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公开(公告)号:US20070093489A1
公开(公告)日:2007-04-26
申请号:US11550004
申请日:2006-10-17
申请人: Muhammad Javaid , Keith Menear , Sylvie Gomez , Marc Hummersone , Niall Martin , Graeme Smith , Xiao-Ling Cockcroft
发明人: Muhammad Javaid , Keith Menear , Sylvie Gomez , Marc Hummersone , Niall Martin , Graeme Smith , Xiao-Ling Cockcroft
IPC分类号: A61K31/53
CPC分类号: C07D403/10 , C07D403/14 , C07D411/14 , C07D413/14 , C07D487/04
摘要: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) and where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2; RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.
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公开(公告)号:US20060199804A1
公开(公告)日:2006-09-07
申请号:US11361599
申请日:2006-02-24
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:
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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。
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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:
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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.
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公开(公告)号:US20090209520A1
公开(公告)日:2009-08-20
申请号:US12304636
申请日:2007-06-15
申请人: Muhammad Hashim Javaid , Sylvie Gomez , Xiao-Ling Fan Cockcroft , Keith Allan Menear , Niall Morrison Barr Martin
发明人: Muhammad Hashim Javaid , Sylvie Gomez , Xiao-Ling Fan Cockcroft , Keith Allan Menear , Niall Morrison Barr Martin
IPC分类号: A61K31/55 , C07D295/192 , A61K31/495 , C07D223/04 , C07D211/32 , A61K31/4453 , C12N5/06 , A61P35/00
CPC分类号: C07D295/192 , C07C235/60 , C07D211/16 , C07D211/18 , C07D211/70 , C07D213/74 , C07D217/06 , C07D295/205
摘要: A compound of the formula (I): and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRRC2—(CH2)m—, where m is 0 or 1, RC1 is selected from H, CH3 and CF3, and RC2 is selected from H and CH3, or RC1 and RC2′ together with the carbon atom to which they are attached form the 1,1-cyclopropylene group formula (A): RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20heterocyclyl 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 formula (ii): 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.
摘要翻译: 式(I)的化合物及其药学上可接受的盐,其中:R 2,R 3,R 4和R 5独立地选自H,C 1-7烷氧基,氨基,卤素或羟基; Y是-CRRC2-(CH2)m-,其中m是0或1,RC1选自H,CH3和CF3,RC2选自H和CH3,或RC1和RC2'与它们所代表的碳原子一起 连接形成1,1-环亚丙基基团(A):RN1和RN2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杂环基和C 5-20芳基; 或RN1和RN2与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为式(ⅱ):其中Y1和Y3独立地选自CH和N,Y2选自CX和N,X是H,Cl或F.
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公开(公告)号:US20090163477A1
公开(公告)日:2009-06-25
申请号:US12143208
申请日:2008-06-20
申请人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
发明人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
IPC分类号: A61K31/502 , C07D401/14 , C07D413/14 , A61K31/551 , A61P9/00 , A61P35/00 , A61P29/00 , A61K31/5377 , C07D405/14 , C07D409/14
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, 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:用于治疗通过抑制PARP而改善的癌症或其它疾病,其中:A和B一起表示任选取代的稠合芳环; X可以是NRX或CRXRY; 如果X-NRX则n为1或2,如果X-CRXRY则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2独立地选自氢和C 1-4烷基,或当X是CRXRY,RC1,RC1,RC2,RX和RY时,连同它们所连接的碳原子一起可以形成任选取代的 稠合芳环; R1选自H和卤素; Het选自:其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N,其中Y1,Y2和Y3中只有一个可以是N; 而Q是O或S.
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公开(公告)号:US20120129855A1
公开(公告)日:2012-05-24
申请号:US13361911
申请日:2012-01-30
申请人: Keith Allan Menear , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fernandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
发明人: Keith Allan Menear , Muhammad Hashim Javaid , Sylvie Gomez , Marc Geoffrey Hummersone , Carlos Fernandez Lence , Niall Morrison Barr Martin , David Alan Rudge , Craig Anthony Roberts , Kevin Blades
IPC分类号: A61K31/502 , A61K31/5377 , A61P35/00
CPC分类号: C07D401/10 , C07D401/14 , C07D405/14 , C07D487/04 , C07D491/10
摘要: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; RC is selected from H, C1-4 alkyl; and R1 is selected from C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl, which groups are optionally substituted; or RC and R1 together with the carbon and oxygen atoms to which they are attached form a spiro-C5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C5-7 aromatic ring.
摘要翻译: 式(I)的化合物:其中:A和B一起表示任选取代的稠合芳环; X和Y分别选自CH和CH,CF和CH,CH和CF以及N和CH; RC选自H,C 1-4烷基; 并且R 1选自C 1-7烷基,C 3-20杂环基和C 5-20芳基,该基团任选被取代; 或RC和R 1与它们所连接的碳原子和氧原子一起形成含有C 5-7的含氧杂环基团,其任选被取代或稠合至C5-7芳环。
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公开(公告)号:US07666870B2
公开(公告)日:2010-02-23
申请号:US12143208
申请日:2008-06-20
申请人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-Iai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
发明人: Muhammad Hashim Javaid , Graeme Cameron Murray Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-Iai Loh , Xiao-Ling Fan Cockcroft , Stefano Forte , Keith Allan Menear , Ian Timothy William Matthews , Frank Kerrigan
IPC分类号: C07D403/02 , A61K31/502
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, 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:用于治疗通过抑制PARP而改善的癌症或其它疾病,其中:A和B一起表示任选取代的稠合芳环; X可以是NRX或CRXRY; 如果X = NRX则n为1或2,如果X = CRXRY则n为1; RX选自H,任选取代的C 1-20烷基,C 5-20芳基,C 3-20杂环基,酰氨基,硫代酰氨基,酯,酰基和磺酰基; RY选自H,羟基,氨基; 或RX和RY可以一起形成螺C 3-7环烷基或杂环基; RC1和RC2独立地选自氢和C 1-4烷基,或当X是CRXRY,RC1,RC1,RC2,RX和RY时,连同它们所连接的碳原子一起可以形成任选取代的 稠合芳环; R1选自H和卤素; Het选自:其中Y1选自CH和N,Y2选自CH和N,Y3选自CH,CF和N,其中Y1,Y2和Y3中只有一个可以是N; 而Q是O或S.
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公开(公告)号:US20090181951A1
公开(公告)日:2009-07-16
申请号:US12304794
申请日:2007-06-15
申请人: Muhammad Hashim Javaid , Sylvie Gomez , Xiao-Ling Fan Cockcroft , Keith Allan Menear , Niall Morrison Barr Martin
发明人: Muhammad Hashim Javaid , Sylvie Gomez , Xiao-Ling Fan Cockcroft , Keith Allan Menear , Niall Morrison Barr Martin
IPC分类号: A61K31/55 , C07D241/04 , A61K31/495 , C07D243/08 , A61K31/5513 , A61P35/00 , A61P25/16 , C07D223/04 , C12N5/06 , C12N13/00
CPC分类号: C07D211/34 , C07C235/60 , C07D211/08 , C07D211/70 , C07D217/02 , C07D225/02 , C07D241/04 , C07D243/08 , C07D405/02
摘要: A compound of the formula (I), and pharmaceutically acceptable salts thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; Y is —CRC1RC2—(CH2)m—, where m is 0 or 1, Rc1 is selected from CH3 and CF3, and Rc2 is selected from H and CH3, or RC1 and RC2 together with the carbon atom to which they are attached form the 1,1-cyclopropylene group (a), 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, heterocyclic ring; Het is selected from: (i), 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 (ii), where Q is O or S.
摘要翻译: 式(I)的化合物及其药学上可接受的盐,其中:R 2,R 3,R 4和R 5独立地选自H,C 1-7烷氧基,氨基,卤素或羟基; Y是-CRC1RC2-(CH2)m-,其中m是0或1,Rc1选自CH3和CF3,Rc2选自H和CH3,或RC1和RC2与它们所连接的碳原子一起形成 1,1-环亚丙基(a),RN1和RN2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杂环基和C 5-20芳基; 或RN1和RN2与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:(i)其中Y1和Y3独立地选自CH和N,Y2选自CX和N,X是H,Cl或F; 和(ii),其中Q是O或S.
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