The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

The present application relates to novel amino-substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

The invention relates to biotechnology. The exenatide analogue with the formula H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-As-Leu-Ser-Lys-Gln-Glu-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala- Pro-Pro-Pro-Ser-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-Gly-OH is presented. The invention allows treating and taking preventive measures against diabetes mellitus as well as treating and taking preventive measures against type 2 diabetes mellitus complications, such as diabetic neuropathy, muscular dystrophy and endotheliopathy.

The present invention provides a therapeutic agent for epithelial and endothelial injury, and in particular, for epithelial and endothelial microinjury, and the like. The therapeutic agent according to the present invention comprises, for example, a peptide of the following (a), (b), etc., a derivative thereof, or their salt: (a) a peptide comprising the amino acid sequence shown in any one of SEQ ID NOS: 10, 4, 12 and 6; or (b) a peptide comprising the amino acid sequence shown in any one of SEQ ID NOS: 16, 18, 20 and 22.

The present invention provides pharmaceutical compositions comprising second-generation molecules that are superior than TOCILIZUMAB, by altering the amino acid sequences of the variable and constant regions of TOCILIZUMAB, which is a humanized anti-IL-6 receptor IgG1 antibody, to enhance the antigen-neutralizing ability and increase the pharmacokinetics, so that the therapeutic effect is exerted with a less frequency of administration, and the immunogenicity, safety and physicochemical properties (stability and homogeneity) are improved. The present invention also provides methods for producing these pharmaceutical compositions.

The present inventors have successfully generated second-generation molecules that are superior to TOCILIZUMAB by appropriately combining amino acid sequence alterations in the CDR domains, variable regions, and constant regions.

Synergistic nutraceutical or pharmaceutical anti-inflammatory compositions include a therapeutically effective combination of: an extract selectively enriched in 3-O-acetyl-11-keto-β-boswellic acid (AKBA) derived from Boswellia serrata; and a Boswellia serrata non-acidic resin extract (BNRE). The compositions can be used to prevent, control and treat inflammation and several inflammatory related diseases including asthma, osteoarthritis, rheumatoid arthritis, and/or endothelial dysfunction. The invention further discloses the amelioration of pro-inflammatory biomarker proteins or molecules, whose expression/production is altered during inflammatory diseases.

In one aspect, the invention provides methods of inhibiting the effects of MASP-2-dependent complement activation in a living subject. In one embodiment, the invention provides methods of treating a subject suffering from a complement mediated coagulation disorder, such as disseminated intravascular coagulation. The methods comprise the step of administering, to a subject in need thereof, an amount of a MASP-2 inhibitory agent effective to inhibit MASP-2-dependent complement activation. In some embodiments, the MASP-2 inhibitory agent inhibits cellular injury associated with MASP-2-mediated alternative complement pathway activation, while leaving the classical (C1q-dependent) pathway component of the immune system intact. In another aspect, the invention provides compositions for inhibiting the effects of lectin-dependent complement activation, comprising a therapeutically effective amount of a MASP-2 inhibitory agent and a pharmaceutically acceptable carrier.

The present invention relates to the use of rebamipide in a method of prevention and/or treatment of arterial stiffness and associated diseases, such as hypertension, heart failure, myocardial infarction, stroke, peripheral arterial disease, renal failure, and chronic kidney disease. Rebamipide may also be used in a method of increasing arterial elasticity.

The present application relates to novel substituted quinoline-4-carboxamides and use thereof, to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.

Edoxaban is factor X inhibitor useful for the treatment or the prevention of thrombosis or embolism. A pharmaceutical composition comprising Edoxaban, or a pharmaceutically acceptable salt thereof, a water soluble vinylpyrrolidone polymer selected from the group consisting of povidone and copovidone, and a cellulose ether, and not comprising a sugar alcohol, having good dissolution and bioavailability is provided. A process for its preparation, a dosage form comprising such composition, and the use of said pharmaceutical composition and dosage form as a medicament are also disclosed.