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公开(公告)号：US20090203603A1
公开(公告)日：2009-08-13
申请号：US12338887
申请日：2008-12-18
IPC分类号： A61K38/00
CPC分类号： A61K38/26
摘要： Compositions and methods for the prevention and treatment of nephropathy, including hypertensive and diabetic nephropathy, and nephropathy associated with insulin resistance and metabolic syndrome are described. Compositions of the invention include a compound that binds to a receptor for the glucagon like peptide-1, an incretin, a glucagon-like peptide-1 (GLP-1), an exendin, or an analog (including an agonist analog), derivative, or variant of any of them.
摘要翻译： 描述了预防和治疗肾病，包括高血压和糖尿病肾病以及与胰岛素抵抗和代谢综合征相关的肾病的组合物和方法。 本发明的组合物包括与胰高血糖素样肽-1，肠降血糖素，胰高血糖素样肽-1（GLP-1），毒蜥外泌肽或类似物（包括激动剂类似物）衍生物的受体结合的化合物 ，或其任何变体。
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2.发明授权Methods of modulating cell proliferation and cyst formation in polycystic kidney and liver diseases 有权调节多囊肾和肝脏疾病中细胞增殖和囊肿形成的方法公开(公告)号：US08846764B2
公开(公告)日：2014-09-30
申请号：US11900722
申请日：2007-09-13
IPC分类号： A61K31/155 , A61K31/535 , A61K31/4406 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/421
CPC分类号： A61K31/5375 , A61K31/155 , A61K31/18 , A61K31/20 , A61K31/201 , A61K31/202
摘要： The present invention provides a method for preferentially reducing the proliferation of cystic epithelial cells in the kidney or bile duct in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to preferentially reduce the proliferation of cystic epithelial cells over normal epithelial cells such as tubule epithelial cells in the kidney or bile duct. The present invention also provides a method for preventing or treating autosomal dominant polycystic kidney disease (ADPKD), autosomal recessive polycystic kidney disease (ARPKD), ARPKD associated congenital hepatic fibrosis, ARPKD associated Caroli's disease, or cholangiocarcinoma in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to prevent or treat the disease.
摘要翻译： 本发明提供了一种通过向哺乳动物施用20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以使哺乳动物中的囊肿上皮细胞在肾或胆管中增殖的方法， 优先减少囊肿上皮细胞与正常上皮细胞（如肾脏或胆管中的小管上皮细胞）的增殖。 本发明还提供一种预防或治疗有需要的哺乳动物的常染色体显性多囊肾病（ADPKD），常染色体隐性多囊肾病（ARPKD），与ARPKD相关的先天性肝纤维化，ARPKD相关的卡罗里病或胆管癌的方法， 20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以预防或治疗该疾病。
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公开(公告)号：US20080306155A1
公开(公告)日：2008-12-11
申请号：US12141585
申请日：2008-06-18
申请人： Richard J. Roman , John R. Falck
发明人： Richard J. Roman , John R. Falck
IPC分类号： A61K31/20 , A61K31/201 , A61P13/12 , A61K31/195
CPC分类号： A61K31/202
摘要： A method preserving renal medullary blood flow in a renal disorder in a human or non-human animal is disclosed. The method involves administering 20-HETE or a 20-HETE analog to the human or non-human animal in an amount sufficient to attenuate a fall in renal medullary blood flow following a renal disorder. In addition, a method for preventing and treating ischemic acute renal failure is disclosed. The method involves administering 20-HETE or a 20-HETE agonist to the human or non-human animal in an amount sufficient to prevent or treat ischemic acute renal failure.
摘要翻译： 公开了一种在人或非人动物中保留肾脏疾病中的肾髓质血流的方法。 该方法涉及以足以减轻肾功能障碍后肾髓质血流量下降的量向人或非人动物施用20-HETE或20-HETE类似物。 此外，公开了一种预防和治疗缺血性急性肾衰竭的方法。 该方法涉及以足以预防或治疗缺血性急性肾衰竭的量向人或非人动物施用20-HETE或20-HETE激动剂。
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4.发明授权Use of 20-HETE synthesizing enzyme inhibitors as therapy for cerebral vascular disease 失效使用20-HETE合成酶抑制剂作为脑血管病的治疗公开(公告)号：US07307101B2
公开(公告)日：2007-12-11
申请号：US09937946
申请日：2001-09-06
申请人： Richard J. Roman , David R. Harder , Noriyuki Miyata , Masakazu Sato , Kazuya Kameo , Shigeru Okuyama
发明人： Richard J. Roman , David R. Harder , Noriyuki Miyata , Masakazu Sato , Kazuya Kameo , Shigeru Okuyama
IPC分类号： A01N37/34 , A61K37/275 , C12N9/10
CPC分类号： A61K31/15 , A61K31/20 , A61K31/4164 , A61K31/4192 , A61K48/00
摘要： A method for treating cerebral vascular diseases in a human or non-human animal is disclosed. The method involves inhibiting 20-HETE synthesizing enzyme activity sufficiently to increase or prevent a decrease in cerebral blood flow in the human or non-human animal.
摘要翻译： 公开了一种用于治疗人或非人动物的脑血管疾病的方法。 所述方法包括充分抑制20-HETE合成酶活性以增加或防止人或非人动物中脑血流量的降低。
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公开(公告)号：US06605641B2
公开(公告)日：2003-08-12
申请号：US10017409
申请日：2001-12-14
申请人： Richard J. Roman , John R. Falck , Magdalena Alonso-Galicia , Elizabeth R. Jacobs , David R. Harder
发明人： Richard J. Roman , John R. Falck , Magdalena Alonso-Galicia , Elizabeth R. Jacobs , David R. Harder
IPC分类号： A61K3120
CPC分类号： A61K31/202 , A61K31/00 , A61K31/18 , A61K31/20 , A61K31/201 , Y10S514/826 , Y10S514/866
摘要： 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z), 14(Z)-dienoic acid and 20-, 21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z), 15(Z)-dienoic acid.
摘要翻译： 20-HETE激动剂和拮抗剂以及治疗应用被公开。 在本发明的优选形式中，20-HETE激动剂选自21-羟基乙烯-5（Z），8（Z），11（Z），14（Z） - 四烯酸，20-羟基二十碳烯 -5（Z），14（Z） - 二烯酸和20-，21-二甲基20-HETE。 优选的20-HETE拮抗剂包括5（S）-HETE，15（S）-HETE，19（S）-HETE，19-羟基十五碳五烯（Z），8（Z），11（Z） （Z），15（Z） - 二烯酸。
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公开(公告)号：US06596769B2
公开(公告)日：2003-07-22
申请号：US10021973
申请日：2001-12-14
申请人： Richard J. Roman , John R. Falck , Magdalena Alonso-Galicia , Elizabeth R. Jacobs , David R. Harder
发明人： Richard J. Roman , John R. Falck , Magdalena Alonso-Galicia , Elizabeth R. Jacobs , David R. Harder
IPC分类号： A61K3120
CPC分类号： A61K31/202 , A61K31/00 , A61K31/18 , A61K31/20 , A61K31/201 , Y10S514/826 , Y10S514/866
摘要： 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.
摘要翻译： 20-HETE激动剂和拮抗剂以及治疗应用被公开。 在本发明的优选形式中，20-HETE激动剂选自21-羟基乙烯-5（Z），8（Z），11（Z），14（Z） - 四烯酸，20-羟基二十碳烯 -5（Z），4（Z） - 二烯酸和20-，21-二甲基20-HETE。 优选的20-HETE拮抗剂包括5（S）-HETE，15（S）-HETE，19（S）-HETE，19-羟基十五碳五烯（Z），8（Z），11（Z） （Z），15（Z） - 二烯酸。
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7.发明授权Methods of modulating cell proliferation and cyst formation in polycystic kidney and liver diseases 有权调节多囊肾和肝脏疾病中细胞增殖和囊肿形成的方法公开(公告)号：US09511072B2
公开(公告)日：2016-12-06
申请号：US14302545
申请日：2014-06-12
IPC分类号： A61K31/5375 , A61K31/155 , A61K31/18 , A61K31/20 , A61K31/201 , A61K31/202
CPC分类号： A61K31/5375 , A61K31/155 , A61K31/18 , A61K31/20 , A61K31/201 , A61K31/202
摘要： The present invention provides a method for preferentially reducing the proliferation of cystic epithelial cells in the kidney or bile duct in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to preferentially reduce the proliferation of cystic epithelial cells over normal epithelial cells such as tubule epithelial cells in the kidney or bile duct. The present invention also provides a method for preventing or treating autosomal dominant polycystic kidney disease (ADPKD), autosomal recessive polycystic kidney disease (ARPKD), ARPKD associated congenital hepatic fibrosis, ARPKD associated Caroli's disease, or cholangiocarcinoma in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to prevent or treat the disease.
摘要翻译： 本发明提供了一种通过向哺乳动物施用20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以使哺乳动物中的囊肿上皮细胞在肾或胆管中增殖的方法， 优先减少囊肿上皮细胞与正常上皮细胞（如肾脏或胆管中的小管上皮细胞）的增殖。 本发明还提供一种预防或治疗有需要的哺乳动物的常染色体显性多囊肾病（ADPKD），常染色体隐性多囊肾病（ARPKD），与ARPKD相关的先天性肝纤维化，ARPKD相关的卡罗里病或胆管癌的方法， 20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以预防或治疗该疾病。
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8.发明申请Methods of Modulating Cell Proliferation and Cyst Formation in Polycystic Kidney and Liver Diseases 有权调节多囊肾和肝脏疾病中细胞增殖和囊肿形成的方法公开(公告)号：US20140329811A1
公开(公告)日：2014-11-06
申请号：US14302545
申请日：2014-06-12
IPC分类号： A61K31/5375 , A61K31/18 , A61K31/201 , A61K31/202 , A61K31/155 , A61K31/20
CPC分类号： A61K31/5375 , A61K31/155 , A61K31/18 , A61K31/20 , A61K31/201 , A61K31/202
摘要： The present invention provides a method for preferentially reducing the proliferation of cystic epithelial cells in the kidney or bile duct in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to preferentially reduce the proliferation of cystic epithelial cells over normal epithelial cells such as tubule epithelial cells in the kidney or bile duct. The present invention also provides a method for preventing or treating autosomal dominant polycystic kidney disease (ADPKD), autosomal recessive polycystic kidney disease (ARPKD), ARPKD associated congenital hepatic fibrosis, ARPKD associated Caroli's disease, or cholangiocarcinoma in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to prevent or treat the disease.
摘要翻译： 本发明提供了一种通过向哺乳动物施用20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以使哺乳动物中的囊肿上皮细胞在肾或胆管中增殖的方法， 优先减少囊肿上皮细胞与正常上皮细胞（如肾脏或胆管中的小管上皮细胞）的增殖。 本发明还提供一种预防或治疗有需要的哺乳动物的常染色体显性多囊肾病（ADPKD），常染色体隐性多囊肾病（ARPKD），与ARPKD相关的先天性肝纤维化，ARPKD相关的卡罗里病或胆管癌的方法， 20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以预防或治疗该疾病。
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公开(公告)号：US07507871B2
公开(公告)日：2009-03-24
申请号：US10625870
申请日：2003-07-23
CPC分类号： A01K67/0275 , A01K2217/05 , A01K2227/105 , A01K2267/0306 , A01K2267/0362 , A61K49/0008 , C12N15/8509 , G01N33/6893 , G01N2800/042 , G01N2800/347 , Y10S514/866
摘要： A rat model of diabetic nephropathy is disclosed. In another embodiment of the invention, a method of evaluating a test compound's effect of diabetic nephropathy is disclosed. In one embodiment, this method comprises the steps of (a) exposing the test compound to the rat of claim 1, wherein the rat would develop progressive proteinuria and glomerulosclerosis leading to diabetic nephropathy in the absence of the test compound, and (b) comparing the rat's development of diabetic nephropathy with a control T2DN mimic rat that has not been exposed to the test compound.
摘要翻译： 公开了糖尿病肾病的大鼠模型。 在本发明的另一个实施方案中，公开了评估测试化合物对糖尿病肾病的作用的方法。 在一个实施方案中，该方法包括以下步骤：（a）将测试化合物暴露于权利要求1的大鼠，其中所述大鼠将在不存在测试化合物的情况下发展进展性蛋白尿和肾小球硬化，导致糖尿病性肾病，和（b）比较 大鼠与对照T2DN模拟大鼠的糖尿病肾病的发展没有暴露于测试化合物。
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10.发明申请Methods of modulating cell proliferation and cyst formation in polycystic kidney and liver diseases 有权调节多囊肾和肝脏疾病中细胞增殖和囊肿形成的方法公开(公告)号：US20080167382A1
公开(公告)日：2008-07-10
申请号：US11900722
申请日：2007-09-13
IPC分类号： A61K31/155 , A61P35/00 , A61P13/12
CPC分类号： A61K31/5375 , A61K31/155 , A61K31/18 , A61K31/20 , A61K31/201 , A61K31/202
摘要： The present invention provides a method for preferentially reducing the proliferation of cystic epithelial cells in the kidney or bile duct in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to preferentially reduce the proliferation of cystic epithelial cells over normal epithelial cells such as tubule epithelial cells in the kidney or bile duct. The present invention also provides a method for preventing or treating autosomal dominant polycystic kidney disease (ADPKD), autosomal recessive polycystic kidney disease (ARPKD), ARPKD associated congenital hepatic fibrosis, ARPKD associated Caroli's disease, or cholangiocarcinoma in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to prevent or treat the disease.
摘要翻译： 本发明提供了一种通过向哺乳动物施用20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以使哺乳动物中的囊肿上皮细胞在肾或胆管中增殖的方法， 优先减少囊肿上皮细胞与正常上皮细胞（如肾脏或胆管中的小管上皮细胞）的增殖。 本发明还提供一种预防或治疗有需要的哺乳动物的常染色体显性多囊肾病（ADPKD），常染色体隐性多囊肾病（ARPKD），与ARPKD相关的先天性肝纤维化，ARPKD相关的卡罗里病或胆管癌的方法， 20-HETE合成酶抑制剂或20-HETE拮抗剂，其量足以预防或治疗该疾病。
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