- Pancreatic lipase inhibitor compounds, their synthesis and use
-
The subject invention features compounds having the structure: wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1-C15 alkyl, C1-C8 alkylaryl, —C(O)OR4, —C(O)NR4R5, —CR6R6′OR4, —CR6R6′OC(O)R4, —CR6R6′OC(O)NHR7, —C(O)NR10R11, —C(O)NR8R9 NR8R9, —N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1—C30 alkyl or branched C3-C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, —CH2-aryl, aryl —C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6′ are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
- -
-
-
- Synthesis and use of thiophene- and pyrrole-based heteroaromatic compounds
-
Methods for preparing thiophene and pyrrole-based heterocyclic compounds are disclosed. Also disclosed are libraries of thiophene and pyrrole-based heterocyclic compounds, methods for preparing the libraries of thiophene and pyrrole-based heterocyclic compounds, and methods for using the thiophene and pyrrole-based heterocyclic compounds and compound libraries of the invention. The compounds of the invention have biological activity including anti-cancer activity.
- -
-
-
- Practical synthesis of tetrasubstituted thiophenes for use in compound libraries
-
Tetrasubstituted thiophenes, obtained by optimizing the multi-component reaction originally developed by Gewald, served as key templates for structural diversification and semi-automated library synthesis. Conditions were developed to carry out Gewald's reaction at room temperature and in high yield.
- McKibben, Bryan P.,Cartwright, Craig H.,Castelhano, Arlindo L.
-
p. 5471 - 5474
(2007/10/03)
-