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 is lower alkyl, hydroxy, or hydrogen;R.sup.4 is aryl or hydrogen;R.sup.5 is aryl or hydrogen;m is two or three;n is zero, one or two,provided that when R.sup.3 is 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, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.
Type:
Grant
Filed:
April 24, 1987
Date of Patent:
May 9, 1989
Assignee:
Syntex Pharmaceuticals, Ltd.
Inventors:
Jean C. Pascal, Chi-Ho Lee, Brian J. Alps, Henri Pinhas, Roger L. Whiting
Abstract: N-(lower alkyl)-2-(3'-ureidobenzyl)pyrrolidines and N-(lower alkyl)-2-(3'-ureidobenzyl)-5-(lower alkyl)pyrrolidines are useful for lowering intraocular pressure in mammals, for example, in the treatment of glaucoma.
Type:
Grant
Filed:
February 19, 1988
Date of Patent:
May 2, 1989
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Joseph M. Muchowski, Robin D. Clark, L. David Waterbury
Abstract: Novel aroyl-substituted benzofuran and benzothiophene acetic and propionic acids are disclosed herein. These compounds are useful as analgesic, anti-inflammatory, and antipyretic agents.
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:
September 4, 1987
Date of Patent:
February 28, 1989
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
Abstract: 4-Monosubstituted and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.
Type:
Grant
Filed:
August 14, 1987
Date of Patent:
February 7, 1989
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof whereinR.sup.1 is hydrogen or --C(O)R.sup.7 wherein R.sup.7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof;R.sup.2 is --C(O)R.sup.7 is as defined above;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 and R.sup.9 and R.sup.
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: 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: 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: 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:
January 30, 1987
Date of Patent:
June 28, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
Abstract: Intraocular hypertensive diseases such as glaucoma are treated with compounds represented by formula I ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is alkyl of two to four carbon atoms;R.sub.2 is --(CH.sub.2).sub.n --C.sub.6 H.sub.4 --R.sub.5 ; wheren is an integer from 1 to 4; andR.sub.5 is --H, --OH, halo, lower alkyl, lower alkoxy, ureido, lower alkyl-ureido, lower alkyl-amido, or formamido;R.sub.3 is hydro or hydroxy; andR.sub.4 is hydro, lower alkyl, amino, or lower alkylamino.
Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and 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:
September 23, 1987
Date of Patent:
May 31, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and 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:
January 30, 1987
Date of Patent:
February 23, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
Abstract: A monomer for making a contact lens with improved oxygen permeability and stability is disclosed as having a first portion for increasing wettability and a second portion for increasing oxygen permeability. The first portion includes a side-chain functionality of the structural formula: ##STR1## and is hydrophilic. The second portion includes a siloxane moiety, and is usually hydrophobic.Also disclosed is a cross-linking agent, a polymeric material for making contact lenses, a method for making the polymeric material, and a method for making contact lenses from the material.
Abstract: A carrier is disclosed for supporting an optical blank in the chuck of a lathe, for machining the optical blank into a lens. The carrier has a substantially cylindrical body formed of a machinable material. The cylindrical body has an opening at a first end thereof through which an optical blank can be inserted, and a retaining portion for securing such optical blank in place. In a preferred embodiment, the retaining portion is an annular shoulder extending inwardly at a second end of the cylindrical body.
Abstract: A process for the treatment of a soft contact lens, to increase its resistance to the deposition thereon and diffusion and accumulation therein of substances which will promote its clouding and discoloration in use, and to improve its mechanical strength, includes treating a hydroxyl group-containing acrylic ester soft contact lens or replica with an organic acid anhydride for a sufficient period of time to treat at least a portion of polymer molecules on the outer surfaces, e.g. by esterifying hydroxyl groups on the molecules and facilitating extraction of organic-type impurities. The process is optionally performed in the presence of a medium which partially swells the surface regions of the lens or replica prior to or during the process.
Type:
Grant
Filed:
August 14, 1985
Date of Patent:
August 18, 1987
Assignee:
Sola U.S.A. Inc.
Inventors:
Shaow B. Lin, Lyle M. Bowman, S. Kumar Chandrasekaran, Thomas B. Harvey, III
Abstract: A compound having the formula ##STR1## where Ar=naphthyl, biphenyl, or quinolinyl;X=oxygen or NH;Y=2 to 8;R.sub.1 =phenyl, substituted phenyl, hydrogen, lower alkyl; andR.sub.2 is the same or different from R.sub.3 and is alkyl, cycloalkyl, phenyl, substituted phenyl, thiazolyl; andthe pharmaceutically acceptable salts thereof.Compounds of this general formula are useful as anti-inflammatories, and as anti-psoriatic agents.
Abstract: A contact lens for correction of astigmatism is formed from a single polymeric or copolymeric material. The lens has a central optical zone of greater rigidity than a surrounding non-optical zone. The rigidity of the central optical zone is sufficient for it to retain an astigmatism-correcting shape when worn on an eye, while the surrounding non-optical zone conforms to the shape of the eye.
Type:
Grant
Filed:
August 14, 1985
Date of Patent:
May 19, 1987
Assignee:
Sola U.S.A. Inc.
Inventors:
Robert E. Bauman, S. Kumar Chandrasekaran, Shaow B. Lin, Lyle M. Bowman, Thomas B. Harvey, III
Abstract: A compact, prefilled, ready-to-use, applicator for dispensing a medicament within a body cavity has a reservoir, an automatically-opening closure member and a telescoping plunger assembly. A closure member is disclosed, adapted to open responsive to the pressure of a medicament being dispensed, without disengaging from the reservoir in which the medicament is contained. A telescoping plunger assembly is disclosed, having impeller means disposed within the reservoir opposite the cap member and engaging means to lock the assembly in an extended position for urging the impeller means through the reservoir.
Type:
Grant
Filed:
July 27, 1984
Date of Patent:
January 13, 1987
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
David A. Lowin, Richard A. Fayram, Andrew J. Bivetto