公开(公告)号：EP2424499A1

公开(公告)日：2012-03-07

申请号：EP10717961.6

申请日：2010-04-30

申请人： Abbott Laboratories

发明人： CATRON, Nathaniel ,  FICKES, Michael ,  FISCHER, Cristina ,  HAIGHT, Anthony R. ,  HEEMSTRA, Katherine ,  SANZGIRI, Yeshwant ,  SCHMITT, Eric ,  TONG, Ping ,  ZHANG, Geoff ,  ZHOU, Deliang

IPC分类号： A61K9/00 ,  A61K31/5377 ,  A61K47/00 ,  A61K47/02 ,  A61K47/14 ,  A61K47/20 ,  A61K9/48

CPC分类号： A61K31/5377 ,  A61K9/0095 ,  A61K9/08 ,  A61K9/10 ,  A61K9/4858 ,  A61K47/14 ,  A61K47/183 ,  A61K47/24 ,  A61K47/26

摘要： An orally deliverable pharmaceutical composition comprises a Bcl-2 family protein inhibitory compound, e.g., ABT-263, a heavier-chalcogen antioxidant and a substantially non-aqueous lipid carrier, wherein said compound and said antioxidant are in solution in the carrier. The composition is suitable for oral administration to a subject in need thereof for 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：EP1272500B1

公开(公告)日：2005-05-04

申请号：EP00942860.8

申请日：2000-06-15

申请人： Abbott Laboratories

发明人： STONER, Eric J. ,  PETERSON, Matthew J. ,  KU, Yi-Yin ,  CINK, Russell D. ,  COOPER, Arthur J. ,  DESHPANDE, Mahendra N. ,  GRIEME, Tim ,  HAIGHT, Anthony R. ,  HILL, David R. ,  HSU, Margaret, Chi-Ping ,  KING, Steven A. ,  LEANNA, Marvin R. ,  LEE, Elaine C. ,  MCLAUGHLIN, Maureen A. ,  MORTON, Howard E. ,  NAPIER, James J. ,  PLATA, Daniel J. ,  RAJE, Prasad S. ,  RASMUSSEN, Michael ,  RILEY, David ,  TIEN, Jien-Heh J. ,  WITTENBERGER, Steven J.

IPC分类号： C07H17/08 ,  A61K31/70 ,  A61P31/04

CPC分类号： C07H17/08

摘要： In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4'-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

公开(公告)号：EP0674513A1

公开(公告)日：1995-10-04

申请号：EP94905429.0

申请日：1993-12-16

申请人： ABBOTT LABORATORIES

发明人： KEMPF, Dale J. ,  NORBECK, Daniel W. ,  SHAM, Hing Leung ,  ZHAO, Chen ,  SOWIN, Thomas J. ,  RENO, Daniel S. ,  HAIGHT, Anthony R. ,  COOPER, Arthur J.

IPC分类号： C07D ,  C07D275 ,  A61K31 ,  A61K45 ,  A61P31 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07C33 ,  C07C43 ,  C07C45 ,  C07C53 ,  C07C69 ,  C07C211 ,  C07C215 ,  C07C229 ,  C07C233 ,  C07C235 ,  C07C237 ,  C07C239 ,  C07C247 ,  C07C251 ,  C07C271 ,  C07C275 ,  C07C311 ,  C07C317 ,  C07C323 ,  C07C381 ,  C07D213 ,  C07D233 ,  C07D235 ,  C07D239 ,  C07D241 ,  C07D261 ,  C07D263 ,  C07D265 ,  C07D277 ,  C07D295 ,  C07D303 ,  C07D307 ,  C07D333 ,  C07D401 ,  C07D413 ,  C07D417 ,  C07D521 ,  C07F5 ,  C07K5 ,  A61K38

CPC分类号： C07D413/12 ,  A61K31/425 ,  A61K31/427 ,  A61K31/70 ,  A61K38/00 ,  A61K45/06 ,  C07C33/46 ,  C07C43/164 ,  C07C43/1742 ,  C07C43/2055 ,  C07C43/215 ,  C07C43/23 ,  C07C43/30 ,  C07C43/315 ,  C07C45/004 ,  C07C45/29 ,  C07C45/567 ,  C07C45/62 ,  C07C45/673 ,  C07C45/74 ,  C07C53/134 ,  C07C69/34 ,  C07C69/65 ,  C07C69/732 ,  C07C211/27 ,  C07C215/18 ,  C07C215/20 ,  C07C215/28 ,  C07C229/08 ,  C07C229/26 ,  C07C229/34 ,  C07C233/36 ,  C07C233/40 ,  C07C235/10 ,  C07C235/12 ,  C07C235/34 ,  C07C235/78 ,  C07C237/10 ,  C07C237/20 ,  C07C237/22 ,  C07C239/10 ,  C07C239/18 ,  C07C239/20 ,  C07C247/10 ,  C07C251/40 ,  C07C271/20 ,  C07C271/22 ,  C07C271/34 ,  C07C275/16 ,  C07C275/24 ,  C07C311/03 ,  C07C311/13 ,  C07C311/18 ,  C07C317/10 ,  C07C317/28 ,  C07C317/44 ,  C07C323/12 ,  C07C323/25 ,  C07C381/00 ,  C07D213/26 ,  C07D213/30 ,  C07D213/34 ,  C07D213/40 ,  C07D213/54 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D233/84 ,  C07D235/14 ,  C07D235/16 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/34 ,  C07D277/36 ,  C07D277/40 ,  C07D277/42 ,  C07D277/56 ,  C07D295/13 ,  C07D295/205 ,  C07D295/215 ,  C07D303/36 ,  C07D307/42 ,  C07D333/16 ,  C07D401/12 ,  C07D417/12 ,  C07K5/06026 ,  C07K5/06078 ,  A61K31/00 ,  A61K2300/00 ,  C07C49/233 ,  C07C49/255 ,  C07C49/215 ,  C07C49/245 ,  C07C49/235 ,  C07C49/223

摘要： A retroviral protease inhibiting compound of formula (A) is disclosed for use in combination with other active pharmaceutical agents for treating a human infected by HIV. Intermediates and processes useful in the manufacture of compounds of formula (A) are also disclosed.

公开(公告)号：EP2395986A1

公开(公告)日：2011-12-21

申请号：EP10741615.8

申请日：2010-02-09

申请人： Abbott Laboratories

发明人： SHEKHAR, Shashank ,  YU, Su ,  HAIGHT, Anthony R. ,  CHMURA, Preston E. ,  KISHORE, Vimal

IPC分类号： A61K31/135

CPC分类号： C07C221/00 ,  C07B2200/07 ,  C07C213/02 ,  C07C213/08 ,  C07C213/10 ,  C07C2601/08 ,  C07C215/42 ,  C07C217/52 ,  C07C225/20

摘要： Disclosed herein are methods of making compounds which are agonists or antagonists of one or more of the individual receptors of the S1P receptor family.

摘要翻译： 本文公开了制备作为S1P受体家族的一种或多种单独受体的激动剂或拮抗剂的化合物的方法。

公开(公告)号：EP2424500A1

公开(公告)日：2012-03-07

申请号：EP10718372.5

申请日：2010-04-30

申请人： Abbott Laboratories

发明人： DAVID, Paul ,  FICKES, Michael ,  FISCHER, Cristina ,  HAIGHT, Anthony R. ,  HEEMSTRA, Katherine ,  MARSH, Kennan ,  MAYER, Peter ,  RUBIN, Vitaly ,  SANZGIRI, Yeshwant ,  SCHMITT, Eric ,  TONG, Ping ,  ZHOU, Deliang

IPC分类号： A61K9/00 ,  A61K31/5377 ,  A61K47/00 ,  A61K47/02 ,  A61K47/14 ,  A61K47/20

CPC分类号： A61K31/4965 ,  A61K9/4858 ,  A61K31/5377 ,  A61K47/14 ,  A61K47/24

摘要： An orally deliverable pharmaceutical composition comprises a drug-carrier system having a Bcl-2 family protein inhibitory compound,
e.g ., ABT-263, in solution in a substantially non-aqueous carrier that comprises at least one phospholipid and a pharmaceutically acceptable solubilizing agent. The composition is suitable for oral administration to a subject in need thereof for 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：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：EP2222635A2

公开(公告)日：2010-09-01

申请号：EP08851351.0

申请日：2008-11-20

申请人： Abbott Laboratories

发明人： VON GELDERN, Thomas W. ,  BARKALOW, Jufang, H. ,  BARNES, David M. ,  HAIGHT, Anthony R. ,  HENGEVELD, John E. ,  LI, Xiaofeng ,  MCLAUGHLIN, Maureen A. ,  NOONAN, William T. ,  PEI, Zhonghua ,  WU-WONG, Jinshyun Ruth

IPC分类号： C07C401/00

CPC分类号： C07C401/00 ,  C07C2601/14 ,  C07C2602/24

摘要： The invention relates to compounds that are vitamin D receptor activators, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.

摘要翻译： 本发明涉及作为维生素D受体激活剂的化合物，包含这些化合物的组合物，使用这些化合物和组合物的方法，制备此类化合物的方法以及在此过程中获得的中间体。

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：EP1272500A2

公开(公告)日：2003-01-08

申请号：EP00942860.8

申请日：2000-06-15

申请人： Abbott Laboratories

发明人： STONER, Eric J. ,  PETERSON, Matthew J. ,  KU, Yi-Yin ,  CINK, Russell D. ,  COOPER, Arthur J. ,  DESHPANDE, Mahendra N. ,  GRIEME, Tim ,  HAIGHT, Anthony R. ,  HILL, David R. ,  HSU, Margaret, Chi-Ping ,  KING, Steven A. ,  LEANNA, Marvin R. ,  LEE, Elaine C. ,  MCLAUGHLIN, Maureen A. ,  MORTON, Howard E. ,  NAPIER, James J. ,  PLATA, Daniel J. ,  RAJE, Prasad S. ,  RASMUSSEN, Michael ,  RILEY, David ,  TIEN, Jien-Heh J. ,  WITTENBERGER, Steven J.

IPC分类号： C07H17/08 ,  A61K31/70 ,  A61P31/04

CPC分类号： C07H17/08

摘要： In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4'-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.