1,3-Diaminopropan-2-ol Sulfonamides as potent and selective inhibitors of the glycine transporter type 1
摘要:
High throughput screening led to the discovery of a novel series of 1,3-diaminopropan-2-ol sulfonarnides as selective GlyT-1 inhibitors. Structure-activity relationships of this novel series and optimisation of the initial hit that led to the identification of (2), a potent and selective GlyT-1 inhibitor, are also presented. (c) 2007 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2006.12.063
作为产物:
描述:
(R)-1-azido-3-pyrrolidin-1-yl-propan-2-ol 在
catalyst 作用下,
以
甲醇 为溶剂,
反应 16.0h,
以to yield the title compound as a clear colourless oil (130 mg; 91%)的产率得到(S)-1-amino-3-pyrrolidin-1-ylpropan-2-ol
参考文献:
名称:
Gly1 transporter inhibitors and uses thereof in treatment of neurological and neuropsychiatric disorders
[EN] GLYT1 TRANSPORTER INHIBITORS<br/>[FR] INHIBITEURS DU TRANSPORTEUR GLYT1
申请人:GLAXO GROUP LTD
公开号:WO2005049023A1
公开(公告)日:2005-06-02
The invention provides a compound of formula (I): or a salt, solvate or a physiologically functional derivative thereof, wherein R1 to R10 are as defined in the specification and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
Gly1 transporter inhibitors and uses thereof in treatment of neurological and neuropsychiatric disorders
申请人:Bloomfield Jonathon Nic
公开号:US20050267152A1
公开(公告)日:2005-12-01
The present invention relates to glycine transporter inhibiting compounds of formula (I):
for treating disorders mediated by GlyT1, wherein R
1
—R
9
are as in the description.
本发明涉及公式(I)的甘氨酸转运抑制化合物,用于治疗由GlyT1介导的疾病,其中R1-R9如描述。
GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
申请人:SMITHKLINE BEECHAM PLC
公开号:EP1455777A1
公开(公告)日:2004-09-15
HtrA Inhibitors and CagA Inhibitors and Use Thereof
申请人:PSOMAGEN INC.
公开号:US20220122691A1
公开(公告)日:2022-04-21
The present application relates to new HtrA inhibitors and use thereof. Additionally, the present application also relates to new peptides for inhibiting CagA and use thereof.
[EN] GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS<br/>[FR] INHIBITEURS DE TRANSPORTEURS GLYT1 ET UTILISATONS DE CEUX-CI DANS LE TRAITEMENT DE TROUBLES NEUROLOGIQUES ET NEUROPSYCHIATRIQUES
申请人:SMITHKLINE BEECHAM PLC
公开号:WO2003055478A1
公开(公告)日:2003-07-10
The present invention relates to glycine transporter inhibiting compounds of formula (I): for the manufacture of a medicament for treating disorders mediated GlyT1, wherein R1-R9 are as in the description.