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1. 发明授权

US09272996B2 2-acylaminopropoanol-type glucosylceramide synthase inhibitors 有权
标题翻译： 2-酰基氨基丙醇型葡萄糖神经酰胺合成酶抑制剂
公开(公告)号：US09272996B2
公开(公告)日：2016-03-01
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. Jozefiak , 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. Jozefiak , Frederic Vinick , Yibin Xiang , John Kane , Junkai Liao
IPC分类号： A61K31/397 , A61K31/5377 , A61K31/44 , A61K31/325 , A61K31/42 , A61K31/40 , C07D207/12 , C07D271/12 , C07D317/60 , C07D319/18 , C07D333/16 , C07D407/12 , C07D409/04 , C07D413/04 , C07D417/12 , C07C271/12 , C07D319/20 , C07D407/06
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。

2. 发明授权

US08304447B2 2-acylaminopropoanol-type glucosylceramide synthase inhibitors 有权
标题翻译： 2-酰基氨基丙醇型葡萄糖神经酰胺合成酶抑制剂
公开(公告)号：US08304447B2
公开(公告)日：2012-11-06
申请号：US12601871
申请日：2008-05-30
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： A61K31/40 , A61K31/4025 , C07D207/04 , C07D405/02
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。

3. 发明申请

US20120322787A1 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS 有权
标题翻译： 2-乙酰氨基酚类型葡萄糖苷合成酶抑制剂
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。

4. 发明授权

US08940776B2 2-acylaminopropoanol-type glucosylceramide synthase inhibitors 有权
标题翻译： 2-酰基氨基丙醇型葡萄糖神经酰胺合成酶抑制剂
公开(公告)号：US08940776B2
公开(公告)日：2015-01-27
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： A61K31/42 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/4025 , A61K31/40 , C07D277/20 , C07D277/62 , C07D261/06 , C07D405/02 , C07D271/06 , C07D207/04 , C07D295/125 , C07D319/18 , C07D405/06 , C07D405/12 , C07D407/12 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , 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。

5. 发明申请

US20100256216A1 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS 有权
标题翻译： 2-乙酰氨基酚类型葡萄糖苷合成酶抑制剂
公开(公告)号：US20100256216A1
公开(公告)日：2010-10-07
申请号：US12601871
申请日：2008-05-30
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 , C07D405/06 , C07D207/00 , A61K31/4015
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：或其可药用盐。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。

6. 发明申请

US20120322786A1 2-ACYLAMINOPROPOANOL-TYPE GLUCOSYLCERAMIDE SYNTHASE INHIBITORS 有权
标题翻译： 2-乙酰氨基酚类型葡萄糖苷合成酶抑制剂
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。

7. 发明授权

US08309593B2 2-acylaminopropoanol-type glucosylceramide synthase inhibitors 有权
标题翻译： 2-酰基氨基丙醇型葡萄糖神经酰胺合成酶抑制剂
公开(公告)号：US08309593B2
公开(公告)日：2012-11-13
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： A61K31/4025 , A61K31/40
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。

8. 发明申请

US20110184021A1 2-Acylaminopropoanol-Type Glucosylceramide Synthase Inhibitors 有权
标题翻译： 2-酰基氨基丙醇型葡萄糖神经酰胺合酶抑制剂
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。

9. 发明授权

US07754200B2 Phosphate transport inhibitors 有权
标题翻译：磷酸盐转运抑制剂
公开(公告)号：US07754200B2
公开(公告)日：2010-07-13
申请号：US11438679
申请日：2006-05-22
申请人： Thomas H. Jozefiak , Cecilia M. Bastos , Chad C. Huval
发明人： Thomas H. Jozefiak , Cecilia M. Bastos , Chad C. Huval
IPC分类号： A61K31/74
CPC分类号： C07F9/65502 , C07F9/3821 , C07F9/4012 , C07F9/5537 , C08F8/40 , C08F30/02 , Y02P20/55
摘要： Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1-C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or —CR1R2P(O)(OH)—. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from —Cl, —Br, —F, —CN, —NO2, —ORa, —N(Ra)2, —COORa, —CON(Ra)2, —CORa, —S(O)Ra, —S(O)2Ra, —S(O)2N(Ra)2, —NRaS(O)2Ra, —NRaCORa, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each Ra is independently —H, lower alkyl, substituted lower alkyl, aryl or substituted aryl.Each Rb is independently —H, a lower alkyl group, or a phosphate protecting group.
摘要翻译：公开了由结构式（I）表示的磷酸盐转运抑制化合物：R1和R2独立地为-H，吸电子基团或C1-C10烷基。 Y是共价键，取代亚甲基，未取代的亚甲基或-CR 1 R 2 P（O）（OH） - 。 R3是任选地包含一个或多个胺，铵，醚，硫醚或亚苯基连接基团的烃基，任选地包含一个或多个胺，铵，醚，硫醚或亚苯基连接基团的取代的烃基，杂芳基，取代的杂芳基被一个或多个选自-Cl，-Br，-F，-CN，-NO 2，-OR a，-N（R a）2，-COOR a，-CON（R a）2，-COR a ，-S（O）R a，-S（O）2 R a，-S（O）2 N（R a）2，-NR a（O）2 R a，-NR a COR a，卤代低级烷基，芳基，取代的芳基，或卤代烷氧基。每个R a独立地为-H，低级烷基，取代的低级烷基，芳基或取代的芳基。每个R b独立地是-H，低级烷基或磷酸酯保护基。

10. 发明授权

US07109184B2 Phosphate transport inhibitors 有权
公开(公告)号：US07109184B2
公开(公告)日：2006-09-19
申请号：US10392280
申请日：2003-03-19
申请人： Thomas H. Jozefiak , Cecilia M. Bastos , Chad C. Huval
发明人： Thomas H. Jozefiak , Cecilia M. Bastos , Chad C. Huval
IPC分类号： A10N57/00 , A61K31/675
CPC分类号： C07F9/65502 , C07F9/3821 , C07F9/4012 , C07F9/5537 , C08F8/40 , C08F30/02 , Y02P20/55
摘要： Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1–C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or —CR1R2P(O)(OH)—. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from —Cl, —Br, —F, —CN, —NO2, —ORa, —N(Ra)2, —COORa, —CON(Ra)2, —CORa, —S(O)Ra, —S(O)2Ra, —S(O)2N(Ra)2, —NRaS(O)2Ra, —NRaCORa, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each Ra is independently —H, lower alkyl, substituted lower alkyl, aryl or substituted aryl. Each Rb is independently —H, a lower alkyl group, or a phosphate protecting group.

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