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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

WO2008075109A1 SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY 审中-公开
标题翻译：具有蛋白激酶抑制活性的替代哌啶
公开(公告)号：WO2008075109A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050776
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
发明人： WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , C07D519/00 , A61K31/437 , A61K31/52 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/34 , C07D519/00
摘要： The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR 5 ; J 1 -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 ); Q 3 is a bond or a saturated C 1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR 2 R 3 , CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R 1a and R 1b are the same or different and each is hydrogen or a substituent R 10 ; or R 1a and R 1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R 10 ; and R 2 , R 3 , R 4 , R 5 , R 7 , R 6 , R 8 , and R 10 are as defined in the claims.
摘要翻译：本发明提供了式（I）的PKA和PKB激酶抑制化合物; 或其盐，溶剂合物，互变异构体或N-氧化物，其中E是含有1,2,3或4个选自O，N和S的杂原子的五元杂芳基环，条件是不超过1个杂原子可以不是N; q和r各自为0或1; q + r为1或2; T是N或CR 5; J 1是N = C（R 6），（R 7）C = N，（R 8）N C（O），（R 8）2 CC（O），N = N或（R 0 > 7 ）C = C（R ^{6 ）; Q 3是任选被氟和羟基取代的键或饱和C 1-3烃连接基团; G是NR 2 R 3，CN或OH; m和n各自为0或1，条件是m + n为1或2，并且当环E的相邻环构件为S或O时，m或n各自为0; R 1a和R 1b相同或不同，各自为氢或取代基R 10; 或R 1a和R 1b与它们所连接的碳原子或杂原子一起形成5或6元芳基或杂芳基环，其中芳基或杂芳基环任选地被一个或多个取代基R 10取代; R 2，R 3，R 4，R 5，R 7， R 6，R 8和R 10如权利要求中所定义。}

3. 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。

4. 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。}}

5. 发明申请

WO2011141716A3 MODULATORS OF CHK-1 ACTIVITY 审中-公开
公开(公告)号：WO2011141716A3
公开(公告)日：2011-11-17
申请号：PCT/GB2011/000739
申请日：2011-05-12
申请人： SENTINEL ONCOLOGY LIMITED , BOYLE, Robert George , WALKER, David Winter , BOYCE, Richard Justin
发明人： BOYLE, Robert George , WALKER, David Winter , BOYCE, Richard Justin
IPC分类号： C07D241/26 , A61K31/4965 , A61P35/00
摘要： The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R 1 is cyano or C 1-4 alkyl; R 2 is hydrogen or C 1-4 alkyl; R 3 is hydrogen or C 1-4 alkyl; R 4 and R 5 are the same or different and each is selected from hydrogen, saturated C 1-4 hydrocarbyl and saturated C 1-4 hydrocarbyloxy; R 6 and R 7 are the same or different and each is selected from hydrogen, halogen, CN, C 1-4 alkyl and C 1-4 alkoxy wherein the C 1-4 alkyl and C 1-4 alkoxy are each optionally substituted with hydroxy, C 1-2 alkoxy or by one or more flourine atoms; R 8 is hydrogen or C 1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C 1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group -CH 2 CH 2 - which together with the said one carbon atom forms a cyclopropyl group; m is 1, 2, 3 or 4; n is 0 or 1; and Ar is a monocyclic or bicyclic aryl or heteroaryl group of 5 to 10 ring members containing 0, 1, 2, 3 or 4 heteroatom ring members selected from O, N and S, the aryl or heteroaryl group being optionally substituted with one to four substituents R 13 as defined in the claims. The compounds are inhibitors of Chk-1 kinase and are active against cancers.

6. 发明申请

WO2011141716A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2011141716A2
公开(公告)日：2011-11-17
申请号：PCT/GB2011000739
申请日：2011-05-12
申请人： SENTINEL ONCOLOGY LTD , BOYLE ROBERT GEORGE , WALKER DAVID WINTER , BOYCE RICHARD JUSTIN
发明人： BOYLE ROBERT GEORGE , WALKER DAVID WINTER , BOYCE RICHARD JUSTIN
IPC分类号： C07D241/26 , A61K31/4965 , A61P35/00
CPC分类号： C07D241/26 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61N5/10 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R1 is cyano or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy; R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms; R8 is hydrogen or C1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group -CH2CH2- which together with the said one carbon atom forms a cyclopropyl group; m is 1, 2, 3 or 4; n is 0 or 1; and Ar is a monocyclic or bicyclic aryl or heteroaryl group of 5 to 10 ring members containing 0, 1, 2, 3 or 4 heteroatom ring members selected from O, N and S, the aryl or heteroaryl group being optionally substituted with one to four substituents R13 as defined in the claims. The compounds are inhibitors of Chk-1 kinase and are active against cancers.
摘要翻译：本发明提供式（1）化合物或其盐，N-氧化物或其互变异构体; 其中R1是氰基或C1-4烷基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; R4和R5相同或不同，各自选自氢，饱和C 1-4烃基和饱和C 1-4烃氧基; R 6和R 7相同或不同，各自选自氢，卤素，CN，C 1-4烷基和C 1-4烷氧基，其中C 1-4烷基和C 1-4烷氧基各自任选被羟基，C 1-2烷氧基或通过一个或多个荧光原子; R8是氢或C1-4烷基; Q是部分Ar和氮原子N之间的长度为1至4个碳原子的亚烷基链，其中亚烷基链的1至4个碳原子中的一个或多个可以任选地被一个或两个C 1-4烷基基团，或其中亚烷基链的1至4个碳原子的一个碳原子可以任选被基团-CH 2 CH 2取代，所述基团与所述一个碳原子一起形成环丙基; m为1,2,3或4; n为0或1; 并且Ar是具有0至1个，2个，3个或4个选自O，N和S的杂原子环成员的5至10个环成员的单环或双环芳基或杂芳基，芳基或杂芳基任选被一至四个取代基R 13如权利要求中所定义。这些化合物是Chk-1激酶的抑制剂并且对癌症有活性。

7. 发明申请

WO2010007374A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2010007374A1
公开(公告)日：2010-01-21
申请号：PCT/GB2009/001759
申请日：2009-07-15
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： C07D401/12 , C07D401/14 , A61K31/33 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14
摘要： The invention provides kinase inhibitor compounds of the formula (1): or salts, solvates, tautomers or N-oxides thereof; wherein X is O, CO, X 1 C(X 2 ), C(X 2 )X 1 , X 1 C(X 2 )X 1 , S, SO, SO 2 , NR c , SO 2 NR C or NR c SO 2 ; m is 0-2; n is 0-1; q is 0-2; A is C 1-6 alkylene optionally interrupted by O; R 1 is halogen, cyano, nitro, an optionally substituted acyclic C 1-6 hydrocarbon group, optionally substituted C 3-7 cycloalkyl, optionally substituted phenyl, optionally substituted five membered heteroaryl, NR 2 R 3 , R a -R b , O-R b or C(O)NR 2 R 8 ; R 4 is fluorine, chlorine, methyl or cyano; R 2 is hydrogen or optionally substituted C 1-4 alkyl; R 3 is R a -R b ; or NR 2 R 3 forms a 4 to 7 membered non-aromatic heterocyclic ring; Ra is a bond, C(X 2 ), C(X 2 )X 1 , SO, SO 2 or SO 2 NR c ; R b is hydrogen or an optionally substituted 3 to 7- membered carbocyclic or heterocyclic ring or an optionally substituted C 1-12 acyclic hydrocarbon group; R c is hydrogen or a C 1-4 hydrocarbon group; R d is O, CO, X 1 C(X 2 ), C(X 2 )X 1 , X 1 C(X 2 )X 1 , S, SO, SO 2 , NRC, SO 2 NR c or NR c SO 2 ; X 1 is O, S or NR c ; X 2 is =0, =S or =NR c ; but excluding the compound wherein m, n and q are all O, A is CH 2 and NR 2 R 3 is a 2-phenylmorpholin-4-yl group.
摘要翻译：本发明提供式（1）的激酶抑制剂化合物：或其盐，溶剂合物，互变异构体或N-氧化物; 其中X是O，CO，X1C（X2），C（X2）X1，X1C（X2）X1，S，SO，SO2，NRc，SO2NRC或NRcSO2; m为0-2; n为0-1; q为0-2; A是任选被O中断的C 1-6亚烷基; R 1为卤素，氰基，硝基，任选取代的无环C 1-6烃基，任选取代的C 3-7环烷基，任选取代的苯基，任选取代的五元杂芳基，NR2R3，Ra-Rb，O-Rb或C（O）NR2R8 ; R4是氟，氯，甲基或氰基; R2是氢或任选取代的C 1-4烷基; R3是Ra-Rb; 或NR 2 R 3形成4至7元非芳族杂环; R a是键，C（X 2），C（X 2）X 1，SO，SO 2或SO 2 NR c; Rb是氢或任选取代的3至7元碳环或杂环或任选取代的C 1-12无环烃基; Rc是氢或C 1-4烃基; Rd为O，CO，X1C（X2），C（X2）X1，X1C（X2）X1，S，SO，SO2，NRC，SO2NRc或NRcSO2; X1是O，S或NRc; X2 = 0，= S或= NRc; 但不包括其中m，n和q全部为O的化合物，A为CH 2且NR 2 R 3为2-苯基吗啉-4-基。

8. 发明申请

WO2008075110A1 SUBSTITUTED PIPERIDINES CONTAINING A HETEROARYLAMIDE OR HETEROARYLPHENYL MOIETY 审中-公开
标题翻译：含有异烟酰胺或邻苯二酚的取代的哌啶
公开(公告)号：WO2008075110A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050777
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
IPC分类号： C07D487/04 , C07D473/34 , C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D473/34 , C07D487/04
摘要： The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R )x N * (GP1) (2) GP is a group GP2: 10 (R )r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claims
摘要翻译：本发明提供具有式（I）的PKA和PKB激酶抑制化合物的式（I）化合物：GP 1 JT 2 JN 4 RNH（I）或其盐，溶剂合物，互变异构体或N-氧化物，其中（1） GP是组GP1：HET 2a a QG（HNCO）f 7（R）x N *（GP1）（2）GP是组GP2：10（R）r O 2a a QG（CH 2）w NVHN * ）其中HET是含有至多4个杂原子环成员的单环或双环杂环基; 环V是5至10个环成员的单环或双环杂芳基; 并且J1，J2，R4，R7，R10，Q2a，Ga，x，w和f如权利要求中所定义

9. 发明申请

WO2007125325A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125325A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001522
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00 , C07D473/34
摘要： The invention provides compounds of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein J 1 -J 2 is CH=CH, N=CH, CH=N, HN-C(O) or CH 2 CO; T is N or CH and GP is as defined in the claims. The compounds have activity as inhibitors of PKA and PKB kinases and are useful in the treatment of cancers.
摘要翻译：本发明提供了式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中J 1是H，CH = CH，N = CH，CH = N，HN-C（O）或CH 2 CO; T是N或CH，GP如权利要求中所定义。该化合物具有作为PKA和PKB激酶抑制剂的活性，可用于治疗癌症。

10. 发明申请

WO2006136830A1 ARYL-ALKYLAMINES AND HETEROARYL-ALKYLAMINES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： ARYL-ALKYLAMINES和异丁烯酰胺作为蛋白激酶抑制剂
公开(公告)号：WO2006136830A1
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002287
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , DOWNHAM, Robert , HAMLETT, Christopher , HOWARD, Steven , SORE, Hannah, Fiona , VERDONK, Marinus, Leendert , WALKER, David, Winter , LUKE, Richard, William, Arthur
发明人： WOODHEAD, Steven, John , DOWNHAM, Robert , HAMLETT, Christopher , HOWARD, Steven , SORE, Hannah, Fiona , VERDONK, Marinus, Leendert , WALKER, David, Winter , LUKE, Richard, William, Arthur
IPC分类号： C07D231/12 , A61K31/415 , A61P37/02
CPC分类号： C07D231/12
摘要： The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y 1 and Y 2 is CH and the other is selected from CH, CR 8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y 1 or Y 2 is CR 8 ; R 1 is an aryl or heteroaryl group of 5 to 10 ring members; R 2a and R 3a each are hydrogen, C 1-4 hydrocarbyl or C 1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR 2a R 3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R 18 is hydrogen or methyl; R 19 is hydrogen or methyl; R 24 is hydrogen or R 24 , R 2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R 25 is hydrogen or a C 1-4 alkyl group wherein the C 1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R 25 is attached; and R4 and R 5 each are hydrogen or a substituent as defined in the claims
摘要翻译：本发明提供式（II）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中n为0或1; Y 1和Y 2中的一个是CH，另一个选自CH，CR 8和N; q为0,1或2，条件是当Y 1或Y 2为CR 8时q为0或1。 R 1是5至10个环成员的芳基或杂芳基; R 2a和R 3a各自为氢，C 1-4 - 烃基或C 1-4 - 酰基，其中，烃基和酰基部分任选被氟，羟基，氨基，甲基氨基，二甲基氨基或甲氧基取代; 或NR 2a R 3a形成任选含有选自O和N的第二杂原子环成员的咪唑基或饱和单环4-7元杂环基; R 18是氢或甲基; R 19是氢或甲基; R 24是氢或R 24，R 2a和中间的氮原子和碳原子一起形成氮杂环丁烷，吡咯烷或哌啶环; R 25是氢或C 1-4烷基，其中C 1-4烷基任选被羟基或氨基取代，条件是在羟基或氨基与R 25连接的氧原子之间至少有两个碳原子; 且R 4和R 5各自为氢或权利要求中所定义的取代基

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