40 results about "Nitric oxide synthetase" patented technology

Improved treatments of joint diseases, such as, e.g. osteoarthritis and rheumatoid arthritis, and pain, wherein a strontium-containing compound is administered alone or in combination with one or more second therapeutically and / or prophylactically active substances, selected from the group consisting of bisphosphonates, glucosamine, pallitative agents, analgesic agents, disease modifying anti-rheumatic compounds (DMARDs), selective estrogen receptor modulators (SERMs), aromatase inhibitors, non-steroidal anti-inflammatory agents (NSAIDs), COX-2 inhibitors, COX-3 inhibitors, opioids, inhibitors / antagonists of IL-1, inhibitors / antagonists of TNF-alpha, inhibitors of matrix metallo-proteinases (MMPs), cathepsin K inhibitors, inhibitors / antagonists of RANK-ligand, statins, glucocorticoids, chondroitin sulphate, NMDA receptor antagonists, inhibitors of interleukin-I converting enzyme, Calcitonin gene related peptide antagonists, glycine antagonists, vanilloid receptor antagonists, inhibitors of inducible nitric oxide synthetase (iNOS), N-acetylcholine receptor agonists, neurokinin antagonists, neuroleptic agents, PAR2 receptor antagonists and anabolic growth factors acting on joint tissue components. Pharmaceutical compositions comprising a strontium-containing compound and a second therapeutically and / or prophylactically active substance as defined above.

A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.

The present invention is directed to a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein:R2 is selected from the group consisting of H and methyl; andR2 is selected from the group consisting of H and methyl.The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.

The present invention relates to the field of medicinal chemistry, in particular to a class of 3-cyanoquinoline derivatives (I), a dual inhibitor of tyrosine protein kinase and nitric oxide synthase, wherein G1, G2, G3, G4, X, Z, See the specification for the definition of n. The invention also discloses a preparation method of compound I, a pharmaceutical composition containing it, and an application for treating tumor diseases.

A composition for preventing and / or treating piles contains at least one NO synthetase (NOS) inhibitor, especially iNOS inhibitor, at least one vascular angiogenesis inhibitor, especially VEGF inhibitor, and at least one matrix metal proteinase (MMP) inhibitor, especially MMP1, MMP3, MMP9 and / or MMP12 inhibitor.

The present invention relates to an anti-inflammatory use of macrolactin compounds such as macrolactin A, 7-O-malonyl macrolactin A and 7-O-succinyl macrolactin A, which are produced from a novel Bacillus strain of Bacillus polyfermenticus KJS-2 (KCCM10769P). The macrolactin compounds provided by the present invention were confirmed to greatly suppress the expression and formation of inducible nitric oxide synthetase (iNOS) and cyclooxygenase-2 (COX-2) which are proteins related to the formation of inflammatory mediators, and to accordingly inhibit the formation of nitric oxide (NO) and of prostaglandin E2 (PGE2) which are the metabolites of the proteins. In addition, the macrolactin compounds provided by the present invention were confirmed to have excellent effects in inhibiting the formation of tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6) and granulocyte macrophage colony-stimulating factor (GM-CSF), which are pro-inflammatory cytokines. Therefore, the macrolactin compounds produced by the Bacillus polyfermenticus KJS-2 strain according to the present invention can provide excellent anti-inflammatory agents.