C07C229/58

Carboxylic acid ester prodrug inhibitors of MEK

The invention generally relates to compounds having structure I: ##STR00001## wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.

Carboxylic acid ester prodrug inhibitors of MEK

The invention generally relates to compounds having structure I: ##STR00001## wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.

2-(SUBSTITUTED BENZENE MATRIX) AROMATIC FORMATE FTO INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF
20200079727 · 2020-03-12 ·

The invention provides 2-(substituted phenylhetero) aromatic formate FTO inhibitors, a preparation method thereof, and applications thereof. Specifically, disclosed in the present invention are a 2-(substituted phenylhetero) aromatic formate compound represented by the following formula (I), and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, which can be used as an FTO targeting inhibitor for treating diseases associated with FTO targets, including obesity, metabolic syndrome (MS), type 2 diabetes (T2D), Alzheimer's diseases, and cancers such as breast cancers, small-cell lung cancers, human bone marrow rhabdomyosarcoma, pancreatic cancer, malignant glioblastoma and the like.

##STR00001##

2-(SUBSTITUTED BENZENE MATRIX) AROMATIC FORMATE FTO INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF
20200079727 · 2020-03-12 ·

The invention provides 2-(substituted phenylhetero) aromatic formate FTO inhibitors, a preparation method thereof, and applications thereof. Specifically, disclosed in the present invention are a 2-(substituted phenylhetero) aromatic formate compound represented by the following formula (I), and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, which can be used as an FTO targeting inhibitor for treating diseases associated with FTO targets, including obesity, metabolic syndrome (MS), type 2 diabetes (T2D), Alzheimer's diseases, and cancers such as breast cancers, small-cell lung cancers, human bone marrow rhabdomyosarcoma, pancreatic cancer, malignant glioblastoma and the like.

##STR00001##

Small Molecule Inhibitors of PBRM1-BD2

The present disclosure provides novel inhibitors of PBRM1, specifically the 2.sup.nd bromodomain of PBRM1 (PBRM1-BD2), pharmaceutical compositions and methods of use thereof.

Small Molecule Inhibitors of PBRM1-BD2

The present disclosure provides novel inhibitors of PBRM1, specifically the 2.sup.nd bromodomain of PBRM1 (PBRM1-BD2), pharmaceutical compositions and methods of use thereof.

Imidazole derivatives as prodrugs of diclofenac

The present invention relates to a compound of formula (I): ##STR00001## wherein R.sub.1 is R.sub.3IPU and R.sub.2 is the acyloxy residue of diclofenac, and specified by the following structures: ##STR00002## wherein OHR.sub.3IPU is selected from ##STR00003## and R.sub.4 and R.sub.5 may be the same or different selected from H and CH.sub.3 and salts, solvates and hydrates thereof.