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1.发明申请Novel polyamine analog conjugates and quinone conjugates as therapies for cancers and prostate diseases 审中-公开新型多胺类似物共轭物和醌共轭物作为癌症和前列腺疾病的疗法公开(公告)号：US20040006049A1
公开(公告)日：2004-01-08
申请号：US10385224
申请日：2003-03-10
IPC分类号： A61K031/665 , A61K038/00
CPC分类号： C07D295/185 , A61K38/00 , A61K47/65 , C07C45/46 , C07C67/343 , C07C211/13 , C07C211/18 , C07C2601/02 , C07D207/34 , C07D219/10 , C07D235/18 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D493/04 , C07K5/1013 , C07K7/06 , C07C47/575 , C07C69/734
摘要： Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.
摘要翻译： 提供了其中细胞死亡和细胞生长抑制剂（例如多胺类似物或萘醌）与由诸如前列腺特异性抗原（PSA）和组织蛋白酶B之类的酶识别和切割的多肽缀合的肽缀合物，以及包含这些缀合物的组合物。 还提供了使用这些缀合物治疗前列腺疾病的方法。
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2.发明申请Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor 失效用于癌症治疗的环烷基取代多胺及其合成方法公开(公告)号：US20030195377A1
公开(公告)日：2003-10-16
申请号：US10313530
申请日：2002-12-06
发明人： Benjamin Frydman , Aldonia L. Valasinas , Andrei V. Blokhin , Aparajita Sarkar , Hirak S. Basu , Venodhar K. Reddy , Laurence J. Marton , Yu Wang
IPC分类号： C07C211/17
CPC分类号： A61K31/132 , C07C211/18 , C07C2601/02
摘要： Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
摘要翻译： 公开了可用于治疗由异常细胞增殖表现的癌症和其它疾病的构象限制性多胺化合物。 还公开了合成这些化合物的改进方法。 在本发明的一种方法中，含有含碳或含碳原子的化合物与烯烃化合物的双键反应形成环丙基环作为合成中的第一步。
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公开(公告)号：US20050010060A1
公开(公告)日：2005-01-13
申请号：US10909978
申请日：2004-08-02
申请人： Andrei Blokhin , Benjamin Frydman , Laurence Marton , Karen Neder , Jerry Sun
发明人： Andrei Blokhin , Benjamin Frydman , Laurence Marton , Karen Neder , Jerry Sun
IPC分类号： A61K38/00 , A61K47/48 , C07C45/00 , C07C45/46 , C07C46/00 , C07C50/32 , C07C67/343 , C07C69/708 , C07C69/96 , C07C229/22 , C07C233/31 , C07C237/22 , C07C255/54 , C07C305/20 , C07D207/34 , C07D219/10 , C07D235/18 , C07D295/185 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D487/22 , C07D493/04 , C07F9/12 , C07F9/655 , C07K5/103 , C07K7/06 , C07C50/10
CPC分类号： C07D295/185 , A61K38/00 , A61K47/65 , C07C45/00 , C07C45/46 , C07C46/00 , C07C50/32 , C07C67/343 , C07C69/708 , C07C69/96 , C07C229/22 , C07C233/31 , C07C237/22 , C07C255/54 , C07C305/20 , C07D207/34 , C07D219/10 , C07D235/18 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D493/04 , C07F9/12 , C07F9/65517 , C07F9/65522 , C07K5/1013 , C07K7/06 , C07C47/575 , C07C69/734
摘要： Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.
摘要翻译： 提供了新的醌，以及包含这些新型醌的组合物。 还提供了使用该类醌来治疗各种适应症（包括癌症）的方法。
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公开(公告)号：US20040192665A1
公开(公告)日：2004-09-30
申请号：US10627211
申请日：2003-07-25
IPC分类号： A61K031/555 , C07D487/22 , A61K031/409
CPC分类号： A61K41/0071 , A61K47/546
摘要： Conjugates of porphyrins with chemotherapeutic agents are disclosed, as well as methods of making the conjugates and methods of treating patients with the conjugates. Porphyrin compounds, such as mesoporphyrin IX, can be covalently linked to chemotherapeutic compounds, such as doxorubicin. The resulting conjugates display decreased systemic toxicity, while preserving the antineoplastic effects of the chemotherapeutic agent. The conjugates are thus useful in treating cancer and other diseases marked by uncontrolled cell proliferation.
摘要翻译： 公开了具有化学治疗剂的卟啉的缀合物，以及制备缀合物的方法和用缀合物治疗患者的方法。 卟啉化合物，如中卟啉IX，可以共同连接化学治疗化合物，如多柔比星。 所得到的缀合物显示降低的全身毒性，同时保护化疗剂的抗肿瘤作用。 因此，缀合物可用于治疗以不受控制的细胞增殖为特征的癌症和其它疾病。
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公开(公告)号：US20030130356A1
公开(公告)日：2003-07-10
申请号：US10272269
申请日：2002-10-16
发明人： Benjamin Frydman , Aldonia L. Valasinas , Andrei V. Blokhin , Hirak S. Basu , Laurence J. Marton
IPC分类号： A61K031/13 , C07C215/08
CPC分类号： C07C215/18 , C07C211/14
摘要： Oligoamine compounds with anti-cancer and anti-proliferative activity are provided, as well as methods for making and using the compounds. The compounds are shown to be active against prostate cancer cell lines and against prostate cancer tumors in mice. The compounds are also useful in treatment of breast cancer and other cancers.
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公开(公告)号：US20020183512A1
公开(公告)日：2002-12-05
申请号：US10139978
申请日：2002-05-06
发明人： Andrei V. Blokhin , Benjamin Frydman , Laurence J. Marton , Karen M. Neder , Jerry Shunneng Sun
IPC分类号： C07H015/04 , C07D211/06 , C07D223/04 , C07C050/12
CPC分类号： C07D295/185 , A61K38/00 , A61K47/65 , C07C45/00 , C07C45/46 , C07C46/00 , C07C50/32 , C07C67/343 , C07C69/708 , C07C69/96 , C07C229/22 , C07C233/31 , C07C237/22 , C07C255/54 , C07C305/20 , C07D207/34 , C07D219/10 , C07D235/18 , C07D307/79 , C07D307/92 , C07D311/92 , C07D317/70 , C07D493/04 , C07F9/12 , C07F9/65517 , C07F9/65522 , C07K5/1013 , C07K7/06 , C07C47/575 , C07C69/734
摘要： Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.
摘要翻译： 提供了新的醌，以及包含这些新型醌的组合物。 还提供了使用该类醌来治疗各种适应症（包括癌症）的方法。
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