Akzo Nobel N.v.

N.v. Organon

Merck Sharp + Dohme B.v.

Msd Oss B.v.

Fredericus Antonius Dijcks

Dirk Leysen

Hubert Jan Jozef Loozen

Duncan R Rae

Ian Craig Carlyle

Simon N Thorn

Antonius Gerardus Hendrikus Ederveen

Gerrit Herman Veeneman

Simon James Anthony Grove

Arthur A Oubrie

Herman Thijs Stock

Gerardus Stephanus Ruigt

Scott James Lusher

Gerardus Stephanus Franciscus Ruigt

Joannes Theodorus Maria Linders

Joannes Theodorus Linders

Simon James Grove

Samira Addo

Simon Nicholas Thorn

Duncan Robertson Rae

The present invention relates to novel N-substituted azetidine derivatives &#x3c; of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N&#x2014;R5; R1 is H, (C1-8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2-6)alkynyl, (C1-4)alkylcarbonyl, (C1-4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1-3)-alkyl, (C3-6)heterocycloalkyl(C1-3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1-2)alkyl; R5 is H, (C1-3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1-3)-alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, &#x3e; to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular ER-positive breast cancer, more in particular ER-positive, hormone treatment-resistant breast cancer. Said N-substituted azetidine derivatives have estrogen receptor alpha (ERa) antagonistic and&#x2014;in certain embodiments&#x2014;selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells. 

N-substituted azetidine derivatives

The present invention relates to substituted steroid compounds having the formula Wherein Ris H or halogen; Ris H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; Ris H or halogen; Ris H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; Ris methyl or ethyl; Ris H or methyl; Ris H or methyl; Ris 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.

Substituted 16,17-annellated steroid compounds for use in womens healthcare

The invention provides 15&#x3b2;-substituted steroidal compounds having selective estrogen receptor activity according to Formula I: wherein,

15 &#x3b2;-substituted steroids having selective estrogenic activity

The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.

Benzylamine derivatives which are useful in treating psychiatric disorders

Benzylamine derivatives which are useful in treating psychiatric

Growing community of inventors

Oss, Netherlands

Fredericus Antonius Dijcks