Publication number: 20040029917
Abstract: Compounds of formula (I) or a derivative thereof, wherein; R is C1-6allkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6allkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6akoxyC1-6alkyl, aminoC1-6allkyl, (C1-6allkyl)aminoC1-6alkyl, di(C1-6allkyl)aminoC1-6alkyl; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 is hydrogen or C1-6alkyl; R4 and R5 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6akylamino, di(C1-4alkyl)amino, hydroxyC1-6alkyl, C1-6akoxyC1-6alkyl, aminoC1-6allkyl, (C1-4alkyl)aminoC1-6alkyl, di(C1-4alkyl)aminoC1-4alkyl, aryl, and COX wherein X may be hydroxy, C1-6alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6allkyl)amino; with the proviso that, when R3 is hydrogen, then R R4 and R5 are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more ti
Type:
Application
Filed:
July 30, 2003
Publication date:
February 12, 2004
Inventors:
Daniela Barlocco, Giorgio Cignarella, Giuseppe Giardina, Mario Grugni, Silvano Ronzoni
Publication number: 20030195191
Abstract: Compounds of formula (I): wherein R1 is bicyclyl or heterobicyclyl, R2 and R3 are each independently hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocyclyl, (C1-6)alkylthio, (C2-6)alkenylthio, (C2-6)alkynylthio, aryloxy, arylthio, heterocyclyloxy, heterocyclythio, (C1-6)alkoxy, (C1-6)alkenyloxy, aryl(C1-6)alkoxy, aryl(C1-6)alkylthio, amino, mono- or di-(C1-6)alkylamino, acylamino, sulfonylamino, cycloalkyl, cycloalkenyl, carboxylic acid (C1-6) ester, hydroxy, halogen, carboxamide: CONR8R9 where R8 and R9 are independently selected from the group consisting of hydrogen, alkyl, aryl, arylalkyl and heterocyclyl and includes R8 and R9 as part of a heterocyclyl group, or R2 and R3 together form a cyclic alkyl or alkenyl; R4 and R5 are each independently aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino; R6 and R7 are each hydrogen or together form a fused aryl ring; and m and n are each independently from 0 to 2; with the proviso that when n=1 neither R4 nor R
Type:
Application
Filed:
May 12, 2003
Publication date:
October 16, 2003
Inventors:
Gordon Burton, Barry Sidney Orlek
Patent number: 6610678
Abstract: This invention concerns compounds of formula
including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R1 is C1-6alkyl, NR6R7, OR6 or SR7; R2 is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R3 is Ar1 or Het1; R4 and R5 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R6 is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R7 is hydrogen, C1-8alkyl, mono- or di(C3-6cyclo-alkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R6 is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar2CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R6 and R7 taken together with the nitrogen atom to which they are attached ma
Type:
Grant
Filed:
October 8, 2002
Date of Patent:
August 26, 2003
Inventors:
Charles Huang, Keith M. Wilcoxen, Chen Chen, Mustapha Haddach, James R. McCarthy
Publication number: 20030109700
Abstract: 1 Compounds of formula (1) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re, are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmac
Type:
Application
Filed:
July 11, 2002
Publication date:
June 12, 2003
Inventor:
Gary Michael Ksander