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公开(公告)号：US20090312392A1
公开(公告)日：2009-12-17
申请号：US12387273
申请日：2009-04-30
IPC分类号： A61K31/40 , C07D207/04 , A61P43/00
CPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , A61K31/498 , A61K31/5375 , C07D295/13 , C07D317/54 , C07D319/18 , C07D321/10 , Y02A50/473
摘要： The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
摘要翻译： 本发明提供通过抑制GlyCer合酶抑制葡萄糖基神经酰胺（GlyCer）形成的氨基神经酰胺样化合物，从而降低糖鞘脂的含量。 本发明的化合物具有改善的GlcCer合酶抑制活性，因此可用于治疗与改变的鞘糖脂水平相关的各种病症和疾病的治疗方法。
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公开(公告)号：US07196205B2
公开(公告)日：2007-03-27
申请号：US11091836
申请日：2005-03-28
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , A61K31/4025 , C07D295/185 , C07D319/18 , C07D498/04
摘要： Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
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3.发明授权Synthesis of UDP-glucose: N-acylsphingosine glucosyltransferase inhibitors 有权UDP-葡萄糖的合成：N-酰基鞘氨醇葡糖基转移酶抑制剂公开(公告)号：US07615573B2
公开(公告)日：2009-11-10
申请号：US11702425
申请日：2007-02-05
IPC分类号： A61K31/40 , A61K31/445 , A61K31/5375 , C07D405/06
CPC分类号： C07D405/06 , A61K31/4025 , C07D295/185 , C07D319/18 , C07D498/04
摘要： Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
摘要翻译： 公开了UDP-葡萄糖：N-酰基鞘氨醇葡糖基转移酶的新型对映体合成神经酰胺样抑制剂。 还公开了在合成过程中形成的新型中间体。
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公开(公告)号：US07253185B2
公开(公告)日：2007-08-07
申请号：US11119541
申请日：2005-04-29
IPC分类号： A61K31/445 , A61K31/40 , C07D207/04 , C07D211/06
CPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , A61K31/498 , A61K31/5375 , C07D295/13 , C07D317/54 , C07D319/18 , C07D321/10 , Y02A50/473
摘要： The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
摘要翻译： 本发明提供通过抑制GlyCer合酶抑制葡萄糖基神经酰胺（GlyCer）形成的氨基神经酰胺样化合物，从而降低糖鞘脂的含量。 本发明的化合物具有改善的GlcCer合酶抑制活性，因此可用于治疗与改变的鞘糖脂水平相关的各种病症和疾病的治疗方法。
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公开(公告)号：US06916802B2
公开(公告)日：2005-07-12
申请号：US10839497
申请日：2004-05-05
IPC分类号： A61K31/397 , A61K31/40 , A61K31/4025 , A61K31/445 , A61K31/451 , A61K31/5377 , C07D295/13 , C07D317/54 , C07D319/18 , C07D321/10 , C07D413/02 , A61K31/5375 , C07D207/16 , C07D211/34
CPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , A61K31/498 , A61K31/5375 , C07D295/13 , C07D317/54 , C07D319/18 , C07D321/10 , Y02A50/473
摘要： The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
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公开(公告)号：US20080146533A1
公开(公告)日：2008-06-19
申请号：US11881738
申请日：2007-07-27
IPC分类号： A61K31/397 , A61K31/5375 , A61K31/498 , A61P9/10 , A61P31/04 , A61P13/12 , A61K31/445 , A61K31/40
CPC分类号： A61K31/397 , A61K31/40 , A61K31/445 , A61K31/498 , A61K31/5375 , C07D295/13 , C07D317/54 , C07D319/18 , C07D321/10 , Y02A50/473
摘要： The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
摘要翻译： 本发明提供通过抑制GlyCer合酶抑制葡萄糖基神经酰胺（GlyCer）形成的氨基神经酰胺样化合物，从而降低糖鞘脂的含量。 本发明的化合物具有改善的GlcCer合酶抑制活性，因此可用于治疗与改变的鞘糖脂水平相关的各种病症和疾病的治疗方法。
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7.发明申请AMORPHOUS AND A CRYSTALLINE FORM OF GENZ 112638 HEMITARTRATE AS INHIBITOR OF GLUCOSYLCERAMIDE SYNTHASE 审中-公开作为葡萄糖酸合成酶抑制剂的非晶形态和晶体结构112638 HEMITARTRATE公开(公告)号：US20130137743A1
公开(公告)日：2013-05-30
申请号：US13511768
申请日：2010-11-24
申请人： Hanlan Liu , Chris Willis , Renu Bhardwaj , Diane P. Copeland , Abizer Harianawala , Jeffrey Skell , John Marshall , Jianmei Kochling , Gerard Palace , Judith Peterschmitt , Craig Siegel , Seng Cheng
发明人： Hanlan Liu , Chris Willis , Renu Bhardwaj , Diane P. Copeland , Abizer Harianawala , Jeffrey Skell , John Marshall , Jianmei Kochling , Gerard Palace , Judith Peterschmitt , Craig Siegel , Seng Cheng
IPC分类号： C07D319/16 , A61K45/06 , A61K31/4025
CPC分类号： A61K31/4025 , A61K45/06 , C07D319/16 , C07D405/06
摘要： The hemitartrate salt of a compound represented by the following structural formula: (Formula I Hemitartrate), which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of the Formula (I) Hemitartrate are characterized by a variety of properties and physical measurements. As well, methods of producing crystalline Formula (I) Hemitartrate, and using it to inhibit glucosylceramide synthase or lowering glycosphingolipid concentrations in subjects to treat a number of diseases, are also discussed. Pharmaceutical compositions are also described.
摘要翻译： 公开了由以下结构式表示的化合物的盐酸盐：（式I Hemitartrate），其可用于药物应用。 式（I）的特殊单晶形式酒石酸盐的特征在于多种性质和物理测量。 此外，还讨论了生产结晶式（I）酒石酸盐并使用其抑制葡萄糖神经酰胺合成酶或降低受试者中的糖鞘醇浓度以治疗许多疾病的方法。 还描述了药物组合物。
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公开(公告)号：US20120322787A1
公开(公告)日：2012-12-20
申请号：US13595349
申请日：2012-08-27
申请人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Frederic Vinick , Thomas H. Jozefiak , Yibin Xiang , John Kane , Junkai Liao
发明人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Frederic Vinick , Thomas H. Jozefiak , Yibin Xiang , John Kane , Junkai Liao
IPC分类号： A61K31/4025 , A61P3/10 , A61P13/12 , C07D409/14 , A61K31/4439 , A61K31/397 , A61K31/422 , C07D417/14 , A61K31/428 , A61K31/4245 , A61K31/444 , A61K31/5377 , C07D405/10 , C07D413/14
CPC分类号： C07D417/14 , C07D295/125 , C07D319/18 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D413/14
摘要： A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-α, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译： 化合物由结构式（I）表示：或其药学上可接受的盐。 药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐。 治疗有需要的受试者的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。 受试者患有2型糖尿病; 肾脏肥大或与糖尿病肾病相关的增生; 泰撒 戈谢的 或法布里氏病。 分别在有需要的受试者中降低血浆TNF-α，降低血糖水平，降低糖化血红蛋白水平，抑制葡萄糖神经酰胺合成酶和降低糖鞘醇浓度的方法包括向受试者施用治疗有效量的由结构式（ I）或其药学上可接受的盐。
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公开(公告)号：US20110184021A1
公开(公告)日：2011-07-28
申请号：US13122135
申请日：2009-10-02
申请人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Thomas H. Jozafiak , Frederic Vinick , Yibin Xiang , John Kane , Junkai Liao
发明人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Thomas H. Jozafiak , Frederic Vinick , Yibin Xiang , John Kane , Junkai Liao
IPC分类号： A61K31/453 , A61K31/40 , A61K31/4025 , A61K31/4439 , A61K31/422 , A61K31/428 , A61P13/12
CPC分类号： A61K31/4025 , C07C271/12 , C07D207/12 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/16 , C07D407/06 , C07D407/12 , C07D409/04 , C07D413/04 , C07D417/12
摘要： A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译： 用于治疗多囊肾病的化合物由结构式（I）表示：或其药学上可接受的盐。 药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐。 在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。 分别在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。
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公开(公告)号：US20120322786A1
公开(公告)日：2012-12-20
申请号：US13595251
申请日：2012-08-27
申请人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Thomas H. Jozafiak , Frederic Vinick , Yibin Xiang , John Kane , Junkai Liao
发明人： Craig Siegel , Cecilia M. Bastos , David J. Harris , Angeles Dios , Edward Lee , Richard Silva , Lisa M. Cuff , Mikaela Levine , Cassandra A. Celatka , Thomas H. Jozafiak , Frederic Vinick , Yibin Xiang , John Kane , Junkai Liao
IPC分类号： A61K31/4025 , A61K31/4439 , A61K31/397 , A61K31/428 , A61K31/5377 , A61K31/40 , A61K31/422
CPC分类号： A61K31/4025 , C07C271/12 , C07D207/12 , C07D317/60 , C07D319/18 , C07D319/20 , C07D333/16 , C07D407/06 , C07D407/12 , C07D409/04 , C07D413/04 , C07D417/12
摘要： A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译： 用于治疗多囊肾病的化合物由结构式（I）表示：或其药学上可接受的盐。 药物组合物包含由结构式（I）表示的化合物或其药学上可接受的盐。 在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。 分别在有需要的受试者中治疗多囊肾病的方法包括向受试者施用治疗有效量的由结构式（I）表示的化合物或其药学上可接受的盐。
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