913346-12-0

Upstream product

• 21573-10-4 1-cyclopropyl-butane-1,3-dione 
• 58537-99-8 4-hydroxy-2,6-dimethylbenzonitrile 
• 473924-31-1 2-chloro-1-cyclopropylbutane-1,3-dione 

Relevant academic research and scientific papers

Development of a Practical Synthesis of the Progesterone Receptor Antagonist 4-{[3-Cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy}-2,6- dimethylbenzo-nitrile

The development and implementation of a scaleable process for the manufacture of the nonsteroidal progesterone receptor antagonist 8 is described. Key aspects of the synthesis include (i) a telescoped chlorination- etherification sequence to prepare diket

Unusual base-catalyzed exchange in the synthesis of deuterated PF-2413873

The preparation of deuterated PF-2413873 (4-[3-cyclopropyl-1- (methanesulfonylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy-2, 6-dimethylbenzonitrile, 1) is described for use as a bioanalytical standard in clinical trials. Two strategies were investigated. The sul

Compounds Useful In Therapy

Compounds of Formula (I): and pharmaceutically acceptable salts, solvates (including hydrates) of said compounds and salts, or prodrugs of said compound, or pharmaceutically acceptable salts or solvates of said prodrugs, wherein the substituents are as herein defined, are useful in therapy, for example they may be useful for treating progesterone-mediated conditions such as endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.

Compounds useful in therapy

Compounds of formula (I), [image] or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii) one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6 alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.