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    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    1.
    发明申请
    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
    化合物作为ATR激酶的抑制剂有用

    公开(公告)号：WO2014143242A8

    公开(公告)日：2015-03-05

    申请号：PCT/US2013073477

    申请日：2013-12-06

    Applicant: VERTEX PHARMA

    Inventor： CHARRIER JEAN-DAMIEN ,  DAVIS CHRIS ,  DURRANT STEVEN ,  FRAYSSE DAMIEN ,  JIMENEZ JUAN-MIGUEL ,  KAY DAVE ,  KNEGTEL RONALD ,  O'DONNELL MICHAEL ,  PIERARD FRANCOISE ,  PINDER JOANNE ,  STORCK PIERRE-HENRI ,  TWIN HEATHER

    IPC: C07D487/04 ,  A61K31/437 ,  A61P35/00

    CPC classification number: C07D487/04 ,  A61K31/437 ,  C07D491/107 ,  C07D519/00

    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I); or a pharmaceutically acceptable salt, wherein the variables R1, R2, R3, and R4 are as defined herein.

    Abstract translation: 本发明涉及可用作ATR蛋白激酶抑制剂的化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明化合物具有式（I）; 或其药学上可接受的盐，其中变量R1，R2，R3和R4如本文所定义。

    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
    2.
    发明申请
    COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE 审中-公开
    化合物作为ATR激酶的抑制剂有用

    公开(公告)号：WO2014089379A1

    公开(公告)日：2014-06-12

    申请号：PCT/US2013073457

    申请日：2013-12-06

    Applicant: VERTEX PHARMA

    Inventor： AHMAD NADIA ,  BOYALL DEAN ,  CHARRIER JEAN-DAMIEN ,  DAVIS CHRIS ,  DAVIS REBECCA ,  DURRANT STEVEN ,  ETXEBARRIA I JARDI GORKA ,  FRAYSSE DAMIEN ,  JIMENEZ JUAN-MIGUEL ,  KAY DAVID ,  KNEGTEL RONALD ,  MIDDLETON DONALD ,  ODONNELL MICHAEL ,  PANESAR MANINDER ,  PIERARD FRANCOISE ,  PINDER JOANNE ,  SHAW DAVID ,  STORCK PIERRE-HENRI ,  STUDLEY JOHN ,  TWIN HEATHER

    IPC: C07D487/04 ,  A61K31/495 ,  A61P35/00

    CPC classification number: C07D487/04 ,  C07D453/02 ,  C07D471/08 ,  C07D487/08 ,  C07D491/107 ,  C07D498/04 ,  C07D498/10

    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula (I) or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula (I-A) or a pharmaceutically acceptable salt, wherein the variables are as defined herein.

    Abstract translation: 本发明涉及可用作ATR蛋白激酶抑制剂的化合物。 本发明还涉及包含本发明化合物的药学上可接受的组合物; 使用本发明化合物治疗各种疾病，病症和病症的方法; 制备本发明化合物的方法; 用于制备本发明化合物的中间体; 以及在体外应用中使用化合物的方法，如生物和病理现象中激酶的研究; 由这种激酶介导的细胞内信号转导途径的研究; 和新型激酶抑制剂的比较评估。 本发明的化合物具有式（I）或其药学上可接受的盐，其中变量如本文所述。 此外，本发明的化合物具有式（I-A）或其药学上可接受的盐，其中变量如本文所定义。

    Compounds useful as inhibitors of atr kinase
    5.
    发明专利
    Compounds useful as inhibitors of atr kinase 未知

    公开(公告)号：NZ731337A

    公开(公告)日：2019-02-22

    申请号：NZ73133713

    申请日：2013-12-06

    Applicant: VERTEX PHARMA

    Inventor： AHMAD NADIA ,  BOYALL DEAN ,  CHARRIER JEAN-DAMIEN ,  DAVIS CHRIS ,  DAVIS REBECCA ,  DURRANT STEVEN ,  ETXEBARRIA I JARDI GORKA ,  FRAYSSE DAMIEN ,  JIMENEZ JUAN-MIGUEL ,  KAY DAVID ,  KNEGTEL RONALD ,  MIDDLETON DONALD ,  ODONNELL MICHAEL ,  PANESAR MANINDER ,  PIERARD FRANCOISE ,  PINDER JOANNE ,  SHAW DAVID ,  STORCK PIERRE-HENRI ,  STUDLEY JOHN ,  TWIN HEATHER

    IPC: C07D487/04 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/495 ,  A61K31/519 ,  A61P35/00 ,  C07D213/75

    Abstract: Disclosed are 2-amino-6-fluoro-N-(pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives and analogues useful as inhibitors of ATR kinase as represented by the general formula (I); or a pharmaceutically acceptable salt thereof, wherein: R1 is–C(J1)2CN or halo; R9 is H; each J1 is independently H, methyl or ethyl; or two occurrences of J1, together with the carbon atom to which they are attached, form a 3-4 membered optionally substituted carbocyclic ring; R2 is H; halo; -CN; NH2; or a methyl or ethyl group optionally substituted with fluoro; or a C1-3aliphatic chain wherein up to two methylene units of the aliphatic chain are optionally replaced with -O-, -NR-, -C(O)-, or –S(O)n; R3 is H; halo; alkyl optionally substituted with 1-3 occurrences of halo; cycloalkyl; heterocyclyl; -CN; or an aliphatic chain wherein up to two methylene units of the aliphatic chain are optionally replaced with -O-, -NR-, -C(O)-, or –S(O)n; R4 is Q1 or an aliphatic chain wherein up to four methylene units of the aliphatic chain are optionally replaced with -O-, -NR-, -C(O)-, or -S(O)n-; R4 is optionally substituted with 0-5 occurrences of JQ; or R3 and R4, taken together with the atoms to which they are bound, form a 5-6 membered aromatic or non-aromatic ring having 0-2 heteroatoms selected from oxygen, nitrogen and sulfur; the ring formed by R3 and R4 is optionally substituted with 0-3 occurrences of JZ; provided that the compound is not 2-amino-6-fluoro-N-[5-fluoro-4-[4-[4-(oxetan-3-yl)piperazine-1-carbonyl]-1-piperidyl]-3-pyridyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide. Also disclosed are the compounds selected from 2-amino-6-fluoro-N-(5-fluoro-4-(4-(4-(3-methyloxetan-3-yl)piperazine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide; 4-(1-(3-(2-amino-6-fluoropyrazolo[1,5-a]pyrimidine-3-carboxamido)-5-fluoropyridin-4-yl)piperidine-4-carbonyl)-1-methylpiperazine 1-oxide; 2-amino-6-fluoro-N-(5-fluoro-4-(4-(4-(1-methylazetidin-3-yl)piperazine-1-carbonyl)piperidin-1-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide; and 2-amino-6-fluoro-N-(5-fluoro-4-(1-methyl-1H-imidazol-5-yl)pyridin-3-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide. There is also disclosed a pharmaceutical composition having properties of inhibitor of ATR protein kinase for treating cancer comprising an effective amount of a compound as defined above and a pharmaceutically acceptable carrier.

    COMPUESTOS DE PIRAZOLOPIRIDINA UTILES COMO INHIBIDORES DE QUINASAS
    9.
    发明专利
    COMPUESTOS DE PIRAZOLOPIRIDINA UTILES COMO INHIBIDORES DE QUINASAS 未知

    公开(公告)号：AR080856A1

    公开(公告)日：2012-05-16

    申请号：ARP110100282

    申请日：2011-01-27

    Applicant: VERTEX PHARMA

    Inventor： DAVIS CHRISTOPHER JOHN ,  BOYALL DEAN ,  FRAYSEE DAMIEN ,  JIMENEZ JUAN MANUEL ,  BRENCHLEY GUY ,  GOLEC JULIAN M C ,  TWIN HEATHER ,  YOUNG STEPHEN ,  SETTIMO LUCA ,  MILLER ANDREW W

    IPC: C07D471/04 ,  A61K31/437 ,  A61P3/10 ,  A61P11/06 ,  A61P35/00

    Abstract: Composiciones farmacéuticamente aceptables que comprenden dichos compuestos y métodos para usar las composiciones en el tratamiento de varias enfermedades, condiciones o trastornos y procesos para preparar compuestos. Reivindicacion 1: Un compuesto representado por la formula estructural (1) o una sal farmacéuticamente aceptable del mismo, donde T es -NH- o está ausente, cada Jc1 y Jc2 es independientemente -CN, -F, -Cl, -OR, -CH2OR, o -CF3; cada U1, U2 y U3 es independientemente -H, Z, o Jb donde no más de uno entre U1, U2 y U3 es -H; o dos de U1, U2 y U3 se unen entre sí para formar un anillo de cicloalquilo C1-6 que tiene 0-1 heteroátomos independientemente sustituidos con uno o más Je; Z es Y2-Q2; Y2 está ausente o es alquilo C1-6 opcionalmente e independientemente sustituido con uno o más Jd; Q2 está ausente o es un cicloalquilo C3-8 que tiene 0-1 heteroátomos opcionalmente e independientemente substituido con uno o más Je, donde no ambos Y2 y Q2 están ausentes; cada Jb es independientemente -F, -OR, -CN, -CF3, -N(R)2, -C(O)N(R)2, alquilo C1-6 opcionalmente e independientemente substituido con uno o más Ja; cada Ja es independientemente -F, -OR, -N(R)2, o -C(O)N(R) 2; cada Jd es independientemente -OR, -CN, -C(O)N(R)2, -N(R)2 o F; cada Je es independientemente alquilo C1-6, -OR, - N(R)2CF3, o F; cada R es -H o alquilo C1-6; y donde existe un centro quiral en el átomo indicado por *.

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