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25 条记录 (耗时 0.024 秒)

    Heterocyclic Compounds as Janus Kinase Inhibitors
    22.
    发明申请
    Heterocyclic Compounds as Janus Kinase Inhibitors 审中-公开
    杂环化合物作为Janus激酶抑制剂

    公开(公告)号：US20130071415A1

    公开(公告)日：2013-03-21

    申请号：US13699818

    申请日：2011-05-27

    申请人： Yarlagadda S. Babu ,  Pravin L. Kotian ,  Minwan Wu

    发明人： Yarlagadda S. Babu ,  Pravin L. Kotian ,  Minwan Wu

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.

    摘要翻译： 本发明提供了本文所述的式I化合物或其盐。 本发明还提供包含式I化合物的药物组合物，制备式I化合物的方法，可用于制备式I化合物的中间体和使用式I化合物抑制免疫应答或治疗癌症或血液恶性肿瘤的治疗方法。

    Nucleosides preparation thereof and use as inhibitors of rna viral polymerases
    23.
    发明申请
    Nucleosides preparation thereof and use as inhibitors of rna viral polymerases 审中-公开
    核苷的制备及用作rna病毒聚合酶的抑制剂

    公开(公告)号：US20050033051A1

    公开(公告)日：2005-02-10

    申请号：US10496116

    申请日：2002-11-14

    申请人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Minwan Wu

    发明人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Minwan Wu

    IPC分类号： A61K31/13 ,  A61K31/575 ,  A61K31/66 ,  A61K31/662 ,  A61K31/663 ,  A61K31/704 ,  A61K31/7056 ,  A61K36/28 ,  A61K38/20 ,  A61K38/21 ,  A61P31/14 ,  A61P31/16 ,  A61P31/20 ,  A61P43/00 ,  C07F9/10 ,  C07F9/6512 ,  C07F9/6561 ,  C07F9/02

    CPC分类号： C07F9/65616 ,  A61K31/13 ,  A61K31/66 ,  A61K36/28 ,  A61K38/20 ,  A61K38/208 ,  A61K38/21 ,  A61K38/212 ,  C07F9/10 ,  C07F9/6512 ,  Y02A50/393 ,  Y02A50/465 ,  A61K2300/00

    摘要： Compounds represented by the formula (I) R is H, OH, alkyl, O-alkyl, CH2—O-alkyl, (CH2)nOH, (CH2)nNH2, (CH2)nCONH2, (CH2)nOOOH; R1 is H, OH, alkyl, O-alkyl, CH2—O-alkyl, C6H11, CH2OH; R2 is H, alkyl, OH, CH2OH, CH2—O-alkyl, CH(OH)-alkyl, CH(OH)CH2OH, CH2-halogen; R3 and R4 independently is H, OH, alkyl; Z is OR5, OR6, or aminoacids and esters thereof R5 and R6 independently is H, alkyl, aryl, pivaloyloxymethyl, C(R7)2OC(O) X (R8)a formula (II), R7 independently is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, or —OR9; R9 is C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl or C5-C12 aryl; provided that at least one R8 is not H; and a is 1 when X is CH2, or direct bond, or 1 or 2 when X is N with the proviso that when a is 2 and X is N, (a) two N-linked R groups can be taken together to form a carbocyclic or oxygen containing heterocycle, (b) one N-linked R8 additionally can be —OR9 or (c) both N-linked R8 groups can be —H; R10 is H or C1-C8 alkyl; R11 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl n is 1-5 m is 0 to 5 X is S, N(R8) or direct bond Y is O, S, N (R8), and CHR1 B is selected from the group consisting of adenine, guanine, cytosine, uracil, thymine, modified purines and pyrimidines such as inosin-9-yl, 2-amino-purin-9-yl, 2amino-6-chloro-purin-9-yl, 2-6-diamino-purin-9-yl, 3-carboxamido-1, 2, 4-triazol-1-yl, 3-deaza-adenin-9-yl, 3-deaza-guanin-9-yl, 3-deaza-inosin-9-yl, 3-deaza-2-amino-purin-9-yl, 3-deaza-2-amino-6-chloro-purin-9-yl, 3-deaza-2, 6-diamino-purin-9-yl, 7-deaza-adenin-9-yl, 7-deaza-guanin-9-yl, 7-deaza-inosin-9-yl, 7-deaza-2-amino-purin-9-yl, 7-deaza-2-amino-6-chloro-purin-9-yl, 7-deaza-2-6-diamino-purin-9-yl, 7-deaza-8-aza-adenin-9-yl, 7-deaza-8-aza-guanin-9-yl, 7-deaza-8-aza-inosnin-9-yl, 7-deaza-8-aza-2-amino-purin-9-yl, 7-deaza-8-aza-2-amino-6-chloro-purin-9-yl, 7-deaza-8-aza-2-6-diamino-purin-9-yl, -8-aza-adenin-9-yl,-8-aza-guanin-9-yl, -8-aza-inosnin-9-yl, -8-aza-2-amino-purin-9-yl, -8-aza-2-amino-6-chloro-purin-9-yl, -8-aza-2-6-diamino-purin-9-yl, 5-aza-thymin-1-yl, 5-aza-cytosin-1-yl, 5-aza-uracil-1-yl, 6-aza-thymin-1-yl, 6-aza-cytosin-1-yl, 6-aza-uracil-1-yl, 2-thiouracil-1-yl, 4-thiouracil-1-yl, 2 thiocytosine-1-yl, uracil-5-yl, 2-thiouracil-5-yl, 4-thiouracil-5-yl, substituted pyridine derivatives such as 6-azauracil, and azacyzosine. In general, attachment may be at different positions in the ring at nitrogen or carbon. These B ring systems may be substituted with halo, alkyl, substituted alkyl (F, Cl, Br, I, OH), NH2, N3, aryl, substituted aryl (F, Cl, Br, I, OH, NH2), aralkyl; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.

    摘要翻译： 由式（I）R表示的化合物是H，OH，烷基，O-烷基，CH 2 -O-烷基，（CH 2）n OH，（CH 2）n NH 2，（CH 2）n CONH 2，（CH 2） R 1是H，OH，烷基，O-烷基，CH 2 -O-烷基，C 6 H 11，CH 2 OH; R 2是H，烷基，OH，CH 2 OH，CH 2 -O-烷基，CH（OH） - 烷基，CH（OH）CH 2 OH， R 3和R 4独立地是H，OH，烷基; Z为OR 5，OR 6或其氨基酸及其酯R 5和R 6独立地为H，烷基，芳基，新戊酰氧基甲基，C（R 7）2 OC（O）X（R 式（II）中，R 7独立地是-H，C 1 -C 12烷基，C 5 -C 12芳基，C 2 -C 12烯基，C 2 -C 12炔基，C 7 -C 12链烯基芳基，C 7 -C 12炔基芳基或 C 6 -C 12烷芳基，其中任何一个是未取代的或被1或2个卤素，氰基，叠氮基，硝基或-OR 9取代。 R 9是C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12炔基或C 5 -C 12芳基; 条件是至少一个R 8不是H; 当X为CH 2或直接键合时，a为1，X为N时为1或2，条件是当a为2且X为N时，（a）两个N-连接的R基团可以一起形成 碳环或含氧杂环，（b）一个N-连接的R 8另外可以是-OR 9或（c）两个N-连接的R 8基团可以是-H; R 10是H或C 1 -C 8烷基; R 11选自H，烷基，烯基，炔基，芳基，酰氧基烷基和新戊酰氧基烷基

    Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
    24.
    发明申请
    Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases 有权

    公开(公告)号：US20060122391A1

    公开(公告)日：2006-06-08

    申请号：US11269819

    申请日：2005-11-09

    申请人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Minwan Wu

    发明人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Minwan Wu

    IPC分类号： C07F9/6512

    CPC分类号： C07F9/65616 ,  A61K36/28 ,  A61K38/208 ,  A61K38/212 ,  C07F9/6512 ,  Y02A50/393 ,  Y02A50/465 ,  A61K2300/00

    摘要： Compounds represented by the formula: A is (CH2)nR2, —CH═CH2, CH2—CH═CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)CH2OH, CH2—CH(OH)CH3, CH2CH(OH)CH2OH, or CH(OH)CH(OH)CH3, R,R1 individually is H, NH2OH, Cl, Br, I, aryl, substituted aryl, heterocycle, NR3R4, OR3 or SR3, R2 is H, OH, F, N3, NH2, CO2H, SH, alkyl, substituted alkyl, S-alkyl, O-acyl, CONH2, or CONH-alkyl, n is 1-3, y is O, S or NH, W is O or S, Z, Z′ individually is OR3, OR4, O(CH2)m—O—(CH2)xCH3, NH—CH(alkyl)CO2R3, alkyl, substituted alkyl, OCH2CH2S—C(O)CH3, OCH2CH2S—C(O)CH(CH3)2, OCH2CH2S—C(O)C(CH3)3, OCH2CH2—SC(O)aryl, OCH2CH2—S—S—OCH2CH2OH, OCH2OC(O)C(CH3)3, OCH2—O—C(O)OCH(CH3)2, or OCH2—O—C(O)CH(CH3)2 R3, R4 individually is H, alkyl, substituted alkyl, aryl, or substituted aryl; Both R3 and R4 can form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring; m is 1-3, x is 0-19; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.