53841-99-9Relevant academic research and scientific papers
New V1a receptor antagonist. Part 2. Identification and optimization of triazolobenzazepines
Baska, Ferenc,Bata, Imre,Bozó, éva,Domány-Kovács, Katalin,Kurkó, Dalma,L?vei, Klára,Szántó, Gábor,Szokoli, Teodóra,Szondiné Kordás, Krisztina
, (2020)
Solid preclinical evidence links vasopressin to social behavior in animals, so, extensive work has been initiated to find new vasopressin V1a receptor antagonists which can improve deteriorated social behavior in humans and can treat the core symptoms of autistic behavior, as well. Our aim was to identify new chemical entities with antagonizing effects on vasopressin V1a receptors. Continuing our previous work, we found an in vitro and in vivo orally active V1a selective antagonist molecule (40) among [1,2,4]triazolo[4,3-a][1]benzazepines.
LPA RECEPTOR ANTAGONISTS AND USES THEREOF
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, (2021/12/17)
The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non alcoholic steatohepatitis (NASH).
Triazole derivative having HSP90 (Heat Shock Protein) inhibiting activity, as well as preparation method and application of triazole derivative
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Paragraph 0217; 0218; 0219; 0220, (2017/08/02)
The invention discloses a triazole derivative having an HSP90 (Heat Shock Protein) inhibiting activity, as well as a preparation method and an application of the triazole derivative. Specifically, the invention relates to the triazole derivative having a structure as shown in a formula (I), a stereisomer of the triazole derivative and a pharmaceutically acceptable salt, wherein the definition of each substituent group in the formula (I) and the definition in a description are the same. The compound with a novel structure has the HSP90 inhibiting activity, can be used to cure cancers, neurodegenerative disorders, inflammation diseases, autoimmune diseases, ischemic brain injuries and the like, and has a broad application prospect.
ALDOSTERONE SYNTHASE INHIBITORS
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, (2012/11/13)
This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
Targeting the polyamine transport system with benzazepine- and azepine-polyamine conjugates
Tomasi, Sophie,Renault, Jacques,Martin, Bénédicte,Duhieu, Stephane,Cerec, Virginie,Le Roch, Myriam,Uriac, Philippe,Delcros, Jean-Guy
experimental part, p. 7647 - 7663 (2011/02/22)
The polyamine transport system (PTS) whose activity is up-regulated in cancer cells is an attractive target for drug design. Two heterocyclic (azepine and benzazepine) systems were conjugated to various polyamine moieties through an amidine bound to afford 18 compounds which were evaluated for their affinity for the PTS and their ability to use the PTS for cell delivery. Structure-activity relationship studies and lead optimization afforded two attractive PTS targeting compounds. The azepine-spermidine conjugate 14 is a very selective substrate of the PTS that may serve as a vector for radioelements used for diagnoses or therapeutics in nuclear medicine. The nitrobenzazepine-spermine conjugate 28 is a very powerful PTS inhibitor with very low intrinsic cytotoxicity, able to prevent the growth of polyamine depleted cells in presence of exogenous polyamines.
LXR modulators
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Page/Page column 62-63, (2010/11/26)
A compound of formula I wherein A, X, q, R1, R2a, R2b, R2c, R3a, and R3b are defined herein.
COMPOUNDS, COMPOSITIONS AND METHODS
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Page/Page column 51, (2010/11/24)
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
Lipoxygenase Inhibitors, III: Synthesis of Tetrahydrobenzazepinone Phenylhydrazones
Buege, Axel,Locke, Christian,Koehler, Thomas,Nuhn, Peter
, p. 99 - 104 (2007/10/02)
Tetrahydro-2H-benzazepin-2-ones as starting substances are synthesized by Beckmann rearrangement or Schmidt reaction.The tetrahydrobenzazepinones are transformed into the thiones, thiolactim ethers and phenylhydrazones.The compounds are tested as inhibitors of soja lipoxygenase.
