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61. 发明授权

US07101871B2 Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes 有权
公开(公告)号：US07101871B2
公开(公告)日：2006-09-05
申请号：US10501059
申请日：2003-10-14
申请人： Tesfaye Biftu , Gui-Bai Liang , Xiaoxia Qian , Ann E. Weber , Danqing Dennis Feng
发明人： Tesfaye Biftu , Gui-Bai Liang , Xiaoxia Qian , Ann E. Weber , Danqing Dennis Feng
IPC分类号： C07D243/08 , A61K31/551 , A61P3/10
CPC分类号： C07D243/08 , C07D401/06 , C07D403/06 , C07K5/06191
摘要： The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) 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.

62. 发明授权

US06291480B1 Diaryl piperidyl pyrrole derivatives as antiprotozoal agents 有权
标题翻译：二芳基哌啶基吡咯衍生物作为抗原虫剂
公开(公告)号：US06291480B1
公开(公告)日：2001-09-18
申请号：US09710147
申请日：2000-11-10
申请人： Tesfaye Biftu , Danqing Dennis Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Michael H. Fisher , Matthew J. Wyvratt
发明人： Tesfaye Biftu , Danqing Dennis Feng , Gui-Bai Liang , Mitree M. Ponpipom , Xiaoxia Qian , Michael H. Fisher , Matthew J. Wyvratt
IPC分类号： C07D40104
CPC分类号： C07D401/14 , A23K20/116 , A23K50/75 , A61K45/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
摘要翻译：三取代吡咯是可用于治疗和预防人类和动物中的原生动物疾病的抗原虫剂，包括控制家禽中的球虫病。

63. 发明授权

US5114961A 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
标题翻译： 2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US5114961A
公开(公告)日：1992-05-19
申请号：US624449
申请日：1990-12-10
申请人： Tesfaye Biftu , Robert L. Bugianesi , Nirindar N. Girotra , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
发明人： Tesfaye Biftu , Robert L. Bugianesi , Nirindar N. Girotra , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
IPC分类号： C07D307/12 , C07D405/12 , C07D417/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D307/12 , C07D405/12 , C07D417/12
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3, 4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.
摘要翻译：本发明涉及具体取代的式（I）的四氢呋喃，其中R 4是烷硫基，烷基亚磺酰基或烷基磺酰基基团，并且在3,4或5位上的至少一个取代基含有杂环，杂芳基或取代的苯硫基部分。

64. 发明授权

US5011847A 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
标题翻译： 2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US5011847A
公开(公告)日：1991-04-30
申请号：US362909
申请日：1989-06-08
申请人： Tesfaye Biftu , Mitree M. Ponpipom , Nirindar N. Girotra
发明人： Tesfaye Biftu , Mitree M. Ponpipom , Nirindar N. Girotra
IPC分类号： A61K31/44 , A61K31/443 , A61K31/495 , A61P1/04 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , C07D405/04 , C07F9/6558
CPC分类号： C07D405/04 , C07F9/65586
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein Ar is a pyridyl, dimethoxy-pyridyl or a dimethoxy-pyrazinyl group, R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group, R.sup.6 is an alkyl or a substituted alkyl and the substituents at positions 3, 4 and 5 are acyclic.

65. 发明授权

US5010100A Certain 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
标题翻译：某些2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US5010100A
公开(公告)日：1991-04-23
申请号：US362919
申请日：1989-06-08
申请人： Tesfaye Biftu , John C. Chabala , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo
发明人： Tesfaye Biftu , John C. Chabala , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo
IPC分类号： C07C45/00 , C07C45/72 , C07D307/12 , C07D307/14 , C07D307/16 , C07D307/18 , C07D307/20 , C07D307/24 , C07D307/34 , C07D307/42 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/14 , C07D417/04
CPC分类号： C07D307/18 , C07C45/00 , C07C45/72 , C07D307/12 , C07D307/14 , C07D307/16 , C07D307/20 , C07D307/24 , C07D307/34 , C07D307/42 , C07D405/04 , C07D405/14 , C07D407/12 , C07D409/14 , C07D417/04
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group, Y is an alkyl or substituted alkyl group and R.sup.6 is an alkoxy or a substituted alkoxy or alkyl group.
摘要翻译：本发明涉及式（I）的具体取代的四氢呋喃其中R 4是烷硫基，烷基亚磺酰基或烷基磺酰基，Y是烷基或取代的烷基，R 6是烷氧基或取代的烷氧基或烷基。

66. 发明授权

US5001123A 2,5-diaryl tetrahydrofurans and analogs thereof as PAF antagonists 失效
公开(公告)号：US5001123A
公开(公告)日：1991-03-19
申请号：US362907
申请日：1989-06-08
申请人： Tesfaye Biftu , Nirindar N. Girotra , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
发明人： Tesfaye Biftu , Nirindar N. Girotra , Robert L. Bugianesi , Mitree M. Ponpipom , Soumya P. Sahoo , Chan H. Kuo
IPC分类号： A61K31/44 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/54 , A61P3/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P37/08 , C07D405/04 , C07D405/14 , C07D417/14 , C07D521/00 , C07F9/6558
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D405/04 , C07D405/14 , C07F9/65586
摘要： The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein Ar is a pyridyl, a dimethoxy-pyridyl or dimethoxy-pyrazyl group, R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio group.

67. 发明授权

US4539332A 2,5-Diaryl tetrahydrofurans and analogs thereof as PAF-antagonists 失效
标题翻译： 2,5-二芳基四氢呋喃及其类似物作为PAF拮抗剂
公开(公告)号：US4539332A
公开(公告)日：1985-09-03
申请号：US551666
申请日：1983-11-14
申请人： Tesfaye Biftu , San-Bao Hwang , Thomas W. Doebber , Thomas R. Beattie , Tsung-Ying Shen
发明人： Tesfaye Biftu , San-Bao Hwang , Thomas W. Doebber , Thomas R. Beattie , Tsung-Ying Shen
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。

68. 发明授权

US10442819B2 Tricyclic compounds as inhibitors of mutant IDH enzymes 有权
公开(公告)号：US10442819B2
公开(公告)日：2019-10-15
申请号：US15532549
申请日：2015-12-01
申请人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
发明人： Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
IPC分类号： A61K31/351 , A61K31/4353 , A61K31/5355 , A61K31/551 , C07D471/04 , C07D471/14 , C07D498/08 , C07D471/08 , C07D498/04 , C07D498/10 , A01N43/00
摘要： The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.

69. 发明申请

US20150315141A1 Thrombin Inhibitors 有权
标题翻译：凝血酶抑制剂
公开(公告)号：US20150315141A1
公开(公告)日：2015-11-05
申请号：US14443470
申请日：2013-11-15
申请人： Harry CHOBANIAN , Tesfaye BIFTU , Barbara PIO , Zhicai WU , MERCK SHARP & DOHME CORP.
发明人： Harry Chobanian , Tesfaye Biftu , Barbara Pio , Zhicai Wu
IPC分类号： C07D207/16 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D207/34 , C07D401/06
CPC分类号： C07D207/16 , C07D207/34 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06
摘要： Compounds of the invention, which may be useful in inhibiting thrombin and associated thrombotic occlusions, have the following structure: or a pharmaceutically acceptable salt thereof, wherein m is 0 or 1; R is a heterocycle, —(CR8R9)1-2NH2, or —(CR8R9)1-2OH, wherein R8 and R9, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; W is a) —CHR1R2, where R1 is —C(CH3)3, and R2 is —(CH2)1-2OH, b) a 5- or 6-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N and O, wherein substituted heterocycle is substituted with R3, c) a 9- or 10-membered unsubstituted or substituted heterocycle having 1 or 2 heteroatoms selected from N, O and S, wherein substituted heterocycle is mono-substituted with R3, or disubstituted with R3 and R4, or d) a 3-, 4-, or 5-membered carbocyclic ring which is unsubstituted, mono-substituted with R3, di-substituted with R3 and R4, or tri-substituted with R3, R4 and R5; R3 is —CF3, —COOH, —COOR7, —C(O)R6, —CH(OH)R6, —CH2R6, R6, =O, halogen, R7, —OH, —NH2, or —NHSO2R7; and R10 is H or C1-6 alkyl.
摘要翻译：可用于抑制凝血酶和相关血栓闭塞的本发明化合物具有以下结构：或其药学上可接受的盐，其中m为0或1; R是杂环， - （CR 8 R 9）1-2 NH 2或 - （CR 8 R 9）1-2 OH，其中R 8和R 9各自独立地为H，C 1-6烷基，-CH 2 F，-CHF 2，CF 3 或-CH 2 OH; W是a）-CHR 1 R 2，其中R 1是-C（CH 3）3，并且R 2是 - （CH 2）1-2 OH，b）具有1或2个选自N的杂原子的5或6元未取代或取代的杂环， O，其中取代的杂环被R 3取代，c）具有1或2个选自N，O和S的杂原子的9或10元未取代或取代的杂环，其中取代的杂环被R 3单取代或被R 3二取代和R 4，或d）未被取代的，被R 3和R 4二取代或被R3，R4和R5三取代的R3单取代的3-，4-或5-元碳环; R3是-CF3，-COOH，-COOR7，-C（O）R6，-CH（OH）R6，-CH2R6，R6，= O，卤素，R7，-OH，-NH2或-NHSO2R7; R 10为H或C 1-6烷基。

70. 发明授权

US08895603B2 Crystalline forms of a dipeptidyl peptidase-IV inhibitor 有权
标题翻译：二肽基肽酶-IV抑制剂的结晶形式
公开(公告)号：US08895603B2
公开(公告)日：2014-11-25
申请号：US14118998
申请日：2012-06-25
申请人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
发明人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
IPC分类号： A61K31/4162 , C07D231/00 , C07D487/04 , A61K31/4439 , A61K31/4985 , A61K31/513
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
摘要： Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
摘要翻译：（2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。

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