公开(公告)号：EP2424849A1

公开(公告)日：2012-03-07

申请号：EP10717392.4

申请日：2010-04-30

申请人： Abbott Laboratories

发明人： BORCHARDT, Thomas ,  BRACKEMYER, Paul ,  CATRON, Nathaniel ,  HENRY, Rodger ,  LOU, Xiaochun ,  RAVN, Matthew ,  ZHANG, Geoff ,  ZHOU, Deliang

IPC分类号： C07D295/155 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D295/155

摘要： ABT-263 bis-HCl and crystalline polymorphs thereof are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

公开(公告)号：EP1745053A1

公开(公告)日：2007-01-24

申请号：EP05724824.7

申请日：2005-03-07

申请人： ABBOTT LABORATORIES

发明人： LAW, Devalina ,  HENRY, Rodger, F. ,  LOU, Xiaochun

IPC分类号： C07D501/22 ,  A61K31/546 ,  A61P31/04

CPC分类号： G01N1/30 ,  C07D501/00 ,  G01N2001/302

摘要： The present invention relates to trihemihydrate, novel lower hydrate and anhydrate forms of 7-[2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamide]-3-vinyl-3-cephem-4-carboxylic acid (syn isomer), methods for their preparation, and pharmaceutical compositions comprising these forms.

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.

公开(公告)号：EP2203430B1

公开(公告)日：2011-06-15

申请号：EP08831558.5

申请日：2008-09-17

申请人： Abbott Laboratories

发明人： DONNER, Pamela L. ,  RANDOLPH, John T. ,  KRUEGER, Allan C. ,  BETEBENNER, David A. ,  HUTCHINSON, Douglas K. ,  LIU, Dachun ,  LIU, Yaya ,  LONGENECKER, Kenton L. ,  MARING, Clarence J. ,  PRATT, John K. ,  ROCKWAY, Todd W. ,  STEWART, Kent D. ,  WAGNER, Rolf ,  BARNES, David M. ,  CHEN, Shuang ,  FRANCZYK II, Thaddeus S. ,  GAO, Yi ,  HAIGHT, Anthony R. ,  HENGEVELD, John E. ,  HENRY, Rodger F. ,  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 ,  C07D239/553 ,  A61K31/513 ,  A61K31/506 ,  A61P31/14

CPC分类号： C07D239/22 ,  A61K31/513 ,  C07D239/54 ,  C07D239/553 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10

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. The compounds are usefull in the treatment of hepatitis C and are of the following general structure: Formula (I)

公开(公告)号：EP2222646A1

公开(公告)日：2010-09-01

申请号：EP08831873.8

申请日：2008-09-17

申请人： Abbott Laboratories

发明人： WAGNER, Rolf ,  TUFANO, Michael D. ,  STEWART, Kent D. ,  ROCKWAY, Todd W. ,  RANDOLPH, John T. ,  PRATT, John K. ,  MOTTER, Christopher E. ,  MARING, Clarence J. ,  LONGENECKER, Kenton L. ,  LIU, Yaya ,  LIU, Dachun ,  KRUEGER, Allan C. ,  KATI, Warren M. ,  HUTCHINSON, Douglas K. ,  HUANG, Peggy P. ,  FLENTGE, Charles A. ,  DONNER,Pamela L. ,  DEGOEY, David A. ,  BETEBENNER, David A. ,  BARNES, David M. ,  CHEN, Shuang ,  FRANCZYK II, Thaddeus S. ,  GAO, Yi ,  HAIGHT, Anthony R. ,  HENGEVELD, John E. ,  HENRY, Rodger F. ,  KOTECKI, Brian J. ,  LOU, Xiaochun ,  SARRIS, Kathy ,  ZHANG, Geoff G. Z.

IPC分类号： C07D239/22 ,  C07D239/54 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  A61P31/12 ,  A61K31/513

CPC分类号： A61K31/513 ,  A61K31/5377 ,  C07D239/22 ,  C07D239/54 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  C07D417/14

摘要： Present application relates to the compounds of formula I useful to treat hepatitis C (HCV) infections. In the structure of the disclosed compounds is the uracil or thymine derivative linked via a phenylene into either fused 2-ring cyclic system (R6) or alternatively via additional two-atom linker (L) to a 5-6 membered monocycle (R6). Application further discloses polymorphs and pseudopolymorphs of two specific compounds: N-(6(3-t-butyl-5-(2>4-dioxo-3,4-dihydropyrimidin-1 (2H)- y!)2-methoxy-phenyl)naphthalen-2-yl)methanesulfonamide and (E)-N-(4(3-t- butyl-5-(2,4-dioxo-3)4-dihydropyrimidin-1 (2H)-yl)2-methoxy-styryl- phenyl)methanesulfonamide.

公开(公告)号：EP2203430A1

公开(公告)日：2010-07-07

申请号：EP08831558.5

申请日：2008-09-17

申请人： Abbott Laboratories

发明人： DONNER, Pamela L. ,  RANDOLPH, John T. ,  KRUEGER, Allan C. ,  BETEBENNER, David A. ,  HUTCHINSON, Douglas K. ,  LIU, Dachun ,  LIU, Yaya ,  LONGENECKER, Kenton L. ,  MARING, Clarence J. ,  PRATT, John K. ,  ROCKWAY, Todd W. ,  STEWART, Kent D. ,  WAGNER, Rolf ,  BARNES, David M. ,  CHEN, Shuang ,  FRANCZYK II, Thaddeus S. ,  GAO, Yi ,  HAIGHT, Anthony R. ,  HENGEVELD, John E. ,  HENRY, Rodger F. ,  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 ,  C07D239/553 ,  A61K31/513 ,  A61K31/506 ,  A61P31/14

CPC分类号： C07D239/22 ,  A61K31/513 ,  C07D239/54 ,  C07D239/553 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10

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. The compounds are usefull in the treatment of hepatitis C and are of the following general structure: Formula (I)

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.

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。