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公开(公告)号：US20070078106A1
公开(公告)日：2007-04-05
申请号：US11469515
申请日：2006-09-01
申请人： Thomas Spector , David Porter , Saad Rahim
发明人： Thomas Spector , David Porter , Saad Rahim
IPC分类号： A61K31/7072 , A61K31/513 , A61K9/48 , A61K9/20
CPC分类号： A61K31/70 , A61K9/0031 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/48 , A61K31/505 , A61K31/513 , A61K31/7072 , A61K45/06 , C07D239/54 , C07H19/06 , A61K2300/00
摘要： Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 alkyl C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.
摘要翻译： 尿嘧啶还原酶灭活剂，特别是5-取代的尿嘧啶或5,6-二氢-5-取代的尿嘧啶，可加强5-氟尿嘧啶，尤其用于治疗癌症。 5-取代基选自溴，碘，氰基，卤素取代的C 1-4烷基C 2-6亚烯基，1-卤代-C 2 -6个链烯基和卤素取代的C 2-6炔基。
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公开(公告)号：US5643913A
公开(公告)日：1997-07-01
申请号：US336717
申请日：1994-11-09
IPC分类号： A61K31/513 , A61K31/505
CPC分类号： A61K31/513
摘要： Pharmaceutical compositions containing 5-substituted uracil compounds are disclosed. The compositions are preferably in the form of a tablet or capsule.
摘要翻译： 公开了含有5-取代的尿嘧啶化合物的药物组合物。 组合物优选为片剂或胶囊剂的形式。
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3.发明授权Methods for preventing or reducing neurotoxicity associated with administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs 有权与5-FU和5-FU前药组合施用DPD抑制剂相关的预防或减少神经毒性的方法公开(公告)号：US08658618B2
公开(公告)日：2014-02-25
申请号：US12904974
申请日：2010-10-14
申请人： Thomas Spector
发明人： Thomas Spector
IPC分类号： A61K31/70 , A61K31/505
CPC分类号： A61K31/513 , A61K2300/00
摘要： Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme in both nervous and non-nervous tissues within the patient and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU generated from a prodrug is in substantial excess of DPD inhibitor in the patient.
摘要翻译： 提供了用于改进DPD抑制剂与5-FU和/或5-FU前药组合的给药和给药方法，包括首先向有需要的患者施用DPD抑制剂，其基本上消除了神经和非 - 患者内的神经组织，然后施用5-FU或5-FU前药，其中由前药产生的5-FU或5-FU的水平在患者体内显着超过DPD抑制剂。
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4.发明申请METHODS FOR PREVENTING OR REDUCING NEUROTOXICITY ASSOCIATED WITH ADMINISTERING DPD INHIBITORS IN COMBINATION WITH 5-FU AND 5-FU PRODRUGS 有权与5-FU和5-FU PRODRUGS组合联合使用DPD抑制剂预防或降低神经毒性的方法公开(公告)号：US20110130359A1
公开(公告)日：2011-06-02
申请号：US12904974
申请日：2010-10-14
申请人： Thomas Spector
发明人： Thomas Spector
IPC分类号： A61K31/513 , A61K31/7068 , A61K31/7072 , A61P35/04
CPC分类号： A61K31/513 , A61K2300/00
摘要： Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme in both nervous and non-nervous tissues within the patient and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU generated from a prodrug is in substantial excess of DPD inhibitor in the patient.
摘要翻译： 提供了用于改进DPD抑制剂与5-FU和/或5-FU前药组合的给药和给药方法，包括首先向有需要的患者施用DPD抑制剂，其基本上消除了神经和非 - 患者内的神经组织，然后施用5-FU或5-FU前药，其中由前药产生的5-FU或5-FU的水平在患者体内显着超过DPD抑制剂。
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公开(公告)号：US06268374B1
公开(公告)日：2001-07-31
申请号：US08030259
申请日：1993-07-23
IPC分类号： A61K3170
CPC分类号： A61K31/70 , A61K9/0031 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/48 , A61K31/505 , A61K31/513 , A61K31/7072 , A61K45/06 , C07D239/54 , C07H19/06 , A61K2300/00
摘要： The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularly useful in cancer chemotherapy, especially in combination with antimetabolite antineoplastic agents such as 5-fluorouracil.
摘要翻译： 本发明涉及一组5-取代的尿嘧啶衍生物，其是尿嘧啶还原酶的灭活剂，并且其特别可用于癌症化疗，特别是与抗代谢药抗肿瘤剂如5-氟尿嘧啶组合。
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6.发明申请METHODS FOR ADMINISTERING DPD INHIBITORS IN COMBINATION WITH 5-FU AND 5-FU PRODRUGS 审中-公开用于联合5-FU和5-FU PRODRUGS的DPD抑制剂的施用方法公开(公告)号：US20130184232A1
公开(公告)日：2013-07-18
申请号：US13686240
申请日：2012-11-27
IPC分类号： A61K31/513
CPC分类号： A61K31/513 , A61K31/505 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
摘要翻译： 提供了用于改进DPD抑制剂与5-FU和/或5-FU前药组合的给药和给药方法，包括首先向有需要的患者施用基本上消除酶活性的DPD抑制剂，然后施用5-FU 或5-FU前药，其中5-FU或5-FU前药的水平在患者体内基本上超过DPD抑制剂。
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公开(公告)号：US5817664A
公开(公告)日：1998-10-06
申请号：US470317
申请日：1995-06-06
IPC分类号： A61K31/7105 , A61K20060101 , A61K31/505 , A61K31/513 , A61K31/70 , A61K45/00 , A61K45/06 , A61P35/00 , C07D239/54 , C07H19/06
CPC分类号： A61K31/70 , A61K31/505 , A61K31/513 , A61K31/7072 , A61K45/06 , A61K9/0031 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/48 , C07D239/54 , C07H19/06
摘要： The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularily useful in cancer chemotherapy, especially in combination with antimetabolite antineoplastic agents such as 5-fluorouracil (5-FU).
摘要翻译： 本发明涉及一种5-取代的尿嘧啶衍生物，其是尿嘧啶还原酶的灭活剂，其特别用于癌症化疗，特别是与抗代谢药抗肿瘤剂如5-氟尿嘧啶（5-FU）组合。
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公开(公告)号：US5393883A
公开(公告)日：1995-02-28
申请号：US832228
申请日：1992-02-07
申请人： Todd A. Blumenhopf , Thomas Spector , Devron R. Averett , Robert W. Morrison, Jr. , Eric C. Bigham , Virgil L. Styles
发明人： Todd A. Blumenhopf , Thomas Spector , Devron R. Averett , Robert W. Morrison, Jr. , Eric C. Bigham , Virgil L. Styles
IPC分类号： C07D473/16 , A61K31/415 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/52 , A61K31/522 , A61K31/535 , A61K31/70 , A61K45/06 , A61P31/12 , C07D213/53 , C07D213/78 , C07D417/00 , C07D473/18 , C07D473/32 , C07D413/00
CPC分类号： A61K45/06 , A61K31/52 , A61K31/70 , Y10S514/934
摘要： The present invention relates to novel ribonucleotide reductase inhibitors and new combinations comprising an antiviral compound, such as acyclovir, and a thiocarbonohydrazone ribonucleotide reductase inhibitor for the chemotherapeutic treatment of virus infections, especially viruses of the herpes group.
摘要翻译： 本发明涉及新型核糖核苷酸还原酶抑制剂和包含抗病毒化合物如阿昔洛韦和硫代碳腙腙核糖核苷酸还原酶抑制剂的新组合，用于化学治疗病毒感染，特别是疱疹病毒的病毒。
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9.发明授权Methods for administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs 有权给予DPD抑制剂与5-FU和5-FU前药组合的方法公开(公告)号：US08318756B2
公开(公告)日：2012-11-27
申请号：US11294643
申请日：2005-12-05
IPC分类号： A61K31/505
CPC分类号： A61K31/513 , A61K31/505 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
摘要翻译： 提供了用于改进DPD抑制剂与5-FU和/或5-FU前药组合的给药和给药方法，包括首先向有需要的患者施用基本上消除酶活性的DPD抑制剂，然后施用5-FU 或5-FU前药，其中5-FU或5-FU前药的水平在患者体内基本上超过DPD抑制剂。
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10.发明申请Methods for administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs 有权给予DPD抑制剂与5-FU和5-FU前药组合的方法公开(公告)号：US20060148753A1
公开(公告)日：2006-07-06
申请号：US11294643
申请日：2005-12-05
申请人： Thomas Spector , William Peters , Donald Kufe , Brian Huber
发明人： Thomas Spector , William Peters , Donald Kufe , Brian Huber
IPC分类号： A61K31/7072 , A61K31/513
CPC分类号： A61K31/513 , A61K31/505 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
摘要翻译： 提供了用于改进DPD抑制剂与5-FU和/或5-FU前药组合的给药和给药方法，包括首先向有需要的患者施用基本上消除酶活性的DPD抑制剂，然后施用5-FU 或5-FU前药，其中5-FU或5-FU前药的水平在患者体内基本上超过DPD抑制剂。
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