公开(公告)号：US20060199804A1

公开(公告)日：2006-09-07

申请号：US11361599

申请日：2006-02-24

申请人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Graeme Smith

发明人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Graeme Smith

IPC分类号： A61K31/551 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/53 ,  A61K31/506 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC分类号： C07D251/54 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D417/04 ,  C07D471/04

摘要： Compounds of formula I: A-B-C  (I)and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of:  where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is: 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:  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:  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:

公开(公告)号：US20060063767A1

公开(公告)日：2006-03-23

申请号：US11213504

申请日：2005-08-26

申请人： Muhammad Javaid ,  Graeme Smith ,  Niall Morrison Barr Martin ,  Sylvie Gomez ,  Vincent Junior Ming-lai Loh ,  Xiao-Ling Cockcroft ,  Stefano Forte ,  Keith Menear ,  Ian Timothy William Matthews

发明人： Muhammad Javaid ,  Graeme Smith ,  Niall Morrison Barr Martin ,  Sylvie Gomez ,  Vincent Junior Ming-lai Loh ,  Xiao-Ling Cockcroft ,  Stefano Forte ,  Keith Menear ,  Ian Timothy William Matthews

IPC分类号： A61K31/502 ,  C07D403/02

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06

摘要： A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het is selected from: where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N, where only one or two of Y1, Y2 and Y3 can be N; and where Q is O or S.

摘要翻译： 式（I）的化合物：

公开(公告)号：US07504397B2

公开(公告)日：2009-03-17

申请号：US11361599

申请日：2006-02-24

申请人： Marc Geoffrey Hummersone ,  Sylvie Gomez ,  Keith Allan Menear ,  Xiao-Ling Fan Cockcroft ,  Graeme Cameron Murray Smith

发明人： Marc Geoffrey Hummersone ,  Sylvie Gomez ,  Keith Allan Menear ,  Xiao-Ling Fan Cockcroft ,  Graeme Cameron Murray Smith

IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D239/00 ,  C07D239/02

CPC分类号： C07D251/54 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D417/04 ,  C07D471/04

摘要： Compounds of formula I: A-B-C  (I) and isomers, salts, solvates, chemically protected forms, and prodrugs thereof are provided, wherein variables A, B and C are defined herein and wherein such compounds act as mTor inhibitors.

摘要翻译： 式I化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> ABC（I）<？in-line-formula description =“In-line Formulas”end =“tail 提供了异构体，盐，溶剂化物，化学保护形式和前体药物，其中变量A，B和C在本文中定义，并且其中这些化合物作为mTor抑制剂。

公开(公告)号：US08101602B2

公开(公告)日：2012-01-24

申请号：US13014275

申请日：2011-01-26

申请人： Keith Menear ,  Graeme Cameron Murray Smith ,  Karine Malagu ,  Heather Mary Ellen Duggan ,  Niall Morrison Barr Martin ,  Frederic Georges Marie Leroux

发明人： Keith Menear ,  Graeme Cameron Murray Smith ,  Karine Malagu ,  Heather Mary Ellen Duggan ,  Niall Morrison Barr Martin ,  Frederic Georges Marie Leroux

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： A61K31/5377 ,  A61K31/565 ,  A61K45/06 ,  C07D413/14 ,  C07D471/04 ,  C07D475/08 ,  C07D475/10

摘要： There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. 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.

摘要翻译： 提供式I化合物或其药学上可接受的盐。 还提供了制备式1化合物的方法和式1化合物作为药物和用于治疗癌症的用途。

公开(公告)号：US20060199803A1

公开(公告)日：2006-09-07

申请号：US11361213

申请日：2006-02-24

申请人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Peter Edwards ,  Ming-lai Loh ,  Graeme Smith

发明人： Marc Hummersone ,  Sylvie Gomez ,  Keith Menear ,  Xiao-Ling Cockcroft ,  Peter Edwards ,  Ming-lai Loh ,  Graeme Smith

IPC分类号： A61K31/551 ,  A61K31/541 ,  A61K31/519 ,  A61K31/5377 ,  C07D487/02

CPC分类号： C07D471/04

摘要： Compounds of formula l: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof one of X1, X2 and X3 is N, and the others are CH; RN1 and RN2 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms; RN3 and RN4 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms and their use in treating diseases ameliorated by the inhibition of mTOR.

摘要翻译： 式1化合物及其异构体，盐，溶剂合物，化学保护形式及其前药之一，X 1，X 2和X 3， 是N，其他是CH; R N1和R N2与它们所连接的氮原子一起形成具有4至8个环原子的含氮杂环; R 3 N 3和R 4 N 4与它们所连接的氮原子一起形成具有4至8个环原子的含氮杂环，并且其用于治疗改善的疾病 通过抑制mTOR。

公开(公告)号：US20060135770A1

公开(公告)日：2006-06-22

申请号：US11315528

申请日：2005-12-22

申请人： Muhammad Javaid ,  Graeme Smith ,  Niall Martin ,  Sylvie Gomez ,  Vincent Loh ,  Xiao-Ling Cockcroft ,  Keith Menear

发明人： Muhammad Javaid ,  Graeme Smith ,  Niall Martin ,  Sylvie Gomez ,  Vincent Loh ,  Xiao-Ling Cockcroft ,  Keith Menear

IPC分类号： C07D403/14

CPC分类号： C07C235/60 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/08 ,  C07D215/36 ,  C07D231/14 ,  C07D231/18 ,  C07D231/20 ,  C07D241/44 ,  C07D261/10 ,  C07D261/18 ,  C07D263/32 ,  C07D271/12 ,  C07D277/18 ,  C07D295/14 ,  C07D295/18 ,  C07D295/26 ,  C07D307/14 ,  C07D307/52 ,  C07D317/68 ,  C07D333/34 ,  C07D333/62 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06 ,  C07D495/04

摘要： A compound of the formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; n is 1 or 2; RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is selected from: where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and where Q is O or S.

摘要翻译： 式（I）的化合物及其异构体，盐，溶剂合物，化学保护形式及其前药，其中：R 2，R 3，R 3， 4和R 5独立地选自H，C 1-7烷氧基，氨基，卤素或羟基; n为1或2; R N1和R N2独立地选自H和R，其中R是任选取代的C 1-10烷基，C 3 -20个杂环基和C 5-20-20芳基; 或R N1和R N2，以及它们所连接的氮原子一起形成任选取代的5-7元含氮杂环; Het选自：其中Y 1和Y 3独立地选自CH和N，Y 2选自CX和N和X 是H，Cl或F; 而Q是O或S.

公开(公告)号：US07049313B2

公开(公告)日：2006-05-23

申请号：US10373114

申请日：2003-02-24

申请人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Stephen Philip Jackson ,  Mark James O'Connor ,  Alan Yin Kai Lau ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffery Hummersone ,  Roger John Griffin

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Stephen Philip Jackson ,  Mark James O'Connor ,  Alan Yin Kai Lau ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffery Hummersone ,  Roger John Griffin

IPC分类号： A61K31/535 ,  C07D413/00 ,  A61P35/00

CPC分类号： C07D409/04 ,  C07D417/04

摘要： The application concerns a compound of formula I: wherein one of P and Q is O, and the other of P and Q is CH, where there is a double bond between whichever of Q and P is CH and the carbon atom bearing the R3 group; Y is either O or S; R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; R3 is a phenyl or pyridyl group, attached by a first bridge group selected from —S—, —S(═O)—, —S(═O)2—, —O—, —NRN— and CRC1RC2— to an optionally substituted C5-20 carboaryl group, the phenyl or pyridyl group and optionally substituted C5-20 carboaryl group being optionally further linked by a second bridge group, so as to form an optionally substituted C5-7 ring, the phenyl or pyridyl group being further optionally substituted.

摘要翻译： 本申请涉及式I化合物：其中P和Q中的一个为O，P和Q中的另一个为CH，其中Q和P中的任一个为CH且具有R 1的碳原子之间为双键， SUP> 3 组; Y是O或S; R 1和R 2独立地是氢，任选取代的C 1-7烷基，C 3-20 或杂环基，或C 5-20-20芳基，或者可以一起形成任选取代的具有4至8个环原子的杂环; R 3是通过选自-S - ， - S（-O） - ， - S（-O）2 N的第一桥基团连接的苯基或吡啶基） - ， - O - ， - NR N - 和CR C1 - C2 - 与任选取代的C 5-20 - 苯基或吡啶基和任选取代的C 5-20碳芳基任选地通过第二桥基进一步连接，从而形成任选取代的C 5-7 苯基或吡啶基进一步任选被取代。

公开(公告)号：US20040002492A1

公开(公告)日：2004-01-01

申请号：US10373114

申请日：2003-02-24

申请人： Kudos Pharmaceuticals Ltd

发明人： Graeme Cameron Murray Smith ,  Niall Morrison Barr Martin ,  Stephen Philip Jackson ,  Mark James O'Connor ,  Alan Yin Kai Lau ,  Xiao-Ling Fan Cockcroft ,  Ian Timothy Williams Matthews ,  Keith Allan Menear ,  Laurent Jean Martin Rigoreau ,  Marc Geoffery Hummersone ,  Roger John Griffin

IPC分类号： A61K031/542 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/4436 ,  A61K031/4433 ,  A61K031/382 ,  A61K031/381 ,  C07D417/02 ,  C07D413/02 ,  C07D49/02

CPC分类号： C07D409/04 ,  C07D417/04

摘要： The application concerns a compound of formula I: 1 wherein one of P and Q is O, and the other of P and Q is CH, where there is a double bond between whichever of Q and P is CH and the carbon atom bearing the R3 group; Y is either O or S; R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; R3 is a phenyl or pyridyl group, attached by a first bridge group selected from nullSnull, nullS(nullO)null, nullS(nullO)2null, nullOnull, nullNRNnull and CRC1RC2null to an optionally substituted C5-20 carboaryl group, the phenyl or pyridyl group and optionally substituted C5-20 carboaryl group being optionally further linked by a second bridge group, so as to form an optionally substituted C5-7 ring, the phenyl or pyridyl group being further optionally substituted.

摘要翻译： 本申请涉及式I化合物：其中P和Q中的一个为O，P和Q中的另一个为CH，其中Q和P中的任一个为CH且具有R 1的碳原子之间为双键， 3>组 Y是O或S; R 1和R 2独立地是氢，任选取代的C 1-7烷基，C 3-20杂环基或C 5-20芳基，或者可以一起形成任选取代的具有4至8个环的杂环 原子 R 3是苯基或吡啶基，其通过选自-S - ， - S（= O） - ， - S（= O）2 - ， - O - ， - NR N - 和任选取代的C 5-20碳芳基，苯基或吡啶基和任选取代的C 5-20碳芳基任选进一步通过第二桥基连接，从而形成任选取代的 C5-7环，苯基或吡啶基进一步任选被取代。