C07C237/36

NOVEL ANTHRANILIC AMIDES AND THE USE THEREOF

Disclosed are anthranilic amide derivatives having the formula:

##STR00001##

Compositions are disclosed that include the anthranilic amide derivatives and the use of the anthranilic amide derivatives for the manufacture of a medicament. Further disclosed are methods of inhibiting or treating cancer, inhibiting or reversing an epithelial to mesenchymal cellular transition, and/or inhibiting MEK1/2 and/or MEK 5 enzymatic activity in a subject by administering to the subject an effective amount of a disclosed anthranilic amide derivative.

NOVEL ANTHRANILIC AMIDES AND THE USE THEREOF

Disclosed are anthranilic amide derivatives having the formula:

##STR00001##

Compositions are disclosed that include the anthranilic amide derivatives and the use of the anthranilic amide derivatives for the manufacture of a medicament. Further disclosed are methods of inhibiting or treating cancer, inhibiting or reversing an epithelial to mesenchymal cellular transition, and/or inhibiting MEK1/2 and/or MEK 5 enzymatic activity in a subject by administering to the subject an effective amount of a disclosed anthranilic amide derivative.

Anthranilic amides and the use thereof

Disclosed are anthranilic amide derivatives having the formula. Compositions are disclosed that include the anthranilic amide derivatives and the use of the anthranilic amide derivatives for the manufacture of a medicament. Further disclosed are methods of inhibiting or treating cancer, inhibiting or reversing an epithelial to mesenchymal cellular transition, and/or inhibiting MEK1/2 and/or MEK 5 enzymatic activity in a subject by administering to the subject an effective amount of a disclosed anthranilic amide derivative. ##STR00001##

Anthranilic amides and the use thereof

Disclosed are anthranilic amide derivatives having the formula. Compositions are disclosed that include the anthranilic amide derivatives and the use of the anthranilic amide derivatives for the manufacture of a medicament. Further disclosed are methods of inhibiting or treating cancer, inhibiting or reversing an epithelial to mesenchymal cellular transition, and/or inhibiting MEK1/2 and/or MEK 5 enzymatic activity in a subject by administering to the subject an effective amount of a disclosed anthranilic amide derivative. ##STR00001##

Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof

The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof

The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.

COVALENT INHIBITORS OF EQUINE ENCEPHALITIS VIRUS

Embodiments and methods for a new class of potent non-peptidic covalent inhibitors of nsP2 cysteine protease that inhibit Venezuelan equine encephalitis virus's (VEEV) replication in neuroblasts are disclosed. More particularly, an acrylate and vinyl sulfone-based chemical series were investigated as promising starting scaffolds against VEEV and as inhibitors of the cysteine protease domain of VEEV's non-structural protein 2 (nsP2). The invention discloses compounds of Formula I and analogues for treatment of VEEV.

COVALENT INHIBITORS OF EQUINE ENCEPHALITIS VIRUS

Embodiments and methods for a new class of potent non-peptidic covalent inhibitors of nsP2 cysteine protease that inhibit Venezuelan equine encephalitis virus's (VEEV) replication in neuroblasts are disclosed. More particularly, an acrylate and vinyl sulfone-based chemical series were investigated as promising starting scaffolds against VEEV and as inhibitors of the cysteine protease domain of VEEV's non-structural protein 2 (nsP2). The invention discloses compounds of Formula I and analogues for treatment of VEEV.

Benzoylglycine derivatives and methods of making and using same

Disclosed are compounds of formulae: and pharmaceutically acceptable salts thereof, wherein the variables, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds. ##STR00001##

Amide derivative

An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect, and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. Provided is a pharmaceutical composition containing, as an active ingredient, a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula (I), R.sup.1 and R.sup.2 are the same or different, and represent a C.sub.1-C.sub.6 alkyl group, a halogeno C.sub.1-C.sub.6 alkyl group or a C.sub.3-C.sub.6 cycloalkyl group; n represents 0, 1 or 2; each X represents a C.sub.1-C.sub.6 alkyl group, a C.sub.3-C.sub.6 cycloalkyl group, a halogen atom or the like; and Y represents a hydrogen atom, a C.sub.1-C.sub.6 alkoxy group, a C.sub.3-C.sub.6 cycloalkoxy group or a halogeno C.sub.1-C.sub.6 alkoxy group.