5-Aryl thiazolidine-2,4-diones: discovery of PPAR dual α/γ agonists as antidiabetic agents
摘要:
A novel series of 5-aryl tliiazolidine-2,4-diones based dual PPARalpha/gamma agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia. (C) 2003 Elsevier Ltd. All rights reserved.
[EN] INHIBITORS OF THE NOTCH TRANSCRIPTIONAL ACTIVATION COMPLEX AND METHODS FOR USE OF THE SAME<br/>[FR] INHIBITEURS DU COMPLEXE D'ACTIVATION DE TRANSCRIPTION DU RÉCEPTEUR NOTCH ET PROCÉDÉS D'UTILISATION DE CES DERNIERS
申请人:UNIV MIAMI
公开号:WO2016154255A1
公开(公告)日:2016-09-29
Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.
Oxidative and Reductive Cross-Coupling Reactions Catalyzed by an Anionic “Ligandless” Palladium Complex
作者:Felix Schroeter、Swantje Lerch、Thomas Strassner
DOI:10.1021/acs.oprd.8b00274
日期:2018.12.21
anionic complex [NBu4][Pd(DMSO)Cl3], which can be synthesized on a gram scale in a single step starting from commercially available starting materials, has been shown to be an active catalyst in the Mizoroki–Heck reaction of aryl halides. We present two new catalytic applications of this complex: the base-free oxidative Heck reaction and the reductive homodimerization of aryl halides. This complex outperformed
designed and synthesized non-peptide organic molecular ligands for integrinαvβ3. Candidate ligands featured amidino analog and carboxy groups as binding sites on either side of a spacer, which consisted of benzophenone or an analog, such as diphenyl sulfide, diphenyl sulfoxide, diphenyl sulfone, or diphenyl ether. Competitive binding assays to integrinαvβ3 with respect to [125I]echistatin were used to determine
我们设计并合成了整合素α v β 3的非肽有机分子配体。候选配体的特点是脒基类似物和羧基作为间隔基两侧的结合位点,间隔基由二苯甲酮或类似物组成,例如二苯硫醚、二苯亚砜、二苯砜或二苯醚。使用与[ 125 I]echistatin 相关的整联蛋白α v β 3的竞争性结合测定来确定合成配体的抑制活性。带有由二苯甲酮间隔物分隔的 2-氨基苯并咪唑基和甘氨酰基团的配体表现出比代表天然整合素 α v β 3的线性 Arg-Gly-Asp (RGD) 三肽更有效的结合结合母题。具有2-氨基苯并咪唑基和羧基以及二苯亚砜或二苯醚间隔基的配体抑制[ 125 I]echistatin 的结合,其IC 50 值与线性RGD 三肽的IC 50值相似。 全尺寸图像
Compositions for repelling crawling insects
申请人:——
公开号:US20020094993A1
公开(公告)日:2002-07-18
The present invention relates to novel compositions, comprising a repellent and an additive, where the additive is selected from the group consisting of phenol, benzaldehyde, benzoic acid or derivatives thereof and is present in a ratio of from 10:100 to 200:100% by weight to the repellent, and to their use for repelling crawling harmful insects, in particular ants or cockroaches.
Inhibitors of the Notch transcriptional activation complex and methods for use of the same
申请人:UNIVERSITY OF MIAMI
公开号:US10501413B2
公开(公告)日:2019-12-10
Disclosed herein are inhibitors of the Notch transcriptional activation complex, and methods for their use in treating or preventing diseases, such as cancer. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: Formula (I), wherein the substituents are as described.