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1. 发明专利

IL291570A Pharmaceutical compounds 未知
公开(公告)号：IL291570A
公开(公告)日：2022-05-01
申请号：IL29157022
申请日：2022-03-21
申请人： SENTINEL ONCOLOGY LTD , ROBERT GEORGE BOYLE , MERIEL RUTH MAJOR , STUART TRAVERS , DAVID WINTER WALKER , MICHAL CZYZEWSKI , DEREK JOHN LONDESBROUGH , JULIAN SCOTT NORTHEN , STEFANIA SANTONI
发明人： ROBERT GEORGE BOYLE , MERIEL RUTH MAJOR , STUART TRAVERS , DAVID WINTER WALKER , MICHAL CZYZEWSKI , DEREK JOHN LONDESBROUGH , JULIAN SCOTT NORTHEN , STEFANIA SANTONI
摘要： The invention provides a composition of matter which: • (i) consists of at least 90 % by weight of an atropisomer (2A) and 0-10 % by weight of an atropisomer of formula (2B); or • (ii) consists of at least 90 % by weight of an atropisomer (2B) and 0-10 % by weight of an atropisomer of formula (2A); wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by: formula (2A) and formula (2B) or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R1 is trifluoromethyl; R2 is hydrogen; R3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R5 as defined herein; and R4; R5 when present, R6 and R7 independently selected from various substituents as defined herein. Also provided are individual atropisomers thereof as well as of various compounds having a five-membered heteroaromatic ring containing 1 or 2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, with three rings Ar1, X and Y, and substituents R1-R7 all being defined as in formulas (1A) or (1B) below; pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers. Formula (1A), formula (1B).

2. 发明专利

IL291570D0 Pharmaceutical compounds 未知
公开(公告)号：IL291570D0
公开(公告)日：2022-05-01
申请号：IL29157022
申请日：2022-03-21
申请人： SENTINEL ONCOLOGY LTD , ROBERT GEORGE BOYLE , MERIEL RUTH MAJOR , STUART TRAVERS , DAVID WINTER WALKER , MICHAL CZYZEWSKI , DEREK JOHN LONDESBROUGH , JULIAN SCOTT NORTHEN , STEFANIA SANTONI
发明人： ROBERT GEORGE BOYLE , MERIEL RUTH MAJOR , STUART TRAVERS , DAVID WINTER WALKER , MICHAL CZYZEWSKI , DEREK JOHN LONDESBROUGH , JULIAN SCOTT NORTHEN , STEFANIA SANTONI
IPC分类号： A61P35/00
摘要： The invention provides a composition of matter which: • (i) consists of at least 90 % by weight of an atropisomer (2A) and 0-10 % by weight of an atropisomer of formula (2B); or • (ii) consists of at least 90 % by weight of an atropisomer (2B) and 0-10 % by weight of an atropisomer of formula (2A); wherein the atropisomer of formula (2A) and the atropisomer of formula (2B) are represented by: formula (2A) and formula (2B) or are pharmaceutically acceptable salts or tautomers thereof, wherein ring X is a benzene or pyridine ring; ring Y is selected from a benzene ring, a pyridine ring and a thiophene ring; R1 is trifluoromethyl; R2 is hydrogen; R3 is hydrogen; m is 0 or 1; n is 0, 1 or 2; Ar1 is a monocyclic aromatic ring selected from benzene and pyridine; each monocyclic aromatic ring being unsubstituted or substituted with 1 or 2 substituents R5 as defined herein; and R4; R5 when present, R6 and R7 independently selected from various substituents as defined herein. Also provided are individual atropisomers thereof as well as of various compounds having a five-membered heteroaromatic ring containing 1 or 2 nitrogen atoms or 1 nitrogen and 1 oxygen atom, with three rings Ar1, X and Y, and substituents R1-R7 all being defined as in formulas (1A) or (1B) below; pharmaceutical compositions and the uses of the atropisomers and compositions are inhibitors of PLK1- and PLK4 kinases, for example in the treatment of cancers. Formula (1A), formula (1B).

3. 发明专利

AU7879398A Improved swim fin 未知
公开(公告)号：AU7879398A
公开(公告)日：1999-02-18
申请号：AU7879398
申请日：1998-08-05
申请人： NORMAN DAVID WINTER
发明人： NORMAN DAVID WINTER
IPC分类号： A63B31/11

4. 发明专利

AU2002395A Star post installation holder 未知
公开(公告)号：AU2002395A
公开(公告)日：1995-11-30
申请号：AU2002395
申请日：1995-05-12
申请人： BARRY DAVID WINTER
发明人： WINTER BARRY DAVID
IPC分类号： E04H17/08 , E04H17/26

5. 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。

6. 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。

7. 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.

8. 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。

9. 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。

10. 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

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