Quantitative structure-activity relationships of 6-anilinouracils as inhibitors of Bacillus subtilis DNA polymerase III
摘要:
Quantitative structure-activity relationships (QSAR) of a series of 6-anilinouracil derivatives were developed for their inhibitory activity against the wild-type DNA polymerase III (pol III) and a mutant enzyme, pol III/azp-12, derived from Bacillus subtilis. Interaction between inhibitors and both enzymes appears to result solely from hydrophobic binding. Comparison of the substituent contributions indicates increased hydrophobic character and a minor change of shape of the inhibitor binding site of the mutant enzyme. Because the two enzymes have identical Km values for substrates, the inhibitor binding site is thought to be distinct from the enzyme active site.
A compound represented by the following general formula (1) or a salt thereof, which has superior inhibitory activity against type 4 PLA
2
, and thus has prostaglandin and/or leucotriene production suppressing action [X represents a halogen atom, an alkyl group which may be substituted, or the like, Y represents hydrogen atom or an alkyl group which may be substituted, and Z represents hydrogen atom or an alkyl group which may be substituted].
Heterocyclic derivatives as modulators of ion channels
申请人:Vertex Pharmaceuticals Incorporated
公开号:EP2316829A1
公开(公告)日:2011-05-04
The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
POLYAMIC ACID COMPOSITION, LIQUID CRYSTAL ALIGNING FILM, AND LIQUID CRYSTAL DISPLAY ELEMENT
申请人:CHISSO CORPORATION
公开号:EP1064319A1
公开(公告)日:2001-01-03
US8772327B2
申请人:——
公开号:US8772327B2
公开(公告)日:2014-07-08
[EN] POLYAMIC ACID COMPOSITION, LIQUID CRYSTAL ALIGNING FILM, AND LIQUID CRYSTAL DISPLAY ELEMENT<br/>[FR] COMPOSITION D'ACIDE POLYAMIQUE, COUCHE D'ALIGNEMENT DE CRISTAUX LIQUIDES ET ELEMENT D'AFFICHAGE A CRISTAUX LIQUIDES
申请人:CHISSO CORPORATION
公开号:WO1999033902A1
公开(公告)日:1999-07-08
(EN) The present invention provides a polyimide alignment film having excellent electrical properties and excellent reliability for use in the field of electronic materials which comprises a polyimide resin produced from a polyamic acid composition comprising a polyamic acid forming a polyimide resin of a low residual voltage and a high voltage holding ratio, and a polyamic acid forming a polyimide resin of a large pre-tilt angle, blended them in the ratio of the former to the latter of 50/50 to 95/5 (weight ratio), a polyamic acid composition for providing such a polyimide aligning film and a liquid crystal display element produced from such an aligning film.(FR) L'invention concerne une couche d'alignement polyimide comprenant d'excellentes propriétés électriques et une excellente fiabilité, utilisable dans le domaine des matériaux électroniques. Cette couche d'alignement comprend une résine polyimide produite à partir d'une composition d'acide polyamique comprenant une résine polyimide à faible tension résiduelle et à taux de maintien de tension élevée, et un acide polyamique permettant de former une résine polyimide pour présentant un angle de pré-inclinaison important. On mélange ces deux produit à raison d'un rapport entre le premier et le second allant 50/50 à 95/5 (en poids). L'invention concerne également une composition d'acide polyamique permettant de préparer une telle couche d'alignement polyimide et un élément d'affichage à cristaux liquides fabriqué avec une telle couche d'alignement.