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1. 发明授权

US07973164B2 Quinoline derivatives 失效
标题翻译：喹啉衍生物
公开(公告)号：US07973164B2
公开(公告)日：2011-07-05
申请号：US12280848
申请日：2007-03-01
申请人： Frederic Henri Jung , Patrick Ple
发明人： Frederic Henri Jung , Patrick Ple
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C07D215/233
摘要： The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译：本发明涉及式I的喹啉衍生物或其药学上可接受的盐，其中X 1，p，R 1，q，R 2，R 3，R 4，R 5，环A，r和R 6中的每一个在描述; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。

2. 发明申请

US20090036474A1 Quinazoline derivatives for use against cancer 审中-公开
标题翻译：用于抗癌的喹唑啉衍生物
公开(公告)号：US20090036474A1
公开(公告)日：2009-02-05
申请号：US11665115
申请日：2005-10-07
申请人： Patrick Ple , Frederic Henri Jung
发明人： Patrick Ple , Frederic Henri Jung
IPC分类号： A61K31/517 , C07D403/12 , A61P9/00
CPC分类号： C07D417/14 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of p, R1, q, R2, R3, R4, R5, Ring A, X1, R6, r and R7 has any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物或其药学上可接受的盐，溶剂化物或前体药物，其中p，R1，q，R2，R3，R4，R5，环A，X1，R6，r和 R7具有描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病或治疗与血管生成和/或血管通透性相关的疾病状态的药物中的用途。

3. 发明授权

US08153643B2 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：US08153643B2
公开(公告)日：2012-04-10
申请号：US11665125
申请日：2005-10-07
申请人： Patrick Ple , Frederic Henri Jung
发明人： Patrick Ple , Frederic Henri Jung
IPC分类号： A61K31/517 , C07D403/02 , C07D403/10
CPC分类号： C07D471/04 , C07D239/88 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物或其药学上可接受的盐，溶剂合物或前体药物，其中X1，p，R1，q，R2，R3，R4，R5，环A，r和R6各自具有在说明书中以前定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病或治疗与血管生成和/或血管通透性相关的疾病状态的药物中的用途。

4. 发明申请

US20090233924A1 Quinazoline derivatives 有权
标题翻译：喹唑啉衍生物
公开(公告)号：US20090233924A1
公开(公告)日：2009-09-17
申请号：US11665125
申请日：2005-10-07
申请人： Patrick Ple , Frederic Henri Jung
发明人： Patrick Ple , Frederic Henri Jung
IPC分类号： A61K31/5377 , C07D239/72 , A61K31/517 , C07D401/12 , C07D413/00
CPC分类号： C07D471/04 , C07D239/88 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物或其药学上可接受的盐，溶剂化物或前体药物，其中X1，p，R1，q，R2，R3，R4，R5，环A，r和R6各自具有在说明书中以前定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病或治疗与血管生成和/或血管通透性相关的疾病状态的药物中的用途。

5. 发明申请

US20120165351A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：US20120165351A1
公开(公告)日：2012-06-28
申请号：US13410448
申请日：2012-03-02
申请人： Patrick Ple , Frederic Henri Jung
发明人： Patrick Ple , Frederic Henri Jung
IPC分类号： A61K31/517 , A61P35/00 , A61P9/00 , C07D417/12
CPC分类号： C07D239/88 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The invention concerns quinazoline derivatives of Formula I or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders or in the treatment of disease states associated with angiogenesis and/or vascular permeability.
摘要翻译：本发明涉及式I的喹唑啉衍生物或其药学上可接受的盐，溶剂化物或前体药物，其中X1，p，R1，q，R2，R3，R4，R5，环A，r和R6各自为在描述中定义的含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病或治疗与血管生成和/或血管通透性相关的疾病状态的药物中的用途。

6. 发明申请

US20090233950A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：US20090233950A1
公开(公告)日：2009-09-17
申请号：US12280857
申请日：2007-03-01
申请人： Frederic Henri Jung , Patrick Ple
发明人： Frederic Henri Jung , Patrick Ple
IPC分类号： A61K31/517 , C07D401/00
CPC分类号： C07D401/12
摘要： The invention concerns quinazoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译：本发明涉及式I的喹唑啉衍生物或其药学上可接受的盐，其中X 1，p，R 1，q，R 2，R 3，R 4，R 5，环A，r和R 6中的每一个在描述; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。

7. 发明申请

US20090076075A1 QUINOLINE DERIVATIVES 审中-公开
标题翻译：喹啉衍生物
公开(公告)号：US20090076075A1
公开(公告)日：2009-03-19
申请号：US12280852
申请日：2007-03-01
申请人： Frederic Henri Jung , Remy Robert Morgentin , Patrick Ple
发明人： Frederic Henri Jung , Remy Robert Morgentin , Patrick Ple
IPC分类号： A61K31/4709 , C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D411/14 , C07D413/14
摘要： The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译：本发明涉及式I的喹啉衍生物或其药学上可接受的盐，其中X 1，p，R 1，q，R 2，R 3，R 4，R 5，R A，R和R 6各自具有上文在描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。

8. 发明申请

US20090076074A1 QUINOLINE DERIVATIVES 失效
标题翻译：喹啉衍生物
公开(公告)号：US20090076074A1
公开(公告)日：2009-03-19
申请号：US12280848
申请日：2007-03-01
申请人： Frederic Henri Jung , Patrick Ple
发明人： Frederic Henri Jung , Patrick Ple
IPC分类号： A61K31/4709 , C07D401/12
CPC分类号： C07D401/12 , C07D215/233
摘要： The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译：本发明涉及式I的喹啉衍生物或其药学上可接受的盐，其中X 1，p，R 1，q，R 2，R 3，R 4，R 5，环A，r和R 6中的每一个在描述; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。

9. 发明申请

US20090042910A1 QUINOLINE DERIVATIVES FOR TREATING CANCER 审中-公开
标题翻译：用于治疗癌症的喹诺酮衍生物
公开(公告)号：US20090042910A1
公开(公告)日：2009-02-12
申请号：US12280854
申请日：2007-03-01
申请人： Frederic Henri Jung , Patrick Ple
发明人： Frederic Henri Jung , Patrick Ple
IPC分类号： A61K31/506 , C07D401/12
CPC分类号： C07D401/14
摘要： The invention concerns quinoline derivatives of Formula I or a pharmaceutically-acceptable salt thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
摘要翻译：本发明涉及式I的喹啉衍生物或其药学上可接受的盐，其中X 1，p，R 1，q，R 2，R 3，R 4，R 5，环A，r和R 6中的每一个在描述; 其制备方法，含有它们的药物组合物及其在制备用于治疗细胞增殖性疾病的药物中的用途。

10. 发明授权

US06977259B2 Quinoline derivatives and their use as aurora 2 kinase inhibitors 失效
标题翻译：喹啉衍生物及其作为极光2激酶抑制剂的用途
公开(公告)号：US06977259B2
公开(公告)日：2005-12-20
申请号：US10182454
申请日：2001-01-24
申请人： Andrew Austen Mortlock , Frederic Henri Jung
发明人： Andrew Austen Mortlock , Frederic Henri Jung
IPC分类号： A61K31/4709 , A61K31/506 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D521/00 , A61K31/4965 , A01N43/54 , A61K31/505 , C07D239/02 , C07D401/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12
摘要： A compound of formula (I) or a salt, ester, amide or prodrug thereof; R5 is an optionally substituted 6-membered aromatic ring containing at least one nitrogen atom, and R1, R2, R3, R4 are independently selected from halogeno, cyano, nitro, C1-3alkylsulphonyl, —N(OH)R7— (wherein R7 is hydrogen, or C1-3 alkyl), or R9X1— (wherein X1 represents a direct bond, —O—, —CH2—, —OC(O)—, —C(O)—, —S—, —SO—, —SO2—, —NR10C(O)—, —C(O)NR11—, —SO2NR12—, —NR13SO2— or —NR14— (wherein R10, R11, R12, R13 and R14 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl), and R9 is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy); provided that at least one of R2 or R3 is other than hydrogen. These compounds are inhibitors of aurora 2 kinase. Thus they, and pharmaceutical compositions containing them, are useful in methods of treatment of proliferative disease such as cancer and in particular cancers such as colorectal or breast cancer where aurora 2 is upregulated.
摘要翻译：式（I）化合物或其盐，酯，酰胺或前药; R 5是含有至少一个氮原子的任选取代的6元芳香环，R 1，R 2，R 2， 3，R 4独立地选自卤素，氰基，硝基，C 1-3烷基磺酰基，-N（OH）R 7，（其中R 7为氢或C 1-3烷基）或R 9 X 1 O / - （其中X 1表示直接键，-O-，-CH 2 - ， - OC（O） - ， - C（O） - ， - S - ， - SO - ， - SO 2 - ， - NRO 10 C（O） - ， - C（O）NR 11 - -SO 2 - ， - NR 12 - ， - SO 2 - ， - NR 14 - （其中R 10，R 11，R 12，R 13和R 14）各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3烷基）任选取代的烃基，任选取代的杂环基或任选取代的烷氧基）; 条件是R 2或R 3 3中的至少一个不是氢。这些化合物是极光2激酶的抑制剂。因此，它们和含有它们的药物组合物可用于治疗增殖性疾病如癌症的方法，特别是诸如结直肠癌或乳腺癌的癌症，其中极光2被上调。

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