Abstract: Nortriptyline functionalized compounds are provided for conjugation to antigenic compositions, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies, which find use in immunoassays for the determination of nortriptyline in a sample, while the enzyme conjugates find use in an enzyme assay for the determination of nortriptyline in a sample.
Abstract: The invention concerns a method of inhibiting both thromboxane synthetase and cyclic-AMP phosphodiesterase in a mammal having a disease characterized by elevated thromboxane levels or an imbalance of prostacyclin/thromboxane levels with a compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt or ester thereof, wherein:X is chosen from the group consisting of: ##STR2## and a covalent bond in which R.sup.1 is H, alkyl having 1-6 carbon atoms, optionally substituted phenyl or optionally substituted phenyl lower alkyl, when R.sup.2 is H or OH, or R.sup.1 and R.sup.2 taken together represent oxo, alkylidene having 1-6 carbon atoms or optionally substituted benzylidene;R.sup.3 is H or alkyl having 1-6 carbon atoms, R.sup.4 is H and R.sup.3 and R.sup.4 are either cis or trans to each other, or R.sup.3 and R.sup.4 taken together represent a covalent bond;n is an integer from 0-3;Het is 1-imidazolyl or 3-pyridyl; and the dotted line represents an optional covalent bond.
Type:
Grant
Filed:
May 29, 1986
Date of Patent:
December 20, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Keith A. M. Walker, John J. Bruno, Gregory R. Martinez
Abstract: Compounds useful for treating inflammation, swelling and associated pain, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: a is an integer of 0-3;b is an integer of 0-2;n is an integer of 3-12;each X and each Y are independently -halo, --R.sup.1, -alkoxy, or -phenyl; andB is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or --CH.sub.2 CH.sub.2 OH; andm is an integer of 3-8.Novel compounds are those wherein n is at least 6 if both a and b are 0.
Type:
Grant
Filed:
April 6, 1984
Date of Patent:
December 20, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, James P. Dunn, Stefan H. Unger, Thomas R. Thieme
Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.
Type:
Grant
Filed:
April 28, 1986
Date of Patent:
December 20, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
D. V. K. Murthy, Michael C. Venuti, John M. Young
Abstract: This invention covers a compound of the formula ##STR1## wherein R is hydrogen, lower alkyl or a pharmaceutically acceptable, non-toxic salt of a compound wherein R is hydrogen; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, Y is lower alkyl or ##STR2## wherein Z is hydrogen, halo, methyl, methoxy or trifluoromethyl; and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..
Type:
Grant
Filed:
February 27, 1987
Date of Patent:
December 20, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gary F. Cooper, John H. Fried, L. David Waterbury
Abstract: Compounds useful for treating inflammation, pain and swelling, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Y and Z are each independently halo, alkyl or alkoxy;l and m are each independently integers of 0-4;b is an integer of 2-12; andX is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or CH.sub.2 CH.sub.2 OH; andn is an integer of 3-7.
Type:
Grant
Filed:
July 15, 1983
Date of Patent:
December 20, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Stefan H. Unger, Thomas R. Thieme
Abstract: A device is disclosed for use in a simultaneous calibration assay method wherein a conjugate of a catalyst and a member of a specific binding pair ("mip") is employed. The present device comprises a surface to which a receptor is non-diffusively bound. The receptor is capable of specific binding to the conjugate of the catalyst and mip and is substantially incapable of binding to the catalyst or the mip apart from the conjugate. The surface may be an integral part of, or separate from, a support.
Abstract: A portable analyzer is disclosed. The analyzer comprises in combination a housing, an optical system comprising a light source, a detector, and one or more means for activating the optical system in generating a signal in response to a test element, means for manually moving the test element from a first position to a second position corresponding to a point of initiation of an operative condition of the optical system, means biasing the moving means toward said first position for controlling movement of the test element from the second position to the first position, means cooperative with said optical system, for processing the signal, and means, cooperative with the means for processing the signal, for displaying the processed signal.
Abstract: Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenendioxy or ethylene-1,2-dioxy, andR is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2 wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen, or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers, especially as antidepressants.
Abstract: A method is disclosed for determining an analyte in a sample suspected of containing the analyte. The analyte is a member of a specific binding pair (sbp) consisting of ligand and complementary receptor. The method comprises combining in an aqueous medium (1) said sample, (2) a first reagent comprising a non-dispersed surface to which is bound an sbp member that becomes bound to the surface in relation to the amount of analyte in the sample. The volume of the aqueous medium containing the above reagents is sufficiently large to allow complete immersion of the first reagent therein and determination of the analyte but not so large to result in substantial interference in the determination upon addition of a second reagent reactive with the conjugate of enzyme and sbp member and capable of generating a signal. The second reagent is present in a medium of sufficient volume to substantially increase the volume of the liquid medium and reduce interference in the determination.
Type:
Grant
Filed:
May 14, 1986
Date of Patent:
November 22, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Pyare Khanna, Dennis M. Bleile, Cynthia D. Stiso
Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,R.sup.2 is the same as R.sup.1, or R.sup.2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-alkoxy, and m is 1 or 2;X is the same and is either --C(O)OR.sup.4 or --C(O)NR.sup.5 R.sup.6,whereinR.sup.4 is alkyl, phenyl or benzyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo; andR.sup.5 and R.sup.6 are independently hydrogen, lower alkyl, cycloalkyl or phenyl optionally substituted with one or two lower alkyl groups, lower alkoxy groups or halo.
Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, Y is hydrogen or morpholinoethyl, and where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, particularly for treatment of allograft rejection, especially including cardiac allograft rejection, pancreatic allograft rejection and renal allograft rejection, and for treating autoimmune diabetes.
Type:
Grant
Filed:
January 22, 1988
Date of Patent:
November 22, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee
Abstract: New oxazole derivatives of formula 1 and their pharmacetically acceptable salts have anthelmintic activity: ##STR1## where R is H, OH, or acyloxy of 8 to 22 carbon atoms;R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each independently H or acyl of 1 to 6 carbon atoms.
Type:
Grant
Filed:
April 9, 1987
Date of Patent:
November 15, 1988
Assignees:
Syntex Corporation, The Regents of the University of California
Inventors:
Philip Crews, Thomas R. Matthews, Emilio Q. Cabana, Madeline Adamczeski
Abstract: The present invention is concerned with a method for determining the presence of a malignant condition at a locus of interest. An exfoliative cell specimen obtained from the locus is contacted with an antibody specific for an antigenic site that is usually only found in the specimen when a malignant condition is present. The contact is made under conditions for detectable binding of the antibody to such antigenic site. After contact, the presence of binding of the antibody to the antigenic site is observed. The binding of the antibody is related to the presence of a malignant condition at the locus. The invention finds utility, for example, in the detection of cervical carcinoma.
Type:
Grant
Filed:
March 30, 1984
Date of Patent:
November 1, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Anthony C. Allison, Vera Morhenn, Alain B. Schreiber
Abstract: A non-stinging aqueous anti-inflammatory steroid formulation suitable for intranasal administration comprises: an anti-inflammatory steroid in an amount between about 0.01% and about 0.05% (w/v); propylene glycol in an amount between about 2% and about 10% (w/v); PEG 400 in an amount between about 10% and about 25% (w/v); polysorbate 20 in an amount between about 1% and about 4% (w/v); an effective amount of a preservative; an effective amount of a stabilizer; an effective amount of an antioxidant; water; and pH buffering agent sufficient to adjust the pH of the resulting solution to between about 3.5 and about 7.
Type:
Grant
Filed:
May 22, 1986
Date of Patent:
November 1, 1988
Assignee:
Syntex Pharmaceuticals International Ltd.
Inventors:
Eric Benjamin, Shabbir Anik, Ya-Yun T. Lin
Abstract: Novel aroyl-substituted benzofuran and benzothiophene acetic and proprionic acids are disclosed herein. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.
Abstract: This invention relates to a process for making a compound of formula I ##STR1## in the form of a stereoisomer or mixture thereof, wherein R is hydrogen, lower alkyl; X is hydrogen, halo, trifluoromethyl, lower alkyl or lower alkoxy, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta., or a pharmaceutically acceptable, non-toxic salt of the compound wherein R is hydrogen; novel intermediates useful for preparing these compounds; processes for making the intermediates; and a stereoisomer of the compound of formula I wherein R is methyl and X is hydrogen and a process for making same.
Type:
Grant
Filed:
September 13, 1985
Date of Patent:
October 25, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gary F. Cooper, Douglas L. Wren, Albert R. Van Horn, Tsung-Tee Li, Colin C. Beard
Abstract: Compounds of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen or an ether-forming group and X is hydrogen, halo, trifluoromethyl, lower alkyl, or lower alkoxy, are useful intermediates for making PGE and PGF derivatives having an allenic function.
Abstract: A method is disclosed for reducing the oxygen content of a medium in which are present cells, usually anaerobic microorganisms, to extend the time during which the cells remain viable. The method comprises having in fluid contact with the aqueous medium an effective amount of an oxidase and substrate for the oxidase. The oxidase and substrate for the oxidase in an aqueous medium can be in fluid, e.g., air, contact with a separately contained aqueous medium in which the cells are present. Alternatively, the cells can be present in the same aqueous medium as the oxidase and substrate for the oxidase. The aqueous medium containing the oxidase and the substrate for the oxidase can further contain a hydrogen peroxide scavenger in an effective amount.
Type:
Grant
Filed:
May 23, 1986
Date of Patent:
October 4, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Richard Armenta, Ian Gibbons, Edwin F. Ullman
Abstract: Fluorescent antigen conjugates are provided comprising antigens covalently bonded to at least one 2,7-dialiphatic substituted-9-phenyl-6-hydroxy-3H-xanthen-3-one, wherein the 1- and 8-positions are unsubstituted. Also provided are novel fluorescent compounds absorbing at wavelengths in excess of 500 nm, having active functionalities for linking to the antigen. Finally, methods are provided for analyzing antigens in serum, whereby serum interference is avoided.