulfonamide difumarate monohydrate comprising the steps of contacting, under elevated temperature or at ambient temperature, 2-(cyclohexylmethyl)-N-{ 2-[(2S)-1-methylpyrrolidin-2-yl]ethyl} -1,2,3,4-tetrahydroisoquinoline-7-sulfonamide dissolved in a suitable solvent or in a mixture of solvents, with fumaric acid, optionally dissolved in a solvent or in a mixture of solvents and isolating the precipitated solid.
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