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1.发明授权
公开(公告)号：US4539332A
公开(公告)日：1985-09-03
申请号：US551666
申请日：1983-11-14
IPC分类号： C07D307/06 , A61K31/34 , A61K31/341 , A61P43/00 , C07C45/00 , C07C45/72 , C07D307/10 , C07D307/12 , C07D307/14 , C07D307/18 , C07D307/20
CPC分类号： C07D307/18 , C07C45/00 , C07C45/72 , C07D307/12 , C07D307/14 , C07D307/20
摘要： Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.
摘要翻译： 制备在3,4位取代或未取代的2,5-二芳基四氢呋喃的类似物。 发现这些化合物具有有效和特异性的PAF（血小板活化因子）拮抗活性，从而可用于治疗由PAF介导的各种疾病或病症，例如炎症，心血管疾病，哮喘，肺水肿，成人呼吸窘迫综合征 ，疼痛和血小板聚集。
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2.发明授权Method of use of 2,5-diaryl tetrahydrofurans and analogs thereof as PAF-antagonists 失效使用2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂的方法
公开(公告)号：US4595693A
公开(公告)日：1986-06-17
申请号：US617294
申请日：1984-06-04
申请人： Tesfaye Biftu , Thomas W. Doebber , San-Bao Hwang , Thomas R. Beattie , Tsung-Ying Shen , Robert Stevenson
发明人： Tesfaye Biftu , Thomas W. Doebber , San-Bao Hwang , Thomas R. Beattie , Tsung-Ying Shen , Robert Stevenson
IPC分类号： A61K31/34 , C07D307/12
CPC分类号： A61K31/34 , C07D307/12
摘要： Analogs of 2,5-Diaryl tetrahydrofurans which were substituted or unsubstituted at 3,4-positions were prepared.These compounds are found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by the PAF, for example, inflammation, cardiovascular disorder, asthma, lung edema, adult respiratory distress syndrome, pain, and aggregation of platelets.
摘要翻译： 制备在3,4位取代或未取代的2,5-二芳基四氢呋喃的类似物。 发现这些化合物具有有效和特异性的PAF（血小板活化因子）拮抗活性，从而可用于治疗由PAF介导的各种疾病或病症，例如炎症，心血管疾病，哮喘，肺水肿，成人呼吸窘迫综合征 ，疼痛和血小板聚集。
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3.发明授权Epibatidine and derivatives thereof as cholinergic receptor agonists and antagonists 失效作为胆碱能受体激动剂和拮抗剂，表鬼巴菌素及其衍生物
公开(公告)号：US6077846A
公开(公告)日：2000-06-20
申请号：US612964
申请日：1996-12-17
申请人： Changgeng Qian , Tongchuan Li , Tesfaye Biftu , Tsung-Ying Shen
发明人： Changgeng Qian , Tongchuan Li , Tesfaye Biftu , Tsung-Ying Shen
IPC分类号： C07D487/08 , A61K31/44 , A61K31/4439 , A61K31/465 , A61P1/04 , A61P3/04 , A61P21/00 , A61P25/00
CPC分类号： A61K31/465 , A61K31/44 , A61K31/4439
摘要： This invention relates to the treatment of conditions that can be treated with a nicotinic agonist by administering to a patient an effective amount of a 7-azabicyclo[2.2.1]-heptane or heptene. Specific conditions that may be treated include excess body weight, ulcerative colitis, aplthous ulcer, smoking, Parkinson's Disease, Alzeimer's Disease, and Tourette's Syndrome
摘要翻译： PCT No.PCT / US94 / 10121 Sec。 371日期：1996年12月17日 102（e）日期1996年12月17日PCT 1994年9月9日PCT PCT。 公开号WO95 / 07078 日期1995年3月16日本发明涉及通过向患者施用有效量的7-氮杂双环[2.2.1] - 庚烷或庚烯来治疗可用烟碱激动剂治疗的病症。 可以治疗的具体情况包括体重过多，溃疡性结肠炎，溃疡，吸烟，帕金森病，阿尔茨海默病和图雷特综合征
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4.发明授权Epibatidine and derivatives thereof as nicotine cholinergic receptor agonists 失效作为尼古丁胆碱能受体激动剂的表鬼酸及其衍生物公开(公告)号：US06177451B1
公开(公告)日：2001-01-23
申请号：US08476611
申请日：1995-06-07
申请人： Changgeng Qian , Tongchuan Li , Tesfaye Biftu , Tsung-Ying Shen
发明人： Changgeng Qian , Tongchuan Li , Tesfaye Biftu , Tsung-Ying Shen
IPC分类号： A61K3144
CPC分类号： A61K31/465 , A61K31/44 , A61K31/4439
摘要： The present invention provides methods of treatment utilizing pharmaceutical compositions comprising an effective nicotine agonist amount of epibatidine (1) or a synthetic 7-azabicyclo[2.2.1]-heptane or heptene derivative thereof, and a pharmaceutically acceptable earner, excipient or diluent.
摘要翻译： 本发明提供使用包含有效尼古丁激动剂量的表阿巴定（1）或其合成7-氮杂双环[2.2.1] - 庚烷或庚烯衍生物的药物组合物和药学上可接受的进料器，赋形剂或稀释剂的治疗方法。
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5.发明申请DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES 有权用于治疗或预防糖尿病的胰蛋白酶IV抑制剂公开(公告)号：US20150011590A1
公开(公告)日：2015-01-08
申请号：US14376787
申请日：2013-02-12
发明人： Ann E. Weber , Tesfaye Biftu
IPC分类号： C07D487/04 , A61K31/155 , A61K31/4439 , A61K31/4162
CPC分类号： C07D487/04 , A61K31/155 , A61K31/4162 , A61K31/4439 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式I的新型取代二氢吡咯并吡唑，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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6.发明申请SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES 有权作为用于治疗糖尿病的DIPEPTIDYDEPDDIV-IV抑制剂的取代的七分子杂环化合物公开(公告)号：US20130203786A1
公开(公告)日：2013-08-08
申请号：US13643121
申请日：2011-05-16
IPC分类号： C07D487/04 , A61K31/506 , A61K45/06 , A61K31/519 , A61K31/437 , A61K31/4162 , A61K31/4439
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06 , C07D471/04
摘要： The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译： 本发明涉及结构式（I）的新型氨基取代的七元杂环化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防其中二肽基肽酶-IV酶 涉及糖尿病，特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。
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7.发明申请NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS 有权用作抗糖尿病药物的新型CYABAZABENZIMIDAZOLE衍生物公开(公告)号：US20130123237A1
公开(公告)日：2013-05-16
申请号：US13812536
申请日：2012-02-23
申请人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
发明人： Rajan Anand , James M. Apgar , Tesfaye Biftu , Ping Chen , Lin Chu , Vincent J. Colandrea , Guizhen Dong , James F. Dropinski , Danqing Feng , Jacqueline D. Hicks , Jinlong Jiang , Alexander J. Kim , Kenneth J. Leavitt , Bing Li , Xiaoxia Qian , Iyassu Sebhat , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： A61K31/5377 , A61K31/437 , A61K31/4985 , A61K31/351 , A61K31/397 , A61K31/4412 , C07D471/04 , A61K31/496
CPC分类号： A61K31/5377 , A61K31/351 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/4412 , A61K31/496 , A61K31/4985 , A61K31/519 , A61K45/06 , C07D471/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制由AMPK激活的蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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8.发明授权(Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds 失效（嘧啶基）（苯基）取代的稠合杂芳基p38抑制和PKG激酶抑制化合物公开(公告)号：US07196095B2
公开(公告)日：2007-03-27
申请号：US10477367
申请日：2002-06-21
申请人： Tesfaye Biftu , Richard Beresis , Richard Berger , Steven L. Colletti , James B. Doherty , Dennis D. Feng , Gui-Bai Liang , Dennis M. Schmatz , Xiaoxia Qian , David A. Claremon , Nigel J. Liverton , Charles J. McIntyre , Ernest W. Kovacs
发明人： Tesfaye Biftu , Richard Beresis , Richard Berger , Steven L. Colletti , James B. Doherty , Dennis D. Feng , Gui-Bai Liang , Dennis M. Schmatz , Xiaoxia Qian , David A. Claremon , Nigel J. Liverton , Charles J. McIntyre , Ernest W. Kovacs
IPC分类号： C07D403/04 , C07D403/14 , C07D417/04 , C07D417/14 , A61K31/506 , A61P19/02
CPC分类号： C07D403/04 , A23K20/10 , A23K20/111 , A61K31/429 , A61K31/4355 , A61K31/506 , A61K31/519 , A61K31/53 , A61K45/06 , C07D453/02 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/14 , C07D513/04 , A61K2300/00
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis
摘要翻译： 式（I）化合物及其药学上可接受的盐可用于治疗细胞因子介导的疾病如关节炎和治疗和/或预防原虫感染疾病如球虫病
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公开(公告)号：US20060293303A1
公开(公告)日：2006-12-28
申请号：US10573363
申请日：2004-12-06
申请人： Tesfaye Biftu , Matthew Wyvratt , Michael Fisher
发明人： Tesfaye Biftu , Matthew Wyvratt , Michael Fisher
IPC分类号： A61K31/506 , C07D471/04
CPC分类号： C07D471/04
摘要： Compounds described by the Formula (I) or (II): or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidieal agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria. African typanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
摘要翻译： 由式（I）或（II）表示的化合物：或其药学上可接受的盐或N-氧化物。 该化合物可用于治疗和预防哺乳动物和鸟类中的原生动物疾病。 用于控制家禽中球虫病的方法包括单独施用有效量的化合物，或与一种或多种抗球虫剂组合施用。 用于控制家禽中球虫病的组合物包含单独的化合物，或与一种或多种抗球虫剂组合。 用于治疗和预防哺乳动物原生动物疾病的方法，例如弓形体病，疟疾。 非洲typanosomias，恰加斯病和机会性感染包括单独施用化合物，或与一种或多种抗原虫剂组合施用。
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公开(公告)号：US20060178358A1
公开(公告)日：2006-08-10
申请号：US10548154
申请日：2004-03-02
申请人： Matthew Wyvratt , Tesfaye Biftu , Michael Fisher , Dennis Schmatz
发明人： Matthew Wyvratt , Tesfaye Biftu , Michael Fisher , Dennis Schmatz
IPC分类号： A61K31/506 , C07D471/04
CPC分类号： C07D471/04 , C07D519/00
摘要： Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidial agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
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