C07D205/085

Carbamate derivatives of lactam based N-acylethanolamine acid amidase (NAAA) inhibitors

Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

Carbamate derivatives of lactam based N-acylethanolamine acid amidase (NAAA) inhibitors

Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.

Ethynylbenzene derivatives
09738604 · 2017-08-22 · ·

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##

Ethynylbenzene derivatives
09738604 · 2017-08-22 · ·

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##

Azetidinimines as carbapenemases inhibitors

The present application relates to novel azetidinimine of formula (I). Wherein R.sub.1-R.sub.6 are as defined in claim 1. The azetidinimine of the invention are useful as antibiotics and as inhibitors of a carbapenemases. The present invention thus further relates to their use in antibiotic therapies and their methods of synthesis. ##STR00001##

Azetidinimines as carbapenemases inhibitors

The present application relates to novel azetidinimine of formula (I). Wherein R.sub.1-R.sub.6 are as defined in claim 1. The azetidinimine of the invention are useful as antibiotics and as inhibitors of a carbapenemases. The present invention thus further relates to their use in antibiotic therapies and their methods of synthesis. ##STR00001##

Diaryl-B-Lactam Compound and Preparation Method and Pharmaceutical Use Thereof

The present invention relates to the field of synthetic medicinal chemistry and provides a series of novel diaryl-β-lactam compounds having significant anti-tumor activity, and the pharmaceutical use thereof. The present invention also comprises the use of these compounds, pharmaceutical salts, and pharmaceutical composition thereof for preparing a pharmaceutical for the prevention or treatment of tumor-associated disease. The diaryl-β-lactam compounds of the present invention have the following general formula (I).

##STR00001##

Diaryl-B-Lactam Compound and Preparation Method and Pharmaceutical Use Thereof

The present invention relates to the field of synthetic medicinal chemistry and provides a series of novel diaryl--lactam compounds having significant anti-tumor activity, and the pharmaceutical use thereof. The present invention also comprises the use of these compounds, pharmaceutical salts, and pharmaceutical composition thereof for preparing a pharmaceutical for the prevention or treatment of tumor-associated disease. The diaryl--lactam compounds of the present invention have the following general formula (I).

##STR00001##

Ethynylbenzene derivatives
10597361 · 2020-03-24 · ·

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##

Ethynylbenzene derivatives
10597361 · 2020-03-24 · ·

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##