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公开(公告)号:US20070238875A1
公开(公告)日:2007-10-11
申请号:US11752582
申请日:2007-05-23
IPC分类号: C07D239/72
CPC分类号: A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups, with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
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公开(公告)号:US20070093512A1
公开(公告)日:2007-04-26
申请号:US11562047
申请日:2006-11-21
申请人: George COCKERILL , Karen Lackey
发明人: George COCKERILL , Karen Lackey
IPC分类号: A61K31/519 , C07D487/02
CPC分类号: C07D405/04 , C07D239/94 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/02
摘要: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.
摘要翻译: 描述了杂芳族化合物,其制备方法,含有它们的药物组合物,使用方法及其在药物中的用途。 特别地,本发明涉及蛋白酪氨酸激酶抑制的喹唑啉和吡啶并嘧啶衍生物。
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公开(公告)号:US20060189637A1
公开(公告)日:2006-08-24
申请号:US11400284
申请日:2006-04-07
申请人: George Cockerill , Karen Lackey
发明人: George Cockerill , Karen Lackey
IPC分类号: A61K31/519 , C07D487/02
CPC分类号: C07D405/04 , C07D239/94 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/02
摘要: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.
摘要翻译: 描述了杂芳族化合物,其制备方法,含有它们的药物组合物,使用方法及其在药物中的用途。 特别地,本发明涉及蛋白酪氨酸激酶抑制的喹唑啉和吡啶并嘧啶衍生物。
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公开(公告)号:US20070015775A1
公开(公告)日:2007-01-18
申请号:US11532926
申请日:2006-09-19
IPC分类号: A61K31/517 , C07D405/02
CPC分类号: A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups, with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
摘要翻译: 一种制备式(I)化合物的方法,包括步骤:(a)使其中L和L'是合适的离去基团的式(II)化合物与式(III)化合物反应, line-formula description =“In-line Formulas”end =“lead”?> UNH SUB>(III)<?in-line-formula description =“In-line Formulas”end =“tail” 制备式(IV)的化合物,随后(b)用R'取代基取代离去基团L'。
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公开(公告)号:US20050143401A1
公开(公告)日:2005-06-30
申请号:US11061578
申请日:2005-02-18
申请人: George Cockerill , Karen Lackey
发明人: George Cockerill , Karen Lackey
IPC分类号: A61K31/517 , A61K31/519 , A61P11/00 , A61P17/06 , A61P19/02 , A61P35/00 , A61P43/00 , B60J11/00 , B60R19/42 , C07D239/94 , C07D405/04 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D417/02 , C07D49/02
CPC分类号: C07D405/04 , C07D239/94 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/02
摘要: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.
摘要翻译: 描述了杂芳族化合物,其制备方法,含有它们的药物组合物,使用方法及其在药物中的用途。 特别地,本发明涉及蛋白酪氨酸激酶抑制的喹唑啉和吡啶并嘧啶衍生物。
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公开(公告)号:US20050130996A1
公开(公告)日:2005-06-16
申请号:US11050033
申请日:2005-02-03
IPC分类号: A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/10 , A61P17/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D221/00 , C07D239/00 , C07D239/94 , C07D405/04 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D45/02
CPC分类号: A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要: A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups, with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
摘要翻译: 一种制备式(I)化合物的方法,包括步骤:(a)使其中L和L'是合适的离去基团的式(II)化合物与式(III)化合物反应, line-formula description =“In-line Formulas”end =“lead”?> UNH SUB>(III)<?in-line-formula description =“In-line Formulas”end =“tail” 制备式(IV)的化合物,随后(b)用R'取代基取代离去基团L'。
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公开(公告)号:US20080004294A1
公开(公告)日:2008-01-03
申请号:US11832187
申请日:2007-08-01
申请人: George Cockerill , Karen Lackey
发明人: George Cockerill , Karen Lackey
IPC分类号: A61K31/517 , A61K31/519 , C07D239/72 , C07D471/04
CPC分类号: C07D405/04 , C07D239/94 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/02
摘要: Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein tyrosine kinase inhibition.
摘要翻译: 描述了杂芳族化合物,其制备方法,含有它们的药物组合物,使用方法及其在药物中的用途。 特别地,本发明涉及蛋白酪氨酸激酶抑制的喹唑啉和吡啶并嘧啶衍生物。
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公开(公告)号:US20050267133A1
公开(公告)日:2005-12-01
申请号:US10521910
申请日:2003-07-21
申请人: Matthew Brown , Mui Cheung , Scott Dickerson , David Drewry , Karen Lackey , Andrew Peat , Stephen Thomson , James Veal , Jayme Wilson
发明人: Matthew Brown , Mui Cheung , Scott Dickerson , David Drewry , Karen Lackey , Andrew Peat , Stephen Thomson , James Veal , Jayme Wilson
IPC分类号: A61K31/519 , A61P3/06 , A61P5/48 , A61P9/10 , A61P9/12 , A61P15/08 , A61P17/14 , A61P25/28 , A61P35/00 , A61P37/04 , A61P43/00 , C07D487/02 , C07D487/04
CPC分类号: C07D487/04 , A61K31/519
摘要: The present invention relates generally to inhibitors of the kinases and more particularly to novel pyrazolopyrimidine compounds
摘要翻译: 本发明一般涉及激酶的抑制剂,更具体地涉及新的吡唑并嘧啶化合物
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公开(公告)号:US5342947A
公开(公告)日:1994-08-30
申请号:US960498
申请日:1992-10-09
申请人: Karen Lackey , Daniel D. Sternbach
发明人: Karen Lackey , Daniel D. Sternbach
IPC分类号: C07D491/22 , C07D491/147
CPC分类号: C07D491/22
摘要: The present invention relates to the synthesis of water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: n represents the integer 1 or 2;R.sup.1 represents independently, hydrogen, lower alkyl, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl; andR.sup.2 represents hydrogen andthe pharmaceutically acceptable salts thereof.
摘要翻译: 本发明涉及式(I)的水溶性喜树碱衍生物的合成,其中:n表示整数1或2; R 1独立地表示氢,低级烷基,(C 3-7)环烷基,(C 3-7)环烷基低级烷基,低级烯基,羟基低级烷基,低级烷氧基低级烷基; 和R2代表氢及其药学上可接受的盐。
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公开(公告)号:US20060128745A1
公开(公告)日:2006-06-15
申请号:US11336010
申请日:2006-01-20
申请人: Karen Lackey , Edgar Wood
发明人: Karen Lackey , Edgar Wood
IPC分类号: A61K31/4745 , C07D471/02
CPC分类号: C07D471/04
摘要: The present invention is related to aza-oxindole derivatives, compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis. In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.
摘要翻译: 本发明涉及氮杂 - 羟基吲哚衍生物,含有它们的组合物及其使用和制造方法。 这些化合物通常在药理学上作为通常通过改变促分裂原活化的信号通路而减轻的疾病状态中的药物有用,特别是在病理学上涉及异常细胞增殖的蛋白激酶的抑制或拮抗作用中。 这种疾病状态包括肿瘤生长,再狭窄,动脉粥样硬化,疼痛和血栓形成。 特别地,本发明涉及一系列取代的羟吲哚化合物,其表现出Trk家族蛋白酪氨酸激酶抑制,并且其可用于癌症治疗和慢性疼痛适应症。
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