通过立体保守方法合成了新的(R)-4-benzamido-5-oxopentanoic酸衍生物,并在体外评估了其抑制[125I](BH)-CCK-8与任一大鼠外周血(CCK-A)结合的能力)或中枢(CCK-B)CCK受体,或[3H] pentagastrin与兔胃腺的结合,以及在体内抑制五肽胃泌素在灌注的大鼠胃中输注所诱导的酸分泌。该系列的母体化合物(洛格米特)是CCK-A受体的第一种非肽类,有效和选择性拮抗剂。化学处理洛格鲁胺的结构导致发现CCK-B /胃泌素受体的选择性拮抗剂。讨论了构效关系。其中一些新衍生物与兔胃腺细胞和大鼠皮质膜表现出不同的亲和力,提示胃胃泌素受体(任意称为CCK-B1受体)与先前假设的与CCK中枢受体(称为CCK-B2)的关系不那么紧密。该系列中最有效的化合物,即(R)-4-(3,5-dichlorobenzamido)-5-(8-azaspiro [4.5] d
Pyrazolopyrimidine Derivatives or Pharmaceutically Acceptable Salts Thereof
申请人:UNOKI Gen
公开号:US20090054472A1
公开(公告)日:2009-02-26
A pyrazolopyrimidine derivative represented by formula (1) and pharmaceutically acceptable salt thereof exhibit excellent inhibitory activity against MAPKAP-K2. Accordingly, medicines containing this compound as an active ingredient are expected to be effective for treating diseases mediated by MAPKAP-K2 such as, for example, inflammatory disorder, autoimmune diseases, destructive osteopathy, cancer and/or tumor growth.
The Pyrazolo[1,5-a]pyrimidine derivatives represented by formula I and their pharmaceutically acceptable salts exhibit excellent MAPKAP-K2 inhibiting activity. Drugs comprising the compounds as effective ingredients are therefore expected to be useful as therapeutic or prophylactic agents for MAPKAP-K2 mediated disorder, such as inflammatory disease, autoimmune disease, destructive bone disorder, cancer and/or tumour growth.
式 I 所代表的吡唑并[1,5-a]嘧啶衍生物及其药学上可接受的盐类具有优异的 MAPKAP-K2 抑制活性。 因此,以这些化合物为有效成分的药物有望成为治疗或预防 MAPKAP-K2 介导的疾病(如炎症、自身免疫性疾病、破坏性骨病、癌症和/或肿瘤生长)的药物。
Antioxidant compounds and their use
申请人:University of Pittsburgh—Of the Commonwealth System of Higher Education
公开号:US10858381B2
公开(公告)日:2020-12-08
Disclosed herein are novel amine-functionalized porphyrin compounds, as wells as pharmaceutically acceptable salts or esters thereof. The disclosed compounds can be used to impart antioxidant, anti-inflammatory, anti-microbial, and/or cell-adhesion specificity to a surface or material in need thereof, such as a surface of an indwelling medical implant, or a marine surface.
PROCESS FOR THE PREPARATION OF N-[(3-AMINOOXETAN-3-YL)METHYL]-2-(1,1-DIOXO-3,5-DIHYDRO-1,4-BENZOTHIAZEPIN-4-YL)-6-METHYL-QUINAZOLIN-4-AMINE
申请人:F. Hoffmann-La Roche AG
公开号:EP3097098B1
公开(公告)日:2020-03-04
Rewritable optical information recording medium, recording and reproducing methods, as well as recording and reproducing apparatus
申请人:Tamada Sakuya
公开号:US20060088786A1
公开(公告)日:2006-04-27
A rewritable optical information recording medium including a recording layer composed of an organic dye film is provided, in which recording and erasing information can be performed reversibly by laser light irradiation. A rewritable optical information recording medium including at least one organic dye film which is substantially made of only at least one kind of organic dye compounds as a recording film is provided. The recording and erasure of information are performed by a reversible physical change of the organic dye film substance caused by laser light irradiation. Specifically, data recording is performed by a physical change locally caused by the irradiation of recording laser light, data reproduction is performed by detecting change in intensity of returned light of reproducing laser light having less power than the recording laser light, and data erasure is performed by applying at least once continuous light or pulse light having laser power more than the reproducing laser light and less than the recording laser light. The physical change is a change in shape.