C07H15/02

CATECHOLAMINE PRODRUGS FOR USE IN THE TREATMENT OF PARKINSON'S DISEASE

The present invention provides compounds of formula (I) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.

Accordingly, the present invention relates to compounds of formula (Id)

##STR00001##

wherein
R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or
R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or
R1 and R2 are both represented by substituent (i) below; or
R1 and R2 are both represented by substituent (ii) below; or
R1 is substituent (i) and R2 is substituent (ii); or
R1 is substituent (ii) and R2 is substituent (i);

##STR00002##

wherein * indicates the attachment point; and
wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

Tris- or neopentyl glycol-based amphiphiles and uses thereof

The present invention relates to a TRIS- or neopentyl glycol-based amphipathic compound, a method of preparing the same, and a method of extracting, solubilizing, stabilizing, or crystallizing a membrane protein using the same. By using the TRIS- or neopentyl glycol-based compound according to the present invention, a superior membrane protein solubilization effect is exhibited, a membrane protein can be stably stored for a long time in an aqueous solution, and the structural fluidity of the membrane protein can be excellently maintained. Accordingly, the TRIS- or neopentyl glycol-based compound can be utilized in analyzing functions and structures of membrane proteins. Membrane protein structure and function analysis is currently one of the most attractive fields of research in biology and chemistry. Since more than half of the new drugs under development target membrane proteins, the compound can be applied to membrane protein structure research closely related to drug discovery.

METHODS OF PREVENTING OR TREATING ATHEROSCLEROSIS WITH INHIBITORS OF SPECIFIC ISOENZYMES OF HUMAN NEURAMINIDASE
20200239512 · 2020-07-30 ·

The present invention provides a method of preventing or treating atherosclerosis or a symptom thereof comprising administering to a subject in need thereof a specific inhibitor of neuraminidase 1 (neu1); neuraminidase 3 (neu3); or a bispecific inhibitor of neu1 or neu3 of formula I; (I) and a compound of formula I.

##STR00001##

METHODS OF PREVENTING OR TREATING ATHEROSCLEROSIS WITH INHIBITORS OF SPECIFIC ISOENZYMES OF HUMAN NEURAMINIDASE
20200239512 · 2020-07-30 ·

The present invention provides a method of preventing or treating atherosclerosis or a symptom thereof comprising administering to a subject in need thereof a specific inhibitor of neuraminidase 1 (neu1); neuraminidase 3 (neu3); or a bispecific inhibitor of neu1 or neu3 of formula I; (I) and a compound of formula I.

##STR00001##

METHOD FOR PREPARING SURFACTANT COMPOSITIONS COMPRISING ALKYL LIDURONAMIDES D-GLUCURONAMIDES AND L-RHAMNOSIDES FROM ULVANS

The present invention relates to a novel process for preparing surfactant compositions based on alkyl L-iduronamides, alkyl L-rhamnosides and alkyl D-glucuronamides, to the compositions obtained via said process and to the uses thereof.

CATECHOLAMINE PRODRUGS FOR USE IN THE TREATMENT OF PARKINSON’S DISEASE

The present invention provides compounds of formula (I) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.

Accordingly, the present invention relates to compounds of formula (Id)

##STR00001##

wherein R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or R1 and R2 are both represented by substituent (i) below; or R1 and R2 are both represented by substituent (ii) below; or R1 is substituent (i) and R2 is substituent (ii); or R1 is substituent (ii) and R2 is substituent (i);

##STR00002##

wherein * indicates the attachment point; and
wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

CATECHOLAMINE PRODRUGS FOR USE IN THE TREATMENT OF PARKINSON'S DISEASE

The present invention provides compounds of formula (I) that are prodrugs of catecholamine for use in treatment of neurodegenerative diseases and disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating neurodegenerative or neuropsychiatric diseases and disorders using the compounds of the invention, in particular Parkinson's disease.

Accordingly, the present invention relates to compounds of formula (Id)

##STR00001## wherein R1 is H and R2 is selected from one of the substituents (i) and (ii) below; or R1 is selected from one of the substituents (i) and (ii) below and R2 is H; or R1 and R2 are both represented by substituent (i) below; or R1 and R2 are both represented by substituent (ii) below; or R1 is substituent (i) and R2 is substituent (ii); or R1 is substituent (ii) and R2 is substituent (i);

##STR00002## wherein * indicates the attachment point; and wherein the carbon atom at the attachment point on substituent (i) is in the S-configuration; or a pharmaceutically acceptable salt thereof.

A TRIFLUOROMETHYL THIANTHRENIUM COMPOUND, PROCESS FOR PREPARING THE SAME AND THE USE THEREOF

The present inventions refers a novel trifluoromethyl thianthrenium compound referred to as TT-CF.sub.3.sup.+X.sup.?, a process for preparing the same and the use thereof for trifluoromethylating organic compounds.

Vaccines against Streptococcus pneumoniae serotype 4

The present invention relates to synthetic saccharides of general formula (I) that are related to Streptococcus pneumoniae serotype 4 capsular polysaccharide and conjugates thereof. Said conjugate and a pharmaceutical composition containing said conjugate are useful for prevention and/or treatment of diseases associated with Streptococcus pneumoniae, and more specifically of diseases associated with Streptococcus pneumoniae serotype 4. Furthermore, the synthetic saccharides of general formula (I) are useful as marker in immunological assays for detection of antibodies against Streptococcus pneumoniae bacteria.

Vaccines against Streptococcus pneumoniae serotype 4

The present invention relates to synthetic saccharides of general formula (I) that are related to Streptococcus pneumoniae serotype 4 capsular polysaccharide and conjugates thereof. Said conjugate and a pharmaceutical composition containing said conjugate are useful for prevention and/or treatment of diseases associated with Streptococcus pneumoniae, and more specifically of diseases associated with Streptococcus pneumoniae serotype 4. Furthermore, the synthetic saccharides of general formula (I) are useful as marker in immunological assays for detection of antibodies against Streptococcus pneumoniae bacteria.