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    Biphenyl vasopressin agonists
    4.
    发明授权
    Biphenyl vasopressin agonists 失效

    公开(公告)号：US06903091B2

    公开(公告)日：2005-06-07

    申请号：US10121156

    申请日：2002-04-11

    申请人： Amedeo A. Failli ,  Thomas J. Caggiano ,  Jay S. Shumsky ,  Eugene J. Trybulski ,  Kevin A. Memoli ,  John P. Dusza

    发明人： Amedeo A. Failli ,  Thomas J. Caggiano ,  Jay S. Shumsky ,  Eugene J. Trybulski ,  Kevin A. Memoli ,  John P. Dusza

    IPC分类号： A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/5517 ,  A61P5/02 ,  A61P13/00 ,  A61P13/02 ,  C07D243/10 ,  C07D243/38 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04 ,  A61P3/10

    CPC分类号： C07D243/10 ,  C07D243/38 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04

    摘要： A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or (3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

    Biphenyl vasopressin agonists
    6.
    发明授权
    Biphenyl vasopressin agonists 失效
    联苯加压素激动剂

    公开(公告)号：US07465722B2

    公开(公告)日：2008-12-16

    申请号：US11502982

    申请日：2006-08-11

    申请人： Amedeo A. Failli ,  John P. Dusza ,  Thomas J. Caggiano ,  Jay S. Shumsky ,  Kevin A. Memoli ,  Eugene J. Trybulski

    发明人： Amedeo A. Failli ,  John P. Dusza ,  Thomas J. Caggiano ,  Jay S. Shumsky ,  Kevin A. Memoli ,  Eugene J. Trybulski

    IPC分类号： C07D487/02 ,  A61K31/551

    CPC分类号： C07D243/10 ,  C07D243/38 ,  C07D401/06 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04

    摘要： A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or(2) a 5-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, (C1-C6) lower alkoxy, or halogen; or(3) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; represents a 5-membered aromatic (unsaturated) heterocyclic ring having one sulfur atom, optionally substituted by (C1-C6) lower alkyl, halogen, or (C1-C6) lower alkoxy; R1 is a moiety of the formula and R2, R3, R7, R8 and R9 are, independently, selected from a group consisting of hydrogen, (C1-C3) lower alkyl, OCH3, halogen, CF3, —SCH3, OCF3, SCF3, or CN; or a pharmaceutically acceptable salt, or pro-drug form thereof.

    摘要翻译： 式（I）或（II）的化合物：其中：Y是选自NR或 - （CH 2）n的部分; 其中R是氢或（C1-C6）低级烷基，n是1; （C1-C6）低级烷基，卤素，氰基，CF3，羟基，（C1-C6）低级烷氧基，（C1-C6）低级烷氧基，（C1-C6）低级烷氧基，（C1-C6） C 1 -C 6低级烷氧基羰基，羧基-CONH 2，-CONH [（C 1 -C 6）低级烷基]，-CON [（C 1 -C 6）低级烷基] 或（2）任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的具有一个氮原子的6元芳族（不饱和）杂环; 表示：（1）任选被一个或两个取代基取代的苯环，所述取代基独立地选自氢，（C 1 -C 6）低级烷基，卤素，氰基，CF 3，羟基，（C 1 -C 6）低级烷氧基或 （C 1 -C 6）低级烷氧基羰基，羧基，-CONH 2，-CONH [（C 1 -C 6）低级烷基]，-CON [（C 1 -C 6）低级烷基] 或（2）任选被（C 1 -C 6）低级烷基，（C 1 -C 6）低级烷氧基或卤素取代的具有一个氮原子的5元芳族（不饱和）杂环; 或（3）具有一个氮原子，任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的6元芳族（不饱和）杂环; 表示任选被（C 1 -C 6）低级烷基，卤素或（C 1 -C 6）低级烷氧基取代的具有一个硫原子的5元芳族（不饱和）杂环; R1是下式的部分，R2，R3，R7，R8和R9独立地选自氢，（C1-C3）低级烷基，OCH3，卤素，CF3，-SCH3，OCF3，SCF3， 或CN; 或其药学上可接受的盐或其前体药物形式。

    Tricyclic pyridine N-oxides vasopressin agonists
    7.
    发明授权
    Tricyclic pyridine N-oxides vasopressin agonists 失效
    三环吡啶N-氧化物加压素激动剂

    公开(公告)号：US06235900B1

    公开(公告)日：2001-05-22

    申请号：US09494929

    申请日：2000-02-01

    申请人： Amedeo A. Failli ,  Jay S. Shumsky ,  Eugene J. Trybulski

    发明人： Amedeo A. Failli ,  Jay S. Shumsky ,  Eugene J. Trybulski

    IPC分类号： C07D22318

    CPC分类号： C07D471/04

    摘要： The present invention provides compounds of the general formula: as well as methods and pharmaceutical compositions utilizing these compounds for the inducement of temporary delay of urination or the treatment of disorders which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders.

    摘要翻译： 本发明提供了以下通式的化合物：以及利用这些化合物诱导临时延迟排尿或治疗可由血管加压素激动剂活性（包括尿崩症，夜间遗尿）补救或缓解的病症的方法和药物组合物 ，夜尿症，尿失禁，出血和凝血障碍。

    Substituted tetrahydro-pyrimidine-2(1H)-thione HDL-C elevators useful as antiatherosclerotic agents
    9.
    发明授权
    Substituted tetrahydro-pyrimidine-2(1H)-thione HDL-C elevators useful as antiatherosclerotic agents 失效
    用作抗动脉粥样硬化剂的取代的四氢嘧啶-2（1H） - 硫酮HDL-C电梯

    公开(公告)号：US06340687B1

    公开(公告)日：2002-01-22

    申请号：US09145895

    申请日：1998-09-02

    申请人： Amedeo A. Failli ,  Jay S. Shumsky ,  Kevin A. Memoli ,  Donald P. Strike

    发明人： Amedeo A. Failli ,  Jay S. Shumsky ,  Kevin A. Memoli ,  Donald P. Strike

    IPC分类号： C07D23940

    CPC分类号： C07D239/10

    摘要： Antiatherosclerotic agents are provided having the following structure: wherein: R1 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, or phenylalkyl of 7-10 carbon atoms; and R2, R3, R4, R5, and R6 are each, independently, hydrogen, halogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, aralkyl of 7-10 carbon atoms, alkoxy of 1-6 carbon atoms, aryloxy of 6-12 carbon atoms, aralkyloxy of 7-12 carbon atoms, fluoroalkoxy of 1-6 carbon atoms, trifluoromethyl, alkylthio of 1-3 carbon atoms, alkylsulfonyl of 1-3 carbon atoms, —SCF3, nitro, alkylamino in which the alkylamino moiety has 1-6 carbon atoms, or dialkylamino in which each alkyl group has 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 提供具有以下结构的抗动脉粥样硬化剂：其中：R1是氢，1-6个碳原子的烷基，3-8个碳原子的环烷基，2-7个碳原子的链烯基，2-7个碳原子的炔基或苯基烷基 7-10个碳原子; 和R 2，R 3，R 4，R 5和R 6各自独立地为氢，卤素，1-6个碳原子的烷基，3-8个碳原子的环烷基，2-7个碳原子的烯基，2-7个碳原子的炔基 7-10个碳原子的芳烷基，1-6个碳原子的烷氧基，6-12个碳原子的芳氧基，7-12个碳原子的芳烷氧基，1-6个碳原子的氟烷氧基，三氟甲基，1-3个碳原子的烷硫基 ，1-3个碳原子的烷基磺酰基，-SCF 3，硝基，其中烷基氨基部分具有1-6个碳原子的烷基氨基，或每个烷基具有1-6个碳原子的二烷基氨基; 或其药学上可接受的盐。

    Substitued tetrahydro-1,3,5-triazin-2[1H]-thiones as anti-atherosclerotic agents
    10.
    发明授权
    Substitued tetrahydro-1,3,5-triazin-2[1H]-thiones as anti-atherosclerotic agents 失效
    将取代的四氢-1,3,5-三嗪-2 [1H] - 噻二唑作为抗动脉粥样硬化剂

    公开(公告)号：US06268364B1

    公开(公告)日：2001-07-31

    申请号：US09483711

    申请日：2000-01-14

    申请人： Kevin A. Memoli ,  Donald P. Strike ,  Amedeo A. Failli ,  Robert J. Steffan

    发明人： Kevin A. Memoli ,  Donald P. Strike ,  Amedeo A. Failli ,  Robert J. Steffan

    IPC分类号： A61K3153

    CPC分类号： C07D251/08

    摘要： This invention provides compounds of formula 1 having the structure wherein R1, R2, R3, R4, and R5 are each independently, hydrogen, halogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkyl, alkoxy, aryloxy, fluoroalkoxy, trifluoromethyl, alkylthio, alkylsulfony, —SCF3, nitro, alkylamino, or dialkylamino; R6 is hydrogen, alkyl, cycloalkyl, or arylalkyl; and R7 is alkyl, cycloalkyl, or arylalkyl or a pharmaceutically acceptable salt thereof which are useful as antiatherosclerotic agents.

    摘要翻译： 本发明提供具有其中R 1，R 2，R 3，R 4和R 5各自独立地为氢，卤素，烷基，环烷基，烯基，炔基，苯基烷基，烷氧基，芳氧基，氟烷氧基，三氟甲基，烷硫基，烷基磺酰基， SCF 3，硝基，烷基氨基或二烷基氨基; R 6是氢，烷基，环烷基或芳基烷基; 和R7是可用作抗动脉粥样硬化剂的烷基，环烷基或芳烷基或其药学上可接受的盐。