Patents Assigned to Syntex (U.S.A.) Inc.
  • Analogs of parathyroid hormone and parathyroid hormone related peptide: synthesis and use for the treatment of osteoporosis
    Patent number: 5589452
    Abstract: Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, said residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence:Haa(Laa Laa Haa Haa).sub.2 Laaand their pharmaceutically acceptable salts are useful for the prophylaxis and treatment of ostoporosis in mammals. Processes for the production of the polypeptides via solid phase and recombinant methods are provided.
    Type: Grant
    Filed: July 14, 1992
    Date of Patent: December 31, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: John L. Krstenansky, John J. Nestor, Jr., Teresa H. Ho, Brian H. Vickery, Chinh T. Bach
  • Processes for preparing 2-(1-azabicyclo[2.2.2]oct-3-yl)-1H-benz[de] isoquinolin-1-one derivatives and intermediates useful therein
    Patent number: 5567818
    Abstract: This invention relates to processes 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]isoquinolin-1-one, and to intermediates useful in such processes.
    Type: Grant
    Filed: July 8, 1994
    Date of Patent: October 22, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Bruce A. Kowalczyk, Charles A. Dvorak
  • Preparation of acyclovir using 1,3 dioxolane
    Patent number: 5567816
    Abstract: A process for the preparation of acyclovir includes contacting an at least partially silylated guanine or mixture of at least partially silylated guanines with 1,3-dioxolane in the presence of a selective alkylation catalyst selected from the group consisting of trifluoromethanesulfonic acid, trimethylsilyl trifluoromethanesulfonate, and bistrimethylsilyl sulfonate, and hydrolyzing the product thus formed.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: October 22, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: George C. Schloemer, Yeun-Kwei Han, Peter J. Harrington
  • Preparation of N-9 substituted guanine compounds
    Patent number: 5565565
    Abstract: The invention relates to efficient and selective processes for the synthesis of the antiviral N-9 substituted guanine compounds acyclovir and ganciclovir.
    Type: Grant
    Filed: August 4, 1994
    Date of Patent: October 15, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Eric Lodewijk, Yeun-Kwei Han, George C. Schloemer, Sam L. Nguyen
  • High dose formulations of mycophenolate mofetil and mycophenolic acid
    Patent number: 5554384
    Abstract: Mycophenolate mofetil and mycophenolic acid can be conveniently manufactured into high dose oral formulations by the hot melt filling of a supercooled mycophenolate mofetil or mycophenolic acid liquid into a pharmaceutical dosage form. High dose oral pharmaceutical formulations and manufacturing methods therefor are disclosed.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: September 10, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Glenn J. Samuels, Jung-Chung Lee, Charles Lee, Stephen Berry, Paul J. Jarosz
  • 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: 5550289
    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 27, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Deborah A. Eppstein, Philip L. Felgner, Thomas R. Gadek, Gordon H. Jones, Richard B. Roman
  • 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
  • Process for preparing pharmaceutical compositions containing crystalline anhydrous mycophenolate mofetil salts
    Patent number: 5545637
    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: June 2, 1995
    Date of Patent: August 13, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Roger C. Fu, De-Mei Leung, Jeffrey S. Fleitman, Michele C. Rizzolio, Andrew R. Miksztal
  • 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
  • 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
  • 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
  • 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
  • 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