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1. 发明申请

US20120035253A1 CRYSTALLINE FORMS OF GENISTEIN 有权
标题翻译：基因组的结晶形式
公开(公告)号：US20120035253A1
公开(公告)日：2012-02-09
申请号：US13133085
申请日：2009-12-11
申请人： Anders Berkenstam , Stefan Rehnmark , Michael-Robin Witt , Keith Lorimer , Stephen Watt
发明人： Anders Berkenstam , Stefan Rehnmark , Michael-Robin Witt , Keith Lorimer , Stephen Watt
IPC分类号： A61K31/352 , A61P35/00 , A61P31/00 , A61P43/00 , A61P11/00 , C07D311/36 , A61P29/00
CPC分类号： A61K31/353 , A61K31/352 , C07B2200/13 , C07D311/22
摘要： The disclosure relates to new crystalline forms of genistein. The disclosed crystalline forms include crystalline genistein sodium salt dihydrate; crystalline genistein potassium salt dihydrate; crystalline genistein calcium salt; crystalline genistein magnesium salt; crystalline genistein L-lysine salt; crystalline genistein N-methylglucamine salt; crystalline genistein N-ethylglucamine salt; crystalline genistein diethylamine salt; and crystalline genistein monohydrate. The disclosure also relates to the novel genistein salts represented by these crystalline forms. Therapeutic compositions containing at least one of these crystalline forms of genistein and/or a genistein salt and a pharmaceutically acceptable carrier are described. The disclosure also relates to methods of treating cancer comprising the step of administering to a patient in need thereof a therapeutically effective amount of a therapeutic composition containing the compounds of the disclosure, of a crystalline form of genistein, or of a genistein salt.
摘要翻译：本公开涉及染料木素的新结晶形式。所公开的结晶形式包括结晶染料木黄酮钠盐二水合物; 结晶染料木黄酮钾盐二水合物; 结晶染料木素钙盐; 结晶染料木素镁盐; 结晶染料木素L-赖氨酸盐; 结晶染料木素N-甲基葡糖胺盐; 结晶染料木素N-乙基葡糖胺盐; 结晶染料木素二乙胺盐; 和结晶染料木素一水合物。本公开还涉及由这些结晶形式表示的新型染料木素盐。描述了含有染料木素和/或染料木黄酮盐和药学上可接受的载体的这些结晶形式中的至少一种的治疗组合物。本公开还涉及治疗癌症的方法，其包括向有需要的患者施用治疗有效量的含有本发明化合物的染料木素结晶形式或染料木黄酮盐的治疗组合物的步骤。

2. 发明授权

US07863325B2 Crystalline genistein sodium salt dihydrate 有权
标题翻译：结晶染料木黄酮钠盐二水合物
公开(公告)号：US07863325B2
公开(公告)日：2011-01-04
申请号：US12636395
申请日：2009-12-11
申请人： Anders Berkenstam , Stefan Rehnmark , Michael-Robin Witt , Stephen Watt
发明人： Anders Berkenstam , Stefan Rehnmark , Michael-Robin Witt , Stephen Watt
IPC分类号： A61K31/352 , C07D311/30
CPC分类号： C07D311/30 , A61K31/352
摘要： The disclosure relates to a new crystalline form of genistein. The disclosed crystalline form is crystalline genistein sodium salt dihydrate. The disclosure also relates to the novel genistein salt composition represented by this crystalline form. Therapeutic compositions containing crystalline genistein sodium salt and a pharmaceutically acceptable carrier are described. The disclosure also relates to therapeutic methods comprising the step of administering to a patient in need thereof a therapeutically effective amount of a therapeutic composition containing the crystalline form of the disclosure or crystalline genistein sodium salt dihydrate.
摘要翻译：本公开涉及染料木素的新结晶形式。所公开的结晶形式是结晶染料木黄酮钠盐二水合物。本公开还涉及由该结晶形式表示的新颖的染料木黄酮盐组合物。描述了含有结晶染料木素钠盐和药学上可接受的载体的治疗组合物。本公开还涉及治疗方法，其包括向有需要的患者施用治疗有效量的含有本发明的结晶形式或结晶染料木黄酮钠盐二水合物的治疗组合物的步骤。

3. 发明授权

US07238498B2 Screening methods 失效
标题翻译：筛选方法
公开(公告)号：US07238498B2
公开(公告)日：2007-07-03
申请号：US11306504
申请日：2005-12-30
申请人： Anders Berkenstam , Göran Bertilsson , Lorenz Poellinger
发明人： Anders Berkenstam , Göran Bertilsson , Lorenz Poellinger
IPC分类号： C12P21/06
CPC分类号： G01N33/57496
摘要： A mammalian polypeptide designated Inhibitory PAS Domain Protein (IPAS) is useful for the inhibition of angiogenesis and/or tumor progression. Screening methods exist to identify compounds potentially useful as medicaments for the treatment of medical conditions related to angiogenesis or tumor progression.
摘要翻译：称为抑制性PAS结构域蛋白（IPAS）的哺乳动物多肽可用于抑制血管发生和/或肿瘤进展。存在筛选方法来鉴定潜在地用作治疗与血管发生或肿瘤进展相关的医学病症的药物的化合物。

4. 发明授权

US09012495B2 Crystalline forms of genistein 有权
标题翻译：结晶形式的染料木素
公开(公告)号：US09012495B2
公开(公告)日：2015-04-21
申请号：US13133085
申请日：2009-12-11
申请人： Anders Berkenstam , Stefan Rehnmark , Michael-Robin Witt , Keith Lorimer , Stephen Watt
发明人： Anders Berkenstam , Stefan Rehnmark , Michael-Robin Witt , Keith Lorimer , Stephen Watt
IPC分类号： A61K31/352 , C07D311/74 , C07D311/22
CPC分类号： A61K31/353 , A61K31/352 , C07B2200/13 , C07D311/22
摘要： The disclosure relates to new crystalline forms of genistein. The disclosed crystalline forms include crystalline genistein sodium salt dihydrate; crystalline genistein potassium salt dihydrate; crystalline genistein calcium salt; crystalline genistein magnesium salt; crystalline genistein L-lysine salt; crystalline genistein N-methylglucamine salt; crystalline genistein N-ethylglucamine salt; crystalline genistein diethylamine salt; and crystalline genistein monohydrate. The disclosure also relates to the novel genistein salts represented by these crystalline forms. Therapeutic compositions containing at least one of these crystalline forms of genistein and/or a genistein salt and a pharmaceutically acceptable carrier are described. The disclosure also relates to methods of treating cancer comprising the step of administering to a patient in need thereof a therapeutically effective amount of a therapeutic composition containing the compounds of the disclosure, of a crystalline form of genistein, or of a genistein salt.
摘要翻译：本公开涉及染料木素的新结晶形式。所公开的结晶形式包括结晶染料木黄酮钠盐二水合物; 结晶染料木黄酮钾盐二水合物; 结晶染料木素钙盐; 结晶染料木素镁盐; 结晶染料木素L-赖氨酸盐; 结晶染料木素N-甲基葡糖胺盐; 结晶染料木素N-乙基葡糖胺盐; 结晶染料木素二乙胺盐; 和结晶染料木素一水合物。本公开还涉及由这些结晶形式表示的新型染料木素盐。描述了含有染料木素和/或染料木黄酮盐和药学上可接受的载体的这些结晶形式中的至少一种的治疗组合物。本公开还涉及治疗癌症的方法，其包括向有需要的患者施用治疗有效量的含有本发明化合物的染料木素结晶形式或染料木黄酮盐的治疗组合物的步骤。

5. 发明授权

US06436654B1 Methods for identifying compounds that modulate HIF-1&agr; 失效
标题翻译：鉴定调节HIF-1α的化合物的方法
公开(公告)号：US06436654B1
公开(公告)日：2002-08-20
申请号：US09438833
申请日：1999-11-12
申请人： Anders Berkenstam , Lorenz Poellinger
发明人： Anders Berkenstam , Lorenz Poellinger
IPC分类号： G01N3353
CPC分类号： C07K14/4702 , A61K38/00
摘要： The present invention relates to a method for identifying compounds capable of modulating the function of a functional domain of human HIF-1&agr;, said method comprising (i) contacting a candidate compound with a variant of human HIF-1&agr;, said variant essentially lacking at least one functional domain of human HIF-1&agr;, or having a mutation making at least one functional domain of human HIF-1&agr; essentially inactive, said functional domain or domains being selected from the group consisting of (a) the PAS-B domain located in human HIF-1&agr; between amino acids 178 and 390, (b) the C-terminal nuclear localization sequence (NLS) located in human HIF-1&agr; essentially at amino acids 718 to 721, and (c) the transactivator/coactivator domain (N-TAD) located in human HIF-1&agr; essentially between amino acids 531 to 584, and (d) the transactivator/coactivator domain (C-TAD) located in human HIF-1&agr; essentially between amino acids 813 and 826, and (ii) determining the effect of the candidate compound on the said variant.
摘要翻译：本发明涉及鉴定能够调节人HIF-1α功能区功能的化合物的方法，所述方法包括（i）将候选化合物与人HIF-1α的变体接触，所述变体基本上至少缺少所述功能域或域选自（a）位于人中的PAS-B结构域，所述功能域选自人HIF-1α的一个功能结构域，或具有至少一个人HIF-1α功能区域基本上无活性的突变。氨基酸178和390之间的HIF-1α，（b）基本上在氨基酸718至721处位于人HIF-1α中的C末端核定位序列（NLS），和（c）反式激活因子/共激活因子结构域（N-TAD ）基本上位于人HIF-1α之间，基本上在氨基酸531至584之间，和（d）基本上在氨基酸813和826之间位于人HIF-1α中的反式激活因子/共激活因子结构域（C-TAD），和（ii）确定效应的烛光所述变体上的化合物。

6. 发明申请

US20100160426A1 CRYSTALLINE GENISTEIN SODIUM SALT DIHYDRATE 有权
标题翻译：水溶性硫酸钠
公开(公告)号：US20100160426A1
公开(公告)日：2010-06-24
申请号：US12636395
申请日：2009-12-11
申请人： Anders BERKENSTAM , Stefan Rehnmark , Michael-Robin Witt , Stephen Watt
发明人： Anders BERKENSTAM , Stefan Rehnmark , Michael-Robin Witt , Stephen Watt
IPC分类号： A61K31/352 , C07D311/30 , A61P31/00 , A61P35/00 , A61P1/18
CPC分类号： C07D311/30 , A61K31/352
摘要： The disclosure relates to a new crystalline form of genistein. The disclosed crystalline form is crystalline genistein sodium salt dihydrate. The disclosure also relates to the novel genistein salt composition represented by this crystalline form. Therapeutic compositions containing crystalline genistein sodium salt and a pharmaceutically acceptable carrier are described. The disclosure also relates to therapeutic methods comprising the step of administering to a patient in need thereof a therapeutically effective amount of a therapeutic composition containing the crystalline form of the disclosure or crystalline genistein sodium salt dihydrate.
摘要翻译：本公开涉及染料木素的新结晶形式。所公开的结晶形式是结晶染料木黄酮钠盐二水合物。本公开还涉及由该结晶形式表示的新颖的染料木黄酮盐组合物。描述了含有结晶染料木素钠盐和药学上可接受的载体的治疗组合物。本公开还涉及治疗方法，其包括向有需要的患者施用治疗有效量的含有本发明的结晶形式或结晶染料木黄酮钠盐二水合物的治疗组合物的步骤。

7. 发明申请

US20060228778A1 Novel vitamin D receptor related polypeptides, nucleic acid sequence encoding the same and uses thereof 审中-公开
标题翻译：新型维生素D受体相关多肽，编码其的核酸序列及其用途
公开(公告)号：US20060228778A1
公开(公告)日：2006-10-12
申请号：US11369263
申请日：2006-03-06
申请人： Anders Berkenstam , Mats Dahlberg
发明人： Anders Berkenstam , Mats Dahlberg
IPC分类号： A61K48/00 , A61K38/17 , C07K14/72 , C07K16/28 , C07H21/04 , C12P21/06 , A61K31/59
CPC分类号： C07K14/721 , A61K38/00 , A61K39/00 , A61K48/00
摘要： The present invention relates to novel vitamin D receptor related (VDRR) polypeptides, and formulations containing the same. Nucleic acid sequences encoding the VDRR polypeptides, expression vectors containing such sequences and host cells transformed with such expression vectors are also disclosed, as are methods for the expression of the novel VDRR polypeptides of the invention. The invention further relates to VDRR polypeptides for use as medicaments, and use of substances affecting VDRR signal transduction for the manufacture of medicaments for metabolic, proliferative or inflammatory conditions. The present invention also relates to methods for identifying clones encoding a VDRR polypeptide, methods for identifying ligands to a VDRR and methods for identifying substances for treatment of conditions affected by a VDRR polypeptide. More specifically, the novel VDRR polypeptide can be the polypeptide designated VDRRγ, which may be regulated by any small chemical molecule similar in structure to known ligands for nuclear receptors.
摘要翻译：本发明涉及新型的维生素D受体相关（VDRR）多肽及其制剂。还公开了编码VDRR多肽的核酸序列，含有这些序列的表达载体和用这种表达载体转化的宿主细胞，以及用于表达本发明的新型VDRR多肽的方法。本发明还涉及用作药物的VDRR多肽，以及影响VDRR信号转导的物质用于制备用于代谢，增殖或炎症病症的药物的用途。本发明还涉及用于鉴定编码VDRR多肽的克隆的方法，用于鉴定VDRR的配体的方法以及鉴定用于治疗受VDRR多肽影响的病症的物质的方法。更具体地，新型VDRR多肽可以是称为VDRRγ的多肽，其可以由结构上与核受体的已知配体相似的任何小的化学分子调节。

8. 发明授权

US07214770B2 Screening Methods 失效
标题翻译：筛选方法
公开(公告)号：US07214770B2
公开(公告)日：2007-05-08
申请号：US09896791
申请日：2001-06-29
申请人： Anders Berkenstam , Göran Bertilsson , Lorenz Poellinger
发明人： Anders Berkenstam , Göran Bertilsson , Lorenz Poellinger
IPC分类号： C07K1/10
CPC分类号： C07K14/4703 , C07K14/47
摘要： The present invention relates a mammalian polypeptide designated Inhibitory PAS Domain Protein (IPAS) which polypeptide is useful for the inhibition of angiogenesis and/or tumor progression. The invention also relates to screening methods for compounds potentially useful as medicaments for the treatment of medical conditions related to angiogenesis or tumor progression.
摘要翻译：本发明涉及称为抑制性PAS结构域蛋白（IPAS）的哺乳动物多肽，该多肽可用于抑制血管生成和/或肿瘤进展。本发明还涉及可用作治疗与血管发生或肿瘤进展有关的医学病症的药物的化合物的筛选方法。

9. 发明授权

US07118885B2 Nucleic acid encoding vitamin D receptor related polypeptide 失效
标题翻译：编码维生素D受体相关多肽的核酸
公开(公告)号：US07118885B2
公开(公告)日：2006-10-10
申请号：US09143828
申请日：1998-08-31
申请人： Anders Berkenstam , Mats Dahlberg
发明人： Anders Berkenstam , Mats Dahlberg
IPC分类号： C12N15/11 , C12N5/10 , C12N15/63
CPC分类号： C07K14/721 , A61K38/00 , A61K39/00 , A61K48/00
摘要： The present invention relates to novel vitamin D receptor related (VDRR) polypeptides, and formulations containing the same. Nucleic acid sequences encoding the VDRR polypeptides, expression vectors containing such sequences and host cells transformed with such expression vectors are also disclosed, as are methods for the expression of the novel VDRR polypeptides of the invention. The invention further relates to VDRR polypeptides for use as medicaments, and use of substances affecting VDRR signal transduction for the manufacture of medicaments for treating metabolic, proliferative or inflammatory conditions. The present invention also relates to methods for identifying clones encoding a VDRR polypeptide, methods for identifying ligands to a VDRR and methods for identifying substances for treatment of conditions affected by a VDRR polypeptide. More specifically, the novel VDRR polypeptide can be the polypeptide designated VDRRγ, which may be regulated by any small chemical molecule similar in structure to known ligands for nuclear receptors.
摘要翻译：本发明涉及新型的维生素D受体相关（VDRR）多肽及其制剂。还公开了编码VDRR多肽的核酸序列，含有这些序列的表达载体和用这种表达载体转化的宿主细胞，以及用于表达本发明的新型VDRR多肽的方法。本发明还涉及用作药物的VDRR多肽，以及影响VDRR信号转导的物质用于制备用于治疗代谢，增殖或炎性疾病的药物的用途。本发明还涉及用于鉴定编码VDRR多肽的克隆的方法，用于鉴定VDRR的配体的方法以及鉴定用于治疗受VDRR多肽影响的病症的物质的方法。更具体地，新型VDRR多肽可以是称为VDRRγ的多肽，其可以由结构上与核受体的已知配体相似的任何小的化学分子调节。

10. 发明申请

US20060115849A1 SCREENING METHODS 失效
标题翻译：筛选方法
公开(公告)号：US20060115849A1
公开(公告)日：2006-06-01
申请号：US11306504
申请日：2005-12-30
申请人： Anders Berkenstam , Goran Bertilsson , Lorenz Poellinger
发明人： Anders Berkenstam , Goran Bertilsson , Lorenz Poellinger
IPC分类号： C12Q1/68 , G01N33/574 , C07H21/04 , C12N9/99
CPC分类号： G01N33/57496
摘要： A mammalian polypeptide designated Inhibitory PAS Domain Protein (IPAS) is useful for the inhibition of angiogenesis and/or tumor progression. Screening methods exist to identify compounds potentially useful as medicaments for the treatment of medical conditions related to angiogenesis or tumor progression.
摘要翻译：称为抑制性PAS结构域蛋白（IPAS）的哺乳动物多肽可用于抑制血管发生和/或肿瘤进展。存在筛选方法来鉴定潜在地用作治疗与血管发生或肿瘤进展相关的医学病症的药物的化合物。

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