Synthesis and structure–activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists
摘要:
A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives was synthesized, and their structure-activity relationships were examined in order to identify potent and selective arginine vasopressin V-2 receptor agonists. Attempts to substitute other chemical groups in place of the 2-pyridilmethyl moiety of 1a led to the discovery that potent V-2 binding affinity could be obtained with a wide range of functional groups. This structural tolerance allowed for the manipulation of other attributes, such as selectivity against V-1a receptor affinity or avoidance of the undesirable inhibition of cytochrome P450 (CYP), without losing potent affinity for the V-2 receptor. Some representative compounds obtained in this study were also found to decrease urine volume in awake rats. (C) 2009 Elsevier Ltd. All rights reserved.
[EN] COMPOUNDS AND METHODS FOR MODULATING ADENOSINE A2B RECEPTOR AND ADENOSINE A2A RECEPTOR<br/>[FR] COMPOSÉS ET PROCÉDÉS DE MODULATION DU RÉCEPTEUR A2B DE L'ADÉNOSINE ET DU RÉCEPTEUR A2A DE L'ADÉNOSINE
申请人:CORVUS PHARMACEUTICALS INC
公开号:WO2019046784A1
公开(公告)日:2019-03-07
Disclosed herein, inter alia, are compositions and methods for modulating Adenosine Receptors. In an aspect is provided a method of inhibiting Adenosine A2B Receptor activity and Adenosine A2A Receptor activity, the method including contacting the Adenosine A2B Receptor and Adenosine A2A Receptor with a compound as described herein, including embodiments.
[EN] A3 ADENOSINE RECEPTOR AGONISTS FOR USE IN MEDICINE<br/>[FR] ANALOGUES DU RÉCEPTEUR A3 DE L'ADÉNOSINE POUR LE TRAITEMENT D'UNE MALADIE
申请人:BIOINTERVENE INC
公开号:WO2022040241A1
公开(公告)日:2022-02-24
The disclosure provides adenosine analogs for the treatment of disease such as pain and inflammatory conditions.
该披露提供了用于治疗疾病如疼痛和炎症症状的腺苷类似物。
Synthesis of imidazo[1,5-a]pyridines from 1,1-dibromo-1-alkenes
作者:Aimin Zhang、Xiaoling Zheng、Junfa Fan、Wang Shen
DOI:10.1016/j.tetlet.2009.12.013
日期:2010.2
An efficient method is developed for the synthesis of imidazo[1,5-a]pyridine from the reaction of 1,1-dibromo-1-alkenes with 2-aminomethylpyridines. The reaction requires an inorganic base, such as Na2CO3, and moderate heating in DMF to proceed. Moderate to good yields are obtained. As demonstrated by the authors and others, 1,1-dibromo-1-alkenes are employed as synthons for activated carboxyl groups
开发了一种由1,1-二溴-1-烯烃与2-氨基甲基吡啶反应合成咪唑并[1,5- a ]吡啶的有效方法。该反应需要无机碱,例如Na 2 CO 3,并在DMF中进行适度加热。获得了中等至良好的产量。正如作者和其他人所证明的,1,1-二溴-1-烯烃被用作活化羧基的合成子。
[EN] 3-AMINO-4H-BENZO[E][1,2,4]THIADIAZINE 1,1-DIOXIDE DERIVATIVES AS INHIBITORS OF MRGX2<br/>[FR] DÉRIVÉS DE 1,1-DIOXYDE DE 3-AMINO-4H-BENZO[E][1,2,4]THIADIAZINE EN TANT QU'INHIBITEURS DE MRGX2
申请人:SOLENT THERAPEUTICS LLC
公开号:WO2020223255A1
公开(公告)日:2020-11-05
Disclosed are compounds of Formula (1), tautomers thereof, and pharmaceutically acceptable salts of the compounds or tautomers, wherein L, R1, R2, R3, R4 and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with MRGX2.
Certain 6-benzamidomethyl-2(1H)-pyridone derivatives
申请人:Riker Laboratories, Inc.
公开号:US04555573A1
公开(公告)日:1985-11-26
Certain substituted pyridine compounds are useful synthetic intermediates for preparing compounds of pharmaceutical interest. A synthetic process for using these intermediates is also described.