C07D471/08

Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.

Macrocyclic immunomodulators

Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): ##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

3,9-diazaspiro[5,5]undecane compound as FLT3 and AXL inhibitors

Disclosed in the present invention is a novel compound as FLT3 and AXL inhibitors. Specifically, disclosed are a compound represented by formula (I) and a pharmacologically acceptable salt thereof. (I) ##STR00001##

SMALL MOLECULE INHIBITORS TARGETING CLOSTRIDIOIDES DIFFICILE SPORULATION

Disclosed herein are compounds that can prevent and treat C. difficile by inhibiting sporulation. Also disclosed herein are compositions and formulations comprising the compound disclosed herein. Methods of preventing and treating C. difficile comprising administering the compounds described herein are also disclosed.

SMALL MOLECULE INHIBITORS TARGETING CLOSTRIDIOIDES DIFFICILE SPORULATION

Disclosed herein are compounds that can prevent and treat C. difficile by inhibiting sporulation. Also disclosed herein are compositions and formulations comprising the compound disclosed herein. Methods of preventing and treating C. difficile comprising administering the compounds described herein are also disclosed.

Substituted imidazolidin-2-one derivatives as PRMT5 inhibitors

The present invention relates to substituted imidazolidin-2-one derivatives of formula (I) or pharmaceutically acceptable salts thereof. The present invention further provides the methods of preparation of compound of formula (I) and utility as PRMT5 inhibitors. The compounds are useful as medicaments in the treatment of conditions and disorders mediated by PRMT5, such as cancer, metabolic disorders, inflammation, autoimmune disease and hemoglobinopathies.

Substituted imidazolidin-2-one derivatives as PRMT5 inhibitors

The present invention relates to substituted imidazolidin-2-one derivatives of formula (I) or pharmaceutically acceptable salts thereof. The present invention further provides the methods of preparation of compound of formula (I) and utility as PRMT5 inhibitors. The compounds are useful as medicaments in the treatment of conditions and disorders mediated by PRMT5, such as cancer, metabolic disorders, inflammation, autoimmune disease and hemoglobinopathies.

POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
20220411442 · 2022-12-29 ·

The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

POLYCYCLIC AMINES AS OPIOID RECEPTOR MODULATORS
20220411442 · 2022-12-29 ·

The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.

Apelin receptor (APJ) agonists and uses thereof

This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.