UCHP Method for Oligosaccharide Combinatorial Library Synthesis
摘要:
A new methodology for oligosaccharide combinatorial library synthesis using a special hydroxy protecting group, the uni-chemo hydroxy protection (UCHP) group, was developed. The UCHP group was composed of oligomeric amino acid derivatives. The amino terminals of UCHP groups were protected by either Boc or Fmoc groups. By using these two types of UCHP, five kinds of trigalactoses [Gal beta 1-3Gal beta 1-3Gal, Gal beta 1-3(Gal beta 1-4) Gal, Gal beta 1-4Gal beta 1-3Gal, Gal beta 1-3Gal beta 1-4Gal, and Gal beta 1-4Gal beta 1-4Gal] were successfully synthesized on a solid support as a model of oligosaccharide combinatorial library. Each step of all reactions was also successfully monitored using a combination of two colorimetric tests, chloranil and methyl red-DIC.
UCHP Method for Oligosaccharide Combinatorial Library Synthesis
摘要:
A new methodology for oligosaccharide combinatorial library synthesis using a special hydroxy protecting group, the uni-chemo hydroxy protection (UCHP) group, was developed. The UCHP group was composed of oligomeric amino acid derivatives. The amino terminals of UCHP groups were protected by either Boc or Fmoc groups. By using these two types of UCHP, five kinds of trigalactoses [Gal beta 1-3Gal beta 1-3Gal, Gal beta 1-3(Gal beta 1-4) Gal, Gal beta 1-4Gal beta 1-3Gal, Gal beta 1-3Gal beta 1-4Gal, and Gal beta 1-4Gal beta 1-4Gal] were successfully synthesized on a solid support as a model of oligosaccharide combinatorial library. Each step of all reactions was also successfully monitored using a combination of two colorimetric tests, chloranil and methyl red-DIC.
2' FLUORO SUBSTITUTED CARBA-NUCLEOSIDE ANALOGS FOR ANTIVIRAL TREATMENT
申请人:Gilead Sciences, Inc.
公开号:US20170226140A1
公开(公告)日:2017-08-10
Provided are methods for treating Orthomyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I:
wherein R
2
is halogen. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.
A hydantoin derivative represented by formula (I):
wherein the all symbols are defined in the disclosure. The hydantoin derivative has an inhibitory activity on metalloprotease and hence is useful as analgesic and cardiovascular drug.
A compound of Formula I, Formula II, Formula III, or Formula IV:
or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
[Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia.
[Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.
[Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia.
[Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.