76706-60-0Relevant academic research and scientific papers
PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor
Hangeland, Jon J.,Abell, Lynn M.,Adam, Leonard P.,Jiang, Ji,Friends, Todd J.,Haque, Lauren E.,Neels, James,Onorato, Joelle M.,Chen, Alice Ye A.,Taylor, David S.,Yin, Xiaohong,Harrity, Thomas W.,Basso, Michael D.,Yang, Richard,Sleph, Paul G.,Gordon, David A.,Huang, Christine S.,Wexler, Ruth R.,Finlay, Heather J.,Lawrence, R. Michael
, p. 673 - 678 (2018/07/25)
Screening of a small set of nonselective lipase inhibitors against endothelial lipase (EL) identified a potent and reversible inhibitor, N-(3-(3,4-dichlorophenyl)propyl)-3-hydroxy-1-methyl-2-oxo-1,2-dihydropyridine-4-carboxamide (5; EL IC50 = 6
QUINOLINONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE
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, (2013/04/13)
The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
PYRIDINEDIONE CARBOXAMIDE INHIBITORS OF ENDOTHELIAL LIPASE
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, (2013/04/13)
The present invention provides compounds of Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS
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, (2013/04/13)
The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds
PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS
-
, (2013/04/13)
The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provi
PYRIMIDINONE CARBOXAMIDES AS INHIBITORS OF ENDOTHELIAL LIPASE
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, (2013/10/22)
The present invention provides compounds of Formula (I): (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
Synthesis, structural activity-relationships, and biological evaluation of novel amide-based allosteric binding site antagonists in NR1A/NR2B N-methyl-d-aspartate receptors
Mosley, Cara A.,Myers, Scott J.,Murray, Ernest E.,Santangelo, Rose,Tahirovic, Yesim A.,Kurtkaya, Natalie,Mullasseril, Praseeda,Yuan, Hongjie,Lyuboslavsky, Polina,Le, Phuong,Wilson, Lawrence J.,Yepes, Manuel,Dingledine, Ray,Traynelis, Stephen F.,Liotta, Dennis C.
, p. 6463 - 6480 (2011/03/17)
The synthesis and structure-activity relationship analysis of a novel class of amide-based biaryl NR2B-selective NMDA receptor antagonists are presented. Some of the studied compounds are potent, selective, non-competitive, and voltage-independent antagonists of NR2B-containing NMDA receptors. Like the founding member of this class of antagonists (ifenprodil), several interesting compounds of the series bind to the amino terminal domain of the NR2B subunit to inhibit function. Analogue potency is modulated by linker length, flexibility, and hydrogen bonding opportunities. However, unlike previously described classes of NR2B-selective NMDA antagonists that exhibit off-target activity at a variety of monoamine receptors, the compounds described herein show much diminished effects against the hERG channel and α1-adrenergic receptors. Selections of the compounds discussed have acceptable half-lives in vivo and are predicted to permeate the blood-brain barrier. These data together suggest that masking charged atoms on the linker region of NR2B-selective antagonists can decrease undesirable side effects while still maintaining on-target potency.
Synthesis, structure and quantitative structure-activity relationships of σ receptor ligands, 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazines
Fujimura, Ken-Ichi,Matsumoto, Junzo,Niwa, Masashi,Kobayashi, Tadayuki,Kawashima, Yoichi,In, Yasuko,Ishida, Toshimasa
, p. 1675 - 1683 (2007/10/03)
A set of the title compounds having different substituents (R1, R2) on their phenyl groups was synthesized to find σ receptor binding affinity. Among the compounds, 2b (R1=R2=Cl) has the most potent σ1-binding activity, while 2a (R1=R2=H, SA4503) was most selective to σ1 over σ2 receptor. The crystal structures of 2a and 2b were shown, by X-ray crystallography, to be similar except for the one torsional angle of their propylene parts. Quantitative structure-activity relationship study suggested the affinity of the compounds to the σ1 receptor was dependent on the electronic feature, Swain-Lupton's R or S(π) that was derived by molecular orbital method, of R1 and R2.
Phenylacetamide derivatives and pharmaceutical compositions thereof
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, (2008/06/13)
The present invention provides novel phenylacetamide derivatives having the following formula STR1 wherein: X is a hydrogen, halogen, hydroxy, nitro, amino, R1, NR1 R2, NHR1 or OR1 wherein R1/su
Novel phenylacetamide derivatives and processes for the preparation thereof
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, (2008/06/13)
The present invention provides novel phenylacetamide derivatives having the following formula wherein:, X is a hydrogen, halogen, hydroxy, nitro, amino, R1, NR1R2, NHR1 or OR1 wherein R1 and R2 are an optionally substituted C1 8 alky
