Patent classifications
C07H5/04
POSACONAZOLE DERIVATIVE, PHARMACEUTICAL COMPOSITION AND USE THEREOF
The present disclosure provides a posaconazole derivative, a pharmaceutical composition and use thereof, which specifically include a compound represented by the following formula (I), a racemate, stereoisomer, tautomer, oxynitride, or a pharmaceutically acceptable salt thereof:
##STR00001##
The compounds of the present disclosure have strong antifungal activity, high safety, and good water solubility, without the need for the addition of a cosolvent (such as hydroxypropyl--cyclodextrin, sulfobutyl ether--cyclodextrin, and the like) with potential safety risks. Furthermore, the formulation process of the compound could have less difficulty and less cost, and therefore can be used to prepare improved antifungal drugs.
Heparan sulfate synthesis
The invention provides an efficient modular chemical synthesis for heparan sulfate oligosaccharides based on orthogonal protection strategies. Modular disaccharide building blocks, themselves the product of a novel combinatorial synthesis, are combined in numerous ways to produce a range of oligosaccharides.
Heparan sulfate synthesis
The invention provides an efficient modular chemical synthesis for heparan sulfate oligosaccharides based on orthogonal protection strategies. Modular disaccharide building blocks, themselves the product of a novel combinatorial synthesis, are combined in numerous ways to produce a range of oligosaccharides.
NEW 5-AZIDO-5-DEOXY-2 :3-ISOPROPYLIDENE-D-ARABINOSE COMPOUNDS; THEIR METHOD OF MANUFACTURE AND THEIR USE FOR THE SYNTHESIS OF ARA-N3, KDO-N3 AND 4EKDO-N3
Disclosed are new compounds of formulae:
##STR00001##
Wherein: R.sup.1 and R.sup.2 can be independently H; a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, butyl; aryl including phenyl, para-methoxyphenyl; or R.sup.1,R.sup.2 together with the carbon C-6 can be a cyclopentylidene or cyclohexylidene; each of these groups being substituted or not; and R.sup.3 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl; or aryl including phenyl, methylphenyl, ethylphenyl, each of these groups being substituted or not. The invention also relates to their method of manufacture and their use for the synthesis of Ara-N.sub.3, Kdo-N.sub.3 and 4eKdo-N.sub.3.
NEW 5-AZIDO-5-DEOXY-2 :3-ISOPROPYLIDENE-D-ARABINOSE COMPOUNDS; THEIR METHOD OF MANUFACTURE AND THEIR USE FOR THE SYNTHESIS OF ARA-N3, KDO-N3 AND 4EKDO-N3
Disclosed are new compounds of formulae:
##STR00001##
Wherein: R.sup.1 and R.sup.2 can be independently H; a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, butyl; aryl including phenyl, para-methoxyphenyl; or R.sup.1,R.sup.2 together with the carbon C-6 can be a cyclopentylidene or cyclohexylidene; each of these groups being substituted or not; and R.sup.3 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl; or aryl including phenyl, methylphenyl, ethylphenyl, each of these groups being substituted or not. The invention also relates to their method of manufacture and their use for the synthesis of Ara-N.sub.3, Kdo-N.sub.3 and 4eKdo-N.sub.3.
Method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose
Disclosed is a method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-
##STR00001##
Wherein: R.sup.1 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl; aryl including phenyl; each of these groups being substituted or not; and R.sup.2 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl, tert-butyl, isobutyl; each of these groups being substituted or not; with a deprotecting reagent including a Lewis or Brnsted acid in a polar aprotic solvent, thereby obtaining a free C-1 OH group. The method can also start with the preparation from commercially available
Method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-D-mannose
Disclosed is a method of preparation of 6-azido-2,4-diacetamido-2,4,6-trideoxy-
##STR00001##
Wherein: R.sup.1 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl; aryl including phenyl; each of these groups being substituted or not; and R.sup.2 can be a C.sub.1 to C.sub.6 alkyl including methyl, ethyl, isopropyl, tert-butyl, isobutyl; each of these groups being substituted or not; with a deprotecting reagent including a Lewis or Brnsted acid in a polar aprotic solvent, thereby obtaining a free C-1 OH group. The method can also start with the preparation from commercially available
BINDERS AND MATERIALS MADE THEREWITH
A curable aqueous composition is disclosed comprising a carbohydrate, a crosslinking agent, and an amine base, wherein the curable aqueous composition has a pH adjusted by the amine base. Further disclosed is a method of forming a curable aqueous solution.
BINDERS AND MATERIALS MADE THEREWITH
A curable aqueous composition is disclosed comprising a carbohydrate, a crosslinking agent, and an amine base, wherein the curable aqueous composition has a pH adjusted by the amine base. Further disclosed is a method of forming a curable aqueous solution.
Binders and associated products
The present invention relates to a water-soluble pre-reacted binder composition, a method of its manufacture, a use of said pre-reacted binder composition, a method of manufacturing a collection of matter bound by a polymeric binder, a binder solution or dispersion comprising said pre-reacted binder composition, as well as products comprising the pre-reacted binder composition in a cured state.