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    • 1. 发明授权
    • Purine derivatives having phosphodiesterase IV inhibition activity
    • 具有磷酸二酯酶IV抑制活性的嘌呤衍生物
    • US06319928B1
    • 2001-11-20
    • US09418331
    • 1999-10-14
    • Mark ChasinDavid J. CavallaPeter HoferPeter WintergerstAndre Gehrig
    • Mark ChasinDavid J. CavallaPeter HoferPeter WintergerstAndre Gehrig
    • C07D47318
    • C07D473/20C07D473/18C07D473/24C07D473/34
    • A compound of the formula: wherein R2 is O or S; R3, R6a and R8 are the same or different and each represent a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl; R6b represents a H or R6a, or together R6b, N, and R6a make a 3 to 8 member ring containing at least one carbon, from one to three nitrogen atoms, from zero to two oxygen atoms, from zero to two sulfur atoms, said ring optionally substituted with alkoxy, CO2H, CONH2, ═NOH, ═NOCONH2, ═O; and where aryl is phenyl or naphthyl, the heterocyclyl is a 5, 6 or 7 membered ring including from one to three nitrogen atoms, and from zero to two oxygen atoms, from zero to two sulfur atoms, and can be substituted as in aryl on the carbons or nitrogens of that ring; or a pharmaceutically acceptable salt thereof, provided that when R3 is propyl, R8 is not cyclopentyl, noradamantyl, or dicyclopropylmethyl.
    • 下式的化合物:其中R 2是O或S; R 3,R 6a和R 8相同或不同,并且各自表示未支链或未支化或被OH,烷氧基,CO 2 H,= NOH = NOCONH2或= O; 未取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基,其中环烷基部分未被取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代; 未取代或被Cl,NH 2,烷基氨基,二烷基氨基,酰氨基,C 1 -C 8烷基酰氨基,C 1 -C 3二烷基氨基,OH,烷氧基,HC = NOH,HC = NOCONH 2,C 1 -C 3烷基,苯基或苄基取代的芳基; 芳烷基(C1-4); 杂环基 杂环基烷基(C1-C4); 和杂芳基; R6b表示H或R6a,或R6b,N和R6a一起形成含有至少一个碳,1-3个氮原子,0至2个氧原子,0至2个硫原子的3至8元环 所述环任选被烷氧基取代,CO 2 H,CONH 2,= NOH,= NOCONH 2,= O; 并且其中芳基为苯基或萘基,杂环基为5,6或7元环,包括1至3个氮原子,0至2个氧原子,0至2个硫原子,并且可以如 该环的碳或氮; 或其药学上可接受的盐,条件是当R 3为丙基时,R 8不是环戊基,去甲金刚烷基或二环丙基甲基。
    • 2. 发明授权
    • Purine derivatives having phosphodiesterase IV inhibition activity
    • 具有磷酸二酯酶IV抑制活性的嘌呤衍生物
    • US06228859B1
    • 2001-05-08
    • US09210556
    • 1998-12-11
    • David J. CavallaMark ChasinPeter HoferAndre GehrigPeter Wintergerst
    • David J. CavallaMark ChasinPeter HoferAndre GehrigPeter Wintergerst
    • C07D47334
    • C07D473/30C07D473/34
    • Disclosed are compounds of the formula (I): wherein R3 is selected from the group consisting of C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said alkyl moiety of said alkoxy or cycloalkoxy substituent is optionally substituted in one position with hydroxy; R8 is selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; or benzyl, wherein said benzyl is optionally substituted in one or two positions with halogen, alkoxy, cycloalkoxy or polycycloalkyl, and wherein said alkyl moiety of said alkoxy or cycloalkoxy is optionally substituted in one position with hydroxy; R6a and R6b are independently selected from the group consisting of hydrogen, C1-10 alkyl, C1-10 alkenyl, C3-10 cycloalkyl, C4-10 cycloalkylalkyl, or C3-10 cycloalkenyl, wherein said alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or cycloalkenyl is optionally substituted in one position with hydroxy; and pharmaceutically acceptable salts thereof.
    • 公开了式(I)的化合物:其中R 3选自C 1-10烷基,C 1-10烯基,C 3-10环烷基,C 4-10环烷基烷基或C 3-10环烯基,其中所述烷基,烯基,环烷基 环烷基烷基或环烯基任选在一个位置被羟基取代; 或苄基,其中所述苄基在一个或两个位置任选被卤素,烷氧基,环烷氧基或多环烷基取代,并且其中所述烷氧基或环烷氧基取代基的所述烷基部分任选在一个位置被羟基取代; R 8选自 的氢,C 1-10烷基,C 1-10烯基,C 3-10环烷基,C 4-10环烷基烷基或C 3-10环烯基,其中所述烷基,烯基,环烷基,环烷基烷基或环烯基任选在一个位置被羟基取代; 或苄基,其中所述苄基在一个或两个位置任选被卤素,烷氧基,环烷氧基或多环烷基取代,并且其中所述烷氧基或环烷氧基的所述烷基部分任选在一个位置被羟基取代; R 6a和R 6b独立地选自 由氢,C 1-10烷基,C 1-10烯基,C 3-10环烷基,C 4-10环烷基烷基或C 3-10环烯基组成的基团,其中所述烷基,链烯基,环烷基,环烷基烷基或环烯基任选在一个位置被羟基取代 ;及其药学上可接受的盐。
    • 5. 发明授权
    • Purine derivatives having phosphodiesterase IV inhibition activity
    • 具有磷酸二酯酶IV抑制活性的嘌呤衍生物
    • US06294541B1
    • 2001-09-25
    • US09418330
    • 1999-10-14
    • David J. CavallaMark ChasinPeter HoferAndre GehrigPeter Wintergerst
    • David J. CavallaMark ChasinPeter HoferAndre GehrigPeter Wintergerst
    • C07D27320
    • C07D473/24C07D473/18C07D473/20C07D473/30C07D473/34
    • A compound of the formula: wherein R3 represent a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl; R8 represents H or a C1-8 alkyl which is unbranched or branched and unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C3-8 cycloalkyl which is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; C4-8 cycloalkylalkyl wherein the cycloalkyl portion is unsubstituted or substituted with OH, alkoxy, CO2H, ═NOH, ═NOCONH2, or ═O; aryl which is unsubstituted or substituted with Cl, NH2, alkylamino, dialkylamino, amido, C1-C8 alkylamido, C1-C3 dialkylamido, OH, alkoxy, HC═NOH, HC═NOCONH2, C1-C3 alkyl, phenyl or benzyl; aralkyl (C1-4); heterocyclyl; heterocyclylalkyl (C1-C4); and heteroaryl.
    • 下式的化合物:其中R 3表示未支链或未支化或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 1-8烷基; 未取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基,其中环烷基部分未被取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代; 未取代或被Cl,NH 2,烷基氨基,二烷基氨基,酰氨基,C 1 -C 8烷基酰氨基,C 1 -C 3二烷基氨基,OH,烷氧基,HC = NOH,HC = NOCONH 2,C 1 -C 3烷基,苯基或苄基取代的芳基; 芳烷基(C1-4); 杂环基 杂环基烷基(C1-C4); R 8表示H或未分支或未被取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 1-8烷基; 未取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代的C 3-8环烷基; C4-8环烷基烷基,其中环烷基部分未被取代或被OH,烷氧基,CO 2 H,= NOH,= NOCONH 2或= O取代; 未取代或被Cl,NH 2,烷基氨基,二烷基氨基,酰氨基,C 1 -C 8烷基酰氨基,C 1 -C 3二烷基氨基,OH,烷氧基,HC = NOH,HC = NOCONH 2,C 1 -C 3烷基,苯基或苄基取代的芳基; 芳烷基(C1-4); 杂环基 杂环基烷基(C1-C4); 和杂芳基。