Patent classifications
C07H9/06
Selective glycosidase inhibitors and uses thereof
The invention provides compounds of formula (I) with substituents as specified in claim 1 for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceuticals compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to over-expression of O-GlcNAcase or accumulation of O-GlcNac. ##STR00001##
Selective glycosidase inhibitors and uses thereof
The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
Selective glycosidase inhibitors and uses thereof
The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
SYNTHESIS OF 6-AZIDO-6-DEOXY-2-N-ACETYL-HEXOSAMINE-NUCLEOSIDE DIPHOSPHATE
The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.
Glucosamine derivatives for the prevention or treatment of joint disorders
There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis. ##STR00001##
HEXOSE DERIVATIVES, PREPARATION AND USES THEREOF
A compound of formula I:
##STR00001##
or a salt thereof, wherein: R.sup.1 is —OC (H) (X) (CH.sub.2).sub.nC(═O)OH; R.sup.2 is —OH, —N.sub.3, or —N(H)C(═O)CH.sub.3; or R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached form R.sup.3 is —H, —CH.sub.3, —CH.sub.2C(═O)OH, or —CH.sub.2OH; X is —H, —CH.sub.3, —CH.sub.2OH, or CH.sub.2C(═O)OH; and n is 0 or 1.
HEXOSE DERIVATIVES, PREPARATION AND USES THEREOF
A compound of formula I:
##STR00001##
or a salt thereof, wherein: R.sup.1 is —OC (H) (X) (CH.sub.2).sub.nC(═O)OH; R.sup.2 is —OH, —N.sub.3, or —N(H)C(═O)CH.sub.3; or R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached form R.sup.3 is —H, —CH.sub.3, —CH.sub.2C(═O)OH, or —CH.sub.2OH; X is —H, —CH.sub.3, —CH.sub.2OH, or CH.sub.2C(═O)OH; and n is 0 or 1.
GLUCOSAMINE DERIVATIVES FOR THE PREVENTION OR TREATMENT OF JOINT DISORDERS
There are provided compounds of Formula (A) and pharmaceutically acceptable salts and esters thereof, and pharmaceutical compositions thereof, used for the prevention or treatment in a mammal of joint and bone disorders such as arthritis and osteoporosis.
##STR00001##
Process for making chloro-substituted nucleoside phosphoramidate compounds
The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): ##STR00001##
which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).
Process for making chloro-substituted nucleoside phosphoramidate compounds
The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): ##STR00001##
which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).