公开(公告)号：US07064114B2

公开(公告)日：2006-06-20

申请号：US09957434

申请日：2001-09-19

申请人： Seang Yiv ,  Mingshu Li ,  Osmond D'Cruz ,  Faith M. Uckun

发明人： Seang Yiv ,  Mingshu Li ,  Osmond D'Cruz ,  Faith M. Uckun

IPC分类号： A61K31/715 ,  A61K31/723 ,  A61K31/731

CPC分类号： A61K9/0034 ,  A61K9/06 ,  A61K9/1075

摘要： A pharmaceutical composition adapted for use as a spermicide, the composition comprising a gel-microemulsion comprising an oil-in-water microemulsion and a polymeric hydrogel. The gel-microemulsion can be used in a spermicidal method.Also, a gel-microemulsion pharmaceutical composition adapted for use as a formulation base for additional therapeutic agents. Examples of additional agents include, anti-microbial agents and spermicidal agents. Such gel-microemulsions with additional therapeutic agents can be used in methods for appropriate therapeutic treatment.Also, a gel-microemulsion pharmaceutical composition that is adapted for use as both a spermicide and formulation base for anti-microbial agents to provide a dual function contraceptive/anti-microbial formulation. Method of using such a composition as a dual function contraceptive/anti-microbial formulation are also included.

公开(公告)号：US06407078B1

公开(公告)日：2002-06-18

申请号：US09497297

申请日：2000-02-03

申请人： Osmond D'Cruz ,  Faith M. Uckun ,  Taracad Venkatachalam

发明人： Osmond D'Cruz ,  Faith M. Uckun ,  Taracad Venkatachalam

IPC分类号： A61K3170

CPC分类号： A61K31/7072 ,  C07H19/06 ,  C07H19/10

摘要： Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient contains a thymine ring (e.g. AZT) that has 5-halo, 6-alkoxy substitution. Additional improvements in anti-HIV activity for certain AZT derivatives are seen by providing the pentose ring of AZT with aryl phosphate substitution.

摘要翻译： 可以通过避孕组合物提供避孕活性以及抗病毒保护，所述避孕组合物含有基于嘧啶的核苷或具有杀精或精子固定活性的核苷酸。 在一个实例中，活性成分含有具有5-卤代，6-烷氧基取代的胸腺嘧啶环（例如AZT）。 通过提供AZT的戊糖环与芳基磷酸酯取代，可以看到某些AZT衍生物的抗HIV活性的进一步改善。

公开(公告)号：US06337348B1

公开(公告)日：2002-01-08

申请号：US09505386

申请日：2000-02-16

申请人： Faith M. Uckun ,  Osmond D'Cruz ,  Wanhong Dong

发明人： Faith M. Uckun ,  Osmond D'Cruz ,  Wanhong Dong

IPC分类号： A61K3128

CPC分类号： C07F9/005

摘要： Organometallic oxovanadium (IV) complexes having potent spermicidal activity, particularly those having at least one bidentate ligand. Preferred compounds are stable oxovanadium (IV) complexes having, as ancillary ligands linked via nitrogen or oxygen-metal bonds, bis and/or mono-1,10-phenanthroline; 2,2′-bipyridyl; or 2-hydroxyacetophenone.

摘要翻译： 有机金属氧化钒（IV）配合物具有有效的杀精活性，特别是具有至少一个二齿配体的那些。 优选的化合物是稳定的氧化钒（IV）络合物，其具有作为通过氮或氧 - 金属键连接的辅助配体，双和/或单-1,10-菲咯啉; 2,2'-联吡啶基 或2-羟基苯乙酮。

公开(公告)号：US06635651B2

公开(公告)日：2003-10-21

申请号：US10157474

申请日：2002-05-28

申请人： Faith M. Uckun

发明人： Faith M. Uckun

IPC分类号： A61K31517

CPC分类号： A61K31/00 ,  A61K31/517 ,  C07D239/94

摘要： The present invention describes a therapeutic method useful for treating or preventing a condition of platelet aggregation in a subject including administering a pharmaceutically effective amount of a compound or composition that inhibits JAK-3 and/or tyrosine phosphorylation of STAT-3 and inhibits thrombin induced platelet aggregation. The condition of platelet aggregation includes hematopoietic and cerbrovascular diseases.

公开(公告)号：US06335364B1

公开(公告)日：2002-01-01

申请号：US09352648

申请日：1999-06-29

申请人： Faith M. Uckun ,  Chen Mao ,  He Huang

发明人： Faith M. Uckun ,  Chen Mao ,  He Huang

IPC分类号： A61K3135

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.

摘要翻译： 新型微管蛋白结合化合物（SPIKETS）具有强大的微管蛋白解聚活性和对微管蛋白聚合的抑制活性。 这些化合物是抑制细胞增殖的有效剂，例如在癌细胞中。 该化合物适于与微管蛋白上的新型SP结合袋有利地相互作用，该口袋可用于筛选抗微管蛋白，抗增殖和抗癌药物。

公开(公告)号：US06737537B2

公开(公告)日：2004-05-18

申请号：US10146971

申请日：2002-05-15

申请人： Faith M. Uckun ,  Rama K. Narla

发明人： Faith M. Uckun ,  Rama K. Narla

IPC分类号： C07F1500

CPC分类号： C07F15/0093

摘要： The present invention describes platinum (II) compounds and compositions useful for treating a subject with a tumor and/or inducing apoptosis in a population of cells. The present invention also describes pharmaceutical compositions containing the aforementioned inventive compound(s) in combination with a pharmaceutically acceptable carrier. Additionally, the invention further provides a method of inducing apoptosis in a population of cells and a method of treating a subject with a tumor, wherein the method comprises administering to the subject a therapeutically effective amount of the aforementioned compound(s) or composition(s).

摘要翻译： 本发明描述了铂（II）化合物和用于治疗患有肿瘤的受试者和/或诱导细胞群中凋亡的组合物。 本发明还描述了含有上述本发明化合物与药学上可接受的载体组合的药物组合物。 另外，本发明还提供了诱导细胞群中细胞凋亡的方法和用肿瘤治疗受试者的方法，其中所述方法包括向受试者施用治疗有效量的上述化合物或组合物 ）。

公开(公告)号：US06362228B1

公开(公告)日：2002-03-26

申请号：US09742563

申请日：2000-12-20

申请人： Faith M. Uckun ,  Taracad K. Ventatachalam

发明人： Faith M. Uckun ,  Taracad K. Ventatachalam

IPC分类号： A61K3117

摘要： Novel phenylethyl-thiourea (PHET) compounds as inhibitors of reverse transcriptase and effective agents for the treatment of HIV infection, including mutant, drug-sensitive, drug-resistant, and multi-drug resistant strains of HIV.

公开(公告)号：US07071176B2

公开(公告)日：2006-07-04

申请号：US10726073

申请日：2003-12-01

申请人： Faith M. Uckun ,  Rakesh Vig

发明人： Faith M. Uckun ,  Rakesh Vig

IPC分类号： A61K31/685 ,  C07F9/6512

CPC分类号： A61K31/7052 ,  C07H19/10 ,  C07H19/20 ,  Y10S514/885

摘要： Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.

摘要翻译： 在芳基上具有对溴取代的d4T的芳基磷酸酯衍生物显示出作为抗HIV剂的效力显着增加，而没有不希望的细胞毒性活性水平。 特别地，这些衍生物是HIV逆转录酶的有效抑制剂。 在本发明的优选方面，磷酸芳基基团的磷进一步被可被酯化或取代的氨基酸残基取代，例如甲氧基乙酰基。

公开(公告)号：US06482816B1

公开(公告)日：2002-11-19

申请号：US09723220

申请日：2000-11-27

申请人： Faith M. Uckun ,  Xing-Ping Liu

发明人： Faith M. Uckun ,  Xing-Ping Liu

IPC分类号： C07C24510

CPC分类号： C07F9/80

摘要： Novel organic arsenic compounds are described as cytotoxic agents with potent anti-tumor activity against cancer cells and particularly, with regard to human leukemic cells and breast cancer cells.

摘要翻译： 新型有机砷化合物被描述为对癌细胞具有强抗肿瘤活性的细胞毒性剂，特别是关于人类白血病细胞和乳腺癌细胞。

公开(公告)号：US06262053B1

公开(公告)日：2001-07-17

申请号：US09338679

申请日：1999-06-23

申请人： Faith M. Uckun ,  Xing-Ping Liu ,  Rama Narla

发明人： Faith M. Uckun ,  Xing-Ping Liu ,  Rama Narla

IPC分类号： A61K3153

CPC分类号： C07D251/70

摘要： Novel pharmaceutical compositions including melamine derivatives and methods for the treatment of cancer including prostate, brain, breast, and leukemia are described. The methods are directed to administering a therapeutically effective amount of a pharmaceutical composition including melamine derivatives having potent cytotoxic activity.

摘要翻译： 描述了包括三聚氰胺衍生物和用于治疗癌症的方法的新型药物组合物，包括前列腺，脑，乳腺和白血病。 该方法涉及给予治疗有效量的药物组合物，包括具有强力细胞毒活性的三聚氰胺衍生物。