Deuterated elagolix-like compositions and methods
AssigneeLupin Limited
InventorsJames Garegnani, Nicholas Hart, Richard Holl
Life of this patent
Estimating the term…
Abstract
New deuterated analogs of elagolix are provided. The novel deuterated elagolix analogs differ from the only previously disclosed deuterated elagolix analogs in structure based on the exclusion of deuterium at certain sites in the compounds and the inclusion of deuterium at other sites. Also provided are new formulations for deuterated elagolix compounds and methods of using such compounds and formulations in the modification of mammalian physiology and especially in the treatment and prevention of a number of diseases and disorders, including endometriosis-associated pain and uterine fibroid conditions.
Claims20
A method of treating endometriosis-associated pain in a human female patient comprising orally administering a pharmaceutically acceptable composition comprising about 40-about 120 mg of a compound comprising a chemical structure according to the formula
- or a pharmaceutically acceptable salt thereof to the patient, wherein (a) the compound comprises between 1-9 deuterium atoms;
- (b) R1, R2, R3, R4, R5, and R6 are either deuterium or hydrogen;
- (c) R7 is either fluorine or chlorine;
- and (c) at least one of the deuterium atoms is at a position selected from R1, R2, R3, R4, R5, and R6 or substitutes a hydrogen at position H73, H74, or H75.
A pharmaceutically acceptable formulation for oral administration comprising about 40 mg to about 120 mg of a compound that modulates GnRH receptor activity in human patients and which comprises a chemical structure according to the formula
- or a pharmaceutically acceptable salt thereof, wherein (a) the compound comprises between 1-9 deuterium atoms;
- (b) R1, R2, R3, R4, R5, and R6 are either deuterium or hydrogen;
- (c) R7 is either fluorine or chlorine;
- and (c) at least one of the deuterium atoms is at a position selected from R1, R2, R3, R4, R5, and R6 or substitutes a hydrogen at position H73, H74, or H75.
A pharmaceutically acceptable compound comprising a structure according to the formula
- or a pharmaceutically acceptable salt thereof, wherein (a) the compound comprises between 1-11 deuterium atoms;
- (b) R1, R2, R3, R4, R5, and R6 are either deuterium or hydrogen;
- (c) R7 is either fluorine or chlorine;
- (d) at least one of the 1-11 deuterium atoms is located at a position selected from R1, R2, R3, R4, R5, and R6;
- and (e) at least one of H73, H74, and H75 is a hydrogen.
Dependencies are inferred from the claim text.