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    Macrolides
    1.
    发明授权
    Macrolides 失效
    大环内酯类

    公开(公告)号：US07462600B2

    公开(公告)日：2008-12-09

    申请号：US11313523

    申请日：2005-12-21

    申请人： Louis S. Chupak ,  Mark E. Flanagan ,  Takushi Kaneko ,  Thomas V. Magee ,  Mark C. Noe ,  Usa Reilly

    发明人： Louis S. Chupak ,  Mark E. Flanagan ,  Takushi Kaneko ,  Thomas V. Magee ,  Mark C. Noe ,  Usa Reilly

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： Macrolide compounds per se, as shown below and defined herein, and their use, e.g., as antibacterial and antiprotozoal agents in animals, including humans: Also disclosed are methods of preparing the compounds, intermediates, and pharmaceutical compositions thereof, and methods of treating or preventing disease by administering the compounds to subjects in need. This abstract is only an excerpt and is not limiting of the invention.

    摘要翻译： 大环内酯类化合物本身，如下文所示和定义，以及它们在动物（包括人）中作为抗细菌剂和抗原虫药的用途：还公开了制备化合物，中间体及其药物组合物的方法，以及治疗或 通过将化合物给予需要的受试者来预防疾病。 该摘要仅是摘录而不是本发明的限制。

    Ether derivatives useful as inhibitors of PDE4 isozymes
    5.
    发明授权
    Ether derivatives useful as inhibitors of PDE4 isozymes 失效
    醚衍生物可用作PDE4同功酶的抑制剂

    公开(公告)号：US06828333B2

    公开(公告)日：2004-12-07

    申请号：US10066503

    申请日：2002-01-31

    申请人： Anthony Marfat ,  Robert J. Chambers ,  Thomas V. Magee

    发明人： Anthony Marfat ,  Robert J. Chambers ,  Thomas V. Magee

    IPC分类号： A61K3144

    CPC分类号： C07D213/82 ,  C07D277/56 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12

    摘要： This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1, or 2; Y is ═C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1-C4) alkyl; —(C2-C4) alkynyl; fluorinated-(C1-C3) alkyl; fluorinated-(C1-C3) alkoxy; —OR16; and —C(═O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1-C4) alkyl; —(C3-C7) cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one of them must be —H, and they are selected independently of each other and of RA and RB; R1 and R2 are each a member independently selected from the group consisting of H; F; Cl; CN; NO2; —(C1-C4) alkyl; —(C2-C4) alkynyl; fluorinated-(C1-C3)alkyl; OR16; and —C(═O)NR22aR22b; —R3 is H; —(C1-C3)alkyl; phenyl; benzyl; or OR16; R4, R5 and R6 are defined as set forth in the specification; J1 and J2 are each independently a moiety comprising a saturated or unsaturated six-membered monocyclic carbon ring; and D is a member independently selected from the group consisting of partial Formulas (1.1.1) through (1.1.5) as set forth in the specification; a pharmaceutically acceptable salt thereof; which are useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinaphils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease.

    摘要翻译： 本申请针对的是化合物，其中j为1; k为0或1; m为1,2或3; n为1或2; W 1和W 2独立地是-O-或-S（= O）t - ，其中t是0,1或2; Y是= C（R a a a） - ，其中R a是选自H的成员; F; Cl; CN; NO2; - （C 1 -C 4）烷基; - （C 2 -C 4）炔基; 氟化 - （C 1 -C 3）烷基; 氟化 - （C1-C3）烷氧基; -OR <16>; 和-C（= O）NR 22 aR 22 b; R 22a和R 22b定义如说明书中所述; -R A和R B各自独立地选自H; F; CF3; - （C 1 -C 4）烷基; - （C 3 -C 7）环烷基; 苯基; 和苄基; 其中所述环烷基，苯基和苄基部分各自独立地被0至3个如本说明书所述定义的取代基R 10取代; R 16和R 17定义如说明书所述; -R＆lt; C＆gt;和R D具有与上述R A和R B相同的含义，不同之处在于它们之一必须是-H，并且它们彼此独立地选自和R 和R B; R 1和R 2各自独立地选自H; F; Cl; CN; NO2; - （C 1 -C 4）烷基; - （C 2 -C 4）炔基; 氟化 - （C 1 -C 3）烷基; OR <16>; 和-C（= O）NR 22 aR 22 b; -R 3为H; - （C 1 -C 3）烷基; 苯基; 苄基; 或OR 16; R 4，R 5和R 6是取代的

    Ether derivatives useful as inhibitors of PDE4 isozymes
    7.
    发明授权
    Ether derivatives useful as inhibitors of PDE4 isozymes 失效

    公开(公告)号：US07183293B2

    公开(公告)日：2007-02-27

    申请号：US10918820

    申请日：2004-08-13

    申请人： Anthony Marfat ,  Robert J. Chambers ,  Thomas V. Magee

    发明人： Anthony Marfat ,  Robert J. Chambers ,  Thomas V. Magee

    IPC分类号： C07D405/12 ,  A61K31/44

    CPC分类号： C07D213/82 ,  C07D277/56 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12

    摘要： This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1, or 2; Y is ═C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1–C4)alkyl; —(C2–C4)alkynyl; fluorinated-(C1–C3)alkyl; fluorinated-(C1–C3)alkoxy; —OR16; and —C(═O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1–C4)alkyl; —(C3–C7)cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one of them must be —H, and they are selected independently of each other and of RA and RB; R1 and R2 are each a member independently selected from the group consisting of H; F; Cl; CN; NO2; —(C1–C4)alkyl; —(C2–C4)alkynyl; fluorinated-(C1–C3)alkyl; OR16; and —C(═O)NR22aR22b; —R3 is H; —(C1–C3)alkyl; phenyl; benzyl; or OR16; R4, R5, and R6 are defined as set forth in the specification; J1 and J2 are each independently a moiety comprising a saturated or unsaturated six-membered monocyclic carbon ring; and D is a member independently selected from the group consisting of partial Formulas (1.1.1) through (1.1.5) as set forth in the specification; a pharmaceutically acceptable salt thereof; which are useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease.

    Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes
    9.
    发明授权
    Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes 失效
    可用作PDE4同功酶抑制剂的烟酰胺联芳衍生物

    公开(公告)号：US06649633B2

    公开(公告)日：2003-11-18

    申请号：US10062813

    申请日：2002-01-31

    申请人： Robert J. Chambers ,  Anthony Marfat ,  Thomas V. Magee

    发明人： Robert J. Chambers ,  Anthony Marfat ,  Thomas V. Magee

    IPC分类号： A61K3144

    CPC分类号： C07D213/82 ,  C07D405/12

    摘要： This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; Y is —C(R1a); Q1 is phenyl or substituted phenyl; Q2 is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.

    摘要翻译： 本申请涉及可用作PDE4抑制剂的化合物，用于治疗由下列通式的嗜酸性粒细胞，特别是哮喘，慢性支气管炎和慢性阻塞性肺疾病的活化和脱颗粒调节的疾病，其中j为0或1，条件是当j 为0，n必须为2; k为0或1; m为0,1或2; n为1或2; W 1是-O-; 或-S（= O）t - ，其中t为0,1或2; Y是-C（R 1a）; Q 1是苯基或取代的苯基; Q 2是联苯基或取代的联苯基; 并且其余变量被定义为说明书中所阐述的。 本申请还涉及包含那些化合物的药物组合物和治疗由嗜酸性粒细胞，特别是哮喘，慢性支气管炎和慢性阻塞性肺疾病的活化和脱颗粒调节的疾病的方法。