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
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
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
Abstract: Compounds of the formula: ##STR1## wherein: m is 0 or 1;R.sup.1 is hydrogen, hydroxy, or lower alkyl;R.sup.2 is hydrogen, or lower alkyl;R.sup.3 is ##STR2## or R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached represent a group of the formula: ##STR3## wherein: n is 0 or 1;p is 0, 1, 2 or 3;q is 0 or 1;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, or optionally substituted phenyl;R.sup.5 is optionally substituted phenyl;X is (CH.sub.2).sub.p, or 4-piperidin-1-yl;Y is CH, CH--O--, CH--S--, or nitrogen;Z is CH.sub.2, NH, sulfur, or oxygen; andA is a substituted furanyl group.
Type:
Grant
Filed:
March 9, 1995
Date of Patent:
August 13, 1996
Assignee:
Syntex Pharmaceuticals, Limited
Inventors:
Jean-Claude Pascal, Gary McCort, Dominique Blondet, Fran.cedilla.oise Gellibert
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
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
Abstract: Compounds of the Formula I ##STR1## wherein X is hydrogen, chloro, amino or hydroxy; R.sup.1 is an achiral amino acid acyl residue with a tertiary .alpha.-carbon atom. Preferred achiral amino acid acyl residues have the formula ##STR2## wherein each R.sup.2 is alkyl with 1 to 6 carbon atoms, cycloalkyl with 3 to 5 carbon atoms, or benzyl; or the two R.sup.2 groups link together to form a polymethylene group with 3 to 9 carbon atoms, and pharmaceutically acceptable salts thereof are antiviral agents with improved absorption. Intermediates for the preparation of the compounds of Formula I are also described.
Type:
Grant
Filed:
July 28, 1994
Date of Patent:
August 6, 1996
Assignee:
Syntex (USA) Inc.
Inventors:
John J. Nestor, Scott W. Womble, Hans Maag
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
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
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.
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
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
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.
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
Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, m, n and q are defined as in the specification, and the pharmaceutically acceptable salts thereof. The compounds have calcium entry blocking activity with selectivity for cerebral blood vessels, and have protective activity against some of the deleterious effects resultant upon cerebral ischemia.
Type:
Grant
Filed:
September 20, 1993
Date of Patent:
May 7, 1996
Assignee:
Syntex Pharmaceuticals, Ltd.
Inventors:
Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting, Calum B. MacFarlane, Serge Beranger
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
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
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
Abstract: Piperazine derivatives, particularly ranolazine, are useful for treatment of tissues experiencing a physical or chemical insult, and specifically for treating cardioplegia, hypoxic and/or reperfusion injury to cardiac or skeletal muscle or brain tissue, and for use in transplants.
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