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1. 发明授权

US5821246A Aniline derivatives 失效
标题翻译：苯胺衍生物
公开(公告)号：US5821246A
公开(公告)日：1998-10-13
申请号：US836362
申请日：1997-05-21
申请人： Dearg Sutherland Brown , Jeffrey James Morris , Andrew Peter Thomas
发明人： Dearg Sutherland Brown , Jeffrey James Morris , Andrew Peter Thomas
IPC分类号： A61K31/505 , A61K31/517 , A61P35/00 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/51 , A61K31/535 , C07D239/82 , C07D403/00
CPC分类号： C07D401/12 , C07D239/94 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention concerns aniline derivatives of formula I ##STR1## wherein m is 1, 2 or 3, n is 0, 1, 2 or 3, Q is phenyl or naphthyl or a 5- or 6-membered heteroaryl moiety containing 1, 2 or 3 heteroatoms selected from oxygen, nitrogen and sulfur, and X, R.sup.1 and R.sup.2 are defined in the claims; or pharmaceutical compositions containing them, and the methods of using the compounds as tyrosine kinase inhibitors and for the treatment of proliferative diseases such as cancer.
摘要翻译： PCT No.PCT / GB95 / 02606 Sec。 371日期：1997年5月12日 102（e）日期1997年5月12日PCT提交1995年11月8日PCT公布。公开号WO96 / 15118 日期：1996年5月23日本发明涉及式I的苯胺衍生物（I）其中m为1,2或3，n为0,1,2或3，Q为苯基或萘基或5-或6-元含有1,2或3个选自氧，氮和硫的杂原子的杂芳基部分，X，R 1和R 2定义在权利要求中; 或含有它们的药物组合物，以及使用该化合物作为酪氨酸激酶抑制剂和治疗增殖性疾病例如癌症的方法。

2. 发明申请

US20090018134A1 Compounds - 945 审中-公开
标题翻译：化合物 - 945
公开(公告)号：US20090018134A1
公开(公告)日：2009-01-15
申请号：US12170128
申请日：2008-07-09
申请人： Kurt Gordon PIKE , Jeffrey James Morris
发明人： Kurt Gordon PIKE , Jeffrey James Morris
IPC分类号： A61K31/5377 , C07D413/04 , A61P35/04 , C07D413/14
CPC分类号： C07D413/14 , C07D413/04 , C07D417/14
摘要： A compound of formula (I) or a pharamaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.
摘要翻译：式（I）化合物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途，例如用于治疗增殖性疾病如癌症，特别是在由mTOR激酶介导的疾病中的用途，以及 /或一种或多种PI3K酶。

3. 发明授权

US07153964B2 Pyrimidine compounds 有权
标题翻译：嘧啶化合物
公开(公告)号：US07153964B2
公开(公告)日：2006-12-26
申请号：US10220139
申请日：2001-02-26
申请人： Elizabeth Janet Pease , Gloria Anne Breault , Jeffrey James Morris
发明人： Elizabeth Janet Pease , Gloria Anne Breault , Jeffrey James Morris
IPC分类号： C07D239/47 , C07D239/48 , C07D471/04 , C07D471/14 , A61K31/437 , A61P35/00
CPC分类号： C07D239/47 , C07D239/48 , C07D401/12 , C07D413/12 , C07D417/12
摘要： Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2 is substituted on a ring carbon by one group selected from sulphamoyl, N—(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), N,N-di-(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), C1-4alkylsulphonyl (optionally substituted by halo or hydroxy) or a substituent of the formula (Ia) or (Ia′): wherein Q1, Q2, G, R1, Y, Z, Q3, n and m are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) inhibitors are also described
摘要翻译：式（I）的嘧啶衍生物其中：Q 1'和Q 2个独立地选自如上所定义的任选取代的芳基或碳连接的杂芳基; 且Q 1和Q 2中的一个或Q 1和Q 2 2中的一个在环碳上被一个选自氨磺酰基，N-（C 1-4烷基）氨磺酰基（任选被卤素或羟基取代）的基团，N，N-二 - （C 1-4 - 烷基）氨磺酰基（任选被卤素或羟基取代），C 1-4烷基磺酰基（任选被卤素或羟基取代）或式（Ia）或（Ia'）的取代基：其中Q < Q 1，Q 2，G，R 1，Y，Z，Q 3，n和m如上定义中; 和其药学上可接受的盐和体内可水解的酯。还描述了其制备方法，药物组合物及其作为细胞周期蛋白依赖性丝氨酸/苏氨酸激酶（CDK）抑制剂的用途

4. 发明授权

US06649608B2 2,4-di(hetero-)arylamino (oxy)-5-substituted pyrimidines as antineoplastic agents 失效
标题翻译： 2,4-二（异 - ）芳基氨基（氧基）-5-取代的嘧啶作为抗肿瘤剂
公开(公告)号：US06649608B2
公开(公告)日：2003-11-18
申请号：US10203154
申请日：2002-08-06
申请人： Elizabeth Janet Pease , Gloria Anne Breault , Emma Jane Williams , Robert Hugh Bradbury , Jeffrey James Morris
发明人： Elizabeth Janet Pease , Gloria Anne Breault , Emma Jane Williams , Robert Hugh Bradbury , Jeffrey James Morris
IPC分类号： C07D23948
CPC分类号： C07D239/47 , C07D231/12 , C07D233/56 , C07D239/48 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D471/04
摘要： Pyrimidine derivatives of the formula (I), wherein: Q1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one or both Q1 and Q2 are substituted on a ring carbon by one substituent of the formula (Ia) or (Ia′), wherein: Y, Z, n, m Q3, G, R1, are as defined within; and pharmaceutically acceptable salts and in in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.
摘要翻译：式（I）的嘧啶衍生物，其中：Q 1和Q 2独立地选自如上定义的任选取代的芳基或碳连接的杂芳基; 并且Q1和Q2中的一个或两个在环碳上由式（Ia）或（Ia'）的一个取代基取代，其中：Y，Z，n，m Q3，G，R 1如 ; 和其药学上可接受的盐及其体内可水解的酯。还描述了其制备方法，药物组合物及其作为细胞周期蛋白依赖性丝氨酸/苏氨酸激酶（CDK）和粘着斑激酶（FAK）抑制剂的用途。

5. 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。

6. 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。

7. 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。

8. 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

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