Di-or triaza-spiro [4,5] decane derivatives
AssigneeHoffman-La Roche Inc.
InventorsGeo Adam, Andrea Cesura, François Jenck, Sabine Kolczewski, Stephan Röver, Jürgen Wichmann
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AssigneeHoffman-La Roche Inc.
InventorsGeo Adam, Andrea Cesura, François Jenck, Sabine Kolczewski, Stephan Röver, Jürgen Wichmann
Estimating the term…
The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R2 is hydrogen; lower alkyl; ═O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is —CH(OH)—; —C(O)—; —CHR3—; —CR3═; —O—; —S—; —CH(COOR4)— or C(COOR4)═; Y is —CH2—; —CH═; —CH(COOR4)—, —C(COOR4)═; or —C(CN)—; R3 is hydrogen or lower alkoxy; R4 is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.
Compounds of the general formula I
A compound according to claim 2, 8-(cis-4-isopropyl-cyclohexyl)-1-phenyl-1,8-diaza-spiro[4.5]decan-4-one.
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula I
A method of treating disorders in mammals related to the orphanin FQ receptor selected from the group consisting of anxiety, stress, depression, trauma, Alzheimer's mediated memory loss, epilepsy, arterial blood pressure disorders, obesity, acute pain, chronic pain, Na+ excretion, control of water balance, and symptoms associated with drug withdrawal comprising administering to said mammal a therapeutically effective amount for treating said disorder of a compound of formula I
Dependencies are inferred from the claim text.