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1.发明申请New Acetyl Coenzyme A Carboxylase (ACC) Inhibitors And Uses In Treatments Of Obesity And Diabetes Mellitus - 087 审中-公开新型乙酰辅酶A羧化酶（ACC）抑制剂及其在肥胖和糖尿病治疗中的应用 - 087公开(公告)号：US20090306133A1
公开(公告)日：2009-12-10
申请号：US12339600
申请日：2008-12-19
申请人： David Blomberg , Anders Holmen , Petra Johannesson , Pernilla Sorme , Pernilla Stahlberg , Kay Brickmann , Volker Schnecke , Eric Wellner , Ragnar Hovland , Asa Mansson , Alleyn Plowright
发明人： David Blomberg , Anders Holmen , Petra Johannesson , Pernilla Sorme , Pernilla Stahlberg , Kay Brickmann , Volker Schnecke , Eric Wellner , Ragnar Hovland , Asa Mansson , Alleyn Plowright
IPC分类号： A61K31/4709 , C07D215/38 , C07D401/14 , A61P9/10 , A61P3/10 , A61K31/47
CPC分类号： C07C311/45 , C07C271/20 , C07C311/18 , C07C311/19 , C07C2601/14 , C07D213/81 , C07D213/82 , C07D215/36 , C07D215/52 , C07D217/02 , C07D271/06 , C07D277/54 , C07D277/64 , C07D277/82 , C07D309/04 , C07D319/18 , C07D333/34 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to Acetyl Coenzyme A Carboxylase (ACC) inhibitors according to formula (I), or an enantiomer thereof, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, E, L, Z and n are as defined herein, to processes for preparing such compounds, to pharmaceutical compositions containing them, to the use of such inhibitors and to methods for their therapeutic use, particularly in the treatments of obesity and diabetes mellitus.
摘要翻译： 本发明涉及式（I）的乙酰辅酶A羧化酶（ACC）抑制剂或其对映异构体或其药学上可接受的盐，其中R1，R2，R3，R4，R5，E，L，Z和n 本文定义的方法，制备此类化合物的方法，含有它们的药物组合物，使用这些抑制剂及其治疗用途的方法，特别是在治疗肥胖症和糖尿病中。
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公开(公告)号：US20100317653A1
公开(公告)日：2010-12-16
申请号：US12849158
申请日：2010-08-03
申请人： Alan Martin BIRCH , Suzanne Saxon Bowker , Roger John Butlin , Craig Samuel Donald , William Mccoull , Thorsten Nowak , Alleyn Plowright
发明人： Alan Martin BIRCH , Suzanne Saxon Bowker , Roger John Butlin , Craig Samuel Donald , William Mccoull , Thorsten Nowak , Alleyn Plowright
IPC分类号： A61K31/55 , C07D413/12 , A61K31/5377 , C07D413/14 , A61K31/496 , A61K31/454 , A61K31/444 , C07D271/07 , A61K31/4245 , C07D417/14 , A61K31/541 , A61K31/506 , A61P3/04 , A61P3/10
CPC分类号： C07D271/113 , C07D413/12
摘要： Compounds of formula (I), and salts and pro-drugs thereof: wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.
摘要翻译： 式（I）化合物及其盐和前药：其中例如R 1为任选取代的芳基或杂芳基; Y是选自例如直接键和（取代的）烷基链的连接基团; R2是任选取代的芳基，任选取代的环烷基或任选取代的杂环基; 被描述。 还描述了制备这些化合物的方法及其作为DGAT抑制剂的用途，例如用于治疗肥胖症。
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公开(公告)号：US20070112008A1
公开(公告)日：2007-05-17
申请号：US11582526
申请日：2006-10-17
申请人： Andrew Myers , Alleyn Plowright , Daniel Kung , Brian Lanman
发明人： Andrew Myers , Alleyn Plowright , Daniel Kung , Brian Lanman
IPC分类号： A61K31/498 , C07D487/04
CPC分类号： C07D471/18
摘要： In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I), and methods for the synthesis thereof. In another aspect, the present invention provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. In yet another aspect, the present invention provides methods for treating cancer comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof.
摘要翻译： 鉴于需要开发新型治疗剂及其合成方法，本发明提供了新的通式（I）化合物及其合成方法。 另一方面，本发明提供包含式（I）化合物和药学上可接受的载体的药物组合物。 另一方面，本发明提供了治疗癌症的方法，包括向有需要的受试者施用治疗有效量的式（I）化合物。
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公开(公告)号：US07659279B2
公开(公告)日：2010-02-09
申请号：US10555085
申请日：2004-04-27
IPC分类号： A61K31/517 , C07D239/88
CPC分类号： C07D403/12 , C07D403/14
摘要： The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use as therapeutic agents in the treatment of erbB tyrosine kinase mediated diseases such as cancer.
摘要翻译： 本发明涉及式（I）的喹唑啉衍生物： 其中X1，Q1，Z，R1，R2，Y，a和m如描述中所定义，其是erbB酪氨酸激酶抑制剂，特别是EGFR酪氨酸激酶抑制剂。 还要求他们的准备过程; 含有它们的药物组合物; 以及它们在治疗erbB酪氨酸激酶介导的疾病如癌症中的用途。
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公开(公告)号：US20070043010A1
公开(公告)日：2007-02-22
申请号：US10573352
申请日：2004-09-22
IPC分类号： A61K31/33
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention concerns a quinazoline derivative of the Formula (I): wherein each of the variables have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
摘要翻译： 本发明涉及式（I）的喹唑啉衍生物：其中每个变量具有说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤中的抗增殖剂的药物中的用途。
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公开(公告)号：US20060211714A1
公开(公告)日：2006-09-21
申请号：US10555085
申请日：2004-04-27
IPC分类号： A61K31/517 , C07D403/02
CPC分类号： C07D403/12 , C07D403/14
摘要： The invention concerns quinazoline derivatives of the formula: (I); wherein X1, Q1, Z, R1, R2, Y, a and m are as defined in the description, which are erbB tyrosine kinase inhibitors, particularly EGFR tyrosine kinase inhibitors. Also claimed are processes for their preparation; pharmaceutical compositions containing them; and their use as therapeutic agents in the treatment of erbB tyrosine kinase mediated diseases such as cancer.
摘要翻译： 本发明涉及式（I）的喹唑啉衍生物： 其中X 1，Q 1，Z，R 1，R 2，Y，a和m分别为 在描述中定义，其是erbB酪氨酸激酶抑制剂，特别是EGFR酪氨酸激酶抑制剂。 还要求他们的准备过程; 含有它们的药物组合物; 以及它们在治疗erbB酪氨酸激酶介导的疾病如癌症中的用途。
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公开(公告)号：US08003676B2
公开(公告)日：2011-08-23
申请号：US12302192
申请日：2007-05-29
申请人： Craig Johnstone , Alleyn Plowright
发明人： Craig Johnstone , Alleyn Plowright
IPC分类号： A61K31/4245 , A61P7/12 , A61P3/04 , C07D271/113
CPC分类号： C07D271/113
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein: n is 1, 2 or 3 and each R is independently selected from fluoro, chloro, cyano, methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译： 提供抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其盐，其中：n为1,2或3，并且每个R独立地选自氟，氯， 氰基，甲基，乙基，甲氧基，乙氧基，三氟甲基，三氟甲氧基和二氟甲氧基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。
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公开(公告)号：US07795283B2
公开(公告)日：2010-09-14
申请号：US11792922
申请日：2005-12-09
申请人： Alan Martin Birch , Suzanne Saxon Bowker , Roger John Butlin , Craig Samuel Donald , William McCoull , Thorsten Nowak , Alleyn Plowright
发明人： Alan Martin Birch , Suzanne Saxon Bowker , Roger John Butlin , Craig Samuel Donald , William McCoull , Thorsten Nowak , Alleyn Plowright
IPC分类号： A61K31/4245 , C07D271/113
CPC分类号： C07D271/113 , C07D413/12
摘要： Compounds of formula (I), and salts and pro-drugs thereof: Formula (I) wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.
摘要翻译： 式（I）化合物及其盐和前药：式（I）其中例如R 1为任选取代的芳基或杂芳基; Y是选自例如直接键和（取代的）烷基链的连接基团; R2是任选取代的芳基，任选取代的环烷基或任选取代的杂环基; 被描述。 还描述了制备这些化合物的方法及其作为DGAT抑制剂的用途，例如用于治疗肥胖症。
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公开(公告)号：US20100029727A1
公开(公告)日：2010-02-04
申请号：US12302192
申请日：2007-05-29
申请人： Craig Johnstone , Alleyn Plowright
发明人： Craig Johnstone , Alleyn Plowright
IPC分类号： A61K31/4245 , C07D271/113 , A61P7/12 , A61P3/04
CPC分类号： C07D271/113
摘要： Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein: n is 1, 2 or 3 and each R is independently selected from fluoro, chloro, cyano, methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
摘要翻译： 提供抑制乙酰CoA（乙酰辅酶A）：二酰基甘油酰基转移酶（DGAT1）活性的式（I）化合物或其盐，其中：n为1,2或3，并且每个R独立地选自氟，氯， 氰基，甲基，乙基，甲氧基，乙氧基，三氟甲基，三氟甲氧基和二氟甲氧基; 以及其制备方法，含有它们的药物组合物及其作为药物的用途。
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公开(公告)号：US20080096874A1
公开(公告)日：2008-04-24
申请号：US11792922
申请日：2005-12-09
申请人： Alan Birch , Suzanne Bowker , Roger Butlin , Craig Donald , William Mccoull , Thorsten Nowak , Alleyn Plowright
发明人： Alan Birch , Suzanne Bowker , Roger Butlin , Craig Donald , William Mccoull , Thorsten Nowak , Alleyn Plowright
IPC分类号： A61K31/4245 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P3/04 , A61P3/10 , C07D271/113 , C07D413/12 , C07D413/14 , C07D417/14
CPC分类号： C07D271/113 , C07D413/12
摘要： Compounds of formula (I), and salts and pro-drugs thereof: Formula (I) wherein for example R1 is optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; R2 is an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described.
摘要翻译： 式（I）化合物及其盐和前药：式（I）其中例如R 1为任选取代的芳基或杂芳基; Y是选自例如直接键和（取代的）烷基链的连接基团; R 2是任选取代的芳基，任选取代的环烷基或任选取代的杂环基; 被描述。 还描述了制备这些化合物的方法及其作为DGAT抑制剂的用途，例如用于治疗肥胖症。
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