TH128478A - Aeryl cyclohexyl ether of dihydrotetracenzobenzolines - Google Patents

Abstract

DC60 (19/02/53) The present invention relates to the aryl cyclohexyl ether of the dihydro-tetraazabenzoazulene derivative, i.e., the aryl cyclohexyl ether of the 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene derivative of formula I (chemical formula) I, where R1, R2 and R3 are defined as given herein. The compounds according to the invention act as V1a receptor regulators, and specifically as V1a receptor antagonists, their production, pharmaceutical compositions containing them, and their use as important drugs. The active compounds of the present invention are useful in The potential of the compounds to act as peripheral and central nervous system agents in conditions of menstrual pain, male or female sexual dysfunction, hypertension, chronic heart failure, vasopressin deficiency, cirrhosis, nephrotic syndrome, anxiety, depression, obsessive-compulsive disorder, autism spectrum disorder, schizophrenia, and aggressive behavior. The present invention relates to the aryl cyclohexyl ether of the dihydro-tetraazaebenzoazule derivative, i.e., the aryl cyclohexyl ether of the 5,6-dihydro-4H-2,3,5,10b-tetraazae-benzo(e)azule derivative of formula I (formula), where R1, R2, and R3 are defined herein. The compounds according to the invention act as V1a receptor modulators, and specifically as V1a receptor antagonists, their production, pharmaceutical compositions containing them, and their use as active medicines. The active compounds of the present invention are useful in... It is a therapeutic agent that acts on the peripheral and central nervous systems in conditions such as menstrual pain, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate vasopressin release, cirrhosis, nephrotic syndrome, anxiety, depression, obsessive-compulsive disorder, autism spectrum disorder, schizophrenia, and aggressive behavior.

Claims (1)

Revised 10/10/2018, Page 1 of 9. Claim 1. Compounds of general formula I (chemical formula structure) I, where R1 is an aryl or heteroaryl, unsubstituted or independently substituted by one or more substituents chosen from A, R2 is H, C1-12-alkyl, unsubstituted or substituted by one or more OH, halo, cyano or C1-12-alkoxy, -(CH2)q-Ra, where Ra is a phenyl or heteroaryl with 5 or 6 members, each unsubstituted or independently substituted by one or more substituents chosen from A, -(CH2)rNRiRii, -C(O)-C1-12-alkyl, where C1-12-alkyl is unsubstituted or substituted by one or more substituents. Or more of OH, halo, cyano or C1-12-alkoxy, -C(O)(CH2)qOC(O)-C1-12-alkyl, -C(O)(CH2)qNRiRii, -C(O)O-C1-12-alkyl, where the alkyl is unsubstituted or substituted by one or more OH, halo, cyano or C1-12-alkyl, -S(O)2-C1-12-alkyl, -S(O)2NRiRii, Ri and Rii each independently being H, C1-12-alkyl, or combined with the nitrogen to which they are bound to form 3 to 7 heterocycloalkyl members consisting of one or two heteroatoms chosen from N, O or S, where the heterocycloalkyl is unsubstituted or substituted by one or more independent substituents. Selected by B, ---------------------------------------------------------------------------------------------------- 1. Compounds of general formula I (formula) where R1 is an aryl or heteroaryl, unsubstituted or independently substituted by one or more substituents chosen from A, R2 is H, C1-12-alkyl, unsubstituted or substituted by one or more OH, halo, cyano or C1-12-alkoxy, -(CH2)q-R5, where Ra is a phenyl or heteroaryl with 5 or 6 members, each unsubstituted or independently substituted by one or more substituents chosen from A, -(CH2),NRiRii, -C(O)-C1-12-alkyl, where the C1-12-alkyl is unsubstituted or substituted by one or more substituents. Or more of OH, halo, cyano or C1-12-alkoxy, -S(O)2-C1-12-alkyl, -S(O)2NRiRii, Ri and Rii, each independently of the other, are H, C1-12-alkyl, or combined with the nitrogen to which they are bound, forming 3 to 7 member heterocycloalkyls consisting of one or two heteroaltoms chosen from N, O or S, which are either unsubstituted or independently substituted by one or more substituents. The chosen compound is B, q is 1, 2, 3, or 4, r is 2, 3, or 4, A is halo, cyano, OH, C1-7-alkyl, halo-C1-7-alkyl, C1-7-alxoxy, halo-C1-7-alxoxy, or hydroxy-C1-7-alkyl, B is oxo, halo, OH, C1-7-alkyl, or C1-7-alxoxy, R3 is C1 or F, or its pharmaceutically acceptable salt.