C07D215/58

Peptidomimetics and methods of using the same

Disclosed herein are compounds useful for modulating the mu-opioid receptor (MOR) and/or delta-opioid receptor (DOR), and methods of using these compounds to treat diseases and conditions, such as pain. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: ##STR00001##
wherein the substituents are as described.

Peptidomimetics and methods of using the same

Disclosed herein are compounds useful for modulating the mu-opioid receptor (MOR) and/or delta-opioid receptor (DOR), and methods of using these compounds to treat diseases and conditions, such as pain. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: ##STR00001##
wherein the substituents are as described.

Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation

In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by NO bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

Benzenesulfonyl-asymmetric ureas and medical uses thereof

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

Benzenesulfonyl-asymmetric ureas and medical uses thereof

Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor.

NEW COMPOUND HAVING FGFR INHIBITORY ACTIVITY AND PREPARATION AND APPLICATION THEREOF
20190367520 · 2019-12-05 ·

A new compound having an FGFR inhibitory activity and preparation and application thereof are provided. In particular, the compound according to the invention has a structure as shown in formula I, in which each group and substituent are as defined in the description. Also, a preparation method for the compound and a use thereof in preparation of a drug for treating and/or preventing a tumor-related disease and/or an FGFR-related disease are provided.

##STR00001##

PROCESS FOR THE PREPARATION OF QUINOLONE BASED COMPOUNDS

The present invention relates to an improved process for the preparation of quinolone based compounds of general formula (I) using intermediate compound of general formula (XII). Invention also provides an improved process for the preparation of compound of formula (I-a) using intermediate compound of formula (XII-a) and some novel impurities generated during process. Compounds prepared using this process can be used to treat anemia.

PROCESS FOR THE PREPARATION OF QUINOLONE BASED COMPOUNDS

The present invention relates to an improved process for the preparation of quinolone based compounds of general formula (I) using intermediate compound of general formula (XII). Invention also provides an improved process for the preparation of compound of formula (I-a) using intermediate compound of formula (XII-a) and some novel impurities generated during process. Compounds prepared using this process can be used to treat anemia.

Compounds and methods for the treatment of microbial infections

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I): ##STR00001##
The present methods include administering to a subject an effective amount of one or more compounds of Formula (I). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE

The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.

##STR00001##