公开(公告)号：WO2008014222A1

公开(公告)日：2008-01-31

申请号：PCT/US2007/074159

申请日：2007-07-24

Applicant: ABBOTT LABORATORIES ,  VISWANATH, Shekhar ,  BARTELT, Larry ,  LEANNA, Robert ,  RASMUSSEN, Michael ,  DHAON, Madhup ,  HENRY, Rodger ,  BORCHARDT, Thomas ,  CHEN, Shuang ,  ZHANG, Geoff

Inventor： VISWANATH, Shekhar ,  BARTELT, Larry ,  LEANNA, Robert ,  RASMUSSEN, Michael ,  DHAON, Madhup ,  HENRY, Rodger ,  BORCHARDT, Thomas ,  CHEN, Shuang ,  ZHANG, Geoff

IPC: C07D498/18 ,  A61K31/395 ,  A61P37/06 ,  A61K31/4353

CPC classification number: C07D498/18

Abstract: A rapamycin analog composition includes a crystalline form of a rapamycin analog. The crystal can be a hydrate, dehydrate, solvate, or desolvate. The rapamycin analog can have a structure of Formula (I), which is optionally a prodrug, salt, derivative, or combination thereof: Formula (I)

Abstract translation: 雷帕霉素类似物组合物包括雷帕霉素类似物的结晶形式。 该晶体可以是水合物，脱水剂，溶剂化物或去溶剂化物。 雷帕霉素类似物可以具有式（I）的结构，其可任选地是前药，盐，衍生物或其组合：式（I）

公开(公告)号：WO2009039134A1

公开(公告)日：2009-03-26

申请号：PCT/US2008/076592

申请日：2008-09-17

Applicant: ABBOTT LABORATORIES ,  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.

Inventor： 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: C07D239/22 ,  C07D239/54 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  A61K31/513 ,  A61P31/12

CPC classification number: C07D239/54 ,  A61K31/513 ,  A61K45/06 ,  C07D239/22 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  A61K2300/00

Abstract: 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.

Abstract translation: 本发明涉及：（a）特别是抑制HCV的化合物及其盐; （b）可用于制备这些化合物和盐的中间体; （c）包含这些化合物和盐的组合物; （d）制备这种中间体，化合物，盐和组合物的方法; （e）使用这些化合物，盐和组合物的方法; 和（f）包含这些化合物，盐和组合物的试剂盒。

公开(公告)号：WO2012040404A1

公开(公告)日：2012-03-29

申请号：PCT/US2011/052668

申请日：2011-09-21

Applicant: ABBOTT LABORATORIES ,  CHEN, Shuang ,  NAPIER, James J. ,  ZHANG, Geoff G. Z. ,  BRACKEMEYER, Paul J.

Inventor： CHEN, Shuang ,  NAPIER, James J. ,  ZHANG, Geoff G. Z. ,  BRACKEMEYER, Paul J.

IPC: C07D471/08 ,  A61K31/439 ,  A61P25/00 ,  A61P25/28

CPC classification number: C07D451/14 ,  A61K31/439 ,  A61K45/06 ,  C07D471/08

Abstract: The invention relates to a crystalline monohydrate of ( 4s )-4-(5-phenyl-1,3,4- thiadiazol-2-yloxy)-1-azatricyclo[3.3.1.1 3,7 ]decane dihydrogen citrate, compositions comprising such compound, and a process for preparing such compound.

Abstract translation: 本发明涉及（4s）-4-（5-苯基-1,3,4-噻二唑-2-基氧基）-1-氮杂三环[3.3.1.13,7]癸烷二氢二氢柠檬酸盐的结晶一水合物，包含这种化合物 ，以及这种化合物的制备方法。

公开(公告)号：WO2009039127A1

公开(公告)日：2009-03-26

申请号：PCT/US2008/076576

申请日：2008-09-17

Applicant: ABBOTT LABORATORIES ,  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.

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

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

Abstract: 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.

Abstract translation: 本申请涉及可用于治疗丙型肝炎（HCV）感染的式I化合物。 所公开的化合物的结构是通过亚苯基连接成稠合的2-环环系（R6）或者另外通过另外的两个原子连接基（L）与5-6元单环（R6）连接的尿嘧啶或胸腺嘧啶衍生物。 应用进一步公开了两种特定化合物的多晶型物和假多晶型物：N-（6（3-叔丁基-5-（2,4-二氧代-3,4-二氢嘧啶-1（2H） - 基）-2-甲氧基 - 苯基 ）萘-2-基）甲磺酰胺和（E）-N-（4（3-叔丁基-5-（2,4-二氧代-3）4-二氢嘧啶-1（2H） - 基）2-甲氧基 - 苯乙烯基 - 苯基）甲磺酰胺。

公开(公告)号：WO2008058096A2

公开(公告)日：2008-05-15

申请号：PCT/US2007/083687

申请日：2007-11-06

Applicant: ABBOTT LABORATORIES ,  SCHRIMPF, Michael R ,  NERSESIAN, Diana L ,  SIPPY, Kevin B ,  JI, Jianguo ,  LI, Tao ,  SCANIO, Marc ,  SHI, Lei ,  LEE, Chih-hung ,  BUNNELLE, Willaim H ,  ZHANG, Geoff G.Z. ,  BRACKEMEYER, Paul J ,  CHEN, Shuang ,  HENRY, Rodger F

Inventor： SCHRIMPF, Michael R ,  NERSESIAN, Diana L ,  SIPPY, Kevin B ,  JI, Jianguo ,  LI, Tao ,  SCANIO, Marc ,  SHI, Lei ,  LEE, Chih-hung ,  BUNNELLE, Willaim H ,  ZHANG, Geoff G.Z. ,  BRACKEMEYER, Paul J ,  CHEN, Shuang ,  HENRY, Rodger F

IPC: C07D451/14 ,  A61K31/395

CPC classification number: C07D471/18 ,  A61K31/095 ,  A61K31/439 ,  A61K31/444 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07C309/29 ,  C07D451/14 ,  C07D471/08 ,  C07F5/022

Abstract: The invention relates to compounds that are azaadamantane derivatives, particularly ether- or amine-substituted azaadamantane derivatives and salts and prodrugs thereof, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.

Abstract translation: 本发明涉及为氮杂金刚烷衍生物，特别是醚或胺取代的氮杂金刚烷衍生物及其盐和前药的化合物，包含此类化合物的组合物，使用此类化合物和组合物的方法，制备这类化合物的方法 化合物和在这些过程中获得的中间体。

公开(公告)号：WO2012071336A1

公开(公告)日：2012-05-31

申请号：PCT/US2011/061678

申请日：2011-11-21

Applicant: ABBOTT LABORATORIES ,  CATRON, Nathaniel D. ,  CHEN, Shuang ,  GONG, Yuchuan ,  ZHANG, Geoff G.

Inventor： CATRON, Nathaniel D. ,  CHEN, Shuang ,  GONG, Yuchuan ,  ZHANG, Geoff G.

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D471/04

Abstract: Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}- sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide 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.

Abstract translation: 盐酸盐和4-（4 - {[2-（4-氯苯基）-4,4-二甲基环己-1-烯-1-基]甲基}哌嗪-1-基）-N - （{3-硝基 -4 - [（四氢-2H-吡喃-4-基甲基）氨基]苯基} - 磺酰基）-2-（1H-吡咯并[2,3-b]吡啶-5-基氧基）苯甲酰胺是药物的合适的活性药物成分 可用于治疗以一种或多种抗凋亡Bcl-2家族蛋白（例如癌症）过表达为特征的疾病的组合物。

公开(公告)号：WO2009039135A1

公开(公告)日：2009-03-26

申请号：PCT/US2008/076594

申请日：2008-09-17

Applicant: ABBOTT LABORATORIES ,  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.

Inventor： 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: C07D239/22 ,  C07D239/54 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D239/553 ,  A61K31/513 ,  A61K31/506 ,  A61P31/14

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

Abstract: 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)

Abstract translation: 本发明涉及：（a）特别是抑制HCV的化合物及其盐; （b）可用于制备这些化合物和盐的中间体; （c）包含这些化合物和盐的组合物; （d）制备这种中间体，化合物，盐和组合物的方法; （e）使用这些化合物，盐和组合物的方法; 和（f）包含这些化合物，盐和组合物的试剂盒。 该化合物在丙型肝炎的治疗中是有用的，具有以下通用结构：式（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

Applicant: Abbott Laboratories

Inventor： 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: C07D239/22 ,  C07D239/54 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  A61K31/513 ,  A61P31/12

CPC classification number: C07D239/54 ,  A61K31/513 ,  A61K45/06 ,  C07D239/22 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10 ,  A61K2300/00

Abstract: 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

Applicant: Abbott Laboratories

Inventor： 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: C07D239/22 ,  C07D239/54 ,  C07D401/10 ,  C07D403/10 ,  C07D405/10 ,  C07D409/10 ,  C07D413/10 ,  C07D239/553 ,  A61K31/513 ,  A61K31/506 ,  A61P31/14

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

Abstract: 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

Applicant: Abbott Laboratories

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

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

Abstract: 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.