Substituted 3-(phenylmethyl)-1H-indole-5-carboxamides and 1-(phenylmethyl)indole-6-carboxamides as potent, selective, orally active antagonists of the peptidoleukotrienes
摘要:
Substituted indole-5-carboxamides and indole-6-carboxamides have been found to be potent and selective antagonists of the peptidoleukotrienes. Initial derivatives of these series (4-[[5-[(cyclopentylmethyl)carbamoyl]-1-methylindol-3-yl]methyl]-3-methoxy-N-[(2-methylphenyl)sulfonyl] benzamide (5a) and 4-[[6-[(cyclopentylmethyl)carbamoyl]-3-methylindol-1-yl]methyl]-3-methoxy-N-[(2-methylphenyl)sulfonyl]benzamide (6a), respectively), when compared to the corresponding indole amides (e.g. 28 and 29), were found to be approximately 10-fold less potent in vitro and substantially less active when administered orally to guinea pigs. Efforts to improve the potency of the title series by variation of the amide, indole, or sulfonamide substituents led to compounds of comparable in vitro potency to ICI 204,219, but of somewhat lower oral activity. A trend which suggested that more lipophilic transposed amides were needed to increase oral activity was exploited with some success and has led to the discovery of 5q (4-[[5-[(2-ethylbutyl)-carbamoyl]-1-ethylindol-3-yl]methyl]-3-methoxy-N-[(2-methylphenyl)sulfonyl]benzamide), a trans-posed amide with subnanomolar affinity for the leukotriene receptor and an oral ED50 of 5 mg/kg in a model of asthma in guinea pigs. In this model, ICI 204,219 was active at 0.4 mg/kg. The absolute bioavailability of 5q has been found to be 28% in the rat, as compared to 68% for ICI 204,219, with significant levels of 5q observed in the blood of rats up to 24 h postdose.
[EN] ALKYL PYRROLOPYRIMIDINE ANALOGS AND METHODS OF MAKING AND USING SAME<br/>[FR] ANALOGUES D'ALKYLE PYRROLOPYRIMIDINE ET LEURS PROCÉDÉS DE PRÉPARATION ET D'UTILISATION
申请人:UNIV NORTH CAROLINA CHAPEL HILL
公开号:WO2018094227A1
公开(公告)日:2018-05-24
The present disclosure is concerned with benzo annulene compounds that are capable of inhibiting a Mer tyrosine kinase and/or a Tyro3 tyrosine kinase and methods of treating a bacterial infection, a viral infection, and/or a disorder of uncontrolled cellular proliferation such as, for example, a cancer, using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
ORGANOMETALLIC COMPOUND, ORGANIC LIGHT-EMITTING DEVICE INCLUDING ORGANOMETALLIC COMPOUND, AND DIAGNOSTIC COMPOSITION INCLUDING ORGANOMETALLIC COMPOUND
申请人:Samsung Electronics Co., Ltd.
公开号:EP3825320A1
公开(公告)日:2021-05-26
Provided are an organometallic compound represented by Formula 1, an organic light-emitting device including the organometallic compound, and a diagnostic composition including the organometallic compound:
Formula 1 M(L1)n1(L2)n2
wherein, in Formula 1, M, L1, L2, n1 and n2 may each be understood by referring to the descriptions thereof provided herein.
Method for making an organoaminosilane; a method for making a silylamine from the organoaminosilane
申请人:Dow Silicones Corporation
公开号:US10875877B2
公开(公告)日:2020-12-29
A method of making an organoaminosilane compound, comprising i) combining A) a compound comprising a primary or secondary amine, B) monosilane (SiH4), and C) a catalyst, where the catalyst comprises magnesium or boron, where A), B) and C) are combined under sufficient conditions to form the organoaminosilane compound and hydrogen. A method of making a silylamine, the method comprising: i) forming an organoaminosilane compound by i) combining A) a compound comprising a primary or secondary amine, B) monosilane (SiH4), and C) a catalyst, where the catalyst comprises magnesium or boron, and ii) combining ammonia and the organoaminosilane compound produced in i) under sufficient conditions to form a silylamine product and a byproduct, where the byproduct is a primary or secondary amine.
一种制造有机氨基硅烷化合物的方法,包括 i) 将 A) 由伯胺或仲胺组成的化合物、B) 单硅烷(SiH4)和 C) 催化剂结合,其中催化剂包括镁或硼,A)、B)和 C) 在足够的条件下结合以形成有机氨基硅烷化合物和氢。一种制造硅胺的方法,该方法包括:i)通过以下方法形成有机氨基硅烷化合物:i)将A)包含伯胺或仲胺的化合物、B)单硅烷(SiH4)和C)催化剂结合,其中催化剂包含镁或硼;和ii)在充分条件下将氨和i)中产生的有机氨基硅烷化合物结合,形成硅胺产物和副产物,其中副产物是伯胺或仲胺。
High purity trisilylamine, methods of making, and use
申请人:Jiangsu Nata Opto-Electronic Materials Co. Ltd.
公开号:US11111256B2
公开(公告)日:2021-09-07
A composition, comprising: trisilylamine and less than 5 ppmw of halogen. A method of making a silylamine comprising combining ammonia and a compound comprising aminosilane functionality, where the compound comprising aminosilane functionality is according to formula (I) R1 N(R2)a(SiH3)2−a (I), where R1 is an organic polymer, a C-1-20 hydrocarbyl group or —SiR331, where R3 is C1-6 hydrocarbyl, R2 is a C-1-20 hydrocarbyl group, H, or —SiR331, where R3 is as defined above, subscript a is 0 or 1, provided that R1 and R2 may be the same or different except if R1 is phenyl, R2 is not phenyl, under sufficient conditions to cause a reaction to form a silylamine and a byproduct.
[EN] ANTI-WARPING HIGH-TEMPERATURE-RESISTANT REINFORCED POLYAMIDE COMPOSITION AND PREPARATION METHOD THEREFOR<br/>[FR] COMPOSITION DE POLYAMIDE RENFORCÉ, ANTI-GAUCHISSEMENT, RÉSISTANT À UNE TEMPÉRATURE ÉLEVÉE ET SON PROCÉDÉ DE PRÉPARATION<br/>[ZH] 抗翘曲耐高温增强聚酰胺组合物及其制备方法