Abstract: Certain 3,4-disubstituted anilines and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --NH.sub.2 or --NHCH.sub.3 ;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.
Type:
Grant
Filed:
July 9, 1993
Date of Patent:
May 10, 1994
Assignee:
Sterling Winthrop Inc.
Inventors:
William N. Washburn, Lee H. Latimer, Barbara B. Lussier, Carl R. Illig, Alexander L. Weis
Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinZ=H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl or halo-lower-alkyl, wherein said C.sub.1 -C.sub.25 alkyl, cycloalkyl, acetyl and halo-lower-alkyl are optionally substituted with fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy,n is 1-4;y is 1-4; andx is 1 or 2.
Abstract: R=C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl, each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 =CR.sub.4).sub.m Q ,or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2 and R.sub.3 and R.sub.4 are independently H, or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkylThese compounds are combined in a polymer for use as an X-ray contrast agent.
Type:
Grant
Filed:
March 11, 1993
Date of Patent:
May 10, 1994
Assignee:
Sterling Winthrop Inc.
Inventors:
Edward R. Bacon, Carl R. Illig, Thomas J. Caulfield, Brent D. Douty, Kurt A. Josef
Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinR=C.sub.1 -C.sub.25 alkyl, cycloalkyl, unsaturated allyl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy, (CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H, lower-alkyl, optionally substituted with halo;n is 1-5;m is 1-5;p is 1-10; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl.
Type:
Grant
Filed:
February 4, 1993
Date of Patent:
May 3, 1994
Assignee:
Sterling Winthrop Inc.
Inventors:
Kurt A. Josef, Edward R. Bacon, Kimberly G. Estep, Carl R. Illig, Brent D. Douty
Abstract: There is provided a device for placing a capsule into a container, slitting the capsule to release its content, washing the capsule and that part of the device which is in direct contact with the capsule and its content for quantitatively transferring the total content into said container for subsequent analysis.
Abstract: Disclosed are lyophilized biologically active proteinaceous compositions containing low diol polyalkylene oxide, such as polyethylene glycol, covalently attached to a biologically active proteinaceous substance and combined with the cryoprotectant cyclodextrin.
Type:
Grant
Filed:
February 25, 1993
Date of Patent:
March 29, 1994
Assignee:
Sterling Winthrop Inc.
Inventors:
Christopher P. Phillips, Robert A. Snow
Abstract: A hand-held power injection device is provided for injecting liquid, such as contrast media, into the vascular system of a mammal. The device comprises a pistol-shaped housing which encloses a battery-powdered D. C. motor for constant-rate delivery of liquid from a syringe.
Abstract: Disclosed are aqueous compositions containing a contrast agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract, wherein R is a substituted or unsubstituted alkyl group containing from 2 to 8 carbon atoms, wherein said substituents are selected from the group consisting of C.sub.1 -C.sub.6 alkyl, hydroxy and alkoxy; and n is 1 to 5.
Abstract: Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --OH;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety.
Type:
Grant
Filed:
December 31, 1991
Date of Patent:
November 2, 1993
Assignee:
Sterling Winthrop Inc.
Inventors:
William N. Washburn, Barbara B. Lussier, Carl B. Illig, Lee H. Latimer
Abstract: Disclosed is a pre-filled plastic syringe containing a liquid product for terminal sterilization comprising: a syringe barrel equipped with a one-way valve and a slidable plunger to equalize pressure differentials; a filter engaging the one way valve to prevent backward migration of viruses and bacteria; an end cap covering the open end of the barrel to maintain sterility; and an end cap restraining device to prevent plunger blow-out.
Type:
Grant
Filed:
January 31, 1992
Date of Patent:
October 26, 1993
Assignee:
Sterling Winthrop, Inc.
Inventors:
Richard T. Liebert, Neil H. Brown, Randy E. Armbruster, Thomas M. Pack
Abstract: In accordance with the present invention, certain multiply substituted anilines, phenols and pyridines and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression.
Type:
Grant
Filed:
December 31, 1991
Date of Patent:
October 19, 1993
Assignee:
Sterling Drug Inc.
Inventors:
Barbara B. Lussier, Lee H. Latimer, Carl R. Illig, William N. Washburn
Abstract: An elastomeric stopper for a fluid-containing bottle to hermetically seal the content therein and to provide access thereto by the insertion of an infusion device through the stopper, the stopper comprising an annular protuberance which forms a second seal with the shaft of the infusion device to prevent leakage, blow-out and introduction of particulate matter into the bottle.
Abstract: Disclosed is a stopper for a medical vial suitable for piercings by a spike without producing unacceptable amounts of particulate matter, comprising: a stopper body of an elastomeric material; and an abrasion resistant coating covering the top, central, piercable surface of the stopper.
Abstract: Disclosed is a method for terminal steam sterilization of a pre-filled plastic syringe or a pre-filled plastic cartridge, said method comprising the steps of: maintaining a head space in the syringe or cartridge of less than about 10%--of the fill--volume; providing at least a 10% leeway for the plunger therein to slide in response to pressure differential; and sterilizing the syringe or cartridge at an autoclave pressure that is less than the internal pressure of the syringe or cartridge.
Type:
Grant
Filed:
January 29, 1992
Date of Patent:
May 4, 1993
Assignee:
Sterling Winthrop Inc.
Inventors:
Richard T. Liebert, Neil H. Brown, John R. Pistolese