Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors
摘要:
Soluble epoxide hydrolase (sEH) inhibitors are potential drugs for several diseases. Adamantyl ureas are excellent sEH inhibitors but have limited metabolic stability. Herein, we report the effect of replacing the adamantane group by alternative polycyclic hydrocarbons on sEH inhibition, solubility, permeability and metabolic stability. Compounds bearing smaller or larger polycyclic hydrocarbons than adamantane yielded all good inhibition potency of the human sEH (0.4 <= IC50 <= 21.7 nM), indicating that sEH is able to accommodate inhibitors of very different size. Human liver microsomal stability of diamantane containing inhibitors is lower than that of their corresponding adamantane counterparts.
[EN] PYRIDAZINONE DERIVATIVES AND USE THEREOF AS P2X7 RECEPTOR INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDAZINONE ET LEUR UTILISATION COMME INHIBITEURS DU RÉCEPTEUR P2X7
申请人:NISSAN CHEMICAL IND LTD
公开号:WO2009057827A1
公开(公告)日:2009-05-07
Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.
DI- AND TRI-SUBSTITUTED OXATHIAZINE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF, USE THEREOF AS MEDICINE AND DRUG CONTAINING SAID DERIVATIVES AND USE THEREOF
申请人:Boehme Thomas
公开号:US20130345125A1
公开(公告)日:2013-12-26
The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
该发明涉及式(I)的化合物及其生理兼容盐。所述化合物适用于治疗高血糖,例如。
DI AND TRI - SUBSTITUTED OXATHIAZINE DERIVATIVES, METHOD FOR THE PRODUCTION, METHOD FOR THE PRODUCTION THEREOF, USE THEREOF AS MEDICINE AND DRUG CONTAINING SAID DERIVATIVES AND USE THEREOF
申请人:Boehme Thomas
公开号:US20130338150A1
公开(公告)日:2013-12-19
The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
该发明涉及公式(I)的化合物及其生理兼容盐。这些化合物适用于治疗高血糖,例如。
NOVEL AMIDE AND AMIDINE DERIVATIVES AND USES THEREOF
申请人:Peddi Sridhar
公开号:US20100267738A1
公开(公告)日:2010-10-21
The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.