Abstract: 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.
Type:
Grant
Filed:
August 12, 1988
Date of Patent:
September 18, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Robin D. Clark, Jacob Berger, Klaus K. Weinhardt
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 methylenedioxy or ethylene-1,2-dioxy;W is oxygen or sulfur; andZ is --R.sup.1, --OR.sup.2 or --NR.sup.3 R.sup.4, whereinR.sup.1 is lower alkyl, lower haloalkyl, cycloalkyl, optionally substituted phenyl or phenyl lower alkyl, or heteroaryl;R.sup.2 is lower alkyl, optionally substituted phenyl or phenyl lower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, alkyl, optionally substituted phenyl or phenyl lower alkyl; orR.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached represent a heterocycle of the formula: ##STR2## wherein A is --(CH.sub.2).sub.m, --N(R.sup.5)-- or oxygen, in which m is an integer of 0-2 and R.sup.5 is hydrogen or lower alkyl;or a pharmaceutically acceptable salt thereof, are useful as .alpha..sub.2 -blockers.
Type:
Grant
Filed:
October 12, 1988
Date of Patent:
September 11, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Robin D. Clark, Andrew T. Kilpatrick, Michael Spedding
Abstract: A device for collecting biological material is disclosed. The device comprises a shaft with a loop-like collection structure at one end. The collection structure provides a non-cutting, scraping edge to allow collection of the material without cutting. In a preferred embodiment, the collection means retains the material by diverting it into the interior portion of the collection means. The biological material is released from the device by rotation of the shaft or by elution in an appropriate solvent.
Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
Type:
Grant
Filed:
November 14, 1988
Date of Patent:
August 28, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
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:
June 29, 1989
Date of Patent:
August 14, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Anthony C. Allison, Elsie M. Eugui, Peter H. Nelson, Chee-Liang L. Gu, William A. Lee
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:
November 25, 1988
Date of Patent:
August 7, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
D. V. Krishna Murthy, Michael C. Venuti, John M. Young
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:
October 27, 1989
Date of Patent:
August 7, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Deborah A. Eppstein, Philip L. Felgner, Thomas R. Gadek, Gordon H. Jones, Richard B. Roman
Abstract: A device is disclosed for use in a chromatographic system wherein a component of a mixture is partitioned between a liquid phase and an immobile phase. The device comprises at least one strip of a bibulous material. In the chromatographic system the component traverses at least a portion of the strip. The strip generally has a longitudinal edge substantially corresponding to the direction of traverse of the component. The longitudinal edge has the characteristic of substantially the same rate of traversal by the component along this edge when compared to the rate of traversal of the component along the body of the strip. The strips are prepared from a sheet of a bibulous material by non-defomative or non-compressive cutting of the sheet. The preferred cutting means is a laser beam.
Type:
Grant
Filed:
July 5, 1988
Date of Patent:
July 31, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
David Litman, Robert Zuk, Gerald Rowley
Abstract: This invention is directed to a method for treating helminthiasis which comprises administering to an animal in need thereof an anthelmintically effective amount of a compound of Formula (I): ##STR1## where R.sup.1 is hydrogen or --SR.sup.2,whereinR.sup.2 is hydrogen, --C(O)--CH.sub.3, or ##STR2## or a pharmaceutically acceptable salt thereof. This invention is also directed to a composition for treating helminthiasis in an animal which comprises a pharmaceutically acceptable excipient and an anthelmintically effective amount of a compound of Formula (I). This invention is also directed to novel compounds of Formula (I) wherein R.sup.
Type:
Grant
Filed:
October 27, 1988
Date of Patent:
July 24, 1990
Assignees:
Syntex (U.S.A.) Inc., The Regents of the Univ. of California
Inventors:
Phillip Crews, Thomas R. Matthews, Paul Horton
Abstract: A long acting sustained release pharmaceutical composition for dihydropyridine calcium channel blockers wherein the calcium channel blocker and a pH-dependent binde are intimately admixed in essentially spherically shaped non-rugose particles of up to 1.2 mm in diameter.
Type:
Grant
Filed:
July 26, 1987
Date of Patent:
July 10, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Calum B. MacFarlane, Alastair B. Selkirk, Michael J. Dey
Abstract: An apparatus for maintaining a biological sample on a support is disclosed. The apparatus comprises a hollow chamber with internal and external surfaces and a first and second end. The first end is open and is adapted for attachment to the first closure means. The second end is either closed or open. If open, the second end is adapted for attachment to a second closure means. The apparatus provides means for maintaining the support in contact with a liquid medium at all times regardless of the orientation of the apparatus. In a preferred embodiment, the apparatus provides means for maintaining the original orientation of a non-integral support regardless of the orientation of the apparatus. The apparatus is useful for isolating and culturing microorganisms.
Abstract: 2,3-Dihydro-1H-pyrrolo[1,2-a]pyrrole-1,7-dicarboxylates of the formula, ##STR1## in which each R is independently H or lower alkyl, are prepared from from di(lower alkyl) 1,3-acetone-dicarboxylates.
Type:
Grant
Filed:
January 23, 1989
Date of Patent:
June 26, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Hiralal N. Khatri, Michael P. Fleming, George C. Schloemer
Abstract: 3-[.omega.-(3,5-Di-t-butyl-4-hydroxyphenyl)alkanoyl]-pyrroles and their de-oxy analogs, for example, 3-(3,5-di-t-butyl-4-hydroxybenzyl)pyrrole, 2-chloro-4-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole, 3-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole and 3-[2-(3,5-di-t-butyl-4-hydroxyphenyl)-1-oxoethyl]pyrrole, have high pharmacological potency as anti-inflammatory, analgesic and antipyretic agents.
Type:
Grant
Filed:
February 21, 1989
Date of Patent:
June 19, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Joseph M. Muchowski, Robert Greenhouse, John Young, D. V. Krishna Murthy
Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R.sup.1 is aryl, lower alkyl, cycloalkyl or hydrogen;R.sup.2 is aryl, lower alkyl or hydrogen;R.sup.3 lower alkyl, hydroxy, or hydrogen;R.sup.4 aryl or hydrogen;R.sup.5 aryl or hydrogen;m is two or three;n is zero, one or two,provided that when R.sup.3 hydroxy, n is one or two; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilipsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.
Type:
Grant
Filed:
February 21, 1989
Date of Patent:
June 19, 1990
Assignee:
Syntex Pharmaceuticals Ltd.
Inventors:
Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
Abstract: An apparatus and method are described for defining a small interrogation volume in a liquid sample suspected of containing an analyte. The apparatus and method utilize a dual optical fiber probe constructed with the ends of the optical fibers at the liquid/fiber interface spatially oriented such that the intersection of their longitudinal axes forms an included angle ranging from about 40.degree. to 140.degree.. By appropriate choice of the numerical aperture and core diameter of the optical fibers and the separation distance between the longitudinal axes of the optical fibers at the liquid/fiber interface, a finite interrogation volume of predetermined size and independent of the total liquid sample volume can be defined. The apparatus and method substantially reduce background interference with corresponding increase in assay sensitivity.
Type:
Grant
Filed:
April 1, 1988
Date of Patent:
June 19, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Richard P. Watts, Wylie I. Lee, John W. Vorpahl
Abstract: The present invention is concerned with novel monoclonal antibodies which bind to Interleukin-1.beta. and do not bind to Interleukin-1.beta.. The antibodies bind to Interleukin-1.beta. and block receptor binding and biological activity. The antibodies find use in, for example, diagnostic methods such as an assay for the detection of Interleukin-1.beta..
Type:
Grant
Filed:
August 8, 1986
Date of Patent:
June 19, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Anthony C. Allison, Elsie M. Eugui, John S. Kenney, Marvin P. Masada
Abstract: A method is disclosed for separating a substance from a liquid medium. The method comprises combining the liquid medium containing the substance with magnetic particles under conditions for non-specific chemical binding of the magnetic particles. Thereafter, the medium is subjected to a magnetic field gradient to separate the particles from the medium. The preferred non-specific binding is achieved as the result of charge interactions between the particles usually by means of a polyionic reagent. The method of the invention has particular application to the separation of cells and microorganisms from aqueous suspensions and also to the determination of an analyte in a sample suspected of containing the analyte. The analyte is a member of a specific binding pair (sbp). The sample is combined in an assay medium with magnetic particles and a sbp member complementary to the analyte.
Type:
Grant
Filed:
October 26, 1988
Date of Patent:
June 19, 1990
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Edwin F. Ullman, Vartan E. Ghazarossian, Nurith Kurn, Litai Weng
Abstract: A vaccine for immunizing animals against Feline Leukemia Virus (FeLV) infections contains an FeLV antigen emulsified with a polyoxypropylene-polyoxyethylene block polymer, a glycol ether-based surfactant, an immunopotentiating amount of an immunostimulating glycopeptide, and, optionally, a metabolizable non-toxic oil.
Abstract: A unique crystalline polymorphic form of flunisolide is disclosed which is stable in aerosols such as Freon.RTM. mixtures and is valuable in the treatment of respiratory diseases, particularly bronchial asthma and allergic rhinitis.
Type:
Grant
Filed:
September 14, 1981
Date of Patent:
June 12, 1990
Assignee:
Syntex Pharmaceuticals International Limited
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 akoxy, are useful intermediates for making PGE and PGF derivatives having an allenic function.