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公开(公告)号：US20050277642A1
公开(公告)日：2005-12-15
申请号：US11198968
申请日：2005-08-08
IPC分类号： C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D521/00 , A61K31/53 , A61K31/506 , C07D43/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14
摘要： Compounds that selectively inhibit inappropriate kinase activities and methods for their preparation are disclosed. In one embodiment, the compounds are represented by Formula I, As selective inhibitors of inappropriate kinase activities, the compounds of the present invention are useful in the treatment of conditions associated with such activity, including, but not limited to, inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting inappropriate kinase activities and methods of treating conditions associated with such activities.
摘要翻译： 公开了选择性抑制不适当激酶活性的化合物及其制备方法。 在一个实施方案中，化合物由式I代替，作为不适当激酶活性的选择性抑制剂，本发明的化合物可用于治疗与此类活性相关的病症，包括但不限于炎性和自身免疫应答， 糖尿病，哮喘，牛皮癣，炎症性肠病，移植排斥反应和肿瘤转移。 还公开了抑制不适当的激酶活性的方法和治疗与这些活性相关的病症的方法。
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2.发明授权2-(4-oxo-4H-quinazolin-3-yl)acetamides and their use as vasopressin V3 antagonists 有权2-（4-氧代-4H-喹唑啉-3-基）乙酰胺及其作为血管加压素V3拮抗剂的用途公开(公告)号：US07807686B2
公开(公告)日：2010-10-05
申请号：US11908221
申请日：2006-03-10
申请人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Hoc , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
发明人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Hoc , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
IPC分类号： A61K31/517
CPC分类号： C07D409/04 , C07D239/91 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04
摘要： The present invention relates to 2-(4-oxo4H-quinazolin-3-yl) acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
摘要翻译： 本发明涉及式（I）的2-（4-氧代-4-喹唑啉-3-基）乙酰胺衍生物及其作为加压素V3拮抗剂的用途，特别是用于治疗抑郁症。
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公开(公告)号：US07906504B2
公开(公告)日：2011-03-15
申请号：US11852737
申请日：2007-09-10
申请人： Jeffrey Letourneau , Jui-Hsiang Chan , Patrick Jokiel , Michael Ohlmeyer , Irina Neagu , Christopher Riviello , John Richard Morphy , Susan Elizabeth Napier , Koc-Kan Ho
发明人： Jeffrey Letourneau , Jui-Hsiang Chan , Patrick Jokiel , Michael Ohlmeyer , Irina Neagu , Christopher Riviello , John Richard Morphy , Susan Elizabeth Napier , Koc-Kan Ho
IPC分类号： C07D217/24 , A61K31/472
CPC分类号： C07D217/24 , C07D401/12
摘要： Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.
摘要翻译： 本文公开了式I的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物或其药学上可接受的盐或溶剂合物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义。 还公开了包含根据本发明的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物及其在治疗中的用途的药物组合物。
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公开(公告)号：US20080051423A1
公开(公告)日：2008-02-28
申请号：US11843897
申请日：2007-08-23
申请人： Jeffrey Letourneau , Vidyahar Paradkar , Michael Ohlmeyer , Lawrence Dillard , John Baldwin , Christopher Riviello , Angela Wong , Yaing Rong
发明人： Jeffrey Letourneau , Vidyahar Paradkar , Michael Ohlmeyer , Lawrence Dillard , John Baldwin , Christopher Riviello , Angela Wong , Yaing Rong
IPC分类号： C07D235/06 , A61K31/4184 , A61K31/428 , A61K31/47 , A61K31/4985 , A61P19/00 , C07D487/02 , C07D277/82 , A61P27/00 , A61P3/00 , A61P35/00 , C07D215/38
CPC分类号： C07D215/38 , C07D235/30 , C07D401/12 , C07D403/12 , C07D405/12 , C07D487/04
摘要： Nitrogen heterocycle biaryls having a carboxylate terminus are useful for treating endometriosis, osteoporosis, restenosis following angioplasty, rheumatoid arthritis, cancer, macular degeneration and obesity. Compounds of formula: are disclosed. A representative example is
摘要翻译： 具有羧酸酯末端的氮杂环联芳烃可用于治疗子宫内膜异位症，骨质疏松症，血管成形术后的再狭窄，类风湿性关节炎，癌症，黄斑变性和肥胖症。 公开了式的化合物。 一个代表性的例子是
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5.发明申请公开(公告)号：US20070037822A1
公开(公告)日：2007-02-15
申请号：US11422710
申请日：2006-06-07
IPC分类号： A61K31/513 , A61K31/4965 , A61K31/4412 , C07D213/63 , C07D239/02
CPC分类号： C07D213/82 , C07D239/26 , C07D239/36 , C07D241/24 , C07D295/088 , C07D403/04 , C07D403/12 , C07D413/04
摘要： Substituted pyridines, pyrimidines, pyrazines, pyridinones, pyrimidinones, pyrazinones and phenylacetamides useful in treating depression, stress and other disorders are disclosed. The compounds are of the formualae: Other embodiments are also disclosed.
摘要翻译： 公开了用于治疗抑郁症，压力和其它疾病的取代的吡啶，嘧啶，吡嗪，吡啶酮，嘧啶酮，吡嗪酮和苯乙酰胺。 化合物是形式：其他实施方案也被公开。
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公开(公告)号：US20050222203A1
公开(公告)日：2005-10-06
申请号：US10775963
申请日：2004-02-10
申请人： Jeffrey Letourneau , Vidyahar Paradkar , Michael Ohlmeyer , Lawrence Dillard , John Baldwin , Christopher Riviello , Angela Wong , Yaing Rong
发明人： Jeffrey Letourneau , Vidyahar Paradkar , Michael Ohlmeyer , Lawrence Dillard , John Baldwin , Christopher Riviello , Angela Wong , Yaing Rong
IPC分类号： A61K31/4184 , A61K31/4188 , A61K31/428 , A61K31/47 , C07D215/38 , C07D235/30 , C07D277/62 , C07D277/82 , C07D401/12 , C07D403/12 , C07D405/12
CPC分类号： C07D215/38 , C07D235/30 , C07D277/82 , C07D401/12 , C07D403/12 , C07D405/12
摘要： Nitrogen heterocycle biaryls having a carboxylate terminus are useful for treating endometriosis, osteoporosis, restenosis following angioplasty, rheumatoid arthritis, cancer, macular degeneration and obesity. Compounds of formula: are disclosed. A representative example is
摘要翻译： 具有羧酸酯末端的氮杂环联芳烃可用于治疗子宫内膜异位症，骨质疏松症，血管成形术后的再狭窄，类风湿性关节炎，癌症，黄斑变性和肥胖症。 公开了式的化合物。 一个代表性的例子是
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7.发明申请2-(4-Oxo-4H-Quinazolin-3-Yl) Acetamides and Their Use as Vasopressin V3 Antagonists 有权2-（4-氧代-4H-喹唑啉-3-基）乙酰胺及其作为加压素V3拮抗剂的用途公开(公告)号：US20080214553A1
公开(公告)日：2008-09-04
申请号：US11908221
申请日：2006-03-10
申请人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Ho , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
发明人： Jeffrey Letourneau , Christopher Riviello , Koc-Kan Ho , Jui-Hsiang Chan , Michael Ohlmeyer , Patrick Jokiel , Irina Neagu , John Richard Morphy , Susan Elizabeth Napier
IPC分类号： A61K31/517 , C07D403/02
CPC分类号： C07D409/04 , C07D239/91 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04
摘要： The present invention relates to 2-(4-oxo4H-quinazolin-3-yl)acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
摘要翻译： 本发明涉及式（I）的2-（4-氧代-4-喹唑啉-3-基）乙酰胺衍生物及其作为加压素V3拮抗剂的用途，特别是用于治疗抑郁症。
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公开(公告)号：US20080064678A1
公开(公告)日：2008-03-13
申请号：US11852737
申请日：2007-09-10
申请人： Jeffrey Letourneau , Jui-Hsiang Chan , Patrick Jokiel , Michael Ohlmeyer , Irina Neagu , Christopher Riviello , John Morphy , Susan Napier , Koc-Kan Ho
发明人： Jeffrey Letourneau , Jui-Hsiang Chan , Patrick Jokiel , Michael Ohlmeyer , Irina Neagu , Christopher Riviello , John Morphy , Susan Napier , Koc-Kan Ho
IPC分类号： C07D217/24 , A61K31/397 , A61K31/472 , A61P25/00
CPC分类号： C07D217/24 , C07D401/12
摘要： Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.
摘要翻译： 本文公开了式I的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物或其药学上可接受的盐或溶剂合物，其中每个取代基被给出如说明书和权利要求中所阐述的定义。 还公开了包含根据本发明的2-（1-氧代-1H-异喹啉-2-基）乙酰胺衍生物及其在治疗中的用途的药物组合物。
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公开(公告)号：US20050239770A1
公开(公告)日：2005-10-27
申请号：US11143430
申请日：2005-06-02
申请人： Kevin Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn Erickson , Jeffrey Letourneau , Edward McDonald , Katerina Leftheris , Stephen Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John Baldwin , Alaric Dyckman
发明人： Kevin Moriarty , Yvonne Shimshock , Gulzar Ahmed , Junjun Wu , James Wen , Wei Li , Shawn Erickson , Jeffrey Letourneau , Edward McDonald , Katerina Leftheris , Stephen Wrobleski , Zahid Hussain , Ian Henderson , Axel Metzger , John Baldwin , Alaric Dyckman
IPC分类号： A61K31/40 , A61K31/551 , C07D251/52 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D521/00
CPC分类号： C07D251/52 , C07D231/12 , C07D233/56 , C07D249/08 , C07D251/48 , C07D251/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula I: Methods of production, pharmaceutical compositions and methods of treating conditions associated with inappropriate p38 kinase activity or TNF-α expression utilizing compounds of the present invention are also disclosed.
摘要翻译： 公开了通过抑制p38激酶阻断细胞因子产生的N-杂环化合物。 在一个实施方案中，本发明的化合物由式I表示：还公开了使用本发明化合物的生产方法，药物组合物和治疗与不适当的p38激酶活性或TNF-α表达相关的病症的方法。
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公开(公告)号：US07820649B2
公开(公告)日：2010-10-26
申请号：US11852762
申请日：2007-09-10
申请人： Jeffrey Letourneau , Patrick Jokiel , Susan Elizabeth Napier , Koc-Kan Ho , Michael Ohlmeyer , Duncan Robert McArthur , Fiona Jeremiah , Paul David Ratcliffe , Jurgen Schulz
发明人： Jeffrey Letourneau , Patrick Jokiel , Susan Elizabeth Napier , Koc-Kan Ho , Michael Ohlmeyer , Duncan Robert McArthur , Fiona Jeremiah , Paul David Ratcliffe , Jurgen Schulz
IPC分类号： C07D239/88
CPC分类号： C07D403/04 , C07D217/24 , C07D239/91 , C07D401/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/08 , C07D487/04
摘要： Disclosed herein are quinazolinone or isoquinolinone derivatives of formula I, or pharmaceutically acceptable salts or solvates thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising quinazolinone or isoquinolinone according to the present invention and its use in therapy.
摘要翻译： 本文公开的式I的喹唑啉酮或异喹啉酮衍生物或其药学上可接受的盐或溶剂化物，其中每个取代基都给出如说明书和权利要求书中所阐述的定义。 还公开了包含根据本发明的喹唑啉酮或异喹啉酮及其在治疗中的用途的药物组合物。
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