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1. 发明公开

EP1549613A1 SULFONAMIDES HAVING ANTIANGIOGENIC AND ANTICANCER ACTIVITY 审中-公开
标题翻译：抗生素杀虫剂抗生素
公开(公告)号：EP1549613A1
公开(公告)日：2005-07-06
申请号：EP03773182.5
申请日：2003-10-06
申请人： Abbott Laboratories
发明人： COMESS, Kenneth, M. , ERICKSON, Scott, A. , HENKIN, Jack , KALVIN, Douglas, M. , KAWAI, Megumi , KIM, Ki, H. , BAMAUNG, Nwe, Y. , PARK, Chan, Hoon , SHEPPARD, George, S. , VASUDEVAN, Anil , WANG, Jieyi , BARNES, David, M. , FIDANZE, Steve, D. , KOLACZKOWSKI, Lawrence , MANTEI, Robert, A. , PARK, David, C. , SANDERS, William, J. , TEDROW, Jason, S. , WANG, Gary, T.
IPC分类号： C07C311/08
CPC分类号： C07C323/25 , C07C311/08 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/37 , C07C311/44 , C07C311/46 , C07C317/28 , C07C323/49 , C07C323/63 , C07C323/67 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D209/08 , C07D209/42 , C07D213/70 , C07D213/71 , C07D215/36 , C07D215/48 , C07D231/18 , C07D233/54 , C07D233/84 , C07D261/10 , C07D285/06 , C07D285/14 , C07D333/34 , C07D333/38 , C07D413/04
摘要： Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.
摘要翻译：描述了具有甲硫氨酸氨基肽酶-2抑制剂（MetAP2）的化合物。还描述了包含该化合物的药物组合物，使用该化合物的治疗方法，抑制血管发生的方法和治疗癌症的方法。

2. 发明公开

EP1114022A1 PROCESS FOR PRODUCING STEREOSELECTIVE NITRO COMPOUNDS 审中-公开
标题翻译：用于生产STEREO选择性硝基化合物
公开(公告)号：EP1114022A1
公开(公告)日：2001-07-11
申请号：EP99946886.1
申请日：1999-09-13
申请人： ABBOTT LABORATORIES
发明人： JI, Jianguo , BARNES, David, M. , KING, Steven, A. , PLAGGE, Frederick, A. , WITTENBERGER, Steven, J. , ZHANG, Ji
IPC分类号： C07C201/12 , C07D317/64 , C07D405/04 , C07D263/52 , C07C251/18
CPC分类号： C07D317/64 , C07D405/04
摘要： The present invention relates to producing stereoselective nitro compounds by reacting a dicarbonyl compound with a nitrostyrene compound in the presence of a catalyst complex and a base.

3. 发明公开

EP2203431A1 ANTI-INFECTIVE PYRIMIDINES AND USES THEREOF 有权转让
标题翻译：抗感染性嘧啶类及其应用
公开(公告)号：EP2203431A1
公开(公告)日：2010-07-07
申请号：EP08832330.8
申请日：2008-09-17
申请人： Abbott Laboratories
发明人： FLENTGE, Charles, A. , HUTCHINSON, Douglas, K. , BETEBENNER, David, A. , DEGOEY, David, A. , DONNER, Pamela, L. , KATI, Warren, M. , KRUEGER, Allan, C. , LIU, Dachun , LIU, Yaya , LONGENECKER, Kenton, L. , MARING, Clarence, J. , MOTTER, Christopher, E. , PRATT, John, K. , RANDOLPH, John, T. , ROCKWAY, Todd, W. , STEWART, Kent, D. , WAGNER, Rolf , BARNES, David, M. , CHEN, Shuang , FRANCZYK, Thaddeus, S., II , GAO, Yi , HAIGHT, Anthony, R. , HENGEVELD, John, E. , KOTECKI, Brian, J. , LOU, Xiaochun , ZHANG, Geoff, G., Z.
IPC分类号： C07D239/22 , C07D239/54 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K31/513 , A61P31/12
CPC分类号： C07D239/54 , A61K31/513 , A61K45/06 , C07D239/22 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K2300/00
摘要： This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

4. 发明公开

EP1802607A2 SALT AND CRYSTALLINE FORMS THEREOF OF A DRUG 审中-公开
标题翻译： SALZ UND KRISTALLINFORMEN DARAUS EINES MEDIKAMENTS
公开(公告)号：EP1802607A2
公开(公告)日：2007-07-04
申请号：EP05825344.4
申请日：2005-10-09
申请人： ABBOTT LABORATORIES
发明人： ZHANG, Geoff, G. , BRADLEY, Michael, F. , BARNES, David, M. , HENRY, Rodger
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , A61K31/4709 , A61K47/02 , A61K47/12 , C07C31/26
摘要： A crystalline form of D-Glucitol, 1-deoxy-1-(methylamino)-, 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7 -(3-hydroxyazetidin-1-yl)-4-oxo-3-quinolinecarboxylate (salt) as anitbacterial drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
摘要翻译： D-葡萄糖醇，1-脱氧-1-（甲基氨基） - ，1-（6-氨基-3,5-二氟吡啶-2-基）-8-氯-6-氟-1,4-二氢 -7-（3-羟基氮杂环丁烷-1-基）-4-氧代-3-喹啉羧酸酯（盐）作为副细菌药物，制备方法，含有它的组合物和治疗疾病的方法以及使用它们抑制不良生理事件的方法是披露。

5. 发明授权

EP2203431B1 ANTI-INFECTIVE PYRIMIDINES AND USES THEREOF 有权转让
标题翻译：抗感染性嘧啶类及其应用
公开(公告)号：EP2203431B1
公开(公告)日：2011-08-10
申请号：EP08832330.8
申请日：2008-09-17
申请人： Abbott Laboratories
发明人： FLENTGE, Charles, A. , HUTCHINSON, Douglas, K. , BETEBENNER, David, A. , DEGOEY, David, A. , DONNER, Pamela, L. , KATI, Warren, M. , KRUEGER, Allan, C. , LIU, Dachun , LIU, Yaya , LONGENECKER, Kenton, L. , MARING, Clarence, J. , MOTTER, Christopher, E. , PRATT, John, K. , RANDOLPH, John, T. , ROCKWAY, Todd, W. , STEWART, Kent, D. , WAGNER, Rolf , BARNES, David, M. , CHEN, Shuang , FRANCZYK, Thaddeus, S., II , GAO, Yi , HAIGHT, Anthony, R. , HENGEVELD, John, E. , KOTECKI, Brian, J. , LOU, Xiaochun , ZHANG, Geoff, G., Z.
IPC分类号： C07D239/22 , C07D239/54 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K31/513 , A61P31/12
CPC分类号： C07D239/54 , A61K31/513 , A61K45/06 , C07D239/22 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10 , A61K2300/00
摘要： This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.

6. 发明公开

EP2001885A2 OCTAHYDRO-PYRROLO[3,4-B]PYRROLE DERIVATIVES 审中-公开
标题翻译：十八烷基吡咯并[3,4-B]吡咯衍生物
公开(公告)号：EP2001885A2
公开(公告)日：2008-12-17
申请号：EP07757130.5
申请日：2007-02-16
申请人： ABBOTT LABORATORIES
发明人： COWART, Marlon, D. , ZHAO, Chen , SUN, Minghua , BLACK, Lawrence, A. , ZHENG, Guo Zhu , GREGG, Robert, J. , ZHANG, Geoff, G.Z. , SHEIKH, Ahmad, Y. , LOU, Xiaochun , HENRY, Rodger, F. , BARNES, David, M. , KOLACZKOWSKI, Lawrence , HAIGHT, Anthony, R. , CHANG, Sou-Jen , WITTENBERGER, Steven, J. , FICKES, Michael, G.
IPC分类号： C07D487/04 , A61K31/407
CPC分类号： C07D487/04
摘要： Octahydro-pyrrolo[3,4-b]pyrrole derivatives or a pharmaceutically acceptable salt, ester, amide, prodrug, or radiolabeled form thereof, wherein R1 is alkyl, C3-C5 cycloalkyl. or (C3-C5 cycloalkyl)methyl; R2a, R2b, R2c, R2d, R2e, and R2f each are independently hydrogen, methyl, or fluoromethyl; R3a, R3b, R3c, and R3d each are independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile, with the proviso that when one or more of R3a, R3b, R3c, and R3d are alkyl, then at least one of R3a, R3b, R3c, and R3d is fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile; L1 is a bond, oxygen, sulfur, carbonyl, alkylene,. alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR4, -C(=O) NR4-, or -NR4C(=O)-; R4 is hydrogen or alkyl; Cy1 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; Z is a substituent R6 or a group represented by -L3-Cy3; R6 is hydrogen, acyl, acyloxy, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxyimino, alkoxysulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, alkynyl, amido, carboxy, cyano, cycloalkyl, fiuoroalkoxy, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, mercapto, nitro, alkylthio, amino, NHR7, NR7R8, -N(R7)C(=O)R9, -C(=O)NR7R8, or N(R7)SO2(R10); L3 is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR11, -C(=O) NR11-, or -NR11C(=O)-;Cy3 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; R7, R8, R9, R10, and R11 at each occurrence are independently hydrogen,C1-4 alkyl, C3-C4 cycloalkyl, or a (C3-C4 cycloalkyl)amine; are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.
摘要翻译：八氢 - 吡咯并[3,4-b]吡咯衍生物或其药学上可接受的盐，酯，酰胺，前药或放射性标记的形式，其中R 1为C 3 -C 5环烷基。或（C 3 -C 5环烷基）甲基; R2a，R2b，R2c，R2d，R2e和R2f各自独立地为氢，甲基或氟甲基; R3a，R3b，R3c和R3d各自独立地为氢，烷基，氟代烷基，氟代烷氧基，烷氧基，硫代烷氧基，卤素或腈，条件是当R3a，R3b，R3c和R3d中的一个或多个为烷基时， R 3a，R 3b，R 3c和R 3d中的至少一个是氟烷基，氟烷氧基，烷氧基，硫代烷氧基，卤素或腈; L1是一个键，氧，硫，羰基，亚烷基。（= N-O烷基） - ，NR 4，-C（= O）NR 4 - 或-NR 4 C（= O） - ; R4是氢或烷基; Cy1是芳基，环烷基，环烯基，杂芳基或杂环; Z是取代基R6或由-L3-Cy3表示的基团; 烷基羰基，烷基磺酰基，炔基，酰氨基，羧基，氰基，环烷基，氟代烷氧基，卤代烷氧基，卤代烷基，卤素，羟基，羟基烷基，烷基氨基，巯基，硝基，烷硫基，氨基，NHR7，NR7R8，-N（R7）C（= O）R9，-C（= O）NR7R8或N（R7）SO2（R10）。 L3是键，氧，硫，羰基，亚烷基，烷基羰基，烷基氨基，-C（= N-O烷基） - ，NR 11，-C（= O）NR 11 - 或-NR 11 C（= O） - ; Cy 3是芳基，环烷基，环烯基，杂芳基或杂环; R7，R8，R9，R10和R11各自独立地为氢，C1-4烷基，C3-C4环烷基或（C3-C4环烷基）胺; 可用于治疗由组胺-3受体配体阻止或改善的病症或障碍。本文公开了八氢 - 吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物以及制备这些化合物的方法。

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