C07H15/20

Synthetic glucopyranosyl lipid adjuvants

Compounds, particularly, glucopyranosyl lipid adjuvant (GLA) compounds, having the following structure (I) are provided: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein L.sub.1. L.sub.2, L.sub.3, L.sub.4, L.sub.5, L.sub.6, L.sub.7, L.sub.8, L.sub.9, L.sub.10, Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, are as defined herein. Pharmaceutical compositions, vaccine compositions, and related methods for inducing or enhancing immune responses, are also provided.

Total synthesis of shishijimicin A and analogs thereof

In one aspect, the present disclosure provides shishijimicin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, antibody drug conjugates of the compounds are also provided.

Total synthesis of shishijimicin A and analogs thereof

In one aspect, the present disclosure provides shishijimicin analogs of the formula: wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, antibody drug conjugates of the compounds are also provided.

Steviol glycosides, their compositions and their purification

The present invention relates generally to steviol glycosides, as well as compositions comprising such steviol glycosides. The present invention further extends to methods of preparing and purifying such steviol glycosides and methods for enhancing the flavor or sweetness of consumables using these steviol glycosides and compositions. The present invention extends to consumables comprising steviol glycosides, where the such steviol glycosides are present in a concentration at or below their sweetness recognition threshold, and wherein such steviol glycosides enhance the sweetness of the consumable.

Steviol glycosides, their compositions and their purification

The present invention relates generally to steviol glycosides, as well as compositions comprising such steviol glycosides. The present invention further extends to methods of preparing and purifying such steviol glycosides and methods for enhancing the flavor or sweetness of consumables using these steviol glycosides and compositions. The present invention extends to consumables comprising steviol glycosides, where the such steviol glycosides are present in a concentration at or below their sweetness recognition threshold, and wherein such steviol glycosides enhance the sweetness of the consumable.

FLUOROGENIC GLYCOSIDASE SUBSTRATE AND ASSOCIATED DETECTION METHOD

The invention relates to novel glycosidase substrates of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R9, V, X, Y and Z are as defined in claim 1, and a method for detecting the presence of a catalytically active glycosidase by means of one of said substrates.

##STR00001##

Vaccine against <i>Klebsiella pneumoniae</i>

The present invention relates to a synthetic oligosaccharide of general formula (I): T*-[(U.sub.x+4U.sub.x+3U.sub.x+2U.sub.x+1U.sub.x).sub.m(V.sub.x+2V.sub.x+1V.sub.x).sub.1-m-T-O-L-E that is related to Klebsiella pneumoniae serotype O3, O3b and/or O5 lipopolysaccharide and conjugate thereof. Said synthetic oligosaccharide, said conjugate and pharmaceutical composition containing said synthetic oligosaccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Klebsiella pneumoniae. Furthermore, the synthetic oligosaccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Klebsiella pneumoniae serotype O3, O3b and/or O5 bacteria.

Vaccine against <i>Klebsiella pneumoniae</i>

The present invention relates to a synthetic oligosaccharide of general formula (I): T*-[(U.sub.x+4U.sub.x+3U.sub.x+2U.sub.x+1U.sub.x).sub.m(V.sub.x+2V.sub.x+1V.sub.x).sub.1-m-T-O-L-E that is related to Klebsiella pneumoniae serotype O3, O3b and/or O5 lipopolysaccharide and conjugate thereof. Said synthetic oligosaccharide, said conjugate and pharmaceutical composition containing said synthetic oligosaccharide or said conjugate are useful for prevention and/or treatment of diseases associated with Klebsiella pneumoniae. Furthermore, the synthetic oligosaccharide of general formula (I) is useful as marker in immunological assays for detection of antibodies against Klebsiella pneumoniae serotype O3, O3b and/or O5 bacteria.

Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.