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公开(公告)号:US07297792B2
公开(公告)日:2007-11-20
申请号:US11422338
申请日:2006-06-06
申请人: Stephen Garland , David Haigh , Deidre Mary Bernadette Hickey , John Liddle , David Glynn Smith , Robert William Ward , Jason Witherington
发明人: Stephen Garland , David Haigh , Deidre Mary Bernadette Hickey , John Liddle , David Glynn Smith , Robert William Ward , Jason Witherington
IPC分类号: C07D413/00
CPC分类号: C07D471/04 , C07D213/85 , C07D487/04
摘要: The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclcyl and the alkyl moieties may each inedepently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention inlcudes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.
摘要翻译: 本发明包括式(I)化合物或其衍生物,其中Y为CH或N; R 1是未取代或取代的烷基,未取代或取代的环烷基,未取代或取代的烯基,未取代或取代的环烯基,未取代或取代的芳基,芳烷基,其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可以各自独立地是未取代的或取代的,未取代的或取代的杂环基或杂环基烷基,其中杂环基和烷基部分各自是未取代的或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明涉及制备这种化合物的方法,含有这种化合物的药物组合物,以及这种化合物在医药中的用途。
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公开(公告)号:US07109199B2
公开(公告)日:2006-09-19
申请号:US10381292
申请日:2001-09-19
申请人: Stephen Garland , David Haigh , Deidre Mary Bernadette Hickey , John Liddle , David Glynn Smith , Robert William Ward , Jason Witherington
发明人: Stephen Garland , David Haigh , Deidre Mary Bernadette Hickey , John Liddle , David Glynn Smith , Robert William Ward , Jason Witherington
IPC分类号: C07D487/04 , C07D471/04 , A61K31/4162 , A61P3/10
CPC分类号: C07D471/04 , C07D213/85 , C07D487/04
摘要: The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, aralkyl wherein the aryl and the alkyl moieties may each independently be unsubstituted or substituted, aralkenyl wherein the aryl, and alkenyl moieties may each independently be unsubstituted or substituted, unsubstituted or substituted heterocyclyl, or heterocyclylalkyl wherein the heterocyclyl and the alkyl moieties may each independently be unsubstituted or substituted; and R2 is unsubstituted aryl or unsubstituted or substituted or substituted heteroaryl. Additionally the present invention includes a process for preparing such a compound, a pharmaceutical composition containing such a compound, and the use of such a compound in medicine.
摘要翻译: 本发明包括式(I)化合物或其衍生物,其中Y为CH或N; R 1是未取代或取代的烷基,未取代或取代的环烷基,未取代或取代的烯基,未取代或取代的环烯基,未取代或取代的芳基,芳烷基,其中芳基和烷基部分各自独立地为未取代或取代的 芳基和烯基部分可各自独立地为未取代或取代的未取代或取代的杂环基或杂环基烷基,其中杂环基和烷基部分各自独立地为未取代或取代的; R 2是未取代的芳基或未取代或取代或取代的杂芳基。 另外本发明包括制备这种化合物的方法,含有这种化合物的药物组合物,以及这种化合物在医药中的用途。
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公开(公告)号:US06719520B2
公开(公告)日:2004-04-13
申请号:US10446553
申请日:2003-05-28
申请人: Matthew Paul Coghlan , Ashley Edward Fenwick , David Haigh , Julie Caroline Holder , Robert John Ife , Alastair David Reith , David Glynn Smith , Robert William Ward
发明人: Matthew Paul Coghlan , Ashley Edward Fenwick , David Haigh , Julie Caroline Holder , Robert John Ife , Alastair David Reith , David Glynn Smith , Robert William Ward
IPC分类号: A61K3140
CPC分类号: C07D207/456 , C07D401/04 , C07D403/04
摘要: A method for the treatment of conditions associated with a need for inhibition of GSK-3, such as diabetes, dementias such as Alzheimer's disease and manic depression which method comprises the administration of a pharmaceutically effective, non-toxic amount of a compound of formula (I): or a pharmaceutically acceptable derivative thereof, wherein: R is hydrogen, alkyl, aryl, or aralkyl; R1 is hydrogen, alkyl, aralkyl, hydroxyalkyl or alkoxyalkyl; R2 is substituted or unsubstituted aryl or substituted or unsubstituted heterocyclyl; R3 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, alkoxyalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl or aralkyl wherein the aryl moiety is substituted or unsubstituted; or, R1 and R3 together with the nitrogen to which they are attached form a single or fused, optionally substituted, saturated or unsaturated heterocylic ring; to a human or non-human mammal in need thereof, and compounds of formula I.
摘要翻译: 用于治疗与需要抑制GSK-3(例如糖尿病,痴呆症如阿尔茨海默病和躁狂抑郁症)有关的病症的方法包括施用药学上有效的无毒量的式(I)化合物 I):或其药学上可接受的衍生物,其中:R是氢,烷基,芳基或芳烷基; R 1是氢,烷基,芳烷基,羟基烷基或烷氧基烷基; R 2是取代或未取代的芳基或取代或 未取代的杂环基; R 3是氢,取代或未取代的烷基,环烷基,烷氧基烷基,取代或未取代的芳基,取代或未取代的杂环基或芳烷基,其中芳基部分是取代或未取代的; 或R 1和R 3与它们所连接的氮一起形成单个或稠合的,任选取代的饱和或不饱和杂环;给需要的人或非人哺乳动物,以及 公式一
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公开(公告)号:US06232089B1
公开(公告)日:2001-05-15
申请号:US09051529
申请日:1998-08-21
申请人: Derek Richard Buckle , Gary Christie , Ariane Elizabeth Marolewski , Ruth Judik Mayer , David Glynn Smith
发明人: Derek Richard Buckle , Gary Christie , Ariane Elizabeth Marolewski , Ruth Judik Mayer , David Glynn Smith
IPC分类号: C12Q137
CPC分类号: C07D495/04 , C07D333/34 , C07K14/7056 , C12N9/6489 , Y10S435/815
摘要: The present invention is to the discovery of a novel CD23 processing enzyme which is of importance in the human immune response and regulation of IgE production, and is a protein expressed on the surface of a variety of cells.
摘要翻译: 本发明是发现一种在人免疫应答和IgE产生调控中具有重要意义的CD23加工酶,是在多种细胞表面表达的蛋白质。
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5.
公开(公告)号:US06235753B1
公开(公告)日:2001-05-22
申请号:US09180547
申请日:1999-01-21
IPC分类号: C07C25904
CPC分类号: C07D333/54 , C07C259/06 , C07D277/64 , C07D307/80 , C07D333/60
摘要: Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.
摘要翻译: 提供了s-CD23的产生抑制剂和TNF的分泌
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