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    • 1. 发明专利
      IL191196A Pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors, pharmaceutical compositions containing them and use thereof as medicaments and in the manufacture of medicaments for the production of an anti-cancer effect in a warm-blooded animal 未知
    • Pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors, pharmaceutical compositions containing them and use thereof as medicaments and in the manufacture of medicaments for the production of an anti-cancer effect in a warm-blooded animal
    • IL191196A
    • 2016-02-29
    • IL19119608
    • 2008-05-01
    • KUDOS PHARM LTD , GRAEME CAMERON MURRAY SMITH , SYLVIE GOMEZ , XIAO-LING FAN COCKROFT , KEITH ALLAN MENEAR , MARC GEOFFREY HUMMERSONE , KARINE MALAGU , HEATHER MARY ELLEN DUGGAN , GESINE JOHANNA HERMANN
    • GRAEME CAMERON MURRAY SMITH , SYLVIE GOMEZ , XIAO-LING FAN COCKROFT , KEITH ALLAN MENEAR , MARC GEOFFREY HUMMERSONE , KARINE MALAGU , HEATHER MARY ELLEN DUGGAN , GESINE JOHANNA HERMANN
    • There is provided a compound of formula I: wherein: one or two of X 5 , X 6 and X 8 is N, and the others are CH; R 7 is selected from halo, OR O1 , SR S1 , NR N1 R N2 , NR N7a C(-O)R C1 , NR N7b SO 2 R S2a , an optionally substituted C 5-20 heteroaryl group, or an optionally substituted C 5-20 aryl group, where R O1 and R S1 are selected from H, an optionally substituted C 5-20 aryl group, an optionally substituted C 5-20 heteroaryl group, or an optionally substituted C 1-7 alkyl group; R N1 and R N2 are independently selected from H, an optionally substituted C 1-7 alkyl group, an optionally substituted C 5-20 heteroaryl group, an optionally substituted C 5-20 aryl group or R N1 and R N2 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms; R C1 is selected from H, an optionally substituted C 5-20 aryl group, an optionally substituted C 5-20 heteroaryl group, an optionally substituted C 1-7 alkyl group or NR N8 R N9 , where R N8 and R N9 are independently selected from H, an optionally substituted C 1-7 alkyl group, an optionally substituted C 5-20 heteroaryl group, an optionally substituted C 5-20 aryl group or R N8 and R N9 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms; R S2a is selected from H, an optionally substituted C 5-20 aryl group, an optionally substituted C 5-20 heteroaryl group, or an optionally substituted C 1-7 alkyl group; R N7a and R N7b are selected from H and a C 1-4 alkyl group; R N3 and R N4 , together with the nitrogen to which they are bound, form a heterocyclic ring containing between 3 and 8 ring atoms; R 2 is selected from H, halo, OR O2 , SR S2b , NR N5 R N6 , an optionally substituted C 5-20 heteroaryl group, and an optionally substituted C 5-20 aryl group, wherein R O2 and R S2b are selected from H, an optionally substituted C 5-20 aryl group, an optionally substituted C 5-20 heteroaryl group, or an optionally substituted C 1-7 alkyl group; R N5 and R N6 are independently selected from H, an optionally substituted C 1-7 alkyl group, an optionally substituted C 5-20 heteroaryl group, and an optionally substituted C 5-20 aryl group, or R N5 and R N6 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms, or a pharmaceutically acceptable salt thereof, with the proviso that when R 2 is unsubstituted morpholino. R N3 and R N4 together with the nitrogen atom to which they are attached form an unsubstituted morpholino and R 7 is unsubstituted phenyl, and X 5 is CH, then X 6 is not N and X 8 is not CH, or X 6 is not CH and X 8 is not N, and when R 2 is unsubstituted piperidinyl, R N3 and R N4 together with the nitrogen atom to which they are attached form an unsubstituted piperidinyl and R 7 is unsubstituted phenyl, and X 5 is CH, then X 6 is not CH and X is not N. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明申请
      US20100130473A1 COMPOUNDS 审中-公开
    • COMPOUNDS
    • 化合物
    • US20100130473A1
    • 2010-05-27
    • US11817134
    • 2006-02-24
    • Marc Geoffrey Hummersone , Sylvie Gomez , Keith Allan Menear , Xiao-Ling Fan Cockcroft , Graeme Cameron Murray Smith
    • Marc Geoffrey Hummersone , Sylvie Gomez , Keith Allan Menear , Xiao-Ling Fan Cockcroft , Graeme Cameron Murray Smith
    • A61K31/5377 , C07D413/04 , C07D413/14 , C07D471/04 , A61P35/00 , A61K31/53 , A61K31/551 , A61K31/553 , A61K31/519
    • C07D251/70 , C07D239/48 , C07D239/50 , C07D239/94 , C07D295/135 , C07D403/04 , C07D403/12 , C07D405/04 , C07D413/12 , C07D417/04 , C07D471/04
    • Compounds of formula (I): A-B—C and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of formula (i) where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is formula (ii) RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is formula (iii) where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from formula (iv) which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of formula (v).
    • 式（I）化合物：A-B-C及其异构体，盐，溶剂合物，化学保护形式及其前药。其中：B选自式（ⅰ），其中RN为H或Me; 或B是含有一个或两个环杂原子的二价C5杂环残基; A是式（ⅱ）RA 3和RA 5独立地选自卤素，ORO和RAC，其中RO是H或Me，RAC是H或C 1-4烷基; XA选自N和CRA4，其中RA4选自H，ORO，CH2OH，CO2H，NHSO2Me和NHCOMe; RA2和RA6独立地选自H，卤素和ORO; 或RA3和RA4与它们所连接的碳原子一起，或RA2和RA3与它们所连接的碳原子一起可以形成含有至少一个氮环原子的C 5-6杂环或杂芳环; 其中如果X不是RA，RA6的N，1,2或3不是H; C是式（ⅲ），其中X选自N和CH，Y选自N和CH，Z选自N和CRC 6; RC3选自H，卤素和任选取代的含N的C 5-7杂环基; RC5是选自式（iv）的基团，该基团可以被一个或两个C 1-4烷基或羧基选择; RC6为H; 或者当X和Y为N时，RC5和RC6（当Z为CRC6时）与它们所连接的碳原子一起形成选自式（v）的稠合C 6芳环。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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