C07D451/02

Inhibitors of LRRK2 kinase

Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.

METHODS FOR INHIBITING CONVERSION OF CHOLINE TO TRIMETHYLAMINE (TMA)

A method of inhibiting the conversion of choline to trimethylamine (TMA) and lowering TMAO by providing a composition comprising a compound set forth in Formula (I):

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Pyridazinones as PARP7 inhibitors

The present invention relates to pyridazinones and related compounds which are inhibitors of PARP7 and are useful in the treatment of cancer.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT FACTOR D MEDICAL DISORDERS

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.

PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT FACTOR D MEDICAL DISORDERS

Compounds, methods of use, and processes for making inhibitors of complement factor D or a pharmaceutically acceptable salt or composition thereof are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade. The inhibitors of factor D described herein reduce the excessive activation of complement.

ARYL HETEROCYCLIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS

A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

##STR00001##

ARYL HETEROCYCLIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS

A compound of Formula (I), or a pharmaceutically-acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

##STR00001##

ISOQUINOLINONE DERIVATIVES, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING POLY(ADP-RIBOSE) POLYMERASE-1-RELATED DISEASES, COMPRISING THE SAME AS ACTIVE INGREDIENT

The present invention relates to isoquinolinone derivatives, a method for preparing the same, and a pharmaceutical composition for preventing or treating poly(ADP-ribose) polymerase-1 (PARP-1)-related diseases containing the same as an active ingredient. The isoquinolinone derivatives exhibit an excellent PARP-1 inhibitory effect at a concentration of nanomolar units, and further exhibit an excellent cytoprotective effect (apoptosis inhibitory effect) on ophthalmic diseases or disorders, specifically retinal disorders, and thus can be effectively used as a pharmaceutical composition for preventing or treating PARP-1-related diseases, for example, ophthalmic diseases or disorders, which contains the same as an active ingredient.

ISOQUINOLINONE DERIVATIVES, METHOD FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING POLY(ADP-RIBOSE) POLYMERASE-1-RELATED DISEASES, COMPRISING THE SAME AS ACTIVE INGREDIENT

The present invention relates to isoquinolinone derivatives, a method for preparing the same, and a pharmaceutical composition for preventing or treating poly(ADP-ribose) polymerase-1 (PARP-1)-related diseases containing the same as an active ingredient. The isoquinolinone derivatives exhibit an excellent PARP-1 inhibitory effect at a concentration of nanomolar units, and further exhibit an excellent cytoprotective effect (apoptosis inhibitory effect) on ophthalmic diseases or disorders, specifically retinal disorders, and thus can be effectively used as a pharmaceutical composition for preventing or treating PARP-1-related diseases, for example, ophthalmic diseases or disorders, which contains the same as an active ingredient.

Proteasome activity enhancing compounds

The present invention is directed to compounds having the Formulae (Ia), (Ib), (Ic), or (Id); or the Formulae (II), (IIa), (IIb), or (IIc); or the Formulae (III), (IIIa), (IIIb), (IIIc), (IIId), or (IIIe), and pharmaceutically acceptable salts, solvates, clathrates and prodrugs of any Formula thereof, compositions thereof, and methods for the treatment of a condition associated with a dysfunction in proteostasis.