Synthesis and Protein Kinase C Inhibitory Activities of Balanol Analogs with Replacement of the Perhydroazepine Moiety
摘要:
Balanol is a potent protein kinase C (PKC) inhibitor that is structurally composed of a benzophenone diacid, a 4-hydroxybenzamide, and a perhydroazepine ring. A number of balanol analogs in which the perhydroazepine moiety is replaced have been synthesized and their biological activities evaluated against both PKC and cAMP-dependent kinase (PKA). The results suggested that the activity and the isozyme/kinase selectivity of these compounds are largely related to the conformation about this nonaromatic structural element of the molecules.
Trimethysilyl triflate in organic synthesis11Part 11 of this series. Part 10: S. Murata and R. Noyori, Tetrahedron Letters 2107 (1981).
作者:R. Noyori、S. Murata、M. Suzuki
DOI:10.1016/s0040-4020(01)93263-6
日期:——
Trimethylsilyl triflate is a powerful silylating agent for organic compounds and acts as a catalyst which accelerates a variety of nucleophilic reactions in aprotic media. The reactions proceed via one-center, electrophilic coordination of the silyl group to hetero functional groups and exhibit unique selectivities.
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof,
wherein L, X, R
a
, R
b
, R
1
, R
2
and R
3
are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
This invention relates to methods and compositions for preparing linear and cyclic polyolefins. More particularly, the invention relates to methods and compositions for preparing functionalized linear and cyclic polyolefins via olefin metathesis reactions. Polymer products produced via the olefin metathesis reactions of the invention may be utilized for a wide range of materials applications. The invention has utility in the fields of polymer and materials chemistry and manufacture.
Cycloalkyl and heterocycloalkyl compounds as orexin receptor antagonists
申请人:Takeda Pharmaceutical Company Limited
公开号:US09156829B2
公开(公告)日:2015-10-13
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof,
wherein L, X, Ra, Rb, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.