51 results about "Azetidine derivative" patented technology

The present invention relates to novel N-substituted azetidine derivatives < of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N—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, > 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—in certain embodiments—selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells.

The invention provides a synthetic method of a 3-fluoro-azetidine derivative. The synthetic method takes a compound I as the raw material, the compound I is reacted with trimethylsilyl cyanide to obtain a compound II, and a compound VI is obtained through esterification, N-protection and fluoronation or through hydrolysis, fluoro, esterification and N-protection. The synthetic method is mild in reaction condition and easy to operate, the yield of a reaction of each step is high, and the total recovery can reach 85 percent.

Azetidine derivatives of which the following is exemplaryand their use in the treatment of obesity, diabetes or dyslipidemia.

The present invention relates to a solid form of a compound of Formula (I), a method for preparing the solid form, a pharmaceutical composition comprising the solid form, and use of the solid form in the treatment of Janus kinase (JAK) related diseases comprising, for example, inflammatory diseases, autoimmune diseases, and cancers.