摘要:
This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.
摘要翻译:本发明提供具有下式的稠合杂环:其中R 1是选自H,取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R 2是选自H取代或未取代的烯基,取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R 3是选自H,C 1 -C 6取代或未取代的烷基,取代或未取代的芳基烷基和取代的 或未取代的杂芳基烷基。 R 4是选自OH和O - O + X +的成员,其中X + +是正离子,其中 是选自有机正离子和无机阳离子的成员。 取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式:其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。 索引n是从1到4的整数。
摘要:
This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. Also provided are methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein Q is a member selected from O, S, CR1 and N, X and Y are members independently selected from CR2, O, S, N and NR3.
摘要:
There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the β-sheet mimetic is a thrombin inhibitor.
摘要:
Compounds having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein A, A′, B, X, Y, R2, R3, R4 and R5 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are tryptase antagonists.
摘要:
β-sheet mimetics and methods relating to the same are disclosed. The β-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a β-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.