专利号:US-5134146-A 优先权日:1990-05-13 标题:Substituted oxadiazoles and thiadiazoles for use in the treatment of glaucoma 发明人:SHOWELL GRAHAM; LOTTI VICTOR 权利人:MERCK SHARP & DOHME 摘要:The use of compounds for formula (I): ##STR1## or a salt or prodrug thereof; wherein one of X, Y, or Z is an oxygen or sulphur atom and the other two are nitrogen atoms, and the dotted circle represents two double bonds thus forming a 1,3,4-oxadiazole, 1,2,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-thiadiazole nucleus; n R 1 represents a non-aromatic azacyclic or azabicyclic ring system selected from ##STR2## wherein the broken line represents an optional chemical bond; the substituents R 3 and R 4 may be present at any position, including the point of attachment to the oxa- or thia-diazole ring, and independently represent hydrogen, C 1-4 alkyl, halo, C 1-4 alkoxy, hydroxy or carboxy, or R 3 and R 4 together represent carbonyl; n the group R 5 represents hydrogen or C 1-4 alkyl; and n R 2 represents hydrogen, C 1-8 hydrogen, C 1-8 alkyl optionally substituted by hydroxy or fluoro, C 2-8 alkenyl, OR 7 , SR 7 , NR 7 R 8 , CN, CO 2 R 7 , CONR 7 R 8 OR NHCONHR 9 where R 9 is C 1-4 alkyl; wherein R 7 and R 8 independently represent hydrogen or saturated or unsaturated C 1-4 alkyl provided that, when R 7 and R 8 in NR 7 R 8 are both hydrogen, at least one of R 3 and R 4 is C 1-4 alkyl, n in the treatment of glaucoma, novel compounds having such use, formulations containing them and their synthesis.
专利号:US-4975447-A 优先权日:1983-02-04 标 题:6-hydroxyethoxy-2-benzothiazolesulfonamide and topical treatment compositions and method for glaucoma 发明人:SCHOENWALD RONALD D; BARFKNECHT CHARLES F 权利人:UNIV IOWA RES FOUND 摘要:A topical composition for eye treatment of glaucoma, comprising a small but pharmaceutically effective amount of an analog of benzothiazole-2-sulfonamide. The most preferred compound is 6-hydroxyethoxy-2-benzothiazolesulfonamide. The invention also relates to a method of topically treating glaucoma with eye drops to reduce intraocular pressure. Finally, disclosed is a method of synthesis of the preferred and highly effective benzothiazole-2-sulfonamide analogs, particularly the 6-hydroxyethoxy-2-benzothiazolesulfonamide compound.
专利号:US-2014315720-A1 优先权日:2012-10-24 标 题 :Polysaccharide ester microspheres and methods and articles relating thereto 发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY 权利人:CELANESE ACETATE LLC 摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.
1: Gonzalez VH, Uram M, Schupp A, Widmann M, Novack GD. AG-920 (Articaine) Ophthalmic Solution: A Masked, Active-Controlled Evaluation of Its Local Anesthetic Efficacy and Safety in Pediatric Patients. J Ocul Pharmacol Ther. 2024 Jun;40(5):293-296. doi: 10.1089/jop.2023.0187. Epub 2024 Apr 22. 50(6):274-275. doi: 10.1097/ICL.0000000000001083. Epub 2024 Mar 13. 2024 Jan–. 43(8):1386-1392. doi: 10.1097/IAE.0000000000003824. 61(4):393-401. doi: 10.1093/chromsci/bmac039. 2021:8661098. doi: 10.1155/2021/8661098. 7: Taleb A, Zhou YP, Meng LT, Zhu MY, Zhang Q, Naveed M, Li LD, Wang P, Zhou QG, Meng F, Han F. New application of an old drug proparacaine in treating epilepsy via liposomal hydrogel formulation. Pharmacol Res. 2021 Jul;169:105636. doi: 10.1016/j.phrs.2021.105636. Epub 2021 Apr 29. 41(2):465-473. doi: 10.1007/s10792-020-01596-x. Epub 2020 Oct 23.
合成参考文献
参考文献:10.1111/j.1475-1313.2011.00862.x 摘要:Logan NS, Shah P, Rudnicka AR, Gilmartin B, Owen CG. Childhood ethnic differences in ametropia and ocular biometry: the Aston Eye Study. Ophthalmic Physiol Opt. 2011 Sep;31(5):550–8. doi: 10.1111/j.1475-1313.2011.00862.x.