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1. 发明申请

WO2010136755A1 SUBSTITUTED BENZOTRIAZINES AND QUINOXALINES AS INHIBITORS OF P7OS6 KINASE 审中-公开
标题翻译：作为P7OS6激酶的抑制剂的取代苯甲酸和喹唑啉
公开(公告)号：WO2010136755A1
公开(公告)日：2010-12-02
申请号：PCT/GB2010/001036
申请日：2010-05-26
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , WALKER, David, Winter
发明人： BOYLE, Robert, George , WALKER, David, Winter
IPC分类号： C07D401/14 , C07D403/04 , C07D409/14 , A61K31/498 , A61K31/53 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D409/14
摘要： The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X 1 is N or N + (O ); X 2 is N or CH; Q is a C 1-3 alkylene group; R 1 is selected from hydrogen, C 1-4 hydrocarbyl and hydroxy-C 2-4 hydrocarbyl; R 2 , R 3 and R 4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar 2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.
摘要翻译：本发明提供式（1）化合物或其盐或互变异构体; 其中X1是N或N +（O）; X2是N或CH; Q为C1-3亚烷基; R 1选自氢，C 1-4烃基和羟基-C 2-4烃基; R2，R3和R4相同或不同，各自选自氢，氟，氯和甲基; Ar1是任选取代的含有0,1或2个选自O，N和S的杂原子环成员或萘环的单环5或6元芳基或杂芳环，Ar 2是任选取代的单环5或6元杂芳基环含有1,2或3个选自O，N和S的杂原子环成员。式（1）化合物是p70S6激酶的抑制剂，可用于治疗增殖性疾病。

2. 发明申请

WO2008059259A3 ANTICANCER COMPOUNDS WITH A BENZO ( 1, 2, 4 ) TRIAZIN-3YL-AMINE CORE 审中-公开
公开(公告)号：WO2008059259A3
公开(公告)日：2008-05-22
申请号：PCT/GB2007/004371
申请日：2007-11-16
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , TRAVERS, Stuart
发明人： BOYLE, Robert, George , TRAVERS, Stuart
IPC分类号： C07D401/04 , C07D403/04 , C07D405/04 , C07D253/07
摘要： The invention provides compounds of the formulae (1), (2) and (3): (1, 2, 3), or salts, solvates or tautomers thereof; wherein G, A,v, m, X a , X b , X c , X d , X e , R 2 , R 3 , R 4 , Ar 1 , Ar 2 , R 6 , R 10 , R 11 , R 12 and R 13 are as defined in the claims. The compounds have activity against various kinases or, in the case of N-oxides, are reduced in hypoxic tissues to give compounds having kinase inhibiting activity.

3. 发明申请

WO2008139152A1 N-OXIDE-CONTAINING PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：含氧化氮的药物化合物
公开(公告)号：WO2008139152A1
公开(公告)日：2008-11-20
申请号：PCT/GB2008/001595
申请日：2008-05-09
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , TRAVERS, Stuart
发明人： BOYLE, Robert, George , TRAVERS, Stuart
IPC分类号： C07C291/04 , C07C311/32 , C07D401/12 , C07D403/14 , C07D417/14 , A61K31/13 , A61P35/00 , C07D413/14 , C07D417/12
CPC分类号： C07D401/12 , A61K9/0019 , A61K9/19 , A61K31/13 , C07C291/04 , C07C311/08 , C07C2603/26 , C07D403/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention provides a method of preparing a therapeutically active compound having reduced hERG activity, which method comprises: (a) selecting a non-N-oxide drug compound containing a basic tertiary amino group, wherein said non-N-oxide compound is known to have or is suspected of having a therapeutically unacceptable level of hERG inhibitory activity; (b) testing the non-N-oxide drug compound for hERG inhibitory activity; (c) reacting the non-N-oxide drug compound with an oxidising agent to form an N- oxide drug compound having an N-oxide at the basic tertiary amino group; (d) testing the N-oxide drug compound for hERG inhibitory activity; (e) testing the N-oxide drug compound for therapeutically useful activity; (f) comparing the hERG inhibitory activity of the N-oxide drug compound and non- N-oxide drug compound; and (g) when the N-oxide drug compound has therapeutically useful activity and has hERG activity which is at least ten fold less than the hERG inhibitory activity of the non-N-oxide drug compound, formulating the N-oxide drug compound for use in medicine. Also provided by the invention are novel compounds prepared by the aforementioned method and the use of the novel compounds in medicine.
摘要翻译：本发明提供了制备具有降低的hERG活性的治疗活性化合物的方法，该方法包括：（a）选择含有碱性叔氨基的非N-氧化物药物化合物，其中所述非N-氧化物化合物已知为有或怀疑具有治疗上不可接受的水平的hERG抑制活性; （b）测试非N-氧化物药物化合物的hERG抑制活性; （c）使非N-氧化物药物化合物与氧化剂反应形成具有碱性叔氨基的N-氧化物的N-氧化物药物化合物; （d）测试N-氧化物药物化合物的hERG抑制活性; （e）测试N-氧化物药物化合物用于治疗有用的活性; （f）比较N-氧化物药物化合物和非N-氧化物药物化合物的hERG抑制活性; 和（g）当N-氧化物药物化合物具有治疗有用的活性并且具有比非N-氧化物药物化合物的hERG抑制活性小至少十倍的hERG活性时，配制使用的N-氧化物药物化合物在医学上。本发明还提供了通过上述方法制备的新型化合物和该新型化合物在医药中的应用。

4. 发明申请

WO2008015423A1 QUINOLINE AND QUINOXALINE N-OXIDES AS CHK-1 INHIBITORS 审中-公开
标题翻译：喹啉和喹喔啉N-氧化物作为CHK-1抑制剂
公开(公告)号：WO2008015423A1
公开(公告)日：2008-02-07
申请号：PCT/GB2007/002918
申请日：2007-08-01
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , TRAVERS, Stuart
发明人： BOYLE, Robert, George , TRAVERS, Stuart
IPC分类号： C07D241/52 , A61K31/498 , A61P35/00
CPC分类号： C07D241/52
摘要： The invention provides compounds of the formula (1) or salts, solvates or tautomers thereof; wherein Y 1 and Y 2 are both N + -O - or one of Y 1 and Y 2 is N and the other is N + -O - ; G is CH 2 , O, NH, NHCO or CONH; A is a group (CH 2 ) n where n is 1 to 4 provided that when G is O or NH, n is at least 2; Q is N or N + -O - ; V 2 is nitrogen or a group CR 5 ; V 3 is nitrogen or a group CR 5 ; V 4 is nitrogen or CH; provided that no more than two of V 2 , V 3 and V 4 are nitrogen; R 1 and R 2 are the same or different and each is hydrogen or a substituent R 6 ; R 3 and R 4 are the same or different and each is hydrogen or C 1-4 alkyl; or R 3 and R 4 together with the nitrogen atom to which they are attached form an azetidine, pyrrolidine, piperidine, piperazine, N-methylpiperazine or morpholine group; provided that when Q is N + -O - , then R 3 and R 4 are both other than hydrogen; R 5 is hydrogen or a substituent R 6 ; and R 6 is as defined in the claims. The compounds of formula (1) are reduced under hypoxic conditions such as those found in solid tumour cells to give compounds that inhibit or modulate Chk-1 kinase.
摘要翻译：本发明提供式（1）化合物或其盐，溶剂合物或互变异构体; 其中Y 1和Y 2都是N O - ， - O - O - 或Y 1 - / SUP>和Y 2是N，另一个是N + - O - O - G是CH 2，O，NH，NHCO或CONH; A是一个基团（CH 2）n n其中n是1至4，条件是当G是O或NH时，n至少为2; Q是N或N + O - - O - V 2是氮或基团CR 5; V 3是氮或基团CR 5; V 4是氮或CH; 条件是V 2，V 3和V 4中不超过2个为氮; R 1和R 2相同或不同，各自为氢或取代基R 6; R 3和R 4相同或不同，各自为氢或C 1-4烷基; 或R 3和R 4与它们所连接的氮原子一起形成氮杂环丁烷，吡咯烷，哌啶，哌嗪，N-甲基哌嗪或吗啉基团; 条件是当Q是N + O - O - 时，R 3和R 4都不是氢 ; R 5是氢或取代基R 6; 和R 6如权利要求中所定义。式（1）的化合物在例如在实体瘤细胞中发现的缺氧条件下被还原，得到抑制或调节Chk-1激酶的化合物。

5. 发明申请

WO2007144579A1 N-OXIDES OF DIARYLUREA DERIVATIVES AND THEIR USE AS CHK1 INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：二恶嗪衍生物的N-氧化物及其用作治疗癌症的CHK1抑制剂
公开(公告)号：WO2007144579A1
公开(公告)日：2007-12-21
申请号：PCT/GB2007/002123
申请日：2007-06-08
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , TRAVERS, Stuart
发明人： BOYLE, Robert, George , TRAVERS, Stuart
IPC分类号： C07D213/75 , C07D241/20 , C07D401/12 , A61K31/395 , A61P35/00
CPC分类号： C07D401/12 , C07D213/75 , C07D241/20
摘要： The invention provides a Chk-1 kinase inhibiting compound of the formula (I) or a salt, solvate or tautomer thereof, wherein: G is CH 2 , O, NH, NHCO or CONH; A is a group (CH 2 ) n where n is 1 to 4 provided that when G is O or NH, n is at least 2; X 1 is nitrogen or CH; X 2 is nitrogen or a group CR 5 ; X 3 is nitrogen or a group CR 5 ; X 4 is nitrogen or CH; provided that no more than two of X 2 , X 3 and X 4 are nitrogen; and R 1 ; R 2 ; R 3 ; R 4 ;R 5 and R 6 are as defined in the claims.
摘要翻译：本发明提供了抑制式（I）的Chk-1激酶化合物或其盐，溶剂合物或互变异构体，其中：G为CH 2，O，NH，NHCO或CONH; A是一个基团（CH 2）n n其中n是1至4，条件是当G是O或NH时，n至少为2; X 1是氮或CH; X 2是氮或CR 5; X 3是氮或基团CR 5; X 4是氮或CH; 条件是X 2，X 3和X 4不超过2个为氮; 和R 1; [R ^{2 ; [R ^{3 ; R 4，R 5和R 6如权利要求中所定义。}}

6. 发明申请

WO2008015429A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008015429A2
公开(公告)日：2008-02-07
申请号：PCT/GB2007/002926
申请日：2007-08-01
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert, George , TRAVERS, Stuart
发明人： BOYLE, Robert, George , TRAVERS, Stuart
IPC分类号： C07D241/44 , C07D241/52 , C07D253/08 , A61K31/53
CPC分类号： C07D253/10 , C07D241/44 , C07D241/52 , C07D401/04
摘要： The invention provides a compound of the formula (1) or a salt, solvate or tautomer thereof, having PARP inhibitor activity. In formula (1), Q is CN or CONH 2 and is attached at either position "a" or position "b" on the benzene ring; Y 1 is N or N + -O - ; Y 2 is N or CR 3 ; Y 3 is N or N + -O - ; provided that when Y 2 is CR 3 , then Y 3 is N + -O - ; m is 0, 1 or 2; and R 1 and R 2 are as defined in the claims.
摘要翻译：本发明提供了具有PARP抑制剂活性的式（1）化合物或其盐，溶剂化物或互变异构体。在式（1）中，Q是CN或CONH 2并且连接在任何位置“a” 或位置“b” 在苯环上; Y ^{1 是N或N <+> <-O> - ^{- ; Y 2是N或CR 3; Y 3是N或N + + - ^{- ^{- ; 条件是当Y 2是CR 3 3时，那么Y 3是N + 0-O- / SUP>; m是0,1或2; R 1和R 2如权利要求中所定义。}}}}

7. 发明申请

WO2006136829A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006136829A2
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002286
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , ASTRAZENECA AB , CANCER RESEARCH TECHNOLOGY LIMITED , SORE, Hannah, Fiona , BOYLE, Robert, George , HAMLETT, Christopher , SAXTY, Gordon , VERDONK, Marinus, Leendert , WALKER, David, Winter , WOODHEAD, Steven, John , HOWARD, Steven
发明人： CANCER RESEARCH TECHNOLOGY LIMITED , SORE, Hannah, Fiona , BOYLE, Robert, George , HAMLETT, Christopher , SAXTY, Gordon , VERDONK, Marinus, Leendert , WALKER, David, Winter , WOODHEAD, Steven, John , HOWARD, Steven
IPC分类号： C07D231/12 , C07D401/10 , C07D401/12 , C07D401/14
CPC分类号： C07D231/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof; wherein A is a saturated hydrocarbon linker group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; L 1 is a bond or a linker selected from C 1 -C 4 alkenylene, C 1 -C 4 alkynylene, -CONR’, -NR’CO, -S, -C(O)-, -C(NR 11 )-, -C(S)-, -N(R 11 ) 2 , C(=CHR 11 ), -SO- and -SO 2- ; or L 1 together with t R 16 forms and 8-12 membered fused bicyclic heteroaryl ring system; L 3 is a bond or a linker selected from CONH and HNCO; provided that L 1 and L 3 cannot both be linkers simultaneously; and provided also that L 1 and L 3 cannot both be a bond simultaneously; R 16 is an optionally substituted 5- to 12-membered monocyclic or bicyclic carbocyclic or heterocyclic ring; L 2 is absent or is a linker selected from C]-C4 alkylene, Ci-C4 alkenylene, Ci-C4 alkynylene, -CONR’-, -NR’CO-, -O-, -S-, -C(O)-, C(=CHR 11 ), C(S)-, -N(R 11 ) 2 , C 3-4 cycloalkanediyl, -SO- and -SO2-; R 17 is absent or is C 1-6 alkyl or an optionally substituted 5 to 12 membered carbocyclic or heterocyclic ring; provided that when R 17 is absent, then L 2 is also absent; and R 2 , R 3 , R 4 , R 5 , R 11 and R’ are as defined in the claims.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中A是饱和烃连接基团; E是单环或双环碳环或杂环基; L 1是选自C 1 -C 4亚链烯基，C 1 -C 3链烯基的键或连接基团， -CONR'，-NR'CO，-S，-C（O） - ， - C（NR 11） - ， - C（S） - ， -N（R 11）2，C（= CHR 11），-SO-和-SO 2 - >; 或L 1连同t R 16形式和8-12元稠合双环杂芳基环系统; L 3是选自CONH和HNCO的键或接头; 条件是L 1和L 3不能同时都是接头; 并且还提供了L 1和L 3不能同时是键; R 16是任选取代的5至12元单环或双环碳环或杂环; L 2不存在或是选自C 1 -C 4亚烷基，C 1 -C 4亚烯基，C 1 -C 4亚炔基，-CONR' - ， - NR'CO - ， - O - ， - S - ， - （O） - ，C（= CHR 11），C（S） - ， - N（R 11） C 3-4环烷二基，-SO-和-SO 2 - ; R 17不存在或为C 1-6烷基或任选取代的5至12元碳环或杂环; 条件是当R 17不存在时，L 2也不存在; 和R 2，R 3，R 4，R 5，R 11，和R'如权利要求中所定义。

8. 发明申请

WO2006051290A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006051290A2
公开(公告)日：2006-05-18
申请号：PCT/GB2005/004323
申请日：2005-11-09
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , WALKER, David, Winter , CALDWELL, John , COLLINS, Ian
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , WALKER, David, Winter , CALDWELL, John , COLLINS, Ian
IPC分类号： A61K31/505 , A61P35/00 , C07D239/88 , C07D401/12 , C07D401/04 , C07D401/06 , C07D403/12
CPC分类号： C07D403/12 , A61K31/505 , C07D239/88 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B, wherein the ring Q is a benzene ring; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a are absent, or A is a saturated optionally substituted C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R 1 , R la , R 2 , and R 3 are each H; halogen; C 1-6 hydrocarbyl optionally substituted by halogen, OH or C 1-2 alkoxy; CN; CONHR 8 ; NH 2 ; NHCOR 10 or NHCONHR 10 ; R 4 is H or C 1-4 alkyl; R 4a is H, C 1-4 alkyl or a group R 9 ; R 5 and R 6 are each selected from H, R 9 and C 1-4 hydrocarbyl optionally substituted by halogen, C 1-2 alkoxy or R 9 ;or NR 5 R 6 forms a saturated 4-7 membered monocyclic heterocyclic group; R 7 is H or C 1-4 alkyl; R 8 and R 8a each H or saturated C 1-4 hydrocarbyl optionally substituted by fluorine; R 9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R 4 , R 4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR 5 R 6 , R 4 and A form a saturated 4-7 membered monocyclic heterocycle; or R 4 , together with R 7 or R 8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR 5 R 6 and R 7 or R 8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R 10 is optionally substituted phenyl or benzyl.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症，其中环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7，NR 7 CO，C（R 8）= C（R 8）或（R 8）其中X是O，S或NR 7（其中X是O，S或NR 7）其中X是O，S或NR 7 ; 条件是当J 2是-J 1，R 1是N-CO时，E不是NR 7 CO ; m和n各自为0或1，其中m + n = 1或2; A是键，R 4和R 4a不存在，或A是饱和的任选取代的C 1-7烃连接基团，其具有在E和G之间延伸的5个原子的最大链长度，连接基团A中的一个碳原子任选地被O或N取代; R 1，R 2，R 2，R 3和R 3各自为H; 卤素; 任选被卤素，OH或C 1-12烷氧基取代的C 1-6烷基; CN; CONHR ^{8 ; NH _{2 ; NHCOR 10或NHCONHR 10; R 4是H或C 1-4烷基; R 4a是H，C 1-4烷基或基团R 9; R 5和R 6各自选自H，R 9和C 1-4烃基，任选被卤素，C 1-2烷氧基或R 9或NR 5 R 6形成饱和的4-7 元环杂环基; R 7是H或C 1-4烷基; 每个H或任选被氟取代的饱和C 1-4烃基的R 8和R 8 8a; R 9是含有至多3个选自N，O和S的环杂原子的单环或双环碳环或杂环基; 或R 4，R 4a和A一起形成饱和单环4-7元杂环; 或NR 5 R 6，R 4和A形成饱和的4-7元单环杂环; 或R 4，...，以及R 7或R 8，A和E形成4-7元饱和单环杂环; 或NR 5 R 6和R 7或R 8与A和E一起形成4-7元环饱和单环杂环; R 10是任选取代的苯基或苄基。}}

9. 发明申请

WO2006046024A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046024A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004119
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J l -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q 1 is a bond or a saturated C 1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen; R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的化合物，该化合物是式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T是N或CR 5 >; N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q 1是一个键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选地被氧或氮原子代替，或相邻的一对碳原子可以被CONR Q或Q Q取代，其中R q是氢或甲基，或R 0 q是与R 1连接的C 1-4亚烷基链或Q 1的碳原子以形成环状的部分; 并且其中连接基团Q 1的碳原子可以任选地具有一个或多个选自氟和羟基的取代基; Q 2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可以任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q 2不是键; G是氢，NR 2 R 3，OH或SH，条件是当E是芳基或杂芳基且Q 2是键时，则G 是氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3 ，则Q 2是一个键; 和R 2，R 2，R 3，R 4，R 4， SUP＆gt;和R＆gt; 8如权利要求中所定义。}

10. 发明申请

WO2005061463A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：WO2005061463A1
公开(公告)日：2005-07-07
申请号：PCT/GB2004/005464
申请日：2004-12-23
申请人： ASTEX TECHNOLOGY LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis
发明人： BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis
IPC分类号： C07D231/12
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R l and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the inker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR 2 R 3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R l is an aryl or heteroaryl group; and R 2 , R 3 , R 4 and R 5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译：本发明提供下式的化合物：（I）具有蛋白激酶B抑制活性：其中A是含有1至7个碳原子的饱和烃连接基团，该连接基团的最大链长度在R 1之间延伸 >和NR 2 R 3，并且在E和NR 2 R 3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选地被氧或氮代替原子; 并且其中，墨水基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R'位于碳原子a时，并且条件是当存在的氧代基位于相对于NR 2 R 3基团的碳原子a时; E是单环或双环碳环或杂环基; R 1是芳基或杂芳基; R 2，R 3，R 4和R 5如权利要求中所定义。还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

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