Patent number: 6756375
Abstract: The invention provides for a non-steroidal compound having the formula
wherein Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2— or —CH2CH2—; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, —CF3, —OCF3, (1C-8C)Alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)a
Type:
Grant
Filed:
July 24, 2003
Date of Patent:
June 29, 2004
Assignee:
Akzo Nobel N.V.
Inventors:
Gerrit Herman Veeneman, Hubert JanJozef Loozen, Jordi Mestres, Eduard Willem De Zwart
Publication number: 20030144313
Abstract: The invention provides non-steroidal estrogenic compounds with estrogenic and anti-estrogenic compounds effects for treatment of estrogen-deficiency related disorders, which compounds are having formula (I) wherein, one of Ra or Rb is 'Re; Re and 'Re are OH, optionally independently etherified or esterified; X is N or —C(R1)—, wherein R1 is H, halogen, CN, optionally substituted aryl, (1C-4C)alkyl, (2C-4C)alkenyl, (2C-4C)alkynyl or (3C-6C)cycloalkyl, which alkyl, alkenyl, alkynyl and cycloalkyl groups can optionally be substituted with one or more halogens; Y is N or —C(R2)—, with the proviso that X and Y are not both N, wherein R2 has the same meaning as defined for R1; Z is C(R3,'R3)— or —C(R4,'R4)—C(R5,'R5)—, wherein R3, 'R3, R4, 'R4, R5, and 'R5, independently arc H, (1C-4C)alkyl, (2C-4C)alkenyl or (3C-6C) cycloalkyl, which alkyl, alkenyl and cycloalkyl groups can optionally be substituted with one or more halogens.
Type:
Application
Filed:
December 2, 2002
Publication date:
July 31, 2003
Inventors:
Gerrit Herman Veeneman, Eduard Willem De Zwart, Hubert Jan Jozef Loozen, Jordi Mestres