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    • 32. 发明授权
    • Method of using (H.sup.+ /K.sup.+)ATPase inhibitors as antiviral agents
    • 使用(H + / K +)ATP酶抑制剂作为抗病毒剂的方法
    • US5945425A
    • 1999-08-31
    • US737251
    • 1996-10-24
    • Alan E. MoormannDaniel P. BeckerDaniel L. FlynnHui LiClara I. Villamil
    • Alan E. MoormannDaniel P. BeckerDaniel L. FlynnHui LiClara I. Villamil
    • A61K31/00A61K31/4164A61K31/4184A61K31/437A61K31/4402A61K31/4439C07D235/28C07D401/12C07D403/12A61K31/42A61K31/415A61K31/425
    • C07D401/12A61K31/00A61K31/4164A61K31/4184A61K31/437A61K31/4402A61K31/4439C07D235/28C07D403/12
    • A class of compounds which are (H.sup.+ /K.sup.+)ATPase inhibitors can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula III: ##STR1## wherein D is N or CH; wherein R.sup.7 is one or more radicals selected from hydrido, alkoxy, amino, cyano, nitro, hydroxyl, alkyl, halo, haloalkyl, carboxyl, alkanoyl, nitro, amino, alkylamino, aminocarbonyl, aminosulfonyl, alkylaminocarbonyl, alkylcarbonylamino, alkoxycarbonyl, alkylaminosulfonyl, alkylsulfonylamino, alkylthio, alkylsulfinyl and alkylsulfonyl; wherein R.sup.8 is selected from hydrido, alkyl and cycloalkyl; wherein R.sup.9 is one or more radicals selected from hydrido, alkoxy, amino, alkyl, halo, cyano, nitro, hydroxyl, haloalkyl, nitro, carboxyl, alkanoyl, amino, alkylamino, dialkylamino, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, aminosulfonyl, alkylaminosulfonyl, alkylsulfonylamino, alkoxycarbonyl, alkylthio, alkylsulfinyl and alkylsulfonyl; and wherein R.sup.10 and R.sup.11 are independently selected from hydrido, alkyl, aryl, alkylcarbonyl and arylcarbonyl wherein the aryl ring may be further substituted with one or more radicals selected from alkyl, halo, hydrazidylcarbonyl, aminocarbonyl and alkoxy; or wherein R.sup.10 and R.sup.11 together with the nitrogen atom form a heterocyclic ring.
    • PCT No.PCT / US95 / 05021 Sec。 371日期1996年10月24日第 102(e)日期1996年10月24日PCT提交1995年5月1日PCT公布。 出版物WO95 / 29897 1995年11月9日,一类(H + / K +)ATP酶抑制剂的化合物可用于治疗病毒感染。 特别感兴趣的化合物由式III定义:其中D是N或CH; 其中R7是一个或多个选自氢,烷氧基,氨基,氰基,硝基,羟基,烷基,卤素,卤代烷基,羧基,烷酰基,硝基,氨基,烷基氨基,氨基羰基,氨基磺酰基,烷基氨基羰基,烷基羰基氨基,烷氧基羰基,烷基氨基磺酰基, ,烷硫基,烷基亚磺酰基和烷基磺酰基; 其中R8选自氢,烷基和环烷基; 其中R9是一个或多个选自氢,烷氧基,氨基,烷基,卤素,氰基,硝基,羟基,卤代烷基,硝基,羧基,烷酰基,氨基,烷基氨基,二烷基氨基,氨基羰基,烷基氨基羰基,烷基羰基氨基,氨基磺酰基,烷基氨基磺酰基, ,烷氧基羰基,烷硫基,烷基亚磺酰基和烷基磺酰基; 并且其中R 10和R 11独立地选自氢,烷基,芳基,烷基羰基和芳基羰基,其中所述芳基环可以进一步被一个或多个选自烷基,卤素,肼基羰基,氨基羰基和烷氧基的基团取代; 或其中R 10和R 11与氮原子一起形成杂环。
    • 36. 发明授权
    • Meso-azanoradamantanes
    • 中 - 阿氮杂多金刚烷
    • US5530018A
    • 1996-06-25
    • US192213
    • 1994-02-04
    • Daniel P. BeckerDaniel L. FlynnClara I. Villamil
    • Daniel P. BeckerDaniel L. FlynnClara I. Villamil
    • C07D471/18A61K31/40C07D487/04
    • C07D471/18
    • This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfonyl optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfonyl and nitro;n is 0, 1 or 2;m is 0 or 1;X is 0 or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.
    • 本发明涉及下式的化合物或其药学上可接受的盐,其中Z选自由下列组成的组:R1是1-6个碳原子的烷氧基; R 2,R 3,R 4和R 5相同或不同,并且选自氢,卤素,CF 3,羟基,1至6个碳原子的烷氧基,2至7个碳原子的酰基,氨基,被1个 或两个1-6个碳原子的烷基,C 2 -C 7酰基氨基,氨基羰基,任选被1至6个碳原子的一个或两个烷基取代的氨基磺酰基,C 1 -C 6烷基磺酰基和硝基; n为0,1或2; m为0或1; X为0或NR7; 且R 7为氢或1至6个碳原子的烷基。