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    1,5-Diaryl-pyrrole-3-carboxamide derivatives and their use as cannabinoid receptor modulators
    2.
    发明申请
    1,5-Diaryl-pyrrole-3-carboxamide derivatives and their use as cannabinoid receptor modulators 审中-公开

    公开(公告)号：US20060122230A1

    公开(公告)日：2006-06-08

    申请号：US10540276

    申请日：2003-12-18

    Applicant: Anna Berggren ,  Stig Bosfrom ,  Leifeng Cheng ,  Stig Elebring ,  Peter Greasley ,  Mats Nagard ,  Johan Wilstermann ,  Emma Terricabras

    Inventor： Anna Berggren ,  Stig Bosfrom ,  Leifeng Cheng ,  Stig Elebring ,  Peter Greasley ,  Mats Nagard ,  Johan Wilstermann ,  Emma Terricabras

    IPC: A61K31/454 ,  A61K31/4015 ,  A61K31/401

    CPC classification number: C07D401/04 ,  A61K31/402 ,  A61K31/4025 ,  A61K31/454 ,  C07D207/34 ,  C07D401/06

    Abstract: The present invention relates to a compound of formula (I) in which R1 and R2 independently represent phenyl, thienyl or pyridyl each of which is optionally substituted by one, two or three groups represented by Z; and R3 is H, a C1-3alkyl group, a C1-3alkoxymethyl group, trifluoromethyl, a hydroxyC1-3alkyl group, an aminoC1-3alkyl group, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula —CONHNRaRb wherein Ra and Rb are as defined for R4 and R5 respectively; X is CO or SO2; Y is absent or represents NH optionally substituted by a C1-3alkyl group; R4 and R5 independently represent: a C1-6alkyl group; an (amino)C1-4alkyl-group in which the amino is optionally substituted by one or more C1-3alkyl groups; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s; naphthyl; anthracenyl; a saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen wherein the heterocyclic group is optionally substituted; 1-adamantylmethyl; a group —(CH2)t Het where Het represents an aromatic heterocycle optionally substituted; or R4 represents H and R5 is as defined above; or R4 and R5 together with the nitrogen atom to which they are attached represent a saturated 5 to 8 membered heterocyclic group; R6 is H, a C1-3alkyl group, a C1-3alkoxymethyl group, trifluoromethyl, a hydroxyC1-3alkyl group, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula —CONHNRaRb; with provisos; to processes for preparing such compounds, to their use in the treatment of obesity, psychiatric and neurological disorders particularly obesity, to methods for their therapeutic use and to pharmaceutical compositions containing them.

    5 6-diaryl-pyrazine-2-amide derivatives as cb1 antagonists
    3.
    发明申请
    5 6-diaryl-pyrazine-2-amide derivatives as cb1 antagonists 失效

    公开(公告)号：US20050032808A1

    公开(公告)日：2005-02-10

    申请号：US10499054

    申请日：2002-12-18

    Applicant: Anna Berggren ,  Stig Jonas Bostrom ,  Stig Elebring ,  Peter Greasley ,  Emma Terricabras ,  Johan Wilstermann

    Inventor： Anna Berggren ,  Stig Jonas Bostrom ,  Stig Elebring ,  Peter Greasley ,  Emma Terricabras ,  Johan Wilstermann

    IPC: C07D241/24 ,  A61K20060101 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/497 ,  A61P20060101 ,  A61P3/04 ,  A61P7/00 ,  A61P9/10 ,  A61P15/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/00 ,  A61P43/00 ,  C07D20060101

    CPC classification number: C07D241/24

    Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, prodrugs, solvates and crystalline forms thereof, in which R1 and R2 independently represent: a C1-6alkyl group; an optionally substituted (amino)C1-4alkyl-group; an optionally substituted non-aromatic C3-15carbocyclic group; a (C3-12cycloalkyl)C1-3alkyl-group; a group —(CH2)r(phenyl)s in which r is 0, 1, 2, 3 or 4, s is 1 when r is 0 otherwise s is 1 or 2 and the phenyl groups are optionally independently substituted by Z; naphthyl; anthracenyl; an optionally substituted saturated 5 to 8 membered heterocyclic group containing one nitrogen and optionally one of the following: oxygen, sulphur or an additional nitrogen; 1-adamantylmethyl; a group —(CH2)t Het in which t is 0, 1, 2, 3 or 4, and the alkylene chain is optionally substituted and Het represents an optionally substituted aromatic heterocycle; or R1 represents H and R2 is as defined above; or R1 and R2 together with the nitrogen atom to which they are attached represent a saturated optionally substituted 5 to 8 membered heterocyclic group as defined above; X is CO or SO2; Y is absent or represents NH optionally substitututed by a C1-3alkyl group; R3 and R4 independently represent phenyl, thienyl or pyridyl substituted by Z; Z represents a C1-3alkyl group, a C1-3alkoxy group, hydroxy, halo, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, trifluoromethylsulphonyl, nitro, amino, mono or di C1-3alkylamino, mono or di C1-3alkylamido, C1-3alkylsulphonyl, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkyl carbamoyl, sulphamoyl and acetyl; and R5 is H, a C1-3alkyl group, a C1-3alkoxymethyl group, trifluoromethyl, a hydroxyC1-3alkyl group, C1-3alkoxycarbonyl, carboxy, cyano, carbamoyl, mono or di C1-3alkylcarbamoyl, acetyl, or hydrazinocarbonyl of formula —CONHNRaRb; with the provisos; and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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