MODULATORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE
申请人:Durand-Reville Thomas
公开号:US20110021513A1
公开(公告)日:2011-01-27
The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase.
Novel Phenoxyalkylamine Derivatives. VII. Synthesis and Pharmacological Activities of 2-Alkoxy-5-((phenoxyalkylamino)alkyl)benzenesulfonamide Derivatives.
作者:Shunichiro SAKURAI、Kazuya MITANI、Shigeki HASHIMOTO、Koji MORIKAWA、Shingo YASUDA、Eiichi KOSHINAKA、Hideo KATO、Yasuo ITO
DOI:10.1248/cpb.40.1443
日期:——
To find a novel α-blocker with high α-blocking selectivity against dopamine D2-receptor affinity, we performed structural modification of the alkylene chains and the substituents on two benzene rings of 2-alkoxy-5-[(phenoxyalkylamino)alkyl]benzenesulfonamide derivatives. The modification of the alkylene chain between the amino moiety in the center of the molecule and the benzene ring (ring A) was found to be the most significant. 5-[2-[[2-(5-Fluoro-2-methoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzenesulfonamide (II-4), which possesses 1-methylethyl as the alkylene chain, exhibited high α-blocking selectivity as well as potent α-blocking activity.
ACYL PSEUDOPEPTIDES WHICH CARRY A FUNCTIONALIZED AUXILIARY ARM
申请人:BAUER Jacques
公开号:US20130022628A1
公开(公告)日:2013-01-24
The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state.
Compounds of the present invention have immunomodulating properties like adjuvants. In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targeting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.
Borrelidin-producing polyketide synthase and its uses
申请人:Biotica Technology Limited
公开号:EP1961747A2
公开(公告)日:2008-08-27
The present invention relates to the biosynthesis of polyketides and derives from the cloning of nucleic acids encoding a polyketide synthase and other associated proteins involved in the synthesis of the polyketide borrelidin. Materials and methods including enzyme systems, nucleic acids, vectors and cells are provided for the preparation of polyketides including borrelidin and analogues and derivatives thereof. Novel polyketide molecules are also provided.
Disclosed herein are compositions and methods for increasing lifespan, for preventing or treating a disease including an aging-related disorder, for reducing a symptom of aging, and/or boosting an immune system in a mammal. Also disclosed herein are compositions and methods for improving effectiveness of a vaccine in a mammal. The compositions comprise, at least, a therapeutically effective amount of disulfiram and one or more additional ingredients.