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1. 发明授权

US07576082B2 Oxindole derivatives 失效
标题翻译：羟吲哚衍生物
公开(公告)号：US07576082B2
公开(公告)日：2009-08-18
申请号：US11471363
申请日：2006-06-20
申请人： Kin-Chun Luk , Sung-Sau So , Jing Zhang , Zhuming Zhang
发明人： Kin-Chun Luk , Sung-Sau So , Jing Zhang , Zhuming Zhang
IPC分类号： A61K31/535 , A61K31/445 , A61K31/415 , A61K31/40 , C07D413/00 , C07D401/00 , C07D403/02 , C07D487/00 , C07D209/04
CPC分类号： C07D401/14 , C07D209/34 , C07D401/04 , C07D403/04
摘要： The invention describes compounds of the general formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are herein described, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as antiproliferative agents and may be especially useful for the treatment of cancer.
摘要翻译：本发明描述了通式I的化合物或其药学上可接受的盐，其中本文描述了R1，R2，R3和X，其制备方法，含有它们的药物以及这些化合物作为药物活性剂的用途。该化合物显示作为抗增殖剂的活性，并且可能特别可用于治疗癌症。

2. 发明申请

US20070060607A1 4-amino-thieno[3,2-c] pyridine-7-carboxylic acid derivatives 审中-公开
标题翻译： 4-氨基 - 噻吩并[3,2-c]吡啶-7-羧酸衍生物
公开(公告)号：US20070060607A1
公开(公告)日：2007-03-15
申请号：US11516905
申请日：2006-09-07
申请人： David Bartkovitz , Yi Chen , Xin-Jie Chu , Kin-Chun Luk , Pamela Rossman , Sung-Sau So
发明人： David Bartkovitz , Yi Chen , Xin-Jie Chu , Kin-Chun Luk , Pamela Rossman , Sung-Sau So
IPC分类号： A61K31/4743 , C07D498/02
CPC分类号： C07D495/04 , Y02P20/582
摘要： The present invention relates to compounds of the formula medicaments containing them and the use of these compounds as pharmaceutically active agents. The compounds exhibit activity as Raf kinase inhibitors and therefore may be useful for the treatment of diseases mediated by said kinases, especially as anticancer agents.
摘要翻译：本发明涉及含有它们的式药物的化合物以及这些化合物作为药物活性剂的用途。该化合物表现出作为Raf激酶抑制剂的活性，因此可用于治疗由所述激酶介导的疾病，特别是作为抗癌剂。

3. 发明授权

US07129351B2 Pyrimido compounds having antiproliferative activity 失效
标题翻译：具有抗增殖活性的嘧啶化合物
公开(公告)号：US07129351B2
公开(公告)日：2006-10-31
申请号：US10689438
申请日：2003-10-20
申请人： Kin-Chun Luk , Pamela Loreen Rossman , Stefan Scheiblich , Sung-Sau So
发明人： Kin-Chun Luk , Pamela Loreen Rossman , Stefan Scheiblich , Sung-Sau So
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
CPC分类号： C07D487/04 , G01N2800/52
摘要： Disclosed are novel pyrimido compounds that are inhibitors of Src family of tyrosine kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, hepatic and pancreatic tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.
摘要翻译：公开了作为酪氨酸激酶的Src家族抑制剂的新型嘧啶化合物。这些化合物及其药学上可接受的盐是可用于治疗或控制实体瘤，特别是乳腺癌，结肠癌，肝癌和胰腺肿瘤的抗增殖剂。还公开了含有这些化合物的药物组合物和治疗癌症的方法。

4. 发明授权

US07932390B2 Substituted thieno[3,2-C]pyridine carboxylic acid derivatives 有权
标题翻译：取代的噻吩并[3,2-C]吡啶羧酸衍生物
公开(公告)号：US07932390B2
公开(公告)日：2011-04-26
申请号：US11820306
申请日：2007-06-18
申请人： Yi Chen , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
发明人： Yi Chen , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
IPC分类号： A61K31/4365 , C07D515/04
CPC分类号： C07D495/04
摘要： There are provided compounds of the formula wherein R1, R2, R3, X, ring A and ring B are as described. The compounds exhibit anticancer properties.
摘要翻译：提供下式的化合物，其中R 1，R 2，R 3，X，环A和环B如上所述。该化合物具有抗癌性质。

5. 发明授权

US07112676B2 Pyrimido compounds having antiproliferative activity 失效
标题翻译：具有抗增殖活性的嘧啶化合物
公开(公告)号：US07112676B2
公开(公告)日：2006-09-26
申请号：US10689235
申请日：2003-10-20
申请人： Apostolos Dermatakis , Marek Michal Kabat , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
发明人： Apostolos Dermatakis , Marek Michal Kabat , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , G01N2800/52
摘要： Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.
摘要翻译：公开了作为KDR和FGFR激酶的选择性抑制剂的新的嘧啶化合物，并且对LCK具有选择性。这些化合物及其药学上可接受的盐是可用于治疗或控制实体瘤，特别是乳腺癌，结肠癌，肺癌和前列腺肿瘤的抗增殖剂。还公开了含有这些化合物的药物组合物和治疗癌症的方法。

6. 发明申请

US20080009515A1 Substituted thieno[3,2-C]pyridine carboxylic acid derivatives 有权
标题翻译：取代的噻吩并[3,2-C]吡啶羧酸衍生物
公开(公告)号：US20080009515A1
公开(公告)日：2008-01-10
申请号：US11820306
申请日：2007-06-18
申请人： Yi Chen , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
发明人： Yi Chen , Kin-Chun Luk , Pamela Loreen Rossman , Sung-Sau So
IPC分类号： A61K31/4365 , C07D471/04
CPC分类号： C07D495/04
摘要： There are provided compounds of the formula wherein R1, R2, R3, X, ring A and ring B are as described. The compounds exhibit anticancer properties.
摘要翻译：提供下式的化合物其中R 1，R 2，R 3，X，环A和环B如上所述。该化合物具有抗癌性质。

7. 发明申请

US20050075272A1 Pyrimido compounds having antiproliferative activity 失效
标题翻译：具有抗增殖活性的嘧啶化合物
公开(公告)号：US20050075272A1
公开(公告)日：2005-04-07
申请号：US10689235
申请日：2003-10-20
申请人： Apostolos Dermatakis , Marek Kabat , Kin-Chun Luk , Pamela Rossman , Sung-Sau So
发明人： Apostolos Dermatakis , Marek Kabat , Kin-Chun Luk , Pamela Rossman , Sung-Sau So
IPC分类号： A61P35/00 , C07D487/04 , A61K31/00
CPC分类号： C07D487/04 , G01N2800/52
摘要： Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.
摘要翻译：公开了作为KDR和FGFR激酶的选择性抑制剂的新的嘧啶化合物，并且对LCK具有选择性。这些化合物及其药学上可接受的盐是可用于治疗或控制实体瘤，特别是乳腺癌，结肠癌，肺癌和前列腺肿瘤的抗增殖剂。还公开了含有这些化合物的药物组合物和治疗癌症的方法。

8. 发明授权

US07524840B2 7,8-disubstituted pyrazolobenzodiazepines 失效
标题翻译： 7,8-二取代吡唑并苯并二氮杂卓
公开(公告)号：US07524840B2
公开(公告)日：2009-04-28
申请号：US11244251
申请日：2005-10-05
申请人： Jin-Jun Liu , Kin-Chun Luk , Giacomo Pizzolato , Yi Ren , Kshitij Chhabilbhai Thakkar , Peter Michael Wovkulich , Zhuming Zhang
发明人： Jin-Jun Liu , Kin-Chun Luk , Giacomo Pizzolato , Yi Ren , Kshitij Chhabilbhai Thakkar , Peter Michael Wovkulich , Zhuming Zhang
IPC分类号： A61P35/00 , A61K31/55 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.
摘要翻译：本发明提供式I化合物，其中R1，R2，R3，R4和R5如本文所述。本发明还提供了用于制备这些化合物和含有它们的药物组合物的合成。本发明进一步提供了用于抑制激酶，特别是CDK2抑制血管发生，以及用于治疗癌症，特别是乳腺癌，结肠癌，前列腺癌和肺癌的方法。

9. 发明申请

US20110071147A1 4-AMINO-THIENO[3,2-C]PYRIDINE-7-CARBOXYLIC ACID AMIDES 审中-公开
标题翻译： 4-氨基 - 噻吩并[3,2-C]吡啶-7-羧酸酰胺
公开(公告)号：US20110071147A1
公开(公告)日：2011-03-24
申请号：US12952251
申请日：2010-11-23
申请人： Kin-Chun Luk , Lee Apostle McDermott , Pamela Loreen Rossman , Peter Michael Wovkulich , Zhuming Zhang
发明人： Kin-Chun Luk , Lee Apostle McDermott , Pamela Loreen Rossman , Peter Michael Wovkulich , Zhuming Zhang
IPC分类号： A61K31/5355 , C07D471/04 , C07D413/14 , A61K31/4375 , A61P35/00
CPC分类号： C07D495/04
摘要： Disclosed are novel 4-amino-thieno[3,2-c]pyridine-7-carboxylic acid amides, and their pharmaceutically acceptable salts and esters, that are selective inhibitors of KDR and/or FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular solid cancerous tumors of the breast, colon, lung and prostate. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer using these compounds.
摘要翻译：公开了新的4-氨基 - 噻吩并[3,2-c]吡啶-7-羧酸酰胺及其药学上可接受的盐和酯，其是KDR和/或FGFR激酶的选择性抑制剂。这些化合物及其药学上可接受的盐是可用于治疗或控制实体瘤，特别是乳腺，结肠，肺和前列腺的固体癌性肿瘤的抗增殖剂。还公开了含有这些化合物的药物组合物和使用这些化合物治疗癌症的方法。

10. 发明授权

US07217717B2 Phenalene derivatives 失效
标题翻译：萘衍生物
公开(公告)号：US07217717B2
公开(公告)日：2007-05-15
申请号：US10852735
申请日：2004-05-24
申请人： Kin-Chun Luk , Zhuming Zhang
发明人： Kin-Chun Luk , Zhuming Zhang
IPC分类号： A61K31/505 , A61K31/519 , C07D471/12 , C07D487/12
CPC分类号： C07D471/06 , C07D487/06
摘要： Novel 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives are disclosed. These compounds inhibit epidermal growth factor receptor (“EGFR”) tyrosine kinase. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also relates to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.
摘要翻译：公开了新的1,3,4-三氮杂 - 非那烯和1,3,4,6-四氮杂萘衍生物。这些化合物抑制表皮生长因子受体（“EGFR”）酪氨酸激酶。这些化合物及其药学上可接受的盐和酯具有抗增殖活性，尤其可用于治疗或控制癌症，特别是实体瘤。本发明还涉及含有这些化合物的药物组合物以及治疗或控制癌症的方法，特别是乳腺癌，肺癌，结肠癌和前列腺肿瘤的治疗或控制。

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