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1. 发明申请

WO2007001348A2 HETEROARYL-CONTAINING ISOFLAVONES AS AROMATASE INHIBITORS 审中-公开
标题翻译：含有异黄酮作为芳香酶抑制剂
公开(公告)号：WO2007001348A2
公开(公告)日：2007-01-04
申请号：PCT/US2005/030401
申请日：2005-08-26
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , BRUEGGEMEIER, Robert W. , KIM, Young-woo , HACKETT, John C.
发明人： BRUEGGEMEIER, Robert W. , KIM, Young-woo , HACKETT, John C.
IPC分类号： C07D311/04 , C07D311/74
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, SO 2 , and S(CH 2 ) n , wherein n = 1 - 10; R 1 and R 2 may be the same or different and are selected from H, OH, OCH 3 , OCH 2 CH 3 , OCH 2 C 6 H 5 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , CH(CH 3 ) 2 , C(CH 3 ) 3 , NO 2 , F, Cl, Br, CF 3 , SH, SCH 3 , SCH 2 CH 3 , OCOCH 3 , OCOC(CH 3 ) 3 , OCOCH 2 COOH, and CN; and R 3 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。本发明提供式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; R 1和R 2可以相同或不同，并且选自H，OH，OCH 3，OCH 2， CH 3，CH 2，CH 2，CH 2，NH 2，CH 2， NHCH 3，N（CH 3）2，CH 3，CH 2， CH 3 CH 3，CH 2 CH 2 CH 3，CH（CH 3 CH 3） C（CH 3）3，NO 2，F，Cl，Br，CF 3， 3，SH，SCH 3，SCH 2，CH 3，OCOCH 3，OCOC（CH 3 CO 3，COCO 2，CN; R 3是含氮杂环。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。

2. 发明申请

WO2009011811A1 COMPOSITIONS FROM GARCINIA AS AROMATASE INHIBITORS FOR BREAST CANCER CHEMOPREVENTION AND CHEMOTHERAPY 审中-公开
标题翻译：来自GARCINIA的组合物作为用于乳腺癌化疗和化疗的芳香酶抑制剂
公开(公告)号：WO2009011811A1
公开(公告)日：2009-01-22
申请号：PCT/US2008/008572
申请日：2008-07-14
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , BALUNAS, Marcy, J. , SU, Bin , BRUEGGEMEIER, Robert, W. , KINGHORN, Alan, Douglas
发明人： BALUNAS, Marcy, J. , SU, Bin , BRUEGGEMEIER, Robert, W. , KINGHORN, Alan, Douglas
IPC分类号： A01N65/00 , A61K36/00
CPC分类号： A61K36/38
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 Al 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）。公开了衍生自天然产物的新的AIs，用于治疗绝经后乳腺癌的临床效用，并且还可以作为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法证实了Al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。

3. 发明申请

WO2007001348A3 HETEROARYL-CONTAINING ISOFLAVONES AS AROMATASE INHIBITORS 审中-公开
标题翻译：含杂原子的异黄酮作为芳香化酶抑制剂
公开(公告)号：WO2007001348A3
公开(公告)日：2007-10-04
申请号：PCT/US2005030401
申请日：2005-08-26
申请人： UNIV OHIO STATE RES FOUND , BRUEGGEMEIER ROBERT W , KIM YOUNG-WOO , HACKETT JOHN C
发明人： BRUEGGEMEIER ROBERT W , KIM YOUNG-WOO , HACKETT JOHN C
IPC分类号： A01N43/00 , A61K31/424 , A61K31/497
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, SO 2 , and S(CH 2 ) n , wherein n = 1 - 10; R 1 and R 2 may be the same or different and are selected from H, OH, OCH 3 , OCH 2 CH 3 , OCH 2 C 6 H 5 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , CH(CH 3 ) 2 , C(CH 3 ) 3 , NO 2 , F, Cl, Br, CF 3 , SH, SCH 3 , SCH 2 CH 3 , OCOCH 3 , OCOC(CH 3 ) 3 , OCOCH 2 COOH, and CN; and R 3 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的化合物和方法，特别是激素依赖性乳腺癌。提供了式I的化合物：其中X选自O，N，S，SO，SO 2和S（CH 2）n SUB >，其中n = 1-10; R 1和R 2可以相同或不同，并且选自H，OH，OCH 3，OCH 2， SUB <3>，_{2 6 H _{5 ，NH _{2 ， NHCH <3>，N（CH _{3 ）_{2 ，CH _{3 ，CH _{2 CH _{3 ，CH _{2 CH _{2 CH _{3 ，CH（CH _{3 ） C，CH，SUB，F，Cl，Br，CF _{3， 3，SCH，SCH 3，SCH 2，SCH 3，SCH 3，SCH 3，SCH 3，SCH 3，SCH 3， 3），COCOCH 2，COOH和CN;其中，并且R 3是含氮杂环。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中的癌症的方法。还提供了一种合成2-取代异黄酮的方法，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; 第二步使2-（烷硫基）异黄酮脱保护; 第三次应用选择性去苄基化形成最终化合物。}}}}}}}}}}}}}

4. 发明申请

WO2006119148A3 KERATINOCYTE GROWTH FACTOR RECEPTOR - TYROSINE SPECIFIC INHIBITORS FOR THE PREVENTION OF CANCER METASTATIS 审中-公开
标题翻译：杀菌素生长因子受体 - 用于预防癌症分子的酪氨酸特异性抑制剂
公开(公告)号：WO2006119148A3
公开(公告)日：2007-11-08
申请号：PCT/US2006016530
申请日：2006-05-01
申请人： UNIV OHIO STATE RES FOUND , PENTO J THOMAS , LI PUI-KAU , BRUEGGEMEIER ROBERT W , HACKETT JOHN
发明人： PENTO J THOMAS , LI PUI-KAU , BRUEGGEMEIER ROBERT W , HACKETT JOHN
IPC分类号： A61K31/404 , A61K31/47 , C07D209/04 , C07D215/02
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 subject by administering a therapeutically effective amount of a keratinocyte growth facto receptor tyrosine kinase (KGFR TK) inhibitor to the subject in need of such treatment. Als provided are compounds and methods for the treating, inhibiting, or delaying the onset o metastasis in a subject with cancer by administering a therapeutically effective amount of 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事实受体酪氨酸激酶（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。提供的A1是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的化合物和方法。

5. 发明申请

WO2007120379A3 SULFONANILIDE ANALOGS AS SELECTIVE AROMATASE MODULATORS 审中-公开
公开(公告)号：WO2007120379A3
公开(公告)日：2007-10-25
申请号：PCT/US2007/003152
申请日：2007-02-05
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , BRUEGGEMEIER, Robert, W. , SU, Bin , DIAZ-CRUZ, Edgar, S. , LANDINI, Serena
发明人： BRUEGGEMEIER, Robert, W. , SU, Bin , DIAZ-CRUZ, Edgar, S. , LANDINI, Serena
IPC分类号： C07C307/02 , C07C233/00
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, cycloakyl, 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.

6. 发明申请

WO2006119148A2 KERATINOCYTE GROWTH FACTOR RECEPTOR - TYROSINE SPECIFIC INHIBITORS FOR THE PREVENTION OF CANCER METASTATIS 审中-公开
标题翻译：杀菌素生长因子受体 - 用于预防癌症分子的酪氨酸特异性抑制剂
公开(公告)号：WO2006119148A2
公开(公告)日：2006-11-09
申请号：PCT/US2006/016530
申请日：2006-05-01
申请人： THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION , PENTO, J. Thomas , LI, Pui-kau , BRUEGGEMEIER, Robert W. , HACKETT, John
发明人： PENTO, J. Thomas , LI, Pui-kau , BRUEGGEMEIER, Robert W. , HACKETT, John
IPC分类号： C07D403/02
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 subject by administering a therapeutically effective amount of a keratinocyte growth facto receptor tyrosine kinase (KGFR TK) inhibitor to the subject in need of such treatment. Als provided are compounds and methods for the treating, inhibiting, or delaying the onset o metastasis in a subject with cancer by administering a therapeutically effective amount of 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事实受体酪氨酸激酶（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。提供的Als是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的化合物和方法。

7. 发明申请

WO2007120379A2 SULFONANILIDE ANALOGS AS SELECTIVE AROMATASE MODULATORS 审中-公开
标题翻译：磺酰胺类似物作为选择性芳族化合物调节剂
公开(公告)号：WO2007120379A2
公开(公告)日：2007-10-25
申请号：PCT/US2007003152
申请日：2007-02-05
申请人： UNIV OHIO STATE RES FOUND , BRUEGGEMEIER ROBERT W , SU BIN , DIAZ-CRUZ EDGAR S , LANDINI SERENA
发明人： BRUEGGEMEIER ROBERT W , SU BIN , DIAZ-CRUZ EDGAR S , LANDINI SERENA
IPC分类号： 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, cycloakyl, 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。

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