US2015335651A1PendingUtilityA1

DISUBSTITUTED OCTAHYDROPYRROLO[3,4-c]PYRROLES AS OREXIN RECEPTOR MODULATORS

Assignee: JANSSEN PHARMACEUTICA NVPriority: Oct 23, 2009Filed: Jun 9, 2015Published: Nov 26, 2015
Est. expiryOct 23, 2029(~3.2 yrs left)· nominal 20-yr term from priority
A61P 3/10A61P 9/06A61P 3/06A61P 9/04A61P 9/00A61P 5/50A61P 43/00A61P 9/12A61P 25/18A61P 25/00A61P 25/04A61P 25/14A61P 25/28A61P 3/00A61P 25/24A61P 3/04A61P 25/22A61P 25/16A61P 25/20A61P 1/04A61P 1/16A61P 11/00A61P 15/00A61P 19/02A61P 1/00A61P 1/12A61K 31/4192A61K 31/498A61K 31/4439C07D 487/04A61K 31/5377A61K 31/4709A61K 31/428A61K 31/506A61K 31/53A61K 31/407
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Claims

Abstract

Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.

Claims

exact text as granted — not AI-modified
1 . A compound selected from
 [5-(4,6-Dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone;   and pharmaceutically acceptable salts thereof.   
     
     
         2 .- 34 . (canceled) 
     
     
         35 . The compound of  claim 1 , selected from:
 [5-(4,6-Dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone; and   [5-(4,6-Dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone•HCl.   
     
     
         36 . A compound which is [5-(4,6-Dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone. 
     
     
         37 . A pharmaceutical composition comprising a compound selected from:
 [5-(4,6-Dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)-methanone, and pharmaceutically acceptable salts thereof;   and a pharmaceutically acceptable excipient.   
     
     
         38 . A pharmaceutical composition comprising the compound of  claim 36  and a pharmaceutically acceptable excipient. 
     
     
         39 . A method of treating a subject suffering from or diagnosed with a sleep disorder selected from the group consisting of sleep-wake transition disorders, insomnia, restless legs syndrome, jet-lag, disturbed sleep, and sleep disorders secondary to neurological disorders, comprising administering to a subject in need of such treatment an effective amount of a compound selected from [5-(4,6-Dimethyl-pyrimidin-2-yl)-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl]-(2-fluoro-6-[1,2,3]triazol-2-yl-phenyl)methanone, and pharmaceutically acceptable salts thereof. 
     
     
         40 . The method according to  claim 39 , wherein the sleep disorder is selected from insomnia or a sleep disorder secondary to depression. 
     
     
         41 . The method according to  claim 39 , wherein the sleep disorder is insomnia. 
     
     
         42 . A method of treating a subject suffering from or diagnosed with a sleep disorder selected from the group consisting of sleep-wake transition disorders, insomnia, restless legs syndrome, jet-lag, disturbed sleep, and sleep disorders secondary to neurological disorders, comprising administering to a subject in need of such treatment the pharmaceutical composition of  claim 38 . 
     
     
         43 . The method according to  claim 42 , wherein the sleep disorder is selected from insomnia or a sleep disorder secondary to depression. 
     
     
         44 . The method according to  claim 42 , wherein the sleep disorder is insomnia.

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