C07J41/0083

17-HYDROXY-17-PENTAFLUOROETHYL-ESTRA-4,9(10)-DIEN-11-ARYL DERIVATIVES, METHOD OF PRODUCTION THEREOF AND USE THEREOF FOR THE TREATMENT OF DISEASES

The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of Formula I with progesterone antagonizing action and method of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of fibroids of the uterus (myomas, uterine leiomyoma), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause or for fertility control and emergency contraception.

AMORPHOUS ONAPRISTONE COMPOSITIONS AND METHODS OF MAKING THE SAME
20170182065 · 2017-06-29 ·

Amorphous forms of onapristone and methods of making such amorphous forms are provided. Amorphous forms can be characterized by their X-ray powder diffraction patterns and other properties.

Process for the production of 21-methoxy-11-beta-phenyl-19-nor-pregna-4,9-diene-3,20-dione derivatives

The present invention relates to a process for the synthesis of compounds of formula (I), ##STR00001##
wherein the meaning of R is dimethylamino or acetyl group, using the compound of formula (III) or (IV), wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxan-2-yl group, as starting material and methoxymethyl lithium as reagent. ##STR00002##

Industrial process for the synthesis of ulipristal acetate and its 4′-acetyl analogue

The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process. ##STR00001##

Crystalline polymorphic form of ulipristal acetate

A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by dissolving an isopropanol-solvated crystal of ulipristal acetate in a mixed solvent containing ethanol and water, and crystallizing an ulipristal acetate from the solution without addition of a seed crystal to the solution.

Crystalline polymorphic form of ulipristal acetate

A novel crystalline polymorphic form of ulipristal acetate useful as an agent for preventing and/or treating uterine leiomyoma and as a contraceptive, and a process for producing the crystalline polymorphic form are provided. The novel crystalline polymorphic form of ulipristal acetate is obtained by crystallization or transition in association with a specified solvent. The solvent comprises at least one member selected from the group consisting of water, an aliphatic hydrocarbon, an aromatic hydrocarbon, a halogenated hydrocarbon, a linear alcohol, an alkyl ether, an acetate ester, an alkyl ketone, an N-alkylacylamide, and an alkanenitrile.

FARNESOID X RECEPTOR MODULATORS
20170101434 · 2017-04-13 ·

The present application provides a compound of formula I:

##STR00001##

or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1-R.sup.10, m, n, p, and custom-character are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.

METHODS OF MAKING ONAPRISTONE INTERMEDIATES

Methods and systems for making intermediates in the synthesis of onapristone are provided. Aspects include the photoconversion of onapristone synthesis intermediates using a narrow band frequency light source.

Farnesoid X receptor modulators

The present application provides a compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1-R.sup.10, m, n, p, and custom character are as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.

FARNESOID X RECEPTOR MODULATORS
20250376488 · 2025-12-11 ·

The present application provides a compound of formula I:

##STR00001##

or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1-R.sup.10, m, n, p, and custom-character are as described herein. The present invention relates generally to F modulators and to methods of making and using said compounds.