| US 7,524,853 B2 | ||
| Compounds and their use in therapy | ||
| Leena Hirvelae, Oulu (Finland); Nina Johansson, Turku (Finland); Pasi Koskimies, Turku (Finland); Olli Taneli Pentikaeinen, Lieto (Finland); Tommi Nyroenen, Helsinki (Finland); Tiina Annamaria Salminen, Koski (Finland); Mark Stuart Johnson, Turku (Finland); Pekka Lehtovuori, Espoo (Finland); Pauli Saarenketo, Piikkioe (Finland); Bartholomeus Johannes Van Steen, Utrecht (Netherlands); Heinrich-Hubert Thole, Hannover (Germany); Mikko Unkila, Kaarina (Finland); Josef Messinger, Sehnde (Germany); Johanna Kiviniemi, Turku (Finland); Lila Pirkkala, Turku (Finland); and Bettina Husen, Hannover (Germany) | ||
| Assigned to Solvay Pharmaceuticals B.V., Weesp (Netherlands); and Solvay Pharmaceuticals GmbH, Hannover (Germany) | ||
| Filed on Dec. 15, 2004, as Appl. No. 11/11,744. | ||
| Application 11/011744 is a continuation in part of application No. 10/861907, filed on Jun. 07, 2004. | ||
| Claims priority of provisional application 60/477047, filed on Jun. 10, 2003. | ||
| Claims priority of application No. PCT/EP2004/053424 (WO), filed on Dec. 13, 2004. | ||
| Prior Publication US 2005/0176742 A1, Aug. 11, 2005 | ||
| This patent is subject to a terminal disclaimer. | ||
| Int. Cl. A01N 43/54 (2006.01); A61K 31/505 (2006.01); C07D 239/00 (2006.01); C07D 471/00 (2006.01); C07D 487/00 (2006.01); C07D 491/00 (2006.01) | ||
| U.S. Cl. 514—267 [544/250] | 40 Claims |
1. A method of treating or inhibiting a steroid hormone dependent disease or disorder selected from the group consisting of
breast cancer, prostate carcinoma, ovarian cancer, uterine cancer, endometrial cancer, endometrial hyperplasia, endometriosis,
uterine fibroids, uterine leiomyoma, adenomyosis, dysmenorrhea, menorrhagia, metrorrhagia, prostadyna, benign prostatic hyperplasia,
prostatitis, acne, seborrhoea, hirsutism, androgenic alopecia, precocious puberty, adrenal hyperplasia, polycystic ovarian
syndrome and osteoporosis, said method comprising administering to a patient in need thereof an effective amount of a compound
corresponding to formula (I)
 wherein
X is S, SO or SO2
R1 and R2 are individually selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, heteroaryl,
substituted heteroaryl, cycloheteroalkyl, substituted cycloheteroalkyl, arylalkyl, substituted arylalkyl, heteroarylalkyl,
substituted heteroarylalkyl, cycloheteroalkyl-alkyl, substituted cycloheteroalkyl-alkyl,
whereby the cycloheteroalkyl moiety of cycloheteroalkyl-alkyl and substituted cycloheteroalkyl-alkyl is a four- to eight-membered
heterocyclic ring containing at least one heteroatom selected from N, O and S, the number of N atoms being 0-3 and the number
of O and S atoms each being 0-1, which ring may be saturated, partly unsaturated or hydroaromatic;
whereby the cycloheteroalkyl moiety is optionally substituted by up to three substituents independently selected from the
group consisting of oxo, alkyl, aryl or aryl-(C1-C4)-alkyl both optionally substituted in the aryl moiety, hydroxyl, (C1-C6)alkoxy, halogenated (C1-C6)alkyl, halogenated (C1-C6)alkoxy, carboxyl-(C1-C6)alkyl, thiol, nitrile, sulfamoyl, sulphonamide, carboxyl, aryloxy or arylalkyloxy both optionally substituted in the aryl
moiety, (C1-C6)alkylthio, arylthio or arylalkyloxy both optionally substituted in the aryl moiety, (C1-C6)alkylthio, arylthio or arylalkylthio both optionally substituted in the aryl moiety, amino, amido, acyl, and acylamino;
or R2 itself may be independently selected from acyl, carboxyl, or amido,
wherein R1 and R2 cannot be simultaneously unsubstituted alkyl,
the hydrocarbon chain —C(R3)-C(R4)-C(R5)-C(R6)- of the six-membered ring is saturated or contains one or two double bonds
between the carbon atoms;
R3 and R4 are individually selected from the group consisting of hydrogen, oxo, halogen or dihalogen, acyl, alkyl, substituted
alkyl, hydroxyl, carboxyl, amido, amino, nitrile, thio, alkoxy, acyloxy, aryloxy, alkylthio and arylthio;
R5 and R6 are individually selected from the group consisting of hydrogen, halogen, alkyl, substituted alkyl, arylalkyl, substituted
arylalkyl, hydroxyl, alkoxy, aryloxy, acyl or carboxyl,
or a pharmaceutically acceptable salt thereof.
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