公开(公告)号：WO2006042034A3

公开(公告)日：2006-04-20

申请号：PCT/US2005/036024

申请日：2005-10-09

Applicant: ABBOTT LABORATORIES ,  ZHANG, Geoff, G. ,  BRADLEY, Michael, F. ,  BARNES, David, M. ,  HENRY, Rodger

Inventor： ZHANG, Geoff, G. ,  BRADLEY, Michael, F. ,  BARNES, David, M. ,  HENRY, Rodger

IPC: C07D401/14

Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.

公开(公告)号：WO2006042034A2

公开(公告)日：2006-04-20

申请号：PCT/US2005/036024

申请日：2005-10-09

Applicant: ABBOTT LABORATORIES ,  ZHANG, Geoff, G. ,  BRADLEY, Michael, F. ,  BARNES, David, M. ,  HENRY, Rodger

Inventor： ZHANG, Geoff, G. ,  BRADLEY, Michael, F. ,  BARNES, David, M. ,  HENRY, Rodger

CPC classification number: C07D401/14 ,  A61K31/4709 ,  A61K47/02 ,  A61K47/12 ,  C07C31/26

Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.

Abstract translation: 公开了药物的结晶形式，制备方法，含有它的组合物以及治疗疾病和抑制不利生理事件的方法。

公开(公告)号：WO2006034094A1

公开(公告)日：2006-03-30

申请号：PCT/US2005/033278

申请日：2005-09-19

Applicant: ABBOTT LABORATORIES ,  DZIKI, Walter ,  LU, Ziqi ,  RASMUSSEN, Michael, W. ,  WARDROP, Jaqueline ,  ZHANG, Geoff, G. ,  GOLDSTEIN, Mark

Inventor： DZIKI, Walter ,  LU, Ziqi ,  RASMUSSEN, Michael, W. ,  WARDROP, Jaqueline ,  ZHANG, Geoff, G. ,  GOLDSTEIN, Mark

IPC: C07D405/10 ,  A61K31/4025 ,  A61P35/00

CPC classification number: A61K31/4025 ,  C07D405/10

Abstract: Atrasentan Hydrochloride Crystalline Form 1, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.

Abstract translation: 盐酸阿特拉森结晶形式1，含有它的组合物和治疗疾病的方法以及使用其抑制不良生理事件。

公开(公告)号：WO2011156464A8

公开(公告)日：2012-10-11

申请号：PCT/US2011039591

申请日：2011-06-08

Applicant: ABBVIE INC ,  HOFFMAN DOUG H ,  MILLER JONATHAN ,  ZHANG GEOFF G Z

Inventor： HOFFMAN DOUG H ,  MILLER JONATHAN ,  ZHANG GEOFF G Z

IPC: C07D495/04 ,  A61K31/4365 ,  A61P35/00

CPC classification number: C07D495/04

Abstract: Citrate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N'-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.

Abstract translation: 噻吩并[3,2-c]吡啶-3-基}苯基）-N（4- {4-氨基-7- [1-（2-羟乙基）-1H-吡唑-4-基] ' - （3-氟苯基）脲及其结晶形式是用于治疗疾病例如癌症的药物组合物的合适的药物成分。

公开(公告)号：WO2012129099A1

公开(公告)日：2012-09-27

申请号：PCT/US2012/029478

申请日：2012-03-16

Applicant: ABBOTT LABORATORIES ,  WU, Huailiang ,  HOU, Hao ,  JAYASANKAR, Adivaraha ,  PATEL, Ameesha ,  BENO, David ,  SCHMITT, Eric A. ,  ZHANG, Geoff G.

Inventor： WU, Huailiang ,  HOU, Hao ,  JAYASANKAR, Adivaraha ,  PATEL, Ameesha ,  BENO, David ,  SCHMITT, Eric A. ,  ZHANG, Geoff G.

IPC: A61K9/16 ,  A61K9/20

CPC classification number: A61K47/38 ,  A61K9/146 ,  A61K9/1611 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/4866 ,  A61K31/513 ,  A61K47/02 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32

Abstract: A pharmaceutical product comprising at least one phenyl uracil-based pharmaceutically active agent or an agent of related structural type and processes for obtaining such product.

Abstract translation: 包含至少一种基于苯基尿嘧啶的药物活性剂或相关结构类型的药剂的药物产品和用于获得该产品的方法。

公开(公告)号：WO2012112841A2

公开(公告)日：2012-08-23

申请号：PCT/US2012/025570

申请日：2012-02-17

Applicant: ABBOTT LABORATORIES ,  ZHANG, Geoff G. ,  BRACKEMEYER, Paul J. ,  CHEN, Shaung ,  GORDON, Thomas D.

Inventor： ZHANG, Geoff G. ,  BRACKEMEYER, Paul J. ,  CHEN, Shaung ,  GORDON, Thomas D.

IPC: A61K31/4439 ,  C07D413/04 ,  C07D271/06 ,  A61K31/4245 ,  A61P37/06 ,  A61P35/00

CPC classification number: C07D413/04 ,  A61K31/4245 ,  A61K31/4439 ,  C07D271/06

Abstract: The present invention relates to salts and crystalline forms of [1,2,4]oxadiazol-3-yl]-phenoxy}-cycloalkyl carboxylic acids, processes for their preparation, pharmaceutical compositions comprising such compounds, and methods of using them.

Abstract translation: 本发明涉及[1,2,4]恶二唑-3-基] - 苯氧基} - 环烷基羧酸的盐和结晶形式，其制备方法，包含这些化合物的药物组合物及其使用方法。

公开(公告)号：WO2011156473A1

公开(公告)日：2011-12-15

申请号：PCT/US2011/039603

申请日：2011-06-08

Applicant: ABBOTT LABORATORIES ,  ZHANG, Geoff G., Z. ,  BRACKEMEYER, Paul, J. ,  SHEIKH, Ahmad, Y.

Inventor： ZHANG, Geoff G., Z. ,  BRACKEMEYER, Paul, J. ,  SHEIKH, Ahmad, Y.

IPC: C07D495/04 ,  A61K31/4365 ,  A61P35/00

CPC classification number: C07D495/04

Abstract: Salts of N -(4- {4-amino-7-[ 1 -(2-hydroxyethyl)- 1 H -pyrazol-4-yl]thieno[3,2-c]pyridin- 3-yl}phenyl)- N '-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.

Abstract translation: N-（4- {4-氨基-7- [1-（2-羟乙基）-1H-吡唑-4-基]噻吩并[3,2-c]吡啶-3-基}苯基）-N ' - （3-氟苯基）脲及其结晶形式是用于治疗疾病例如癌症的药物组合物的合适的药物成分。

公开(公告)号：WO2009135799A2

公开(公告)日：2009-11-12

申请号：PCT/EP2009/055233

申请日：2009-04-29

Applicant: ABBOTT GMBH & CO. KG ,  ZHANG, Geoff, G., Z. ,  YU, Lian ,  TAO, Jing ,  SUN, Ye ,  MAEGERLEIN, Markus

Inventor： ZHANG, Geoff, G., Z. ,  YU, Lian ,  TAO, Jing ,  SUN, Ye ,  MAEGERLEIN, Markus

IPC: G01N33/15

CPC classification number: G01N33/15 ,  G01N25/4866

Abstract: A viable strategy to enhance the bioavailability of poorly soluble drugs is to use amorphous solids in place of the more commonly used crystalline solids in pharmaceutical formulations. However, amorphous solids are physically meta-stable and tend to revert back to their crystalline counterpart. An effective approach to stabilizing an amorphous drug against crystallization is to disperse it in a polymer matrix. The drug's solubility in the chosen polymer defines the upper limit of drug loading without any risk of crystallization. Measuring the solubility of a drug in a polymer has been a scientific and technological challenge because the high viscosity of polymers makes achieving solubility equilibrium difficult and because pharmaceutically important drug/polymer dispersions are glasses, which undergo structural relaxation over time. The invention provides a method based on Differential Scanning Calorimetry (DSC) for measuring the solubility of crystalline drugs in polymeric matrices. The method relies on the detection of the dissolution endpoint of a drug/polymer mixture prepared by cryomilling.

Abstract translation: 提高难溶性药物的生物利用度的可行策略是使用无定形固体代替药物制剂中更常用的结晶固体。 然而，无定形固体物理上是元稳定的，并且倾向于回复到它们的结晶对应物。 稳定无定形药物抗结晶的有效方法是将其分散在聚合物基质中。 药物在所选聚合物中的溶解度限定了药物负载的上限，而没有结晶的风险。 测量药物在聚合物中的溶解度已经是科学和技术挑战，因为聚合物的高粘度使得难以实现溶解度平衡，并且因为药物重要的药物/聚合物分散体是随时间经历结构松弛的玻璃。 本发明提供了一种基于差示扫描量热法（DSC）测量结晶药物在聚合物基质中的溶解度的方法。 该方法依赖于通过冷冻法制备的药物/聚合物混合物的溶解终点的检测。

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：WO2006042034A8

公开(公告)日：2007-09-07

申请号：PCT/US2005036024

申请日：2005-10-07

Applicant: ABBOTT LAB ,  ZHANG GEOFF G ,  BRADLEY MICHAEL F ,  BARNES DAVID M ,  HENRY RODGER

Inventor： ZHANG GEOFF G ,  BRADLEY MICHAEL F ,  BARNES DAVID M ,  HENRY RODGER

IPC: C07D401/14

CPC classification number: C07D401/14 ,  A61K31/4709 ,  A61K47/02 ,  A61K47/12 ,  C07C31/26

Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.

Abstract translation: 公开了药物的结晶形式，其制备方法，含有它的组合物以及治疗疾病的方法以及使用其抑制不良生理事件。