序号 | 专利名 | 申请号 | 申请日 | 公开(公告)号 | 公开(公告)日 | 发明人 |
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41 | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex | US13954376 | 2013-07-30 | US09359289B2 | 2016-06-07 | Robert Eugene Hormann; David W. Potter; Orestes Chortyk; Colin M. Tice; Glenn Richard Carlson; Andrew Meyer; Thomas R. Opie |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising; the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
42 | Bioavailable Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex | US14817901 | 2015-08-04 | US20160039750A1 | 2016-02-11 | Robert Eugene HORMANN; David W. Potter; Orestes Chortyk; Colin M. Tice; Glenn Richard Carlson; Andrew Meyer; Thomas R. Opie |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
43 | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex | US13603965 | 2012-09-05 | US09169210B2 | 2015-10-27 | Robert Eugene Hormann; David W. Potter; Orestes Chortyk; Colin M. Tice; Glenn Richard Carlson; Andrew Meyer; Thomas R. Opie |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
44 | BIOAVAILABLE DIACYLHYDRAZINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX | US11841617 | 2007-08-20 | US20150240244A1 | 2015-08-27 | Robert Eugene Hormann; David W. Potter; Orestes Chortyk; Colin M. Tice; Glenn Richard Carlson; Andrew Meyer; Thomas R. Opie |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
45 | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex | US11841617 | 2007-08-20 | US09102648B1 | 2015-08-11 | Robert Eugene Hormann; David W. Potter; Orestes Chortyk; Colin M. Tice; Glenn Richard Carlson; Andrew Meyer; Thomas R. Opie |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
46 | Neprilysin inhibitors | US14196624 | 2014-03-04 | US08901169B2 | 2014-12-02 | Erik Fenster; Melissa Fleury; Adam D. Hughes |
In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds. | ||||||
47 | Process for synthesizing a substituted pyrazole | US11988849 | 2006-07-21 | US20090054662A1 | 2009-02-26 | Lushi Tan; James Christopher McWilliams; Frederick W. Hartner; Naoki Yoshikawa; Wenji Li |
The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus. | ||||||
48 | Diacylhydrazine derivatives | US10030691 | 2002-01-14 | US06649613B1 | 2003-11-18 | Günter Hölzemann; Simon Goodman; Horst Kessler; Christoph Gibson; Gabór Sulyok |
Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis. | ||||||
49 | N-disubstituted amino maleimides and succinimides | US44986965 | 1965-04-21 | US3257414A | 1966-06-21 | HAGEMAN HOWARD A; HUBBARD WINCHESTER L |
50 | N-disubstituted amino amic acids | US25892363 | 1963-02-15 | US3240799A | 1966-03-15 | HAGEMAN HOWARD A; HUBBARD WINCHESTER L |
51 | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex | EP11193097.0 | 2004-02-27 | EP2463269B1 | 2016-09-28 | Hormann, Robert Eugene; Potter, David W.; Chortyk, Orestes; Tice, Colin M.; Carlson, Glenn Richard; Meyer, Andrew; Opie, Thomas R. |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
52 | NEPRILYSIN INHIBITORS | EP14713656.8 | 2014-03-04 | EP2964616A1 | 2016-01-13 | FENSTER, Erik; FLEURY, Melissa; HUGHES, Adam D. |
In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds. | ||||||
53 | PROCESS FOR SYNTHESIZING A SUBSTITUTED PYRAZOLE | EP06800239.3 | 2006-07-21 | EP1910303A2 | 2008-04-16 | TAN, Lushi; MCWILLIAMS, James Christopher; HARTNER, Frederick, W.; YOSHIKAWA, Naoki; LI, Wenji |
The present application relates to a process for the synthesis of the compound of formula 1. The compound of formula I is a glucagon receptor antagonist and is useful for treating, preventing or delaying the onset of type 2 diabetes mellitus. | ||||||
54 | BIOAVAILABLE DIACYLHYDRAZINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX | EP04715710 | 2004-02-27 | EP1601642A4 | 2007-04-11 | HORMANN ROBERT EUGENE; POTTER DAVID W; CHORTYK ORESTES; TICE COLIN M; CARLSON GLENN RICHARD; MEYER ANDREW; OPIE THOMAS R |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
55 | BIOAVAILABLE DIACYLHYDRAZINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX | EP04715710.2 | 2004-02-27 | EP1601642A2 | 2005-12-07 | HORMANN, Robert, Eugene; POTTER, David, W.; CHORTYK, Orestes; TICE, Colin, M.; CARLSON, Glenn, Richard; MEYER, Andrew; OPIE, Thomas, R. |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
56 | NEPRILYSIN INHIBITORS | EP14713656 | 2014-03-04 | EP2964616B1 | 2017-05-03 | FENSTER ERIK; FLEURY MELISSA; HUGHES ADAM D |
In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds. | ||||||
57 | BIOAVAILABLE DIACYLHYDRAZINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX | EP04715710.2 | 2004-02-27 | EP1601642B1 | 2017-01-04 | HORMANN, Robert, Eugene; POTTER, David, W.; CHORTYK, Orestes; TICE, Colin, M.; CARLSON, Glenn, Richard; MEYER, Andrew; OPIE, Thomas, R. |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
58 | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex | EP11193097 | 2004-02-27 | EP2463269A1 | 2012-06-13 | HORMANN ROBERT EUGENE; POTTER DAVID W; CHORTYK ORESTES; TICE COLIN M; CARLSON GLENN RICHARD; MEYER ANDREW; OPIE THOMAS R |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. | ||||||
59 | Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex | EP11193098.8 | 2004-02-27 | EP2460786A1 | 2012-06-06 | Hormann, Robert Eugene; Potter, David, W.; Chortyk, Orestes; Tice, Colin, M.; Carlson, Glenn, Richard; Meyer, Andrew; Opie, Thomas, R. |
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. |
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60 | COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS | EP07811437.8 | 2007-08-20 | EP2074097A2 | 2009-07-01 | SUN, Lijun; KOYA, Keizo; CHEN, Shoujun; DEMKO, Zachary; XIA, Zhi-qiang |
Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier. |