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11. 发明授权

US5783599A Methods of treating cancer and viral infections with 5-iodo-6-amino-and 5-iodo-6-nitroso-1 2-benzopyrones 失效
标题翻译：用5-碘-6-氨基和5-碘-6-亚硝基-1-苯并吡喃酮治疗癌症和病毒感染的方法
公开(公告)号：US5783599A
公开(公告)日：1998-07-21
申请号：US607480
申请日：1996-02-27
申请人： Ernest Kun , Jerome Mendeleyev
发明人： Ernest Kun , Jerome Mendeleyev
IPC分类号： A61K31/366 , A61K31/37 , A61K31/35
CPC分类号： A61K31/37 , A61K31/366
摘要： Unsubstituted or substituted 5-iodo-6-amino-1,2-benzopyrones and their metabolites are potent, selective and non-toxic inhibitors and supressants of cancer growth and viral infections in a mammalian host. The compounds are particularly useful for treatment and supression of tumors and viruses associated with AIDS, herpetic episodes and cytomegaloviral infections. The methods of treatment of tumorigenic and viral diseases by 5-iodo-6-amino-1,2-benzopyrones and/or its metabolites are described.
摘要翻译：未取代或取代的5-碘-6-氨基-1,2-苯并吡喃及其代谢物是哺乳动物宿主中有效的选择性和无毒性抑制剂和癌症生长和病毒感染的抑制剂。该化合物特别可用于治疗和抑制与艾滋病，疱疹发作和巨细胞病毒感染相关的肿瘤和病毒。描述了通过5-碘-6-氨基-1,2-苯并吡喃和/或其代谢物治疗致瘤性和病毒性疾病的方法。

12. 发明授权

US5670518A Aromatic nitro and nitroso compounds and their metabolites useful as anti-viral and anti-tumor agents 失效
标题翻译：芳香族硝基和亚硝基化合物及其代谢物可用作抗病毒和抗肿瘤剂
公开(公告)号：US5670518A
公开(公告)日：1997-09-23
申请号：US473043
申请日：1995-06-06
申请人： Ernest Kun , Jerome Mendeleyev , Eva Kirsten
发明人： Ernest Kun , Jerome Mendeleyev , Eva Kirsten
IPC分类号： C07D217/24 , A61K31/04 , A61K31/05 , A61K31/055 , A61K31/06 , A61K31/12 , A61K31/135 , A61K31/165 , A61K31/37 , A61K31/47 , A61K31/472 , A61P31/12 , A61P35/00 , C07C205/13 , C07C205/45 , C07C231/02 , C07C233/65 , C07D311/14 , C07D311/18 , C07J41/00 , A61K31/35
CPC分类号： C07J41/0005 , C07C233/65 , C07D311/14 , C07J41/0044 , C07J41/0072
摘要： Unsubstituted or substituted halo nitro and nitroso compounds and their metabolites are potent, selective and non-toxic inhibitors and supressants of cancer growth and viral infections in a mammalian host. The compounds are particularly useful for treatment and supression of tumors and viruses associated with breast cancer, AIDS, herpetic episodes and cytomegaloviral infections. The methods of treatment of tumorigenic and viral diseases by halo nitro and nitroso compounds and their metabolites are described.
摘要翻译：未取代或取代的卤代硝基和亚硝基化合物及其代谢物是哺乳动物宿主中有效的选择性和无毒性抑制剂和癌症生长和病毒感染的抑制剂。该化合物特别可用于治疗和抑制与乳腺癌，AIDS，疱疹发作和巨细胞病毒感染相关的肿瘤和病毒。描述了通过卤代硝基和亚硝基化合物及其代谢物治疗致瘤性和病毒性疾病的方法。

13. 发明申请

US20090076122A1 PARP Modulators and Treatment of Cancer 审中-公开
标题翻译： PARP调节剂和癌症治疗
公开(公告)号：US20090076122A1
公开(公告)日：2009-03-19
申请号：US12326798
申请日：2008-12-02
申请人： Ernest KUN , Jerome MENDELEYEV , Pal BAUER
发明人： Ernest KUN , Jerome MENDELEYEV , Pal BAUER
IPC分类号： A61K31/404 , A61K31/352 , A61P35/00 , A61P25/00 , A61P3/00 , A61P37/00 , A61P29/00 , A61P31/12
CPC分类号： A61K31/366 , A61K31/404 , C07D209/08 , C07D209/16 , C07D311/10 , Y02A50/411
摘要： The invention relates to a method of modulating poly(ADP-ribose)polymerase-1 (PARP-1) activity in a mammal comprising administering to a mammal an effective amount of an organic aromatic compound having from 4 to about 35 carbon atoms, wherein said organic aromatic compound is capable of binding the arginine-34 moiety located in Zinc finger-1 of the PARP-1 enzyme and wherein said organic aromatic compound has electron donating capabilities such that it's π-electron system will interact with the positively charged (cationic) guanidinium moiety of the specific arginine-34 residue of the Zinc-1 finger of PARP-1 and does not contain benzamide or lactam substituents.In particular, substituted benzopyrones and substituted indoles and their pharmaceutical compositions containing such compounds that modulate the activity of PARP-1, are described. The invention is also directed to the composition of matter, kits and methods for their therapeutic and/or prophylactic use in treating diseases and disorders described herein, by administering effective amounts of such compounds. Preferably, the compositions and methods provided herein inhibit PARP activity.
摘要翻译：本发明涉及一种在哺乳动物中调节聚（ADP-核糖）聚合酶-1（PARP-1）活性的方法，包括向哺乳动物施用有效量的具有4-约35个碳原子的有机芳族化合物，其中所述有机芳族化合物能够结合位于PARP-1酶的锌指-1中的精氨酸-34部分，并且其中所述有机芳族化合物具有给电能力，使得其π电子系统将与带正电荷（阳离子）胍基部分的PARP-1锌锌指的特定精氨酸-34残基，不含有苯甲酰胺或内酰胺取代基。特别地，描述了取代的苯并吡喃酮和取代的吲哚及其含有调节PARP-1活性的化合物的药物组合物。本发明还涉及通过施用有效量的这些化合物来治疗和/或预防用于治疗本文所述疾病和病症的物质，试剂盒和方法的组合物。优选地，本文提供的组合物和方法抑制PARP活性。

14. 发明申请

US20070015837A1 Treatment of Cancer 失效
标题翻译：癌症治疗
公开(公告)号：US20070015837A1
公开(公告)日：2007-01-18
申请号：US11458379
申请日：2006-07-18
申请人： Ernest Kun , Jerome Mendeleyev , Carol Basbaurn , Hassan Lemjabbar-Alaoui , Valeria Ossovaskaya
发明人： Ernest Kun , Jerome Mendeleyev , Carol Basbaurn , Hassan Lemjabbar-Alaoui , Valeria Ossovaskaya
IPC分类号： A61K31/165
CPC分类号： A61K31/166 , A61K31/165 , A61K31/366 , A61K45/06 , A61K2300/00
摘要： The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.
摘要翻译：本发明提供了用于治疗癌症的物质，试剂盒和方法的组合物。特别地，本发明提供了通过抑制聚-ADP-核糖聚合酶来治疗受试者的癌症的组合物和方法，以及提供施用这种组合物的制剂和模式。

15. 发明授权

US6017958A Method of treating malignant tumors with thyroxine analogues having no significant hormonal activity 失效
标题翻译：用无明显激素活性的甲状腺素类似物治疗恶性肿瘤的方法
公开(公告)号：US6017958A
公开(公告)日：2000-01-25
申请号：US833272
申请日：1997-04-03
申请人： Ernest Kun , Jerome Mendeleyev
发明人： Ernest Kun , Jerome Mendeleyev
IPC分类号： A61P35/00 , A61K31/166 , A61K31/19 , A61K31/192 , A61K31/216 , A61K31/235 , C07C69/92 , A61K31/24
CPC分类号： A61K31/235 , A61K31/166 , A61K31/192 , C07C69/92
摘要： The present invention provides methods for treating cancer, particularly malignant tumors, with thyroxine analogues having no significant hormonal activity. A thyroxine analogue is administered to an afflicted mammal in an amount effective to cause depression or regression of malignant tumor growth or to treat cancer. Particularly preferred thyroxine analogues are those capable of causing about 35 percent or more inhibition of initial velocity of microtubule protein assembly in vitro.
摘要翻译：本发明提供了不具有显着激素活性的甲状腺素类似物治疗癌症，特别是恶性肿瘤的方法。将甲状腺素类似物以有效引起恶性肿瘤生长抑制或消退或治疗癌症的量施用于受影响的哺乳动物。特别优选的甲状腺素类似物是能够在体外引起约35％或更多抑制微管蛋白装配的初始速度的那些。

16. 发明授权

US5736576A Method of treating malignant tumors with thyroxine analogues having no significant hormonal activity 失效
标题翻译：用无明显激素活性的甲状腺素类似物治疗恶性肿瘤的方法
公开(公告)号：US5736576A
公开(公告)日：1998-04-07
申请号：US655267
申请日：1996-06-04
申请人： Ernest Kun , Jerome Mendeleyev
发明人： Ernest Kun , Jerome Mendeleyev
IPC分类号： A61K31/166 , A61K31/192 , A61K31/235 , C07C69/92 , A61K31/19 , C07C69/76
CPC分类号： A61K31/235 , A61K31/166 , A61K31/192 , C07C69/92
摘要： The present invention provides methods for treating cancer, particularly malignant tumors, with thyroxine analogues having no significant hormonal activity. A thyroxine analogue is administered to an afflicted mammal in an amount effective to cause depression or regression of malignant tumor growth or to treat cancer.
摘要翻译：本发明提供了不具有显着激素活性的甲状腺素类似物治疗癌症，特别是恶性肿瘤的方法。将甲状腺素类似物以有效引起恶性肿瘤生长抑制或消退或治疗癌症的量施用于受影响的哺乳动物。

17. 发明授权

US5482975A Adenosine diphosphoribose polymerase binding nitroso aromatic compounds useful as retroviral inactivating agents, anti-retroviral agents and anti-tumor agents 失效
标题翻译：可用作逆转录病毒灭活剂的腺苷二磷酸聚糖酶结合亚硝基芳香族化合物，抗逆转录病毒剂和抗肿瘤剂
公开(公告)号：US5482975A
公开(公告)日：1996-01-09
申请号：US21830
申请日：1993-02-24
申请人： Ernest Kun , Jerome Mendeleyev
发明人： Ernest Kun , Jerome Mendeleyev
IPC分类号： A61K31/165 , A61K31/166 , A61K31/37 , A61K31/47 , C07C233/65 , C07D217/24 , C07D311/18
CPC分类号： A61K31/472 , A61K31/165 , A61K31/166 , A61K31/37 , A61K31/47 , A61K31/4725 , C07C233/65 , C07D217/24 , C07D311/18
摘要： The subject invention provides for novel compounds for inactivating viruses. These compounds include 6-nitroso-1,2-benzopyrone, 3-nitrosobenzamide, 5-nitroso-1(2H)-isoquinolinone, 7-nitroso-1(2H)isoquinolinone, 8-nitroso-1(2H)isoquinolinone. The invention also provides for compositions containing one or more of the compounds, and for methods of treating viral infections, cancer, infectious virus concentration with the subject compounds and compositions.
摘要翻译：本发明提供了用于灭活病毒的新化合物。这些化合物包括6-亚硝基-1,2-苯并吡喃酮，3-亚硝基苯甲酰胺，5-亚硝基-1（2H） - 异喹啉酮，7-亚硝基-1（2H）异喹啉酮，8-亚硝基-1（2H）异喹啉酮。本发明还提供含有一种或多种化合物的组合物，以及用于治疗病毒感染，癌症，感染性病毒浓度与本发明化合物和组合物的方法的组合物。

18. 发明授权

US5262564A Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents 失效
标题翻译：用作逆转录病毒灭活剂的有机亚硝基化合物的亚磺酸加合物抗逆转录病毒剂和抗肿瘤剂
公开(公告)号：US5262564A
公开(公告)日：1993-11-16
申请号：US969874
申请日：1992-10-30
申请人： Ernest Kun , Jerome Mendeleyev
发明人： Ernest Kun , Jerome Mendeleyev
IPC分类号： A61K31/195 , C07C311/48 , C07C311/31 , A61K31/095
CPC分类号： A61K31/195 , C07C311/48
摘要： The subject invention provides for novel anti-tumor and anti-retroviral compounds. More specifically, the invention relates to the sulfinic acid adducts of therapeutic C-nitroso compounds. The formation of the adducts increases the stability and more solubility of the C-nitroso compounds. These compounds include the L-cysteinesulfinic acid adducts of 6-nitroso-1,2-benzopyrone and 3-nitrosobenzamide. The invention also provides for compositions containing one or more of the compounds, and for methods of treating retroviral infections, cancer, infectious virus concentration with the subject compounds and compositions.
摘要翻译：本发明提供了新的抗肿瘤和抗逆转录病毒化合物。更具体地，本发明涉及治疗性C-亚硝基化合物的亚磺酸加合物。加合物的形成增加了C亚硝基化合物的稳定性和更高的溶解度。这些化合物包括6-亚硝基-1,2-苯并吡喃酮和3-亚硝基苯甲酰胺的L-半胱氨酸亚磺酸加成物。本发明还提供含有一种或多种化合物的组合物，以及用于治疗逆转录病毒感染，癌症，感染性病毒浓度与本发明化合物和组合物的方法。

19. 发明授权

US5922775A Method of treating malignant tumors with ketone thyroxine analogues having no significant hormonal activity 失效
标题翻译：用无明显激素活性的甲状腺素类似物治疗恶性肿瘤的方法
公开(公告)号：US5922775A
公开(公告)日：1999-07-13
申请号：US956711
申请日：1997-10-23
申请人： Ernestt Kun , Jerome Mendeleyev , Kalman G. Buki
发明人： Ernestt Kun , Jerome Mendeleyev , Kalman G. Buki
IPC分类号： A61K31/12
CPC分类号： A61K31/12
摘要： The present invention provides methods for treating cancer, particularly malignant tumors, with ketone thyroxine analogues having no significant hormonal activity. A ketone thyroxine analogue is administered to an afflicted mammal in an amount effective to cause depression or regression of malignant tumor growth or to treat cancer. Particularly preferred ketone thyroxine analogues are those capable of causing about 35 percent or more inhibition of initial velocity of microtubule protein assembly in vitro.
摘要翻译：本发明提供了不具有显着激素活性的酮甲状腺素类似物治疗癌症，特别是恶性肿瘤的方法。将酮类甲状腺素类似物以有效引起恶性肿瘤生长抑制或消退或治疗癌症的量施用于受影响的哺乳动物。特别优选的酮甲状腺素类似物是能够在体外引起约35％或更多抑制微管蛋白装配的初始速度的那些。

20. 发明授权

US5877185A Synergistic compositions useful as anti-tumor agents 失效
标题翻译：可用作抗肿瘤剂的协同组合物
公开(公告)号：US5877185A
公开(公告)日：1999-03-02
申请号：US377584
申请日：1995-01-13
申请人： Ernest Kun , Jerome Mendeleyev , Eva Kirsten
发明人： Ernest Kun , Jerome Mendeleyev , Eva Kirsten
IPC分类号： A61K31/165 , A61K31/166 , A61K31/195 , A61K31/225 , A61K31/37 , A61K31/47 , A61K45/06 , C07C233/65 , C07D217/24 , C07D311/14 , C07D311/18 , C07J41/00 , A61K31/35 , C07D311/08
CPC分类号： A61K45/06 , A61K31/165 , A61K31/166 , A61K31/195 , A61K31/225 , A61K31/37 , A61K31/47 , A61K31/472 , A61K31/4725 , C07C233/65 , C07D217/24 , C07D311/14 , C07D311/18 , C07J41/0005 , C07J41/0044 , C07J41/0072
摘要： The subject invention provides for novel synergistic compositions useful for inactivating viruses or inducing apoptosis in tumor cells and for treating cancer or retroviral infections. Generally, the compositions comprise one or a plurality of ligands that oxidatively attack a zinc finger of pADPRT in combination with one or a plurality of agents selected from the group consisting of: agents that decrease cellular levels of glutathione and ligands that non-covalently bind to the nicotinamide site of pADPRT but do not effect zinc ejection from a zinc finger of pADPRT.
摘要翻译：本发明提供了可用于灭活病毒或诱导肿瘤细胞凋亡和治疗癌症或逆转录病毒感染的新型协同组合物。通常，组合物包含一种或多种氧化地攻击pADPRT的锌指的配体与一种或多种选自以下的试剂组合：降低谷胱甘肽的细胞水平和非共价结合的配体的试剂 pADPRT的烟酰胺位点，但不影响pADPRT锌指的锌排出。

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