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1. 发明授权

US5968989A Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor 失效
公开(公告)号：US5968989A
公开(公告)日：1999-10-19
申请号：US472817
申请日：1995-06-07
申请人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
发明人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
IPC分类号： A61K31/07 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/23 , A61K31/232 , A61K38/21 , C07C53/00 , C07C57/26 , C07C59/46 , C07C59/80 , C07K14/705 , C12P7/04 , A01N31/04 , A01N37/00
CPC分类号： C07K14/70567 , A61K31/07 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/23 , A61K31/232 , C07C403/20 , C07C57/26 , C07C59/46 , C07C59/80 , C12P7/04 , C07B2200/09 , C07C2101/16
摘要： In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.

2. 发明授权

US5932622A Method for in vivo modulation of non-malignant skin-related processes with 9-cis-retinoic acid 失效
标题翻译：用9-顺 - 视黄酸体内调节非恶性皮肤相关过程的方法
公开(公告)号：US5932622A
公开(公告)日：1999-08-03
申请号：US475174
申请日：1995-06-07
申请人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
发明人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
IPC分类号： A61K31/203 , A61K31/232 , A61K31/07 , C12N5/06
CPC分类号： A61K31/203 , A61K31/232 , Y10S514/863 , Y10S514/864
摘要： A method for modulating non-malignant skin related disorders in a subject has been demonstrated with 9-cis retinoic acid. Wrinkling, acne, keratinization, differentiation and proliferation disorders are treated by administration of 9-cis retinoic acid alone or in a pharmaceutically acceptable carrier to a subject in need thereof.
摘要翻译：用9-顺式视黄酸证明了调节受试者中非恶性皮肤相关疾病的方法。通过将9-顺式视黄酸单独或药学上可接受的载体给予有需要的受试者来治疗皱纹，粉刺，角质化，分化和增殖障碍。

3. 发明授权

US06506917B1 Compounds and compositions useful for modulation of processes mediated by RXR 失效
标题翻译：用于调节由RXR介导的过程的化合物和组合物
公开(公告)号：US06506917B1
公开(公告)日：2003-01-14
申请号：US08480967
申请日：1995-06-07
申请人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
发明人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
IPC分类号： C07C5300
CPC分类号： C12P7/04 , A61K31/07 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/23 , A61K31/232 , C07K14/70567
摘要： In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.
摘要翻译：根据本发明，提供了调节由类视黄醇受体介导的过程的方法，其使用这种受体的高亲和力，高特异性配体。在本发明的一个方面，提供了比视黄酸（即，类固醇）对类视黄醇X受体更有选择性的配体。在本发明的另一方面，已经发现了能够诱导视黄酸受体介导的过程的替代配体（视黄酸除外）。在另一方面，已经开发了用于从容易获得的化合物制备这种类视黄醇受体配体的方法。

4. 发明授权

US07056954B2 Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor 失效
标题翻译：用于调节由类视黄醇受体介导的过程和对其有用的化合物的方法
公开(公告)号：US07056954B2
公开(公告)日：2006-06-06
申请号：US10458880
申请日：2003-06-10
申请人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
发明人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
IPC分类号： A61K31/07
CPC分类号： C07K14/70567 , A61K31/203
摘要： In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.
摘要翻译：根据本发明，提供了调节由类视黄醇受体介导的过程的方法，其使用这种受体的高亲和力，高特异性配体。在本发明的一个方面，提供了比视黄酸（即，类固醇）对类视黄醇X受体更有选择性的配体。在本发明的另一方面，已经发现了能够诱导维甲酸受体介导的过程的替代配体（视黄酸除外）。在另一方面，已经开发了用于从容易获得的化合物制备这种类视黄醇受体配体的方法。

5. 发明授权

US06992108B1 Means for the modulation of processes mediated by retinoid receptors and compounds useful therefor 失效
标题翻译：用于调节由类视黄醇受体介导的过程和对其有用的化合物的方法
公开(公告)号：US06992108B1
公开(公告)日：2006-01-31
申请号：US08482737
申请日：1995-06-07
申请人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
发明人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
IPC分类号： A61K31/19 , A61K31/20
CPC分类号： C12P7/04 , A61K31/07 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/23 , A61K31/232 , C07K14/70567
摘要： A method for modulating lipid metabolism in a subject by administering 9-cis retinoic acid is presented. The 9-cis retinoic acid is more specific for the retinoid X receptor than is retinoic acid.
摘要翻译：提出了通过施用9-顺式视黄酸调节受试者的脂质代谢的方法。类视黄醇X受体比视黄酸更具有9-顺式视黄酸的特异性。

6. 发明授权

US06576676B1 Means for the modulation of processes mediated by retinold receptors and compounds useful therefor 失效
标题翻译：用于调节由retinold受体介导的过程和对其有用的化合物的方法
公开(公告)号：US06576676B1
公开(公告)日：2003-06-10
申请号：US09350648
申请日：1999-07-09
申请人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
发明人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Gregor Eichele , Christina Thaller
IPC分类号： A61K31203
CPC分类号： C07K14/70567 , A61K31/07 , A61K31/19 , A61K31/20 , A61K31/203 , A61K31/23 , A61K31/232 , C07B2200/09 , C07C57/26 , C07C59/46 , C07C59/80 , C07C403/20 , C07C2601/16 , C12P7/04
摘要： In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.
摘要翻译：根据本发明，提供了调节由类视黄醇受体介导的过程的方法，其使用这种受体的高亲和力，高特异性配体。在本发明的一个方面，提供了比视黄酸（即，类固醇）对类视黄醇X受体更有选择性的配体。在本发明的另一方面，已经发现了能够诱导维甲酸受体介导的过程的替代配体（视黄酸除外）。在另一方面，已经开发了用于从容易获得的化合物制备这种类视黄醇受体配体的方法。

7. 发明授权

US5990163A Selective modulation of processes mediated by retinoid X receptors, and compounds useful therefor 失效
标题翻译：由视黄醇X受体介导的过程的选择性调节，以及对其有用的化合物
公开(公告)号：US5990163A
公开(公告)日：1999-11-23
申请号：US372218
申请日：1995-01-13
申请人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Margaret A. Harmon
发明人： Ronald M. Evans , David J. Mangelsdorf , Richard A. Heyman , Marcus F. Boehm , Margaret A. Harmon
IPC分类号： A61K31/201 , A61K31/202 , A61K31/231 , A61K31/232 , A61K31/20 , A61K31/23 , A61K31/335
CPC分类号： A61K31/201 , A61K31/202 , A61K31/231 , A61K31/232
摘要： In accordance with the present invention, ligands have been discovered which selectively bind retinoid X receptors. Such ligands can be used for the selective modulation of retinoid X receptor mediated processes. In a further aspect of the present invention, there are provided pharmaceutical compositions comprising a pharmaceutically acceptable vehicle containing at least one of the above-described selective ligands. Such compositions are useful, for example, for the treatment of a variety of retinoid X receptor mediated disease states.
摘要翻译：根据本发明，已经发现了选择性结合视黄醇X受体的配体。这种配体可用于选择性调节类视黄醇X受体介导的过程。在本发明的另一方面，提供了包含含有至少一种上述选择性配体的药学上可接受的载体的药物组合物。这样的组合物可用于例如治疗各种类视黄醇X受体介导的疾病状态。

8. 发明授权

US5710004A Methods of using novel steroid hormone orphan receptors 失效
标题翻译：使用新型类固醇激素孤儿受体的方法
公开(公告)号：US5710004A
公开(公告)日：1998-01-20
申请号：US694501
申请日：1996-08-07
申请人： Ronald M. Evans , David J. Mangelsdorf , Estelita S. Ong , Anthony E. Oro , Uwe K. Borgmeyer , Vincent Giguere , Tso-Pang Yao
发明人： Ronald M. Evans , David J. Mangelsdorf , Estelita S. Ong , Anthony E. Oro , Uwe K. Borgmeyer , Vincent Giguere , Tso-Pang Yao
IPC分类号： C07K14/705 , C12N15/12 , C12Q1/68 , C07K14/00 , C12P21/06
CPC分类号： C07K14/70567 , C12Q1/6897 , C07K2319/00
摘要： Novel members of the steroid/thyroid superfamily of receptors are described. DNA sequences encoding same, expression vectors containing such DNA and host cells transformed with such expression vectors are also disclosed, as are methods for the expression of the novel receptors of the invention, and various uses thereof.
摘要翻译：描述了类固醇/甲状腺超家族的新成员。还公开了编码该DNA的DNA序列，含有这种DNA的表达载体和用这些表达载体转化的宿主细胞，以及本发明的新型受体的表达方法及其各种用途。

9. 发明授权

US07501487B1 Retinoid receptor compositions and methods 失效
标题翻译：类视黄醇受体组合物和方法
公开(公告)号：US07501487B1
公开(公告)日：2009-03-10
申请号：US08467543
申请日：1995-06-05
申请人： David J. Mangelsdorf , Ronald M. Evans
发明人： David J. Mangelsdorf , Ronald M. Evans
IPC分类号： A07K14/00
CPC分类号： C07K14/70567 , C12N15/64 , C12N15/67 , C12N15/85 , C12N2830/00 , C12N2830/002
摘要： The present invention relates to novel receptor polypeptides, which, upon interaction with certain ligands, or activation by certain compounds, modulate transcription of certain genes by binding to cognate response elements associated with promoters of such genes. The novel receptors of the invention modulate transcription in the presence of retinoid compounds.The receptors of the present invention differ significantly from known retinoic acid receptors, in protein primary sequence and in responsiveness to exposure to various retinoids.The invention provides DNAs encoding the novel receptors, expression vectors for expression of the receptors, cells transformed with such expression vectors, cells co-transformed with such expression vectors and with reporter vectors to monitor modulation of transcription by the receptors, and methods of using such co-transformed cells in screening for compounds which are capable, directly or indirectly, of activating the receptors.The invention also provides nucleic acid probes for identifying DNAs which encode additional retinoid receptors of the same class as the novel receptors disclosed herein.
摘要翻译：本发明涉及新的受体多肽，其在与某些配体相互作用或某些化合物的活化时，通过结合与这些基因的启动子相关的同源反应元件来调节某些基因的转录。本发明的新受体在类视色素化合物存在下调节转录。本发明的受体与已知的视黄酸受体显着不同，蛋白质一级序列和对各种类视黄醇的暴露反应。本发明提供了编码新受体的DNA，用于表达受体的表达载体，用这种表达载体转化的细胞，用这些表达载体共转化的细胞和用报道载体监测受体转录的调节的方法共转化细胞筛选能够直接或间接激活受体的化合物。本发明还提供用于鉴定编码与本文公开的新型受体相同类别的另外的类视黄醇受体的DNA的核酸探针。

10. 发明授权

US5696233A Orphan steroid hormone receptors 失效
标题翻译：孤儿类固醇激素受体
公开(公告)号：US5696233A
公开(公告)日：1997-12-09
申请号：US463694
申请日：1995-06-05
申请人： Ronald M. Evans , David J. Mangelsdorf , Estelita S. Ong , Anthony E. Oro , Uwe K. Borgmeyer , Vincent Giguere , Tso-Pang Yao
发明人： Ronald M. Evans , David J. Mangelsdorf , Estelita S. Ong , Anthony E. Oro , Uwe K. Borgmeyer , Vincent Giguere , Tso-Pang Yao
IPC分类号： C07K14/705 , C12N15/12 , C12Q1/68 , C07K14/72
CPC分类号： C07K14/70567 , C12Q1/6897 , C07K2319/00
摘要： Novel members of the steroid/thyroid superfamily of receptors are described. DNA sequences encoding same, expression vectors containing such DNA and host cells transformed with such expression vectors are also disclosed, as are methods for the expression of the novel receptors of the invention, and various uses thereof.
摘要翻译：描述了类固醇/甲状腺超家族的新成员。还公开了编码该DNA的DNA序列，含有这种DNA的表达载体和用这些表达载体转化的宿主细胞，以及本发明的新型受体的表达方法及其各种用途。

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