Patents Assigned to Theravance, Inc.
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Publication number: 20140329845Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 4, 2014Publication date: November 6, 2014Applicant: THERAVANCE, INC.Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
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Publication number: 20140288112Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: January 15, 2014Publication date: September 25, 2014Applicant: THERAVANCE, INC.Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
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Publication number: 20140288033Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: ApplicationFiled: March 19, 2014Publication date: September 25, 2014Applicant: THERAVANCE, INC.Inventors: Sabine Axt, Timothy J. Church
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Publication number: 20140274877Abstract: The present invention relates to a compound of formula I: wherein x is in the range of from about 1 to about 2. The invention also relates to pharmaceutical compositions containing such compounds; processes for preparing such compounds; and methods of using such compounds to, for example, treat a bacterial infection.Type: ApplicationFiled: March 6, 2014Publication date: September 18, 2014Applicant: THERAVANCE, INC.Inventors: Weijiang Zhang, Ronnie Cheung, Dimitar Filipov, Jack Green, Junning Lee
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Publication number: 20140275554Abstract: The invention relates to a crystalline form of a triethylamine salt of (2Z)-2-(2-amino-5-chlorothiazol-4-yl)-2-(3-N-tert-butoxycarbonylaminopropoxyimino)acetic acid. The invention also relates to processes and intermediates for preparing the crystalline form. The crystalline form is useful as an intermediate for preparing cross-linked glycopeptide-cephalosporin antibiotics.Type: ApplicationFiled: March 6, 2014Publication date: September 18, 2014Applicant: THERAVANCE, INC.Inventors: Weijiang Zhang, Michael R. Tracey, Junning Lee
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Publication number: 20140256702Abstract: 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.Type: ApplicationFiled: March 4, 2014Publication date: September 11, 2014Applicant: THERAVANCE, INC.Inventors: Erik Fenster, Melissa Fleury, Adam D. Hughes
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Publication number: 20140256769Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.Type: ApplicationFiled: January 8, 2014Publication date: September 11, 2014Applicant: THERAVANCE, INC.Inventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
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Publication number: 20140243536Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: November 26, 2013Publication date: August 28, 2014Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
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Publication number: 20140235864Abstract: 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.Type: ApplicationFiled: November 22, 2013Publication date: August 21, 2014Applicant: THERAVANCE, INC.Inventors: Mathai Mammen, Adam Hughes, Yan Chen
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Publication number: 20140194426Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: October 24, 2013Publication date: July 10, 2014Applicant: THERAVANCE, INC.Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
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Publication number: 20140171397Abstract: 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: ApplicationFiled: September 11, 2013Publication date: June 19, 2014Applicant: THERAVANCE, INC.Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
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Patent number: 8754223Abstract: The invention provides a crystalline 1,2-ethanedisulfonic acid salt of biphenyl-2-ylcarbamic acid 1-[2-(2-chloro-4-{[(R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethylamino]methyl}-5-methoxyphenylcarbamoyl)ethyl]piperidin-4-yl ester or a solvate thereof. This invention also provides pharmaceutical compositions comprising such a salt or prepared using such a salt; processes and intermediates for preparing such a salt; and methods of using such a salt to treat a pulmonary disorder.Type: GrantFiled: June 5, 2013Date of Patent: June 17, 2014Assignee: Theravance, Inc.Inventors: Robert S. Chao, Miroslav Rapta, Pierre-Jean Colson
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Patent number: 8754225Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.Type: GrantFiled: June 30, 2011Date of Patent: June 17, 2014Assignee: Theravance, Inc.Inventor: Pierre-Jean Colson
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Publication number: 20140163063Abstract: The invention provides novel quinolinone-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: ApplicationFiled: October 1, 2013Publication date: June 12, 2014Applicant: THERAVANCE, INC.Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
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Patent number: 8735625Abstract: 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: GrantFiled: January 31, 2013Date of Patent: May 27, 2014Assignee: Theravance, Inc.Inventors: Seok-ki Choi, Paul R. Fatheree, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Vivek Sasikumar
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Patent number: 8729119Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: May 22, 2013Date of Patent: May 20, 2014Assignee: Theravance, Inc.Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
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Publication number: 20140135333Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 16, 2014Publication date: May 15, 2014Applicant: THERAVANCE, INC.Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8716313Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.Type: GrantFiled: January 14, 2013Date of Patent: May 6, 2014Assignee: Theravance, Inc.Inventors: Sabine Axt, Timothy J Church
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Publication number: 20140121385Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.Type: ApplicationFiled: January 7, 2014Publication date: May 1, 2014Applicant: THERAVANCE, INC.Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
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Publication number: 20140121378Abstract: The invention provides a process of preparing an intermediate useful in the synthesis of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and a process of preparing a crystalline freebase of the ester.Type: ApplicationFiled: November 26, 2013Publication date: May 1, 2014Applicant: THERAVANCE, INC.Inventor: Pierre-Jean Colson