Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I:
where:
R1 is a group represented by formula (A), (B) or (C);
and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods for their use as therapeutic agents.
Type:
Grant
Filed:
April 29, 2003
Date of Patent:
February 17, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
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:
March 14, 2001
Date of Patent:
February 17, 2004
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 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:
September 26, 2001
Date of Patent:
January 27, 2004
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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:
May 22, 2001
Date of Patent:
December 23, 2003
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: 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:
May 9, 2000
Date of Patent:
November 18, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
John David Allard, Renu Anand Ileller, Paul Klonowski, Harold Edgar VanWart
Abstract: Alkylamino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives are provided which are useful as inhibitors of p38, along with a process for their manufacture and pharmaceutical preparations containing them.
Type:
Grant
Filed:
October 20, 2000
Date of Patent:
November 4, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
James Patrick Dunn, David Michael Goldstein, William Harris, Ian Edward David Smith, Teresa Rosanne Welch
Abstract: The invention relates to compounds of the general formula
wherein
(R1)n is independently from from each other halogen, lower alkyl or lower alkoxy;
R2 is hydrogen, lower alkyl, lower halogen-alkyl, —(CH2)m—OH, —(CH2)m—NR2, —(CH2)mO-lower alkyl, —(CH2)m—C(O)—NR2, or is —(CH2)m-6-membered heteroaryl, optionally substituted by one or more lower alkoxy, —(CH2)m-5 or 6-membered not aromatic heterocyclyl, optionally substituted by hydroxy or lower alkyl;
R is hydrogen or lower alkyl and may be the same or different in case of R2;
n is 0, 1, or 2;
m is 0, 1, 2, 3 or 4;
and pharmaceutically acceptable acid addition salts thereof. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable for the treatment of diseases, related to this receptor.
Type:
Grant
Filed:
May 10, 2002
Date of Patent:
July 29, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Hai-Ying Cai, Michael Patrick Dillon, Guido Galley, Annick Goergler, Sabine Kolczewski, Dawn Muszynski Barsy
Abstract: This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I:
where:
R1 is a group represented by formula (A), (B) or (C);
and other substituents as defined in the specification, and their pharmaceutically acceptable salts or crystal forms thereof; and pharmaceutical compositions containing them; and methods and their use as therapeutic agents.
Type:
Grant
Filed:
May 31, 2002
Date of Patent:
July 22, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
Abstract: The invention provides TCCV-1 or TCCV-2 from human, reagents related thereto including polynucleotides encoding TCCV-1 or TCCV-2, purified polypeptides, and specific antibodies. Methods of making and using these reagents, in particular, methods for screening compounds which modulate TCCV-1 or TCCV-2 activity are provided. Also provided are methods of diagnosis and kits.
Type:
Grant
Filed:
August 23, 2001
Date of Patent:
July 8, 2003
Assignee:
Syntex (U.S.A.) LLC
Inventors:
Paul Shartzer Dietrich, Joseph Gerrard McGivern
Abstract: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I):
wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is 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 methods of preparation thereof.
Type:
Grant
Filed:
March 1, 2002
Date of Patent:
May 27, 2003
Assignee:
Roćhe Palo Alto LLC
Inventors:
Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
Abstract: The present invention provides an optical multimeter for use in calibrating and testing optical components. The optical multimeter includes an optical analog/digital signal generator for delivering an output beam over a wide range of frequencies, duty cycles and amplitudes. The optical signal generator includes a tunable laser. The tunable laser exhibits a small form factor, due in part to a novel wavelength control process which utilizes an open loop system to maintain precise output wavelength control, without the requirement of either a wavelength or position feedback device.
Type:
Grant
Filed:
September 10, 1999
Date of Patent:
August 13, 2002
Assignee:
New Focus, Inc.
Inventors:
Alexander V. Tuganov, Alejandro D. Farinas
Abstract: An image comparison apparatus and method for use in preoperative planning procedures which provides for superposition of a transparent medium with an image thereon, such as a medical x-ray, and a computer-interfaced display screen, and which allows a user to size, orient and spatially manipulate a digital image of on the display screen with respect to the superimposed medical transparency. A computer associated with the display screen periodically receives information updates for displayable images from product and advertising sources and electronic catalogs. The computer also transfers data to market services.
Abstract: An interferometer and related methods for wavelength monitoring are disclosed. The interferometer may be used for the wavelength monitoring or as part of a wavelength feedback and control circuit for an optical signal source. The device operates by creating an output beam on which constructive and destructive optical interference may be detected. The optical interference is generated by a monochromatic beam split into a first beam traversing a stationary path and a second beam traversing a path of variable length. The first and second beams are then recombined to create constructive/destructive interference which may be measured by a detector and correlated with a processor to determine the output wavelength of the optical source. The maximum and minimum of the variable path length are precisely controlled due to use of a micro-positionable semiconductor retroreflector or mirror.
Abstract: The present invention provides an apparatus for passively stabilizing the tuning element in tunable lasers. Lasers stabilized using the passive stabilization of the tuning element exhibit reduced mode hop and increased wavelength stability during temperature variations of the laser or surrounding environment. The stabilization makes the laser suitable for a broad range of applications including optical signal generators and optical multimeters.
Type:
Grant
Filed:
September 10, 1999
Date of Patent:
December 11, 2001
Assignee:
New Focus, Inc.
Inventors:
Alexander V. Tuganov, David F. Arnone, Bruce A. Moore, Emmerich Mueller
Abstract: A high throughput virus in vitro infectivity assay method comprising growing cells in a multi-well format, infecting the cells with intact virion incubated with a test agent, and measuring expression of at least one viral nucleic acid sequence in the cells. The method also preferably comprises incubating intact virion without test agent to define a control. The cells are preferably human keratinocyte cells grown in monolayers. The viral nucleic acid sequence will generally comprise viral mRNA. In one preferred embodiment, the intact virion comprise Human Papilloma Virus, and more preferably Human Papilloma Virus-11. Measuring expression is generally carried out by releasing the viral mRNA from the cells by lysis, amplifying the mRNA as CDNA via RT-PCR, and detecting amplicons with specific probes. Cell lysis may be carried out by heating or by treatment with detergent.