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公开(公告)号：WO2010127198A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/033085
申请日：2010-04-30
Applicant: ABBOTT LABORATORIES , ABBOTT GMBH & CO. KG , CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , GOKHALE, Rajeev , HAIGHT, Anthony R. , HEEMSTRA, Katherine , HILL, David , KNOBLOCH, Martin, Dr. , KOSTELAC, Drazen, Dr. , LAFOUNTAINE, Justin S. , LI, Yanxia , LIEPOLD, Bernd, Dr. , MARSH, Kennan , MILLER, Jonathan Mark , PACKHAEUSER, Claudia, Dr. , SANZGIRI, Yeshwant , SCHMITT, Eric , SHI, Yi , STEIGER, Norbert , TONG, Ping , WU, Huailiang , ZHANG, Geoff , ZHOU, Deliang
Inventor： CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , GOKHALE, Rajeev , HAIGHT, Anthony R. , HEEMSTRA, Katherine , HILL, David , KNOBLOCH, Martin, Dr. , KOSTELAC, Drazen, Dr. , LAFOUNTAINE, Justin S. , LI, Yanxia , LIEPOLD, Bernd, Dr. , MARSH, Kennan , MILLER, Jonathan Mark , PACKHAEUSER, Claudia, Dr. , SANZGIRI, Yeshwant , SCHMITT, Eric , SHI, Yi , STEIGER, Norbert , TONG, Ping , WU, Huailiang , ZHANG, Geoff , ZHOU, Deliang
CPC classification number: A61K31/5377 , A61K9/08 , A61K9/10 , A61K9/146 , A61K9/2054 , A61K9/2077 , A61K9/4858 , A61K9/4866
Abstract: An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis -HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and/or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. 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.
Abstract translation: 可口服递送的药物组合物包含作为唯一或第一活性成分的本文定义的式I化合物或其药学上可接受的盐，例如以游离碱当量分散的ABT-263游离碱或ABT-263双-HCl盐 至少约2.5重量％的组合物，在药学上可接受的载体中; 其中所述活性成分是固态形式和/或所述组合物还包含以有效抑制活性成分在其硫醚键的氧化的量分散在载体中的药学上可接受的较重硫族元素抗氧化剂。 该组合物适合于有需要的受试者的口服给药，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。
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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。
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公开(公告)号：WO2012009699A2
公开(公告)日：2012-01-19
申请号：PCT/US2011/044283
申请日：2011-07-15
Applicant: ABBOTT LABORATORIES , SHEKHAR, Shashank , FRANCZYK, Thaddeus S. , BARNES, David M. , DUNN, Travis B. , HAIGHT, Anthony R. , CHAN, Vincent S.
Inventor： SHEKHAR, Shashank , FRANCZYK, Thaddeus S. , BARNES, David M. , DUNN, Travis B. , HAIGHT, Anthony R. , CHAN, Vincent S.
IPC: C07D239/54 , A61K31/522 , A61P31/14
CPC classification number: C07D239/54 , A61K31/513 , A61K31/7056 , A61K38/21 , A61K45/06 , B01J31/2423 , B01J2231/344 , B01J2231/4227 , B01J2231/4283 , B01J2231/4288 , B01J2231/4294 , B01J2531/824 , A61K2300/00
Abstract: This disclosure is directed to: (a) processes for preparing a compound and salts thereof that, inte r alia , are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.
Abstract translation: 本公开内容涉及：（a）用于制备化合物及其盐的方法，所述化合物及其盐可用于抑制肝炎 C病毒（HCV）; （b）可用于制备该化合物和盐的中间体; （c）包含所述一种或多种化合物的药物组合物; 和（d）使用这种组合物的方法。
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公开(公告)号：WO2010127192A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/033074
申请日：2010-04-30
Applicant: ABBOTT LABORATORIES , 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
Inventor： 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
CPC classification number: A61K31/4965 , A61K9/4858 , A61K31/5377 , A61K47/14 , A61K47/24
Abstract: 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.
Abstract translation: 可口服递送的药物组合物包含在包含至少一种磷脂和药学上可接受的增溶剂的基本上非水性载体中的溶液中具有Bcl-2家族蛋白质抑制化合物例如ABT-263的药物 - 载体体系。 该组合物适合于有需要的受试者的口服给药，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。
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公开(公告)号：WO2010093616A1
公开(公告)日：2010-08-19
申请号：PCT/US2010/023607
申请日：2010-02-09
Applicant: ABBOTT LABORATORIES , SHEKHAR, Shashank , YU, Su , HAIGHT, Anthony R. , CHMURA, Preston E. , KISHORE, Vimal
Inventor： SHEKHAR, Shashank , YU, Su , HAIGHT, Anthony R. , CHMURA, Preston E. , KISHORE, Vimal
IPC: A61K31/135
CPC classification number: C07C221/00 , C07B2200/07 , C07C213/02 , C07C213/08 , C07C213/10 , C07C2601/08 , C07C215/42 , C07C217/52 , C07C225/20
Abstract: 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.
Abstract translation: 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。
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Patent Agency Ranking
公开(公告)号：WO2012009698A1
公开(公告)日：2012-01-19
申请号：PCT/US2011/044282
申请日：2011-07-15
Applicant: ABBOTT LABORATORIES , SHEKHAR, Shashank , FRANCZYK, Thaddeus S. , BARNES, David M. , DUNN, Travis B. , HAIGHT, Anthony R. , CHAN, Vincent S.
Inventor： SHEKHAR, Shashank , FRANCZYK, Thaddeus S. , BARNES, David M. , DUNN, Travis B. , HAIGHT, Anthony R. , CHAN, Vincent S.
IPC: B01J31/24
CPC classification number: C07F9/657163 , B01J31/189 , B01J31/2423 , B01J31/2466 , B01J31/2485 , B01J31/249 , B01J2231/344 , B01J2231/4227 , B01J2231/4283 , B01J2231/4288 , B01J2231/4294 , B01J2531/0205 , B01J2531/0266 , B01J2531/0288 , B01J2531/824 , B01J2540/10 , B01J2540/40 , C07C1/30 , C07C1/321 , C07C15/14 , C07C17/093 , C07C17/361 , C07C41/09 , C07C45/68 , C07C201/10 , C07C253/30 , C07C273/1854 , C07C273/1863 , C07C303/40 , C07C315/04 , C07C319/14 , C07C319/18 , C07C2523/42 , C07C2523/44 , C07C2523/46 , C07C2523/52 , C07C2523/72 , C07C2523/75 , C07C2523/755 , C07C2527/14 , C07C2531/22 , C07C2531/24 , C07D209/34 , C07D239/54 , C07D295/033 , C07F5/027 , C07F9/40 , C07F9/65036 , C07F9/65515 , C07F9/6552 , C07F9/65683 , C07F9/6571 , C07F9/6584 , Y02P20/52 , C07C275/28 , C07C311/08 , C07C311/21 , C07C311/29 , C07C255/10 , C07C321/30 , C07C205/45 , C07C15/06 , C07C49/784 , C07C25/18
Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) methods of using such phosphacycle ligands in bond forming reactions; and (c) methods of preparing phosphacycle ligands.
Abstract translation: 本公开涉及：（a）磷酸基配体; （b）在成键反应中使用这种磷酸基配体的方法; 和（c）制备磷酸基配体的方法。
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公开(公告)号：WO2010127193A1
公开(公告)日：2010-11-04
申请号：PCT/US2010/033075
申请日：2010-04-30
Applicant: ABBOTT LABORATORIES , CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , HAIGHT, Anthony R. , HEEMSTRA, Katherine , SANZGIRI, Yeshwant , SCHMITT, Eric , TONG, Ping , ZHANG, Geoff , ZHOU, Deliang
Inventor： CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , HAIGHT, Anthony R. , HEEMSTRA, Katherine , SANZGIRI, Yeshwant , SCHMITT, Eric , TONG, Ping , ZHANG, Geoff , ZHOU, Deliang
CPC classification number: A61K31/5377 , A61K9/0095 , A61K9/08 , A61K9/10 , A61K9/4858 , A61K47/14 , A61K47/183 , A61K47/24 , A61K47/26
Abstract: 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.
Abstract translation: 可口服递送的药物组合物包含Bcl-2家族蛋白质抑制化合物，例如ABT-263，较重硫族元素抗氧化剂和基本上非水性脂质载体，其中所述化合物和所述抗氧化剂在载体中的溶液中。 该组合物适合于有需要的受试者的口服给药，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。
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8.发明申请N-PHENYL-DIOXO-HYDROPYRIMIDINES USEFUL AS HEPATITIS C VIRUS (HCV) INHIBITORS 审中-公开用作丙型肝炎病毒（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
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）
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9.发明公开METHODS FOR PREPARING S1P RECEPTOR AGONISTS AND ANTAGONISTS 审中-公开VERFAHRENFÜRDIE HERSTELLUNG VON S1P-REZEPTORAGONISTEN UNDONANTONON
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
Applicant: Abbott Laboratories
Inventor： SHEKHAR, Shashank , YU, Su , HAIGHT, Anthony R. , CHMURA, Preston E. , KISHORE, Vimal
IPC: A61K31/135
CPC classification number: C07C221/00 , C07B2200/07 , C07C213/02 , C07C213/08 , C07C213/10 , C07C2601/08 , C07C215/42 , C07C217/52 , C07C225/20
Abstract: 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.
Abstract translation: 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。
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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
Applicant: Abbott Laboratories
Inventor： CATRON, Nathaniel , FICKES, Michael , FISCHER, Cristina , HAIGHT, Anthony R. , HEEMSTRA, Katherine , SANZGIRI, Yeshwant , SCHMITT, Eric , TONG, Ping , ZHANG, Geoff , ZHOU, Deliang
CPC classification number: A61K31/5377 , A61K9/0095 , A61K9/08 , A61K9/10 , A61K9/4858 , A61K47/14 , A61K47/183 , A61K47/24 , A61K47/26
Abstract: 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.
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