Non-steroidal, tetracylic compounds for estrogen-related treatments
AssigneeAkzo Nobel N.V.
InventorsGerrit Herman Veeneman, Eduard Willem De Zwart, Hubert Jan Jozef Loozen, Jordi Mestres
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AssigneeAkzo Nobel N.V.
InventorsGerrit Herman Veeneman, Eduard Willem De Zwart, Hubert Jan Jozef Loozen, Jordi Mestres
Estimating the term…
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 H1 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. These compounds are useful for estrogen-receptor related treatments in view of a desirable profile of activity for estrogen α and estrogen β receptors.
A method of inducing an estrogenic or anti-estrogenic effect in a subject in need thereof, comprising:
A compound having formula II:
A compound having Formula V:
A compound having Formula VT:
Dependencies are inferred from the claim text.