863600-79-7Relevant academic research and scientific papers
DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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, (2012/07/28)
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 31, (2012/08/08)
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
An octahydro-cyclopenta[c]pyrrole series of inhibitors of the type 1 glycine transporter
Lowe III, John A.,DeNinno, Shari L.,Drozda, Susan E.,Schmidt, Christopher J.,Ward, Karen M.,David Tingley III,Sanner, Mark,Tunucci, Don,Valentine, James
supporting information; experimental part, p. 907 - 911 (2010/08/19)
We describe a novel series of inhibitors of the type 1 glycine transporter (GlyT1) as an approach to relieving the glutamatergic deficit that is thought to underlie schizophrenia. Synthesis and SAR follow-up of a series of octahydro-cyclopenta[c]pyrrole derivatives afforded potent in vitro inhibition of GlyT1 as well as in vivo activity in elevating CSF glycine. We also found that a 3-O(c-pentyl), 4-F substituent may serve as a surrogate for the widely used 3-trifluoromethoxy group, suggesting its application as an isostere for future medicinal chemistry studies.
Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc
Lemoine, Rémy C.,Petersen, Ann C.,Setti, Lina,Baldinger, Thomas,Wanner, Jutta,Jekle, Andreas,Heilek, Gabrielle,deRosier, André,Ji, Changhua,Rotstein, David M.
scheme or table, p. 1674 - 1676 (2010/07/03)
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the 3-amino-8-azabicyclo[3.2.1]octane found in the CCR5 antagonist maraviroc.
Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity
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Page/Page column 19, (2010/02/14)
The present application describes modulators of MCP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, n, R1, R2, R3, R4, R5, R10, R
