摘要:
The present invention relates to a low-dosed oral dosage form for treatment and/or prophylaxis of diseases, especially of endometriosis, polycystic ovary syndrome and/or atopic dermatitis. More particularly, the present invention concerns oral dosage forms comprising up to 120 mg N- {[17-(5- Fluoropyridin-3-yl)estra-l,3,5(10),16-tetraen-3-yl]carbonyl} -N-methyl-P-alanine per day.
摘要:
Provided are compounds of general formula A and A', wherein X1 and X2 are each C, CH or N; R3 and R4 are each H, optionally substituted C1-C30 saturated or unsaturated chemical group, or together form an optionally substituted C5-C8 cycle; Z1; Z2 and Z3 are each N or CH; V is C=0, C=S or CH2; n is from 1 to 12; W1 and W2 are each H, CH2, O or S; and R1 and R2 are each H, Cr1C6 alkyl, C1C6 aryl, C1C12 alkylaryl, optionally substituted phenyl, C1C6 alkoxy, C1C6 thioalkoxy, F, CI, Br or I. These compounds inhibit steroid sulfatase (STS), act as selective estrogen receptor modulators (SERMs), increase alkaline phosphatase (ALP) activity, and are useful in the treatment of medical conditions involving hormones such as breast cancer, prostate cancer, endometriosis, osteoporosis, benign prostatic hyperplasia and endometrial cancer.
摘要:
The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R2to R7are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD and in treatment or prevention of steroid hormone de- pendent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the afore- mentioned compounds or pharmaceutically acceptable salts thereof.
摘要:
Die Erfindung betrifft AKR1C3 Inhibitoren und Verfahren zu ihrer Herstellung, ihre Verwendung zur Behandlung und/oder Prophylaxe von Krankheiten sowie ihre Verwendung zur Herstellung von Arzneimitteln zur Behandlung und/oder Prophylaxe von Krankheiten, insbesondere von Blutungsbeschwerden und Endometriose.
摘要:
The present invention relates to substituted steroid compounds having the formula (I) Wherein R 1 is H or halogen; R 2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R 3 is H or halogen; R 4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R 5 is methyl or ethyl; R 6 is H or methyl; R 7 is H or methyl; R 8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.
摘要:
Molecular signature for antipsychotics and SERMs has been identified, namely their upregulation of genes that alter lipid homeostasis, preferably of one or more of the following genes: TNSIGl, SCD, FADS2, LDLR, FDPS, ACAT2, FDFTl, CYP51A1, FASN, DHCR7, RAB26, TM7SF2, SATBl, FAM117, GPNMB, NUPRl, VAC14, and LSS.
摘要:
This invention relates to β-hydroxyketones and β-alkoxyketones of formula (I), to their use as estrogen receptor modulators, and to methods for their preparation.
摘要:
The present invention provides a polypeptide comprising an estrogen or androgen binding region, the binding region capable of binding to an estrogen or androgen at a sufficient affinity or avidity such that upon administration of the polypeptide to a mammalian subject the level of biologically available estrogen or androgen is decreased. The invention also provides for the treatment or prevention of cancers such as ovarian cancer, breast cancer and endometrial cancer using the polypeptides.
摘要:
A process is described for the industrial scale preparation of 7α-[9-(4,4,5,5,5- 5 pentafluorothiopentyI)nonyl]estra-1,3,5(10)-triene-3,17β-diol, a precursor of steroids with hormonal activity which include Fulvestrant.
摘要:
The present invention relates to the single use of the progesterone-receptor antagonist 11ß-(-4-acetylpheny)-17 ß-hydroxy-17a-(1,1,2,2,2-pentafluoroethyl)- estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, as well as to a combination comprising the progesterone- receptor antagonist 11 ß-(4-acetylphenyl)-17ß-hydroxy-17a-(1,1,2,2,2- pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one pure antiestrogen, for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, ovarian cancer endometrial cancer, gastric cancer, colorectal cancer.endometriosis, myeloma, myoma and meningioma. The present invention also relates to a combination of the progesterone-receptor antagonist 11 ß-(4-acetylphenyl)-17ß-hydroxy-17a-(1,1,2,2,2-pentafluoroethyl)-estra-4,9- dien-3-one or a pharmaceutically acceptable derivative or analogue thereof, together with at least one EGF or EGFR targeting drug, for the prophylaxis and treatment of BRCA1- or BRCA2-mediated breast cancer, ovarian cancer endometrial cancer, gastric cancer, colorectal cancer, endometriosis, myeloma, myoma and meningioma.