152533-47-6Relevant articles and documents
COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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Paragraph 0553; 0560; 0561, (2015/07/02)
The present invention provides compounds of Formula A: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease.
Substituted Imidazopyridines as HDM2 Inhibitors
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Paragraph 0761, (2014/07/08)
The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
Tetraaza-cyclopenta[a]indenyl derivatives
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Paragraph 0109, (2015/01/18)
The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues
Wei, Zhi-Liang,Petukhov, Pavel A.,Xiao, Yingxian,Tückmantel, Werner,George, Clifford,Kellar, Kenneth J.,Kozikowski, Alan P.
, p. 921 - 924 (2007/10/03)
Conformationally constrained epibatidine analogues 20a,b and 23a,b were synthesized using a radical cyclization as the key step. Radioligand displacement assays to six defined rat nicotinic acetylcholine receptor (nAChR) subtypes showed that 20a,b bind with moderate affinities, while 23a,b have low affinities. 20a exhibits higher affinity for the β2 containing subtype than for the β4 containing counterpart, while 20b possesses reversed selectivity. Modeling studies suggest that the spatial distribution of the ligand's atoms around the pharmacophore elements may control their nAChR subtype selectivity.
METHOD FOR SYNTHESIS OF HALOPYRIDYL-ACYCLOPENTANE DERIVATIVE AND INTERMEDIATE THEREOF
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, (2008/06/13)
The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optical
2-Bromoethynyl aryl sulfones as versatile dienophiles: A formal synthesis of epibatidine
Zhang, Chunming,Ballay II, Charles J.,Trudcll, Mark L.
, p. 675 - 676 (2007/10/03)
A facile synthesis of 2-bromoethynyl aryl sulfones has been developed; the reactivity of these versatile dienophiles in [4 + 2] cycloaddition reactions as well as application in a formal synthesis of epibatidine is described.
Total Synthesis and Determination of the Absolute Configuration of Epibatidine
Fletcher, Stephen R.,Baker, Raymond,Chambers, Mark S.,Herbert, Richard H.,Hobbs, Sarah C.,et al.
, p. 1771 - 1778 (2007/10/02)
The synthesis of (+)- and (-)-epibatidine (exo-2-(2-chloropyridin-5-yl)-7-azabicycloheptane) via reaction of 5-lithio-2-chloropyridine with (+)- and (-)-N-BOC-7-azabicycloheptan-2-one is described.The absolute configuration of the natural product is shown to be 1R,2R,4S.
The Synthesis of (+)- and (-)-Epibatidine
Fletcher, Stephen R.,Baker, Raymond,Chambers, Mark S.,Hobbs, Sarah C.,Mitchell, Paul J.
, p. 1216 - 1218 (2007/10/02)
The synthesis of the alkaloid epibatidine heptane> in enantiomeric form involving, as the critical step, reaction or 5-lithio-2-chloropyridine with N-tert-butoxycarbonyl-7-azabicycloheptan-2-one is des
