950772-87-9

Upstream product

• 556-48-9 1,4-Cyclohexanediol 
• 1447817-83-5 4-(prop-2-yn-1-yloxy)cyclohexan-1-ol 
• 950772-86-8 8-(2-propyn-1-yloxy)-1,4-dioxaspiro[4.5]decane 

Downstream Products

• 1467100-94-2 4-((5-(trimethylsilyl)penta-2,4-diyn-1-yl)oxy)cyclohexanone 
• 1467100-92-0 4,4'-[hexa-2,4-diyn-1,6-diylbis(oxy)]dicyclohexanone 

Relevant academic research and scientific papers

Harnessing Hypoxia-Dependent Cyanine Photocages for In Vivo Precision Drug Release

Photocaging holds promise for the precise manipulation of biological events in space and time. However, current near-infrared (NIR) photocages are oxygen-dependent for their photolysis and lack of timely feedback regulation, which has proven to be the major bottleneck for targeted therapy. Herein, we present a hypoxia-dependent photo-activation mechanism of dialkylamine-substituted cyanine (Cy-NH) accompanied by emissive fragments generation, which was validated with retrosynthesis and spectral analysis. For the first time, we have realized the orthogonal manipulation of this hypoxia-dependent photocaging and dual-modal optical signals in living cells and tumor-bearing mice, making a breakthrough in the direct spatiotemporal control and in vivo feedback regulation. This unique photoactivation mechanism overcomes the limitation of hypoxia, which allows site-specific remote control for targeted therapy, and expands the photo-trigger toolbox for on-demand drug release, especially in a physiological context with dual-mode optical imaging under hypoxia.

A 5-hydrocarbyloxy-2-oxo-cyclohexyl amide compound and its preparation method and application

The invention belongs to the technical field of agricultural chemistry, and particularly relates to a 5-oxyl-2-oxocyclohexylsulfonamide compound as well as a preparation method and application thereof. The preparation method comprises the following steps:

Folate-based near-infrared fluorescent theranostic gemcitabine delivery

A series of heptamethine cyanine (1-3) derivatives bearing a carbamate ethyl disulfide group and gemcitabine, an anticancer drug, have been newly synthesized. Their disulfide bonds are readily cleaved by various thiols including glutathione, to result in a subsequent decomposition of the carbamate into amine followed by release of the active gemcitabine, which can be monitored by the fluorescence changes. In the biological experiment, prodrug 1 is preferentially up-taken by folate-positive KB cells over folate-negative A549 cells via receptor-mediated endocytosis to release gemcitabine causing cell death and to emit fluorescence in endoplasmic reticulum. Moreover, it is selectively accumulated in the KB cells which were treated to mice by dorsal subcutaneous injection. This drug delivery system is a new theranostic agent, wherein both therapeutic effect and drug uptake can be easily monitored at the subcellular level, by in vivo and in vitro fluorescence imaging.

New ε-caprolactone diyne monomers aiming for biodegradable polymers

A substitution reaction of cyclohexane-1,4-diol with propargyl bromide gave 4-(prop-2-yn-1-yloxy)cyclohexanol. This compound was oxidized to the corresponding ketone (2-C2H) and then to acetylene γ-substituted ε-caprolactone (3-C2H). The latter compound was chain-extended to two butadiynyl monomers: symmetrical 5,5′-[hexa-2,4- diyne-1,6-diylbis(oxy)]bis(oxepan-2-one) (3-C4-3) and unsymmetrical 5-{[5-(trimethylsilyl)penta-2,4-diyn-1-yl]oxy}oxepan-2-one (3-C4TMS) via Eglinton and Cadiot-Chodkiewicz couplings, respectively. Both compounds were obtained through an alternative Baeyer-Villiger oxidation of immediate ketone precursors 2-C4-2 and 2-C4TMS.

NOVEL COMPOUNDS-300

Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4, m, n, q, s, t, X, and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE

Compounds of formula (I), salts and solvates are provided: formula (I), wherein Q, R and R6 are as defined in the claims. Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.