专利号:US-7211598-B2 优先权日:2002-06-28 标 题:Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:GARVEY DAVID S; RANATUNGE RAMANI R; RICHARDSON STEWART K 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor having at least one oxime group or hydrazone group, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor having at least one oxime group or hydrazone group, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention having at least one oxime group or hydrazone group can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-4833271-A 优先权日:1985-08-23 标 题 :Structurally defined oligomers and preparation thereof for the protection of oxidative phosphorylation and which exhibit ionophoretic activity 发明人:NELSON GEORGE L 权利人:NELSON GEORGE L 摘要:Structurally-defined, low molecular weight oligomers and preparation thereof which are active in the protection of oxidative physphorylation of mitochondria and exhibit ionophoretic activity. Said structurally defined low molecular weight oligomers are synthesized using a modified 15-dehydro PGB1 such as 16,16-dimethyl-15-dehydro prostaglandin B1 as a precursor to obtain oligomeric mixtures which are structurally defined and active in the protection of oxidative phosphorylation and exhibit ionophoretic activity. Synthesis of modified 15-dehydro-PGB1; 16,16-dimethyl-15-dehydro-prostagalandin B1; is also described.
专利号:US-7442802-B2 优先权日:2002-06-27 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
专利号:US-5446062-A 优先权日:1993-11-12 标 题:((4-alkoxypyran-4-yl) substituted) ether, arylalkyl-, arylalkenyl-, and arylalkynyl)urea inhibitors of 5-lipoxygenase 发明人:DELLARIA JOSEPH F; BASHA ANWER; BLACK LAWRENCE A; CHERNESKY LINDA J; LEE WENDY 权利人:ABBOTT LAB 摘要:Compounds of the structure where W is selected from where Q is oxygen or sulfur, R6 and R7 are hydrogen or alkyl, or R6 and R7, together with the nitrogen atoms to which they are attached, define a radical of formula Z is -CH2-, oxygen, sulfur, or -NR9, L1 and L2 are selected from a valence bond, alkylene, propenylene, and propynylene; R1 and R2 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is selected from oxygen, >NR10, and L3 is selected from alkylene of one to three carbon atoms, propenylene, propynylene, and R3, R4, and R5 are hydrogen or alkyl of one to four carbon atoms inhibit the synthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
专利号:US-5530114-A 优先权日:1990-04-30 标 题:Oligonucleotide modulation of arachidonic acid metabolism 发明人:BENNETT CLARENCE F; ECKER DAVID J; CROOKE STANLEY T; MIRABELLI CHRISTOPHER K 权利人:ISIS PHARMACEUTICALS INC 摘要:PCT No. PCT/US91/02628 Sec. 371 Date Apr. 3, 1992 Sec. 102(e) Date Apr. 3, 1992 PCT Filed Apr. 17, 1991 PCT Pub. No. WO91/16901 PCT Pub. Date Nov. 14, 1991.Compositions and methods are provided for the treatment and diagnosis of diseases amenable to modulation of the synthesis or metabolism of arachidonic acid and related compounds. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are provided which are specifically hybridizable with nucleic acids encoding 5-lipoxygenase, 5-lipoxygenase activating proteins, LTA4 hydrolase, phospholipase A2, phospholipase C, and coenzyme A-independent transacylase. The oligonucleotide comprises nucleotide units sufficient in identity and number to effect said specific hybridization. In other preferred embodiments, the oligonucleotides are specifically hybridizable with a transcription initiation site, a translation initiation site, and intron/exon junction. Methods of treating animals suffering from disease amenable to therapeutic intervention by modulating arachidonic acid synthesis or metabolism with an oligonucleotide or oligonucleotide analog specifically hybridizable with RNA or DNA corresponding to one of the foregoing proteins are disclosed. Methods for treatment of diseases responding to modulation of arachidonic acid synthesis or metabolism are disclosed.
专利号:US-9750749-B2 优先权日:2010-05-03 标题 :Methods of treating thyroid eye disease 发明人:PHIPPS RICHARD P; GUO NAXIN; FELDON STEVEN 权利人:PHIPPS RICHARD P; GUO NAXIN; FELDON STEVEN; UNIV ROCHESTER 摘要:The present invention relates to a methods and compositions for the treatment of and management of symptoms for thyroid eye disease. The methods include administering to a patient having thyroid eye disease an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space. The pharmaceutical compositions that includes a carrier suitable for ophthalmic delivery and an agent that interferes with hyaluronan synthesis. Combination therapies are also disclosed.
1: Zhang Y, Zhou J, Yang T, Li X, Zhang Y, Huang Z, Mattos GJ, Tiuftiakov NY, Wu Y, Gao J, Qin Y, Bakker E. Complexation Behavior and Clinical Assessment of Isomeric Calcium Ionophores of ETH 1001 in Polymeric Ion-Selective Membranes. ACS Sens. 2024 Dec 27;9(12):6512-6519. doi: 10.1021/acssensors.4c01907. Epub 2024 Nov 25. 59(26):10426-10430. doi: 10.1002/anie.202002417. Epub 2020 Apr 15. 85(2):1006-12. doi: 10.1021/ac3027838. Epub 2012 Dec 31. 82(22):9425-32. doi: 10.1021/ac102099p. Epub 2010 Oct 26. 81(17):7416-9. doi: 10.1021/ac901220d. 63(1):61-71. doi: 10.1016/j.talanta.2003.12.050. 22(12):1581-4. doi: 10.2116/analsci.22.1581. 6(10):1362-8. doi: 10.1039/b603364d. Epub 2006 Aug 14. 385(8):1477-82. doi: 10.1007/s00216-006-0607-y. Epub 2006 Jul 18. 53(1):35-44. doi: 10.2170/jjphysiol.53.35. 75(1):141-4. doi: 10.1021/ac025916y. 18(2-3):111-8. doi: 10.1016/s0956-5663(02)00164-1. 74(11):2603-7. doi: 10.1021/ac011160b. 70(8):1477-88. doi: 10.1021/ac970761t. 70(9):1686-91. doi: 10.1021/ac970903j. 236(2):327-30. doi: 10.1006/abio.1996.0174. 68(3):503-8. doi: 10.1021/ac950789+. 210(1):119-22. doi: 10.1006/abio.1993.1160. 40(1):79-95. doi: 10.2170/jjphysiol.40.79. 29(2):139-42. doi: 10.1016/0165-0270(89)90025-3. 7.
合成参考文献
参考文献:10.1186/s40538-022-00370-8 摘要:Pantoja-Guerra M, Valero-Valero N, Ramírez CA. Total auxin level in the soil–plant system as a modulating factor for the effectiveness of PGPR inocula: a review. Chem. Biol. Technol. Agric. 2023 Jan 27;10(1). doi: 10.1186/s40538-022-00370-8.