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1. 发明授权

US09890166B2 Imidazopyrrolidine derivatives and their use in the treatment of disease 有权
公开(公告)号：US09890166B2
公开(公告)日：2018-02-13
申请号：US14892616
申请日：2014-05-26
申请人： Jutta Blank , Guido Bold , Simona Cotesta , Vito Guagnano , Heinrich Rueeger , Andrea Vaupel
发明人： Jutta Blank , Guido Bold , Simona Cotesta , Vito Guagnano , Heinrich Rueeger , Andrea Vaupel
IPC分类号： C07D487/04 , C07D471/04 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/513 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/5025 , A61K31/513 , A61K31/5377 , C07D471/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

2. 发明授权

US08026247B2 Bicyclic amides as kinase inhibitors 有权
标题翻译：双环酰胺作为激酶抑制剂
公开(公告)号：US08026247B2
公开(公告)日：2011-09-27
申请号：US11575025
申请日：2005-09-14
申请人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W. Manley , Andrea Vaupel
发明人： Guido Bold , Hans-Georg Capraro , Giorgio Caravatti , Andreas Floersheimer , Pascal Furet , Paul W. Manley , Andrea Vaupel
IPC分类号： C07D239/46 , C07D403/12 , C07D413/12 , A61K31/505
CPC分类号： C07D239/47 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula I and to the use of a compound of formula I for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
摘要翻译：本发明涉及式（I）化合物及其在治疗动物或人体中的用途，包括式I化合物的药物组合物和式I化合物在制备药物组合物中的用途用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，特别是肿瘤疾病。

3. 发明申请

US20100029626A1 Cyclic sulfones useful as mitochondrial sodium-calcium exchangers 失效
标题翻译：可用作线粒体钠 - 钙交换剂的环状砜
公开(公告)号：US20100029626A1
公开(公告)日：2010-02-04
申请号：US12446955
申请日：2007-03-13
申请人： Guido Bold , Andrea Vaupel , Carole Pissot Soldermann , Paul W. Manley
发明人： Guido Bold , Andrea Vaupel , Carole Pissot Soldermann , Paul W. Manley
IPC分类号： A61K31/541 , C07D403/12 , A61K31/497 , C07D417/12 , C07D401/12 , A61K31/506
CPC分类号： C07D413/12 , C07D239/34 , C07D239/36 , C07D239/42 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/12 , C07D471/06
摘要： The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases.
摘要翻译：本发明涉及新的式（I）化合物及其在治疗动物或人体中的用途，包括式（I）化合物的药物组合物和式（I）化合物在制备中的用途用于治疗蛋白激酶依赖性疾病，特别是增殖性疾病，特别是肿瘤疾病的药物组合物。

4. 发明申请

US20080319005A1 Phenylacetamides Suitable as Protein Kinase Inhibitors 失效
标题翻译：苯乙酰胺适合作为蛋白激酶抑制剂
公开(公告)号：US20080319005A1
公开(公告)日：2008-12-25
申请号：US11914895
申请日：2006-04-12
申请人： Guido Bold , Pascal Furet , Vito Guagnano , Clive McCarthy , Andrea Vaupel
发明人： Guido Bold , Pascal Furet , Vito Guagnano , Clive McCarthy , Andrea Vaupel
IPC分类号： A61K31/437 , C07D235/06 , A61K31/4164 , C07D471/04
CPC分类号： C07D235/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D473/00
摘要： The invention relates to compounds of the formula (I) wherein the moieties R1, R2, R3, R9, R10 and Q and X, Y and Z are as defined in the specification, and salts thereof, as well as their use, methods of use for them and method of their synthesis, and the like. The compounds are protein kinase inhibitors and can, inter alia, be used in the treatment of various proliferative diseases.
摘要翻译：本发明涉及式（I）化合物，其中部分R 1，R 2，R 3，R 9，R 10和Q和X，Y和Z如说明书中所定义，及其盐，以及它们的用途，用于它们及其合成方法等。这些化合物是蛋白激酶抑制剂，尤其可用于治疗各种增殖性疾病。

5. 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。

6. 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。

7. 发明授权

US07067543B2 Anthranilic acid amides and pharmaceutical use thereof 失效
标题翻译：邻氨基苯甲酸酰胺及其药物用途
公开(公告)号：US07067543B2
公开(公告)日：2006-06-27
申请号：US10494222
申请日：2002-11-07
申请人： Guido Bold , Pascal Furet , Paul W Manley
发明人： Guido Bold , Pascal Furet , Paul W Manley
IPC分类号： C07D213/38 , A61K31/44
CPC分类号： C07C237/40 , C07D213/38 , C07D213/89
摘要： The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (Ia), wherein Ra represents H or lower alkyl, and R1 represents H or perfluoro lower alkyl, R2 represents H, halogen, C2–C7alkyl, C2–C7alkenyl or lower aklynyl; or Ar is represented by the subformula (Ib) and R1 represents perfluoro lower alkyl, and R2 represents bromo, iodo, C2–C7alkyl, C2–C7alkenyl or lower alkynyl, or R1 represents H, and R2 represents fluoro, bromo, iodo, ethyl, C5–C7alkyl, C2–C7alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to 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; to a method for the treatment of such diseases in animals; and to 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）的邻氨基苯甲酸酰胺衍生物，其中Ar由下式表示：其中R aa代表H或低级烷基，和 R 1表示H或全氟低级烷基，R 2表示H，卤素，C 2 -C 7烷基 C 2 -C 7链烯基或低级甲酰胺基; 或Ar由亚式（I B b）表示，R 1表示全氟低级烷基，R 2表示溴，碘，C 1 -C 6烷基，或者R 1，R 2，R 2，R 3，R 6，R 6， / SUB代表H，R 2代表氟，溴，碘，乙基，C 5 -C 7烷基，C 1 -C 6烷基，烯基或低级炔基; 其N-氧化物和互变异构体，以及这种邻氨基苯甲酰胺，其N-氧化物和互变异构体的盐; 进行准备; 其在治疗人或动物体中的应用，其单独使用或与一种或多种其它药学活性化合物的组合用于特别是治疗视网膜病变或年龄的肿瘤疾病如肿瘤疾病相关性黄斑变性; 涉及在动物中治疗这些疾病的方法; 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性疾病，视网膜病变或年龄相关性黄斑变性的药物制剂。

8. 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。

9. 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。

10. 发明授权

US06451973B1 Anilinopeptide derivatives 有权
标题翻译：氨基肽衍生物
公开(公告)号：US06451973B1
公开(公告)日：2002-09-17
申请号：US09214959
申请日：1999-02-01
申请人： Alexander Fässler , Guido Bold , Hans-Georg Capraro , Marc Lang
发明人： Alexander Fässler , Guido Bold , Hans-Georg Capraro , Marc Lang
IPC分类号： C07K508
CPC分类号： C07D295/135 , C07C271/22 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The invention relates to compounds of the formula I, in which R1 and R2 are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R3 and R4 are, independently of each other, sec-lower alkyl or tert-lower alkyl; R5 is phenyl or cyclohexyl; and R6 and R7 are, independently of each other, lower alkyl, or, together with the linking nitrogen atom, pyrrolidino, piperidino, 4-lower alkylpiperidino, 1,2,4-triazol-1-yl or 1,2,4-triazol-4-yl; or a salt thereof, provided that at least one salt-forming group is present. These compounds are inhibitors of HIV protease and are therefore suitable, for example, for treating AIDS or its preliminary stages.
摘要翻译：本发明涉及式I化合物，其中R 1和R 2彼此独立地为低级烷基或低级烷氧基 - 低级烷基; R 3和R 4彼此独立地为低级烷基或叔 - 低级烷基; R5是苯基或环己基; R 6和R 7彼此独立地为低级烷基，或与连接氮原子一起为吡咯烷子基，哌啶子基，4-低级烷基哌啶子基，1,2,4-三唑-1-基或1,2,4-三唑 -4-基或其盐，条件是至少存在一个成盐基团。这些化合物是HIV蛋白酶的抑制剂，因此适用于例如用于治疗AIDS或其初级阶段。

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