Patent classifications
C07D419/12
COVALENT INHIBITORS OF KRAS G12C
Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
Multicyclic compounds and methods of using same
The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders). ##STR00001##
MIXED DISULFIDE CONJUGATES OF THIENOPYRIDINE COMPOUNDS AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to mixed disulfide conjugates of thienopyridine compounds, and their use as therapeutics for the treatment, amelioration, and prevention of cardiovascular diseases.
Compounds and methods for the treatment of isocitrate dehydrogenase related diseases
The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof: ##STR00001##
Compounds and methods for the treatment of isocitrate dehydrogenase related diseases
The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof: ##STR00001##
Simplified structural mimetics of AIPS as quorum sensing inhibitors
Compounds provided are racemic, non-racemic or substantially enantiomerically pure dimers or salts or solvates thereof of formula: ##STR00001## where: W and W are S or NR.sub.1, or WCO or WCO is CHCH, where each R.sub.1 is hydrogen or an alkyl group having 1 to 3 carbon atoms; R and R are hydrogen or an straight-chain or branched alkyl group having 1-3 carbon atoms; R.sub.3 and R.sub.3 are hydrogen or a C1-C3 alkyl; X.sub.1, X.sub.1, X.sub.2 and X.sub.2 are optionally-substituted straight-chain or branched alkyl groups having 3-8 carbon atoms, optionally-substituted cycloalkyl groups having 3-12 carbon atoms; optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted heterocycyl, optionally-substituted cycloalkylalkyl, optionally-substituted arylalkyl, optionally-substituted heteroarylalkyl and optionally-substituted heterocycylalkyl groups and L.sub.1, L.sub.1 and L.sub.2 are divalent chemical moieties. Dimers are employed to modulate quorum sensing and to thus inhibit virulence in Staphylococcus bacteria. Dimers are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.
Simplified structural mimetics of AIPS as quorum sensing inhibitors
Compounds provided are racemic, non-racemic or substantially enantiomerically pure dimers or salts or solvates thereof of formula: ##STR00001## where: W and W are S or NR.sub.1, or WCO or WCO is CHCH, where each R.sub.1 is hydrogen or an alkyl group having 1 to 3 carbon atoms; R and R are hydrogen or an straight-chain or branched alkyl group having 1-3 carbon atoms; R.sub.3 and R.sub.3 are hydrogen or a C1-C3 alkyl; X.sub.1, X.sub.1, X.sub.2 and X.sub.2 are optionally-substituted straight-chain or branched alkyl groups having 3-8 carbon atoms, optionally-substituted cycloalkyl groups having 3-12 carbon atoms; optionally-substituted aryl, optionally-substituted heteroaryl, optionally-substituted heterocycyl, optionally-substituted cycloalkylalkyl, optionally-substituted arylalkyl, optionally-substituted heteroarylalkyl and optionally-substituted heterocycylalkyl groups and L.sub.1, L.sub.1 and L.sub.2 are divalent chemical moieties. Dimers are employed to modulate quorum sensing and to thus inhibit virulence in Staphylococcus bacteria. Dimers are useful in treating infections of Staphylococcus bacteria. Methods for treating such bacterial infections are also provided.
Convenient process for the preparation of statins
Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.
Convenient process for the preparation of statins
Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.
METHODS FOR TREATING CANCER WITH RORGAMMA INHIBITORS
The present invention provides compositions, methods, and kits comprising one or more ROR inhibitors, alone or in combination with one or more anticancer drugs, such as an anti-androgen drug, that are useful for treating cancer, e.g., prostate cancer, such as castration-resistant prostate cancer (CRPC), and numerous other types of cancer including lung cancer, breast cancer, liver cancer, ovarian cancer, endometrial cancer, bladder cancer, colon cancer, lymphoma, and glioma.