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1. 发明申请

US20100240686A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：US20100240686A1
公开(公告)日：2010-09-23
申请号：US12304003
申请日：2007-06-20
申请人： Clifford Jones , Zbigniew Stanley Matusiak
发明人： Clifford Jones , Zbigniew Stanley Matusiak
IPC分类号： A61K31/506 , C07D403/04 , A61P35/00 , A61P35/02 , A61P17/06 , A61P37/00 , A61P25/00 , A61P29/00 , A61P19/00 , A61P27/02
CPC分类号： C07D403/04
摘要： Compounds of formula (I): which possess cell-cycle inhibitory activity are described.
摘要翻译：描述了具有细胞周期抑制活性的式（I）化合物。

2. 发明申请

US20120190679A1 Novel Protein Kinase B Inhibitors - 060 审中-公开
标题翻译：新型蛋白激酶B抑制剂 - 060
公开(公告)号：US20120190679A1
公开(公告)日：2012-07-26
申请号：US13324191
申请日：2011-12-13
申请人： Paul David Johnson , Andrew Leach , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Jeffrey James Morris
发明人： Paul David Johnson , Andrew Leach , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Jeffrey James Morris
IPC分类号： A61K31/519 , A61K31/52 , A61P35/00 , C07D473/34 , C07D487/04 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/519 , C07D473/34
摘要： The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
摘要翻译：本发明涉及一组新的式（I）化合物或其盐：其中Y，Z 1，Z 2，R 1，R 4，R 5和n如说明书中所述，其可用于治疗或预防通过蛋白激酶B（PKB）如癌症介导的疾病或医学病症。本发明还涉及包含所述化合物的药物组合物，使用所述化合物治疗由PKB介导的疾病的方法和制备式（I）化合物的方法。

3. 发明申请

US20090163524A1 Novel Protein Kinase B Inhibitors - 060 有权
标题翻译：新型蛋白激酶B抑制剂 - 060
公开(公告)号：US20090163524A1
公开(公告)日：2009-06-25
申请号：US12249477
申请日：2008-10-10
申请人： Paul David Johnson , Andrew Leach , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Jeffrey James Morris
发明人： Paul David Johnson , Andrew Leach , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Jeffrey James Morris
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04 , A61K31/519 , C07D473/34
摘要： The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
摘要翻译：本发明涉及一组新的式（I）化合物或其盐：其中Y，Z 1，Z 2，R 1，R 4，R 5和n如说明书中所述，其可用于治疗或预防通过蛋白激酶B（PKB）如癌症介导的疾病或医学病症。本发明还涉及包含所述化合物的药物组合物，使用所述化合物治疗由PKB介导的疾病的方法和制备式（I）化合物的方法。

4. 发明申请

US20100093748A1 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：US20100093748A1
公开(公告)日：2010-04-15
申请号：US12520303
申请日：2007-12-21
申请人： Steven John Woodhead , Martyn Frederickson , Christopher Hamlett , Andrew James Woodhead , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Peter Blurton , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Andrew Leach , Jeffrey James Morris
发明人： Steven John Woodhead , Martyn Frederickson , Christopher Hamlett , Andrew James Woodhead , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Peter Blurton , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Andrew Leach , Jeffrey James Morris
IPC分类号： A61K31/497 , C07D487/04 , A61K31/519 , C07D471/04 , A61K31/437
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 CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, 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; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b 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 R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.
摘要翻译：本发明提供式（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为N或CR5基团; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; Q3是任选被氟和羟基取代的键或饱和C 1-3烃连接基团; G为NR2R3，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; R1a和R1b相同或不同，各自为氢或取代基R10; 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被一个或多个取代基R 10取代; 并且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。

5. 发明申请

US20080293687A1 Benzamide Compounds 有权
标题翻译：苯甲酰胺化合物
公开(公告)号：US20080293687A1
公开(公告)日：2008-11-27
申请号：US11661498
申请日：2005-08-31
申请人： Keith Hopkinson Gibson , Elaine Sophie Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Andrew Graham
发明人： Keith Hopkinson Gibson , Elaine Sophie Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Andrew Graham
IPC分类号： A61K31/4427 , C07D213/85 , A61K31/44 , A61K31/496 , A61P35/00 , C07D401/14 , C07D401/06
CPC分类号： C07D417/12 , C07D213/85 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D487/08
摘要： The invention concerns benzamide compounds of Formula (I), wherein R1a, R1b, R1c, R2, R3, R4, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).
摘要翻译：本发明涉及式（I）的苯甲酰胺化合物，其中R1a，R1b，R1c，R2，R3，R4，m和n具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对组蛋白脱乙酰酶（HDAC）的抑制敏感的肿瘤或其它增殖病症中的抗增殖剂的药物中的用途。

6. 发明授权

US5789417A Tricyclic compounds with pharmaceutical activity 失效
标题翻译：具有药物活性的三环化合物
公开(公告)号：US5789417A
公开(公告)日：1998-08-04
申请号：US432161
申请日：1995-06-28
申请人： Francis Thomas Boyle , James William Crook , Zbigniew Stanley Matusiak
发明人： Francis Thomas Boyle , James William Crook , Zbigniew Stanley Matusiak
IPC分类号： A61K31/505 , A61K31/517 , A61K31/519 , A61P35/00 , C07D239/70 , C07D401/12 , C07D403/12 , A61K31/495
CPC分类号： C07D401/12 , C07D239/70 , C07D403/12
摘要： The invention relates to tricyclic compounds of formula (I) ##STR1## wherein R.sup.1 is hydrogen, amino, (1-4C)alkyl, (1-4C)alkoxy, hydroxy-(1-4C)alkyl or fluoro-(1-4C)alkyl; R.sup.2 is hydrogen, (1-4C)alkyl, (3-4C)alkenyl, (3-4C)alkynyl, hydroxy-(2-4C)alkyl, halogeno-(2-4C)alkyl or cyano-(1-4C)alkyl; Ar is optionally-substituted phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl; and R.sup.3 includes a group of the formula --NHCH(CO.sub.2 H)--A.sup.1 --Y.sup.1 wherein A.sup.1 is (1-6C)alkylene and Y.sup.1 is carboxy, tetrazol-5-yl, N-�(1-4C)alkylsulphonyl!carbamoyl, N(phenylsulphonyl)carbamoyl, tetrazol-5-ylthio, tetrazol-5-ylsulphinyl or tetrazol-5-ylsulphonyl; or pharmaceutically-acceptable salts or esters thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-cancer agents.
摘要翻译： PCT No.PCT / GB93 / 02281 Sec。 371日期：1995年6月28日 102（e）日期1995年6月28日PCT提交1993年11月4日PCT公布。出版物WO94 / 11354 日期：1994年5月26日本发明涉及式（I）的三环化合物其中R 1为氢，氨基，（1-4C）烷基，（1-4C）烷氧基，羟基 - （1-4C）烷基或氟 - （1-4C）烷基; R2是氢，（1-4C）烷基，（3-4C）烯基，（3-4C）炔基，羟基 - （2-4C）烷基，卤代 - （2-4C）烷基或氰基 - （1-4C）烷基; Ar是任选取代的亚苯基，噻吩二基，噻唑二基，吡啶二基或嘧啶二基; 并且R 3包括式-NHCH（CO 2 H）-A1-Y1的基团，其中A 1为（1-6C）亚烷基且Y 1为羧基，四唑-5-基，N - [（1-4C）烷基磺酰基]氨基甲酰基，N （苯基磺酰基）氨基甲酰基，四唑-5-基硫代，四唑-5-基亚磺酰基或四唑-5-基磺酰基; 或其药学上可接受的盐或酯; 制造过程; 含有它们的药物组合物; 并将其用作抗癌剂。

7. 发明授权

US08101623B2 Substituted pyrrolo[2,3-d]pyrimidine as a protein kinase B inhibitor 有权
标题翻译：取代的吡咯并[2,3-d]嘧啶作为蛋白激酶B抑制剂
公开(公告)号：US08101623B2
公开(公告)日：2012-01-24
申请号：US12249477
申请日：2008-10-10
申请人： Richard William Arthur Luke , Zbigniew Stanley Matusiak
发明人： Richard William Arthur Luke , Zbigniew Stanley Matusiak
IPC分类号： C07D487/04 , A61K31/519 , A61P35/04
CPC分类号： C07D487/04 , A61K31/519 , C07D473/34
摘要： The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I), methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
摘要翻译：本发明涉及一组新的式（I）化合物或其盐：其中Y，Z 1，Z 2，R 1，R 4，R 5和n如说明书中所述，其可用于治疗或预防通过蛋白激酶B（PKB）如癌症介导的疾病或医学病症。本发明还涉及包含式（I）化合物的药物组合物，使用所述化合物治疗PKB介导的疾病的方法和制备式（I）化合物的方法。

8. 发明授权

US07897778B2 Benzamide compounds 有权
标题翻译：苯甲酰胺化合物
公开(公告)号：US07897778B2
公开(公告)日：2011-03-01
申请号：US11661498
申请日：2005-08-31
申请人： Keith Hopkinson Gibson , Elaine Sophie Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Andrew Graham
发明人： Keith Hopkinson Gibson , Elaine Sophie Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Andrew Graham
IPC分类号： C07D401/00 , C07D211/78
CPC分类号： C07D417/12 , C07D213/85 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D487/08
摘要： The invention concerns benzamide compounds of Formula (I), wherein R1a, R1b, R1c, R2, R3, R4, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).
摘要翻译：本发明涉及式（I）的苯甲酰胺化合物，其中R1a，R1b，R1c，R2，R3，R4，m和n具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对组蛋白脱乙酰酶（HDAC）的抑制敏感的肿瘤或其它增殖病症中的抗增殖剂的药物中的用途。

9. 发明申请

US20100120798A1 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：US20100120798A1
公开(公告)日：2010-05-13
申请号：US12519993
申请日：2007-12-20
申请人： Steven John Woodhead , Christopher Hamlett , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Gregory Richard Carr , Jeffrey James Morris
发明人： Steven John Woodhead , Christopher Hamlett , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Gregory Richard Carr , Jeffrey James Morris
IPC分类号： A61K31/522 , A61K31/52 , C07D473/34 , A61P37/00 , A61P9/00 , A61P11/06 , A61P25/00 , A61P29/00 , 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

10. 发明申请

US20100075942A1 N-PHENYL-4-PYRIDIN-2-YL-BENZAMIDE DERIVATIVES AS HISTONE DEACYLASE (HDAC) INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：作为治疗癌症的HISTONE DEACYLASE（HDAC）抑制剂的N-苯基-4-吡啶-2-基-L-苯甲酰胺衍生物
公开(公告)号：US20100075942A1
公开(公告)日：2010-03-25
申请号：US11813838
申请日：2006-01-12
申请人： Keith Hopkinson Gibson , Elaine Sophie, Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Maybury , Craig Anthony Roberts
发明人： Keith Hopkinson Gibson , Elaine Sophie, Elizabeth Stokes , Michael James Waring , David Michael Andrews , Zbigniew Stanley Matusiak , Mark Maybury , Craig Anthony Roberts
IPC分类号： A61K31/4418 , C07D213/61 , C07D401/12 , C07D213/82 , C07D401/06 , A61K31/496 , A61K31/4523
CPC分类号： C07D213/82 , C07D213/61 , C07D213/65
摘要： The invention concerns benzamide derivatives of Formula (I) wherein R1a, R1b, R1c, R2, R3, R4, W, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of histone deacetylase (HDAC).
摘要翻译：本发明涉及式（I）的苯甲酰胺衍生物，其中R1a，R1b，R1c，R2，R3，R4，W，m和n具有本说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对组蛋白脱乙酰酶（HDAC）的抑制敏感的肿瘤或其它增殖病症中的抗增殖剂的药物中的用途。

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