Synthesis of substituted 5-aminomethyl tetrahydro-isoquinolines and dihydro-isoindoles
摘要:
The synthesis of ten substituted aminomethylene tetrahydro-isoquinolines is described, proceeding in eight steps from 5-hydroxyisoquinoline via reductive amination of N-Boc tetrahydro-isoquinoline 5-carboxaldehyde. Likewise, reductive amination was used to prepare four substituted dihydro-isoindoles from the corresponding aldehyde. The dihydro-isoindole ring system was conveniently accessed via a 2+2+2 cycloaddition reaction. (c) 2006 Elsevier Ltd. All rights reserved.
[EN] KCNT1 INHIBITORS AND METHODS OF USE<br/>[FR] INHIBITEURS DE KCNT1 ET PROCÉDÉS D'UTILISATION
申请人:PRAXIS PREC MEDICINES INC
公开号:WO2020227097A1
公开(公告)日:2020-11-12
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
3- Or 4-monosubstituted phenol derivatives useful as H3 ligands
申请人:Warner-Lambert Company LLC
公开号:EP1593679A1
公开(公告)日:2005-11-09
The invention relates to 3- or 4-monosubstituted phenol derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said 3- or 4-monosubstituted phenol derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
[EN] N-(HETEROCYCLYL AND HETEROCYCLYLALKYL)-3-BENZYLPYRIDIN-2-AMINE DERIVATIVES AS SSTR4 AGONISTS<br/>[FR] DÉRIVÉS DE N-(HÉTÉROCYCLYL ET HÉTÉROCYCLYLALKYL)-3-BENZYLPYRIDIN-2-AMINE SERVANT D'AGONISTES DE SSTR4
申请人:TAKEDA PHARMACEUTICALS CO
公开号:WO2021202775A1
公开(公告)日:2021-10-07
Disclosed are compounds of Formula (1), and pharmaceutically acceptable salts thereof, wherein n, R1, R4, R5, R6, R7, R8, R9, R10, R11, R14, X2, X3 and X12 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 SSTR4.
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators
作者:Anthony B. Pinkerton、Satyamaheshwar Peddibhotla、Fusayo Yamamoto、Lauren M. Slosky、Yushi Bai、Patrick Maloney、Paul Hershberger、Michael P. Hedrick、Bekhi Falter、Robert J. Ardecky、Layton H. Smith、Thomas D. Y. Chung、Michael R. Jackson、Marc G. Caron、Lawrence S. Barak
DOI:10.1021/acs.jmedchem.9b00340
日期:2019.9.12
Neurotensinreceptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensinreceptors have been implicated in a wide variety of CNS disorders, but despite extensive efforts to develop small molecule ligands there are few reports of such compounds. Herein we describe the optimization of a quinazoline based
[EN] AMINOPYRIMIDINE HETEROCYCLIC COMPOUND WITH ADENOSINE RECEPTOR ANTAGONISTIC ACTIVITY<br/>[FR] COMPOSÉ AMINOPYRIMIDINE HÉTÉROCYCLIQUE PRÉSENTANT UNE ACTIVITÉ ANTAGONISTE DU RÉCEPTEUR DE L'ADÉNOSINE
申请人:SUZHOU YUNXUAN YIYAO KEJI YOUXIAN GONGSI
公开号:WO2017088755A1
公开(公告)日:2017-06-01
Disclosed hereinis an aminopyrimidine heterocyclic compound with adenosine receptor antagonistic activity, comprising a compound of the general formula (I), or a pharmaceutically acceptable salt thereof. The aminopyrimidine heterocyclic compound with adenosine receptor antagonistic activitydisclosed herein can be used as an effective adenosine receptor antagonist, and can be used for the treatment or prevention of disorders caused by abnormal level of adenosine.