序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
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.

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.
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