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。

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.

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。

公开(公告)号：US20060211768A1

公开(公告)日：2006-09-21

申请号：US11256501

申请日：2005-10-21

申请人： Ronald Evans ,  David Mangelsdorf ,  Richard Heyman ,  Marcus Boehm ,  Gregor Eichele ,  Christina Thaller

发明人： Ronald Evans ,  David Mangelsdorf ,  Richard Heyman ,  Marcus Boehm ,  Gregor Eichele ,  Christina Thaller

IPC分类号： A61K31/203

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.

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。

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。

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。