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1. 发明申请

WO2011127388A2 INVERSE AGONISTS AND NEUTRAL ANTAGONISTS FOR THE TSH RECEPTOR 审中-公开
标题翻译：反向激动剂和TSH受体的中性拮抗剂
公开(公告)号：WO2011127388A2
公开(公告)日：2011-10-13
申请号：PCT/US2011031752
申请日：2011-04-08
申请人： US HEALTH , GERSHENGORN MARVIN , NEUMANN SUSANNE , HUANG WENWEI , THOMAS CRAIG J
发明人： GERSHENGORN MARVIN , NEUMANN SUSANNE , HUANG WENWEI , THOMAS CRAIG J
IPC分类号： C07D405/06 , A61K31/517 , A61P35/00 , C07D239/91 , C07D401/06
CPC分类号： C07D401/06 , A61K31/517 , C07D239/91 , C07D405/06
摘要： TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.
摘要翻译： TSHR反向激动剂和中枢拮抗剂，可用于治疗格雷夫斯眶前病变，格雷夫斯甲状腺功能亢进症和/或甲状腺癌。

2. 发明申请

WO2007075956A2 METHODS FOR PRODUCING AND USING PANCREATIC ENDOCRINE CELLS 审中-公开
标题翻译：生产和使用胰腺内分泌细胞的方法
公开(公告)号：WO2007075956A2
公开(公告)日：2007-07-05
申请号：PCT/US2006/048918
申请日：2006-12-20
申请人： THE GOVT. OF THE USA AS REPRESENTED BY THE SECRETARY OF THE DEPARTMENT OF HEALTH & HUMAN SERVICES , GERSHENGORN, Marvin, C. , RAAKA, Bruce, M. , GERAS-RAAKA, Elizabeth
发明人： GERSHENGORN, Marvin, C. , RAAKA, Bruce, M. , GERAS-RAAKA, Elizabeth
IPC分类号： C12N5/06 , C12N5/08
CPC分类号： G01N33/507 , C12N5/0676 , C12N2500/25
摘要： Isolated populations of committed mesenchymal cells are disclosed that can proliferate in vitro, and, under appropriate conditions, can differentiate into pancreatic endocrine cells. Committed mesenchymal cells can undergo a mesenchymal-to-epithelial transition to form epithelial cell clusters, which can be transplanted into a recipient, such as a subject with diabetes. Tissue culture media is disclosed that is of use for expanding and differentiating committed mesenchymal cells. Methods for identifying agents of use in treating diabetes are also provided.
摘要翻译：公开了可在体外增殖并且在适当条件下可分化成胰腺内分泌细胞的分离的定向间充质细胞群。承诺的间充质细胞可以经历间充质 - 上皮转化以形成上皮细胞簇，其可以被移植到受体中，例如患有糖尿病的受试者。公开了用于扩增和分化承诺的间充质细胞的组织培养基。还提供了鉴定用于治疗糖尿病的药物的方法。

3. 发明申请

WO1997007233A1 REGULATION OF CELLULAR FUNCTIONS BY ECTOPIC EXPRESSION OF NON-ENDOGENOUS CELL SIGNALLING RECEPTORS 审中-公开
标题翻译：通过非内源细胞信号受体的表达表达调节细胞功能
公开(公告)号：WO1997007233A1
公开(公告)日：1997-02-27
申请号：PCT/US1996013077
申请日：1996-08-12
申请人： CORNELL RESEARCH FOUNDATION, INC. , GERSHENGORN, Marvin, C. , FALCK-PEDERSEN, Erik, S. , CRYSTAL, Ronald, G.
发明人： CORNELL RESEARCH FOUNDATION, INC.
IPC分类号： C12P21/06
CPC分类号： C07K14/72 , A61K38/00
摘要： The present invention is directed to an in vivo cell transformed with DNA encoding a cell signalling receptor not endogenous to the cell. The cell signalling receptor is capable of activating a signal transduction pathway endogenous to the cell, and the cell signalling receptor can be controllably activated thereby controllably activating the signal transduction pathway so as to regulate a cell function controlled by the signal transduction pathway. The invention also provides a method of ectopically expressing a non-endogenous receptor in a cell, and a method of regulating a cell function in vivo. The method of regulating a cell function comprises transforming a cell with DNA encoding a cell signalling receptor not endogenous to the cell, as above, and controllably exposing the cell to an extracellular molecule capable of activating the foreign cell signalling receptor. Activation of the cell signalling receptor activates the endogenous signal transduction pathway so as to regulate a cell function controlled by the endogenous signal transduction pathway.
摘要翻译：本发明涉及用编码细胞内源性的细胞信号传导受体的DNA转化的体内细胞。细胞信号传导受体能够激活细胞内源性的信号转导途径，并且细胞信号传导受体可被可控地激活，从而可控制地激活信号转导途径，从而调节由信号转导途径控制的细胞功能。本发明还提供了在细胞中异位表达非内源受体的方法，以及调节体内细胞功能的方法。调节细胞功能的方法包括如上所述用编码细胞内源性的细胞信号传导受体的DNA转化细胞，并可控地将细胞暴露于能够激活外源细胞信号传导受体的细胞外分子。细胞信号传导受体的激活激活内源性信号转导途径，以调节由内源信号转导途径控制的细胞功能。

4. 发明申请

WO2011127388A3 INVERSE AGONISTS AND NEUTRAL ANTAGONISTS FOR THE TSH RECEPTOR 审中-公开
公开(公告)号：WO2011127388A3
公开(公告)日：2011-10-13
申请号：PCT/US2011/031752
申请日：2011-04-08
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , GERSHENGORN, Marvin , NEUMANN, Susanne , HUANG, Wenwei , THOMAS, Craig, J.
发明人： GERSHENGORN, Marvin , NEUMANN, Susanne , HUANG, Wenwei , THOMAS, Craig, J.
IPC分类号： C07D405/06 , C07D401/06 , C07D239/91 , A61K31/517 , A61P35/00
摘要： TSHR inverse agonists and neutral antagonists that are useful for treating Graves' orbitopathy, Graves' hyperthyroidism and/or thyroid cancer.

5. 发明申请

WO2010047674A1 LOW MOLECULAR WEIGHT THYROID STIMULATING HORMONE RECEPTOR (TSHR) AGONISTS 审中-公开
标题翻译：低分子量甲状腺刺激激素受体（TSHR）激素
公开(公告)号：WO2010047674A1
公开(公告)日：2010-04-29
申请号：PCT/US2008/011958
申请日：2008-10-20
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by the SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES , GERSHENGORN, Marvin, C. , NEUMANN, Susanne , RAAKA, Bruce, M. , THOMAS, Craig, J. , INGLESE, James , SOUTHALL, Noel, T. , TITUS, Steven , ZHENG, Wei , HUANG, Wenwei , KRAUSE, Gerd , KLEINAU, Gunnar
发明人： GERSHENGORN, Marvin, C. , NEUMANN, Susanne , RAAKA, Bruce, M. , THOMAS, Craig, J. , INGLESE, James , SOUTHALL, Noel, T. , TITUS, Steven , ZHENG, Wei , HUANG, Wenwei , KRAUSE, Gerd , KLEINAU, Gunnar
IPC分类号： C07D235/18 , A61K31/4184
CPC分类号： C07D405/06 , A61K31/517 , A61K49/0004 , A61K51/00 , C07D239/91 , C07D401/06 , C07D405/14 , C07D487/04
摘要： Disclosed are oxo-hydroquinazolines of formula I that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
摘要翻译：公开了可用作选择性TSHR激动剂的式I的氧代 - 氢喹唑啉。该化合物可用于检测或治疗甲状腺癌或治疗骨退行性疾病。

6. 发明申请

WO2007136776A3 PYRIMIDINE LOW MOLECULAR WEIGHT LIGANDS FOR MODULATING HORMONE RECEPTORS 审中-公开
标题翻译：用于调节激素受体的吡嗪低分子量配体
公开(公告)号：WO2007136776A3
公开(公告)日：2008-01-24
申请号：PCT/US2007011951
申请日：2007-05-17
申请人： US GOV HEALTH & HUMAN SERV , GERSHENGORN MARVIN C , NEUMANN SUSANNE , THOMAS CRAIG , JAESCHKE HOLGER , MOORE SUSANNA , KRAUSE GERD , RAAKA BRUCE , PASCHKE RALF
发明人： GERSHENGORN MARVIN C , NEUMANN SUSANNE , THOMAS CRAIG , JAESCHKE HOLGER , MOORE SUSANNA , KRAUSE GERD , RAAKA BRUCE , PASCHKE RALF
IPC分类号： C07D495/04 , A61K31/519 , A61P5/06 , A61P5/08
CPC分类号： A61K31/519 , C07D495/04
摘要： Disclosed herein are small molecule modulators hormone receptors, including agonists and antagonists of luteinizing hormone/choriogonadotropin, follicle stimulating hormone and thyroid stimulating hormone receptors. Exemplary disclosed compounds include those of the formula wherein X is -S(O) n R 5 ; n is 0, 1 or 2; Y is -OR 6 or -NR 7 R 8 R 1 and R 2 independently are selected from optionally substituted lower aliphatic, alkoxy, aralkyl, halogen, H and -OR5, wherein R5 is selected from lower alkyl, H, aralkyl, acyl, alkoxycarbonyl and aminocarbonyl; R 3 and R 4 independently are selected from acyl, alkoxycarbonyl, aminocarbonyl, aralkyl, H, lower alkyl and cycloalkyl; R 5 is selected from lower alkyl, aralkyl, cycloalkyl and haloalkyl; R 6 is selected from H, lower alkyl and aralkyl; R 7 and R8 independently are selected from H, lower alkyl, aralkyl and cycloalkyl.
摘要翻译：本文公开了小分子调节剂激素受体，包括促黄体激素/促性腺激素的激动剂和拮抗剂，促卵泡激素和促甲状腺激素受体。示例性的公开的化合物包括下式的那些化合物其中X是-S（O）n R 5; n为0,1或2; Y是-OR 6或-NR 7 R 8 R 12和R 2 O 2 独立地选自任选取代的低级脂族，烷氧基，芳烷基，卤素，H和-OR5，其中R5选自低级烷基，H，芳烷基，酰基，烷氧基羰基和氨基羰基; R 3和R 4独立地选自酰基，烷氧基羰基，氨基羰基，芳烷基，H，低级烷基和环烷基; R 5选自低级烷基，芳烷基，环烷基和卤代烷基; R 6选自H，低级烷基和芳烷基; R 7和R 8独立地选自H，低级烷基，芳烷基和环烷基。

7. 发明申请

WO2007136776A2 PYRIMIDINE LOW MOLECULAR WEIGHT LIGANDS FOR MODULATING HORMONE RECEPTORS 审中-公开
标题翻译：用于调节激素受体的吡嗪低分子量配体
公开(公告)号：WO2007136776A2
公开(公告)日：2007-11-29
申请号：PCT/US2007/011951
申请日：2007-05-17
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by THE SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES , GERSHENGORN, Marvin, C. , NEUMANN, Susanne , THOMAS, Craig , JAESCHKE, Holger , MOORE, Susanna , KRAUSE, Gerd , RAAKA, Bruce , PASCHKE, Ralf
发明人： GERSHENGORN, Marvin, C. , NEUMANN, Susanne , THOMAS, Craig , JAESCHKE, Holger , MOORE, Susanna , KRAUSE, Gerd , RAAKA, Bruce , PASCHKE, Ralf
IPC分类号： C07D495/04 , A61K31/519 , A61P5/06 , A61P5/08
CPC分类号： A61K31/519 , C07D495/04
摘要： Disclosed herein are small molecule modulators hormone receptors, including agonists and antagonists of luteinizing hormone/choriogonadotropin, follicle stimulating hormone and thyroid stimulating hormone receptors. Exemplary disclosed compounds include those of the formula wherein X is -S(O) n R 5 ; n is 0, 1 or 2; Y is -OR 6 or -NR 7 R 8 R 1 and R 2 independently are selected from optionally substituted lower aliphatic, alkoxy, aralkyl, halogen, H and -OR5, wherein R5 is selected from lower alkyl, H, aralkyl, acyl, alkoxycarbonyl and aminocarbonyl; R 3 and R 4 independently are selected from acyl, alkoxycarbonyl, aminocarbonyl, aralkyl, H, lower alkyl and cycloalkyl; R 5 is selected from lower alkyl, aralkyl, cycloalkyl and haloalkyl; R 6 is selected from H, lower alkyl and aralkyl; R 7 and R8 independently are selected from H, lower alkyl, aralkyl and cycloalkyl.
摘要翻译：本文公开了小分子调节剂激素受体，包括促黄体激素/促性腺激素的激动剂和拮抗剂，促卵泡激素和促甲状腺激素受体。示例性的公开的化合物包括下式的那些化合物其中X是-S（O）n R 5; n为0,1或2; Y是-OR 6或-NR 7 R 8 R 12和R 2 O 2 独立地选自任选取代的低级脂族，烷氧基，芳烷基，卤素，H和-OR5，其中R5选自低级烷基，H，芳烷基，酰基，烷氧基羰基和氨基羰基; R 3和R 4独立地选自酰基，烷氧基羰基，氨基羰基，芳烷基，H，低级烷基和环烷基; R 5选自低级烷基，芳烷基，环烷基和卤代烷基; R 6选自H，低级烷基和芳烷基; R 7和R 8独立地选自H，低级烷基，芳烷基和环烷基。

8. 发明申请

WO2007075956A3 METHODS FOR PRODUCING AND USING PANCREATIC ENDOCRINE CELLS 审中-公开
标题翻译：生产和使用胰腺内切细胞的方法
公开(公告)号：WO2007075956A3
公开(公告)日：2007-08-23
申请号：PCT/US2006048918
申请日：2006-12-20
申请人： GOVT OF THE USA AS REPRESENTED , GERSHENGORN MARVIN C , RAAKA BRUCE M , GERAS-RAAKA ELIZABETH
发明人： GERSHENGORN MARVIN C , RAAKA BRUCE M , GERAS-RAAKA ELIZABETH
IPC分类号： C12N5/071
CPC分类号： G01N33/507 , C12N5/0676 , C12N2500/25
摘要： Isolated populations of committed mesenchymal cells are disclosed that can proliferate in vitro, and, under appropriate conditions, can differentiate into pancreatic endocrine cells. Committed mesenchymal cells can undergo a mesenchymal-to-epithelial transition to form epithelial cell clusters, which can be transplanted into a recipient, such as a subject with diabetes. Tissue culture media is disclosed that is of use for expanding and differentiating committed mesenchymal cells. Methods for identifying agents of use in treating diabetes are also provided.
摘要翻译：公开了分离的定向间充质细胞群体，其可以在体外增殖，并且在适当的条件下可以分化成胰腺内分泌细胞。承诺的间充质细胞可以经历间充质 - 上皮转换以形成上皮细胞簇，其可以移植到受体中，例如患有糖尿病的受试者。公开了用于扩增和分化确定的间充质细胞的组织培养基。还提供了用于鉴定用于治疗糖尿病的药剂的方法。

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