US 7,388,006 B2 · Non-steroidal progesting

Abstract

The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.

Claims26

Dependent claims

A compound (I) which is:

(+)-5-{2-hydroxy-3-[1-(2-fluoro-5-trifluoromethylphenyl)-cyclopropyl]-2-trifluoromethyl-propionylamino}-phthalide,
(+)-6-{2-hydroxy-3-[1-(2-fluoro-3-trifluoromethylphenyl)-cyclopropyl]-2-trifluoromethyl-propionylamino}-4-methyl-2,3-benzoxazin-1-one,
(+)-5-{2-hydroxy-3-[1-(2-fluoro-3-trifluoromethylphenyl)-cyclopropyl]-2-trifluoromethyl-propionylamino}-phthalide, or
(+)-6-{2-hydroxy-3-[1-(2-fluoro-5-trifluoromethylphenyl)-cyclopropyl]-2-trifluoromethyl-propionylamino}-4-methyl-2,3-benzoxazin-1-one.

1 more element

Dependencies are inferred from the claim text.

Facts

Application

10/384,775Filed 11 Mar 2003 · us provisional application

Priority

EP 0200553011 Mar 2002

Published

US 2003/0232824 A118 Dec 2003

Granted

17 Jun 2008

Term ends

Not estimatedThe source records don’t support an estimate.

Classification13 codes

C07D 307/88
Benzo [c] furans; Hydrogenated benzo [c] furans: with one oxygen atom directly attached in position 1 or 3
A61K 31/365
Having oxygen as the only ring hetero atom, e.g. fungichromin: lactones
A61K 31/535
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having six-membered rings with at least one nitrogen and one oxygen as the…
A61K 31/565
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids: not substituted in position 17 beta by a…

Non-steroidal progesting

Life of this patent

Non-steroidal progesting

Life of this patent

Abstract

Claims26