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    1,3,8-TRIAZA-SPIRO[4,5]DECAN-4-ON DERIVATIVES
    5.
    发明专利
    1,3,8-TRIAZA-SPIRO[4,5]DECAN-4-ON DERIVATIVES 未知

    公开(公告)号：CA2255171C

    公开(公告)日：2009-09-29

    申请号：CA2255171

    申请日：1998-12-03

    Applicant: HOFFMANN LA ROCHE

    Inventor： WICHMANN JURGEN ,  ADAM GEO ,  ROVER STEPHAN ,  JENCK FRANCOIS ,  CESURA ANDREA ,  GALLEY GUIDO

    IPC: C07D235/02 ,  C07D471/10 ,  A61K31/00 ,  A61K31/41 ,  A61K31/435 ,  A61K31/438 ,  A61K31/53 ,  A61K31/535 ,  A61P3/00 ,  A61P3/04 ,  A61P9/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D207/04 ,  C07D233/30

    Abstract: The present invention relates to compounds of the general formula (see formula I) wherein R1 is hydrogen, lower alkyl, halogen, lower alkoxy, trifluoromethyl, lower alkyl-phenyl or (C5-7)-cycloalkyl; R2 is hydrogen, lower alkyl, phenyl or lower alkyl-phenyl; R3 is hydrogen, lower alkyl, benzyl, lower alkyl-phenyl, lower alkyl- diphenyl, triazinyl, cyanomethyl, lower alkyl-piperidinyl, lower alkyl-naphthyl, (C5-7)-cycloalkyl, lower alkyl-(C5-7)-cycloalkyl, lower alkyl-pyridinyl, lower alkyl-morpholinyl, lower alkyl- dioxolanyl, lower alkyl-oxazolyl or lower alkyl-2-oxo-oxazolidinyl and wherein the ring systems may be substituted by additional lower alkyl, lower alkoxy, trifluoromethyl or phenyl, or -(CH2)n C(O)O-lower alkyl, -(CH2)n C(O)NH2, -(CH2)n C(O)N(lower alkyl)2, -(CH2)n OH or -(CH2)n C(O)NHCH2C6H5; R4 is hydrogen, lower alkyl or nitrilo; A is a ring system, consisting of (a) (C5-15)-cycloalkyl, which may be in addition to R4 optionally substitute d by lower alkyl, trifluoromethyl, phenyl, (C5-7)-cycloalkyl, spiro-undecan- alkyl or by 2-norbornyl, or is one of the following groups (see formula b) (see formula c) (see formula d) dodecahydro-acenaphthylen-1yl (e), bicyclo[6.2.0]dec-9-yl (f) and bicyclononan-9-yl (g); and wherein R5 and R6 are hydrogen, lower alkyl or taken together and with the carbon atoms to which they are attached form a phenyl ring; R7 is hydrogen or lower alkyl; the dotted line represents an optional bond and n is 1 to 4; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are agonists and/or antagonists of the Orphanin FQ (OFQ) receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acu te and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na+ excretion, arterial blood pressure disorders a nd metabolic disorders such as obesity.

    10.
    发明专利
    未知

    公开(公告)号：DE69826891D1

    公开(公告)日：2004-11-11

    申请号：DE69826891

    申请日：1998-12-03

    Applicant: HOFFMANN LA ROCHE

    Inventor： ADAM GEO ,  CESURA ANDREA ,  GALLEY GUIDO ,  JENCK FRANCOIS ,  ROEVER STEPHAN ,  WICHMANN JUERGEN

    IPC: A61K31/435 ,  A61K31/438 ,  A61K31/439 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D221/20 ,  C07D451/04 ,  C07D471/10 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D498/10 ,  C07D498/20

    Abstract: The present invention relates to compounds of the formula wherein X is -O- or -CH2-; Y is -C(O)-, -(CH2)n- or -N(CH3)-; n is 1 or 2 or X and Y taken together are -CH=CH-Z is -NH-, -CH2-, -O- or =CH-; A1 is a group B is -(CH2)m-; m is 0, 1 or 2; R1 and R2 are each independently hydrogen or lower alkyl; R3 is hydrogen or halogen; R4 is hydrogen or hydroxy and the dotted line is (-CH2-CH2-)n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are antagonists of the OFQ receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acute and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na+ excretion and arterial blood pressure disorders and metabolic disorders such as obesity.

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