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21. 发明授权

US06753348B2 BTK inhibitors and methods for their identification and use 失效
标题翻译： BTK抑制剂及其鉴定和使用方法
公开(公告)号：US06753348B2
公开(公告)日：2004-06-22
申请号：US10115175
申请日：2002-04-02
申请人： Fatih M. Uckun , Ravi Malaviya
发明人： Fatih M. Uckun , Ravi Malaviya
IPC分类号： A61K31275
CPC分类号： A61K31/225 , A61K31/275 , A61K31/277 , A61K31/40 , A61K31/445 , A61K31/525
摘要： The invention provides BTK inhibitors, methods for their identification and use, and pharmaceutical compositions comprising BTK inhibitors, including allergy treatments.
摘要翻译：本发明提供了BTK抑制剂，其鉴定和使用方法，以及包含过敏治疗的包含BTK抑制剂的药物组合物。

22. 发明授权

US06727265B2 Phenoxyethyl-thiourea-pyridine compounds and their use for treatment of HIV-infections 失效
标题翻译：苯氧乙基 - 硫脲 - 吡啶化合物及其用于治疗艾滋病毒感染的用途
公开(公告)号：US06727265B2
公开(公告)日：2004-04-27
申请号：US10420032
申请日：2003-04-15
申请人： Fatih M. Uckun , Taracad K. Venkatachalam
发明人： Fatih M. Uckun , Taracad K. Venkatachalam
IPC分类号： A61K3144
CPC分类号： C07D213/75
摘要： The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.
摘要翻译：本发明提供抑制逆转录酶（RT）并抑制逆转录病毒如人免疫缺陷病毒-1（HIV-1）复制的化合物。本发明的化合物是苯氧基乙基 - 硫脲 - 吡啶。本发明另外提供了用于抑制逆转录病毒例如HIV-1的逆转录酶活性的方法，包括使逆转录病毒与本发明的化合物接触。本发明另外提供了一种抑制逆转录病毒如HIV-1复制的方法，其包括使逆转录病毒与本发明的化合物接触。

23. 发明授权

US06689793B2 Piperidinylethyl-, phenoxyethyl-, and &bgr;-fluorophenethyl-substituted thiourea compounds with potent anti-HIV activity 失效
标题翻译：哌啶基乙基，苯氧基乙基和β-氟苯乙基取代的硫脲化合物，具有很强的抗HIV活性
公开(公告)号：US06689793B2
公开(公告)日：2004-02-10
申请号：US10006300
申请日：2001-12-06
申请人： Fatih M. Uckun , Taracad K. Venkatachalam
发明人： Fatih M. Uckun , Taracad K. Venkatachalam
IPC分类号： A61K31445
CPC分类号： C07D213/75 , A61K31/44 , A61K31/4545
摘要： The present invention is directed to derivatives of piperidinylethyl, phenoxyethyl, and fluorophenethyl bromopyridyl thioureas, which have been found to be effective non-nucleoside inhibitors (NNRTI) of NNI-resistant and multi-drug resistant human immunodeficiency virus (HIV)-1 reverse transcriptase (RT). The present invention is further directed to methods of using the above derivatives to treat patients with NNI-resistant or multi-drug resistant human immunodeficiency virus (HIV)-1.
摘要翻译：本发明涉及哌啶基乙基，苯氧基乙基和氟苯乙基溴吡啶基硫脲的衍生物，其已经被发现是NNI抗性和多药耐药的人类免疫缺陷病毒（HIV）-1逆转录酶的有效非核苷抑制剂（NNRTI）（RT）。本发明还涉及使用上述衍生物治疗患有NNI抗性或多重耐药性人类免疫缺陷病毒（HIV）-1的患者的方法。

24. 发明授权

US06627655B2 Vanadium (IV) metallocene complexes having spermicidal activity 失效
标题翻译：钒（IV）金属茂配合物具有杀精活性
公开(公告)号：US06627655B2
公开(公告)日：2003-09-30
申请号：US10222594
申请日：2002-08-15
申请人： Osmond D'Cruz , Phalguni Ghosh , Fatih M. Uckun
发明人： Osmond D'Cruz , Phalguni Ghosh , Fatih M. Uckun
IPC分类号： A61K3128
CPC分类号： A61K31/555 , A61K31/28
摘要： Novel spermicidal compounds which are organometallic cyclopentadienyl metal complexes, particularly vanadium IV complexes, including their corresponding therapeutic compositions are described.
摘要翻译：描述了有机金属环戊二烯基金属络合物，特别是钒IV络合物的新型杀精子化合物，包括它们相应的治疗组合物。

25. 发明授权

US06605589B1 Cathepsin inhibitors in cancer treatment 失效
标题翻译：组织蛋白酶抑制剂在癌症治疗
公开(公告)号：US06605589B1
公开(公告)日：2003-08-12
申请号：US09539739
申请日：2000-03-31
申请人： Fatih M. Uckun , De-Min Zhu
发明人： Fatih M. Uckun , De-Min Zhu
IPC分类号： A01N3718
CPC分类号： A61K38/55
摘要： Embodiments of the present invention provide methods for inhibiting tumor cell growth, or treating cancer cells, in a subject through the administration of a cathepsin inhibitor or inhibitors. Methods for inhibiting inflammatory disease cells as well as other cathepsin expressing cells in a subject with a cathepsin inhibitor or inhibitors are also within the present invention. Furthermore, the present invention relates to inducing cytotoxicity or apoptosis in cells by administering a cytotoxic or an apoptotic dose of a cathepsin inhibitor or inhibitors to the cell. Finally, the present invention relates to the administering of cathepsin expressing vectors to tumor cells so as to inhibit the tumor cells growth.
摘要翻译：本发明的实施方案提供了通过施用组织蛋白酶抑制剂或抑制剂来抑制受试者的肿瘤细胞生长或治疗癌细胞的方法。用组织蛋白酶抑制剂或抑制剂抑制受试者中炎性疾病细胞以及其他组织蛋白酶表达细胞的方法也在本发明中。此外，本发明涉及通过向细胞施用细胞毒性或细胞凋亡剂量的组织蛋白酶抑制剂或抑制剂来诱导细胞中的细胞毒性或细胞凋亡。最后，本发明涉及向肿瘤细胞施用组织蛋白酶表达载体，以抑制肿瘤细胞生长。

26. 发明授权

US06552027B2 Quinazolines for treating brain tumor 失效
公开(公告)号：US06552027B2
公开(公告)日：2003-04-22
申请号：US09903294
申请日：2001-07-11
申请人： Fatih M. Uckun , Rama Krishna Narla , Xing-Ping Liu
发明人： Fatih M. Uckun , Rama Krishna Narla , Xing-Ping Liu
IPC分类号： A61K31517
CPC分类号： C07D239/94 , C07D239/88
摘要： Novel substituted quinozaline compounds and conjugates useful to inhibit the growth of brain tumor cells and to inhibit adhesion and migration of brain tumor cells. The compounds of the invention include 4-(3′-bromo-4′-hydroxy phenyl)-amino-6,7-dimethoxyquinazoline and this compound covalently bound to EGF.

27. 发明授权

US06512003B2 Synthetic spiroketal pyranes as potent anti-cancer agents and use 失效
公开(公告)号：US06512003B2
公开(公告)日：2003-01-28
申请号：US09974070
申请日：2001-10-09
申请人： Fatih M. Uckun , Chen Mao , He Huang
发明人： Fatih M. Uckun , Chen Mao , He Huang
IPC分类号： A61K3138
CPC分类号： C07D493/10 , C07C323/41 , C07D307/12 , C07D307/42 , C07K14/47
摘要： Novel tubulin binding compounds (SPIKETS) having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

28. 发明授权

US06372217B1 Methods for the treatment of CD7+ viral infection with TXU-7-PAP 失效
标题翻译：用TXU-7-PAP治疗CD7 +病毒感染的方法
公开(公告)号：US06372217B1
公开(公告)日：2002-04-16
申请号：US09014028
申请日：1998-01-27
申请人： Fatih M. Uckun
发明人： Fatih M. Uckun
IPC分类号： A61K3940
CPC分类号： A61K47/6849 , A61K47/6825
摘要： The present invention provides a novel biotherapeutic agent comprising a monoclonal antibody TXU-7, which is specific to the CD7 antigen, conjugated to the pokeweed antiviral protein (PAP). This immunoconjugate was designated TXU-7-PAP. The CD7 antigen is present on the surface of the majority of T-lymphocytes, including those that are the cellular target of the human immunodeficiency virus (HIV). The pokeweed antiviral protein displays broad spectrum antiviral activity toward various plant, animal, and human viruses, including HIV. Prior attempts to generate PAP immunoconjugates with anti-HIV activity have been unsuccessful due to the poor stability of the immunoconjugate in vivo. However, the TXU-7-PAP immunoconjugate described herein displayed potent antiviral activity against HIV-1 and low toxicity in various animal models. Preliminary clinical studies in HIV-1-infected patients demonstrated that the immunoconjugate was well-tolerated and reduced the HIV-1 viral load. Thus, this immunoconjugate is expected to improve the prognosis of HIV-1-infected patients.
摘要翻译：本发明提供了一种新颖的生物治疗剂，其包含与所述pokeweed抗病毒蛋白（PAP）缀合的CD7抗原特异性的单克隆抗体TXU-7。将该免疫缀合物命名为TXU-7-PAP。 CD7抗原存在于大多数T淋巴细胞的表面，包括那些是人类免疫缺陷病毒（HIV）的细胞靶标的抗原。 pokeweed抗病毒蛋白显示广泛的抗病毒活性对各种植物，动物和人类病毒，包括艾滋病毒。由于免疫缀合物在体内的稳定性差，以前尝试产生具有抗HIV活性的PAP免疫缀合物已经不成功。然而，本文所述的TXU-7-PAP免疫偶联物在各种动物模型中显示出针对HIV-1的有效抗病毒活性和低毒性。 HIV-1感染患者的初步临床研究表明，免疫缀合物具有良好的耐受性，降低了HIV-1病毒载量。因此，这种免疫缀合物有望改善HIV-1感染患者的预后。

29. 发明授权

US06329420B1 Tubulin binding compounds (COBRA) 失效
标题翻译：微管蛋白结合化合物（COBRA）
公开(公告)号：US06329420B1
公开(公告)日：2001-12-11
申请号：US09569314
申请日：2000-05-11
申请人： Fatih M. Uckun , Shyi-Tai M. Jan , Chen Mao
发明人： Fatih M. Uckun , Shyi-Tai M. Jan , Chen Mao
IPC分类号： A61K3138
CPC分类号： C07D493/10 , C07C323/41 , C07D307/12 , C07D307/42 , C07K14/47
摘要： Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.
摘要翻译：具有有效的微管蛋白解聚活性和对微管蛋白聚合的抑制活性的新型微管蛋白结合化合物。这些化合物是抑制细胞增殖的有效剂，例如在癌细胞中。该化合物适于与新的微管蛋白结合口袋相互作用，该口袋可用于筛选抗微管蛋白，抗增殖和抗癌药物。

30. 发明授权

US06258841B1 Tubulin binding compounds (COBRA) 失效
公开(公告)号：US06258841B1
公开(公告)日：2001-07-10
申请号：US09352649
申请日：1999-06-29
申请人： Fatih M. Uckun , Shyi-Tai M. Jan , Chen Mao
发明人： Fatih M. Uckun , Shyi-Tai M. Jan , Chen Mao
IPC分类号： C07D30712
CPC分类号： C07D493/10 , C07C323/41 , C07D307/12 , C07D307/42 , C07K14/47
摘要： Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

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