Patents Assigned to Syntex (U.S.A.) LLC
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Publication number: 20030158226Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: ApplicationFiled: September 17, 2002Publication date: August 21, 2003Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLCInventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
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Publication number: 20030158178Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.Type: ApplicationFiled: October 30, 2002Publication date: August 21, 2003Applicant: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Publication number: 20030153586Abstract: The present invention provides compounds of the formula: 1Type: ApplicationFiled: August 29, 2002Publication date: August 14, 2003Applicant: Syntex (U.S.A) LLCInventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
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Publication number: 20030144303Abstract: Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.Type: ApplicationFiled: November 6, 2002Publication date: July 31, 2003Applicant: Syntex (U.S.A.) LLCInventors: Ronald Charles Hawley, Sharada Shenvi Labadie, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 6599900Abstract: 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: GrantFiled: May 10, 2002Date of Patent: July 29, 2003Assignee: Syntex (U.S.A.) LLCInventors: Hai-Ying Cai, Michael Patrick Dillon, Guido Galley, Annick Goergler, Sabine Kolczewski, Dawn Muszynski Barsy
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Patent number: 6596876Abstract: 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: GrantFiled: May 31, 2002Date of Patent: July 22, 2003Assignee: Syntex (U.S.A.) LLCInventors: Keith Roger Bley, Robin Douglas Clark, Alam Jahangir, Bruce Andrew Kowalczyk, Francisco Javier Lopez-Tapia, Alexander Victor Muehldorf, Counde O'Yang, Thomas Weitao Sun
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Publication number: 20030130319Abstract: The present invention provides an aminopyrrole compound of the formula: 1Type: ApplicationFiled: August 29, 2002Publication date: July 10, 2003Applicant: Syntex (U.S.A.) LLCInventors: David Michael Goldstein, David Mark Rotstein
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Patent number: 6589787Abstract: 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: GrantFiled: August 23, 2001Date of Patent: July 8, 2003Assignee: Syntex (U.S.A.) LLCInventors: Paul Shartzer Dietrich, Joseph Gerrard McGivern
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Publication number: 20030125383Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: ApplicationFiled: September 17, 2002Publication date: July 3, 2003Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6559153Abstract: This invention relates to compounds which are generally alpha-1B adrenergic receptor antagonists and which are represented by Formula (I): wherein R′, R″, R1, R2, m, n, and A are as defined in the specification, or acceptable prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: August 29, 2001Date of Patent: May 6, 2003Assignee: Syntex (U.S.A.) LLCInventors: Cyrus Kephra Becker, Chris Richard Melville, Jürg Roland Pfister, Xiaoming Zhang
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Patent number: 6559138Abstract: The present invention provides 3-desoxy vitamin D3 analog esters of the formula: and methods for use and preparation of the same, wherein the dotted line, R1, R2, R3, R4 and L are those defined herein.Type: GrantFiled: September 18, 2002Date of Patent: May 6, 2003Assignee: Syntex (U.S.A.) LLCInventor: Milan Radoje Uskokovic
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Patent number: 6552028Abstract: This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: December 19, 2001Date of Patent: April 22, 2003Assignee: Syntex (U.S.A.) LLCInventors: Denis John Kertesz, Michael Garret Roepel
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Patent number: 6518460Abstract: This invention provides processes for the preparation of a compound of Formula I: Y—C(═O)—C(R1)(R2)—CH2—S(O)nR3 wherein: Y is hydroxy or XONX, where each X is independently hydrogen, lower alkyl or lower acyl; R1 is hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, or R1 and R2 together with the carbon atom to which they are attached form a cycloalkyl or heterocyclo group; R3 is aryl; and n is 0, 1 or 2. The invention also provides novel aryl haloalkyl sulfide intermediates useful for the preparation of compounds of Formula I and novel methods of preparing aryl alkyl sulfides.Type: GrantFiled: May 8, 2002Date of Patent: February 11, 2003Assignee: Syntex (U.S.A.) LLCInventors: Jeffrey Allen Campbell, Lawrence Emerson Fisher, Charles Alois Dvorak, Paul Leo McGrane
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Patent number: 6518276Abstract: The present invention provides compounds of the formula: wherein R1, R3, and Ar1 are those defined herein, and R2 is —CR′R″—Ra (where R′ and R″ are hydrogen, hydroxyalkyl or alkyl with at least one being alkyl or hydroxyalkyl and Ra is hydroxyalkyl), Rx—S—Ry— (where Rx is alkyl and Ry is alkylene), alkoxy-substituted alkyl, heterocyclylalkyl or C4-C5 cycloalkyl, wherein each of the hydroxy group present in R2 can be independently Ra—C(═O)—O, RaRbN—C(═O)—O, or Ra—S(O)2—O—, wherein Ra and Rb are independently hydrogen, alkyl, aryl, or aralkyl, and methods for preparation and uses thereof.Type: GrantFiled: August 30, 2001Date of Patent: February 11, 2003Assignee: Syntex (U.S.A.) LLCInventors: Humberto Bartolome Arzeno, Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
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Patent number: 6515198Abstract: The invention provides a method of treatment for an animal having a disease state associated with a genitourinary disorder with a purinergic receptor modulator. Also provided, is a transgenic animal having a disrupted purinergic receptor gene. The invention further provides for a method of screening using the transgenic animal as a positive control.Type: GrantFiled: February 13, 2001Date of Patent: February 4, 2003Assignee: Syntex (U.S.A.) LLCInventors: Debra Ann Cockayne, Anthony P. D. W. Ford, Quan-Ming Zhu, Wilhelm G. Lachnit, Annika B. Malmberg
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Patent number: 6506749Abstract: The present invention provides compounds of the formula: wherein R2 is substituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl-alkyl, optionally substituted heterocyclyl, spiro-substituted cycloalkyl, aralkoxy, alkoxy, -alkylene-S(O)n-alkyl (wherein n is 1 or 2), or —SO2Ar2; and R1, R3, and Ar1 are those defined herein, and methods for preparation and uses thereof.Type: GrantFiled: August 30, 2001Date of Patent: January 14, 2003Assignee: Syntex (U.S.A.) LLCInventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
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Patent number: 6500822Abstract: 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 NR4, 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: GrantFiled: May 22, 2001Date of Patent: December 31, 2002Assignee: Syntex (U.S.A.) LLCInventors: Robert James Weikert, Ann Marie Madera, Russell Stephen Stabler
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Patent number: 6492394Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.Type: GrantFiled: December 22, 1999Date of Patent: December 10, 2002Assignee: Syntex (U.S.A.) LLCInventors: Roland Joseph Billledeau, Chris Allen Broka, Jeffrey Allen Campbell, Jian Jeffrey Chen, Sharon Marie Dankwardt, Nancy Delaet, Leslie Ann Robinson, Keith Adrian Murray Walker
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Patent number: 6479259Abstract: The present invention relates to a voltage-gated sodium channel present in peripheral nerve tissue that is tetrodotoxin-resistant. One aspect of the present invention is purified and isolated DNA encoding this sodium channel. Another aspect of the present invention is the recombinant protein expressed by this DNA, expression vectors comprising the DNA sequence, and host cells transformed with these expression vectors. Another aspect of this invention is the use of this voltage-gated, tetrodotoxin-resistant sodium channel as a therapeutic target for compounds to treat disorders of the peripheral nervous system.Type: GrantFiled: March 16, 2000Date of Patent: November 12, 2002Assignee: Syntex (U.S.A.) LLCInventors: Ronald Herman, Stephen Gregory Delgado, Linda Marie Fish, Lakshmi Sangameswaran, Douglas Kenneth Rabert
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Patent number: 6479507Abstract: The present invention relates to compounds of Formula (I) that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 19, 2001Date of Patent: November 12, 2002Assignee: Syntex (U.S.A.) LLCInventors: Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren