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1.发明申请Compositions and methods comprising farnesyl dibenzodiazepinones for treating neoplastic cells and conditions 失效包含法呢基二苯并二氮杂酮用于治疗肿瘤细胞和病症的组合物和方法公开(公告)号：US20060079508A1
公开(公告)日：2006-04-13
申请号：US11130295
申请日：2005-05-16
申请人： Pierre Falardeau , Francois Berger , Henriette Gourdeau , James McAlpine , Chris Farnet , Violetta Dimitriadou
发明人： Pierre Falardeau , Francois Berger , Henriette Gourdeau , James McAlpine , Chris Farnet , Violetta Dimitriadou
IPC分类号： A61K31/551 , C07D243/10
CPC分类号： C07D243/38 , A61K31/551
摘要： This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms using the farnesylated dibenzodiazepinone compound of Formula I. The invention includes pharmaceutical compositions comprising the compound of Formula I:
摘要翻译： 本发明涉及抑制肿瘤细胞生长和/或增殖的方法，以及使用式I的法呢基化二苯并二氮杂酮化合物治疗肿瘤的方法。本发明包括药物组合物，其包含式I化合物：
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2.发明授权Compositions and methods comprising farnesyl dibenzodiazepinones for treating neoplastic cells and conditions 失效包含法呢基二苯并二氮杂酮用于治疗肿瘤细胞和病症的组合物和方法公开(公告)号：US07358241B2
公开(公告)日：2008-04-15
申请号：US11130295
申请日：2005-05-16
申请人： Pierre Falardeau , Francois Berger , Henriette Gourdeau , James B. McAlpine , Chris M. Farnet , Violetta Dimitriadou
发明人： Pierre Falardeau , Francois Berger , Henriette Gourdeau , James B. McAlpine , Chris M. Farnet , Violetta Dimitriadou
CPC分类号： C07D243/38 , A61K31/551
摘要： This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms using the farnesylated dibenzodiazepinone compound of Formula I. The invention includes pharmaceutical compositions comprising the compound of Formula I:
摘要翻译： 本发明涉及抑制肿瘤细胞生长和/或增殖的方法，以及使用式I的法呢基化二苯并二氮杂酮化合物治疗肿瘤的方法。本发明包括药物组合物，其包含式I化合物：
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公开(公告)号：US20060270662A1
公开(公告)日：2006-11-30
申请号：US11434154
申请日：2006-05-16
IPC分类号： A61K31/551
CPC分类号： A61K31/551
摘要： This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms by administration of the farnesylated dibenzodiazepinone compound of Formula I via continuous intravenous infusion. The invention includes pharmaceutical compositions comprising the compound of Formula I:
摘要翻译： 本发明涉及抑制肿瘤细胞生长和/或增殖的方法，以及通过连续静脉输注给予式I的法呢基化二苯并二氮杂酮化合物来治疗肿瘤的方法。 本发明包括药物组合物，其包含式I化合物：
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公开(公告)号：US20110028458A1
公开(公告)日：2011-02-03
申请号：US12937101
申请日：2009-04-09
IPC分类号： A61K31/551 , C12N5/09 , A61P35/00
CPC分类号： A61K31/5513
摘要： The invention relates to the discovery that dibenzodiazepinone analogues have cell migration inhibiting activities on neoplastic and endothelial cells. The migration of neoplastic cells from various tumor types, such as a glioma tumor that may comprise an EGF and/or PTEN mutation, or a Ras-, Raf, or EGFR-mediated tumor, may be inhibited when contacted by the dibenzodiazepinone analogues of the present invention. The invention includes methods for inhibiting migration of a cell in a subject, by contacting a cell with a dibenzodiazepinone analogue of the present invention.
摘要翻译： 本发明涉及二苯并二氮杂酮类似物在肿瘤和内皮细胞上具有细胞迁移抑制活性的发现。 当来自各种肿瘤类型的肿瘤细胞的迁移，例如可能包含EGF和/或PTEN突变的胶质瘤肿瘤或Ras-，Raf或EGFR介导的肿瘤时，可能会受到抑制，当二苯并二氮杂酮类似物 本发明。 本发明包括通过使细胞与本发明的二苯并二氮杂酮类似物接触来抑制细胞在受试者中迁移的方法。
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公开(公告)号：US06747036B2
公开(公告)日：2004-06-08
申请号：US10046289
申请日：2002-01-16
IPC分类号： A61K31505
CPC分类号： A61K31/675 , A61K31/506 , A61K31/70 , A61K31/704 , A61K38/13 , A61K38/1816 , A61K38/193 , A61K38/2013 , A61K38/202 , A61K38/212 , A61K38/32 , A61K39/39541 , A61K45/06 , A61K2035/124 , C12N5/0644 , C12N2501/03 , C12N2501/145 , A61K31/505 , A61K38/19 , A61K2300/00 , A61K38/20
摘要： The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from the group comprising H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and wherein each Rc is independently selected from the group comprising H, C1-6 alkyl, C2-6 alkynyl, C2-6 alkynyl and an hydroxy protecting group; and wherein said compound is substantially in the form of the (−) enantiomer.
摘要翻译： 本发明提供了一种用于治疗白血病，更特别是急性骨髓性白血病（AML）的宿主的新方法，其包括向宿主施用治疗有效量的具有式I的化合物：其中B为胞嘧啶或5-氟胞嘧啶，R为 选自包括H，单磷酸酯，二磷酸酯，三磷酸酯，被C 1-6烷基取代的羰基，C 2-6烯基，C 2-6炔基，C 6-10芳基，并且其中每个R c独立地选自H，C 1 C6烷基，C2-6炔基，C2-6炔基和羟基保护基; 并且其中所述化合物基本上为（ - ）对映异构体的形式。
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公开(公告)号：US07763604B2
公开(公告)日：2010-07-27
申请号：US11434154
申请日：2006-05-16
IPC分类号： A61K31/5513 , A61P35/00
CPC分类号： A61K31/551
摘要： This invention relates to methods of inhibiting growth and/or proliferation of a neoplastic cell, and methods of treating neoplasms by administration of the farnesylated dibenzodiazepinone compound of Formula I via continuous intravenous infusion. The invention includes pharmaceutical compositions comprising the compound of Formula I:
摘要翻译： 本发明涉及抑制肿瘤细胞生长和/或增殖的方法，以及通过连续静脉输注给予式I的法呢基化二苯并二氮杂酮化合物来治疗肿瘤的方法。 本发明包括药物组合物，其包含式I化合物：
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7.发明授权Substituted 4-aryl-chromene as activator of caspases and inducer of apoptosis and as antivascular agent and the use thereof 有权取代的4-芳基 - 色烯作为胱天蛋白酶的活化剂和细胞凋亡诱导剂和抗血管剂及其用途公开(公告)号：US07968595B2
公开(公告)日：2011-06-28
申请号：US11822535
申请日：2007-07-06
申请人： Sui Xiong Cai , John A. Drewe , Shailaja Kasibhatla , William D. Kemnitzer , Ben Y. Tseng , Charles Blais , Denis Labrecque , Henriette Gourdeau
发明人： Sui Xiong Cai , John A. Drewe , Shailaja Kasibhatla , William D. Kemnitzer , Ben Y. Tseng , Charles Blais , Denis Labrecque , Henriette Gourdeau
IPC分类号： A61K31/353 , C07D311/58
CPC分类号： C07D405/12 , C07D311/58
摘要： The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.
摘要翻译： 本发明涉及基本上不含相应（S） - 立体异构体的由式1R表示的取代的4H-色烯。本发明还涉及发现基本上不含相应的（S） - 立体异构体的化合物1R 是胱天蛋白酶和凋亡诱导剂的激活剂，以及抗血管性药剂。 因此，基本上不含相应（S） - 立体异构体的化合物1R可用于诱发异常细胞发生不受控制的生长和扩散的各种临床条件下的细胞死亡。 基本上不含相应（S） - 立体异构体的化合物1R也可用于治疗由于脉管系统过度生长（如实体瘤和眼新生血管形成）引起的疾病。
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8.发明申请Substituted 4-aryl-chromene as activator of caspases and inducer of apoptosis and as antivascular agent and the use thereof 有权取代的4-芳基 - 色烯作为胱天蛋白酶的活化剂和细胞凋亡诱导剂和抗血管剂及其用途公开(公告)号：US20080085328A1
公开(公告)日：2008-04-10
申请号：US11822535
申请日：2007-07-06
申请人： Sui Xiong Cai , John A. Drewe , Shailaja Kasibhatla , William E. Kemnitzer , Ben Y. Tseng , Charles Blais , Denis Labrecque , Henriette Gourdeau
发明人： Sui Xiong Cai , John A. Drewe , Shailaja Kasibhatla , William E. Kemnitzer , Ben Y. Tseng , Charles Blais , Denis Labrecque , Henriette Gourdeau
IPC分类号： A61K31/352 , A61K31/351 , A61K31/403 , A61K31/4035 , A61K31/436 , A61K31/4412 , A61K31/502 , A61K31/513 , A61K31/661 , A61K33/24 , A61P17/00 , A61P35/00 , A61P35/02 , A61P37/00 , C07D311/68
CPC分类号： C07D405/12 , C07D311/58
摘要： The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.
摘要翻译： 本发明涉及基本上不含相应（S） - 立体异构体的由式1R表示的取代的4H-色烯。本发明还涉及发现基本上不含相应的（S） - 立体异构体的化合物1R 是胱天蛋白酶和凋亡诱导剂的激活剂，以及抗血管性药剂。 因此，基本上不含相应（S） - 立体异构体的化合物1R可用于诱发异常细胞发生不受控制的生长和扩散的各种临床条件下的细胞死亡。 基本上不含相应（S） - 立体异构体的化合物1R也可用于治疗由于脉管系统过度生长（如实体瘤和眼新生血管形成）引起的疾病。
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公开(公告)号：US06630480B1
公开(公告)日：2003-10-07
申请号：US09536459
申请日：2000-03-28
IPC分类号： A61K31505
CPC分类号： A61K31/675 , A61K31/506 , A61K31/70 , A61K31/704 , A61K38/13 , A61K38/1816 , A61K38/193 , A61K38/2013 , A61K38/202 , A61K38/212 , A61K38/32 , A61K39/39541 , A61K45/06 , A61K2035/124 , C12N5/0644 , C12N2501/03 , C12N2501/145 , A61K31/505 , A61K38/19 , A61K2300/00 , A61K38/20
摘要： The present invention provides a novel method for treating leukemia and more particularly acute myelogenous leukemia (AML) in a host comprising administering to the host a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from the group comprising H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and wherein each Rc is independently selected from the group comprising H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and an hydroxy protecting group; and wherein said compound is substantially in the form of the (−) enantiomer.
摘要翻译： 本发明提供了一种用于治疗白血病，更特别是急性骨髓性白血病（AML）的宿主的新方法，其包括向宿主施用治疗有效量的具有式I的化合物：其中B为胞嘧啶或5-氟胞嘧啶，R为 选自包括H，单磷酸酯，二磷酸酯，三磷酸酯，被C 1-6烷基取代的羰基，C 2-6烯基，C 2-6炔基，C 6-10芳基，并且其中每个R c独立地选自H，C 1 C6烷基，C2-6烯基，C2-6炔基和羟基保护基; 并且其中所述化合物基本上为（ - ）对映异构体的形式。
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