Publication number: 20030162826
Abstract: A pharmaceutical composition comprising a compound of formula (I) wherein X is an electron withdrawing group, Y1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R4, —CO2R4, —CONHR4 or —COR4, and each of R1, R2 and R4, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, or a compound of formula (II) wherein each of Y2 and Y3, which may be the same or different, is hydrogen, alkyl, alkenyl, alkynyl, aryl, heterocyclyl, —SO2R9, —CO2R9, —CONHR9 or —COR9, Z is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, heterocyclyl, —CH═C(NHR10)CH((CH2)mCO2R11)(C═O)CH3 or —CH2(C═O)CH((CH2)mCO2R11)(C═O)CH3, R8 is —(CH2),CO2R12, each of R5 to R7 and R9 to R12, which may be the same or different, is hydrogen, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl or heterocyclyl, and each of m and n, which may be the same or different, is 1 t
Type:
Application
Filed:
March 7, 2003
Publication date:
August 28, 2003
Inventors:
Joseph Floyd Clark, Thomas Andrew Daniel Cadoux-Hudson, Christopher Joseph Schofield
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
Patent number: 6562857
Abstract: This invention provides a progesterone receptor agonist of formula 1 having the structure
wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—;
n=1-5; p=1-4; q=1-4;
R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA;
RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl;
R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl;
R5 is hydrogen, alkyl, or substituted alkyl;
R6 is hydrogen, alkyl, substituted alkyl, or CORB,
RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, amino
Type:
Grant
Filed:
January 9, 2002
Date of Patent:
May 13, 2003
Assignee:
Wyeth
Inventors:
Mark A. Collins, Valerie A. Mackner, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley