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1. 发明授权

US06316495B1 Method for inhibition of retroviral replication 有权
标题翻译：抑制逆转录病毒复制的方法
公开(公告)号：US06316495B1
公开(公告)日：2001-11-13
申请号：US09227392
申请日：1999-01-08
申请人： Ernest Kun , Kalman G. Buki
发明人： Ernest Kun , Kalman G. Buki
IPC分类号： A61K3135
CPC分类号： A61K31/47 , A61K31/12 , A61K31/365 , A61K31/37
摘要： A method for inhibition of retroviral replication by manipulation of enzyme adenosine diphosphoribosyl transferase which endogenously inhibits retroviral reverse transcriptase. The method is useful for prevention and treatment of retroviral infections, including HIV. The inhibition of the viral replication is achieved by administration to a mammal susceptible to or infected with a retrovirus drugs which specifically inhibit poly-ADP-ribosylation of adenosine diphosphoribosyl transferase.
摘要翻译：通过操纵内源性抑制逆转录病毒逆转录酶的酶腺苷二磷酸核糖转移酶来抑制逆转录病毒复制的方法。该方法可用于预防和治疗包括HIV在内的逆转录病毒感染。病毒复制的抑制通过给予对特异性抑制腺苷二磷酸核糖基转移酶的多聚-ADP-核糖基化的逆转录病毒药物敏感或感染的哺乳动物实现。

2. 发明授权

US07405227B2 Treatment of cancer 失效
标题翻译：治疗癌症
公开(公告)号：US07405227B2
公开(公告)日：2008-07-29
申请号：US11458379
申请日：2006-07-18
申请人： Ernest Kun , Jerome Mendeleyev , Carol Basbaurn , Hassan Lemjabbar-Alaoui , Valeria Ossovskaya
发明人： Ernest Kun , Jerome Mendeleyev , Carol Basbaurn , Hassan Lemjabbar-Alaoui , Valeria Ossovskaya
IPC分类号： A01N43/42 , A01N43/16 , C07D217/22 , C07D311/02
CPC分类号： A61K31/166 , A61K31/165 , A61K31/366 , A61K45/06 , A61K2300/00
摘要： Methods of treating ovarian cancer, endometrium cancer, cervical cancer, pancreatic cancer, bladder cancer, eve cancer, central nervous system cancer, thyroid cancer and lung cancer are disclosed. Specifically disclosed are methods of treating ovarian adenocarcinoma that has migrated into the abdominal cavity, a transitional cell carcinoma of the bladder, an epithelioid carcinoma in a pancreatic duct, an adenocarcinoma in a pancreatic duct, an adenocarcinoma in the cervical epithelium. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R1, R2, R3, R4, and R5 are described herein, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.
摘要翻译：公开了卵巢癌，子宫内膜癌，子宫颈癌，胰腺癌，膀胱癌，前夕癌，中枢神经系统癌，甲状腺癌和肺癌的治疗方法。具体公开的是治疗已经迁移到腹腔的卵巢腺癌，膀胱移行细胞癌，胰管上皮样癌，胰管腺癌，子宫颈上皮癌中的腺癌的方法。所述方法包括向患者施用治疗有效量的式（Ia）化合物，其中R 1，R 2，R 3， R 4和R 5在本文中描述，其中五个R 1，R 2，R 2， R 3，R 4和R 5取代基总是氢，五个取代基中的至少一个总是硝基，至少位于硝基附近的一个取代基总是碘，及其药学上可接受的盐。

3. 发明授权

US5516941A Specific inactivators of "retroviral" (asymmetric) zinc fingers 失效
标题翻译： “逆转录病毒”（不对称）锌指的特异性灭活剂
公开(公告)号：US5516941A
公开(公告)日：1996-05-14
申请号：US965541
申请日：1992-11-02
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 , C07C231/08
CPC分类号： A61K31/165 , A61K31/166 , A61K31/37 , A61K31/47 , A61K31/472 , 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。

4. 发明授权

US06326402B1 Methods for treating viral infections using a compound capable of inhibiting microtubules 有权
标题翻译：使用能够抑制微管的化合物治疗病毒感染的方法
公开(公告)号：US06326402B1
公开(公告)日：2001-12-04
申请号：US09133071
申请日：1998-08-12
申请人： Ernest Kun , Jerome Mendeleyev
发明人： Ernest Kun , Jerome Mendeleyev
IPC分类号： A61K3119
CPC分类号： A61K31/12 , A61K31/235 , A61K31/337
摘要： The present invention is directed to a method for inhibiting viral replication and treating viral infections by administering a pharmaceutically effective amount of a compound capable of binding a microtubule such as a diiodo thyronine analogue having no significant hormonal activity. The present invention also features novel pharmaceutical compositions comprising the same.
摘要翻译：本发明涉及通过施用药学上有效量的能够结合微管的化合物，例如没有显着激素活性的二碘型甲状腺类似物来抑制病毒复制和治疗病毒感染的方法。本发明还涉及包含其的新型药物组合物。

5. 发明授权

US6004978A Methods of treating cancer with aromatic nitro and nitroso compounds and their metabolites 失效
标题翻译：用芳香族硝基和亚硝基化合物及其代谢物治疗癌症的方法
公开(公告)号：US6004978A
公开(公告)日：1999-12-21
申请号：US473044
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 suppressants of cancer growth and viral infections in a mammalian host. The compounds are particularly useful for treatment and suppression 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。

6. 发明授权

US5652367A Halo-nitro-isoquinolinone compounds and pharmaceutical compositions thereof 失效
标题翻译：卤 - 硝基 - 异喹啉酮化合物及其药物组合物
公开(公告)号：US5652367A
公开(公告)日：1997-07-29
申请号：US474634
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 , C07D217/22
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 vital 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 vital 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重要感染的抑制剂。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重要疾病的方法。

7. 发明授权

US5519053A 5-Iodo-6-amino-1,2-Benzopyrones and their metabolites useful as cytostatic agents 失效
标题翻译： 5-碘-6-氨基-1,2-苯并吡喃及其代谢物可用作细胞抑制剂
公开(公告)号：US5519053A
公开(公告)日：1996-05-21
申请号：US21989
申请日：1993-02-24
申请人： Ernest Kun , Jerome Mendeleyev
发明人： Ernest Kun , Jerome Mendeleyev
IPC分类号： A61K31/365 , A61K31/37 , A61P35/00 , A61P43/00 , C07D311/14 , C07D311/18 , A61K31/35
CPC分类号： A61K31/37 , C07D311/14 , Y10S514/934
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-benzopryrones 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5-碘-6-氨基-1,2-苯并呋喃酮和/或其代谢物治疗致瘤性和病毒性疾病的方法。

8. 发明授权

US5464871A 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：US5464871A
公开(公告)日：1995-11-07
申请号：US76313
申请日：1993-06-11
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 , A61K31/24 , C07C207/04
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 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。

9. 发明申请

US20080319054A1 Treatment of Cancer 失效
标题翻译：癌症治疗
公开(公告)号：US20080319054A1
公开(公告)日：2008-12-25
申请号：US12165437
申请日：2008-06-30
申请人： Ernest Kun , Jerome Mendeleyev , Carol Basbaum , Hassan Lemjabbar-Alaoui , Valeria Ossovskaya
发明人： Ernest Kun , Jerome Mendeleyev , Carol Basbaum , Hassan Lemjabbar-Alaoui , Valeria Ossovskaya
IPC分类号： A61K31/353 , A61K31/166 , A61P35/00 , A61K31/197
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。

10. 发明申请

US20070015814A1 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：US20070015814A1
公开(公告)日：2007-01-18
申请号：US11423685
申请日：2006-06-12
申请人： Ernest Kun , Jerome Mendeleyev , Pal Bauer
发明人： Ernest Kun , Jerome Mendeleyev , Pal Bauer
IPC分类号： A61K31/404 , A61K31/366
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。

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