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1. 发明申请

US20090181110A1 Compositions from Garcinia as Aromatase Inhibitors for Breast Cancer Chemoprevention and Chemotherapy 审中-公开
标题翻译：作为乳腺癌化学预防和化疗的藤黄酸作为芳香酶抑制剂的组合物
公开(公告)号：US20090181110A1
公开(公告)日：2009-07-16
申请号：US12169858
申请日：2008-07-09
申请人： Marcy J. Balunas , Bin Su , Robert W. Brueggemeier , Alan Douglas Kinghorn
发明人： Marcy J. Balunas , Bin Su , Robert W. Brueggemeier , Alan Douglas Kinghorn
IPC分类号： A61K36/38 , C12N9/99 , A61K31/352 , C12N9/00 , A61P35/00
CPC分类号： A61K36/38 , A23L33/105 , A23V2002/00 , A61K31/352 , A23V2250/2118 , A23V2200/308
摘要： Aromatase inhibitors (AIs) are disclosed which are useful in the treatment and prevention of post-menopausal breast cancer. New AIs derived from natural products are disclosed that are evaluated for clinical utility for treating post-menopausal breast cancer and may also act as chemopreventive agents for preventing breast cancer. Several pure compounds demonstrated AI activity using a noncellular, enzyme-based microsomal and a cell-based aromatase assay. Correlations are made between structural classes with levels of aromatase inhibition. The disclosure may be utilized to direct synthetic modification of natural product scaffolds to enhance aromatase inhibition or to standardize botanical dietary supplements for increased aromatase inhibition activity.
摘要翻译：公开了可用于治疗和预防绝经后乳腺癌的芳香酶抑制剂（AI）。公开了从天然产物衍生的新的AI，其被评估用于治疗绝经后乳腺癌的临床效用，并且还可以用作预防乳腺癌的化学预防剂。几种纯化合物使用非细胞，基于酶的微粒体和基于细胞的芳香酶测定来证明AI活性。在具有芳香酶抑制水平的结构类之间进行相关性。本公开可用于引导天然产物支架的合成修饰以增强芳香酶抑制或标准化植物性膳食补充剂以增加芳香酶抑制活性。

2. 发明授权

US07960548B2 Keratinocyte growth factor receptor—tyrosine specific inhibitors for the prevention of cancer metastatis 失效
标题翻译：角质形成细胞生长因子受体 - 酪氨酸特异性抑制剂用于预防癌症转移
公开(公告)号：US07960548B2
公开(公告)日：2011-06-14
申请号：US11414890
申请日：2006-05-01
申请人： J. Thomas Pento , Pui-Kai Li , Robert W. Brueggemeier , John C. Hackett
发明人： J. Thomas Pento , Pui-Kai Li , Robert W. Brueggemeier , John C. Hackett
IPC分类号： C07D471/02 , C07D215/22 , C07D215/227
CPC分类号： C07D209/34 , C07D215/22 , C07D215/227 , C07D215/48 , C07D403/06 , C07D491/04
摘要： Compounds and methods for treating, inhibiting, or delaying the onset of cancer in a subject by administering a therapeutically effective amount of a keratinocyte growth factor receptor tyrosine kinase (KGFR TK) inhibitor to the subject in need of such treatment. Also provided are compounds and methods for the treating, inhibiting, or delaying the onset of metastasis in a subject with cancer by administering a therapeutically effective amount of a KGFR TK inhibitor to the subject in need of such treatment.
摘要翻译：通过向需要这种治疗的受试者施用治疗有效量的角质形成细胞生长因子受体酪氨酸激酶（KGFR TK）抑制剂来治疗，抑制或延迟受试者的癌症发作的化合物和方法。还提供了通过向需要这种治疗的受试者施用治疗有效量的KGFR TK抑制剂来治疗，抑制或延迟患有癌症的受试者的转移起始的化合物和方法。

3. 发明授权

US07741520B2 Sulfonanilide analogs as selective aromatase modulators (SAMs) 失效
标题翻译：磺酰苯胺类似物作为选择性芳香酶调节剂（SAM）
公开(公告)号：US07741520B2
公开(公告)日：2010-06-22
申请号：US11702276
申请日：2007-02-05
申请人： Robert W Brueggemeier , Bin Su , Edgar S Diaz-Cruz , Serena Landini
发明人： Robert W Brueggemeier , Bin Su , Edgar S Diaz-Cruz , Serena Landini
IPC分类号： C07C311/10 , A61K31/18
CPC分类号： C07C233/75 , C07C233/25 , C07C233/60 , C07C255/57 , C07C311/08 , C07C311/21 , C07C2601/08 , C07C2601/14
摘要： Compounds and methods suppressing aromatase activity expression in cancer cells. Provided are compounds are those of formula I: wherein R1 may be alkyl, cycloalkyl, haloalkyl, aryl, substituted aryl, haloaryl, alkoxy, alkylaryl, and arylalkyl; R2 is H, alkyl, aryl, alkylaryl, arylalkyl, and cycloalkyl; R3, with the base nitrogen, forms an amide or sulfonamide; R4 is selected from nitro, amine, amide, and benzamide; or a pharmaceutically acceptable salts thereof. Also provided are small molecule selective aromatase inhibitors having a molecular weight of less 500 g/mol. In some embodiments, the small molecule selective aromatase inhibitors described herein have a molecular weight of less than 450 g/mol. Also provided are methods for suppressing aromatase activity expression in cancer cells comprising the step of administering a pharmaceutically effective amount of a small molecule aromatase inhibitor to a subject in need of such treatment. In one embodiment, the cancer cells are breast cancer cells.
摘要翻译：抑制癌细胞中芳香酶活性表达的化合物和方法。提供的化合物是式I的化合物：其中R 1可以是烷基，环烷基，卤代烷基，芳基，取代的芳基，卤代芳基，烷氧基，烷基芳基和芳基烷基; R2是H，烷基，芳基，烷基芳基，芳基烷基和环烷基; R3与碱式氮形成酰胺或磺酰胺; R4选自硝基，胺，酰胺和苯甲酰胺; 或其药学上可接受的盐。还提供了分子量小于500g / mol的小分子选择性芳香酶抑制剂。在一些实施方案中，本文所述的小分子选择性芳香酶抑制剂具有小于450g / mol的分子量。还提供了抑制癌细胞中芳香酶活性表达的方法，包括向需要这种治疗的受试者施用药学有效量的小分子芳香酶抑制剂的步骤。在一个实施方案中，癌细胞是乳腺癌细胞。

4. 发明申请

US20090253715A1 HETEROARYL-CONTAINING ISOFLAVONES AS AROMATASE INHIBITORS 失效
标题翻译：含有异黄酮作为芳香酶抑制剂
公开(公告)号：US20090253715A1
公开(公告)日：2009-10-08
申请号：US12471751
申请日：2009-05-26
申请人： Robert W. Brueggemeier , Young-Woo Kim , John C. Hackett
发明人： Robert W. Brueggemeier , Young-Woo Kim , John C. Hackett
IPC分类号： A61K31/506 , A61K31/4196 , A61K31/4164 , A61K31/40 , A61K31/4433 , A61P35/00
CPC分类号： C07D311/04 , C07D405/12
摘要： Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO2, and S(CH2)n, wherein n=1-10; R1 and R2 may be the same or different and are selected from H, OH, OCH3, OCH2CH3, OCH2C6H5, NH2, NHCH3, N(CH3)2, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, C(CH3)3, NO2, F, Cl, Br, CF3, SH, SCH3, SCH2CH3, OCOCH3, OCOC(CH3)3, OCOCH2COOH, and CN; and R3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.
摘要翻译：用于治疗和预防癌症，特别是激素依赖性乳腺癌的化合物和方法。提供式I化合物：其中X选自O，N，S，SO，SO 2和S（CH 2）n，其中n = 1-10; R1和R2可以相同或不同，选自H，OH，OCH3，OCH2CH3，OCH2C6H5，NH2，NHCH3，N（CH3）2，CH3，CH2CH3，CH2CH2CH3，CH（CH3）2，C（CH3）3 ，NO 2，F，Cl，Br，CF 3，SH，SCH 3，SCH 2 CH 3，OCOCH 3，OCOC（CH 3）3，OCOCH 2 COOH和CN; R3为含氮杂环。还提供了通过向需要治疗的受试者施用治疗有效量的含杂芳基的异黄酮或其药学上可接受的盐或前药来治疗或预防受试者的癌症的方法。还提供了通过首先使脱氧苯偶姻与相转移催化剂反应以提供2-（烷硫基）异黄酮来合成2-取代的异黄酮的方法; 第二次脱保护2-（烷硫基）异黄酮; 并且第三次施加选择性脱苄基以形成最终化合物。

5. 发明授权

US07572919B2 Heteroaryl-containing isoflavones as aromatase inhibitors 失效
标题翻译：含杂芳基的异黄酮作为芳香酶抑制剂
公开(公告)号：US07572919B2
公开(公告)日：2009-08-11
申请号：US11212229
申请日：2005-08-26
申请人： Robert W. Brueggemeier , Young-Woo Kim , John C. Hackett
发明人： Robert W. Brueggemeier , Young-Woo Kim , John C. Hackett
IPC分类号： C07D311/04 , C07D311/74 , C07D401/02
CPC分类号： C07D311/04 , C07D405/12
摘要： Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO2, and S(CH2)n, wherein n=1-10; R1 and R2 may be the same or different and are selected from H, OH, OCH3, OCH2CH3, OCH2C6H5, NH2, NHCH3, N(CH3)2, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, C(CH3)3, NO2, F, Cl, Br, CF3, SH, SCH3, SCH2CH3, OCOCH3, OCOC(CH3)3, OCOCH2COOH, and CN; and R3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.
摘要翻译：用于治疗和预防癌症，特别是激素依赖性乳腺癌的化合物和方法。提供式I化合物：其中X选自O，N，S，SO，SO 2和S（CH 2）n，其中n = 1-10; R1和R2可以相同或不同，选自H，OH，OCH3，OCH2CH3，OCH2C6H5，NH2，NHCH3，N（CH3）2，CH3，CH2CH3，CH2CH2CH3，CH（CH3）2，C（CH3）3 ，NO 2，F，Cl，Br，CF 3，SH，SCH 3，SCH 2 CH 3，OCOCH 3，OCOC（CH 3）3，OCOCH 2 COOH和CN; R3为含氮杂环。还提供了通过向需要治疗的受试者施用治疗有效量的含杂芳基的异黄酮或其药学上可接受的盐或前药来治疗或预防受试者的癌症的方法。还提供了通过首先使脱氧苯偶姻与相转移催化剂反应以提供2-（烷硫基）异黄酮来合成2-取代的异黄酮的方法; 第二次脱保护2-（烷硫基）异黄酮; 并且第三次施加选择性脱苄基以形成最终化合物。

6. 发明授权

US07105542B2 2-Heterosubstituted 3-aryl-4H-1-benzopyran-4-ones as novel therapeutics in breast cancer 失效
标题翻译： 2-取代的3-芳基-4H-1-苯并吡喃-4-酮作为乳腺癌中的新疗法
公开(公告)号：US07105542B2
公开(公告)日：2006-09-12
申请号：US10634463
申请日：2003-08-04
申请人： Robert W. Brueggemeier , Young-Woo Kim
发明人： Robert W. Brueggemeier , Young-Woo Kim
IPC分类号： A61K31/445 , C07D405/10
CPC分类号： C07D311/56
摘要： The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.
摘要翻译：本发明提供2-异取代的3-芳基-4H-苯并吡喃-4-酮化合物，用于治疗癌症，即乳腺癌。本发明还提供了可以在环境条件下进行的2-（烷硫基）异黄酮的合成方法。本发明还提供了从2-（烷硫基）异黄酮合成2-取代的3-芳基-4H-苯并吡喃-4-酮的方法。本发明还提供了使用2-异取代的3-芳基-4H-苯并吡喃-4-酮化合物治疗哺乳动物乳腺癌的方法。

7. 发明授权

US08476313B2 Heteroaryl-containing isoflavones as aromatase inhibitors 失效
公开(公告)号：US08476313B2
公开(公告)日：2013-07-02
申请号：US12471751
申请日：2009-05-26
申请人： Robert W. Brueggemeier , Young-Woo Kim , John C. Hackett
发明人： Robert W. Brueggemeier , Young-Woo Kim , John C. Hackett
IPC分类号： A61K31/352 , A61K31/44
CPC分类号： C07D311/04 , C07D405/12
摘要： Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO2, and S(CH2)n, wherein n=1-10; R1 and R2 may be the same or different and are selected from H, OH, OCH3, OCH2CH3, OCH2C6H5, NH2, NHCH3, N(CH3)2, CH3, CH2CH3, CH2CH2CH3, CH(CH3)2, C(CH3)3, NO2, F, Cl, Br, CF3, SH, SCH3, SCH2CH3, OCOCH3, OCOC(CH3)3, OCOCH2COOH, and CN; and R3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.

8. 发明授权

US07829557B2 2-heterosubstituted 3-aryl-4H-1-benzopyran-4-ones as novel therapeutics in breast cancer 失效
标题翻译： 2-异取代的3-芳基-4H-1-苯并吡喃-4-酮作为乳腺癌中的新型治疗剂
公开(公告)号：US07829557B2
公开(公告)日：2010-11-09
申请号：US11511192
申请日：2006-08-28
申请人： Robert W. Brueggemeier , Young-Woo Kim
发明人： Robert W. Brueggemeier , Young-Woo Kim
IPC分类号： A61K31/5377 , C07D413/02
CPC分类号： C07D311/56
摘要： The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.
摘要翻译：本发明提供2-异取代的3-芳基-4H-苯并吡喃-4-酮化合物，用于治疗癌症，即乳腺癌。本发明还提供了可以在环境条件下进行的2-（烷硫基）异黄酮的合成方法。本发明还提供了从2-（烷硫基）异黄酮合成2-取代的3-芳基-4H-苯并吡喃-4-酮的方法。本发明还提供了使用2-异取代的3-芳基-4H-苯并吡喃-4-酮化合物治疗哺乳动物乳腺癌的方法。

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