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SUBSTITUTED AZETIDINE DERIVATIVES AS TAAR LIGANDS
专利权人:
发明人:
申请号:
HK17109001.9
公开号:
HK1235395A
申请日:
2017.09.06
申请国别(地区):
HK
年份:
2018
代理人:
摘要:
The present invention relates to a compound of formula I wherein R1 is hydrogen, methoxy or fluoro R2/R2 are independently from each other hydrogen, methoxy or fluoro R3/R4 are independently from each other hydrogen or halogen R is hydrogen or fluoro L1 is -CH2-, -NR-, -0-, -S-, CF2- or CH= R is hydrogen or lower alkyl L2 is a bond, -C(0)NH-, -NH-, -CH2NHC(O)-, -NHC(O)- or -NHC(0)NH- R is hydrogen, halogen, lower alkoxy, cyano or is phenyl optionally substituted by one or more substituents, selected from halogen, lower alkyl substituted by halogen or lower alkoxy, or is a five or six membered heteroaryl, selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl or pyrazolyl, which heteroaryls are optionally substituted by one or more substituents, selected from halogen, lower alkyl, lower alkoxy, cyano, cycloalkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or by phenyl substituted by halogen N is a ring nitrogen atom in position 1 or 2 or to a pharmaceutically suitable acid addition salt thereof. The compounds of formulas I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and may 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 as Parkinsons disease, neurodegenerative disorders such as Alzheimers disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.La présente invention concerne un composé de formule I dans laquelle R1 est un hydrogène, un méthoxy ou un fluoro R2/R2 sont indépendamment lun de lautre un hydrogène, un méthoxy ou un fluo
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