Patent classifications
A61K31/41
Antibacterial compounds
The present application provides compounds of formula: Methods of using these compounds for killing bacterial growth and treating bacterial infections are also provided. ##STR00001##
USES OF COMPLEX OF ANGIOTENSIN II RECEPTOR ANTAGONIST METABOLITE AND NEP INHIBITOR IN TREATING HEART FAILURE
Uses of a complex of an angiotensin II receptor antagonist metabolite and a NEP inhibitor in treating heart failure, specifically related are uses of complex in preparing a medicament for use in heart failure with reduced ejection fraction (HFrEF).
Benzocarbonyl compounds
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
COMBINATION THERAPY WITH ANTI-PVRIG ANTIBODIES FORMULATIONS AND ANTI-PD-1 ANTIBODIES
The present invention is directed to combination treatments with anti-PVRIG antibodies and anti-PD-1 antibodies, in particular nivolumab, using stable liquid pharmaceutical formulations thereof.
COMBINATION THERAPY WITH ANTI-PVRIG ANTIBODIES FORMULATIONS AND ANTI-PD-1 ANTIBODIES
The present invention is directed to combination treatments with anti-PVRIG antibodies and anti-PD-1 antibodies, in particular nivolumab, using stable liquid pharmaceutical formulations thereof.
A PROCESS FOR THE PREPARATION OF HIGHLY PURE VALSARTAN
Disclosed herein is a process for the preparation and purification of Valsartan. The process according to the invention is capable of removing the toxic nitroamine impurities and providing substantially pure Valsartan.
THERAPY
The invention addresses radioresistance in cancer treatment involving radiotherapy and, in particular, limitations associated with the use of the drug sulfasalazine. Specifically, it provides a series of compounds for use as radiosensitizers in the treatment of cancers such as glioblastomas which are lethal and inherently resistant to radiotherapy. In one embodiment, the invention provides compounds of general formula (I), their stereoisomers and pharmaceutically acceptable salts for use as radiosensitizers in the treatment of cancer:
##STR00001##
wherein ring A is selected from optionally substituted phenyl, biphenyl and fluorenyl; each X is independently selected from: —C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —O—C.sub.1-6 alkyl (preferably —O—C.sub.1-3 alkyl, e.g. —OCH.sub.3), —S—C.sub.1-6 alkyl (preferably —S—C.sub.1-3 alkyl, e.g. —SCH.sub.3), —OH, —SH, —CO.sub.2R.sup.1 (where R.sup.1 is H or C.sub.1-6 alkyl, preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —SO.sub.2—C.sub.1-6 alkyl (preferably —SO.sub.2—C.sub.1-3 alkyl, e.g. —SO.sub.2—CH.sub.3), —SO.sub.2—NR.sup.2R.sup.3 (where R.sup.2 is H and R.sup.3 is optionally substituted phenyl), —NR.sup.4R.sup.5 (wherein R.sup.4 and R.sup.5 are independently selected from H, C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), and —CO—C.sub.1-6 alkyl (preferably —CO—C.sub.1-3 alkyl, e.g. —CO—CH.sub.3), halogen (e.g. F, Cl or Br), and optionally substituted tetrazolyl; n is an integer from 0 to 5, preferably 0 to 2, e.g. 1 or 2; and denotes an E or Z double bond.
THERAPY
The invention addresses radioresistance in cancer treatment involving radiotherapy and, in particular, limitations associated with the use of the drug sulfasalazine. Specifically, it provides a series of compounds for use as radiosensitizers in the treatment of cancers such as glioblastomas which are lethal and inherently resistant to radiotherapy. In one embodiment, the invention provides compounds of general formula (I), their stereoisomers and pharmaceutically acceptable salts for use as radiosensitizers in the treatment of cancer:
##STR00001##
wherein ring A is selected from optionally substituted phenyl, biphenyl and fluorenyl; each X is independently selected from: —C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —O—C.sub.1-6 alkyl (preferably —O—C.sub.1-3 alkyl, e.g. —OCH.sub.3), —S—C.sub.1-6 alkyl (preferably —S—C.sub.1-3 alkyl, e.g. —SCH.sub.3), —OH, —SH, —CO.sub.2R.sup.1 (where R.sup.1 is H or C.sub.1-6 alkyl, preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), —SO.sub.2—C.sub.1-6 alkyl (preferably —SO.sub.2—C.sub.1-3 alkyl, e.g. —SO.sub.2—CH.sub.3), —SO.sub.2—NR.sup.2R.sup.3 (where R.sup.2 is H and R.sup.3 is optionally substituted phenyl), —NR.sup.4R.sup.5 (wherein R.sup.4 and R.sup.5 are independently selected from H, C.sub.1-6 alkyl (preferably C.sub.1-3 alkyl, e.g. —CH.sub.3), and —CO—C.sub.1-6 alkyl (preferably —CO—C.sub.1-3 alkyl, e.g. —CO—CH.sub.3), halogen (e.g. F, Cl or Br), and optionally substituted tetrazolyl; n is an integer from 0 to 5, preferably 0 to 2, e.g. 1 or 2; and denotes an E or Z double bond.
5-(Thiophen-2-YL)-1 H-Tetrazole Derivative as BCKDK Inhibitors Useful for Treating Various Diseases
Described herein are compounds of Formula I,
##STR00001##
wherein R.sup.1, R.sup.2, and R.sup.3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.
5-(Thiophen-2-YL)-1 H-Tetrazole Derivative as BCKDK Inhibitors Useful for Treating Various Diseases
Described herein are compounds of Formula I,
##STR00001##
wherein R.sup.1, R.sup.2, and R.sup.3 are defined herein, their use as branched-chain alpha keto acid dehydrogenase kinase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetes, NASH and heart failure.