C07D239/86

Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NRR, C.sub.1-7 alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7 alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R and R are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

4,6-di- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NRR, C.sub.1-7 alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7 alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R and R are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies

The present application discloses compounds which are activators of autophagic flux and pharmaceutical compositions comprising said activators. It further discloses use of said compounds and pharmaceutical compositions in the treatment of neurodegenerative diseases, particularly proteinopathies and tauopathies such as Alzheimer's disease. It further discloses methods of enhancing autophagic flux.

Bicyclic-Fused Heteroaryl or Aryl Compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,

##STR00001##

as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Bicyclic-Fused Heteroaryl or Aryl Compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,

##STR00001##

as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

DNA-PK INHIBITORS

The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions, or disorders.

Bicyclic-fused heteroaryl or aryl compounds

Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.