专利号:US-7141238-B2 优先权日:1998-04-02 标题:Compositions for reducing UV-induced inhibition of collagen biosynthesis in human skin 发明人:FISHER GARY J; VOORHEES JOHN J 权利人:UNIV MICHIGAN 摘要:Exposure of human skin to ultraviolet (UV) radiation from the sun not only induces the production of enzymes (matrix metalloproteinases) that degrade collagen, but also inhibits the synthesis of new collagen by inhibiting the synthesis of procollagen. This UV-induced inhibition of the synthesis of collagen can be prevented by the topical application of a retinoid or c-JUN inhibitor to the skin prior to exposure to UV radiation.
专利号:US-2007172520-A1 优先权日:2005-11-18 标题:Immunotargeting of Nonionic Surfactant Vesicles 发明人:VANAUKER MICHAEL; PLAAS ANNA; HOOD ELIZABETH 权利人:UNIV SOUTH FLORIDA 摘要:An immunoniosmes for targeted delivery of therapeutic agents to specific tissues in a host and methods of synthesis of those niosomes. An antibody molecule having specificity for a target antigen, such as a cell surface marker or other marker differentially expressed on a target cell, is covalently coupled to a functionalized membrane constituent. In a particular embodiment the functionalized membrane constituent is polyoxyethylene sorbitan monostearate functionalized with cyanuric chloride. The niosomes of this invention thus provide a composition that enhances internalization or retention of the bioactive agent of the niosome into the cytoplasm of the cells of the target tissue by providing a high degree of target specificity. Furthermore, the membrane vesicle enhances the life of the therapeutic agent by preventing its degradation in the extracellular environment, while exhibiting lower toxicity than can occur with some liposomes. The niosomes of the present invention are thus particularly useful as vehicles for the delivery of therapeutics to specific target cells.
专利号:US-8653238-B2 优先权日:2006-02-27 标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers 发明人:WENDER PAUL A; GOUN ELENA A; JONES LISA R 权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR 摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.
专利号:US-9650407-B2 优先权日:2011-11-02 标 题 :Reprogramming of cellular adhesion 发明人:GARTNER ZEV JORDAN; SELDEN NICHOLAS SCOTT; TODHUNTER MICHAEL E; LIANG SAMANTHA ISABEL; WEBER ROBERT JOSEPH; JEE NOEL YOUNGHO; LIU JENNIFER S 权利人:UNIV CALIFORNIA 摘要:Disclosed are membrane-anchored polynucleotides, and compositions comprising the membrane-anchored polynucleotides. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds and compositions in research and therapeutic applications.
专利号:US-6787668-B2 优先权日:2000-04-13 标 题 :2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors 发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH 权利人:PHARMACIA CORP 摘要:The present invention is directed to a compound of formula I:or a pharmaceutically acceptable salt thereof, wherein:R1 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.
专利号:US-2003134898-A1 优先权日:2001-08-01 标题 :Dual inhibitors of wax ester and cholesteryl ester synthesis for inhibiting sebum production 发明人:HOMAN REYNOLD 摘要:The present invention provides a method of inhibiting sebum production and treating sebaceous gland disorders comprising administering to a patient in need of said treatment an effective amount of a compound that inhibits both acyl-Coenzyme A:cholesteryl acyltransferase (ACAT), and acyl-Coenzyme A:fatty alcohol acyltransferase (AFAT), provided that the compound is not [(2,4,6-triisopropyl-phenyl)-acetyl]-sulfamic acid 2,6-diisopropyl-phenyl ester or a pharmaceutically acceptable salt or solvate thereof. The method of the invention is useful to treat sebaceous gland disorders caused or exacerbated by the overproduction of sebum, including oily skin, acne, seborrhea, perioral dermatitis, rosacea, and corticosteroid-induced acneiform lesions.
1: Akasaka E, Mabuchi T, Manabe Y, Yahagi E, Yamada-Hiruma A, Yamaoka H, Kojima T, Kato M, Ikoma N, Ozawa A, Haruki Y. Long-term efficacy of psoriasis vulgaris treatments: analysis of treatment with topical corticosteroid and/or vitamin D3 analog, oral cyclosporin, etretinate and phototherapy over a 35-year period, 1975-2010. J Dermatol. 2013 Apr;40(4):238-43. doi: 10.1111/1346-8138.12069. Epub 2013 Jan 21. German.
合成参考文献
参考文献:10.1111/j.1346-8138.2011.01235.x 摘要:YAMAMOTO M, TADA Y, ASAHINA A, SAEKI H, ASANO Y, KIMURA T, SUGAYA M, KIKUCHI K, TAMAKI K, SATO S. Severe generalized pustular psoriasis accompanied by bullae formation with increased serum vascular endothelial growth factor level. The Journal of Dermatology. 2011 Jul 18;39(2):183–5. doi: 10.1111/j.1346-8138.2011.01235.x.