Abstract: The present invention refers to the use of compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): wherein R1 and R2 represent, independently of each other: an optionally substituted phenyl ring, or an optionally substituted 5-membered heteroaromatic ring; one of R3 and R4 is H and the other represents a group wherein W is OH or an ortho-aniline group; each A, independently of each other, represents a —CH2— group or is absent; ?Y—Y? is ?HC—CH?, ?N—CH?, or ?HC—N?; or a salt or solvate thereof, in the prevention or treatment of an autoimmune disease.

Abstract: The nitric ester of Saquinavir, or its non-toxic salts, solvates or crystalline/polymorphic forms, I useful in the treatment of autoimmune diseases, particularly in disease mediated by pro-inflammatory cytokines. Examples of diseases which may be treated include idiopathic Addison's disease, autoimmune hepatitis, biliary cirrhosis, primary sclerosing cholangitis, Guillain Barré syndrome, Hashimoto's thyroiditis, psoriasis, rheumatoid arthritis, Sjogren's syndrome, systemic lupus erythematous, Type 1 diabetes mellitus and uveitis of ischemia-reperfusion, graft versus host diseases, graft rejection, endo and exo-toxemia and gouty arthritis.

Abstract: The present invention describes pharmaceutical compositions containing APOTf for use in preventing (or delaying the onset) and treating autoimmune diseases. Based on the experimental data obtained, the molecule has the surprising capacity to favorably modify the immune response profile both in vitro and in vivo.

Abstract: HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo.

Abstract: The present invention describes pharmaceutical compositions containing APOTf for use in preventing (or delaying the onset) and treating autoimmune diseases. Based on the experimental data obtained, the molecule has the surprising capacity to favourably modify the immune response profile both in vitro and in vivo.

Abstract: Compounds of formula I wherein I, R1-5 represents from one to five substituents independently selected from hydrogen, nitro, cyano, C1-C3-alkyl, halogen, carboxy, amino, trifluoromethyl, hydroxy, C1-C3-alkoxy groups, X is hydrogen, halo, N3, SH, ?O, ?CH2, an aromatic, preferably phenyl, ring optionally substituted by R1-5 groups as defined above, amino, mono- or disubstituted amino groups wherein the substituents are selected from C1-C4 alkyl, phenyl or benzyl groups optionally substituted by R1-5 groups as defined above Y is hydrogen, alkyl C1-C4, amino, or a group of formula —(CH2)0-1A wherein A is an aromatic, preferably phenyl, ring optionally substituted by R1-5 groups as defined above with the proviso that when X and Y are hydrogen, R1-5 cannot represent a 4-hydroxy or 4-alkoxy groups, are useful for the treatment of Tumor Necrosis Factor mediated immunopathological conditions as well as of diseases which may be treated or alleviated by inhibition of Interleukin-10 (IL-10).

Abstract: The present invention relates to an isoxazole derivative, the compound of formula (I) herein after referred to as GIT27-NO, which is the NO-donating structurally modified form of (S,R)-3-phenyl-4,5-dihydro-5-isoxazole acetic acid, herein after referred to as VGX-1027. Treatment of three tumor cell lines, rat astrocytoma C6, mouse fibrosarcoma L929, and mouse melanoma B16 cells with GIT27-NO resulted in a significant reduction of cell respiration and of number of viable cells, while VGX-1027 was completely ineffective. Hemoglobin, which act as NO-scavenger, restored cell viability, thus indicating the NO-mediated tumoricidal effect of compound (I). GIT27-NO triggered apoptotic cell death in L929 cell cultures, while autophagic cell death is mainly responsible for the diminished viability of C6 and B16 cells.

Abstract: HIV-protease inhibitors, particularly saquinavir, showed strong anticancer activity but numerous side effects limited its application. In order to overcome its toxicity original compounds were modified by covalent attachment of NO. The efficacy of parental and NO-modified drug was compared in vitro and in vivo. Anticancer activities of NO-modified saquinavir (Saq-NO) was monitored in vitro using assay for cell viability, proliferation, necrotic, autophagic and apoptotic cell death, differentiation, expression of intracellular molecules such as cyclin D3, p53 and Akt. Antitumor properties and toxicity of the compound was estimated in vivo. Saq-NO abrogated the viability of large spectrum of human and rodent tumor cell lines with IC50 significantly lower than parental drug and expressed strong antimelanoma action in vivo. In contrast to saquinavir, there was no detectable toxicity against primary cells in vitro and in vivo.

Abstract: The present invention relates to an isoxazole derivative, the compound of formula (I) herein after referred to as GIT27-NO, which is the NO-donating structurally modified form of (S,R)-3-phenyl-4,5-dihydro-5-isoxazole acetic acid, herein after referred to as VGX-1027. Treatment of three tumor cell lines, rat astrocytoma C6, mouse fibrosarcoma L929, and mouse melanoma B16 cells with GIT27-NO resulted in a significant reduction of cell respiration and of number of viable cells, while VGX-1027 was completely ineffective. Hemoglobin, which act as NO-scavenger, restored cell viability, thus indicating the NO-mediated tumoricidal effect of compound (I). GIT27-NO triggered apoptotic cell death in L929 cell cultures, while autophagic cell death is mainly responsible for the diminished viability of C6 and B16 cells.

Abstract: Compounds of formula I wherein I, R1-5 represents from one to five substituents independently selected from hydrogen, nitro, cyano, C1-C3-alkyl, halogen, carboxy, amino, trifluoromethyl, hydroxy, C1-C3-alkoxy groups, X is hydrogen, halo, N3, SH, =O, =CH2, an aromatic, preferably phenyl, ring optionally substituted by R1-5 groups as defined above, amino, mono- or disubstituted amino groups wherein the substituents are selected from C1-C4 alkyl, phenyl or benzyl groups optionally substituted by R1-5 groups as defined above Y is hydrogen, alkyl C1-C4, amino, or a group of formula —(CH2)0-1A wherein A is an aromatic, preferably phenyl, ring optionally substituted by R1-5 groups as defined above with the proviso that when X and Y are hydrogen, R1-5 cannot represent a 4-hydroxy or 4-alkoxy groups, are useful for the treatment of Tumor Necrosis Factor mediated immunopathological conditions as well as of diseases which may be treated or alleviated by inhibition of Interleukin-10 (IL-10).

Abstract: The present invention relates to the method(s) of synthesis of and the therapeutic and cosmetic applications of biologically active peptides for improving the appearance of skin, for hastening wound healing and for treating and/or preventing the progression of various conditions, injuries and diseases, including but not limited to viral hepatitis B and C, herpes zoster ganglioneuritis, diabetic peripheral polyneuropathy, nephrotic syndrome, juvenile rheumatoid arthritis, rheumatoid arthritis, psoriatic arthritis, bronchial asthma, respiratory infection, breast cancer, epilepsy, psoriasis, atherosclerosis and other forms of vascular obstructions, myocardial infarction, HIV and SARS infection, brain cell malfunction due to ischemia and trauma, pathologic consequences of ischemia-reperfusion, rejection reaction following organ transplantation, chemical and drug intoxication including but not limited to anesthetic, alcohol and morphine, cancer, type 1 diabetes mellitus, multiple sclerosis, septic shock (Gram nega

Abstract: This invention relates to the use of the protein UK114, possibly associated with ubiquitin, for the treatment of leishmaniasis in humans and animals.