C07D211/52

SMALL MOLECULE MODULATORS OF GLUCOCEREBROSIDASE ACTIVITY AND USES THEREOF
20240262832 · 2024-08-08 · ·

Provided herein are compounds that modulate glucocerebrosidase (GCase), an enzyme whose activity is associated with neurological diseases and disorders (e.g., Gaucher's disease. Parkinson's disease). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating GCase-related diseases and disorders (e.g., Gaucher's disease. Parkinson's disease) with the compounds in a subject, by administering the compounds and/or compositions described herein.

SMALL MOLECULE MODULATORS OF GLUCOCEREBROSIDASE ACTIVITY AND USES THEREOF
20240262832 · 2024-08-08 · ·

Provided herein are compounds that modulate glucocerebrosidase (GCase), an enzyme whose activity is associated with neurological diseases and disorders (e.g., Gaucher's disease. Parkinson's disease). Also provided are pharmaceutical compositions and kits comprising the compounds, and methods of treating GCase-related diseases and disorders (e.g., Gaucher's disease. Parkinson's disease) with the compounds in a subject, by administering the compounds and/or compositions described herein.

Analogs of pridopidine, their preparation and use

This invention provides an isolated compound having the structure: ##STR00001##
or a salt thereof. The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1-propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine 1-oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridne, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.

Analogs of pridopidine, their preparation and use

This invention provides an isolated compound having the structure: ##STR00001##
or a salt thereof. The invention also provides for a process for preparing 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-4-ol, 1-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3-(methylsulfonyl) phenyl)piperidone, 1,4-bis((3-(1-propylpiperidin-4-yl)phenyl)sulfonyl)butane, (3R,4S)-4-(3-(methylsulfonyl)phenyl)-1-propylpiperidin-3-ol, 4-(3-(methylsulfonyl)phenyl)-1-propylpiperidine 1-oxide, 1-(2-methylpentyl)-4-(3-(methylsulfonyl)phenyl)piperidine, 4-(3-(methylsulfinyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridne, and 4-(3-(methylsulfonyl)phenyl)-1-propyl-1,2,3,6-tetrahydropyridine. This invention also provides an impurity or a salt thereof for use, as a reference standard to detect trace amounts of the impurity in a pharmaceutical composition comprising pridopidine or a pharmaceutically acceptable salt thereof. This invention further provides a process for producing a pridopidine drug product comprising obtaining a pridopidine drug substance and mixing the pridopidine drug substance with suitable excipients so as to produce the pridopidine drug product. This invention also provides a process for producing a pridopidine drug product. This invention also provides a process of distributing a pridopidine drug product.

Phenyl derivative

The compound of the formula (I-1): ##STR00001##
wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P.sub.2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P.sub.2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

Phenyl derivative

The compound of the formula (I-1): ##STR00001##
wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P.sub.2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P.sub.2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory diseases.

COMPOUNDS AND USES THEREOF IN THE TREATMENT OF CANCERS AND OTHER MEDICAL CONDITIONS
20180208586 · 2018-07-26 ·

There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders.

##STR00001##

COMPOUNDS AND USES THEREOF IN THE TREATMENT OF CANCERS AND OTHER MEDICAL CONDITIONS
20180208586 · 2018-07-26 ·

There are provided compounds, their preparation and their use in the treatment of medical conditions including cancers and immune disorders.

##STR00001##

Method for the preparation of 1-(2-halogen-ethyl)-4 piperidine-carboxylic acid ethyl esters

The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.

EIS INHIBITORS
20180162867 · 2018-06-14 ·

Compounds and compositions are disclosed, which are useful as inhibitors of acetyltransferase Eis, a mediator of kanamycin resistance in Mycobacterium tuberculosis.