[EN] SULFONAMIDE COMPOUNDS HAVING TRPM8 ANTAGONISTIC ACTIVITY<br/>[FR] COMPOSÉS SULFONAMIDES AYANT UNE ACTIVITÉ D'ANTAGONISTE DE TRPM8
申请人:MITSUBISHI TANABE PHARMA CORP
公开号:WO2012124825A1
公开(公告)日:2012-09-20
Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: (I) wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.
The conventional anticholinergic drugs for administration through inhalation have been considered to have the possibility of aggravating dysuria associated with prostatic hyperplasia mediated by blood, and it has been demanded that the conventional anticholinergic drugs for administration through inhalation will have to show reduced side effects or adverse ractions.
The present invention relates to a compound represented by the general formula (I):
(wherein A represents;
and R1, R2, R3 and R1 each a hydrogen atom or a substituent;
R5 is a substituent; X- is an anion;the symbol:
denotes an exo-form or endo-form, or their mixture), its salt or solvation product thereof. They are useful as a prophylactic and/or therapeutic agent with reduced side effects or adverse reactions for the diseases mediated by the muscarinic receptor.
HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME
申请人:EA PHARMA CO., LTD.
公开号:US20160332999A1
公开(公告)日:2016-11-17
The present invention provides a compound represented by the formula (I):
wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
This disclosure relates to compounds of formula (I) shown below: [formula (I)], or a pharmaceutically acceptable salt thereof. These compounds can be used as imaging probes, e.g., for diagnosis of fibrosis or fibrogenesis.
Selective hydrogenation of lignin-derived compounds under mild conditions
作者:Lu Chen、Antoine P. van Muyden、Xinjiang Cui、Gabor Laurenczy、Paul J. Dyson
DOI:10.1039/d0gc00121j
日期:——
processes used in their production. Here, we show that well-defined Rh nanoparticles dispersed in sub-micrometer size carbon hollow spheres, are able to hydrogenate lignin derived products undermildconditions (30 °C, 5 bar H2), in water. The optimum catalyst exhibits excellent selectivity and activity in the conversion of phenol to cyclohexanol and other related substrates including aryl ethers.
木质素衍生化学品生产中的关键挑战是减少其生产中使用的能源密集型过程。在这里,我们显示了分散在亚微米尺寸的碳空心球中的定义明确的Rh纳米粒子能够在温和条件下(30°C,5 bar H 2)在水中氢化木质素衍生产品。最佳催化剂在苯酚向环己醇和其他相关底物(包括芳基醚)的转化中表现出出色的选择性和活性。