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    DIVALENT NUCLEOBASE COMPOUNDS AND USES THEREFOR
    5.
    发明申请
    DIVALENT NUCLEOBASE COMPOUNDS AND USES THEREFOR 审中-公开
    多种核苷酸化合物及其用途

    公开(公告)号：WO2014169206A3

    公开(公告)日：2015-01-22

    申请号：PCT/US2014033793

    申请日：2014-04-11

    申请人： UNIV CARNEGIE MELLON

    发明人： LY DANITH H ,  GOPALSAMY SURESH KUMAR ,  MANNA ARUNAVA

    IPC分类号： C07H19/22

    CPC分类号： C07K14/003 ,  C07D239/47 ,  C07D239/54 ,  C07D251/16 ,  C07D471/04 ,  C07D475/08 ,  C07D487/04 ,  C07D487/16 ,  C07H1/06 ,  C07H21/04 ,  G01N33/5308

    摘要： Described herein are novel divalent nucleobases that each bind two nucleic acid strands, matched or mismatched when incorporated into a nucleic acid or nucleic acid analog backbone (a genetic recognition reagent, or genetic recognition reagent). In one embodiment, the genetic recognition reagent is a peptide nucleic acid (PNA) or gamma PNA (?PNA) oligomer. Uses of the divalent nucleobases and monomers and genetic recognition reagents containing the divalent nucleobases also are provided.

    摘要翻译： 这里描述的是新颖的二价核碱基，其各自结合两个核酸链，当掺入核酸或核酸模拟主链（遗传识别试剂或遗传识别试剂）时匹配或错配）。 在一个实施方案中，遗传识别试剂是肽核酸（PNA）或γPNA（λPNA）寡聚体。 还提供了含有二价核碱基的二价核碱基和单体和遗传识别试剂的用途。

    PYRIMIDO-DIAZEPINONE COMPOUNDS AND METHODS OF TREATING DISORDERS
    6.
    发明申请
    PYRIMIDO-DIAZEPINONE COMPOUNDS AND METHODS OF TREATING DISORDERS 审中-公开
    吡嗪二酮类化合物和治疗疾病的方法

    公开(公告)号：WO2014145909A3

    公开(公告)日：2014-12-24

    申请号：PCT/US2014030760

    申请日：2014-03-17

    申请人： DANA FARBER CANCER INST INC

    发明人： GRAY NATHANAEL S ,  WALLER DAVID ,  CHOI HWAN GUEN ,  WANG JINHUA ,  DENG XIANMING

    IPC分类号： C07D487/14 ,  A61K31/505 ,  A61K31/519 ,  A61P29/00 ,  A61P35/00 ,  C07D487/12

    CPC分类号： C07D513/04 ,  C07D471/18 ,  C07D487/04 ,  C07D487/14 ,  C07D487/16 ,  C07D487/18 ,  C07D495/14 ,  C07D498/04 ,  C07D498/18 ,  C07F5/022

    摘要： The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), LRKK2, EphA2, polo kinase 1,2,3, or 4, Ack1, Ack2, Ab1, DCAMKL1, ABL1, Ab1 mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Ab1, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Ax1, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.

    摘要翻译： 本发明涉及新型嘧啶二氮杂酮化合物，调节蛋白激酶的方法，包括MPS1（TTK），ERK5（BMK1，MAPK7），LRKK2，EphA2，polo激酶1,2,3或4，Ack1，Ack2，Ab1 ，DCAMKL1，ABL1，Ab1突变体，DCAMKL2，ARK5，BRK，MKNK2，FGFR4，TNK1，PLK1，ULK2，PLK4，PRKD1，PRKD2，PRKD3，ROS1，RPS6KA6，TAOK1，TAOK3，TNK2，Bcr-Ab1，GAK，cSrc， TPR-Met，Tie2，MET，FGFR3，Aurora，Ax1，Bmx，BTK，c-kit，CHK2，Flt3，MST2，p70S6K，PDGFR，PKB，PKC，Raf，ROCK-H，Rsk1，SGK，TrkA，TrkB和 TrkC，以及这些化合物在治疗各种疾病，病症或病症中的用途。

    PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF
    8.
    发明申请
    PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF 审中-公开
    。。。。。。。。。。。。

    公开(公告)号：WO2014159981A2

    公开(公告)日：2014-10-02

    申请号：PCT/US2014/025564

    申请日：2014-03-13

    申请人： SPIROGEN SARL ,  GENENTECH, INC.

    发明人： HOWARD, Philip, Wilson ,  FLYGARE, John, A. ,  PILLOW, Thomas ,  WEI, Binqing

    CPC分类号： A61K47/6869 ,  A61K31/5517 ,  A61K47/6803 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6889 ,  A61P35/00 ,  C07D487/04 ,  C07D487/16 ,  C07D519/00

    摘要： Conjugate compounds of formula (A): wherein: R 2 is, where R 36a and R 36b are independently selected from H, F, C 1-4 saturated aikyl, C 2-3 alkenyl, which alkyl and alkenyl groups are optionally substituted by a group selected from C 1-4 alkyl amido and C 1-4 alkyl ester; or, when one of R 36a and R 36b is H, the other is selected from nitrile and a C 1-4 aikyl ester; R 6 and R 9 are independently selected from H, R, OH, OR, SH, SR, NH 2 , NHR, NRR', NO 2 , Me 3 Sn and halo; R 7 is independently selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR', NO 2 , Me 3 Sn and halo; Y is selected from formulae A1, A2, A3, A4, A5 and A6: L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; R A4 is a C 1-6 alkylene group; either (a) R 10 is H, and R 11 is OH, OR A , where R A is C 1-4 aikyl; or (b) R 10 and R 11 form a nitrogen-carbon double bond between the nitrogen and carbon atoms to which they are bound; or (c) R 10 is H and R 11 is OSO z M, where z is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; R and R' are each independently selected from optionally substituted C 1-12 alkyl, C 3-20 heterocyclyl and C 5-20 aryl groups, and optionally in relation to the group NRR', R and R' together with the nitrogen atom to which they are attached form an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring; wherein R 16 , R 17 , R 19 , R 20 , R 21 and R 22 are as defined for R 6 , R 7 , R 9 , R 10 , R 11 and R 2 respectively; wherein Z is CH or N; wherein T and T' are independently selected from a single bond or a C 1-9 alkylene, which chain may be interrupted by one or more heteroatoms e.g. O, S, N(H), NMe, provided that the number of atoms in the shortest chain of atoms between X and X' is 3 to 12 atoms; and X and X' are independently selected from O, S and N(H).

    摘要翻译： 式（A）的共轭化合物：其中：R 2为，其中R 36a和R 36b独立地选自H，F，C 1-4饱和的烷基，C 2-3链烯基，该烷基和烯基任选被选自C 1 -4-烷基酰氨基和C 1-4烷基酯; 或者当R 36a和R 36b之一为H时，另一个选自腈和C 1-4烷基酯; R 6和R 9独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; R 7独立地选自H，R，OH，OR，SH，SR，NH 2，NHR，NRR'，NO 2，Me 3 Sn和卤素; Y选自式A1，A2，A3，A4，A5和A6：L是连接到细胞结合剂的连接体; CBA是细胞结合剂; n为0〜48的整数; RA4是C1-6亚烷基; （a）R 10是H，R 11是OH，ORA，其中RA是C 1-4烷基; 或（b）R 10和R 11在与它们结合的氮原子和碳原子之间形成氮 - 碳双键; 或（c）R 10为H且R 11为OSOzM，其中z为2或3，M为单价药学上可接受的阳离子; R和R'各自独立地选自任选取代的C 1-12烷基，C 3-20杂环基和C 5-20芳基，并且任选地相对于基团NRR'，R和R'与它们所在的氮原子一起 连接形成任选取代的4-，5-，6-或7-元杂环; 其中R16，R17，R19，R20，R21和R22分别如R6，R7，R9，R10，R11和R2所定义; 其中Z是CH或N; 其中T和T'独立地选自单键或C1-9亚烷基，该链可以被一个或多个杂原子间隔。 O，S，N（H），NMe，条件是X和X'之间的最短原子链中的原子数为3至12个原子; X和X'独立地选自O，S和N（H）。