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pyrazole carboxamide derivatives as modulators of taar for use in the treatment of various disorders, such as depression, diabetes, and parkinson's disease
专利权人:
F. HOFFMANN-LA ROCHE AG;HOFFMANN-LA ROCHE INC.
发明人:
GALLEY, Guido,NORCROSS, Roger,PFLIEGER, Philippe
申请号:
MA37944
公开号:
MA37944B2
申请日:
2013.09.11
申请国别(地区):
MA
年份:
2017
代理人:
摘要:
the present invention relates to compounds of formula (i), wherein r1 is phenyl optionally substituted by halogen, lower alkyl, cycloalkyl, lower alkyl, lower alkoxy, cyano, halogen, lower alkyl substituted by hydroxy, lower alkoxy, substituted by participants. halogen or lower alkoxy substituted internal substituted with hydroxy, or pyridine - 2, 3 - or 4 - yl.optionally substituted by halogen, lower alkyl, lower alkyl, cycloalkyl, halogen, cyano, lower alkyl substituted by hydroxy, lower alkoxy, substituted lower alkoxy, halogen, lower alkoxy, or substituted lower hydroxyl substituted pyri; or midin - 2, 4, or 5 acetate, optionally substituted by halogen, lower alkyl, cycloalkyl, lowerlower alkyl, lower alkyl substituted by hydroxy or halogen substituted or pyrazin) is optionally substituted by halogen, acetate, alkyl, cycloalkyl, lower alkyl, lower alkyl substituted by halogen, lower, less substituted by hydroxy or cyano; and 2,2-difluorobenzo [d] [1,3] - 5 - dioxol acetate or thiazolyl)optionally substituted by halogen, lower alkyl, substituted alkyl, r2 is hydrogen, or r3 is hydrogen, lower alkyl, amino or lower; and z is a bond, - ch2 -, or - o -; or a pharmaceutically suitable acid addition salt.it has now been found that the compounds of formula i have a good affinity for the receptors to trace amines, including taar1 taar).the compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (adhd), stress related disorders, psychotic disorders, such as schizophrenia, neurological diseases such. the parkinson's disease, neurodegenerative diseases such as alzheimer's disease.epilepsy, migraine, hypertension, abuse of alcohol or other drugs and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, impaired energy consumption and the assimilatio no, trouble and malfunction of the homeostasis of body temperature.the effects of sleep and circadian
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