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    Pharmaceutically active compounds
    3.
    发明授权
    Pharmaceutically active compounds 失效
    药物活性化合物

    公开(公告)号：US06794387B2

    公开(公告)日：2004-09-21

    申请号：US10099264

    申请日：2002-03-14

    申请人： Charlotte Moira Norfor Allerton ,  Kevin Neil Dack ,  Mark Ian Kemp

    发明人： Charlotte Moira Norfor Allerton ,  Kevin Neil Dack ,  Mark Ian Kemp

    IPC分类号： C07D48704

    CPC分类号： C07D487/04

    摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X, Y and A have the meanings given herein which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

    摘要翻译： 通式（I）的化合物：其中R 1，R 2，R 3，R 4，X，Y和A具有本文给出的用于治疗和预防性治疗 需要抑制环鸟苷3'，5'-单磷酸磷酸二酯酶（如cGMP PDE5）的医疗条件。

    Fungicidal triazolopyrimid-7-ylideneamines
    5.
    发明授权
    Fungicidal triazolopyrimid-7-ylideneamines 失效
    杀真菌三唑并嘧啶-7-亚胺

    公开(公告)号：US06747033B2

    公开(公告)日：2004-06-08

    申请号：US09879258

    申请日：2001-06-12

    申请人： Waldemar Pfrengle

    发明人： Waldemar Pfrengle

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  A01N43/90

    摘要： Compounds of formula I in which R1 is alkyl, alkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, trihydrocarbylsilyl, formyl, alkanoyl or alkoxycarbonyl group being attached either to the nitrogen in the 3- or 4-position; R2 is hydrogen, alkyl, alkenyl, alkynyl, alkadienyl, haloalkyl, cycloalkyl, bicycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic groups containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R3 is phenyl, cycloalkyl or 5- or 6-membered heteroaryl containing besides carbon atoms one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom as ring members; R4 is halogen, amino, alkoxy, haloalkoxy, alkylamino or dialkylamino; wherein the bent line indicates that the double Bond may be located between the 3- and 9-position or the 4- and 9-Position; and the zigzag line indicates that the groups connected may have the (E)- or (Z)-configuration; R1 to R4 groups may be unsubstituted or substituted as defined in the description; processes for preparing these compounds, constituents comprising them and their use for controlling harmful fungi are described.

    摘要翻译： 式Iin的化合物，其中R 1是烷基，烷氧基烷基，环烷基烷基，烯基，炔基，链烯基，卤代烷基，三烃基甲硅烷基，甲酰基，烷酰基或烷氧基羰基，其连接在3-或4-位的氮上; R 2， 含有1至4个氮原子或1至3个氮原子和1个硫或氧原子的5或6元杂芳基或杂环基，可以是氢，烷基，烯基，炔基，链烯基，卤代烷基，环烷基， R 3是苯基，环烷基或除了碳原子一至四个氮原子或一至三个氮原子以及一个硫或氧原子作为环成员的5-或6-元杂芳基; R 4是卤素 ，氨基，烷氧基，卤代烷氧基，烷基氨基或二烷基氨基;其中所述弯曲线表示双键可位于3-和9-位之间或4-和9-位; 和之字形线表示组 可以具有（E） - 或（Z） - 构型; R 1至R 4基团可以是未被描述的或如说明书中所定义的取代基;制备这些化合物的方法，包含它们的组分及其用于控制 描述有害真菌。

    Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction
    6.
    发明授权
    Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′—monophosphate phosphodiesterase (cGMP PDE5) for the treatment of sexual dysfunction 失效
    抑制5型环鸟嘌呤3'，5'-单磷酸磷酸二酯酶（cGMP PDE5）治疗性功能障碍的吡唑并嘧啶酮

    公开(公告)号：US06723719B1

    公开(公告)日：2004-04-20

    申请号：US09402229

    申请日：1999-09-29

    申请人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    发明人： Mark Edward Bunnage ,  John Paul Mathias ,  Stephen Derek Albert Street ,  Anthony Wood

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  C07D231/40

    摘要： Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R1 is C1 to C3 alkyl substituted with C3 to C6 cycloalkyl, CONR5R6 or a N-linked heterocyclic group; (CH2)nHet or (CH2)nAr; R2 is C1 to C6 alkyl; R3 is C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy; R4 is SO2NR7R8; R5 and R6 are each independently selected from H and C1 to C4 alkyl optionally substituted with C1 to C4 alkoxy, or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic group; R7 and R8, together with the nitrogen atom to which they are attached, form a 4-R10-piperazinyl group; R10 is H or C1 to C4 alkyl optionally substituted with OH, C1 to C4 alkoxy or CONH2; H is an optionally substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors useful in the treatment of, inter alia, male erectile dysfunction and female sexual dysfunction.

    摘要翻译： 式（IA）和（IB）化合物或其药学或兽医学上可接受的盐，或任一实体的药学上或兽医学上可接受的溶剂化物，其中R 1为被C 3至C 6环烷基取代的C 1至C 3烷基，CONR 5 R 6或N-连接的杂环基; （CH2）nHet或（CH2）nAr; R 2是C 1至C 6烷基; R 3是任选被C 1至C 4烷氧基取代的C 1至C 6烷基; R 4是SO 2 NR 7 R 8; R 5和R 6各自独立地选自H和任选被C 1至C 4烷氧基取代的C 1至C 4烷基，或与它们所连接的氮原子一起形成5-或6-元杂环 组; R 7和R 8与它们所连接的氮原子一起形成4-R 10 - 哌嗪基; R 10是H或任选被OH，C 1至C 4烷氧基或CONH 2取代的C 1至C 4烷基; H是任选取代的C连接的5或6元杂环基; Ar是任选取代的苯基; 并且n为0或1; 是用于治疗男性勃起功能障碍和女性性功能障碍的有效和选择性的cGMP PDE5抑制剂。

    Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors
    10.
    发明授权
    Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors 失效
    治疗p38激酶相关病症的方法和可用作激酶抑制剂的吡咯并三嗪化合物

    公开(公告)号：US06670357B2

    公开(公告)日：2003-12-30

    申请号：US10036293

    申请日：2001-11-07

    申请人： Katerina Leftheris ,  John Hynes ,  Stephen T. Wrobleski ,  Joel Barrish

    发明人： Katerina Leftheris ,  John Hynes ,  Stephen T. Wrobleski ,  Joel Barrish

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  C07D207/50

    摘要： Methods of treating one or more conditions associated with p38 kinase activity are disclosed comprising administering to a patient in need thereof at least one compound having the formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R3 is hydrogen, methyl, perfluoromethyl, methoxy, halogen, cyano, or NH2, preferably methyl, and X, R1 through R6, and Z are as described in the specification. Advantageously the groups —ZR4R5 taken together comprise an —NH-substituted aryl.

    摘要翻译： 公开了治疗与p38激酶活性相关的一种或多种病症的方法，包括向有需要的患者施用至少一种具有式（I）的化合物或其药学上可接受的盐，前药或溶剂化物，其中R 3是氢， 甲基，全氟甲基，甲氧基，卤素，氰基或NH 2，优选甲基，X，R 1至R 6和Z如说明书所述。 有利的是基团-ZR 4 R 5一起包含-NH-取代的芳基。