Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I):
wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
November 12, 2002
Date of Patent:
December 30, 2003
Assignee:
Theravance, Inc.
Inventors:
Edmund J. Moran, John R. Jacobsen, Michael R. Leadbetter, Matthew B. Nodwell, Sean G. Trapp, James Aggen, Timothy J. Church
Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
November 12, 2002
Date of Patent:
November 25, 2003
Assignee:
Theravance, Inc.
Inventors:
Edmund J. Moran, John R. Jacobsen, James B. Aggen
Abstract: Disclosed are glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Type:
Grant
Filed:
May 1, 2001
Date of Patent:
October 21, 2003
Assignee:
Theravance, Inc.
Inventors:
Michael R. Leadbetter, Martin S. Linsell
Abstract: This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.
Abstract: Disclosed are glycopeptide derivatives substituted at the C-terminus and/or the R-terminus with a substituent that comprises one or more saccharide groups and a carboxy group; and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Type:
Grant
Filed:
May 1, 2001
Date of Patent:
September 16, 2003
Assignee:
Theravance, Inc.
Inventors:
Martin S. Linsell, Paul R. Fatheree, Michael R. Leadbetter, Yan Zhu, J. Kevin Judice
Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma and bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Type:
Grant
Filed:
August 14, 2000
Date of Patent:
June 10, 2003
Assignee:
Theravance, Inc.
Inventors:
Edmund J. Moran, John H. Griffin, Seok-Ki Choi
Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.
Type:
Grant
Filed:
October 3, 2000
Date of Patent:
June 10, 2003
Assignee:
Theravance, Inc.
Inventors:
Sabine M. Axt, Timothy J. Church, Witold N. Hruzewicz, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, J. Kevin Judice
Abstract: Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptogramins, tetracycline and/or other compounds at which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.
Abstract: Disclosed are multibinding compounds which are &bgr;2 adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.
Abstract: Novel antibacterial agents that act as multibinding agents are disclosed. The compounds of the invention comprise from 2-10 ligands covalently connected, each of said ligands being capable of binding to a transglycosylase enzyme substrate thereby modulating the biological processes/functions thereof.
Type:
Grant
Filed:
February 19, 1999
Date of Patent:
February 11, 2003
Assignee:
Theravance, Inc.
Inventors:
Qi-Qi Chen, John H. Griffin, Thomas E. Jenkins, J. Kevin Judice, Martin S. Linsell, Michael R. Leadbetter
Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.
Type:
Grant
Filed:
October 17, 2000
Date of Patent:
December 17, 2002
Assignee:
Theravance Inc.
Inventors:
Sabine M. Axt, Timothy J. Church, Witold Hruzewicz, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, J. Kevin Judice
Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.
Type:
Grant
Filed:
November 9, 2001
Date of Patent:
November 12, 2002
Assignee:
Theravance, Inc.
Inventors:
Daniel Marquess, Seok-Ki Choi, David T. Beattie, John H. Griffin, Scott Armstrong, Timothy J. Church, Thomas E. Jenkins, David C. Green
Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.
Type:
Grant
Filed:
October 1, 1999
Date of Patent:
October 8, 2002
Assignee:
Theravance, Inc.
Inventors:
Sabine M. Axt, Timothy J. Church, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, J. Kevin Judice, Huiwei Wu, Witold Hruzewicz
Abstract: Disclosed are derivatives of glycopeptide compounds having at least one substituent of the formula:
—Ra—Y—Rb—(Z)x
where Ra, Rb, Y, Z and x are as defined, and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Type:
Grant
Filed:
November 1, 2000
Date of Patent:
September 24, 2002
Assignee:
Theravance, Inc.
Inventors:
J. Kevin Judice, Paul Ross Fatheree, Bernice M. T. Lam, Michael Leadbetter, Martin Sheringham linsell, YongQi Mu, Sean Gary Trapp, Guang Yang, Yan Zhu
Abstract: Disclosed are derivatives of glycopeptide compounds having at least one substituent of the formula:
—Ra—Y—Rb—(Z)x
where Ra, Rb, Y, Z and x are as defined, and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Type:
Grant
Filed:
September 6, 2000
Date of Patent:
September 3, 2002
Assignee:
Advanced Medicine, Inc.
Inventors:
J. Kevin Judice, Paul Ross Fatheree, Bernice M. T. Lam, Michael R. Leadbetter, Martin S. Linsell, YongQi Mu, Sean Gary Trapp, Guang Yang, Yan Zhu
Abstract: This invention is directed to novel local anesthetic compounds, pharmaceutical compositions containing these compounds, methods of use and methods of preparing these compounds.
Type:
Grant
Filed:
September 28, 2000
Date of Patent:
August 20, 2002
Assignee:
Theravance Inc.
Inventors:
Sabine M. Axt, Timothy J. Church, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, Huiwei Wu
Abstract: This invention relates to novel multibinding compounds (agents) that are H1 histamine receptor antagonists and pharmaceutical compositions comprising such compounds. Accordingly, the multibinding compounds and pharmaceutical compositions of this invention are useful in the treatment and prevention of allergic diseases such as rhinitis, urticaria, asthma, and anaphylaxis, and the like.
Type:
Grant
Filed:
June 7, 1999
Date of Patent:
July 16, 2002
Assignee:
Theravance, Inc.
Inventors:
Robert P. Numerof, Yu-Hua Ji, John H. Griffin
Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.
Type:
Grant
Filed:
December 8, 1999
Date of Patent:
July 16, 2002
Assignee:
Advanced Medicine, Inc.
Inventors:
Daniel Marquess, Seok-Ki Choi, David T. Beattie, John H. Griffin, Scott Armstrong, Timothy J. Church, Thomas E. Jenkins
Abstract: Disclosed are derivatives of glycopeptide compounds having at least one substituent of the formula:
—Ra—Y—Rb—(Z)x
where Ra, Rb, Y, Z and x are as defined, and pharmaceutical compositions containing such glycopeptide derivatives. The disclosed glycopeptide derivatives are useful as antibacterial agents.
Type:
Grant
Filed:
December 22, 1999
Date of Patent:
May 21, 2002
Assignee:
Advanced Medicine, Inc.
Inventors:
J. Kevin Judice, Paul Ross Fatheree, Bernice M. T. Lam, Michael R. Leadbetter, Martin S. Linsell, YongQi Mu, Sean Gary Trapp, Guang Yang, Yan Zhu