C07D211/52

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.

Amido compounds and their use as pharmaceuticals

The present invention relates to inhibitors of 11- hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11- hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Amido compounds and their use as pharmaceuticals

The present invention relates to inhibitors of 11- hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11- hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Small molecule compound and synthesizing method and uses thereof

Provided is a small molecule compound as represented by structural formula (I). The product of the present invention in various concentrations and dosages can achieve an obvious change in the growth period of hairs, promoting the growth of the hairs, thus exhibiting an obvious effect of promoting hair growth. In addition, changes in the weight of a mouse in each group are slow, indicating that the test compound does not cause weight loss in an animal.

Small molecule compound and synthesizing method and uses thereof

Provided is a small molecule compound as represented by structural formula (I). The product of the present invention in various concentrations and dosages can achieve an obvious change in the growth period of hairs, promoting the growth of the hairs, thus exhibiting an obvious effect of promoting hair growth. In addition, changes in the weight of a mouse in each group are slow, indicating that the test compound does not cause weight loss in an animal.

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 for selective histone deacetylase inhibitors, and pharmaceutical composition comprising the same

Provided are urea derivatives of Formula I: ##STR00001##
with histone deacetylase (HDAC) inhibitory activity, optical isomers thereof, pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising the same. The provided urea derivatives of Formula I are selective histone deacetylase (HDAC) inhibitors and are effective for the treatment of histone deacetylase-mediated diseases such as malignant tumors, inflammatory diseases, rheumatoid arthritis, and neurodegeneration.

Compounds for selective histone deacetylase inhibitors, and pharmaceutical composition comprising the same

Provided are urea derivatives of Formula I: ##STR00001##
with histone deacetylase (HDAC) inhibitory activity, optical isomers thereof, pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising the same. The provided urea derivatives of Formula I are selective histone deacetylase (HDAC) inhibitors and are effective for the treatment of histone deacetylase-mediated diseases such as malignant tumors, inflammatory diseases, rheumatoid arthritis, and neurodegeneration.

Substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides and methods of making and using same

The invention relates to certain substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof.