Abstract: Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
Abstract: Compounds effective as IP receptor modulators, particularly IP receptor antagonists, that are of the formula I: wherein A, R1, R2, R3 and R4 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
Type:
Grant
Filed:
September 1, 2005
Date of Patent:
October 9, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Paul Francis Keitz, Alam Jahangir, Francisco Javier Lopez-Tapia, Counde O'Yang
Abstract: The invention provides compounds of the Formula: wherein m, n, A, X, Y, Z, R1, R2, R4, R6, R7, R8, R9 and R10 are as defined herein, and pharmaceutically acceptable salts, solvates, prodrugs, single isomers or racemic or non-racemic mixture of isomers thereof. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, and n are those defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
Abstract: Compounds represented by Formula I: which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R?, R5 and R10 are as defined herein.
Type:
Grant
Filed:
July 2, 2004
Date of Patent:
July 17, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Terrence Joseph Connolly, Paul Francis Keitz, Eun Kyung Lee, Jim Li, Francisco Javier Lopez-Tapia, Patrick Finbar McGarry, Chris Richard Melville, Dov Nitzan, Counde O'Yang, Fernando Padilla, Klaus Kurt Weinhardt
Abstract: Compounds of the Formula I: wherein m, n, k, A, X, Y, Z, Ar, R1, R2, R3, and R4 are as defined herein. The compounds are useful as 5-HT6 receptor antagonists. Also provided are compositions comprising, methods of using, and methods of making the subject compounds.
Type:
Grant
Filed:
December 9, 2005
Date of Patent:
June 12, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
Abstract: Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein m, R1, R2, R3, R4, R5 and R6 are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula (I).
Type:
Grant
Filed:
August 11, 2004
Date of Patent:
May 29, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Robin Douglas Clark, Richard Leo Cournoyer, Counde O′Yang
Abstract: Compounds of the formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9, X, Y and m are as defined herein. Also provided are compositions comprising, methods for using, and methods for preparing compound of formula (I).
Type:
Grant
Filed:
December 9, 2004
Date of Patent:
April 10, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof, wherein X is CH or N, Y is C or S, Z is —(CRaRb)r— or —SO2—, A is —NR3— or —O—, R2 is optionally substituted aryl or optionally substituted heteroaryl, n is 1 or 2, m is 1 when Y is C and m is 2 when Y is S, and p, q, r, R1, R3, R4, R5, R6, R7, R8, R9, R10, Ra and Rb are as defined herein. The compounds are useful in the treatment of 5-HT6 and 5-HT2A mediated diseases.
Type:
Grant
Filed:
January 14, 2005
Date of Patent:
March 27, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Nancy Elisabeth Krauss, Meng Sui, Shu-Hai Zhao
Abstract: The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein, n, X, Y, R1, R2, R3, R4 and R5 are as defined herein. The subject compounds are useful for treatment of 5-HT6 receptor antagonist-mediated diseases. Also provides are methods for preparing, compositions comprising, and methods for using the subject compounds.
Abstract: The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.
Type:
Grant
Filed:
November 25, 2003
Date of Patent:
January 30, 2007
Assignee:
Roche Palo Alto LLC
Inventors:
Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Christoph Martin Stahl
Abstract: Human aggrecanase and polypeptides related thereto, as well as nucleic acid compositions encoding the same, are provided. The subject polypeptides and nucleic acid compositions find use in a variety of applications, including research, diagnostic, and therapeutic agent screening applications. Also provided are methods of inhibiting aggrecanase activity in a host and methods of treating disease conditions associated with aggrecanase activity, e.g. rheumatoid arthritis, osteo-arthritis, infectious arthritis, gouty arthritis, psoriatic arthritis, spondolysis, sports injury, joint trauma, pulmonary disease, fibrosis, and the like.
Type:
Grant
Filed:
September 17, 2003
Date of Patent:
August 22, 2006
Assignee:
Syntex (U.S.A.) LLC
Inventors:
John David Allard, Renu Anand Heller, Paul Klonowski, Harold Edgar Van Wart
Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
Type:
Grant
Filed:
October 14, 2003
Date of Patent:
August 22, 2006
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Charles Alois Dvorak, Lawrence Emerson Fisher, Keena Lynn Green, Ralph New Harris, III, Hans Maag, Anthony Prince, David Bruce Repke, Russell Stephen Stabler
Abstract: A container with first and second opposing, parallel side panels; third and fourth opposing, parallel side panels which define an enclosure; optional first, second, third and fourth corner panels interposed between adjacent ones of the side panels; first and second top flaps respectively associated with the first and second side panels by first and second top creases or fold lines; and third and fourth top flaps respectively associated with the third and fourth side panels by third and fourth top creases or fold lines. The first top crease or fold line is coplanar with a top plane of the container; and the third and fourth top creases are offset below the top plane.
Abstract: The invention provides compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein R1, R2, R3, R4, m and n are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
Abstract: Methods for treatment of IP antagonist mediated diseases or conditions by administration to a subject in need thereof a compound of formula (I) wherein R1, R2, A and X are as defined herein. Also disclosed are compounds and related compositions.
Type:
Grant
Filed:
July 9, 2004
Date of Patent:
July 18, 2006
Assignee:
Roche Palo Alto LLC
Inventors:
Keith Roger Bley, Robin Douglas Clark, Alam Jahangir
Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.
Type:
Grant
Filed:
May 9, 2003
Date of Patent:
June 6, 2006
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Jr., Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein R1, R2, R3, R4, and R5 are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
Type:
Grant
Filed:
October 16, 2003
Date of Patent:
April 4, 2006
Assignee:
Roche Palo Alto LLC
Inventors:
Robin Douglas Clark, Ralph New Harris, III, David Bruce Repke
Abstract: Compounds effective as IP receptor modulators, particularly IP receptor antagonists, that are of the formula I: wherein A, R1, R2, R3 and R4 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
Type:
Grant
Filed:
April 29, 2004
Date of Patent:
February 14, 2006
Assignee:
Roche Palo Alto LLC
Inventors:
Paul Francis Keitz, Alam Jahangir, Francisco Javier Lopez-Tapia, Counde O'Yang
Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Type:
Grant
Filed:
November 21, 2003
Date of Patent:
January 10, 2006
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm