Patents by Inventor Thomas J. Caulfield
Thomas J. Caulfield has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Publication number: 20100113462Abstract: The present invention relates to novel compounds of the formula I: wherein in any of its stereoisomeric forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.Type: ApplicationFiled: November 30, 2009Publication date: May 6, 2010Applicant: SANOFI-AVENTISInventors: Thomas J. CAULFIELD, Jennifer Williford CLEMENS, Robert S. FRANCIS, Brian S. FREED, Stanly JOHN, Tieu-Binh LE, Brian PEDGRIFT, Antonio D. RAMOS, Gerard Charles ROSSE, Martin SMRCINA, David S. THORPE, William WIRE, Jianhong ZHAO
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Patent number: 7005440Abstract: The use of triaryl acid derivatives of formula (I) and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: November 28, 2000Date of Patent: February 28, 2006Assignee: Aventis Pharma Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko, Robert Morris
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Patent number: 6984645Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula wherein A, B, X, Y, R1, R2 and R3 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing dual aP2/k-FABP inhibitors alone or in combination with at least one other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: November 15, 2002Date of Patent: January 10, 2006Assignee: Bristol-Myers Squibb CompanyInventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
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Publication number: 20030225091Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1Type: ApplicationFiled: November 15, 2002Publication date: December 4, 2003Inventors: David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Thomas J. Caulfield, Rex A. Parker
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Patent number: 6635655Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: September 14, 2000Date of Patent: October 21, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko
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Patent number: 6624309Abstract: Benzoic acid derivatives of the formula where X is oxygen, sulfur, —NH, —NR1, —N—CN, —N—OR1 or —N—NO2; Y is a single bond, —C═C—, or —NH; R1 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heterocyclo, or (heterocyclo)alkyl; and R2 is aryl or heterocyclo. The compounds of formula I are useful in the treatment of arrhythmia.Type: GrantFiled: September 25, 2002Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss
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Publication number: 20020137968Abstract: Benzoic acid derivatives of the formula I 1Type: ApplicationFiled: October 10, 2001Publication date: September 26, 2002Inventors: John Lloyd, George C. Rovnyak, Philip D. Stein, Saleem Ahmad, Karnail S. Atwal, Thomas J. Caulfield, Michael A. Poss
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Patent number: 5620677Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-5;m is 1-15;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.Type: GrantFiled: February 1, 1994Date of Patent: April 15, 1997Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Eugene R. Cooper, John L. Toner, Donald A. Upson, Brent D. Douty, Thomas J. Caulfield, Edward R. Bacon, Kimberly G. Estep, Kurt A. Josef, Shaughnessy Robinson, Paul P. Spara
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Patent number: 5607660Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an iodophenoxy alkane, iodophenyl alkenylalkyl ether or an iodophenyl alkynylalkyl ether x-ray producing agent in combination with a cellulose derivative in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.Type: GrantFiled: May 20, 1994Date of Patent: March 4, 1997Assignee: Sterling Winthrop Inc.Inventors: Robert W. Lee, Carl R. Illig, Thomas J. Caulfield
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Patent number: 5476644Abstract: The present invention provides compounds of the formula ##STR1## chelated with a paramagnetic metal ion wherein Z1 and Z2 each represent the atoms necessary to complete a monocyclic or polycyclic carbocyclic or heterocyclic ring system, said Z1 and Z2 independently optionally substituted with R.sup.6 and R.sup.7, respectively;R.sup.l, R.sup.2, R.sup.3 and R.sup.4 are independently carboxyalkyl (C.sub.1 -C.sub.2), --(CH.sub.2).sub.n --C(.dbd.O)--NH--R.sup.8, or --(CH.sub.2).sub.n --C(.dbd.O)--O--R.sup.8R.sup.5 is carboxyalkyl (C.sub.1 -C.sub.2);R.sup.6 and R.sup.7 are independently hydrogen, benzyl, or benzyloxy, said benzyl or benzyloxy optionally substituted with one, two or three substituents selected from the group consisting of amino, isocyanato (--N.dbd.C.dbd.O), isothiocyanato (--N.dbd.C.dbd.S), --NH--C(.dbd.O)--X or --NH--C(.dbd.S)--X;R.sup.8 is alkyl (C.sub.1 -C.sub.20), --(CH.sub.2).sub.m --Ar, or polyhydroxyalkyl (C.sub.1 -C.sub.Type: GrantFiled: April 13, 1994Date of Patent: December 19, 1995Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Thomas J. Caulfield, John L. Toner, Peng Guo, David L. Ladd
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Patent number: 5466435Abstract: Disclosed are contrast agents of the formula ##STR1## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;(CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in an aqueous, pharmaceutically acceptable carrier comprising a cellulose derivative.Type: GrantFiled: April 4, 1994Date of Patent: November 14, 1995Assignee: Sterling Winthrop Inc.Inventors: Edward J. Baker, Edward R Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef, John L. Toner, Robert W. Lee
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Patent number: 5422114Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising an x-ray producing agent of the formula or a pharmaceutically acceptable salt thereof ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract, whereinZ is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.Type: GrantFiled: February 25, 1994Date of Patent: June 6, 1995Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Thomas J. Caulfield, Robert W. Lee, Edward J. Baker
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Patent number: 5348727Abstract: A compound of the formula: ##STR1## wherein Z.dbd.H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, wherein thealkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.dbd.C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p -(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C-Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is [1-5]1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, these compounds are useful as X-ray contrast agents or aryl-lower alkyl.Type: GrantFiled: March 11, 1993Date of Patent: September 20, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef
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Patent number: 5330740Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl acetyl, or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl and halo-lower-alkyl are optionally substituted with, fiuoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;n is 1-5;y is 1-4; andx is 1 or 2in a pharmaceutically acceptable carrier.Type: GrantFiled: March 1, 1993Date of Patent: July 19, 1994Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Thomas J. Caulfield
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Patent number: 5326553Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxycarbonyloxy, (CR.sub.1 R.sub.2).sub.p-- (CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.Type: GrantFiled: February 2, 1993Date of Patent: July 5, 1994Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Eugene R. Cooper, John L. Toner, Donald A. Upson, Brent D. Douty, Thomas J. Caulfield, Bacon, Edward R., Kimberly G. Estep, Kurt A. Josef, Shaughnessy Robinson, Paul P. Spara
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Patent number: 5316755Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy,(CR.sub.1 R.sub.2).sub.p -(CR.sub.3 =CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p -C.ident.C-Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-5;m is 1-15;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.Type: GrantFiled: February 2, 1993Date of Patent: May 31, 1994Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Eugene R. Cooper, John L. Toner, Donald A. Upson, Brent D. Douty, Thomas J. Caulfield, Edward R. Bacon, Kimberly G. Estep, Kurt A. Josef, Shaughnessy Robinson, Paul P. Spara
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Patent number: 5310537Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl and halo-lower-alkyl are optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy,n is 1-4;y is 1-4; andx is 1 or 2.Type: GrantFiled: March 1, 1993Date of Patent: May 10, 1994Assignee: Sterling Winthrop Inc.Inventors: Carl R. Illig, Thomas J. Caulfield
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Patent number: 5310538Abstract: R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 =CR.sub.4).sub.m Q ,or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2 and R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkylThese compounds are combined in a polymer for use as an X-ray contrast agent.Type: GrantFiled: March 11, 1993Date of Patent: May 10, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef
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Patent number: 4977286Abstract: Novel, optically active azido alcohols are synthesized from N-haloacetyl oxazolidinone and are coupled with protected, activated carbohydrate residues in stereoselective glycosidic fashion to provide glycolipids in substantially pure stereochemical form. In accordance with certain preferred embodiments, the glycosphingolipids globotriaosylceramide, lactosyl ceramide, and galactosyl ceramide are synthesized in substantially pure stereochemical form from alkenyl, C-18 azido alcohols and protected fluoroglycosides and are employed as antigens in the production of antibodies useful, for example, in the treatment of disease.Type: GrantFiled: September 9, 1988Date of Patent: December 11, 1990Assignee: Trustees of the University of PennsylvaniaInventors: Kyriacos C. Nicolaou, Thomas J. Caulfield
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Patent number: RE40558Abstract: The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.Type: GrantFiled: October 20, 2005Date of Patent: October 28, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Zaid Jayyosi, Gerard M. McGeehan, Michael F. Kelley, Richard F. Labaudiniere, Litao Zhang, Robert D. Groneberg, Daniel G. McGarry, Thomas J. Caulfield, Anne Minnich, Mark Bobko