Patents Assigned to Syntex (U.S.A.)
  • N-[1, (1-1)-dialkyloxy]-and N-[1, (1-1)-dialkenyloxy]-alk-1-yl-n,n,n-tetrasubstituted ammonium lipids and uses therefor
    Patent number: 5545412
    Abstract: This invention relates to compounds of the formula ##STR1## or an optical isomer thereof wherein R.sup.1 and R.sup.2 are the same or different and are an alkyl or alkenyl group of 6 to 24 carbon atoms; R.sup.3, R.sup.4 and R.sup.5 are the same or different and are alkyl of 1 to 8 carbon atoms, aryl, aralkyl of 7 to 11 carbon atoms, or when two or three of R.sup.3, R.sup.4, and R.sup.5 are taken together to form quinuclidino, piperidino, pyrrolidino, or morpholino, n is 1 to 8; and X is a pharmaceutically acceptable anion.
    Type: Grant
    Filed: April 3, 1995
    Date of Patent: August 13, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Deborah A. Eppstein, Philip L. Felgner, Thomas R. Gadek, Gordon H. Jones, Richard B. Roman
  • Crystalline anhydrous mycophenolate mofetil and intravenous formulation thereof
    Patent number: 5543408
    Abstract: The crystalline anhydrous salt formed by complexing mycophenolate mofetil with an anion selected from the group chloride, sulfate, phosphate and acetate (in particular the hydrochloride salt), and pharmaceutical compositions, intravenous formulations and a kit thereof, and associated methods of treatment.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: August 6, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Roger C. Fu, De-Mei Leung, Jeffrey S. Fleitman, Michele C. Rizzolio, Andrew R. Miksztal
  • 4-amino derivatives of 5-substituted mycophenolic acid
    Patent number: 5538969
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: July 23, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • 6-substituted mycophenolic acid and derivatives
    Patent number: 5536747
    Abstract: The disclosed 6-substituted derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: July 16, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John W. Patterson, David Morgans, Jr., David B. Smith, Fancisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Eric B. Sjogren, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • Method of use of 8-phenylcyclopentenoquinoline and 8-phenylcyclohexenoquinoline derivatives
    Patent number: 5530005
    Abstract: The use of 8-phenylcyclopentenoquinolines and 8-phenylcyclohexenoquinolines for treating atopic dermatitis, allograft rejection, graft-vs-host disease, and anti-autoimmune disease, and inducing immunosuppression, is disclosed.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: June 25, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Sabine Axt
  • Processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl) biphenyl-4-ylmethyl]-1H-indole-3-carboxylic acid
    Patent number: 5527918
    Abstract: The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrasol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrasolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: June 18, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin, Stephen R. Stabler
  • Method of using 4-amino 6-substituted mycophenolic acid and derivatives
    Patent number: 5525602
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: June 11, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John W. Patterson, David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • N--2--chlorobenzyl--2--oxo and n--2--chlorobenzyl--2,2--dioxo--1,2,3--oxathiazolidine derivatives, their preparation and synthesis of thieno[3,2--c]pyridine derivatives therefrom
    Patent number: 5516910
    Abstract: Compounds of the formula: ##STR1## wherein: A is oxo or dioxo;R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen or lower alkyl of one to six carbon atoms;R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently hydrogen, lower alkyl of one to six carbon atoms, alkoxy, acyl or halo;are advantageously converted to thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: May 14, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gary F. Cooper, Keith E. McCarthy
  • Method for detection of specific nucleic acid sequences
    Patent number: 5516641
    Abstract: A kit is disclosed for a method for detecting the presence of a target polynucleotide sequence. The kit comprises a first polynucleotide sequence and a second polynucleotide sequence complementary to non-contiguous portions of a target polynucleotide sequence, which first and second sequences are covalently attached when they are hybridized to the target sequence. The presence of the covalently attached first and second sequences is related to the presence of the target polynucleotide sequence. The invention may be applied to target polynucleotide sequences in DNA or RNA. Specific target polynucleotide sequences of interest will frequently be characteristic of particular microorganisms, viruses, viroids, or genetic characteristics, including genetic abnormalities.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: May 14, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Edwin F. Ullman, Thomas C. Goodman, Paul D. Stull
  • Method of using 4-amino derivatives of 5-substituted mycophenolic acid
    Patent number: 5512568
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: April 30, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • Compositions useful in heterogeneous immunoassays
    Patent number: 5512659
    Abstract: A method for carrying out an immunoassay for an analyte in which a sample suspected of containing an analyte and reagents useful for detecting the analyte of interest are combined in an aqueous medium, wherein one of the reagents includes a support and one includes a label, the improvement comprising employing as the reagents a first and second conjugate, each comprised of a specific binding pair (sbp) member bound to a small molecule wherein the small molecules of each conjugate are different.
    Type: Grant
    Filed: August 4, 1989
    Date of Patent: April 30, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Edwin F. Ullman, Hriar Kirakossian, Mary C. Ericson, Richard P. Watts
  • Process for preparing 2-(1-azabicyclo 2.2.2!oct-3-yl)-2,3,3A,4,5,6-hexahydro-1H-benz de!isoqui nolin-1-one
    Patent number: 5510486
    Abstract: This invention relates to a process for preparing 2-(1-azabicyclo 2.2.2!oct-3-yl)-2,3,3a,4,5,6-tetrahydro-1H-benz de!isoquin olin-1-one, particularly 2-(1-azabicyclo 2.2.2!oct-3S-yl)-2,3,3aS,4,5,6-tetrahydro-1H-benz de!isoqu inolin-1-one, and to intermediates useful in such process.
    Type: Grant
    Filed: July 26, 1994
    Date of Patent: April 23, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: James Robinson, III, John C. Rohloff, Bruce A. Kowalczyk
  • 5-substituted derivatives of mycophenolic acid
    Patent number: 5493030
    Abstract: The disclosed hexenoic acid side-chain derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil, including immune, inflammatory, tumor, proliferative, viral or psoriatic disorders.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: February 20, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Morgans, Jr., David B. Smith, Francisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, John C. Rohloff, Eric B. Sjogren, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • 2-(1-azabicyclo[2.2.2]oct-3 s-yl)-6-hydroxy-2,4,5,6-tetrahydro-1H-benz[DE]i s [2.2.2]oct-3's-yl)-6-hydroxy-2,3,3a,4,5,6-hexahydro-1h-benz [DE]isoquinolin-1-one and individual stereoisomers thereof
    Patent number: 5492914
    Abstract: This invention relates to 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,4,5,6-tetrahydro-1H-benz[de ]isoquinolin-1-one and 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,3,3a,4,5,6-hexahydro-1H-ben z[de]isoquinolin-1-one and their individual stereoisomers and uses and the processes for their making.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: February 20, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark, Paul E. Weller, Douglas L. Wren
  • Isoquinolinone and dihydroisoquinolinone 5-HT.sub.3 receptor antagonists
    Patent number: 5491148
    Abstract: 5-HT.sub.3 receptor antagonist compounds of Formula I: ##STR1## in which X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino;R.sup.1 is hydrogen, lower alkyl, phenyl or halogen;R.sup.
    Type: Grant
    Filed: April 26, 1991
    Date of Patent: February 13, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Robin D. Clark
  • Immunoassay for homocysteine
    Patent number: 5478729
    Abstract: This invention pertains to methods to detect a compound in the presence of a homolog that is immunologically related to the analyte. The invention is particularly suited for the detection of homocysteine in the presence of cysteine. The methods of this invention involve chemically modifying both the analyte and the homolog to increase their immunogenicity and facilitate antibody recognition. More importantly, this modification is done to make these compounds immunologically distinct. Antibodies to the immunologically distinct compounds are then prepared. An assay protocol comprises chemically modifying the analyte and homolog and then immunochemically detecting the modified analyte by means of the aforementioned antibodies.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: December 26, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Reuel B. Van Atta, Thomas C. Goodman, Edwin F. Ullman
  • 8-phenylcyclopentenoquinoline and 8-phenylcyclohexenoquinoline derivatives
    Patent number: 5475003
    Abstract: The disclosed derivatives of 8-phenylcyclopentenoquinolines and 8-phenylcyclohexenoquinolines are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft, rejection agents, anti-graft-vs-host disease agents, anti-allergic agents, bronchodilation agents, anti-autoimmune agents, and analgetic agents.
    Type: Grant
    Filed: March 3, 1994
    Date of Patent: December 12, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robert S. Wilhelm, Sabine Axt
  • High dose ranolazine formulations
    Patent number: 5472707
    Abstract: Mycophenolate mofetil, mycophenolic acid, and ranolazine can be conveniently manufactured into high dose oral formulations by the hot melt filling of a supercooled mycophenolate mofetil, mycophenolic acid, or ranolazine liquid into a pharmaceutical dosage form. High dose oral pharmaceutical formulations and manufacturing methods therefor are disclosed.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: December 5, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Glenn J. Samuels, Jung-Chung Lee, Charles Lee, Stephen Berry, Paul J. Jarosz
  • Controlled delivery of pharmaceuticals from preformed porous polymeric microparticles
    Patent number: 5470582
    Abstract: A controlled release pharmaceutical composition comprising a physiologically active agent dispersed in preformed porous polymeric microparticles is provided. The active agent concentration may be up to about 10% by weight to achieve controlled release. Each of the porous microparticles has a plurality of preformed pores into which active agent is loaded and from which the active agent is subsequently released to the environment of use. The compositions are capable of delivering physiologically effective amounts of active agent for at least about thirty days, which delivery may be reversibly controlled by exposure to ultrasound.
    Type: Grant
    Filed: February 5, 1993
    Date of Patent: November 28, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Andreas Supersaxo, Jim H. Kou
  • Process for preparing1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl1-1H-indole- 3-carboxylic acid
    Patent number: 5468867
    Abstract: The present invention relates to a process for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such process.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: November 21, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Lawrence E. Fisher, Lee A. Flippin, Michael G. Martin