Patents Assigned to Syntex (U.S.A.)
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Patent number: 6979693Abstract: The present invention relates to certain pyrazole derivatives 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: February 1, 2002Date of Patent: December 27, 2005Assignee: Syntex (U.S.A.) LLCInventors: David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjogren, Francisco Xavier Talamas
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Patent number: 6967093Abstract: A novel human glycosylsulfotransferase expressed in high endothelial cells (GST-3) 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 selectin mediated binding events and methods of treating disease conditions associated therewith.Type: GrantFiled: March 22, 2001Date of Patent: November 22, 2005Assignees: The Regents of the University of California, Syntex (U.S.A) LLCInventors: Annette Bistrup, Steven D. Rosen, Stefan Hemmerich
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Patent number: 6951918Abstract: This invention relates to compounds of Formula (I) wherein R1-R7, A, Z and n are as described in the Summary of the Invention that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for their preparation.Type: GrantFiled: February 7, 2002Date of Patent: October 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Sharon Marie Dankwardt, Harold Edgar Van Wart, Keith Adrian Murray Walker
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Patent number: 6933142Abstract: Mammalian glycosylsulfotransferases expressed in high endothelial cells (HEC-GLCNAC6ST) 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 diagnostic, and therapeutic agent screening applications. Also provided are methods of inhibiting selectin mediated binding events and methods of treating disease conditions associated therewith, particularly by administering an inhibitor of at least one of HEC-GLCNAC6ST or KSGal6ST, or homologues thereof.Type: GrantFiled: August 23, 2000Date of Patent: August 23, 2005Assignees: The Regents of the University of California, Syntex (USA), LLCInventors: Annette Bistrup, Steven D. Rosen, Stefan Hemmerich
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Patent number: 6903086Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; 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: GrantFiled: March 1, 2002Date of Patent: June 7, 2005Assignee: SYNTEX (U.S.A.) LLCInventors: Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
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Patent number: 6900220Abstract: This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is carbon or nitrogen, Y is carbon, and X—Y considered together are two adjoining atoms of the ring A, said ring being a fused aromatic ring of five to six atoms per ring optionally incorporating one to two heteroatoms per ring, chosen from N, O, or S; and the other substituents 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 methods of preparation thereof.Type: GrantFiled: January 2, 2002Date of Patent: May 31, 2005Assignee: Syntex (U.S.A.) LLCInventors: Cyrus Kephra Becker, Joan Marie Caroon, Chris Richard Melville, Fernando Padilla, Jürg Roland Pfister, Xiaoming Zhang
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Patent number: 6900336Abstract: This invention relates to compounds which are generally EP4 receptor agonists and which are represented by Formula I: wherein A is a —CH2—CH2—, or —CH?CH—; B is absent, an aryl, or heteroaryl group; R1 is alkyl, alkenyl, alkynyl, cycloalkylalkyl, heterocyclylalkyl, aryl, arylalkyl or heteroaryl, when B is aryl or heteroaryl and R3, R4, R5 and R6 are not simultaneously hydrogen, or R1 is heterocyclylalkyl, aryl, or heteroaryl when B is absent and R3, R4, R5 and R6 are simultaneously hydrogen; and the other substituents 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 methods of preparation thereof.Type: GrantFiled: July 16, 2002Date of Patent: May 31, 2005Assignee: Syntex (U.S.A.) LLCInventors: Todd Richard Elworthy, Tara Mirzadegan, Michael Garret Roepel, David Bernard Smith, Keith Adrian Walker
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Patent number: 6893842Abstract: 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: April 29, 2003Date of Patent: May 17, 2005Assignee: Syntex (U.S.A.) LLCInventors: Paul Shartzer Dietrich, Joseph Gerrard McGivern
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Patent number: 6872744Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —O—, —S—, or —S(O)—; and the other substituents are as defined in the specification; or individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.Type: GrantFiled: September 26, 2002Date of Patent: March 29, 2005Assignee: Syntex (U.S.A.) LLCInventors: Chris Allen Broka, Jeffrey Allen Campbell
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Patent number: 6864266Abstract: This invention relates to the (R)-isomers of compounds which are generally muscarinic receptor antagonists and which are represented by Formula I: wherein p, R1, R2, R3 and A are as defined in the specification, or individual isomers, racemic or non-racemic mixtures of isomers, or acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use and preparation as therapeutic drugs.Type: GrantFiled: July 1, 2003Date of Patent: March 8, 2005Assignee: Syntex (U.S.A.) LLCInventors: Christine E. Brotherton-Pleiss, Ann Marie Madera, Robert James Weikert
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Patent number: 6861423Abstract: Disorders mediated by p38 kinase inhibitors are treated with compounds of the formula: or salts thereof, wherein: R1 is hydrogen or alkyl; R2 is substituted cycloalkyl, heterosubstituted cycloalkyl, helcroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl-alkly, heterocyclyl, heterocyclyl spiro cycloalkyl, aralkoxy, alkoxy, -alkylene-S(O)n-alkyl (where is 1 or 2) or —SO2Ar2; R3 is hydrogen, amino, monoalkylamino, dialkylamino, acylamino, —NR8—C(?O)—Rb (where Ra is hydrogen or alkyl and Rh is heterocyclyl or heteroalkyl), alkyl, cycloalkyl, phthalimidoalkyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(O) R (where R is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino) or acyl; and each of Ar1 and Ar2 is independently aryl.Type: GrantFiled: August 29, 2002Date of Patent: March 1, 2005Assignee: Syntex (U.S.A.) LLCInventors: Jian Jeffrey Chen, James Patrick Dunn, David Michael Goldstein, Julie Anne Lim
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Patent number: 6852518Abstract: Novel glycosylsulfotransferases (GST-4?, GST-4?, and GST-6) 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 various diagnostic and therapeutic agent screening applications. Also provided are methods of inhibiting selectin mediated binding events and methods of treating disease conditions associated therewith, particularly by administering an inhibitor of at least one of GST-4?, GST-4?, and GST-6.Type: GrantFiled: June 13, 2000Date of Patent: February 8, 2005Assignees: The Regents of the University of California, Syntex (U.S.A.) LLCInventors: Steven D. Rosen, Jin Kyu Lee, Stefan Hemmerich
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Patent number: 6852726Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein X is —S(O)n— or —C(O)—, A is C1-6alkyl, aryl, heteroaryl, hydroxyalkyl, or —(CH2)p—NRaRb, and the other substituents 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 methods of preparation thereof.Type: GrantFiled: January 31, 2003Date of Patent: February 8, 2005Assignee: Syntex LLCInventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
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Patent number: 6849657Abstract: This invention relates to 8-aza prostanoid analogs which are generally EP4 receptor agonists and are represented by Formula I: wherein Q, B, X, J, Z, A and R1-R6 are as defined, their synthesis and use for treatment of osteoporosis and increasing bone density.Type: GrantFiled: July 16, 2002Date of Patent: February 1, 2005Assignee: Syntex (U.S.A.) LLCInventors: Todd Richard Elworthy, Michael Garret Roepel, David Bernard Smith
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Patent number: 6846834Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.Type: GrantFiled: October 23, 2001Date of Patent: January 25, 2005Assignees: Amgen Inc., Syntex (U.S.A.) LLCInventors: Michelle F. Browner, David L. Clark, Timothy D. Cushing, Xiaolin Hao, Ronald C. Hawley, Xiao He, Juan C. Jaen, Sharada S. Labadie, Marie-Louise Smith, Francisco X. Talamas, Nigel P. C. Walker, Marc Labelle
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Patent number: 6844175Abstract: A novel human glycosylsulfotransferase expressed in high endothelial cells (GST-3) and polypeptides related thereto, as well as nucleic acid compositions encoding the same, are provided. The subject polypeptides and nucleic acid find use in a variety of applications, including research, diagnostic, and therapeutic agent screening applications.Type: GrantFiled: November 8, 2001Date of Patent: January 18, 2005Assignees: The Regents of the University of the California, Syntex (U.S.A.) INCInventors: Annette Bistrup, Steven D. Rosen, Kirsten Tangemann, Stefan Hemmerich
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Patent number: 6844366Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: October 9, 2002Date of Patent: January 18, 2005Assignee: 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: 6844466Abstract: 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: GrantFiled: September 17, 2002Date of Patent: January 18, 2005Assignee: Syntex (U.S.A.) LLCInventors: Paula Nanette Belloni, Denis John Kertesz, Michael Klaus, Jean-Marc Lapierre
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Patent number: 6838472Abstract: 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: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
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Patent number: 6825202Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R1, R2, R3 or R4 are as defined in the specification, 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: GrantFiled: August 9, 2002Date of Patent: November 30, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao