[EN] PI-3 KINASE INHIBITOR PRODRUGS<br/>[FR] PROMEDICAMENTS D'INHIBITEURS DE PI-3 KINASE
申请人:SEMAFORE PHARMACEUTICALS INC
公开号:WO2004089925A1
公开(公告)日:2004-10-21
The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
(R)-Amination mediated by (R)-specific ω-transaminases generally requires costly d-alanine in excess to obtain the desired chiralamines in high yield. Herein, a one-pot, trienzymatic cascade comprising an (R)-specific ω-transaminase, an amine dehydrogenase, and a formate dehydrogenase was developed for the economical and eco-friendly synthesis of (R)-chiral amines. Using inexpensive ammonium formate as the
SULFAMIDE AND SULFAMATE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
申请人:Smil David
公开号:US20070293530A1
公开(公告)日:2007-12-20
This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I), and racemic and scalemic mixtures, diastereomers and enantiomers thereof:
or an N-oxide, hydrate, solvate, pharmaceutically acceptable salt, prodrug or complex thereof, wherein Y, L, Z, W, M, R
a
, R
b
and R
c
are as defined in the specification.
这项发明涉及用于抑制组蛋白去乙酰化酶的化合物。更具体地,该发明提供了符合式(I)的化合物,以及它们的外消旋和内消旋混合物、非对映体和对映体:
或其N-氧化物、水合物、溶剂合物、药学上可接受的盐、前药或其复合物,其中Y、L、Z、W、M、R
a
、R
b
和R
c
如规范中所定义。
Indium-Triflate-Catalyzed Ritter Reaction in Liquid Sulfur Dioxide
作者:Daniels Posevins、Krista Suta、Māris Turks
DOI:10.1002/ejoc.201600013
日期:2016.3
as a reaction solvent facilitates the Ritterreaction between alcohols and nitriles. In(OTf)3 was found to be a viable catalyst for this transformation. The newly developed catalytic conditions for the Ritterreaction were successfully applied to the synthesis of various amides, which were formed in good to excellent yields. The catalytic activation of secondary alcohols for Ritterreactions in liquid
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.