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公开(公告)号：US07547722B2
公开(公告)日：2009-06-16
申请号：US11752007
申请日：2007-05-22
申请人： Kevin Michael Foote , Zbigniew Stanley Matusiak , Alexander Graham Dossetter , Jean Claude Arnould , Maryannick Andree Lamorlette , Benedicte Delouvrie , Annie Hamon
发明人： Kevin Michael Foote , Zbigniew Stanley Matusiak , Alexander Graham Dossetter , Jean Claude Arnould , Maryannick Andree Lamorlette , Benedicte Delouvrie , Annie Hamon
IPC分类号： A61K31/40 , A61K31/407 , A61K31/381 , C07D401/00 , C07D495/02 , C07D207/06
CPC分类号： C07D495/04
摘要： The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
摘要翻译： 本发明涉及一组式（I）的新型噻吩并吡咯化合物：其中：R1，R2，R3，R4和R5如说明书中所定义，可用作促性腺激素释放激素拮抗剂。 本发明还涉及所述化合物的药物制剂，使用所述化合物的治疗方法和所述化合物的制备方法。
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![6H-THIENO [2,3-b]pyrrole derivatives as antagonists of gonadotropin releasing hormone (GnRH)](/abs-image/US/2007/09/11/US07268158B2/abs.jpg.150x150.jpg)
2.发明授权6H-THIENO [2,3-b]pyrrole derivatives as antagonists of gonadotropin releasing hormone (GnRH) 失效6H-THIENO [2,3-b]吡咯衍生物作为促性腺激素释放激素（GnRH）的拮抗剂公开(公告)号：US07268158B2
公开(公告)日：2007-09-11
申请号：US11380961
申请日：2006-05-01
申请人： Kevin Michael Foote , Zbigniew Matusiak , Alexander Graham Dossetter , Jean Claude Arnould , Maryannick Andree Lamorlette , Benedicte Delouvrie , Annie Hamon
发明人： Kevin Michael Foote , Zbigniew Matusiak , Alexander Graham Dossetter , Jean Claude Arnould , Maryannick Andree Lamorlette , Benedicte Delouvrie , Annie Hamon
IPC分类号： A61K31/40 , A61K31/407 , A61K31/181 , C07D401/00 , C07D495/02 , C07D207/06
CPC分类号： C07D495/04
摘要： The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
摘要翻译： 本发明涉及一组式（I）的新型噻吩并吡咯化合物：其中：R 1，R 2，R 3， R 4和R 5如说明书中所定义，其可用作促性腺激素释放激素拮抗剂。 本发明还涉及所述化合物的药物制剂，使用所述化合物的治疗方法和所述化合物的制备方法。
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![6H-thieno[2, 3-b]pyrrole derivatives as antagonists of gonadotropin releasing hormone (GnRH)](/abs-image/US/2006/11/07/US07132442B2/abs.jpg.150x150.jpg)
3.发明授权6H-thieno[2, 3-b]pyrrole derivatives as antagonists of gonadotropin releasing hormone (GnRH) 有权6H-噻吩并[2,3-b]吡咯衍生物作为促性腺激素释放激素（GnRH）的拮抗剂公开(公告)号：US07132442B2
公开(公告)日：2006-11-07
申请号：US10524978
申请日：2003-08-19
申请人： Kevin Michael Foote , Zbigniew Matusiak , Alexander Graham Dossetter , Jean Claude Arnould , Maryannick Andree Lamorlette , Benedicte Delouvrie , Annie Hamon
发明人： Kevin Michael Foote , Zbigniew Matusiak , Alexander Graham Dossetter , Jean Claude Arnould , Maryannick Andree Lamorlette , Benedicte Delouvrie , Annie Hamon
IPC分类号： A61K31/40 , A61K31/407 , A61K31/381 , C07D401/00 , C07D495/02 , C07D207/06
CPC分类号： C07D495/04
摘要： The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R3, R4 and R5 are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
摘要翻译： 本发明涉及一组式（I）的新型噻吩并吡咯化合物：其中：R 1，R 2，R 3， R 4和R 5如说明书中所定义，其可用作促性腺激素释放激素拮抗剂。 本发明还涉及所述化合物的药物制剂，使用所述化合物的治疗方法和所述化合物的制备方法。
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公开(公告)号：US08569298B2
公开(公告)日：2013-10-29
申请号：US12999025
申请日：2009-06-15
IPC分类号： C07D217/24 , C07D401/12 , A61K31/4709
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.
摘要翻译： 本发明涉及抑制粘着斑激酶功能的化合物，其制备方法，含有它们作为活性成分的药物组合物，作为药物的用途，以及它们在制备用于温热治疗的药物中的用途， 血液动物如人类的疾病如癌症。
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![N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-(3,4-dimethylpiperazin-1-yl)benzamide and salts thereof](/abs-image/US/2013/12/10/US08604022B2/abs.jpg.150x150.jpg)
5.发明授权N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-1h-pyrazol-3-yl]-4-(3,4-dimethylpiperazin-1-yl)benzamide and salts thereof 有权N- [5- [2-（3,5-二甲氧基苯基）乙基] -1H-吡唑-3-基] -4-（3,4-二甲基哌嗪-1-基）苯甲酰胺及其盐公开(公告)号：US08604022B2
公开(公告)日：2013-12-10
申请号：US13359008
申请日：2012-01-26
IPC分类号： A61K31/415 , A61K31/496 , A61K31/5377 , A61K31/454 , A61K31/4439 , A61K31/551 , C07D231/40 , C07D413/12 , C07D401/12 , C07D401/14 , C07D413/14 , C07D403/12
CPC分类号： C07D231/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , C07D487/04
摘要： There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
摘要翻译： 提供式（I）化合物或其药学上可接受的盐。 还提供了制备式1化合物的方法和式1化合物作为药物和用于治疗癌症的用途。
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公开(公告)号：US20110306613A1
公开(公告)日：2011-12-15
申请号：US13156684
申请日：2011-06-09
IPC分类号： A61K31/5377 , A61P35/00 , C07D413/14
CPC分类号： A61K31/5377 , A61K31/505 , C07D413/14 , C07D471/04
摘要： There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
摘要翻译： 提供式（I）的嘧啶基化合物，其中：R2是或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。
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公开(公告)号：US07504408B2
公开(公告)日：2009-03-17
申请号：US10520266
申请日：2003-07-04
IPC分类号： A61K31/517 , C07D239/88 , C07D239/94 , C07D239/93
CPC分类号： C07D405/12 , C07D405/14
摘要： The invention concerns quinazoline derivatives of Formula (I) wherein each of Z, m, R1, n, R3, Z2 and R14 have 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 as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease.
摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中Z，m，R 1，n，R 3，Z 2和R 14中的每一个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在实体瘤疾病的遏制和/或治疗中作为抗侵袭性或抗增殖剂的药物的用途。
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公开(公告)号：US20080004302A1
公开(公告)日：2008-01-03
申请号：US11769417
申请日：2007-06-27
申请人： Maria-Elena Theoclitou , David Buttar , Kevin Michael Foote , Thorsten Nowak , David Alan Rudge , Andrew Peter Thomas
发明人： Maria-Elena Theoclitou , David Buttar , Kevin Michael Foote , Thorsten Nowak , David Alan Rudge , Andrew Peter Thomas
IPC分类号： A61K31/506 , C07D413/14
CPC分类号： C07D413/14
摘要： There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
摘要翻译： 提供式（I）的化合物：其制备方法，其药物组合物和治疗用途。
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公开(公告)号：US07067532B2
公开(公告)日：2006-06-27
申请号：US10415812
申请日：2001-10-26
IPC分类号： A61K31/47 , C07D215/38 , C07D413/00 , C07D417/00 , C07D205/08 , C07D401/00 , C07D279/10
CPC分类号： C07D215/56 , C07D215/54 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention provides a compound of Formula (Ia), or a pharmaceutically acceptable salt pro-drug or solvate thereof. The invention also provides a process for the preparation of a compound of Formula (Ia), pharmaceutical compositions of a compound of Formula (Ia) and methods for the treatment or prevention of cancer comprising administering an effective amount of a compound of Formula (Ia).
摘要翻译： 本发明提供式（Ia）化合物或其药学上可接受的盐前体药物或其溶剂合物。 本发明还提供了制备式（Ia）化合物，式（Ia）化合物的药物组合物和治疗或预防癌症的方法的方法，包括给予有效量的式（Ia）化合物， 。
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公开(公告)号：US08552004B2
公开(公告)日：2013-10-08
申请号：US13540057
申请日：2012-07-02
IPC分类号： A61K31/506 , C07D403/14
CPC分类号： A61K31/5377 , A61K31/505 , C07D413/14 , C07D471/04
摘要： There is provided pyrimidinyl compounds of Formula (I), wherein: R2 is or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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