http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-051457-A1

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filingDate 2005-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6df9ee1ea4de6a18e00bfe7980032f8c
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publicationDate 2007-01-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-051457-A1
titleOfInvention INDAZOLES, BENZISOXAZOLES AND BENZISOTIAZOLES, PROCEDURE TO PREPARE THEM, PHARMACEUTICAL COMPOSITIONS AND ITS USE AS A STROGEN AGENT
abstract The compounds are modulators of estrogen receptors. Claim 1: A compound of formula (1), or an acid addition salt or a stereoisomeric form thereof; characterized in that: R1 is hydrogen or a C1-6 alkyl, C3-6 cycloalkyl, trifluoromethyl, -N = NCR5R6, -SO2NR7R8, phenyl, phenylC1-3alkyl or C1-3 alkyl substituted by a saturated heterocyclic radical, where the phenyl is unsubstituted or substituted by at least one substituent selected from the group consisting of a hydroxyl, a halogen, nitro, a cyano, a C1-3 alkyl, a C1-3 alkoxy and a trifluoromethyl; R1 may also be a salt; each of R2 and R3 is independently a hydrogen group or a hydroxyl, halogen, nitro, cyano, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, trifluoromethyl, -NR7R8, -CONR7R8, -COR9 or -CO2R9; R2 may also be a phenyl or a saturated or unsaturated heterocycle, where the phenyl is unsubstituted or substituted by at least one substituent selected from the group consisting of hydroxyl, halogen, nitro, cyano, C1-3 alkyl, C1-3 alkoxy, trifluoromethyl a saturated heterocyclic radical; X is O, S, SO, SO or NR4; R4 is hydrogen or a C1-6 alkyl, C3-6 cycloalkyl, phenyl, phenylC1-3alkyl, C1-3 alkyl group substituted by a saturated heterocyclic radical, a group -COR7, -CO2R7 or -SO2NR7R8, where the phenyl is unsubstituted or substituted by at least one substituent selected from the group consisting of a hydroxyl, a halogen, a nitro, a cyano, a C1-3 alkyl, a C1-3 alkoxy, a trifluoromethyl, a phenylC1-3alkyl and a phenylC1-3alkoxy; Y is a direct link, O, S, SO, SO2, NR4, CO, - (CR10R11) n- or -R10C = CR11-; each of R5, R6, R7 and R8 is independently hydrogen or a C1-6 alkyl or C3-6 cycloalkyl group; R9 is hydrogen, C1-6 alkyl, phenyl or a saturated or unsaturated heterocyclic radical, where the phenyl is unsubstituted or substituted by at least one substituent selected from the group consisting of hydroxyl, halogen, nitro, cyano, C1-3 alkyl, C1 -3 alkoxy, trifluoromethyl and a saturated heterocyclic radical; each of R10 and R11 is independently hydrogen or a cyano group, C1-6 alkyl, -CO-phenyl, -CO (unsaturated heterocyclic radical) or -CONR7R8, where the phenyl is unsubstituted or is substituted by at least one substituent selected within from the group consisting of hydroxyl, halogen, nitro, cyano, C1-3 alkyl, C1-3 alkoxy and trifluoromethyl; n is 1 or 2; A is C3-15 cycloalkyl, C3-15 cycloalkene, phenyl or naphthyl, where the cycloalkyl or cycloalkene is unsubstituted or substituted by at least one C1-6 alkyl, and where the phenyl or naphthyl is unsubstituted or substituted by at least one substituent selected from the group consisting of hydroxyl, halogen, nitro, cyano, C1-3 alkyl, C1-3 alkoxy and trifluoromethyl; when X is NR4, Y and R2 together with the indazolo ring that carries them can also form a 1H-pyran [4,3,2-cd] indazole; provided that: when X is O, S or NR4, R1 is hydrogen or C1-6 alkyl, C3-6 cycloalkyl or trifluoromethyl, and Y is a direct bond, A is not optionally substituted phenyl or optionally substituted naphthyl; when X is NR4 where R4 is H or C1-6 alkyl and R1O is 6-OCH3, Y is not CO; when X is O, R1O is 6-OH or 6-OCH3, Y is a direct bond and A is cyclopentyl, (R2, R3) or (R3, R2) is different from (H, Cl) at position 4.5 ; when X is O, R1O is 6-OH, R2 and R3 are H and Y is CH = CH, A is not phenyl or 4-methoxyphenyl; when X is SO2, A is phenyl and R1O is 5- or 6-OCH3, (R2, R3) or (R3, R2) is different from (H, OCH3) in position 6- or 5-.
priorityDate 2004-10-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 53.