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1. 发明授权

US06245807B1 Treatment of human prostate disease 失效
标题翻译：治疗人类前列腺疾病
公开(公告)号：US06245807B1
公开(公告)日：2001-06-12
申请号：US09028400
申请日：1998-02-24
申请人： Arthur Pardee , Chiang J. Li
发明人： Arthur Pardee , Chiang J. Li
IPC分类号： C07D31182
CPC分类号： A61K31/352
摘要： We have now discovered that unexpectedly compounds of the following formulae I or 11 can be used to selectively stimulate the death of mammalian prostate cells, including both epithelial cell and prostate cancer cells, and thus are useful in treating prostate diseases: wherein R and R1 are each independently selected from the group consisting of hydrogen, hydroxy, thio (SH), halogen, substituted and unsubstituted alkyl, substituted and unsubstituted alkenyl, substituted and unsubstituted aryl, and substituted and unsubstituted alkoxy, and salts thereof, wherein the dotted double bond between the ring carbons to which R and R1 are bonded represent an optional ring double bond. Preferred compounds of formula I include those in which at least one of the substituents R and R1 is hydrogen and/or at least one of said substituents is allyl. Specifically preferred compounds include &bgr;-lapachone (i.e., R and R1 both being hydrogen), allyl-&bgr;-lapachone, particularly 3-allyl-&bgr;-lapachone (i.e. R being allyl and R1 being hydrogen) and 3-bromo-&bgr;-lapachone (i.e. R being bromo and R1 being hydrogen).
摘要翻译：我们现在已经发现意想不到的是，下列化学式I或11的化合物可用于选择性刺激哺乳动物前列腺细胞，包括上皮细胞和前列腺癌细胞的死亡，因此可用于治疗前列腺疾病：其中R和R1是各自独立地选自氢，羟基，硫代（SH），卤素，取代和未取代的烷基，取代和未取代的烯基，取代和未取代的芳基，以及取代和未取代的烷氧基及其盐，其中， R和R1键合的环碳代表任选的环双键。优选的式I化合物包括其中至少一个取代基R和R 1为氢和/或至少一个所述取代基的化合物为烯丙基。特别优选的化合物包括β-拉帕酮（即，R和R 2都是氢），烯丙基-β-拉帕酮，特别是3-烯丙基-β-拉帕酮（即，R是烯丙基，R 1是氢）和3-溴-β-拉帕酮（即R为溴，R 1为氢）。

2. 发明申请

US20060183793A1 Method of treating hematologic tumors and cancers 审中-公开
公开(公告)号：US20060183793A1
公开(公告)日：2006-08-17
申请号：US11315430
申请日：2005-12-21
申请人： Arthur Pardee , Kenneth Anderson , Deepak Gupta , Chiang Li , Youzhi Li
发明人： Arthur Pardee , Kenneth Anderson , Deepak Gupta , Chiang Li , Youzhi Li
IPC分类号： A61K31/353
CPC分类号： A61K45/06 , A61K31/136 , A61K31/337 , A61K31/352 , A61K31/353 , A61K31/4184 , A61K31/4745 , A61K31/475 , A61K31/704 , A61K31/7048 , A61K2300/00
摘要： Multiple myeloma and other hematologic tumors and/or malignancies can be treated by administration of a G1 and/or S phase drug, which is preferably β-lapachone, or a derivative or analog thereof, combined with a G2/M phase drug such as a taxane derivative, which is advantageously paclitaxel. This combination of the G1 and/or S phase drug with the G2/M phase drug results in an unexpectedly greater than additive (i.e., synergistic) apoptosis in multiple myeloma cells. The invention includes methods of treating multiple myeloma by administering the combination of the G1 and/or S phase drug and the G2/M phase drug, pharmaceutical compositions comprising the combination of drugs used in these methods, as well as pharmaceutical kits.

3. 发明申请

US20060078903A1 Methods and compositions for the diagnosis and treatment of cyclin A-1 associated conditions 有权
标题翻译：用于诊断和治疗细胞周期蛋白A-1相关病症的方法和组合物
公开(公告)号：US20060078903A1
公开(公告)日：2006-04-13
申请号：US11113644
申请日：2005-04-25
申请人： Heide Ford , Ricardo Coletta , Arthur Pardee , Justin Lamb
发明人： Heide Ford , Ricardo Coletta , Arthur Pardee , Justin Lamb
IPC分类号： C12Q1/68 , G01N33/574
CPC分类号： C12N15/113 , C12N2310/111 , C12N2310/14 , G01N33/57415 , G01N2333/9121
摘要： The present invention relates to compositions and methods for cancer therapeutics. In particular, the present invention provides compositions and methods for inhibiting cancer metastasis by inhibiting cyclin A1.
摘要翻译：本发明涉及癌症治疗剂的组合物和方法。特别地，本发明提供通过抑制细胞周期蛋白A1抑制癌症转移的组合物和方法。

4. 发明授权

US06960658B1 Maspin transcriptional regulatory sequences and uses thereof 失效
标题翻译： Maspin转录调控序列及其用途
公开(公告)号：US06960658B1
公开(公告)日：2005-11-01
申请号：US09617174
申请日：2000-07-17
申请人： Arthur Pardee , Ming Zhang
发明人： Ruth Sager
IPC分类号： C07K14/81 , C12Q1/68 , G01N33/574 , C07H21/04
CPC分类号： G01N33/57434 , C07K14/811 , C12Q1/6886 , C12Q1/6897 , C12Q2600/112 , C12Q2600/136 , G01N2333/811 , G01N2500/00
摘要： Isolated nucleic acid molecules that include transcriptional regulatory sequences of the maspin gene are described. These nucleic acid molecules are useful for identifying compounds and proteins that alter expression of maspin in mammary cells and other cell types.
摘要翻译：描述了包括maspin基因的转录调控序列的分离的核酸分子。这些核酸分子可用于鉴定改变乳腺细胞和其他细胞类型中maspin表达的化合物和蛋白质。

5. 发明申请

US20050171031A1 Method and composition for the treatment of cancer 审中-公开
标题翻译：治疗癌症的方法和组成
公开(公告)号：US20050171031A1
公开(公告)日：2005-08-04
申请号：US11069637
申请日：2005-03-01
申请人： Arthur Pardee , Chiang Li , Youzhi Li
发明人： Arthur Pardee , Chiang Li , Youzhi Li
IPC分类号： C07D311/92 , A61K31/122 , A61K31/337 , A61K31/35 , A61K31/352 , A61K31/4184 , A61K31/427 , A61K31/437 , A61K31/704 , A61K31/7042 , A61K38/00 , A61K45/00 , A61K45/06 , A61P35/00 , A61K31/7048 , A61K31/4745 , A61K31/404 , A61K31/12
CPC分类号： A61K31/337 , A61K31/122 , A61K31/35 , A61K45/06 , Y10S514/922 , A61K31/335 , A61K2300/00
摘要： We have discovered that the administration of a G1 and/or S phase drug such as β-lapachone in combination with a G2/M drug such as a taxane derivative such as paclitaxel resulted in a unexpected greater than additive (i.e., synergistic) reduction in the number of tumors (and tumor volume) as compared with the administration of these agents alone. In addition, no signs of toxicity or weight loss were observed. The present invention relates to a method for treating a mammalian tumor using combinations such as a taxane derivative, preferably paclitaxel, and a β-lapachone, or a derivative or analog thereof.
摘要翻译：我们已经发现，G1和/或S期药物如β-拉帕酮与G2 / M药物如紫杉烷衍生物如紫杉醇的组合的给药导致意想不到的大于添加剂（即协同）的减少与单独施用这些药物相比，肿瘤的数量（和肿瘤体积）。此外，没有观察到毒性或体重减轻的迹象。本发明涉及使用组合例如紫杉烷衍生物，优选紫杉醇和β-拉帕酮或其衍生物或类似物来治疗哺乳动物肿瘤的方法。

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