Patent classifications
C07D498/06
METHODS AND COMPOUNDS FOR RESTORING MUTANT p53 FUNCTION
Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The present disclosure describes compounds and methods to recover wild-type function to p53 mutants. The compounds of the present invention can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds can be used to reduce the progression of cancers that contain a p53 mutation.
TRICYCLIC PYRIDONES AND PYRIMIDONES
A compound of Formula (I) is provided: (I) where the variables are defined herein.
##STR00001##
TRICYCLIC PYRIDONES AND PYRIMIDONES
A compound of Formula (I) is provided: (I) where the variables are defined herein.
##STR00001##
QUINOLONE COMPOUND
The present invention provides a compound represented by the formula (I)
##STR00001##
wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R.sup.1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R.sup.2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R.sup.3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
QUINOLONE COMPOUND
The present invention provides a compound represented by the formula (I)
##STR00001##
wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R.sup.1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R.sup.2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R.sup.3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT
An organic compound represented by the formula [1]:
##STR00001##
R.sub.1 to R.sub.19 are independently selected from the group consisting of a hydrogen atom, a deuterium atom, a halogen atom, and a substituent, and R.sub.9 and R.sub.19 are optionally bonded together. When R.sub.9 and R.sub.19 are bonded together, the bonding is selected from the group consisting of direct bonding, bonding via an oxygen atom or a sulfur atom, and bonding via CR.sub.20R.sub.21. R.sub.20 and R.sub.21 independently have the same meaning as R.sub.1 to R.sub.19. X.sub.1 and X.sub.2 independently denote an oxygen atom, a sulfur atom, CR.sub.20R.sub.21, or a single bond. Ar denotes an aromatic hydrocarbon group or a heterocyclic group, n denotes an integer in the range of 0 to 2, and m denotes an integer in the range of 1 to 4. When n is 0, any one of R.sub.1 to R.sub.8 is directly bonded to any one of R.sub.9 to R.sub.19.
ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT
An organic compound represented by the formula [1]:
##STR00001##
R.sub.1 to R.sub.19 are independently selected from the group consisting of a hydrogen atom, a deuterium atom, a halogen atom, and a substituent, and R.sub.9 and R.sub.19 are optionally bonded together. When R.sub.9 and R.sub.19 are bonded together, the bonding is selected from the group consisting of direct bonding, bonding via an oxygen atom or a sulfur atom, and bonding via CR.sub.20R.sub.21. R.sub.20 and R.sub.21 independently have the same meaning as R.sub.1 to R.sub.19. X.sub.1 and X.sub.2 independently denote an oxygen atom, a sulfur atom, CR.sub.20R.sub.21, or a single bond. Ar denotes an aromatic hydrocarbon group or a heterocyclic group, n denotes an integer in the range of 0 to 2, and m denotes an integer in the range of 1 to 4. When n is 0, any one of R.sub.1 to R.sub.8 is directly bonded to any one of R.sub.9 to R.sub.19.
Substituted quinolines as PDE-10 inhibitors
Provided herein are Cyclic Nucleotide Phosphodiesterase inhibitors, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.
Substituted quinolines as PDE-10 inhibitors
Provided herein are Cyclic Nucleotide Phosphodiesterase inhibitors, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.
Antiviral compounds highly effective as HCV-NS5A inhibitor
Provided are compounds antiviral compounds represented by formula Ia and Ib: ##STR00001##
that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.