194427-22-0

Upstream product

• 120-92-3 cyclopentanone 
• 132439-40-8 1-cyclopropylcyclopentylazide 
• 132439-41-9 1-cyclopropylcyclopentylamine 
• 59819-64-6 1-cyclopropylcyclopentanol 
• 194427-20-8 N-(1-Cyclopropylcyclopent-1-yl)-4(S)-4-(3,4-dichlorophenyl)-4-hydroxymethylhept-6-enamide 
• 194427-21-9 N-(1-Cyclopropylcyclopent-1-yl)-4(S)-4-(3,4-dichlorophenyl)-4-methanesulphonyloxymethylhept-6-enamide 

Relevant academic research and scientific papers

Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3- (substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption

A series of piperidone analogues of 1b-q, seeking replacements for the polar sulfamide moiety in clinical candidate UK-224,671 1a, possessing reduced H-bonding potential as a strategy to improve oral absorption, were prepared. These studies led to the successful identification of 1n, which demonstrated equivalent pharmacology and metabolic stability to 1a, and greatly improved oral absorption as assessed in rat PK studies.

Piperidone tachykinin antagonists

The present invention provides compounds of formula (I) and the pharmaceutically acceptable acid addition salts thereof, wherein X is a direct link or C1-C4alkylene; and R is C3-C7cycloalkyl optionally substituted by 1 or 2 substituents each independently selected from fluoro and C3-C7cycloalkyl: with the proviso that X is not methylene when R is cyclopropyl, together with processes for the preparation of, intermediates used in the preparation of, compositions containing and uses of, such compounds. These compounds are useful as tachykinin antagonists.