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1. 发明授权

US07122573B2 Analogs of green tea polyphenols as chemotherapeutic and chemopreventive agents 有权
标题翻译：绿茶多酚类似物作为化学治疗剂和化学预防剂
公开(公告)号：US07122573B2
公开(公告)日：2006-10-17
申请号：US10313968
申请日：2002-12-06
申请人： Nurulain Zaveri , Wan-Ru Chao , Ahlem Bensari
发明人： Nurulain Zaveri , Wan-Ru Chao , Ahlem Bensari
IPC分类号： C07D311/02 , A61K31/352
CPC分类号： C07D311/62
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of polyphenol catechins that occur in green tea, such as epigallocatichin-3-gallate (EGCG), and have the structure of formula (I) wherein R1 through R11 are defined herein. Preferred R4 moieties are selected from O, S, NH and CH2, and in exemplary compounds, R4 is O and R5 is a tri-substituted aroyloxy substituent, such as a 3,4,5-substituted benzoyloxy group. Pharmaceutical compositions are provided as well, as are methods of chemotherapy and chemoprevention.
摘要翻译：提供了可用作化学治疗和化学预防剂的新型化合物。这些化合物是在绿茶中发生的多酚儿茶素类似物，如表没食子儿茶素-3-没食子酸酯（EGCG），并具有式（I）的结构，其中R 1至R 11， / SUP>。优选的R 4部分选自O，S，NH和CH 2，在示例性化合物中，R 4是O，R SUP > 5是三取代的芳氧基取代基，例如3,4,5-取代的苯甲酰氧基。也提供药物组合物，以及化疗和化学预防的方法。

2. 发明授权

US07109236B2 Analogs of green tea polyphenols as chemotherapeutic and chemopreventive agents 有权
公开(公告)号：US07109236B2
公开(公告)日：2006-09-19
申请号：US10731690
申请日：2003-12-08
申请人： Nurulain Zaveri , Wan-Ru Chao , Ahlem Bensari
发明人： Nurulain Zaveri , Wan-Ru Chao , Ahlem Bensari
IPC分类号： C07D311/02 , A61K31/352
CPC分类号： C07D311/62
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of polyphenol catechins that occur in green tea, such as epigallocatichin-3-gallate (EGCG), and have the structure of formula (I) wherein R1 through R11 are defined herein. Preferred R4 moieties are selected from O, S, NH and CH2, and in exemplary compounds, R4 is O and R5 is a tri-substituted aroyloxy substituent, such as a 3,4,5-substituted benzoyloxy group. Pharmaceutical compositions are provided as well, as are methods of chemotherapy and chemoprevention.

3. 发明授权

US07329687B2 Flavanoid compounds as chemotherapeutic, chemopreventive, and antiangiogenic agents 失效
标题翻译：类黄酮化合物作为化学治疗，化学预防和抗血管生成剂
公开(公告)号：US07329687B2
公开(公告)日：2008-02-12
申请号：US10418736
申请日：2003-04-18
申请人： Nurulain Zaveri , Wan-Ru Chao
发明人： Nurulain Zaveri , Wan-Ru Chao
IPC分类号： C07D311/00 , C07D311/94 , C07D311/82 , A61K31/35 , A61K31/355
CPC分类号： C07C45/30 , C07C45/46 , C07C45/71 , C07C45/74 , C07C49/835 , C07C49/84 , C07D311/32 , C07D311/92 , C07D311/94 , C07D491/04 , C07C47/575 , C07C49/83
摘要： Compounds useful as chemotherapeutic, chemopreventive, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones. The compounds have the structure of formula (I) wherein R1 through R3 and R5 through R11 are defined herein, and α, β, and γ are optional bonds, providing that when α is absent, β is present, and when β is absent, α is present. When α is present, preferred R4 moieties are selected from O, S, NH and CH2, and when α is absent, preferred R4 groups are selected from OH, SH, NH2 and CH3. When γ is present, the preferred R5 substituent is O, while when γ is absent, the preferred R5 substituent is OH. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
摘要翻译：提供了可用作化学治疗，化学预防和抗血管生成剂的化合物。化合物是类黄酮，包括黄烷酮，黄烷醇和查尔酮。化合物具有式（I）的结构，其中R 1至R 3和R 5至R 11中的至少一个在本文中定义，并且α，β和γ是任选的键，条件是当α不存在时，存在β，当β不存在时，存在α。当存在α时，优选的R 4部分选自O，S，NH和CH 2，当不存在α时，优选的R 4 O >基团选自OH，SH，NH 2和CH 3。当存在γ时，优选的R 5取代基是O，而当不存在γ时，优选的R 5取代基是OH。还提供药物组合物，以及合成和使用的方法。

4. 发明申请

US20120252773A1 Method and composition for inhibiting cell proliferation and angiogenesis 审中-公开
标题翻译：抑制细胞增殖和血管生成的方法和组合物
公开(公告)号：US20120252773A1
公开(公告)日：2012-10-04
申请号：US13457416
申请日：2012-04-26
申请人： Khalid Amin , Joy M. Calaoagan , Wan-Ru Chao , Peter D. Hobbs , Keith R. Laderoute , Richard H. Peters , Masato Tanabe
发明人： Khalid Amin , Joy M. Calaoagan , Wan-Ru Chao , Peter D. Hobbs , Keith R. Laderoute , Richard H. Peters , Masato Tanabe
IPC分类号： A61K31/573 , C12N5/071 , A61P29/00 , A61P35/00 , A61K31/58 , A61P27/02
CPC分类号： A61K31/56
摘要： A method is provided for treating a patient with a medical condition that involves angiogenesis or HIF-1 overexpression with a compound having the structure of formula (I) wherein Z, x, y, and R1 through R11 are as defined herein.
摘要翻译：提供了一种治疗患有涉及血管生成或HIF-1过表达的医学病症的患者的方法，其具有式（I）结构的化合物，其中Z，x，y和R 1至R 11如本文所定义。

5. 发明授权

US07772218B2 Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one 有权
标题翻译：从21-羟基-19-去甲孕烯-4-烯-3-酮合成抗雌激素和其它治疗类固醇
公开(公告)号：US07772218B2
公开(公告)日：2010-08-10
申请号：US10915302
申请日：2004-08-09
申请人： Richard H. Peters , Jyanwei Liu , John G. Johansson , Kenneth J. Ryan , Wan-Ru Chao , Masato Tanabe
发明人： Richard H. Peters , Jyanwei Liu , John G. Johansson , Kenneth J. Ryan , Wan-Ru Chao , Masato Tanabe
IPC分类号： C07J41/00 , C07J43/00
CPC分类号： C07J1/00 , C07J5/00
摘要： Syntheses of steroids such as 3-hydroxy-7α-methyl-21-[2′-methoxy-4′-(diethylaminomethyl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate (“SR 16234”) and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.
摘要翻译：类固醇如3-羟基-7α-甲基-21- [2'-甲氧基-4' - （二乙基氨基甲基） - 苯氧基] -19-去甲基-1,3,5（10）柠檬酸三烯酸盐（“SR 16234” ）及其类似物，其中21-羟基-19-去甲基-4-烯-3-酮用作原料或中间体。后一种化合物可以容易地由雌酮-3-甲基醚制备。这些合成中的某些中间体也具有作为治疗剂的价值，例如在前列腺疾病如前列腺癌的治疗中。

6. 发明授权

US06503896B1 Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权
公开(公告)号：US06503896B1
公开(公告)日：2003-01-07
申请号：US09872826
申请日：2001-05-31
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： A61K3156
CPC分类号： C07J41/0072 , A61K9/02 , C07J41/0077 , C07J43/003
摘要： Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.

7. 发明授权

US06281205B1 Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use 有权
标题翻译：抗雌激素类固醇，以及相关的药物组合物和使用方法
公开(公告)号：US06281205B1
公开(公告)日：2001-08-28
申请号：US09220408
申请日：1998-12-24
申请人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
发明人： Masato Tanabe , Richard H. Peters , Wan-Ru Chao , Ling Jong
IPC分类号： A61K3156
CPC分类号： C07J41/00 , A61K9/02 , C07J41/0072 , C07J41/0077 , C07J43/003
摘要： Novel anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependent disorders. Preferred compounds have a 1,3,5(10)-estratriene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5(10)-estratrienes. Therapeutic methods and pharmaceutical compositions are provided as well.
摘要翻译：提供了新的抗雌激素化合物，其可用于治疗多种疾病，特别是雌激素依赖性疾病。优选的化合物具有1,3,5（10） - 三亚甲基核，并且在C-17或C-11位置被分子部分取代，这使得化合物有效地竞争性阻断雌激素与其受体的结合。特别优选的化合物是17-脱氧-1,3,5（10） - 雌三烯。也提供治疗方法和药物组合物。

8. 发明授权

US07078427B2 Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents 有权
标题翻译：吲哚-3-甲醇代谢物的类似物作为化学治疗和化学预防剂
公开(公告)号：US07078427B2
公开(公告)日：2006-07-18
申请号：US10772036
申请日：2004-02-03
申请人： Ling Jong , Wan-Ru Chao
发明人： Ling Jong , Wan-Ru Chao
IPC分类号： A61K31/40 , C07D209/02
CPC分类号： C07D487/04 , C07D209/08 , C07D209/30 , C07D209/42
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
摘要翻译：提供了可用作化学治疗和化学预防剂的新型化合物。化合物是吲哚-3-甲醇代谢物的类似物，其中选择化合物的结构和取代基以增强化合物的总体功效，特别是关于治疗活性，口服生物利用度，长期安全性，患者耐受性和治疗窗口。这些化合物不仅可用于治疗癌症，还可用于预防癌症。一类优选的新化合物具有式（I）的结构，其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7，R 8，R 8， 9，R 10，R 11和R 12在本文中定义。还提供药物组合物，以及合成和使用的方法。

9. 发明申请

US20060128785A1 Analogs of indole-3-carbinol metabolites as chemotherapeutic and chemopreventive agents 有权
标题翻译：吲哚-3-甲醇代谢物的类似物作为化学治疗和化学预防剂
公开(公告)号：US20060128785A1
公开(公告)日：2006-06-15
申请号：US11350232
申请日：2006-02-07
申请人： Ling Jong , Wan-Ru Chao
发明人： Ling Jong , Wan-Ru Chao
IPC分类号： A61K31/405 , C07D403/14
CPC分类号： C07D487/04 , C07D209/08 , C07D209/30 , C07D209/42
摘要： Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer. One preferred class of the novel compounds have the structure of formula (III) wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, R20, and R21 are defined herein. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.
摘要翻译：提供了可用作化学治疗和化学预防剂的新型化合物。化合物是吲哚-3-甲醇代谢物的类似物，其中选择化合物的结构和取代基以增强化合物的总体功效，特别是关于治疗活性，口服生物利用度，长期安全性，患者耐受性和治疗窗口。这些化合物不仅可用于治疗癌症，还可用于预防癌症。一类优选的化合物具有式（III）的结构，其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7，R 8，R 8， 11，R 12，R 20和R 21在本文中定义。还提供药物组合物，以及合成和使用的方法。

10. 发明申请

US20050009801A1 Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one 有权
标题翻译：从21-羟基-19-去甲孕烯-4-烯-3-酮合成抗雌激素和其它治疗类固醇
公开(公告)号：US20050009801A1
公开(公告)日：2005-01-13
申请号：US10915302
申请日：2004-08-09
申请人： Richard Peters , Jyanwei Liu , John Johansson , Kenneth Ryan , Wan-Ru Chao , Masato Tanabe
发明人： Richard Peters , Jyanwei Liu , John Johansson , Kenneth Ryan , Wan-Ru Chao , Masato Tanabe
IPC分类号： A61P5/36 , C07J1/00 , C07J5/00 , A61K31/58 , A61K31/56
CPC分类号： C07J1/00 , C07J5/00
摘要： Syntheses of steroids such as 3-hydroxy-7α-methyl-21-[2′-methoxy-4′-(diethylaminomethyl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate (“SR 16234”) and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.
摘要翻译：类固醇如3-羟基-7α-甲基-21- [2'-甲氧基-4' - （二乙基氨基甲基） - 苯氧基] -19-去甲基-1,3,5（10）三烯柠檬酸盐（“SR 16234” ）及其类似物，其中21-羟基-19-去甲基-4-烯-3-酮用作原料或中间体。后一种化合物可以容易地由雌酮-3-甲基醚制备。这些合成中的某些中间体也具有作为治疗剂的价值，例如在前列腺疾病如前列腺癌的治疗中。

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