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1.发明申请
公开(公告)号：WO2011149492A1
公开(公告)日：2011-12-01
申请号：PCT/US2010/057587
申请日：2010-11-22
Applicant: ABBOTT LABORATORIES , BRUNCKO, Milan , DING, Hong , DOHERTY, George , ELMORE, Steven , HASVOLD, Lisa , HEXAMER, Laura , KUNZER, Aaron R. , SONG, Xiaohong , SOUERS, Andrew, J. , SULLIVAN, Gerard , TAO, Zhi-Fu , WANG, Gary, T. , WANG, Le , WANG, Xilu , WENDT, Michael , MANTEI, Robert , HANSEN, Todd, M.
Inventor： BRUNCKO, Milan , DING, Hong , DOHERTY, George , ELMORE, Steven , HASVOLD, Lisa , HEXAMER, Laura , KUNZER, Aaron R. , SONG, Xiaohong , SOUERS, Andrew, J. , SULLIVAN, Gerard , TAO, Zhi-Fu , WANG, Gary, T. , WANG, Le , WANG, Xilu , WENDT, Michael , MANTEI, Robert , HANSEN, Todd, M.
IPC: C07D471/04 , A61K31/437 , A61K35/00
CPC classification number: C07D401/12 , A61K31/496 , C07D209/82 , C07D401/14 , C07D403/12 , C07D471/04 , C07D519/00 , Y02A50/463
Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
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公开(公告)号：WO2010080503A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068496
申请日：2009-12-17
Applicant: GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , ABBOTT LABORATORIES , BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , CZABOTAR, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , HASVOLD, Lisa, A. , PETROS, Andrew, M. , SOUERS, Andrew, J. , TAO, Zhi-Fu , WANG, Le , WANG, Xilu , DESHAYES, Kurt
Inventor： BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , CZABOTAR, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , HASVOLD, Lisa, A. , PETROS, Andrew, M. , SOUERS, Andrew, J. , TAO, Zhi-Fu , WANG, Le , WANG, Xilu , DESHAYES, Kurt
IPC: A01N43/00
CPC classification number: C07D417/14 , C07D471/06 , C07D473/00 , C07D487/04 , C07D495/04 , C07D513/04 , C07D513/06
Abstract: In one aspect, the present invention provides for a compound of Formula I; in which the variable X 1a , X 1b , X 1c , X 1d , Q, A, R 1 , B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.
Abstract translation: 一方面，本发明提供式I的化合物; 其中变量X1a，X1b，X1c，X1d，Q，A，R1，B，L，E和下标m和n具有如本文所述的含义。 另一方面，本发明提供包含式I化合物的药物组合物以及使用式I化合物治疗以表达或过表达为特征的疾病和病症（例如癌症，血小板增多症等）的方法 的Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。
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公开(公告)号：WO2007137107A2
公开(公告)日：2007-11-29
申请号：PCT/US2007/069112
申请日：2007-05-17
Applicant: ABBOTT LABORATORIES , IYENGAR, Rajesh, R. , ZHAO, Gang , FREEMAN, Jennifer, C. , GAO, Ju , JUDD, Andrew, S. , KYM, Philip, R. , LYNCH, John, K. , MULHERN, Mathew, M. , SOUERS, Andrew, J.
Inventor： IYENGAR, Rajesh, R. , ZHAO, Gang , FREEMAN, Jennifer, C. , GAO, Ju , JUDD, Andrew, S. , KYM, Philip, R. , LYNCH, John, K. , MULHERN, Mathew, M. , SOUERS, Andrew, J.
IPC: C07C211/22 , C07C275/30 , C07C279/18 , C07C335/16 , C07D213/55 , C07D213/75
CPC classification number: C07C335/22 , C07C229/46 , C07C275/30 , C07C275/32 , C07C275/38 , C07C279/28 , C07C2601/08 , C07C2601/14 , C07D213/55 , C07D213/75 , C07D277/30 , C07D333/22 , C07D333/36 , C07D401/04 , C07D401/12 , C07D409/12 , C07D409/14
Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 3 , X, Q, Z, A, D, m, and n are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
Abstract translation: 本发明涉及式（I）化合物，其中R 1，R 3，X，Q，Z，A，D，m和n如本文所定义。 还公开了治疗DGAT-1相关疾病或病症的药物组合物和方法。
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4.发明申请2-AMINOQUINOLINES AS MELANIN CONCENTRATING HORMONE RECEPTOR ANTAGONISTS 审中-公开2-AMINOQUINOLINES作为MELANIN浓缩HORMONE受体拮抗剂
公开(公告)号：WO2003105850A1
公开(公告)日：2003-12-24
申请号：PCT/US2003/018959
申请日：2003-06-17
Applicant: ABBOTT LABORATORIES
Inventor： COLLINS, Christine, A. , GAO, Ju , KYM, Philip, R. , LEWIS, Jared, C. , SOUERS, Andrew, J. , VASUDEVAN, Anil , WODKA, Dariusz
IPC: A61K31/47
CPC classification number: C07D215/38 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D411/12 , C07D413/12
Abstract: The present invention is related to compounds of formula (I), or a therapeutically suitable salt or prodrug thereof, which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor and are useful for the prevention or treatment of eating disorders, weight gain and obesity.
Abstract translation: 本发明涉及通过黑色素浓缩激素受体拮抗黑色素浓缩激素（MCH）的作用的式（I）化合物或其治疗上合适的盐或前药，并且可用于预防或治疗饮食 疾病，体重增加和肥胖。
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公开(公告)号：WO2008131000A2
公开(公告)日：2008-10-30
申请号：PCT/US2008/060472
申请日：2008-04-16
Applicant: ABBOTT LABORATORIES , ELMORE, Steven, W. , SOUERS, Andrew, J. , BRUNCKO, Milan , SONG, Xiaohong , WANG, Xilu , HASVOLD, Lisa, A. , WANG, Le , KUNZER, Aaron, R. , PARK, Cheol-min , WENDT, Michael, D. , TAO, Zhi-fu
Inventor： ELMORE, Steven, W. , SOUERS, Andrew, J. , BRUNCKO, Milan , SONG, Xiaohong , WANG, Xilu , HASVOLD, Lisa, A. , WANG, Le , KUNZER, Aaron, R. , PARK, Cheol-min , WENDT, Michael, D. , TAO, Zhi-fu
IPC: C07D209/34 , C07D401/12 , C07D413/06 , C07D417/04 , A61P35/00 , A61K31/404
CPC classification number: C07D209/42 , A61K31/5377 , C07D209/34 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D491/113
Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
Abstract translation: 公开了抑制抗细胞凋亡Mcl-1蛋白活性的化合物，含有该化合物的组合物以及治疗涉及过表达或未调节的Mcl-1蛋白的疾病的方法。
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Patent Agency Ranking6.发明申请SULFONAMIDE DERIVATIVES AS BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES 审中-公开作为治疗癌症和免疫疾病的BCL-2-选择性病毒诱导剂的磺酰胺衍生物
公开(公告)号：WO2011068561A1
公开(公告)日：2011-06-09
申请号：PCT/US2010/036919
申请日：2010-06-01
Applicant: ABBOTT LABORATORIES , BRUNCKO, Milan , DING, Hong , DOHERTY, George A. , ELMORE, Steven, W. , HASVOLD, Lisa , HEXAMER, Laura , KUNZER, Aaron , MANTEI, Robert, A. , McCLELLAN, William, J. , PARK, Chang, H. , PARK, Cheol-Min , PETROS, Andrew, M. , SONG, Xiaohong , SOUERS, Andrew, J. , SULLIVAN, Gerard, M. , TAO, Zhi-Fu , WANG, Gary, T. , WANG, Le , WANG, Xilu , WENDT, Michael, D. , HANSEN, Todd, M.
Inventor： BRUNCKO, Milan , DING, Hong , DOHERTY, George A. , ELMORE, Steven, W. , HASVOLD, Lisa , HEXAMER, Laura , KUNZER, Aaron , MANTEI, Robert, A. , McCLELLAN, William, J. , PARK, Chang, H. , PARK, Cheol-Min , PETROS, Andrew, M. , SONG, Xiaohong , SOUERS, Andrew, J. , SULLIVAN, Gerard, M. , TAO, Zhi-Fu , WANG, Gary, T. , WANG, Le , WANG, Xilu , WENDT, Michael, D. , HANSEN, Todd, M.
IPC: C07D405/12 , A61K31/404 , A61P35/00 , C07D209/32 , C07D211/96 , C07D213/64 , C07D215/20 , C07D217/16 , C07D235/26 , C07D249/04 , C07D295/14 , C07D309/14 , C07D401/12 , C07D295/125 , C07D231/56 , C07D405/14
CPC classification number: C07D401/12 , A61K31/407 , A61K31/495 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D209/32 , C07D211/58 , C07D211/96 , C07D213/64 , C07D215/20 , C07D217/16 , C07D231/56 , C07D235/26 , C07D241/04 , C07D249/04 , C07D295/125 , C07D295/14 , C07D295/155 , C07D309/04 , C07D309/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D417/12 , C07D471/04 , C07D487/04
Abstract: Disclosed are compounds (I) which inhibit the activity of anti-apoptotic Bc1-2 or Bc1 xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti apoptotic Bc1-2 protein.
Abstract translation: 公开了抑制抗凋亡Bc1-2或Bc1 xL蛋白活性的化合物（I），含有该化合物的组合物和治疗其中表达抗凋亡Bc1-2蛋白的疾病的方法。
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7.发明申请APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES 审中-公开用于治疗癌症和免疫和自发性疾病的病毒诱导剂
公开(公告)号：WO2010083442A1
公开(公告)日：2010-07-22
申请号：PCT/US2010/021245
申请日：2010-01-15
Applicant: ABBOTT LABORATORIES , KUNZER, Aaron, R. , ELMORE, Steven, W. , HEXAMER, Laura , PARK, Cheol-Min , SOUERS, Andrew, J. , SULLIVAN, Gerard, M. , WANG, Gary, T. , WANG, Xilu , WENDT, Michael, D.
Inventor： KUNZER, Aaron, R. , ELMORE, Steven, W. , HEXAMER, Laura , PARK, Cheol-Min , SOUERS, Andrew, J. , SULLIVAN, Gerard, M. , WANG, Gary, T. , WANG, Xilu , WENDT, Michael, D.
IPC: C07C311/51 , C07D207/36 , C07D211/96 , C07D231/18 , C07D261/10 , C07D275/03 , C07D277/36 , C07D333/34 , C07D285/135 , C07D295/155 , C07D285/125 , C07D295/26 , A61K31/18 , A61P35/00
CPC classification number: C07D277/54 , C07C311/00 , C07C311/51 , C07D207/36 , C07D211/96 , C07D231/18 , C07D261/10 , C07D275/03 , C07D277/36 , C07D277/60 , C07D285/125 , C07D285/135 , C07D295/155 , C07D295/26 , C07D333/34 , C07D333/36 , C07D333/42 , C07D333/62 , C07D409/12 , C07D413/04 , C07D413/06 , C07D417/14 , C07D487/04 , C07D513/04
Abstract: Disclosed are compounds of Formula (1), in which A 1 , Z 1 , Z 1A , Z 2 , Z 2A , L 1 and Z 3 are as defined in the claims, which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and their use in treating diseases during which anti-apoptotic Bcl-2 protein is expressed.
Abstract translation: 公开了式（1）的化合物，其中A1，Z1，Z1A，Z2，Z2A，L1和Z3如权利要求中所定义，其抑制抗凋亡Bcl-2蛋白的活性，含有这些化合物的组合物及其 用于治疗抗凋亡Bcl-2蛋白表达的疾病。
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公开(公告)号：WO2010080478A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/068400
申请日：2009-12-17
Applicant: GENENTECH, INC. , THE WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH , ABBOTT LABORATORIES , BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
Inventor： BAELL, Jonathon, Bayldon , BUI, Chinh, Thien , COLMAN, Peter , DUDLEY, Danette, A. , FAIRBROTHER, Wayne, J. , FLYGARE, John, A. , LASSENE, Guillaume, Laurent , NDUBAKU, Chudi , NIKOLAKOPOULOS, George , RYE, Carl, Steven , SLEEBS, Brad, Edmund , SMITH, Brian, John , WATSON, Keith, Geoffrey , ELMORE, Steven, W. , PETROS, Andrew, M. , SOUERS, Andrew, J.
IPC: A61K31/535
CPC classification number: C07D417/14 , C07D417/12 , C07D487/04
Abstract: In one aspect, the present invention provides for a compound of Formula (I) in which, the variables X 1 , X 2a , X 2b , X 2c , R 1 , B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula (I) as well as methods for using compounds of Formula (I) for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-x L proteins.
Abstract translation: 一方面，本发明提供式（I）的化合物，其中变量X1，X2a，X2b，X2c，R1，B，L，E，A和下标n如本文所定义。 在另一方面，本发明提供包含式（I）化合物的药物组合物以及使用式（I）化合物治疗由表达特征的疾病和病症（例如癌症，血小板增多症等）的方法 或过度表达Bcl-2抗凋亡蛋白，例如抗凋亡Bcl-xL蛋白。
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9.发明申请
公开(公告)号：WO2011119345A3
公开(公告)日：2011-09-29
申请号：PCT/US2011/027895
申请日：2011-03-10
Applicant: ABBOTT LABORATORIES , DING, Hong , ELMORE, Steven , HEXAMER, Laura , KUNZER, Aaron, R. , PARK, Cheol-Min , SOUERS, Andrew, J. , SULLIVAN, Gerard , WENDT, Michael
Inventor： DING, Hong , ELMORE, Steven , HEXAMER, Laura , KUNZER, Aaron, R. , PARK, Cheol-Min , SOUERS, Andrew, J. , SULLIVAN, Gerard , WENDT, Michael
IPC: C07D295/112 , C07D295/195 , C07D417/04 , C07D211/58 , C07C311/51 , A61K31/451 , A61K31/495 , A61K31/18 , A61P35/00
Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti apoptotic Bcl-2 protein.
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10.发明申请
公开(公告)号：WO2010083441A2
公开(公告)日：2010-07-22
申请号：PCT/US2010/021243
申请日：2010-01-15
Applicant: ABBOTT LABORATORIES , HEXAMER, Laura , DING, Hong , ELMORE, Steven, W. , KUNZER, Aaron, R. , SONG, Xiaohong , SOUERS, Andrew, J. , SULLIVAN, Gerard, M. , TAO, Zhi-fu , WENDT, Michael, D.
Inventor： HEXAMER, Laura , DING, Hong , ELMORE, Steven, W. , KUNZER, Aaron, R. , SONG, Xiaohong , SOUERS, Andrew, J. , SULLIVAN, Gerard, M. , TAO, Zhi-fu , WENDT, Michael, D.
IPC: C07D209/08 , C07D213/71 , C07D231/56 , C07D235/04 , C07D265/02 , C07D285/14
CPC classification number: C07D295/155 , C07D209/08 , C07D213/71 , C07D231/56 , C07D235/04 , C07D265/02 , C07D285/14 , C07D311/14
Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
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