A61K31/527

PYRAZINOQUINAZOLINONE DERIVATIVES WITH ANTIBACTERIAL ACTIVITY, METHODS AND USES THEREOF

The present disclosure relates to compounds and compositions displaying antibacterial activity, particularly against Gram-positive bacteria. The compounds comprise a class of pyrazinoquinazolinone derivatives, including neofiscalin A and fiscalin C, or pharmaceutically acceptable salts, esters, solvates or prodrugs thereof. The present disclosure further relates to methods for treating a patient with a bacterial infection with the disclosed compounds and compositions.

Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators
10005782 · 2018-06-26 · ·

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby. ##STR00001##

Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators
10005782 · 2018-06-26 · ·

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby. ##STR00001##

FUSED, SPIROCYCLIC HETEROAROMATIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
20180169104 · 2018-06-21 ·

Disclosed are methods for treating various bacterial infections with (2R,4S,4aS)-11-fluoro-2,4-dimethyl-8-[(4S)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,2,4,4a-tetrahydro-2H,6H-spiro[1,4-oxazino[4,3-a][1,2]oxazolo[4,5-g]quinoline-5,5-pyrimidine]-2,4,6(1H,3H)-trione, or a pharmaceutically acceptable salt thereof.

FUSED, SPIROCYCLIC HETEROAROMATIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
20180169104 · 2018-06-21 ·

Disclosed are methods for treating various bacterial infections with (2R,4S,4aS)-11-fluoro-2,4-dimethyl-8-[(4S)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]-1,2,4,4a-tetrahydro-2H,6H-spiro[1,4-oxazino[4,3-a][1,2]oxazolo[4,5-g]quinoline-5,5-pyrimidine]-2,4,6(1H,3H)-trione, or a pharmaceutically acceptable salt thereof.

FUSED HETEROAROMATIC PYRROLIDINONES

Disclosed are compounds of Formula 1,

##STR00001##

and pharmaceutically acceptable salts thereof, wherein G, L.sup.1, L.sup.2, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

FUSED HETEROAROMATIC PYRROLIDINONES

Disclosed are compounds of Formula 1,

##STR00001##

and pharmaceutically acceptable salts thereof, wherein G, L.sup.1, L.sup.2, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

CDK inhibitors
09957276 · 2018-05-01 · ·

Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

Dihydropyrimido fused ring derivative as HBV inhibitor

Disclosed is a dihydropyrimido fused ring derivative as a HBV inhibitor, and in particular relates to a compound shown as formula (I) or a pharmaceutically acceptable salt thereof. ##STR00001##

Ethynyl derivatives

The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.