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1. 发明申请

WO2012040404A1 MONOHYDRATE OF AN AZAADAMANTANE DERIVATIVE 审中-公开
标题翻译：亚胺丹衍生物的单一化合物
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
申请人： ABBOTT LABORATORIES , CHEN, Shuang , NAPIER, James J. , ZHANG, Geoff G. Z. , BRACKEMEYER, Paul J.
发明人： CHEN, Shuang , NAPIER, James J. , ZHANG, Geoff G. Z. , BRACKEMEYER, Paul J.
IPC分类号： C07D471/08 , A61K31/439 , A61P25/00 , A61P25/28
CPC分类号： C07D451/14 , A61K31/439 , A61K45/06 , C07D471/08
摘要： 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.
摘要翻译：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。

2. 发明申请

WO2011089202A1 METHOD FOR EVALUATING THE SOLUBILITY OF A CRYSTALLINE SUBSTANCE IN A POLYMER 审中-公开
标题翻译：评估聚合物中晶体物质的溶解性的方法
公开(公告)号：WO2011089202A1
公开(公告)日：2011-07-28
申请号：PCT/EP2011/050792
申请日：2011-01-21
申请人： ABBOTT GMBH & CO. KG , ZHANG, Geoff G. Z. , YU, Lian , TAO, Jing , SUN, Ye , MAEGERLEIN, Markus
发明人： ZHANG, Geoff G. Z. , YU, Lian , TAO, Jing , SUN, Ye , MAEGERLEIN, Markus
IPC分类号： G01N25/48 , G01N33/15
CPC分类号： G01N33/15 , G01N25/4866 , G01N2013/006
摘要： A method for evaluating the solubility of a crystalline substance in a polymer comprises a) providing at least one sample of an intimate crystalline substance/polymer mixture at a predetermined crystalline substance concentration; b) annealing the sample at a constant temperature T a for a period of time; c) heating the annealed sample while recording the heat flux over time by DSC; d) identifying a DSC dissolution endotherm in the recorded heat flux, if any; e) considering the crystalline substance concentration as a concentration above the crystalline substance solubility in the polymer at temperature T a when there is a DSC dissolution endotherm identified, and considering the crystalline substance concentration as a concentration less than or equal to the crystalline substance solubility in the polymer at temperature T a when there is no DSC dissolution endotherm identified. Thus, the method yields the upper and lower bounds for the equilibrium solubility at a given temperature or the upper and lower bounds for the equilibrium solubility temperature at a given crystalline substance concentration. The method improves accuracy of measurement near the glass transition temperature.
摘要翻译：用于评价结晶物质在聚合物中的溶解度的方法包括a）以预定的结晶物质浓度提供至少一种紧密结晶物质/聚合物混合物的至少一个样品; b）在恒温Ta下将样品退火一段时间; c）加热退火样品，同时通过DSC随时间记录热通量; d）识别记录的热通量中的DSC溶解吸热（如果有的话）; e）当确定DSC溶解吸热时，考虑结晶物质浓度高于结晶物质在聚合物中的溶解度的浓度，考虑到结晶物质浓度小于或等于结晶物质溶解度的浓度聚合物在温度Ta时没有DSC溶解吸热确定。因此，该方法产生在给定温度下的平衡溶解度的上限和下限，或者给定在给定结晶物质浓度下的平衡溶解度温度的上限和下限。该方法提高玻璃化转变温度附近的测量精度。

3. 发明申请

WO2009039127A1 URACIL OR THYMINE DERIVATIVE FOR TREATING HEPATITIS C 审中-公开
标题翻译：尿嘧啶或用于治疗乙型肝炎的衍生物C
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
申请人： 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.
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.
摘要翻译：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。

4. 发明申请

WO2009039135A1 N-PHENYL-DIOXO-HYDROPYRIMIDINES USEFUL AS HEPATITIS C VIRUS (HCV) INHIBITORS 审中-公开
标题翻译：用作丙型肝炎病毒（HCV）抑制剂的N-苯基二氧化二氢亚胺嘧啶
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
申请人： 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.
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)
摘要翻译：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）

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