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    • 2. 发明授权
    • Method for treating disease states in mammals with naphthalene
lipoxygenase-inhibiting agents
    • 用萘脂氧合酶抑制剂治疗哺乳动物疾病状态的方法
    • US5134161A
    • 1992-07-28
    • US181869
    • 1988-04-15
    • Michael C. VenutiJohn M. Young
    • Michael C. VenutiJohn M. Young
    • C07C46/00C07C50/10C07C50/24C07C50/32
    • C07C46/00C07C50/10C07C50/24C07C50/32Y10S514/886Y10S514/887
    • Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;both X groups are the same and X is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6, whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.The compounds of this invention are also useful for the treatment of disease-states caused by lipoxygenase activity in mammals, particularly 5-lipoxygenase activity, when administered systemically.
    • 哺乳动物中的牛皮癣通过局部施用下式的萘来减轻:其中:R 1是低级烷氧基或任选取代的苯氧基,R 2与R 1相同,或R 2是氢,低级烷基,任选取代的苯基或任选地 取代的苯基烷基,R 3是氢,低级烷基,低级烷氧基,卤素,任选取代的苯基,任选取代的苯基 - 低级烷基或任选取代的苯基 - 低级烷氧基,m是1或2; 两个X基团相同,X是-C(O)OR 4或-C(O)NR 5 R 6,其中R 4是烷基,任选被一个或两个低级烷基,低级烷氧基或卤素取代的苯基或苄基; 且R 5和R 6独立地为氢,低级烷基,环烷基或任选被一个或两个低级烷基,低级烷氧基或卤素取代的苯基。 当系统给药时,本发明的化合物也可用于治疗由哺乳动物的脂氧合酶活性引起的疾病状态,特别是5-脂氧合酶活性。
    • 6. 发明授权
    • Transglutaminase inhibitors
    • 转谷氨酰胺酶抑制剂
    • US4970297A
    • 1990-11-13
    • US25426
    • 1987-03-13
    • Arlindo L. CastelhanoDiana H. PliuraMichael C. Venuti
    • Arlindo L. CastelhanoDiana H. PliuraMichael C. Venuti
    • A61K38/00C07D261/04C07K5/06
    • C07D261/04C07K5/06191A61K38/00Y02P20/55
    • This invention is directed to compounds of the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein:n is 0, 1 or 2;p and q are independently 0, 1 or 2 and the sum of (p+q) is less than or equal to 3;X is selected from the group consisting of: halo; --OR.sup.2, --SR.sup.2, --S(O)R.sup.2, --S(O).sub.2 R.sup.2, and --S(O).sub.2 NHR.sup.2, wherein R.sup.2 is lower alkyl, mono-, di- or tri-fluoro alkyl of 2 or 3 carbon atoms, optionally substituted aryl;R is H or an N-protecting group;R.sup.1 is alkylthio, arylthio, amino, alkylamino, optionally substituted arylamino, or optionally substituted aralkylamino; and when the sum of n+p+q is greater than or equal to one, R.sup.1 is also hydroxy, alkoxy, or aralkoxy; andeach (aa) is independently an .alpha.-amino acid residue with an optionally protected amino acid side chain.
    • 本发明涉及下式的化合物:其中n为0,1或2;其中:n为0,1或2; p和q独立地为0,1或2,(p + q)的和小于或等于3; X选自:卤素; -OR 2,-SR 2,-S(O)R 2,-S(O)2 R 2和-S(O)2 NHR 2,其中R 2是低级烷基,2或3个碳原子的一,二或三氟烷基 ,任选取代的芳基; R为H或N-保护基; R 1是烷硫基,芳硫基,氨基,烷基氨基,任选取代的芳基氨基或任选取代的芳烷基氨基; 并且当n + p + q的总和大于或等于1时,R 1也是羟基,烷氧基或芳烷氧基; 并且每个(aa)独立地是具有任选保护的氨基酸侧链的α-氨基酸残基。
    • 8. 发明授权
    • (2-Oxo-1,2,3,5-tetrahydroimidazo-[2,1-B]quinazolinyl) oxyalkylamides
properties having phosphodiosterase inhibiting
    • (2-氧代-1,2,3,5-四氢咪唑并[2,1-B]喹唑啉基)氧烷基酰胺性质,其具有磷酸二酯酶抑制
    • US4690925A
    • 1987-09-01
    • US734633
    • 1985-05-15
    • John H. FriedMichael C. Venuti
    • John H. FriedMichael C. Venuti
    • A61K31/505A61P7/02A61P9/00A61P35/00A61P43/00C07C205/44C07C205/56C07D487/04C12N9/99
    • C07D487/04C07C205/44C07C205/56
    • Compounds according to the formula ##STR1## , its optical isomers, or a pharmaceutically acceptable salt thereof wherein:m and n are integers of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or .alpha.-amino acid side chains;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.6, halo, --NH.sub.2, --N(R.sub.6).sub.2, --NHCOR.sub.6, --COOH, or --COO(R.sub.6) group wherein R.sub.6 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an --NH.sub.2, --N(R.sub.6).sub.2, --NHCOR.sub.6, --COOH, or --COOR.sub.6 group wherein R.sub.6 is lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy; andZ is --OR.sub.7 or --NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or lower alkyl.
    • 式(I)的化合物,其旋光异构体或其药学上可接受的盐,其中:m和n为1至6的整数; R1是氢或1至4个碳的烷基; R2是氢或R1和R2组合形成氧代基团; R3为氢,1-6个碳原子的烷基,苯基,苄基,羟基低级烷基及其1至6个碳原子的脂族酰化物或7至12个碳原子的芳基酰化物,氨基甲酰基烷基,羧基烷基,烷氧基羰基烷基或α-氨基酸侧 链条 R4是氢,1-6个碳原子的烷基,苄基或羟基低级烷基; R5是氢,1至6个碳原子的烷基,3至8个碳原子的环烷基或4-12个碳原子的环烷基低级烷基,其中环烷基环是未取代的或被低级烷基,低级烷氧基,-OH,-OCOR6 ,卤素,-NH 2,-N(R 6)2,-NHCOR 6,-COOH或-COO(R 6)基团,其中R 6是低级烷基; 苯基或苯基低级烷基,其中苯基未被取代或被1个或多个低级烷基,卤代或低级烷氧基或-NH 2,-N(R 6)2,-NHCOR 6,-COOH或-COOR 6基团取代,其中R 6是低级烷基 ; Y是氢,1-4个碳原子的烷基,卤代或低级烷氧基; 并且Z是-OR 7或-NR 7 R 8,其中R 7和R 8独立地是氢或低级烷基。