http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2311972-T3

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_ae84948901b77f34fd51c41264d8d19c
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filingDate 2005-01-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2009-02-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_298b535e132ee01f8626bb7619c44092
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_edb4694bf845f51757da453f29918ea3
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1d0b5129479075f22bfb5bbdbc797cbd
publicationDate 2009-02-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2311972-T3
titleOfInvention 1,3,5-TRISUBSTITUTED DERIVATIVES OF 4,5-DIHIDRO-1H-PIRAZOL HAVING CB1 ANTAGONIST ACTIVITY.
abstract Compounds of general formula (I) (See formula) where: - R1 and R2 independently represent phenyl, thienyl or pyridyl, groups which may be substituted with 1, 2 or 3 substituents Y, which may be the same or different, of the C1-alkyl group - 3 or branched or linear C1-3 alkoxy, phenyl, hydroxy, chloro, bromine, fluoro, iodine, trifluoromethyl, trifluoromethylthio, trifluoromethoxy, methylsulfonyl, carboxyl, trifluoromethylsulfonyl, cyano, carbamoyl, sulfamoyl and acetyl, or R1 and / or R2 and R1 and / or R2 naphthyl, - X represents one of the subgroups (i) or (ii), (See formula) where - R3 represents a hydrogen atom or a branched or linear C1-3 alkyl group, - R4 represents a branched C1-8 alkyl group or linear or C 3-8 cycloalkyl-C 1-2 alkyl, branched or linear C 1-8 alkoxy, C 3-8 cycloalkyl, C 5-10 cycloalkyl, C 6-10 tricycloalkyl, groups that may contain one or more heteroatoms of the group (O , N, S) and which may be substituted with a hydro group xi, 1-3 methyl groups, an ethyl group or 1-3 fluorine atoms, or R4 represents a group, phenoxy, benzyl, phenethyl or phenylpropyl, optionally substituted on its phenyl ring with 1-3 Y substituents, where Y has the meaning mentioned above, or R4 represents a pyridyl or thienyl group, or R4 represents a NR5R6 group where R5 and R6 - together with the nitrogen atom to which they are attached - form a saturated, unsaturated, heterocyclic, monocyclic or bicyclic group having 4 to 10 ring atoms, heterocyclic group containing one or two heteroatoms of the group (O, N, S) such a heterocyclic group may be substituted with a branched or linear C1-3 alkyl group, phenyl, hydroxy or trifluoromethyl or a fluorine atom , or R3 and R4 - together with the nitrogen atom to which they are attached - form a heterocyclic, monocyclic or bicyclic, saturated or unsaturated group having 4 to 10 ring atoms, heterocyclic group containing one or two heteroatoms of the group (O, N, S) such a heterocyclic group may be substituted with a branched or linear C1-3 alkyl group, phenyl, amino, hydroxy or trifluoromethyl or a fluorine atom, - R7 represents a benzyl, phenyl, thienyl group or pyridyl, groups which may be substituted in their aromatic ring with 1, 2, 3 or 4 substituents Y, where Y has the meaning indicated above, which may be the same or different, or R7 represents branched or linear C1-8 alkyl, alkenyl C3-8, C3-10 cycloalkyl, C5-10 cycloalkyl, C6-10 tricycloalkyl or C5-8 cycloalkenyl or R7 represents naphthyl or R7 represents an amino group or R7 represents a C1-8 dialkylamino group, a C1-8 monoalkylamino group or a heterocyclic, monocyclic or bicyclic, saturated or unsaturated group having 4 to 10 ring atoms, heterocyclic group containing one or two nitrogen atoms and such heterocyclic group may contain a heteroatom of the group (O, S) and such group or heterocyclic may be substituted with a branched or linear C1-3 alkyl group, phenyl, hydroxy or trifluoromethyl or a fluorine atom, - R8 represents a hydrogen atom or a branched or linear C1-3 alkyl group, R9 represents an atom of hydrogen or a branched or linear C1-8 alkyl group, C3-8 cycloalkyl or C2-10 heteroalkyl groups which may be substituted with a keto group, trifluoromethyl group or a fluorine atom, or R9 represents an amino, hydroxy, phenoxy group or benzyloxy or R9 represents a branched or linear C1-8 alkoxy group, which may be substituted with a hydroxy group, a trifluoromethyl group or a fluorine atom, or R9 represents a phenyl, benzyl, pyridyl, thienyl, pyridylmethyl or phenethyl group wherein the aromatic rings may be substituted with 1, 2 or 3 of the substituents Y, where Y has the meaning indicated above, or R9 represents a group NR10R11 with the proviso that R8 represents an atom of hi driogen or a methyl group and where R10 and R11 are the same or different and represent C1-4 alkyl or C2-4 trifluoroalkyl or R10 and R11 - together with the nitrogen atom to which they are attached - form a saturated or unsaturated heterocyclic moiety that it has 4 to 8 ring atoms, heterocyclic moiety containing one or two atoms of the group (O, N, S) such saturated or unsaturated heterocyclic moiety can be substituted with a C1-2 or R8 and R9 alkyl group - together with the atom of nitrogen to which they are attached - they form a heterocyclic, monocyclic or bicyclic, saturated or unsaturated moiety having 4 to 10 ring atoms, heterocyclic moiety containing one or two atoms of the group (O, N, S) or a keto group or a group -SO2-, a moiety that may be substituted with a C1-2 alkyl group, hydroxy, phenyl, methylamino, dimethylamino, acetidinyl, pyrrolidinyl, piperidinyl or hexahydro-1H-azepinyl, and all stereoisomers, as well as salts and prophane Drugs, which are derivatives of the compounds of formula (I) in which a group that is readily removed after administration is present, selected from the group consisting of an amidine, enamine, a Mannich base, a hydroxyl-methylene derivative , a derivative of O- (acyloxymethylene carbamate), carbamate or enaminone.
priorityDate 2004-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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