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1. 发明授权

US07816544B2 Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species 有权
标题翻译：通过光化学生成氧化吡啶类物质合成罗卡酰胺天然产物
公开(公告)号：US07816544B2
公开(公告)日：2010-10-19
申请号：US10593502
申请日：2005-03-23
申请人： Guilford Jones, II , Baudouin Gerard , John A. Porco, Jr.
发明人： Guilford Jones, II , Baudouin Gerard , John A. Porco, Jr.
IPC分类号： C07D313/00 , C07D307/93 , C07D311/00
CPC分类号： C07D307/93 , C07D311/30 , C07D313/08 , C07D493/08
摘要： The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
摘要翻译：本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。特别地，新的仿生合成方法包括从3-羟基色酮衍生物光化学生成氧化吡啶鎓物质，随后将氧化吡啶类物质偶氮环加成到偶极子体。该方法可用于形成含有阿格林核心结构的加合物。还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-和B受体依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

2. 发明申请

US20110065786A1 SYNTHESIS OF ROCAGLAMIDE NATURAL PRODUCTS VIA PHOTOCHEMICAL GENERATION OF OXIDOPYRYLIUM SPECIES 审中-公开
标题翻译：通过氧化亚光谱物种的光化学生成合成山梨酰胺天然产物
公开(公告)号：US20110065786A1
公开(公告)日：2011-03-17
申请号：US12900874
申请日：2010-10-08
申请人： John A. Porco, JR. , Baudouin Gerard , Guilford Jones, II
发明人： John A. Porco, JR. , Baudouin Gerard , Guilford Jones, II
IPC分类号： A61K31/343 , C07D307/77 , A61P35/00
CPC分类号： C07D307/93 , C07D311/30 , C07D313/08 , C07D493/08
摘要： The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
摘要翻译：本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。特别地，新的仿生合成方法包括从3-羟基色酮衍生物光化学生成氧化吡啶鎓物质，随后将氧化吡啶类物质偶氮环加成到偶极子体。该方法可用于形成含有阿格林核心结构的加合物。还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。本发明还涉及用于制造用于治疗癌症或癌性病症的药物，与细胞过度增殖相关的病症或NF-和B受体依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

3. 发明申请

US20090299081A1 Asymmetric Synthesis of Rocaglamides via Enantioselective Photocycloaddition Mediated by Chiral Bronsted Acids 有权
标题翻译：通过手性布朗斯台德酸介导的对映选择性光环加成反应的罗卡胶的非对称合成
公开(公告)号：US20090299081A1
公开(公告)日：2009-12-03
申请号：US12301727
申请日：2007-05-21
申请人： John A. Porco, JR. , Baudouin Gerard
发明人： John A. Porco, JR. , Baudouin Gerard
IPC分类号： C07D307/77 , C07D313/06
CPC分类号： C07D317/12 , C07D307/93 , C07D317/72 , C07D493/08 , C07D493/10
摘要： The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
摘要翻译：本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。合成方法通常涉及在3-羟基色酮衍生物中光化学生成氧化吡啶鎓物质，随后在TADDOL衍生物存在下，将氧化吡啶类物质的对映选择性1,3-偶极环加成到偶极嗜酸细胞。该方法可用于形成含有阿格林核心结构的加合物。还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-κB依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

4. 发明授权

US08404088B2 Asymmetric synthesis of rocaglamides via enantioselective photocycloaddition mediated by chiral bronsted acids 有权
标题翻译：通过手性青涩酸介导的对映选择性光环加成不对称合成罗卡胶
公开(公告)号：US08404088B2
公开(公告)日：2013-03-26
申请号：US13423370
申请日：2012-03-19
申请人： John A. Porco, Jr. , Baudouin Gerard
发明人： John A. Porco, Jr. , Baudouin Gerard
IPC分类号： C07D311/94
CPC分类号： C07D317/12 , C07D307/93 , C07D317/72 , C07D493/08 , C07D493/10
摘要： The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
摘要翻译：本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。合成方法通常涉及在3-羟基色酮衍生物中光化学生成氧化吡啶鎓物质，随后在TADDOL衍生物存在下，将氧化吡啶类物质的对映选择性1,3-偶极环加成到偶极嗜酸细胞。该方法可用于形成含有阿格林核心结构的加合物。还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-和B受体依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

5. 发明申请

US20120238766A1 ASYMMETRIC SYNTHESIS OF ROCAGLAMIDES VIA ENANTIOSELECTIVE PHOTOCYCLOADDITION MEDIATED BY CHIRAL BRONSTED ACIDS 有权
标题翻译：不对称合成通过由CHIRAL BRONSTED ACIDS介导的选择性光合作用的聚酰胺
公开(公告)号：US20120238766A1
公开(公告)日：2012-09-20
申请号：US13423370
申请日：2012-03-19
申请人： John A. Porco, JR. , Baudouin Gerard
发明人： John A. Porco, JR. , Baudouin Gerard
IPC分类号： C07D307/93 , C07D311/94 , C07D313/08
CPC分类号： C07D317/12 , C07D307/93 , C07D317/72 , C07D493/08 , C07D493/10
摘要： The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
摘要翻译：本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。合成方法通常涉及在3-羟基色酮衍生物中光化学生成氧化吡啶鎓物质，随后在TADDOL衍生物存在下，将氧化吡啶类物质的对映选择性1,3-偶极环加成到偶极嗜酸细胞。该方法可用于形成含有阿格林核心结构的加合物。还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-和B受体依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

6. 发明申请

US20080177093A1 Synthesis of Rocaglamide Natural Products Via Photochemical Generation of Oxidopyrylium Species 有权
标题翻译：通过光化学生成氧化吡啶类物种合成罗格列酰胺天然产物
公开(公告)号：US20080177093A1
公开(公告)日：2008-07-24
申请号：US10593502
申请日：2005-03-23
申请人： Guilford Jones ll , Baudouin Gerard , John A. Porco Jr
发明人： Guilford Jones ll , Baudouin Gerard , John A. Porco Jr
IPC分类号： A61K31/335 , C07D307/93 , C07D311/30 , A61K31/34 , A61P35/00 , A61K31/35 , C07D313/08
CPC分类号： C07D307/93 , C07D311/30 , C07D313/08 , C07D493/08
摘要： The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
摘要翻译：本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。特别地，新的仿生合成方法包括从3-羟基色酮衍生物光化学生成氧化吡啶鎓物质，随后将氧化吡啶类物质偶氮环加成到偶极子体。该方法可用于形成含有阿格林核心结构的加合物。还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-κB依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

7. 发明申请

US20140275010A1 QUATERNARY SALTS 审中-公开
标题翻译：季刊
公开(公告)号：US20140275010A1
公开(公告)日：2014-09-18
申请号：US14204078
申请日：2014-03-11
申请人： Guo Zhu Zheng , Yuan Wang , Gregg F. Keany , Kenzo Arai , Kazunobu Kira , Xiang Liu , Nick Gearhart , Baudouin Gerard
发明人： Guo Zhu Zheng , Yuan Wang , Gregg F. Keany , Kenzo Arai , Kazunobu Kira , Xiang Liu , Nick Gearhart , Baudouin Gerard
IPC分类号： C07D407/06 , C07D405/14 , C07D487/08 , C07D487/10
CPC分类号： C07D407/06 , C07D405/14 , C07D487/08 , C07D487/10
摘要： The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.
摘要翻译：本发明提供季盐，如式I的那些：以及其在治疗癌症的方法中的用途。

8. 发明授权

US08137509B2 Asymmetric synthesis of rocaglamides via enantioselective photocycloaddition mediated by chiral brønsted acids 有权
标题翻译：通过手性布朗斯台德酸介导的对映选择性光环加成对罗卡胶的不对称合成
公开(公告)号：US08137509B2
公开(公告)日：2012-03-20
申请号：US12301727
申请日：2007-05-21
申请人： John A. Porco, Jr. , Baudouin Gerard
发明人： John A. Porco, Jr. , Baudouin Gerard
IPC分类号： C07D307/93 , C07D311/94
CPC分类号： C07D317/12 , C07D307/93 , C07D317/72 , C07D493/08 , C07D493/10
摘要： The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
摘要翻译：本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。合成方法通常涉及在3-羟基色酮衍生物中光化学生成氧化吡啶鎓物质，随后在TADDOL衍生物存在下，将氧化吡啶类物质的对映选择性1,3-偶极环加成到偶极嗜酸细胞。该方法可用于形成含有阿格林核心结构的加合物。还提供了将阿格林核心结构转化为阿格林，罗卡酰胺和巴格林环系统的方法。本发明还涉及用于制造用于治疗癌症或癌症病症的药物，与细胞过度增殖相关的疾病或NF-和B受体依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。

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