W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel
W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel
W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel
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drops may be prepared; for vaginal administration they may be prepared as<br />
pessaries, tampons, creams, gels, pastes, foams or spray formulations; for<br />
parenteral administration, aqueous and non-aqueous sterile injectable<br />
solutions or suspensions may be prepared.<br />
In a particularly preferred embodiment, the compounds of the invention are<br />
administered topically, for instance, in the form of ointments, creams,<br />
suspensions, lotions, powders, solutions, pastes, gels, sprays, aerosols or oils.<br />
The present invention will be further better detailed in the following<br />
Experimental Section.<br />
EXPERIMENTAL SECTION<br />
Synthesis- General Information<br />
NMR spectra were recorded at 25°C and 30 °C with Bruker spectrometers.<br />
Chemical shifts 1 H and 13 C NMR spectra are expressed in ppm relative to TMS<br />
or to DSS for spectra recorded in D 2 O. The cyclohexanediol moiety is<br />
numbered as in Fig. 5. Subscripts D refer to the cyclohexanediol (ps-Man)<br />
residue of 7 and 9 and 2 . Mass spectrometry was performed with a<br />
ThermoFisher LCQ apparatus (ESI ionization), or ion-trap ESI Esquire 6000<br />
from Bruker, or an Microflex apparatus (MALDI ionization) from Bruker, or<br />
Apex Il ICR FTMS (ESI ionization - HR-MS). Optical rotations [α] D were<br />
measured in a 1-dm path-length cell with 1 mL capacity on a Perkin-Elmer 241<br />
polarimeter. Thin layer chromatography (TLC) was carried out with precoated<br />
Merck F254 silica gel plates. Unless otherwise specified the TLC were<br />
revealed with molibdic reagent. Flash chromatography (FC) was carried out<br />
with Macherey-Nagel silica gel 60 (230-400 mesh). Final dendritic compounds<br />
were purified by size exclusion chromatography using sephadex LH20 from GE<br />
Healthcare Life Science. Solvents were dried by standard procedures and