公开(公告)号：US20070093489A1

公开(公告)日：2007-04-26

申请号：US11550004

申请日：2006-10-17

Applicant: Muhammad Javaid ,  Keith Menear ,  Sylvie Gomez ,  Marc Hummersone ,  Niall Martin ,  Graeme Smith ,  Xiao-Ling Cockcroft

Inventor： Muhammad Javaid ,  Keith Menear ,  Sylvie Gomez ,  Marc Hummersone ,  Niall Martin ,  Graeme Smith ,  Xiao-Ling Cockcroft

IPC: A61K31/53

CPC classification number: C07D403/10 ,  C07D403/14 ,  C07D411/14 ,  C07D413/14 ,  C07D487/04

Abstract: 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.

公开(公告)号：US20060063767A1

公开(公告)日：2006-03-23

申请号：US11213504

申请日：2005-08-26

Applicant: 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

Inventor： 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: A61K31/502 ,  C07D403/02

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D417/06

Abstract: 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.

Abstract translation: 式（I）的化合物：

公开(公告)号：US20060135770A1

公开(公告)日：2006-06-22

申请号：US11315528

申请日：2005-12-22

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

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

IPC: C07D403/14

CPC classification number: 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

Abstract: 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.

Abstract translation: 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.