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US5399584.Pdf |||||||||||||| O US005399584A United States Patent 19) 11 Patent Number: 5,399,584 Ares et al. 45) Date of Patent: Mar. 21, 1995 (54 USE OF FLAVONEDERIVATIVES FOR 75308 2/1982 Romania. GASTROPROTECTION 90578 11/1986 Romania . 75 Inventors: Jeffrey J. Ares, Hamilton, Ohio; 555888 5/1977 U.S.S.R. Sunil V. Kakodkar, Bethlehem, Pa.; OTHER PUBLICATIONS Gary R. Kelm, Cincinnati; Peter D. Remington's Pharmaceutical Sciences, 16th edition, Murray, Fairfield, both of Ohio; (1980) p. 431. Jared L. Randall, Plymouth, N.Y.; Alcaraz, M. J. & J. R. S. Hoult, "Actions of Flavonoids Candice L. Slough, Middletown, and the Novel Anti-Inflammatory Flavone, Hypola Ohio etin-8-Glucoside, on Prostaglandin Biosynthesis and 73) Assignee: The Procter & Gamble Company, Glucoside, on Prostaglandin Biosynthesis and Inactiva Cincinnati, Ohio (List continued on next page.) (21) Appl. No.: 15,771 Primary Examiner-Raymond J. Henley, III ar. Attorney, Agent, or Firm-David L. Suter; Jacobus C. (22 Filed: Feb. 10, 1993 Rasser; Milton B. Graff, IV Related U.S. Application Data 57) ABSTRACT 63 Continuation-in-part of Ser. No. 878,582, May 5, 1992, The subject invention relates to methods for preventing abandoned. or treating damage to the mucosal lining of the gastroin 51) Int. Cl. ..................... A61K 31/38; A61K31/35; testinal tract of a human or lower animal by administer- A61K 31/19; A61K 31/40; A61K 49/00 E. ad effective amount of a compound having (52) U.S.C. .................................... 514/432; 514/413; 514/456; 514/570; 514/922; 514/925; 514/926; 514/927; 424/10 58 Field of Search ............... 514/432, 456, 925, 926, 514/927, 434, 570, 413,922; 424/10 56) References Cited U.S. PATENT DOCUMENTS 3,155,579 il/1964 Perrault................................. 167/65 3,495,009 2/1970 Tronche ... 514/456 4,707,360 1 1/1987 Brasey ....... 54/.456 4,891,356 l/1990 Szabo ...................................... 514/2 5,106,871 4/1992 Komazawa et al. ................ 514/571 wherein X and Y are each independently selected from FOREIGN PATENT DOCUMENTS O and S; R1 y R2 and R3 are each independently selected from hydrogen, hydroxy, halo, unsubstituted or mono 88.8982 9/1981 Belgium . substituted straight or branched C1-C4 alkanyl, and E. 1/33; Epean Pat. Off. unsubstituted or substituted straight or branched C1-C4 48-42448 4/1973 Japan.apan . alkanoxy;- and each 1of R2 R', R5, R63. and R7 is hydrogen or, 48-99312 12/1973 Japan. if one or more of R, R2 and R3 is other than hydrogen, 48-99313 12/1973 Japan . each of R, R, R and R is selected from hydrogen, 51-23268 2/1976 Japan. halo, trifluoromethyl, and unsubstituted straight or 55-27112 2/1980 Japan. branched C1-C4 alkanyl. 55-143913 11/1980 Japan. 3-5424 1/1991 Japan . 19 Claims, No Drawings 5,399,584 Page 2 OTHER PUBLICATIONS Ciaceri, G. & G. Attaguile, "Effects of Luteolin, Apige tion', Biochemical Pharmacology, vol. 34, No. 14 nin, and Acacetin on Experimentally Induced Gastric Ulcer', Minerva Med., vol. 63, No. 29 (1972), pp. (1985), pp. 2477-2482. 1665-668. Arakawa, T., A. Nakamura, H. Yamada, H. Nebiki, H. Corvazier, E. & J. Maclouf, "Interference of Some Satoh, T. Fukoda & K. Kobayashi, "Protection of Gas Flavonoids and Non-Steroidal Anti-Inflammatory tric Surface Epithelial Cells of Rats by 16, 16-Dimethyl Drugs with Oxidative Metabolism of Arachidonic Acid Prostaglandin E2 and Sofalcone, a Synthetic Flavonoid by Human Platelets and Neutrophils', Biochimica et Derivative of Sophoradin, against Ethanol', Digestion, Biophysica Acta, vol. 835 (1985), pp. 315-321. vol. 41 (1988), pp. 61-67. Cristoni, A., S. Malandrino & M.J. Magistretti, “Effect Barnaulov, O. D., O. A. Manicheva, G. G. Zapesoch of a Natural Flavonoid on Gastric Mucosal Barrier', naya, V. L. Shelyuto & V. I. Glyzin, “Effect of Some Arzneim-Forsch., vol.39(I), No. 5 (1989), pp. 590-592. Flavonoids on the Ulcerogenic Activity of Reserpine in Gabor, M. & A. Kekes-Szabo, "Effect of Bioflavoids in Mice', Khim.-Farm. Zh., vol. 16, No. 3 (1982), pp. Experimental Gastric Ulcer', Kiserletes Orvos 300-303. , tudomany, vol. 24, (1972), pp. 1-4. Barnaulov, O. D., O. A. Manicheva & P. P. Denisenko, Goel, R. K. V. B. Pandey, S. P. D. Dwivedi & Y. V. “A Method for Evaluating the Effect of Drugs on the Rao “Antiinflammatory and Anti-Ulcer Effects of Ka Ulcerogenic Activity of Reserpine in Mice”, Farmakol. empferol, a Flavone, isolated from Rhamnus procumb Toksikol. (Moscow), vol. 45, No. 4 (1982), pp. 105-110. ens', Indian Journal of Experimental Biology, vol. 26 Barnaulov, O. D., O. A. Manicheva & N. F. Komis (Feb. 1988), pp. 121-124. sarenko, "Comparative Evaluation of the Effect of Hatamaya, K. S. Yokomori, Y. Kawashina, R. Saziki & Some Flavonoids on Changes in the Gastric Wall of K. Kyogoku, "Anti-Ulcer Effect of Isoprenyl Flavo Reserpine-Treated or Immobilized Mice', Khim.-K- noids. III. Synthesis and Anti-Ulcer Activity of Metab him. Zh., vol. 17, No. 8 (1983), pp. 946-951. olites of 2'Carboxymethoxy-4,4'-bis(3-me Barnaulov, O. D., O.A. Manicheva, V. L. Shelyuto, M. thyl-2-butenyloxy)chalcone' Chemical & Pharmaceu M. Konopleva & V. I. Glyzin, "Effect of Flavonoids on tical Bulletin, vol. 33, No. 4 (Apr., 1985)), 1327-1333. the Development of Experimental Stomach Dystrophy Ilarionov, I., L. Rainova & N. Nakov, “On the Antin in Mice', Khim.-Far. Zh., vol. 18, No. 8 (1984), pp. flammatory and Antiulcer Activity of Some Flavonoids 935-941. Isolated from the Genus Genista L., Farmatsiya (So Barnaulov, O. D., O. A. Manicheva, I. I. Chemesova & fia), vol. 29, No. 6 (1979), pp. 39-46. N. F. Komissarenko, "Comparative Evaluation of the Konturek, S.J., M. E. Kitler, T. Brzozowski & T. Ra Effect of Flavonoids on the Development of Experi decki, "Gastric Protection by Meciadanol-A New mental Lesions of the Mouse Stomach', Khim.-Farm. Synthetic Flavonoid-Inhibiting Histidine Decarboxyl Zh., vol. 18, No. 11 (1984), pp. 1330-1333. ase', Digestive Diseases and Sciences, vol. 31, No. 8 Barnaulov, O. D., O. A. Manicheva, R. K. Yakovlev, (Aug. 1986), pp. 847-852. “Evaluation of the Effects of Flavonoids from the Ae Konturek, S.J., T. Radecki, T. Brzozowski, D. Droz rial Parts of Astragalus Quisqualis Bunge and A. Floc dowicz, I. Piastucki, M. Muramatsu, M. Tanaka & H. cosifolius Sumn. on the Development of Experiemntal Aihara, "Antiulcer and Gastroprotective Effects of Lesions in the Mouse Stomach', Rastit. Resur., vol. 21, Solon, a Synthetic Flavonoid Derivative of Sophora No. 1 (1985), pp. 85-90. din. Role of Endogenous Protaglandins”, European Boughton-Smith, N. K. & B. J. R. Whittle, “Failure of Journal of Pharmacology, vol. 125, (1986), pp. 185-192. the Inhibition of Rat Gastric Mucosal 5-Lipoxygenase Konturek, S.J., T. Mrzozowski, D. Drozdowicz, W. by Novel Acetohydroxamic Acids to Prevent Pawlik, & R. Sendur, "Gastro-protective and Ulcer Ethanol-induced Damage', British Journal of Pharma Healing Effects of Sonon, A Synthetic Flavonoid De cology, vol. 95 (1988), pp. 155-162. rivative of Sophoradin', Hepato-Gastroenterology, Brasseur, T., "Proprietes Anti-inflammatoires de Fla vol. 34 (1987, pp. 164-170. Prostaglandins, European vonoides, J. Pharm. Belg., vol. 44, No. 3 (1989), pp. Journal of Pharmacology, vol. 125, (1986), pp. 185 235-241. (List continued on next page.) 5,399,584 Page 3 OTHER PUBLICATIONS hibitor in Rats', Agents and Actions, vol. 15, No/ 3/4 Kyogoku, K., K. Hatayama, S. Yokomori, R. Saziki, S. (1984), pp. 143-145. Nakane, M. Sasajima, J. Sawada, M. Ohzeki & I. Ta Pfister, J. R., W. E. Wymann, M. E. Schuler & A. P. naka, “Anti-ulcer Effect of Isoprenyl Flavonoids, II. Roskowski, "Inhibition of Histamine-Induced Gastric Synthesis and Anti-ulcer Activity of New Chalcones Secretion by Flavone-6-carboxylic Acids', J. Med. Related to Sophoradin', Chemical & Pharmaceutical Chem., vol. 23 (1980, pp. 335-338. Bulletin, vol. 27, No. 12 (1979), pp. 2943-2953. Rainova, L., N. Nakov, S. Bogdanova, E. Minkov & D. Lin, Y. L. & S. Y. 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