专利号:US-2003157061-A1 优先权日:2001-12-05 标 题 :Combinations of a cyclooxygenase-2 selective inhibitor and a TNFalpha antagonist and therapeutic uses therefor 发明人:BENNETT DENNIS A 权利人:PHARMACIA CORP 摘要:A method for the prevention, treatment, or inhibition of pain, inflammation, or inflammation-related disorder and for the prevention, treatment, or inhibition of a cardiovascular disease or disorder in a subject that is in need of such prevention, treatment or inhibition, involves the administration to the subject of a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist. A method can also involve the treatment, prevention, or inhibition of cancer in a subject in need of such treatment, prevention, or inhibition, by administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist which is selected from the group consisting of a compound that affects the synthesis of TNFα, a compound that inhibits the binding of TNFα with a receptor specific for TNFα, and a compound that interferes with intracellular signaling triggered by TNFα binding with a receptor. Compositions, pharmaceutical compositions and kits that can be used with the methods are also described.
专利号:WO-2023075715-A1 优先权日:2021-10-26 标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids) 发明人:OYTUN FARUK; CAN EFE 权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI 摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.
专利号:WO-2011059609-A9 优先权日:2009-10-13 标 题 :Dendrimer compositions and methods of synthesis
专利号:WO-2011028334-A2 优先权日:2009-08-26 标题:Synthesis and isolation of dendrimer systems
专利号:US-8633204-B2 优先权日:2006-09-15 标 题 :4-methylpyridopyrimidinone compounds 发明人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN 权利人:CHENG HENGMIAO; BHUMRALKAR DILIP; DRESS KLAUS RUPRECHT; HOFFMAN JACQUI ELIZABETH; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; LE PHUONG THI QUY; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; PLEWE MICHAEL BRUNO; TRAN KHANH TUAN; PFIZER 摘要:The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), n nand to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-Kα).
专利号:US-7772246-B2 优先权日:2007-08-01 标题:Pyrazole compounds as RAF inhibitors 发明人:CUI JINGRONG JEAN; DEAL JUDITH GAIL; GU DANLIN; GUO CHUANGXING; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; KEPHART SUSAN ELIZABETH; LINTON MARIA ANGELICA; MCALPINE INDRAWAN JAMES; PAIRISH MASON ALAN; PALMER CYNTHIA LOUISE 权利人:PFIZER 摘要:The present invention is directed to compounds of Formula (I), n nand to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
1: Zhang R, Liu Z, Zhang H, Zhang Y, Lin D. The COX-2-Selective Antagonist (NS-398) Inhibits Choroidal Neovascularization and Subretinal Fibrosis. PLoS One. 2016 Jan 13;11(1):e0146808. doi: 10.1371/journal.pone.0146808. eCollection 2016. 2: Kim J, Shim M. COX-2 inhibitor NS-398 suppresses doxorubicin-induced p53 accumulation through inhibition of ROS-mediated Jnk activation. Mol Carcinog. 2016 Jan 12. doi: 10.1002/mc.22458. [Epub ahead of print] doi: 10.1007/s13277-015-3694-6. doi: 10.1016/j.neuroscience.2014.10.021. Epub 2014 Oct 18. 5: Que W, Li S, Chen J. NS-398 enhances the efficacy of bortezomib against RPMI8226 human multiple myeloma cells. Mol Med Rep. 2013 May;7(5):1641-5. doi: 10.3892/mmr.2013.1394. Epub 2013 Mar 26. doi: 10.1007/s13277-013-0677-3. Epub 2013 Mar 1. Retraction in: Wang X, Liang Y, Wang J, Wang M. Tumour Biol. 2015 Aug;36(9):7297. doi: 10.1016/j.prostaglandins.2012.08.007. Epub 2012 Sep 5.
合成参考文献
参考文献:10.1016/j.bcp.2011.06.028 摘要:Cerella C, Sobolewski C, Chateauvieux S, Henry E, Schnekenburger M, Ghelfi J, Dicato M, Diederich M. COX-2 inhibitors block chemotherapeutic agent-induced apoptosis prior to commitment in hematopoietic cancer cells. Biochem Pharmacol. 2011 Nov 15;82(10):1277–90. doi: 10.1016/j.bcp.2011.06.028. 摘要:Ma XT, Yu LW, Wang S, Zhang H, Du RY, Cui ZR. [Molecular mechanism of cyclooxygenase-2 inhibitor in inhibition of proliferation of colon cancer cells by modulating Stat5 signal transduction pathway]. Zhonghua Yi Xue Za Zhi. 2005 Sep 21;85(36):2566–9. 摘要:Lee SM, Gai WW, Cheung TK, Peiris JS. Antiviral activity of a selective COX-2 inhibitor NS-398 on avian influenza H5N1 infection. Influenza Other Respir Viruses. 2011 May;5(Suppl 1):230–2. 参考文献:10.1007/s12012-011-9127-x 摘要:Panaro MA, Pricci M, Meziani F, Ragot T, Andriantsitohaina R, Mitolo V, Tesse A. Cyclooxygenase-2-derived prostacyclin protective role on endotoxin-induced mouse cardiomyocyte mortality. Cardiovasc Toxicol. 2011 Dec;11(4):347–56. doi: 10.1007/s12012-011-9127-x. 参考文献:10.1016/j.bmc.2011.06.069 摘要:Zhang L, Feng L, Jia Q, Xu J, Wang R, Wang Z, Wu Y, Li Y. Effects of β-glucosidase hydrolyzed products of harpagide and harpagoside on cyclooxygenase-2 (COX-2) in vitro. Bioorg Med Chem. 2011 Aug 15;19(16):4882–6. doi: 10.1016/j.bmc.2011.06.069.