专利号:WO-9614060-A1 优先权日:1994-11-04 标题 :Use of receptor agonists to stimulate superoxide dismutase activity 发明人:MARKLUND STEFAN L; STRAALIN PONTUS 权利人:MARKLUND STEFAN L; STRAALIN PONTUS 摘要:The present invention relates to the use of a substance for the manufacture of a composition for stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells. In particular, the invention relates to the use of a substance for the manufacture of a composition for prophylaxis or treatment of a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical. Further, the invention relates to a method for determining the effect of a substance with respect to stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells and to substances which have been selected by said method. Within the scope of the invention is a method of preventing, diminishing, controlling or inhibiting a disease or disorder connected with the presence or formation of superoxide radicals and other toxic intermediates derived from the superoxide radical in a patient who has been established to have a high risk of developing a such disease or disorder, or who has developed a such disease or disorder, the method comprising administering an effective amount of a substance which is capable of stimulating the release of EC-SOD from cells or stimulating the synthesis of EC-SOD in cells.
专利号:WO-0217958-A1 优先权日:2000-08-29 标 题:Agent for influencing angiogenesis 发明人:BADER MICHAEL; PESQUERO JOAO BOSCO; MADEDDU PAOLO; EMAMUELI COSTANCA 权利人:MAX DELBRUECK CENTRUM; BADER MICHAEL; PESQUERO JOAO BOSCO; MADEDDU PAOLO; EMAMUELI COSTANCA 摘要:The invention relates to an agent for influencing angiogenesis, i.e. the new formation of blood vessels. The application areas for this agent are the medical field and the pharmaceutical industry. The aim of the invention is to discover new agents for influencing angiogenesis and to provide corresponding substances that can be used in the medical field to produce said agents. The inventive agent is characterised in that it influences angiogenesis, i.e. promotes or inhibits the latter. The promotion of angiogenesis is achieved, for example, by increasing the synthesis of the B1 receptor (transcription-mediated amplification, e.g. by cytokines), or by increasing its activity (agonistic substances). The inhibition of angiogenesis is achieved, for example, by antagonists of the kinin B1 receptor, such as des-Arg<9>-Leu<8>-bradykinin (DALBK) or non-peptide substances and by inhibiting the synthesis of the protein, e.g. using glucucorticoids.
专利号:US-6988446-B2 优先权日:1996-07-05 标 题:Purified nitric oxide synthase 发明人:ROSAZZA JOHN P N; CHEN YIJUN 权利人:UNIV IOWA RES FOUND 摘要:The present invention provides a novel constitutive nitric oxide synthase (NOS) that utilizes both L -arginine and arginine-rich peptides, oligopeptides or proteins, e.g., bradykinin (BK), as substrates in the synthesis of nitric oxide (NO). Also provided are methods of controlling, regulating or modulating NO synthesis in a subject.
专利号:US-5939392-A 优先权日:1993-06-03 标 题 :Method of thrombin inhibition 发明人:ANTONSSON KARL THOMAS; BYLUND RUTH ELVY; GUSTAFSSON NILS DAVID; NILSSON NILS OLOV INGEMAR 权利人:ASTRA AB 摘要:The invention relates to new competitive tripeptide inhibitors of trypsin-like serine proteases, their synthesis, pharmaceutical compositions containing the compounds as active ingredients, and the use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory inhibitors for prophylaxis and treatment of related diseases.
专利号:WO-9807746-A1 优先权日:1996-08-19 标题:B1-bradykinin receptor antagonists and use thereof 发明人:REGOLI DOMENICO; PLANTE GERARD E; GOBEIL FERNAND; NEUGEBAUER WITOLD A; ZUCCOLLO ADRIANA; CATANZARO ORLANDO L 权利人:UNIV SHERBROOKE; REGOLI DOMENICO; PLANTE GERARD E; GOBEIL FERNAND; NEUGEBAUER WITOLD A; ZUCCOLLO ADRIANA; CATANZARO ORLANDO L 摘要:The present invention relates to novel antagonists to a B1-bradykinin (B1-BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the B1 receptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B1-BK receptors in these two models. B1-BK antagonists abolished the vasocontraction induced by B1-BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels. The present B1-antagonists are useful for treating any condition wherein B1-receptor is expressed, particularly during inflammation, and more particularly wherein B1-receptor expression results in diabetic vasculopathy, other diabetic symptoms associated with an insulitis and a post-capillary resistance building as a consequence of the presence of a B1-receptor.
专利号:US-5723444-A 优先权日:1993-06-03 标 题:Starting materials in the synthesis of thrombin and kinogenase inhibitors
参考文献:10.1016/0162-3109(96)00074-4 摘要:Hess JF, Derrick AW, MacNeil T, Borkowski JA. The agonist selectivity of a mouse B1 bradykinin receptor differs from human and rabbit B1 receptors. Immunopharmacology. 1996 Jun;33(1-3):1–8. doi: 10.1016/0162-3109(96)00074-4. 参考文献:10.1016/0162-3109(96)00060-4 摘要:Siebeck M, Spannagl E, Schorr M, Stumpf B, Fritz H, Whalley ET, Cheronis JC. Effect of combined B1 and B2 kinin receptor blockade in porcine endotoxin shock. Immunopharmacology. 1996 Jun;33(1-3):81–4. doi: 10.1016/0162-3109(96)00060-4. 参考文献:10.1016/0162-3109(96)00019-7 摘要:Schremmer-Danninger E, Offner A, Siebeck M, Heinz-Erian P, Gais P, Roscher AA. Autoradiographic visualization of B1 bradykinin receptors in porcine vascular tissues in the presence or absence of inflammation. Immunopharmacology. 1996 Jun;33(1-3):95–100. doi: 10.1016/0162-3109(96)00019-7. 参考文献:10.1016/0162-3109(96)00024-0 摘要:Zuzack JS, Burkard MR, Cuadrado DK, Greer RA, Selig WM, Whalley ET. Inducible bradykinin B1 receptor in isolated human ileum. Immunopharmacology. 1996 Jun;33(1-3):113–5. doi: 10.1016/0162-3109(96)00024-0. 参考文献:10.1016/0162-3109(96)00027-6 摘要:Abbas F, Clayton J, Marshall K, Scott H, Senior J. Comparison of the effects of bradykinin and related compounds on isolated mouse and human uterus. Immunopharmacology. 1996 Jun;33(1-3):127–9. doi: 10.1016/0162-3109(96)00027-6.