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公开(公告)号:US08993560B2
公开(公告)日:2015-03-31
申请号:US13414873
申请日:2012-03-08
IPC分类号: A61K31/55 , C07D401/12 , C07D403/12 , A61K31/4725 , A61K45/06 , C07D401/14
CPC分类号: C07D403/12 , A61K9/0014 , A61K31/4725 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14
摘要: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (SYK) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory diseases and/or allergic conditions, in cancer therapy, specifically heme malignancies, and autoimmune conditions.
摘要翻译: 式(I)的化合物或其盐; 其是脾脏酪氨酸激酶(SYK)的抑制剂,因此潜在地用于治疗由肥大细胞,巨噬细胞和B细胞的不适当活化引起的疾病以及相关的炎症反应和组织损伤,例如炎症性疾病和/或过敏性疾病 ,在癌症治疗中,特别是血红素恶性肿瘤和自身免疫病症。
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公开(公告)号:US20120202811A1
公开(公告)日:2012-08-09
申请号:US13451196
申请日:2012-04-19
IPC分类号: A61K31/5377 , A61P13/08
CPC分类号: A61K31/5377 , C07D401/06 , C07D413/14
摘要: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译: 式(I)的化合物,其中R 1是2-茚满基,R 2是1-甲基丙基,R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团,R 4表示甲基和R 5 表示氢或甲基,或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物,其制备方法,含有它们的药物组合物及其在药物中的用途,特别是其用作 催产素拮抗剂。
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公开(公告)号:US07919492B2
公开(公告)日:2011-04-05
申请号:US12850386
申请日:2010-08-04
IPC分类号: A61K31/5377
CPC分类号: A61K31/5377 , C07D401/06 , C07D413/14
摘要: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译: 式(I)的化合物,其中R 1是2-茚满基,R 2是1-甲基丙基,R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团,R 4表示甲基和R 5 表示氢或甲基,或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物,其制备方法,含有它们的药物组合物及其在药物中的用途,特别是其用作 催产素拮抗剂。
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公开(公告)号:US20110152262A1
公开(公告)日:2011-06-23
申请号:US13035366
申请日:2011-02-25
IPC分类号: A61K31/5355 , C07D413/14 , A61P15/12 , A61P15/06
CPC分类号: A61K31/5377 , C07D401/06 , C07D413/14
摘要: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译: 式(I)的化合物,其中R 1是2-茚满基,R 2是1-甲基丙基,R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团,R 4表示甲基和R 5 表示氢或甲基,或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物,其制备方法,含有它们的药物组合物及其在药物中的用途,特别是其用作 催产素拮抗剂。
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公开(公告)号:US07514437B2
公开(公告)日:2009-04-07
申请号:US10499177
申请日:2002-12-20
申请人: Alan David Borthwick , Richard Jonathan Hatley , Deirdre Mary Bernadette Hickey , John Liddle , David George Hubert Livermore , Andrew McMurtrie Mason , Neil Derek Miller , Fabrizio Nerozzi , Steven Leslie Sollis , Anna Katrin Szardenings , Paul Graham Wyatt
发明人: Alan David Borthwick , Richard Jonathan Hatley , Deirdre Mary Bernadette Hickey , John Liddle , David George Hubert Livermore , Andrew McMurtrie Mason , Neil Derek Miller , Fabrizio Nerozzi , Steven Leslie Sollis , Anna Katrin Szardenings , Paul Graham Wyatt
IPC分类号: A61K31/497 , A61K31/4965 , C07D241/00 , C07D241/02
CPC分类号: C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I) and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.
摘要翻译: 一种治疗或预防通过催产素作用介导的疾病或病症的方法,其包括向有需要的哺乳动物施用有效量的式(I)化合物和/或其生理上可接受的衍生物,其中所述取代基具有 说明中给出的含义。 公开了式(I)的新化合物及其制备方法。
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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:US20050014793A1
公开(公告)日:2005-01-20
申请号:US10900489
申请日:2004-07-28
申请人: Deirdre Hickey , Robert Ife , Colin Leach , John Liddle , Ivan Pinto , Stephen Smith , Steven Stanway
发明人: Deirdre Hickey , Robert Ife , Colin Leach , John Liddle , Ivan Pinto , Stephen Smith , Steven Stanway
IPC分类号: C07D215/20 , A61K31/435 , A61K31/437 , A61K31/4375 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61P3/10 , A61P9/00 , A61P9/10 , A61P19/02 , A61P29/00 , C07D211/74 , C07D215/36 , C07D221/04 , C07D401/12 , C07D471/04 , C07D495/04 , C07D513/04 , A61K31/4439 , C07
CPC分类号: C07D221/04 , C04B35/632 , C07D211/74 , C07D215/36 , C07D401/12 , C07D471/04 , C07D495/04 , C07D513/04
摘要: Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis.
摘要翻译: 式(I)化合物:是Lp-PLA2酶的抑制剂,可用于治疗,特别是治疗动脉粥样硬化。 式(I)化合物:是Lp-PLA2酶的抑制剂,可用于治疗,特别是治疗动脉粥样硬化。
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公开(公告)号:US08202864B2
公开(公告)日:2012-06-19
申请号:US13035366
申请日:2011-02-25
IPC分类号: A61K31/5377 , C07D413/14
CPC分类号: A61K31/5377 , C07D401/06 , C07D413/14
摘要: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译: 式(I)的化合物,其中R 1是2-茚满基,R 2是1-甲基丙基,R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团,R 4表示甲基和R 5 描述了氢或甲基,或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物,以及其制备方法,含有它们的药物组合物及其在药物中的用途,特别是其作为催产素的用途 拮抗剂
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19.
公开(公告)号:US08071594B2
公开(公告)日:2011-12-06
申请号:US10561498
申请日:2004-06-22
申请人: John Liddle
发明人: John Liddle
IPC分类号: A61K31/496 , C07D241/08 , C07D413/02
CPC分类号: A61K31/5377 , A61K9/0053 , C07D241/08 , C07D413/06 , C07D413/14
摘要: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the notrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.
摘要翻译: 式(1)的化合物,其中R 1是2-茚满基,R 2是1-甲基丙基,R 3是2-甲基-1,3-恶唑-4-基,R 4和R 5与它们所连接的雄激素原子一起代表吗啉代 ,其制备方法,含有它们的药物组合物及其在医药中的用途。
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公开(公告)号:US20100305127A1
公开(公告)日:2010-12-02
申请号:US12850386
申请日:2010-08-04
IPC分类号: A61K31/5377 , A61P15/06 , A61P15/12
CPC分类号: A61K31/5377 , C07D401/06 , C07D413/14
摘要: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
摘要翻译: 式(I)的化合物,其中R 1是2-茚满基,R 2是1-甲基丙基,R 3是选自2,6-二甲基-3-吡啶基或4,6-二甲基-3-吡啶基的基团,R 4表示甲基和R 5 表示氢或甲基,或者R4和R5与它们所连接的氮原子一起代表吗啉代及其药学上可接受的衍生物,其制备方法,含有它们的药物组合物及其在药物中的用途,特别是其用作 催产素拮抗剂。
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