C07D235/24

COMPOUNDS, COMPOSITIONS AND METHODS OF USE
20200270211 · 2020-08-27 ·

Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.

Imidazolecarboxamides and Their Use as FAAH Inhibitors

A compound having a structure selected from the following:

##STR00001##

or a pharmaceutically acceptable salt thereof. The compound may be used as an inhibitor of fatty acid amide hydrolase.

Imidazolecarboxamides and Their Use as FAAH Inhibitors

A compound having a structure selected from the following:

##STR00001##

or a pharmaceutically acceptable salt thereof. The compound may be used as an inhibitor of fatty acid amide hydrolase.

Benzimidazole derivatives as PI3 kinase inhibitors

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3 OH kinase family (hereinafter PI3 kinases), suitably, PI3K, PI3K, PI3K, and/or PI3K. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K selective benzimidazoles compounds for treating cancer.

Benzimidazole derivatives as PI3 kinase inhibitors

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3 OH kinase family (hereinafter PI3 kinases), suitably, PI3K, PI3K, PI3K, and/or PI3K. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K selective benzimidazoles compounds for treating cancer.

BACTERIAL EFFLUX PUMP INHIBITORS

Disclosed herein are compounds of formula I and salts thereof. Also disclosed are compositions comprising compounds of formula I and methods using compounds of formula I.

##STR00001##

1, 4, 6-TRISUBSTITUTED-2-ALKYL-1H-BENZO[D]IMIDAZOLE DERIVATIVES AS DIHYDROOROTATE OXYGENASE INHIBITORS

The present invention provides 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors, in which R.sub.1 to R.sub.3 and m have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomer thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

##STR00001##

1, 4, 6-TRISUBSTITUTED-2-ALKYL-1H-BENZO[D]IMIDAZOLE DERIVATIVES AS DIHYDROOROTATE OXYGENASE INHIBITORS

The present invention provides 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors, in which R.sub.1 to R.sub.3 and m have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomer thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

##STR00001##

Benzodiazepine derivatives as RSV inhibitors

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: ##STR00001##
which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Imidazolecarboxamides and their use as FAAH inhibitors

A compound having a structure selected from the following: ##STR00001##
or a pharmaceutically acceptable salt thereof. The compound may be used as an inhibitor of fatty acid amide hydrolase.