165377-40-2Relevant academic research and scientific papers
PIPERAZINE DERIVATIVES
-
Page/Page column 11-12, (2008/06/13)
Compounds of general formula (I) in which R1 and R0 have any of the meanings given in the specification have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.
Synthesis and structure - Activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis
Aranapakam, Venkatesan,Davis, Jamie M.,Grosu, George T.,Baker, Jannie,Ellingboe, John,Zask, Arie,Levin, Jeremy I.,Sandanayaka, Vincent P.,Du, Mila,Skotnicki, Jerauld S.,DiJoseph, John F.,Sung, Amy,Sharr, Michele A.,Killar, Loran M.,Walter, Thomas,Jin, Guixian,Cowling, Rebecca,Tillett, Jeff,Zhao, Weiguang,McDevitt, Joseph,Xu, Zhang Bao
, p. 2376 - 2396 (2007/10/03)
The matrix metalloproteinases (MMPs) are a family of zinc-containing endopeptidases that play a key role in both physiological and pathological tissue degradation. In our preceding paper, we have reported on a series of novel and orally active N-hydroxy-α-phenylsulfonylacetamide derivatives. However, these compounds had two drawbacks (moderate selectivity and chirality issues). To circumvent these two problems, a series of novel and orally active N-substituted 4-benzenesulfonylpiperidine-4-carboxylic acid hydroxyamide derivatives have been synthesized. The present paper deals with the synthesis and SAR of these compounds. Among the several compounds synthesized, derivative 55 turned out to be a potent, selective, and an orally active MMP inhibitor in the clinically relevant advanced rabbit osteoarthritis model. Detailed pharmacokinetics and metabolism data are described.
1,4-(diphenlyalkyl) piperazine derivatives
-
, (2008/06/13)
This invention relates to novel compounds of the formula [I], STR1 wherein R 1 and R 2 are the same or different and each represents a lower alkoxy group; A and B are the same or different and each represents a lower alkylene group.The compounds of this i
