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1. 发明申请

US20080194593A1 A2B ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译： A2B腺苷受体拮抗剂
公开(公告)号：US20080194593A1
公开(公告)日：2008-08-14
申请号：US12013348
申请日：2008-01-11
申请人： Rao Kalla , Thao Perry , Elfatih Elzein , Xiaofen Li , Jeff Zablocki , Dewan Zeng , Dengming Xiao , Vaibhav Varkhedkar , Prabha Ibrahim , Venkata Palle , Hongyan Zhong
发明人： Rao Kalla , Thao Perry , Elfatih Elzein , Xiaofen Li , Jeff Zablocki , Dewan Zeng , Dengming Xiao , Vaibhav Varkhedkar , Prabha Ibrahim , Venkata Palle , Hongyan Zhong
IPC分类号： A61K31/522 , A61P35/00
CPC分类号： C07D473/06 , A61K31/522 , C07D473/08
摘要： Disclosed are methods for treating asthma, inflammatory gastrointestinal tract disorders, cancer, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis using A2B adenosine receptor antagonists having the structure of Formula I or Formula II:
摘要翻译：公开了使用具有式I或式II结构的Aβ2A腺苷受体拮抗剂治疗哮喘，炎症性胃肠道疾病，癌症，心血管疾病，神经障碍和与不良血管发生相关的疾病的方法：

2. 发明申请

US20080318983A1 A2B ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译： A2B腺苷受体拮抗剂
公开(公告)号：US20080318983A1
公开(公告)日：2008-12-25
申请号：US12147382
申请日：2008-06-26
申请人： Rao Kalla , Thao Perry , Elfatih Elzein , Vaibhav Varkhedkar , Xiaofen Li , Prabha Ibrahim , Venkata Palle , Dengming Xiao , Jeff Zablocki , Dewan Zeng , Hongyan Zhong
发明人： Rao Kalla , Thao Perry , Elfatih Elzein , Vaibhav Varkhedkar , Xiaofen Li , Prabha Ibrahim , Venkata Palle , Dengming Xiao , Jeff Zablocki , Dewan Zeng , Hongyan Zhong
IPC分类号： A61K31/522 , A61P35/00
CPC分类号： A61K31/522 , C07D473/06 , C07D473/08
摘要： Disclosed are methods for treating asthma, inflammatory gastrointestinal tract disorders, cancer, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis using A2B adenosine receptor antagonists having the structure of Formula I or Formula II:
摘要翻译：公开了使用具有式I或式II结构的A2B腺苷受体拮抗剂治疗哮喘，炎症性胃肠道疾病，癌症，心血管疾病，神经障碍和与不良血管发生相关的疾病的方法：

3. 发明申请

US20090099212A1 A3 ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
标题翻译： A3腺苷受体拮抗剂
公开(公告)号：US20090099212A1
公开(公告)日：2009-04-16
申请号：US12253019
申请日：2008-10-16
申请人： Jeff Zablocki , Rao Kalla , Dewan Zeng
发明人： Jeff Zablocki , Rao Kalla , Dewan Zeng
IPC分类号： A61K31/52
CPC分类号： A61K31/52
摘要： Disclosed are novel methods of antagonizing the A3 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the formula: wherein R is hydrogen or acyl; R1 is hydrogen, halo, optionally substituted C1-4 alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl; R2 is optionally substituted C1-4 alkyl; Y is C1-4 alkylene; and Z is phenyl, optionally substituted with halo, optionally substituted C1-4 alkyl, or C1-4 alkoxy. The A3 adenosine receptors may be antagonized in order to treat a disease state is chosen from renal failure, nephritis, hypertension, oedemas, Alzheimers disease, stress, depression, cardiac arrhythmia, restoration of cardiac function, asthma, respiratory disorders, ischemia-induced injury of the brain, heart and kidney, and diarrhea. Preferred compounds selectively antagonize A3 adenosine receptors over A1 adenosine receptors, A2A adenosine receptors and A2B adenosine receptors.
摘要翻译：公开了一种拮抗哺乳动物中的A3腺苷受体的新方法，包括向有需要的哺乳动物施用治疗有效剂量的下式化合物：其中R是氢或酰基; R 1是氢，卤素，任选取代的C 1-4烷基，任选取代的烯基，任选取代的芳基或任选取代的杂芳基; R2是任选取代的C 1-4烷基; Y为C 1-4亚烷基; 且Z为苯基，任选被卤素，任选取代的C 1-4烷基或C 1-4烷氧基取代。可以拮抗A3腺苷受体以治疗疾病状态，其选自肾衰竭，肾炎，高血压，高血糖，阿尔茨海默病，压力，抑郁，心律失常，心脏功能恢复，哮喘，呼吸障碍，缺血诱导的损伤的大脑，心脏和肾脏以及腹泻。优选的化合物选择性拮抗Aβ腺苷受体，A1腺苷受体，A2A腺苷受体和A2B腺苷受体。

4. 发明申请

US20050059683A1 A1 adenosine receptor antagonists 失效
标题翻译： A1腺苷受体拮抗剂
公开(公告)号：US20050059683A1
公开(公告)日：2005-03-17
申请号：US10897047
申请日：2004-07-22
申请人： Jeff Zablocki , Rao Kalla , Dewan Zeng
发明人： Jeff Zablocki , Rao Kalla , Dewan Zeng
IPC分类号： A61K31/52 , A61P1/12 , A61P3/10 , A61P7/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P25/24 , A61P25/28
CPC分类号： A61K31/52
摘要： Disclosed are novel methods of antagonizing the A1 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the formula: wherein R1 is optionally substituted C1-4 alkyl; Y is C1-4 alkylene; and Z is phenyl that is optionally substituted with halo, hydroxy, amino, cyano, or optionally substituted C1-4 alkyl or a pharmaceutically acceptable salt, ester, or prodrug thereof. The A1 adenosine receptors are antagonized in order to treat a disease state is chosen from renal failure, renal dysfunction, nephritis, hypertension, oedema, Alzheimers disease, stress, depression, cardiac arrhythmia, restoration of cardiac function, congestive heart failure, diabetes, asthma, respiratory disorders, ischaemia-induced injury of the brain, heart and kidney, and diarrhea.
摘要翻译：公开了一种拮抗哺乳动物中的A1腺苷受体的新方法，包括向有需要的哺乳动物施用治疗有效剂量的下式化合物：其中R 1为任选取代的C 1-4烷基; Y为C 1-4亚烷基; 并且Z是任选被卤素，羟基，氨基，氰基或任选取代的C 1-4烷基取代的苯基或其药学上可接受的盐，酯或前药。 A1腺苷受体被拮抗以治疗疾病状态，选自肾衰竭，肾功能不全，肾炎，高血压，水肿，阿尔茨海默病，压力，抑郁，心律失常，心脏功能恢复，充血性心力衰竭，糖尿病，哮喘，呼吸障碍，局部缺血引起的脑，心脏和肾脏的损伤以及腹泻。

5. 发明授权

US07022710B2 A1 adenosine receptor antagonists 失效
标题翻译： A1腺苷受体拮抗剂
公开(公告)号：US07022710B2
公开(公告)日：2006-04-04
申请号：US10897047
申请日：2004-07-22
申请人： Jeff Zablocki , Rao Kalla , Dewan Zeng
发明人： Jeff Zablocki , Rao Kalla , Dewan Zeng
IPC分类号： A61K31/52
CPC分类号： A61K31/52
摘要： Disclosed are novel methods of antagonizing the A1 adenosine receptor in a mammal, comprising administering to a mammal in need thereof a therapeutically effective dose of a compound of the formula: wherein R1 is optionally substituted C1-14 alkyl; Y is C1-14 alkylene; and Z is phenyl that is optionally substituted with halo, hydroxy, amino, cyano, or optionally substituted C1-4 alkyl or a pharmaceutically acceptable salt, ester, or prodrug thereof. The A1 adenosine receptors are antagonized in order to treat a disease state is chosen from renal failure, renal dysfunction, nephritis, hypertension, edema, Alzheimers disease, stress, depression, cardiac arrhythmia, restoration of cardiac function, congestive heart failure, diabetes, asthma, respiratory disorders, ischemia-induced injury of the brain, heart and kidney, and diarrhea.
摘要翻译：公开了一种拮抗哺乳动物中的Aβ1 - 腺苷受体的新方法，其包括向有需要的哺乳动物施用治疗有效剂量的下式化合物：其中R 1〜 >是任选取代的C 1-14烷基; Y是C 1-14亚烷基; Z是任选被卤素，羟基，氨基，氰基或任选取代的C 1-4烷基取代的苯基或其药学上可接受的盐，酯或前药。拮抗A 1 N 1腺苷受体以治疗疾病状态，其选自肾衰竭，肾功能障碍，肾炎，高血压，水肿，阿尔茨海默病，压力，抑郁，心律失常，心脏功能恢复，充血性心力衰竭，糖尿病，哮喘，呼吸系统疾病，脑，心脏和肾脏的局部缺血诱导的损伤和腹泻。

6. 发明授权

US08188099B2 Method of decreasing hepatotoxic side effects using A2B adenosine receptor antagonists 有权
标题翻译：使用A2B腺苷受体拮抗剂降低肝毒性副作用的方法
公开(公告)号：US08188099B2
公开(公告)日：2012-05-29
申请号：US12853510
申请日：2010-08-10
申请人： Luiz Belardinelli , Dewan Zeng , Hongyan Zhong
发明人： Luiz Belardinelli , Dewan Zeng , Hongyan Zhong
IPC分类号： A61K31/522
CPC分类号： C07D473/06 , A61K9/0019 , A61K9/0053 , A61K31/522
摘要： The invention is related to a method of decreasing hepatotoxic side effects using an A2B adenosine receptor antagonist and utility in the treatment of liver damage caused by undergoing hepatotoxic treatment, such as chemotherapy or radiation. The invention also relates to pharmaceutical compositions for use in the method.
摘要翻译：本发明涉及一种使用A2B腺苷受体拮抗剂降低肝毒性副作用并用于治疗由肝脏毒性治疗如化疗或放射引起的肝损伤的方法。本发明还涉及用于该方法的药物组合物。

7. 发明授权

US07795268B2 Method of treating hepatic disease using A2B adenosine receptor antagonists 有权
标题翻译：使用A2B腺苷受体拮抗剂治疗肝病的方法
公开(公告)号：US07795268B2
公开(公告)日：2010-09-14
申请号：US11687236
申请日：2007-03-16
申请人： Dewan Zeng , Hongyan Zhong , Luiz Belardinelli
发明人： Dewan Zeng , Hongyan Zhong , Luiz Belardinelli
IPC分类号： A61K31/522
CPC分类号： C07D473/06 , A61K9/0019 , A61K9/0053 , A61K31/522
摘要： The invention is related to methods of treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases.
摘要翻译：本发明涉及使用A2B腺苷受体拮抗剂治疗肝纤维化的方法，并且用于治疗酒精滥用，外科手术，病毒性肝炎，摄入肝毒性药物或其他肝脏疾病引起的肝损伤。

8. 发明申请

US20070219221A1 METHOD OF PREVENTING AND TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS 有权
标题翻译：使用A2B腺苷受体拮抗剂预防和治疗恶性疾病的方法
公开(公告)号：US20070219221A1
公开(公告)日：2007-09-20
申请号：US11687236
申请日：2007-03-16
申请人： Dewan Zeng , Hongyan Zhong , Luiz Belardinelli
发明人： Dewan Zeng , Hongyan Zhong , Luiz Belardinelli
IPC分类号： A61K31/522
CPC分类号： C07D473/06 , A61K9/0019 , A61K9/0053 , A61K31/522
摘要： The invention is related to methods of preventing and treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment and prevention of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases. The invention also relates to pharmaceutical compositions for use in the method.
摘要翻译：本发明涉及使用Aβ2A腺苷受体拮抗剂预防和治疗肝纤维化的方法，并且可用于治疗和预防酒精滥用，手术干预，病毒性肝炎，肝毒性摄入引起的肝损伤药物或其他肝脏疾病。本发明还涉及用于该方法的药物组合物。

9. 发明申请

US20120258974A1 USE OF A2B ADENOSINE RECEPTOR ANTAGONISTS FOR TREATING HEART FAILURE AND ARRHYTHMIA IN POST-MYOCARDIAL INFARCTION PATIENTS 审中-公开
标题翻译：使用A2B腺苷受体拮抗剂治疗心肌梗死患者心脏衰竭和ARRHYTHMIA
公开(公告)号：US20120258974A1
公开(公告)日：2012-10-11
申请号：US13440926
申请日：2012-04-05
申请人： Luiz Belardinelli , Hongyan Zhong , Dewan Zeng
发明人： Luiz Belardinelli , Hongyan Zhong , Dewan Zeng
IPC分类号： A61K31/522 , A61P9/04 , A61P9/00 , A61P9/06
CPC分类号： A61K31/40 , A61K9/0014 , A61K9/0019 , A61K9/0075 , A61K9/02 , A61K9/2054 , A61K9/2059 , A61K9/4866 , A61K31/403 , A61K31/522 , A61K45/06 , A61K47/06 , A61K47/26 , A61K47/38 , A61K47/44 , A61K2300/00
摘要： Provided are methods of improving the cardiac condition of post-myocardial infarction (MI) patients and reducing cardiovascular death and hospitalization due to heart failure or arrhythmias, by administering a therapeutically effective amount of an A2B adenosine receptor antagonist.
摘要翻译：提供了通过施用治疗有效量的A2B腺苷受体拮抗剂来改善心肌梗死后（MI）患者的心脏状况并减少因心力衰竭或心律失常引起的心血管死亡和住院的方法。

10. 发明申请

US20110184002A1 METHOD OF TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS 有权
标题翻译：使用A2B腺苷受体拮抗剂治疗恶性疾病的方法
公开(公告)号：US20110184002A1
公开(公告)日：2011-07-28
申请号：US12853510
申请日：2010-08-10
申请人： Luiz Belardinelli , Dewan Zeng , Hongyan Zhong
发明人： Luiz Belardinelli , Dewan Zeng , Hongyan Zhong
IPC分类号： A61K31/522 , A61P1/16
CPC分类号： C07D473/06 , A61K9/0019 , A61K9/0053 , A61K31/522
摘要： The invention is related to methods of preventing and treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment and prevention of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases. The invention also relates to pharmaceutical compositions for use in the method.
摘要翻译：本发明涉及使用A2B腺苷受体拮抗剂预防和治疗肝纤维化的方法，并且用于治疗和预防酒精滥用，外科手术，病毒性肝炎，摄入肝毒性药物或其他肝脏疾病引起的肝损伤。本发明还涉及用于该方法的药物组合物。

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