1268511-99-4Relevant academic research and scientific papers
Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists
Cherney, Robert J.,Nelson, David J.,Lo, Yvonne C.,Yang, Gengjie,Scherle, Peggy A.,Jezak, Heather,Solomon, Kimberly A.,Carter, Percy H.,Decicco, Carl P.
, p. 5063 - 5065 (2008)
A series of cis-3,4-disubstituted piperidines was synthesized and evaluated as CC chemokine receptor 2 (CCR2) antagonists. Compound 24 emerged with an attractive profile, possessing excellent binding (CCR2 IC50 = 3.4 nM) and functional antagonism (calcium flux IC50 = 2.0 nM and chemotaxis IC50 = 5.4 nM). Studies to explore the binding of these piperidine analogs utilized a key CCR2 receptor mutant (E291A) with compound 14 and revealed a significant reliance on Glu291 for binding.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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, (2014/01/08)
The present invention provides a compound, solid forms, and compositions thereof, which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same. The present invention also provides methods of making provided compound and solid forms.
BICYCLIC OXAZOLE AND THIAZOLE COMPOUNDS AND THEIR USE AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS
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Page/Page column 132, (2012/03/26)
In one aspect, the invention relates to novel bicyclic oxazole and thiazole compounds which are positive allosteric modulators of the metabotropic glutamate receptor subtype 5 ("mGluR5"); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions; and methods for the treatment or prevention of disorders associated with glutamate dysfunction and diseases in which the mGluR5 subtype of receptors is involved. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
METHYLPYRROLOPYRIMIDINECARBOXAMIDES
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Page/Page column 109, (2012/06/18)
The compounds of Formula (I), wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
METHYLPYRROLOPYRIMIDINECARBOXAMIDES
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Page/Page column 176, (2011/04/14)
The compounds of formula (I) wherein R1, R2, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, and the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiestera
METHYLPYRROLOPYRIDINECARBOXAMIDES
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Page/Page column 91, (2011/04/14)
The compounds of formula (I) wherein R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, and the stereoisomers of the compounds and the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
DIPEPTIDYL PEPTIDASE-IV INHIBITING COMPOUNDS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE AGENT
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Page/Page column 90, (2010/11/24)
The present invention relates to novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV), methods of preparing the same and pharmaceutical compositions containing the same as an active agent.
Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole
Ashton, Wallace T.,Sisco, Rosemary M.,Dong, Hong,Lyons, Kathryn A.,He, Huaibing,Doss, George A.,Leiting, Barbara,Patel, Reshma A.,Wu, Joseph K.,Marsilio, Frank,Thornberry, Nancy A.,Weber, Ann E.
, p. 2253 - 2258 (2007/10/03)
A series of β-aminoacylpiperidines bearing various fused five-membered heterocyclic rings was synthesized as dipeptidyl peptidase IV inhibitors. Potent and relatively selective inhibition could be obtained, depending on choice of heterocycle, regioisomerism, and substitution. In particular, one analog (74, DPP-IV IC50 = 26 nM) exhibited good oral bioavailability and acceptable half-life in the rat, albeit with rather high clearance.
CHEMICAL COMPOUNDS
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Page/Page column 104, (2010/02/15)
The use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein X1, X2, X3, X4, Ra, p, R1,Z,Y, R2, R3 and R4 are as d
