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51. 发明申请

US20060074112A1 N-aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF receptor tyrosine kinase inhibitors 审中-公开
标题翻译： N-芳基（硫代）邻氨基苯甲酸酰胺衍生物，其制备及其作为VEGF受体酪氨酸激酶抑制剂的用途
公开(公告)号：US20060074112A1
公开(公告)日：2006-04-06
申请号：US11254897
申请日：2005-10-20
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul Manley , Jeanette Wood , Stefano Ferrari , Francesco Hofmann , Jurgen Mestan , Andreas Huth , Martin Kruger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul Manley , Jeanette Wood , Stefano Ferrari , Francesco Hofmann , Jurgen Mestan , Andreas Huth , Martin Kruger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： C07D213/56 , A61K31/44 , C07D233/54
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y═SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each, other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述的是式（I）的化合物，其中W是O或S; X是NR 8; Y是CR 9 R 10其中R 9是（CH 2）n - 和R 10彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO 2; R 1是芳基; R 2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二甲酰亚氨基，并且在Y-SO的情况下 2不能表示2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地是H或除氢以外的取代基; R 7和R 8分别独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

52. 发明授权

US5981533A Pyrazole derivatives and processes for the preparation thereof 失效
标题翻译：吡唑衍生物及其制备方法
公开(公告)号：US5981533A
公开(公告)日：1999-11-09
申请号：US930904
申请日：1997-10-03
申请人： Peter Traxler , Pascal Furet , Guido Bold , Jorg Frei , Marc Lang
发明人： Peter Traxler , Pascal Furet , Guido Bold , Jorg Frei , Marc Lang
IPC分类号： C07D231/38 , A61K31/505 , A61P35/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： 4-Amino-1H-pyrazolo[3,4-d]pyrimidine derivatives of formula I ##STR1## wherein the symbols are as defined in claim 1, and intermediates for their manufacture are described.The compounds of formula I inhibit especially the tyrosine kinase activity of the receptor for epidermal growth factor and can be used, for example, in the case of epidermal hyperproliferation (psoriasis) and as anti-tumor agents.
摘要翻译： PCT No.PCT / EP96 / 01263。 371日期1997年10月3日第 102（e）日期1997年10月3日PCT 1996年3月22日PCT公布。公开号WO96 / 31510PC。日期：19964年10月10日 - 描述了式I的氨基-1H-吡唑并[3,4-d]嘧啶衍生物，其中符号如权利要求1中所定义，其中描述其制备方法。式I的化合物特别地抑制表皮生长因子受体的酪氨酸激酶活性，并且可以用于例如表皮过度增生（牛皮癣）和作为抗肿瘤剂的情况。

53. 发明授权

US08053457B2 3-imidazolyl-indoles for the treatment of proliferative diseases 失效
标题翻译： 3-咪唑基 - 吲哚，用于治疗增殖性疾病
公开(公告)号：US08053457B2
公开(公告)日：2011-11-08
申请号：US12593721
申请日：2008-03-27
申请人： Andreas Boettcher , Nicole Buschmann , Pascal Furet , Jean-Marc Groell , Jorg Kallen , Joanna Hergovich Lisztwan , Keiichi Masuya , Lorenz Mayr , Andrea Vaupel
发明人： Andreas Boettcher , Nicole Buschmann , Pascal Furet , Jean-Marc Groell , Jorg Kallen , Joanna Hergovich Lisztwan , Keiichi Masuya , Lorenz Mayr , Andrea Vaupel
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/496 , A61K31/506 , C07D401/14 , C07D403/14
CPC分类号： C07D403/04
摘要： The invention relates to 3-heterocyclyl indolyl compounds of formula I capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively: wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.
摘要翻译：本发明涉及能够分别抑制p53或其变体和MDM2和/或MDM4或其变体之间的相互作用的式I的3-杂环基吲哚基化合物：其中R1，R2，R3，R4，RA，Y和 Y如说明书中所定义。由于它们的活性，所述化合物可用于治疗由MDM2和/或MDM4或其变体如炎性或增殖性疾病或保护细胞的活性介导的各种疾病和疾病。

54. 发明申请

US20090118277A1 3 Unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidines as Kinase Inhibitors 审中-公开
标题翻译： 3未取代的N-（芳基 - 或杂芳基） - 吡唑并[1,5-a]嘧啶作为激酶抑制剂
公开(公告)号：US20090118277A1
公开(公告)日：2009-05-07
申请号：US12296156
申请日：2007-04-02
申请人： Keiichi Masuya , Andrea Vaupel , Patricia Imbach , Pascal Furet
发明人： Keiichi Masuya , Andrea Vaupel , Patricia Imbach , Pascal Furet
IPC分类号： A61K31/519 , C07D487/04 , A61K31/5377 , A61P43/00 , C07D413/14
CPC分类号： C07D487/04
摘要： The invention relates to 3-unsubstituted N-(aryl- or heteroaryl)-pyrazolo[1,5-a]pyrimidine compounds, their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase, especially tie-2 kinase, activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.
摘要翻译：本发明涉及3-未取代的N-（芳基 - 或杂芳基） - 吡唑并[1,5-a]嘧啶化合物，它们作为激酶抑制剂的用途，包含所述化合物的新药物制剂，用于诊断或治疗性治疗的所述化合物温血动物，特别是人类，其用于治疗疾病或用于制备可用于治疗响应于激酶调节的疾病的药物制剂，特别是tie-2激酶，活性，治疗方法，包括施用所述化合物与温血动物，特别是人类，以及所述化合物的制备方法。

55. 发明授权

US07122547B1 Anthranilic acid amides and the use thereof as medicaments 失效
标题翻译：邻氨基苯甲酸酰胺及其作为药物的用途
公开(公告)号：US07122547B1
公开(公告)日：2006-10-17
申请号：US09831506
申请日：1999-11-09
申请人： Andreas Huth , Dieter Seidelmann , Karl-Heinz Thierauch , Guido Bold , Paul William Manley , Pascal Furet , Jeanette Marjorie Wood , Jürgen Mestan , Jose Brüggen , Stefano Ferrari , Martin Krüger , Eckhard Ottow , Andreas Menrad , Michael Schirner
发明人： Andreas Huth , Dieter Seidelmann , Karl-Heinz Thierauch , Guido Bold , Paul William Manley , Pascal Furet , Jeanette Marjorie Wood , Jürgen Mestan , Jose Brüggen , Stefano Ferrari , Martin Krüger , Eckhard Ottow , Andreas Menrad , Michael Schirner
IPC分类号： A61K31/505 , C07D239/26
CPC分类号： C07C237/32
摘要： The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
摘要翻译：本发明涉及邻氨基苯甲酸酰胺及其用作治疗由持续血管发生引起的疾病的药物，以及邻氨基苯甲酸酰胺生产中的中间产物。

56. 发明申请

US20060178409A1 Anthranilic acid amides and their use as VEGF receptor tyrosine kinase inhibitors 失效
标题翻译：邻氨基苯甲酸酰胺及其作为VEGF受体酪氨酸激酶抑制剂的用途
公开(公告)号：US20060178409A1
公开(公告)日：2006-08-10
申请号：US11374720
申请日：2006-03-14
申请人： Guido Bold , Pascal Furet , Paul Manley
发明人： Guido Bold , Pascal Furet , Paul Manley
IPC分类号： C07D213/63 , A61K31/4412
CPC分类号： C07D213/64 , C07D213/70
摘要： The invention relates to anthranilic acid amide derivatives of formula I, wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.
摘要翻译：本发明涉及式I的邻氨基苯甲酰胺衍生物，其中R 1代表H或低级烷基，R 2代表H或低级烷基，R 3，表示全氟低级烷基，X为O或S，或其N-氧化物或互变异构体，与该邻氨基苯甲酸酰胺，其N-氧化物及其互变异构体的盐形成的盐; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗肿瘤的药物制剂视网膜病变或年龄相关性黄斑变性疾病。

57. 发明授权

US07002022B2 N-Aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF 失效
标题翻译： N-芳基（硫代）邻氨基苯甲酸酰胺衍生物，其制备及其作为VEGF的用途
公开(公告)号：US07002022B2
公开(公告)日：2006-02-21
申请号：US10828951
申请日：2004-04-21
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： C07C49/76 , C07C49/786 , C07C49/82 , C07C49/825 , C07C49/884
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R2 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述的是式（I）的化合物，其中W是O或S; X是NR 8; Y为CR 9 R 10 - （CH 2）n其中R 9和R 10为氢， / SUB>彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO 2; R 2是芳基; R 2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二甲酰亚氨基，并且在Y = SO的情况下 2不能表示2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地是H或除氢以外的取代基; 和R 7和R 8彼此独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

58. 发明申请

US20050096356A1 Anthranilic acid amides and their use as vegf receptor tyrosine kinase inhibitors 失效
标题翻译：邻氨基苯甲酸酰胺及其作为vegf受体酪氨酸激酶抑制剂的用途
公开(公告)号：US20050096356A1
公开(公告)日：2005-05-05
申请号：US10494591
申请日：2002-11-07
申请人： Guido Bold , Pascal Furet , Paul Manley
发明人： Guido Bold , Pascal Furet , Paul Manley
IPC分类号： A61K31/44 , A61K31/4412 , A61P9/10 , A61P9/14 , A61P11/06 , A61P15/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07D213/64 , C07D213/70 , C07D213/62
CPC分类号： C07D213/64 , C07D213/70
摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age—related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.
摘要翻译：本发明涉及式（I）的邻氨基苯甲酰胺衍生物，其中R 1代表H或低级烷基，R 2代表H或低级烷基，R 3 表示全氟低级烷基，X是O或S，或其N-氧化物或互变异构体，与邻氨基苯甲酸酰胺的盐，它们的N-氧化物及其互变异构体; 其制备方法，其用于治疗人或动物体的应用，其单独使用或与一种或多种其它药学活性化合物组合用于特别是肿瘤性疾病如肿瘤疾病的治疗，视网膜病变或年龄相关性黄斑变性; 用于治疗动物，特别是人类中的这种疾病的方法，以及使用这样的化合物 - 单独或与一种或多种其它药学活性化合物组合 - 用于制备用于治疗肿瘤的药物制剂视网膜病变或年龄相关性黄斑变性疾病。

59. 发明授权

US08293746B2 Pyrimidinyl aryl urea derivatives being FGF inhibitors 有权
标题翻译：嘧啶基芳基脲衍生物是FGF抑制剂
公开(公告)号：US08293746B2
公开(公告)日：2012-10-23
申请号：US12158873
申请日：2006-12-20
申请人： Guido Bold , Pascal Furet , Vito Guagnano
发明人： Guido Bold , Pascal Furet , Vito Guagnano
IPC分类号： C07D403/12 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12
摘要： The invention relates to heteroaryl aryl ureas of the formula IA, wherein the radicals and symbols have the meanings as defined herein, the use of such compounds in the treatment of protein kinase dependent diseases; to pharmaceutical preparations comprising said heteroaryl aryl ureas, to processes for the manufacture of such novel compounds and to methods of treatment comprising the use of such heteroaryl aryl ureas.
摘要翻译：本发明涉及式IA的杂芳基芳基脲，其中基团和符号具有本文定义的含义，这些化合物在治疗蛋白激酶依赖性疾病中的用途; 涉及包含所述杂芳基芳基脲的药物制剂，以及制备这些新化合物的方法和包括使用这种杂芳基芳基脲的治疗方法。

60. 发明授权

US06448277B2 VEGF receptor tyrosine kinase inhibitors 失效
标题翻译： VEGF受体酪氨酸激酶抑制剂
公开(公告)号：US06448277B2
公开(公告)日：2002-09-10
申请号：US09850434
申请日：2001-05-07
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul William Manley , Jeanette Marjorie Wood , Stefano Ferrari , Francesco Hofmann , Jürgen Mestan , Andreas Huth , Martin Krüger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： A61K31166
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is S02; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述了式（I）的化合物，其中W是O或S; X为NR8; Y为CR 9 R 10 - （CH 2）n，其中R 9和R 10彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO2; R1是芳基; R2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二酰亚氨基，并且在Y = SO 2的情况下不能代表2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地为H或氢以外的取代基; 且R 7和R 8彼此独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

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