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-2002010128-A1 优先权日:2000-04-13 标题 :Treatment of hyperproliferative, inflammatory and related mucocutaneous disorders using inhibitors of mevalonate synthesis and metabolism 发明人:PARKS THOMAS P; GRAYSON STEPHEN 摘要:The present invention provides methods for treating a variety of hyperproliferative and inflammatory mucocutaneous disorders, including, basal cell carcinoma, squamous cell carcinoma, psoriasis and atopic dermatitis, as well as skin irritation and disorders associated with skin aging and skin photodamage using inhibitors of cholesterol metabolism. The present invention further relates to the discovery that the combined use of several inhibitors of cholesterol metabolism produces synergistic effects. Furthermore, the present invention is directed to the use of inhibitors of cholesterol metabolism as excipients to enhance the effects of antiinflammatory drugs.
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-4975448-A 优先权日:1983-02-04 标题 :6-amino-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-amino-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-amino-2-benzothiazolesulfonamide compound.
专利号:US-6531614-B2 优先权日:1993-12-15 标题 :Method of prostaglandin synthesis 发明人:CONROW RAYMOND E 权利人:ALCON MFG LTD 摘要:Methods of synthesizing 9-Halo-13,14-dihydroprostaglandins useful in the treatment of glaucoma and ocular hypertension are disclosed. Also disclosed are ophthalmic, pharmaceutical compositions comprising such prostaglandins.
专利号:US-5512577-A 优先权日:1994-06-02 标 题:Bicyclic hexahydroaporphine and 1-benzyloctahydroisoquinoline therapeutic compositions and processes for utilizing said compositions 发明人:ROCHE VICTORIA F; OHIA S EDET; ROCHE EDWARD B 权利人:UNIV CREIGHTON 摘要:The invention relates to the method of synthesis of bicyclic hexahydroaporphine compounds which may provide improved therapy for diseases characterized by an increase in intraocular pressure. More specifically, the present invention relates to the preparation of agents which may provide for improved treatment of patients with glaucoma or ocular hypertension. The present invention describes the intraocular pressure lowering capabilities of several of the bicyclic hexahydroaporphine structures.
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