利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

149 条记录 (耗时 0.039 秒)

    Sydnonimine N-acyl derivatives and method for preparing same
    52.
    发明授权
    Sydnonimine N-acyl derivatives and method for preparing same 失效
    西尼尼因N-酰基衍生物及其制备方法

    公开(公告)号：US4245100A

    公开(公告)日：1981-01-13

    申请号：US855246

    申请日：1977-11-28

    申请人： Leonid E. Kholodov ,  Vladimir G. Yashunsky ,  Roald A. Altshuler ,  Mikhail D. Mashkovsky ,  Valentina V. Ogorodnikova ,  Zoya A. Olovyanishnikova ,  Anna S. Vitvitskaya ,  Valery A. Parshin ,  Ekaterina A. Kelekhsaeva

    发明人： Leonid E. Kholodov ,  Vladimir G. Yashunsky ,  Roald A. Altshuler ,  Mikhail D. Mashkovsky ,  Valentina V. Ogorodnikova ,  Zoya A. Olovyanishnikova ,  Anna S. Vitvitskaya ,  Valery A. Parshin ,  Ekaterina A. Kelekhsaeva

    IPC分类号： C07D271/04 ,  A61K31/42

    CPC分类号： C07D271/04

    摘要： N-acyl sydnonimines of the formula: ##STR1## wherein R is phenyl, .beta.-phenylethyl, dl-.alpha.-methyl-.beta.-phenylethyl or l-.alpha.-methyl-.beta.-phenylethyl; R' is hydrogen, phenyl; X is a lower alkyl, phenyl, ##STR2## wherein R" is hydrogen, a halogen, a lower fluorinated alkyl; R'" is hydrogen, a halogen, a lower alkyl; when R is dl-.alpha.-methyl-.beta.-phenylethyl, R' is H, R" is Cl, R'" is only Cl, while when R' is H, X is NHC.sub.6 H.sub.5 R is only l-.alpha.-methyl-.beta.-phenylethyl; when X is phenyl, R and R' are each phenyl only.The method for preparing sydnonimine N-acylderivatives comprises reacting N-nitrosoderivatives of N-substituted nitriles of .alpha.-aminoacids of the formula: ##STR3## wherein R is phenyl, .beta.-phenylethyl, di-.alpha.-methyl-.beta.-phenylethyl or l-.alpha.-methyl-.beta.-phenylethyl; R' is H, phenyl; when R' is phenyl R is phenyl only, with an acylation agent in a solvent medium in the presence of a basic-character catalyst, followed by isolation of the desired product.

    摘要翻译： 其中R为苯基，β-苯乙基，dl-α-甲基-β-苯乙基或1-α-甲基-β-苯基乙基的N-酰基次磺酰亚胺：其中R为苯基， R'是氢，苯基; X是低级烷基，苯基，其中R“是氢，卤素，低级氟化烷基; R“'是氢，卤素，低级烷基; 当R是dl-α-甲基-β-苯基乙基时，R'是H，R“是Cl，R”'仅为Cl，而当R'是H时，X是NHC 6 H 5 R只是1-α-甲基 β-苯乙基; 当X是苯基时，R和R'各自为苯基。 制备sydnonimine N-酰基衍生物的方法包括使下式的α-氨基酸的N-取代腈的N-亚硝基衍生物：其中R是苯基，β-苯乙基，二 - α-甲基-β-苯乙基或1- α-甲基-β-苯乙基; R'是H，苯基; 当R'是苯基时，R仅为苯基，与酰基化剂在溶剂介质中，在碱性字符催化剂存在下，然后分离所需产物。

    3-Arylthioalkyl-4-optionally substituted sydnones
    53.
    发明授权
    3-Arylthioalkyl-4-optionally substituted sydnones 失效
    3-芳硫基烷基-4-任选取代的钠盐

    公开(公告)号：US3883548A

    公开(公告)日：1975-05-13

    申请号：US34875573

    申请日：1973-04-06

    申请人： SEARLE & CO

    发明人： HILL JOHN B

    IPC分类号： C07D271/04 ,  C07D85/50

    CPC分类号： C07C255/00 ,  C07D271/04

    摘要： WHEREIN R is hydrogen, lower alkyl, phenyl or bromo, Alk is alkylene having more than 1 and fewer than 5 carbon atoms, x is oxygen, thio, sulfinyl or sulfonyl, x is 0 or 1, and Ar is naphthyl, phenyl or substituted phenyl, preferably having an arylthioalkyl substituent, as typified by 3-(2(phenylthio)ethyl)sydnone, are disclosed.

    Preparation and the valuable anti-inflammatory and antibiotic properties of substituted sydnones, represented by the formula

    摘要翻译： 取代的sydnone的制备和有价值的抗炎和抗生素性质，由式WHEREIN R表示为氢，低级烷基，苯基或溴，Alk是具有多于1个且少于5个碳原子的亚烷基，x是氧，硫代， 亚磺酰基或磺酰基，x为0或1，Ar为萘基，苯基或取代的苯基，优选具有芳基硫代烷基取代基，以3- [2-（苯硫基）乙基]钠盐为代表。

    Dye sensitized photoelectric conversion device
    59.
    发明授权
    Dye sensitized photoelectric conversion device 有权

    公开(公告)号：US10170250B2

    公开(公告)日：2019-01-01

    申请号：US15918438

    申请日：2018-03-12

    申请人： King Fahd University of Petroleum and Minerals

    发明人： Umer Mehmood ,  Shakeel Ahmed ,  Ibnelwaleed A. Hussein

    IPC分类号： H01G9/20 ,  C07D413/04 ,  C07D271/10 ,  C07D271/04 ,  C07D271/06 ,  C07D271/08 ,  H01L51/00 ,  C09B23/16 ,  C09B57/00 ,  C09B23/10

    摘要： An oxadiazole dye for use as an organic photosensitizer. The oxadiazole dye comprising donor-π-spacer-acceptor type molecules in which at least one of an oxadiazole group acts as a π-conjugated bridge (spacer), a naphthyl unit acts as an electron-donating unit, a carboxyl group act as an electron acceptor group, and a cyano group acts as an anchor group. An optional thiophene group acts as part of the π-conjugated bridge (spacer). The dye for use as organic photosensitizers in a dye-sensitized solar cell. The dye for use in photodynamic therapies. Computational DFT and time dependent DFT (TD-DFT) modeling techniques showing Light Harvesting Efficiency (LHE), Free Energy for Electron Injection (ΔGinject), Excitation Energies, and Frontier Molecular Orbitals (FMOs) indicate that the series of dye comprise a more negative ΔGinject and a higher LHE value; resulting in a higher incident photon to current efficiency (IPCE).

    PROTEASOME CHYMOTRYPSIN-LIKE INHIBITION USING PI-1833 ANALOGS
    60.
    发明申请
    PROTEASOME CHYMOTRYPSIN-LIKE INHIBITION USING PI-1833 ANALOGS 审中-公开

    公开(公告)号：US20180215742A1

    公开(公告)日：2018-08-02

    申请号：US15882094

    申请日：2018-01-29

    申请人： H. Lee Moffitt Cancer Center and Research Institute, Inc.

    发明人： Harshani R. Lawrence ,  Said M. Sebti ,  Sevil Ozcan

    IPC分类号： C07D413/04 ,  C07D271/04 ,  C07D271/06

    CPC分类号： C07D413/04 ,  C07D271/04 ,  C07D271/06

    摘要： Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e. substitution of one of the hydrogens by methyl) demonstrated chiral discrimination in proteasome CT-L activity inhibition (the S-enantiomer was 35-40 fold more potent than the R-enantiomer).