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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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公开(公告)号:US20110166139A1
公开(公告)日:2011-07-07
申请号:US12999025
申请日:2009-06-15
IPC分类号: A61K31/5377 , C07D401/12 , C07D217/24 , C07D409/14 , C07D401/14 , C07D413/14 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/4545 , A61P35/00 , A61P35/02
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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公开(公告)号:US20100022476A1
公开(公告)日:2010-01-28
申请号:US11722439
申请日:2005-12-16
申请人: Kevin Michael Foote
发明人: Kevin Michael Foote
IPC分类号: A61K31/675 , A61P35/00 , C07D401/12 , A61K31/517 , A61K31/496
CPC分类号: C07F9/65583 , C07D403/12 , C07D403/14
摘要: The invention provided a compound of formula: (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient.
摘要翻译: 本发明提供了一种式(I)化合物,其用于治疗疾病,特别是增殖性疾病如癌症和用于制备用于治疗增殖性疾病的药物; 本发明还用于制备这些化合物以及含有它们作为活性成分的药物组合物。
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公开(公告)号:US20090118336A1
公开(公告)日:2009-05-07
申请号:US12299369
申请日:2007-05-02
申请人: Laurent David , Kevin Michael Foote , Annea Lisius
发明人: Laurent David , Kevin Michael Foote , Annea Lisius
IPC分类号: A61K31/4439 , C07D401/14 , C07D417/14 , C07D401/04
CPC分类号: C07D401/04 , C07D417/14
摘要: The invention concerns pyrazole derivatives of Formula I or pharmaceutically-acceptable salts thereof, wherein each of R, Ring A, m, R1, R2 and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
摘要翻译: 本发明涉及式I的吡唑衍生物或其药学上可接受的盐,其中R,环A,m,R 1,R 2和R 3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治疗中的用途,例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。
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公开(公告)号:US20080214495A1
公开(公告)日:2008-09-04
申请号:US11994846
申请日:2006-07-05
申请人: Christer Alstermark , Kosrat Amin , Kjell Andersson , Yantao Chen , Ulf Fahlander , Kevin Michael Foote , Kenneth Granberg , Daniel Hovdal
发明人: Christer Alstermark , Kosrat Amin , Kjell Andersson , Yantao Chen , Ulf Fahlander , Kevin Michael Foote , Kenneth Granberg , Daniel Hovdal
IPC分类号: A61K31/501 , C07D401/14 , A61K31/497 , A61K31/496 , A61K31/397 , A61P9/00
CPC分类号: C07D409/14 , C07D401/04 , C07D401/14
摘要: The invention relates to compounds of formula (I), wherein R1 and R3 are independently selected from carbon and nitrogen; R2 is oxo or thioxo; n is 0, 1 or 2; each R10 is independently selected from hydrogen and C1-3alkyl; R4 and R5 are each selected from carbon and nitrogen, wherein at least one of R4 and R5 is nitrogen; R6 is hydrogen or oxo; R7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R11 is independently selected from hydrogen, hydroxy, oxo, C1-5alkyl, carboxy, hydroxyC1-5alkyl, carboxyC1-5alkyl, C1-5alkoxy-oxoC1-5alkyl, carbamoyl, C1-5alkylcarbamoyl, di (C1-5 alkyl)carbamoyl, carbamoylC1-4alkyl,C1-5alkylcarbamoylC1-4alkyl, di(C1-5alkyl)carbamoylC1-4alkyl, hydroxyC1-5alkylcarbamoyl, C1-5 alkoxyC1-5alkylcarbamoyl, hydroxyC1-5alkylcarbamoylC1-4alkyl, C1-5alkoxyC1-5 alkylcarbamoylC1-4 alkyl, CONR80(CH2)xS(O)pR90, CONH(CH2)qNR100R100, —C1-5 alkyl-Y1, —COOCHR170R180 and —CON R170R180; R8 is a bond, C1-4alkylene or C2-6alkenylene; R9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R9 is substituted by 0 or 1 halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.
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公开(公告)号:US07402583B2
公开(公告)日:2008-07-22
申请号:US11374423
申请日:2006-03-14
IPC分类号: A61K31/4965 , A61K31/47 , C07D401/00
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 thereof, a process for t he preparation of a compound of Formula (1a) and pharmaceutical compositions of a compound of Formula (1a).
摘要翻译: 本发明提供式(Ia)化合物或其药学上可接受的盐,制备式(1a)化合物的方法和式(1a)化合物的药物组合物。
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公开(公告)号:US20130005725A1
公开(公告)日:2013-01-03
申请号:US13540057
申请日:2012-07-02
IPC分类号: A61K31/5377 , A61P35/00 , C07D413/14 , C07D471/04
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:US08252802B2
公开(公告)日:2012-08-28
申请号:US13156684
申请日:2011-06-09
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.
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:US20110053923A1
公开(公告)日:2011-03-03
申请号:US12642952
申请日:2009-12-21
IPC分类号: A61K31/537 , C07D413/14 , A61K31/5377 , C07D498/08 , A61P35/00
CPC分类号: C07D403/04 , C07D401/14 , C07D405/14 , C07D498/08
摘要: There is provided pyrimidinyl indole compounds of Formula (I), 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)的嘧啶基吲哚化合物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: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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