C07D211/06

Prodrugs of fumarates and their use in treating various diseases

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. ##STR00001##

Disubstituted piperidines as butyrylcholinesterase inhibitors

This invention relates to new inhibitors of butyrylcholinesterase with general formulas I and II, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of Alzheimer's disease and other forms of dementia. ##STR00001##

Substituted 4-phenylpiperidines, their preparation and use

The present invention provides a compound having the structure: ##STR00001## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each independently H, halogen, CF.sub.3 or C.sub.1-C.sub.4 alkyl, wherein two or more of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 are other than H; R.sub.6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is H, R.sub.2 is CF.sub.3, R.sub.3 is H, R.sub.4 is CF.sub.3, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is H, R.sub.3 is H, R.sub.4 is F, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, then B is other than ##STR00002##
or a pharmaceutically acceptable salt thereof.

AMINO- OR AMMONIUM-CONTAINING SULFONIC ACID, PHOSPHONIC ACID AND CARBOXYLIC ACID DERIVATIVES AND THEIR MEDICAL USE

The present invention relates to amino- or ammonium-containing sulfonic acid, phosphonic acid and carboxylic acid derivatives, in particular the compounds of formula 1, 2, 3, 4, 5 or 6 and their medical use, including their use in treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder.

##STR00001##

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
20180244606 · 2018-08-30 ·

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
20180244606 · 2018-08-30 ·

Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.

Lipids and lipid compositions for the delivery of active agents

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.4, n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. ##STR00001##

Lipids and lipid compositions for the delivery of active agents

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.4, n and p are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. ##STR00001##

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

NOVEL COMPOUND HAVING BLT INHIBITORY ACTIVITY AND COMPOSITION, FOR PREVENTING OR TREATING INFLAMMATORY DISEASES, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.