Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 areas defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
March 12, 2009
Date of Patent:
December 28, 2010
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Yu-Hua Ji, YongQi Mu, Viengkham Malathong
Abstract: Disclosed are methods of purifying glycopeptides that are substituted with one or more substituents each comprising one or more phosphono groups that are useful as antibacterial agents. The methods include contacting a solution of the glycopeptide derivatives with a polystyrene-containing resin, eluting the resin with an aqueous solution, and isolating the purified glycopeptide derivative.
Type:
Grant
Filed:
November 17, 2008
Date of Patent:
December 28, 2010
Assignee:
Theravance, Inc.
Inventors:
Donald E. Schmidt, Jr., Jeanmarie Donovan Sganga
Abstract: The invention provides a crystalline freebase form of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compound, processes and intermediates for preparing the crystalline compound, and methods of using the crystalline compound to treat diseases such as hypertension.
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
July 19, 2007
Date of Patent:
December 14, 2010
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Yu-Hua Ji, YongQi Mu, Eric L. Stangeland, Aaron Kushner, Craig Husfeld
Abstract: The invention provides novel benzoimidazolone-carboxamide-derived carbamate 5-HT4 receptor agonist compounds of formula (I): wherein R1, R2, R3, R4, a, and b are defined in the disclosure. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
December 6, 2007
Date of Patent:
December 14, 2010
Assignee:
Theravance, Inc.
Inventors:
Daniel D. Long, Seok-Ki Choi, Paul R. Fatheree, Adam A. Goldblum, Daniel Marquess
Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
July 19, 2007
Date of Patent:
December 14, 2010
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
Abstract: The present invention relates to the preparation of a ?2 adrenergic agonist in crystalline salt form. In particular the invention relates to preparation of a crystalline salt of compound (I) in particular a crystalline monohydrochloride salt. The invention also relates to a new crystalline form (polymorph) of the monohydrochloride salt of compound (Ia) and a process for preparing it.
Type:
Grant
Filed:
March 30, 2005
Date of Patent:
December 7, 2010
Assignee:
Theravance, Inc.
Inventors:
Darren Michael Caine, Ian Leonard Paternoster, Peter David Penberthy Shapland
Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
February 21, 2008
Date of Patent:
November 16, 2010
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
Abstract: The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
September 5, 2008
Date of Patent:
November 16, 2010
Assignee:
Theravance, Inc.
Inventors:
Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Vivek Sasikumar
Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, Ar1, Ar2, E, a, b, c and z are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Type:
Grant
Filed:
May 8, 2009
Date of Patent:
September 28, 2010
Assignee:
Theravance, Inc.
Inventors:
Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
Abstract: The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
January 15, 2008
Date of Patent:
August 31, 2010
Assignee:
Theravance, Inc.
Inventors:
Paul Fatheree, Roland Gendron, Adam A Goldblum, Daniel D Long, Daniel Marquess, S. Derek Turner, Seok-Ki Choi
Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
Type:
Grant
Filed:
January 31, 2008
Date of Patent:
August 17, 2010
Assignee:
Theravance, Inc.
Inventors:
Seok-Ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert M. McKinnell, Vivek Sasikumar
Abstract: This invention relates to cinnamate salts of 5-[(R)-2-(2-{4-[4-(2-amino-2-methyl-propoxy)-phenylamino]-phenyl}-ethylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one.