Azabicyclo (3.1.0) hexane derivatives useful as modulators...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C548S262200

Reexamination Certificate

active

07875643

ABSTRACT:
The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof:whereinG is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl;p is an integer ranging from 0 to 5;R1is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5;each R2is independently hydrogen or C1-4alkyl;n is 2, 3, 4 or 5;R3is C1-4alkyl;R4is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5;R5is selected from a group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl;and when R1corresponds to R5, p is 1;processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.

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Epstein J W et al: “1-Aryl-3-Azabicyclo[3.1. Oihexanes, A New Series of Nonnarcotic Analgesic Agents” Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 24, No. 5, 1981, pp. 481-490, XP002381888, ISSN: 0022-2623.

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