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    Peroxisome proliferator activated receptor agonists
    2.
    发明授权
    Peroxisome proliferator activated receptor agonists 失效
    过氧化物酶体增殖物激活受体激动剂

    公开(公告)号：US07544812B2

    公开(公告)日：2009-06-09

    申请号：US10496770

    申请日：2002-11-26

    Applicant: Tracey Ann Gibson ,  Richard Duane Johnston ,  Nathan Bryan Mantlo ,  Richard Craig Thompson ,  Leonard Larry Winneroski ,  Yanping Xu ,  Xiaodong Wang

    Inventor： Tracey Ann Gibson ,  Richard Duane Johnston ,  Nathan Bryan Mantlo ,  Richard Craig Thompson ,  Leonard Larry Winneroski ,  Yanping Xu ,  Xiaodong Wang

    IPC: A61K31/4166 ,  C07D233/32

    CPC classification number: C07D401/06 ,  C07D233/32 ,  C07D233/70 ,  C07D233/76 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12

    Abstract: The present invention is directed to compounds represented by the following structural Formula (I), (a) R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and —CH2—C(O)—R17-R18, wherein R17 is O or NH and R18 is optionally substituted benzyl; (b) R2 is selected from the group consisting of C1-C6 alkyl, C1-C6 alkenyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C1-C4 alkyl sulfonamide, C1-C4 alkyl amide, OR10 and C3-C6 cycloalkyl; (c) W is O or S; (d) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may optionally be replaced with O, NH, S, and optionally two carbons together may form a double bond; (e) Y is selected from the group consisting of C, O, S, NH and a single bond; and (f) E is selected from the group consisting of C(R3)(R4)A, A, and a substituted or unsubstituted group selected from the group consisting of (CH2)n COOR19.

    Abstract translation: 本发明涉及由以下结构式（I）表示的化合物，（a）R 1选自氢，取代或未取代的选自C 1 -C 8烷基，芳基-C 0-4 - 烷基，杂芳基 C 0-4烷基，C 3 -C 6环烷基芳基-C 0-2 - 烷基和-CH 2 -C（O）-R 17 -R 18，其中R 17是O或NH，R 18是任选取代的苄基; （b）R 2选自C 1 -C 6烷基，C 1 -C 6烯基，芳基-C 0-4 - 烷基，杂芳基-C 0-4 - 烷基，C 1 -C 4烷基磺酰胺，C 1 -C 4烷基酰胺，OR 10 和C 3 -C 6环烷基; （c）W为O或S; （d）X是任选取代的C1-C5亚烷基连接体，其中连接体的一个碳原子可以任选地被O，NH，S取代，并且任选地两个碳可以一起形成双键; （e）Y选自C，O，S，NH和单键; 和（f）E选自C（R 3）（R 4）A，A和选自（CH 2）n COOR 19的取代或未取代的基团。

    Peroxisome proliferator activated receptor agonists
    6.
    发明授权
    Peroxisome proliferator activated receptor agonists 失效
    过氧化物酶体增殖物激活受体激动剂

    公开(公告)号：US07345070B2

    公开(公告)日：2008-03-18

    申请号：US11054226

    申请日：2005-02-09

    Applicant: Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  James Ray McCarthy ,  Christopher John Rito ,  Leonard Larry Winneroski ,  Yanping Xu

    Inventor： Dawn Alisa Brooks ,  Alexander Glenn Godfrey ,  Sarah Beth Jones ,  James Ray McCarthy ,  Christopher John Rito ,  Leonard Larry Winneroski ,  Yanping Xu

    IPC: A31K31/421 ,  C07D263/32

    CPC classification number: C07D413/04 ,  C07D263/32 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

    Abstract: Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: n is 2, 3, or 4 and W is CH2, CH(OH), C(O) or O; R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryl-alkyl, heteroaryl-alkyl, cycloalkyl-alkyl, or t-butyl; R2 is H, alkyl, haloalkyl or phenyl; Y is an unsubstituted or substituted thiophen-2,5-diyl or phenylene; R3 is alkyl or haloalkyl; R4 is a substituted or unsubstituted phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, quinolyl, pyridyl or benzo[1,3]dioxol-5-yl group; and R5 is H, alkyl, or aminoalkyl; are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.

    Abstract translation: 由以下结构式（I）表示的化合物及其药学上可接受的盐，溶剂合物和水合物，其中：n为2,3或4，W为CH 2，CH（OH），C （O）或O; R 1是未取代或取代的芳基，杂芳基，环烷基，杂环烷基，芳基 - 烷基，杂芳基 - 烷基，环烷基 - 烷基或叔丁基; R2是H，烷基，卤代烷基或苯基; Y是未取代或取代的噻吩-2,5-二基或亚苯基; R3是烷基或卤代烷基; R4是取代或未取代的苯基，萘基，1,2,3,4-四氢萘基，喹啉基，吡啶基或苯并[1,3]二氧杂环戊烯-5-基; 并且R 5是H，烷基或氨基烷基; 可用于调节过氧化物酶体增殖物激活受体，特别是用于治疗糖尿病。

    Antimycobacterial agents
    10.
    发明授权
    Antimycobacterial agents 失效
    抗分枝杆菌药

    公开(公告)号：US06310058B1

    公开(公告)日：2001-10-30

    申请号：US09578973

    申请日：2000-05-25

    Applicant: Marvin J. Miller ,  Yanping Xu

    Inventor： Marvin J. Miller ,  Yanping Xu

    IPC: A61K3155

    CPC classification number: C07D403/12 ,  C07D413/12

    Abstract: Compounds represented by the formula [1] R1 is H or a substituent; R2 and R3 are C1-C3 alkyl; R4 is siderophore group e.g. CH3—(CH2)n—C(O)—N(OH)—(CH2)m— with n=10-22, m=2-6; X is O, S, or NH; X1 is O or NH; Y is H or alkyl; Z is H or substituted amino, e.g., t-BocNH or CbzNH, and r is 2-4; are useful in the method provided for treating tuberculosis. [1] is prepared by coupling [7], wherein HX1 is HO— or H2N—,  with [4] obtained as the free acid after saponification of the methyl ester.

    Abstract translation: 由式[1] R 1表示的化合物是H或取代基; R2和R3是C1-C3烷基; R4是铁载体基团 CH 3 - （CH 2）n -C（O）-N（OH） - （CH 2）m - ，其中n = 10-22，m = 2-6; X是O，S或NH; X1是O或NH; Y是H或烷基; Z是H或取代的氨基，例如t-BocNH或CbzNH，r是2-4; 可用于治疗结核病的方法。 [1]通过偶联[7]制备，其中HX1是HO-或H2N-，其中[4]在甲酯皂化后作为游离酸获得。

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