[EN] C-17 AND C-3 MODIFIED TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY<br/>[FR] TRITERPÉNOÏDES MODIFIÉS EN C-17 ET C-3 PRÉSENTANT UNE ACTIVITÉ INHIBITRICE DE LA MATURATION DU VIH
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2012106190A1
公开(公告)日:2012-08-09
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III. These compounds are useful for the treatment of HIV and AIDS.
The present invention is concerned with 2-aminoquinoline derivatives of formula I
where R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, A, and n are as defined in the specification and claims, their use 5-HT
5A
receptor antagonists, their manufacture, and pharmaceutical compositions containing them.
Pharmaceutical compositions comprising at least one compound of the formula (I) and a pharmaceutically acceptable carrier which is useful in a medicine
wherein the symbols and substituents have the following meaning
—X— is e.g.
and Y being e.g.
or the pharmaceutically acceptable salts, esters or amides and prodrugs can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
含有至少一个式(I)的化合物和药用可接受的载体的药物组合物,在药物中有用
其中符号和取代基具有以下含义
—X— 例如
Y 例如
或者药用可接受的盐、酯或酰胺和前药可以被应用来调节由E-、P-或L-选择素结合介导的体外和体内结合过程。
Substituted benzimidazole derivatives as melanocortin 4 receptor antagonists
申请人:Santhera Pharmaceuticals (Schweiz) AG
公开号:EP2439197A1
公开(公告)日:2012-04-11
The present invention relates to substituted benzimidazole derivatives as melanocortin-4 receptor (MC-4R) modulators.
本发明涉及取代苯并咪唑衍生物作为黑色素皮质素-4受体(MC-4R)调节剂。
[EN] HOMOALLYLAMINES AS FORMALDEHYDE-RESPONSIVE TRIGGERS<br/>[FR] HOMOALLYLAMINES EN TANT QUE DÉCLENCHEURS SENSIBLES AU FORMALDÉHYDE
申请人:UNIV CALIFORNIA
公开号:WO2017034927A1
公开(公告)日:2017-03-02
Probes for formaldehyde (FA) including a homoallylamine trigger group attached to a detectable moiety are provided. Aspects of the probes include luminogenic or fluorogenic probes, such as a probe including a quencher in energy-receiving proximity to a fluroophore. Also provided are methods of using the probes for sensitive and bioorthogonal detection of FA in a sample. Aspects of the methods include selectively reacting the probe with the formaldehyde in the sample to a release (e.g., via a 2-aza- Cope rearrangement) a reporter group comprising a detectable moiety. Aspects of the methods detecting formaldehyde in a cell, tissue, organ or fluid in a subject. Also provided are compositions and kits including the subject probes that find use in practicing various embodiments of the subject methods.