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heterocyclic derivatives as receptors associated with taillers
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
ANNICK GOERGLER,GUIDO GALLEY,PHILIPPE PFLIEGER,ROGER NORCROSS
申请号:
BR112014015832
公开号:
BR112014015832A8
申请日:
2013.01.08
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
Patent Summary: "Heterocyclic Derivatives as Receptors Associated with Varying Amines (Taars)". The present invention relates to the compounds of formula I wherein R1 is a one or two membered heteroaryl group selected from the group consisting of formula (a), (b), (c), (d), (e ), (f), (g), (h), (i) or (j); R2 is hydrogen or halogen; or R 1 and R 2 may form together with the carbon atoms to which the following rings of formula (k), (1), (m), (n) or (o) are attached; R3 is hydrogen, halogen or lower alkyl; n is 1 or 2; R4 is phenyl, optionally substituted by one or two substituents selected from halogen or cyano, or is pyridinyl, optionally substituted by halogen, or is tetrahydropyran, or is -nh-c (o) -phenyl, optionally substituted by halogen; R5 is hydrogen or halogen; R6 - R13 are phenyl, optionally substituted by halogen; R14 is -nh-c (o) -phenyl, substituted by halogen; R15 is hydrogen, lower alkyl substituted by halogen or is halogen; R16 is hydrogen or lower alkoxy; R17 is pyridinyl, optionally substituted by lower alkoxy or halo-substituted lower alkyl; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, to all their corresponding enantiomers and / or optical isomers, and to all tautomeric forms of the compounds of formula i. The compounds of formula I have a good affinity for the receptors for tamarins, especially for taar1. The compounds may be used to treat depression, anxiety disorders, bipolar disorder, attention-deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological disorders such as parkinson's disease, neurodegenerative disorders. such as alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, energy consumption and assimilation disorders, body temperature homeostasis disorders and malfunctions, sleep disorders and circadian rhythm;
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