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公开(公告)号：US20130005702A1
公开(公告)日：2013-01-03
申请号：US13536174
申请日：2012-06-28
申请人： Valerio BERDINI , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio BERDINI , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/415 , C07D401/10 , A61K31/451 , A61K31/4439 , C12N5/09 , A61K31/5377 , A61K31/4155 , C07D403/10 , A61K31/551 , A61P35/00 , C07D231/12 , C07D413/10
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: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译： 本发明提供具有蛋白激酶B抑制活性的式（I）化合物：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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公开(公告)号：US20110144080A1
公开(公告)日：2011-06-16
申请号：US10596788
申请日：2004-12-23
申请人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/415 , C07D231/12 , C07D401/10 , A61K31/454 , A61K31/4439 , C07D413/10 , A61K31/5377 , C07D403/10 , A61K31/4155 , A61K31/496 , A61K31/497 , A61K31/551 , C07D401/04 , C07D401/14 , A61K31/4545 , A61P35/00
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 R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, 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 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 NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 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，连接基团在R1和NR2R3之间延伸的最大链长为5个原子 并且在E和NR2R3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原子替代; 并且其中连接基团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 3基团位于碳原子a时， 存在时的氧代基相对于NR 2 R 3基团位于碳原子a; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且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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公开(公告)号：US08691806B2
公开(公告)日：2014-04-08
申请号：US13536174
申请日：2012-06-28
申请人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/397 , 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: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译： 本发明提供具有蛋白激酶B抑制活性的式（I）化合物：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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公开(公告)号：US08247576B2
公开(公告)日：2012-08-21
申请号：US10596788
申请日：2004-12-23
申请人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
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 R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, 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 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 NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 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，连接基团在R1和NR2R3之间延伸的最大链长为5个原子 并且在E和NR2R3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原子替代; 并且其中连接基团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 3基团位于碳原子a时， 存在时的氧代基相对于NR 2 R 3基团位于碳原子a; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且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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公开(公告)号：US20090221579A1
公开(公告)日：2009-09-03
申请号：US11577155
申请日：2005-10-14
申请人： Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
发明人： Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
IPC分类号： A61K31/5377 , C07D239/47 , A61K31/513 , C07D413/10 , C12N9/99 , A61P25/28
CPC分类号： C07D239/47 , C07D401/06 , C07D401/08 , C07D403/08 , C07D405/08 , C07D405/12 , C07D405/14 , C07D409/08
摘要： This invention relates to novel compounds having the structural formula Ia or formula Ib: Ia Ib and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译： 本发明涉及具有结构式Ia或式Ib：Ia Ib的新化合物及其药学上可接受的盐，互变异构体或体内可水解的前体，组合物及其使用方法。 这些新型化合物提供治疗或预防Abeta相关病理学，如认知障碍，阿尔茨海默病，神经变性和痴呆。
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公开(公告)号：US20080287399A1
公开(公告)日：2008-11-20
申请号：US11721779
申请日：2005-12-12
申请人： Jeffrey Scott Albert , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Suzanna Cowan , Miles Stuart Congreve , Phil Edwards , Martyn Frederickson , Christopher William Murray , Sahil Patel
发明人： Jeffrey Scott Albert , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Suzanna Cowan , Miles Stuart Congreve , Phil Edwards , Martyn Frederickson , Christopher William Murray , Sahil Patel
IPC分类号： A61K31/675 , A61K31/497 , A61K31/47 , C07D215/12 , C07F9/28 , C07D413/02 , C07D401/02 , A61K31/5377 , A61P25/28
CPC分类号： C07D213/73 , C07D213/74 , C07D213/81 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/10 , C07D409/14 , C07D413/12
摘要： This invention relates to novel compounds having the structural formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译： 本发明涉及具有结构式（I）的新化合物及其药学上可接受的盐，组合物和使用方法。 这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。
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7.发明授权1,5-benzodiazepine derivatives having CCK antagonistic or agonistic activity 失效具有CCK拮抗或激动活性的1,5-苯并二氮杂衍生物
公开(公告)号：US5646140A
公开(公告)日：1997-07-08
申请号：US525659
申请日：1995-10-13
申请人： Elizabeth Ellen Sugg , Christopher Joseph Aquino , Jerzy Ryszard Szewczyk , Harry Finch , Robin Arthur Ellis Carr
发明人： Elizabeth Ellen Sugg , Christopher Joseph Aquino , Jerzy Ryszard Szewczyk , Harry Finch , Robin Arthur Ellis Carr
IPC分类号： A61K38/00 , A61K31/551 , A61K38/02 , A61P3/00 , A61P5/00 , A61P43/00 , C07D243/12 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/097 , A61K31/55
CPC分类号： C07K5/0821 , C07K5/0202 , C07K5/0207 , C07K5/06139 , C07K5/06191 , C07K5/0827 , A61K38/00
摘要： This invention pertains to novel benzodiazepine compounds of formula (I) ##STR1## which exhibit agonistic activity for CCK-A receptors, enabling them to modulate the hormones gastrin and cholecystokinin (CCK) in mammals for use in medicine as anorectic agents in the regulation of appetite, the treatment of obesity and the maintenance of weight loss.
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公开(公告)号：US20090062282A1
公开(公告)日：2009-03-05
申请号：US11577154
申请日：2005-10-14
申请人： Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
发明人： Jeffrey Scott Albert , Don Andisik , James Arnold , Dean Brown , Owen Callaghan , James Campbell , Robin Arthur Ellis Carr , Gianni Chessari , Miles Stuart Congreve , Phil Edwards , James R. Empfield , Martyn Frederickson , Gerard M. Koether , Jennifer Krumrine , Russ Mauger , Christopher William Murray , Sahil Patel , Mark Sylvester , Scott Throner
IPC分类号： A61K31/5377 , C07D239/22 , A61K31/513 , C12N9/99 , A61P25/28 , C07D413/10
CPC分类号： C07D239/47 , C07D401/10 , C07D403/06 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/10
摘要： This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia, Ib), and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aβ related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译： 本发明涉及具有结构式Ia或式Ib的新化合物：（Ia，Ib）及其药学上可接受的盐，互变异构体或体内可水解的前体，组合物及其使用方法。 这些新型化合物提供治疗或预防Abeta相关病理学，如认知障碍，阿尔茨海默病，神经变性和痴呆。
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