Patent classifications
A61K31/625
Salicylic acid derivatives, pharmaceutically acceptable salt thereof, composition thereof and method of use thereof
The present invention relates to novel compounds, compositions containing same and methods for inhibiting STAT3 and/or STAT5 activity or for the treatment of a STAT3 or STAT5-dependent cancer using said compounds; or a pharmaceutically acceptable salt, solvate or prodrug thereof. ##STR00001##
Cyclic Amines
The present invention is directed to novel cyclic amines which inhibit the P2X7 receptor.
Cyclic amines
The present invention is directed to novel cyclic amines which inhibit the P2X.sub.7 receptor.
PREVENTION OR TREATMENT OF CARDIOVASCULAR DISEASES WITH HIGH PENETRATION PRODRUGS OF ASPIRIN AND OTHER NSAIDS
The present disclosure provides 2-(diethylamino)ethyl acetoxybenzoate hydrochloride, other high penetration prodrugs of aspirin and other NSAIDs, and pharmaceutically acceptable salts thereof for use and methods thereof in the prevention or treatment of cardiovascular diseases and conditions. Pharmaceutical compositions, treatment kits and devices including 2-(diethylamino)ethyl acetoxybenzoate hydrochloride, other high penetration prodrugs of aspirin and other NSAIDs, and pharmaceutically acceptable salts thereof, as well as dosage forms, dosages, and methods of use thereof through topical administration are described.
PREVENTION OR TREATMENT OF CARDIOVASCULAR DISEASES WITH HIGH PENETRATION PRODRUGS OF ASPIRIN AND OTHER NSAIDS
The present disclosure provides 2-(diethylamino)ethyl acetoxybenzoate hydrochloride, other high penetration prodrugs of aspirin and other NSAIDs, and pharmaceutically acceptable salts thereof for use and methods thereof in the prevention or treatment of cardiovascular diseases and conditions. Pharmaceutical compositions, treatment kits and devices including 2-(diethylamino)ethyl acetoxybenzoate hydrochloride, other high penetration prodrugs of aspirin and other NSAIDs, and pharmaceutically acceptable salts thereof, as well as dosage forms, dosages, and methods of use thereof through topical administration are described.
COMPOSITIONS AND METHODS FOR DETECTING SNP(S) ASSOCIATED WITH DIABETES
In one aspect, provided herein are set of primers and use of the same for the detection of SNPs associated with diabetes. In certain embodiments, the primers used to detect SNP sites associated with diabetes comprise Primer Set 1 to Primer Set 47. The experiments show: the genotyping results of the SNP sites associated with diabetes can be accurately detected by the primers disclosed herein, and the risk of individuals can be comprehensively evaluated and the result is more accurate than the single site analysis. In addition, SNPs disclosed herein are verified as associated with type 2 diabetes and its complications, which are especially suitable for the prevention and individualized treatment for type 2 diabetes in East Asian, for example, in China.
Cyclic Amines
The present invention is directed to novel cyclic amines which inhibit the P2X.sub.7 receptor.
CATALYTIC INHIBITOR OF PROTEIN PHOSPHATASE 5 ACTIVATES THE EXTRINSIC APOPTOTIC PATHWAY BY DISRUPTING COMPLEX II
Protein phosphatase 5 (PP5) is a serine/threonine protein phosphatase involved in the maturation and activation of numerous signaling pathways essential for cancer growth. PP5 activity is essential for the survival of clear cell renal cell carcinoma (ccRCC), however the mechanism remains unclear. Data demonstrates that PP5 interacts with caspase-8, FADD, and RIPK1, components of extrinsic apoptotic pathway Complex II. Specifically, PP5 dephosphorylates and inactivates the death effector proteins RIPK1 and FADD, preserving Complex II integrity and regulating extrinsic apoptosis. Protein phosphatases are considered to be undruggable, however we have developed a specific inhibitor of PP5 (P-053) that prevents substrate binding to the active site. Encouragingly, PP5 inhibition using P-53 in VHL-null ccRCC robustly induces extrinsic apoptosis. Taken together, the data suggests that PP5 promotes ccRCC survival by suppressing extrinsic apoptosis, and small molecule inhibition of PP5 presents a viable therapeutic strategy for ccRCC.
CATALYTIC INHIBITOR OF PROTEIN PHOSPHATASE 5 ACTIVATES THE EXTRINSIC APOPTOTIC PATHWAY BY DISRUPTING COMPLEX II
Protein phosphatase 5 (PP5) is a serine/threonine protein phosphatase involved in the maturation and activation of numerous signaling pathways essential for cancer growth. PP5 activity is essential for the survival of clear cell renal cell carcinoma (ccRCC), however the mechanism remains unclear. Data demonstrates that PP5 interacts with caspase-8, FADD, and RIPK1, components of extrinsic apoptotic pathway Complex II. Specifically, PP5 dephosphorylates and inactivates the death effector proteins RIPK1 and FADD, preserving Complex II integrity and regulating extrinsic apoptosis. Protein phosphatases are considered to be undruggable, however we have developed a specific inhibitor of PP5 (P-053) that prevents substrate binding to the active site. Encouragingly, PP5 inhibition using P-53 in VHL-null ccRCC robustly induces extrinsic apoptosis. Taken together, the data suggests that PP5 promotes ccRCC survival by suppressing extrinsic apoptosis, and small molecule inhibition of PP5 presents a viable therapeutic strategy for ccRCC.
Pharmaceutical suspensions for bismuth subsalicylates
The invention is directed to pharmaceutical compositions for suspending bismuth subsalicylate and methods of use thereof. Formulations of the present invention include at least three-gum systems to prevent the settling out of heavy particles in solution and do not include magnesium aluminum silicate. The pharmaceutical compositions may be used to treat gastrointestinal disorders.