TH127042A - Benzamide derivatives are replaced. - Google Patents

Abstract

DC60 (20/06/55) The invention involves compounds of the formula (chemical formula) I where R is hydrogen or low molecular weight alkyl; R1 is - (CH2) n- (O) o- heterocyclic alkyl. (heterocycloalky) or -C (O) - heterocyclo-alkyl, where the heterocycloalkyl group Will be replaced optionally By low molecular mass alkyl, hydroxy, halogen, or by - (CH2) p-aryl (arly); n is 0,1 or 2; o is 0 or 1; p is 0,1 or 2; R2 is CF3, cycloalkyl, optionally substituted by low molecular mass alkoxy or halogen, or is indan. -2-il (indany-2-yl), or heterocyclic alkyl, is optionally replaced by heteroeryl. (heteroaryl), or is the heteroaryl, where the aromatic ring is optionally replaced by one or two agents, selected from the alkyl mass. Low molecule, halogen, heteroeryl, hydroxyapatite, CF3, OCF3, OCH2 CF3, OCH2-cycloalkyl, OCH2C (CH2 OH) (CH2 CI) (CH3), S-low molecular mass alkyl, low molecular mass alkoxy, CH2-low molecular mass alkyl, low molecular mass alkinyl or cyano, or by -C. (O) - phenyl, -O-phenyl, -O-CH2-phenyl, phenyl or -CH2-phenyl, and where the phenyl ring may be substituted alternatively by halo. Gen, -C (O) - low molecular mass alkyl, -C (O) OH or -C (O) O-low molecular mass alkyl, or aromatic ring is replaced as Alternative by heterocyclic alkyl, OCH2-oxytan-3-il (OCH2-oxetan-3-yl) or O-tetrahydropyran-4-il (O-tetrahydropyran-4-yl), optionally replaced by low molecular mass alkyl; X is the bond, -NR'-, -CH2NH-, -CHR "-, - (CHR") q-O-, -O- (CHR ") q- or - (CH2) 2-; Y is bond or -CH2- R 'is hydrogen or low molecular mass alkyl, R "is hydrogen, low molecular mass alkyl, CF3, low molecular mass alkyl, q is 0, 1, 2. Or 3; Or with salts from the addition of a pharmaceutical acid suitable It has now been found that Compounds of formula I have good affinity to receptors that Associated with low-dose amines (TAARs), specifically for TAAR1, the compound may be used for the treatment of depression, anxiety disorders, bipolar disorders, impaired consciousness and anxiety disorders. Inactivity (ADHD), stress-related disorders, psychological disorders such as schizophrenia, neurological disorders such as Parkinson's disease, degenerative neurological disorders such as Alzheimer's disease. Mercury, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, disease Hyperlipidemia, hypokalemia, metabolic disorders and tissue enhancement, abnormalities and functions of hypothermia, sleep disorders, and Rhythms, cycles of the day, and heart disorders Joint - blood vessels The invention involves a compound of the formula (chemical formula) where R is a low molecular weight hydrogen or alkyl; R1 is - (CH2) n- (O) 0- heterocyclic alkyl. (heterocycloalky) or -C (O) - heterocyclo-alkyl, where the heterocycloalkyl group Will be replaced optionally By low molecular mass alkyl, hydroxy, halogen, or by - (CH2) p-aryl (arly); n is 0,1 or 2; o is 0 or 1; p is 0,1 or 2; R2 is CF3, cycloalkyl, optionally replaced by low-molecular-mass alkoxy or halogen, or is indan-2. - il (indany-2-yl), or heterocyclo-alkyl, is optionally replaced by heteroeryl (heteroaryl), or is the heteroaryl, where the aromatic ring is optionally replaced by one or two agents, selected from the alkyl mass. Low molecule, halogen, heteroeryl, hydroxyapatite, CF3, OCF3, OCH2 CF3, OCH2-cycloalkyl, OCH2C (CH2 OH) (CH2 CI) (CH3), S-low molecular mass alkyl, low molecular mass alkoxy, CH2-low molecular mass alkyl, low molecular mass alkinyl or cyano, or by -C. (O) - phenyl, -O-phenyl, -O-CH2-phenyl, or -CH2-phenyl, and where the phenyl ring may be substituted alternatively by halogens, -C (O) - low molecular mass alkyl, -C (O) OH or -C (O) O-low molecular mass alkyl, or aromatic ring is optionally replaced. By heterocyclic alkyl, OCH2-oxytan-3-il (OCH2-oxetan-3-yl) or O-tetrahydropyran-4-il (O-tetrahydropyran-4-yl), optionally replaced by low molecular mass alkyl; X is the bond, -NR'-, -CH2NH-, -CHR "-, - (CHR") q-O-, -O- (CHR ") q- or - (CH2) 2-; Y is bond or -CH2- R 'is hydrogen or low molecular mass alkyl, R "is hydrogen, low molecular mass alkyl, CF3, low molecular mass alkyl, q is 0,1,2. Or 3; Or with salts from the addition of a pharmaceutical acid suitable It has now been found that Compounds of formula I have good affinity to receptors that Associated with low-dose amines (TAARs), specifically for TAAR1, the compound may be used for the treatment of depression, anxiety disorders, bipolar disorders, impaired consciousness and anxiety disorders. Inactivity (ADHD), stress-related disorders, mental disorders such as schizophrenia, neurological disorders such as Parkinson's disease, degenerative nervous disorders such as Alzheimer's disease. Mercury, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, disease Hyperlipidemia, hypokalemia, metabolic disorders and tissue enhancement, abnormalities and functions of hypothermia, sleep disorders, and Rhythms, cycles of the day, and heart disorders Joint-vascular drug patent

Claims (1)

1. Compounds of the formula (chemical formula) where R is hydrogen or C1-7-alkyl; R1 is - (CH2) n- (O) 0- heterocyclos. Alkyl (heterocycloalky), where the heterocycloalkyl group is alternately replaced by C1-7-alkyl, hydroxyl or halogen. ; n is 0,1 or 2; o is 0 or 1; p is 0,1 or 2; R2 is CF3, tag: drug patent.