C07D455/02

Substituted quinolizine derivatives useful as HIV integrase inhibitors

The present invention relates to Substituted Quinolizine Derivatives of Formula (I): ##STR00001##
and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.9 and R.sup.10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.

Heterocyclic compound

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the description, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

Heterocyclic compound

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): ##STR00001##
wherein each symbol is as described in the description, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

METHIONINE ADENOSYLTRANSFERASE 2A INHIBITOR

The present invention provides a methionine adenosyltransferase 2A inhibitor. The structure of the methionine adenosyltransferase 2A inhibitor is as represented by general formula (I), and the definitions of substituents are as described in the specification. The present invention further provides a preparation method therefor. A compound represented by formula I provided by the present invention has significant methionine adenosyltransferase 2A inhibitory activity, and can be used in the treatment of diseases mediated by overexpression of methionine adenosyltransferase 2A.

##STR00001##

METHIONINE ADENOSYLTRANSFERASE 2A INHIBITOR

The present invention provides a methionine adenosyltransferase 2A inhibitor. The structure of the methionine adenosyltransferase 2A inhibitor is as represented by general formula (I), and the definitions of substituents are as described in the specification. The present invention further provides a preparation method therefor. A compound represented by formula I provided by the present invention has significant methionine adenosyltransferase 2A inhibitory activity, and can be used in the treatment of diseases mediated by overexpression of methionine adenosyltransferase 2A.

##STR00001##

2-PYRIDONE ANTIMICROBIAL COMPOSITIONS

Disclosed herein are compounds of Formula I

##STR00001## wherein R.sup.1, R.sup.2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.

2-PYRIDONE ANTIMICROBIAL COMPOSITIONS

Disclosed herein are compounds of Formula I

##STR00001## wherein R.sup.1, R.sup.2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.

1,4-disubstituted 1,2,3-triazoles, methods for preparing same, and diagnostic and therapeutic uses thereof

A compound having the following general formula (I): ##STR00001##
wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.

1,4-disubstituted 1,2,3-triazoles, methods for preparing same, and diagnostic and therapeutic uses thereof

A compound having the following general formula (I): ##STR00001##
wherein: X is a nitrogen atom and Y is a carbon atom; or X is a carbon atom and Y is a nitrogen atom; the Ar group is an aryl or heteroaryl group; and the RN and RN groups, together with the carbon atoms to which they are bound, form a monocyclic or bicyclic azacycloalkane group. The pharmaceutically acceptable salts thereof, the hydrates or polymorphic crystalline structures thereof, and to the racemates, diastereoisomers, or enantiomers thereof are also described.

ISOQUINOLIN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF

Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.