[EN] ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS<br/>[FR] ÉTHYLÈNE DIAMINE EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE L'HYPOCRÉTINE
申请人:MERCK SHARP & DOHME
公开号:WO2016100161A1
公开(公告)日:2016-06-23
The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
[EN] HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS COMPRISING THE HETEROCYCLIC COMPOUND, AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS DE KINASE, COMPOSITIONS COMPRENANT LE COMPOSÉ HÉTÉROCYCLIQUE, ET LEURS PROCÉDÉS D'UTILISATION
申请人:JS INNOPHARM SHANGHAI LTD
公开号:WO2020248972A1
公开(公告)日:2020-12-17
(I) Disclosed herein are compounds of formula I, and/or a stereoisomer, a stable isotope, or a pharmaceutically acceptable salt or solvate thereof; and therapeutic uses of these compounds, which are inhibitors of rearranged during transfection (RET), potentially useful in the treatment of RET-associated diseases, such as RET-associated cancers.
Heterocyclic compounds as ligands of the GABAA receptor
申请人:——
公开号:US20030105081A1
公开(公告)日:2003-06-05
Disclosed are heterocyclic compounds of the formula
1
and the pharmaceutically acceptable salts thereof wherein the variables A, V, Y, J, E, X, T, G, Q, W, Z, b, n and m are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABA
A
brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA
A
brain receptor.
揭示了具有以下公式的杂环化合物及其药用可接受的盐,其中变量A、V、Y、J、E、X、T、G、Q、W、Z、b、n和m在此处被定义。这些化合物是GABA
A
脑受体的高度选择性激动剂、拮抗剂或逆激动剂,或者是GABA
A
脑受体的激动剂、拮抗剂或逆激动剂的前药。
[EN] 8-SUBSTITUTED QUINOLINES AND RELATED ANALOGS AS SIRTUIN MODULATORS<br/>[FR] QUINOLÉINES SUBSTITUÉES EN 8 ET ANALOGUES ASSOCIÉS UTILISÉS COMME MODULATEURS DE SIRTUINE
申请人:SIRTRIS PHARMACEUTICALS INC
公开号:WO2010101949A1
公开(公告)日:2010-09-10
Provided herein are 8-substituted quinolines and related analogues as sirtuin-modulating compounds of Structural Formula (I) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
[EN] PIPERIDINYL- AND PIPERAZINYL-SUBSTITUTED HETEROAROMATIC CARBOXAMIDES AS MODULATORS OF GPR6<br/>[FR] CARBOXAMIDES HÉTÉROAROMATIQUES SUBSTITUÉS PAR PIPÉRIDINYLE ET PIPÉRAZINYLE EN TANT QUE MODULATEURS DE GPR6
申请人:TAKEDA PHARMACEUTICALS CO
公开号:WO2018183145A1
公开(公告)日:2018-10-04
Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R4, R5, R8, R10, R11, X1, X2, X3, X9, X12, and Z 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, and conditions associated with GPR6.