公开(公告)号：US4757084A

公开(公告)日：1988-07-12

申请号：US776191

申请日：1985-09-13

申请人： Tesfaye Biftu

发明人： Tesfaye Biftu

IPC分类号： A61K31/38 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4433 ,  A61P11/00 ,  A61P29/00 ,  C07C45/72 ,  C07C45/78 ,  C07D333/00 ,  C07D333/16 ,  C07D333/56 ,  C07D333/62 ,  C07D409/04 ,  C07D333/12

CPC分类号： C07D409/04 ,  C07C45/72 ,  C07C45/78 ,  C07D333/16

摘要： Analogs of 2,5-Diaryl tetrahydrothiophenes which were substituted or unsubstituted on 3,4-positions were prepared.These compounds are found to be leukotriene inhibitors and potent and specific PAF (Platelet Activating Factor) antagonists. They are therefore useful in the treatment of various diseases or disorders mediated by the leukotriene and/or 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位上取代或未取代的2,5-二芳基四氢噻吩的类似物。 发现这些化合物是白三烯抑制剂和有效和特异性的PAF（血小板活化因子）拮抗剂。 因此，它们可用于治疗由白细胞三烯和/或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。

公开(公告)号：US4533671A

公开(公告)日：1985-08-06

申请号：US433603

申请日：1982-10-08

申请人： Tesfaye Biftu ,  Bruce E. Witzel ,  Peter L. Barker

发明人： Tesfaye Biftu ,  Bruce E. Witzel ,  Peter L. Barker

IPC分类号： C07D487/04 ,  C07D207/26 ,  A61K31/40

CPC分类号： C07D487/04

摘要： New 5-(2,3-dihydro-1H-pyrrolizin-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]thiazol-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]imidazol-5-oyl)-, and 5-(2,3-dihydro-1H-pyrrolo[2,1-b]oxazol-5-oyl)-pyrrole-2-alkanoic acid derivatives have been prepared. They are found to be effective inhibitors of platelet aggregation and are analgesic and anti-inflammatory agents with low ulcerogenic side effects.

摘要翻译： 新的5-（2,3-二氢-1H-吡咯烷-5-基） - ，5-（2,3-二氢-1H-吡咯并[2,1-b]噻唑-5-基） - ，5-（ 2,3-二氢-1H-吡咯并[2,1-b]咪唑-5-基） - 和5-（2,3-二氢-1H-吡咯并[2,1-b]恶唑-5-基） - 吡咯-2-链烷酸衍生物。 它们被发现是血小板聚集的有效抑制剂，并且具有低溃疡性副作用的止痛剂和抗炎剂。

公开(公告)号：US20170081287A1

公开(公告)日：2017-03-23

申请号：US15310488

申请日：2015-05-19

申请人： Tesfaye BIFTU ,  Purakkattle BIJU ,  Timothy A. BLIZZARD ,  Zhengxia CHEN ,  Matthew J. CLEMENTS ,  Mingxiang CUI ,  Jessica L. FRIE ,  William K. HAGMANN ,  Bin HU ,  Hubert JOSIEN ,  Anilkumar G. NAIR ,  Christopher W. PLUMMER ,  Cheng ZHU ,  Merck Sharp & Dohme Corp.

发明人： Tesfaye Biftu ,  Purakkattle Biju ,  Timothy A. Blizzard ,  Zhengxia Chen ,  Matthew J. Clements ,  Mingxiang Cui ,  Jessica L. Frie ,  William K. Hagmann ,  Bin Hu ,  Hubert Josien ,  Anilkumar G. Nair ,  Christopher W. Plummer ,  Cheng Zhu

IPC分类号： C07D221/16 ,  A61K31/438 ,  C07D405/12 ,  C07D401/12 ,  A61K31/444 ,  C07C61/39 ,  A61K31/192 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/538 ,  C07D413/12 ,  A61K31/55 ,  C07D215/14 ,  A61K31/47 ,  C07D401/04 ,  A61K45/06

CPC分类号： C07D221/16 ,  A61K31/192 ,  A61K31/366 ,  A61K31/397 ,  A61K31/435 ,  A61K31/438 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4985 ,  A61K31/538 ,  A61K31/55 ,  A61K45/06 ,  C07C61/39 ,  C07C2602/08 ,  C07C2603/12 ,  C07D215/14 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K2300/00

摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US08716482B2

公开(公告)日：2014-05-06

申请号：US13390708

申请日：2010-09-15

申请人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

发明人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

IPC分类号： C07D211/32 ,  A61K31/00

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The present invention is directed to novel substituted aminopiperidines 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-ÏV 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的新型取代氨基哌啶，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-κV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。

公开(公告)号：US08415297B2

公开(公告)日：2013-04-09

申请号：US13398887

申请日：2012-02-17

申请人： Tesfaye Biftu ,  Ann E. Weber

发明人： Tesfaye Biftu ,  Ann E. Weber

IPC分类号： A61K31/4162 ,  A61K38/28 ,  C07D487/04 ,  A61P3/10

CPC分类号： C07D309/30 ,  A61K9/2054 ,  A61K31/4162 ,  A61K38/1709 ,  A61K38/26 ,  A61K45/06 ,  C07D487/04

摘要： The present invention is directed to novel substituted aminotetrahydropyrans 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.

公开(公告)号：US20120149683A1

公开(公告)日：2012-06-14

申请号：US13390708

申请日：2010-09-15

申请人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

发明人： Jason M. Cox ,  Tesfaye Biftu ,  Hong Dong Chu ,  Danqing Feng ,  Ann E. Weber

IPC分类号： A61K31/454 ,  C07D401/12 ,  A61K31/497 ,  C07D401/06 ,  A61P3/10 ,  C07D487/04 ,  A61K31/4985 ,  C07D413/06 ,  A61K31/5377 ,  C07D211/56 ,  A61K31/4545

CPC分类号： C07D487/04 ,  C07D519/00

摘要： The present invention is directed to novel substituted aminopiperidines 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-ÏV 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的新型取代氨基哌啶，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-κV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。

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

公开(公告)号：US5780503A

公开(公告)日：1998-07-14

申请号：US474444

申请日：1995-06-07

申请人： Tesfaye Biftu ,  Ralph Scannell ,  Xiong Cai ,  Sajjat Hussoin

发明人： Tesfaye Biftu ,  Ralph Scannell ,  Xiong Cai ,  Sajjat Hussoin

IPC分类号： C07D307/14 ,  C07D471/04 ,  A61K31/34 ,  A61K31/38 ,  A61K31/44 ,  A61K31/47

CPC分类号： C07D471/04 ,  C07D307/14

摘要： Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

公开(公告)号：US4536512A

公开(公告)日：1985-08-20

申请号：US433339

申请日：1982-10-08

申请人： Tesfaye Biftu ,  Bruce E. Witzel ,  Peter L. Barker

发明人： Tesfaye Biftu ,  Bruce E. Witzel ,  Peter L. Barker

IPC分类号： C07D487/04 ,  C07D513/04 ,  C07D519/00 ,  A61K31/40 ,  C07D487/06

CPC分类号： C07D487/04 ,  C07D513/04

摘要： New 5-(2,3-dihydro-1H-pyrrolizin-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]thiazol-5-oyl)-, 5-(2,3-dihydro-1H-pyrrolo[2,1-b]imidazol-5-oyl)-, and 5-(2,3-dihydro-1H-pyrrolo[2,1-b]oxazol-5-oyl)-derivatives of substituted 2,3-dihydro-1H-pyrrolizine-1-alkanoic or carboxylic acids have been prepared. They are found to be effective inhibitors of platelet aggregation and are analgesic/anti-inflammatory agents with low ulcerogenic side effects.

摘要翻译： 新的5-（2,3-二氢-1H-吡咯烷-5-基） - ，5-（2,3-二氢-1H-吡咯并[2,1-b]噻唑-5-基） - ，5-（ 2,3-二氢-1H-吡咯并[2,1-b]咪唑-5-基） - 和5-（2,3-二氢-1H-吡咯并[2,1-b]恶唑-5-基） 已经制备了取代的2,3-二氢-1H-吡咯嗪-1-烷酸或羧酸的衍生物。 它们被发现是血小板聚集的有效抑制剂，并且具有低溃疡性副作用的镇痛/抗炎剂。

公开(公告)号：USD1022708S1

公开(公告)日：2024-04-16

申请号：US29903104

申请日：2023-09-20

申请人： Tesfaye Biftu

设计人： Tesfaye Biftu

摘要： FIG. 1 is a front view of a bottle showing my new design;
FIG. 2 is a left elevational view thereof;
FIG. 3 is a right elevational view thereof;
FIG. 4 is a rear elevational view thereof;
FIG. 5 is a top plan view thereof;
FIG. 6 is a bottom plan view thereof;
FIG. 7 is a front-top-right elevational view thereof;
FIG. 8 is a bottom-rear elevational view thereof;
FIG. 9 is a top-rear elevational view thereof; and,
FIG. 10 is bottom-front-right elevational view thereof.
The broken lines shown illustrate portions of the bottle and form no part of the claimed design.