Patents Represented by Attorney, Agent or Law Firm Richard A. Hake
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Patent number: 5464848Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 is alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, or cyanomethyl;Y is alkylene of 3 to 9 carbon atoms,R.sub.2 and R.sub.3 independently are hydrogen, alkyl, alkoxy, halo, cyano, trifluoromethyl and nitro;R.sub.4 is alkoxy, hydroxy, halomethyl, dihalomethyl, trihalomethyl, dihaloethyl, cycloalkyl, heterocyclyl, alkoxycarbonyl, hydroxyalkyl, alkoxyalkyl, alkanecarbonyloxyalkyl, cyano, halo, thioalkyl, alkylthioalkyl, alkylthio, thio, 2,2,2-trifluoro-ethyl, (4-methylphenyl)sulfonyloxymethyl, N.dbd.Q or CON.dbd.Q, where N.dbd.Q is amino, alkylamino or dialkylamino;R.sub.5 is hydrogen or halo or alkyl.Type: GrantFiled: October 1, 1993Date of Patent: November 7, 1995Assignee: Sterling Winthrop Inc.Inventors: Guy D. Diana, Theodore J. Nitz
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Patent number: 5456904Abstract: The subject invention relates to methods and compositions comprising: a) from about 0.1% to about 5% of a compound having the structure selected from the group consisting of: ##STR1## wherein each R is independently selected from the group consisting of hydrogen, alkyl, and aryl; each R' is independently selected from the group consisting of hydrogen, alkoxy, and alkyl; Z and Z' are independently selected from the group consisting of NH, O, and CH.sub.2 such that when Z or Z' is NH, the other is not O; or a pharmaceutically acceptable salt of any of the aforementioned compounds; and b) a pharmaceutically-acceptable topical carrier.Type: GrantFiled: June 28, 1993Date of Patent: October 10, 1995Assignee: The Procter & Gamble CompanyInventor: Rodney D. Bush
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Patent number: 5364867Abstract: 4-Phenylpiperidines of the formula ##STR1## wherein R.sub.1 is hydrogen, hydroxy or lower-alkoxy;R.sub.2 is hydrogen, hydroxy, lower-alkanoyl, aroyl, lower-alkoxycarbonyl, lower-alkanoyloxy, lower-alkoxycarbonyl, or CONR.sub.3 R.sub.4 ; R.sub.3 and R.sub.4 are the same or different lower-alkyl or R.sub.3 and R.sub.4 together represent a lower-alkylene chain;X is methylene or carbonyl;Y is methylene, C.dbd.NOH, hydroxymethylene or carbonyl;or pharmaceutically acceptable acid addition salts thereof, are useful in the treatment of psychoses and other ailments of the central nervous system.Type: GrantFiled: November 30, 1992Date of Patent: November 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne
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Patent number: 5364865Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## Y is a bond or lower alkylene; R.sub.2 and R.sub.3 are independently hydrogen, lower-alkyl or halogen;R.sub.4 is ##STR3## R.sub.5 is hydrogen, lower-alkyl or halogen; R.sub.6 is hydrogen, lower-alkyl or halogen;R.sub.7 is hydrogen or lower-alkyl;R.sub.8 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.9 is lower-alkyl;R.sub.10 is lower-alkyl, trifluoromethyl or difluoromethyl;or pharmaceutically acceptable acid addition salts thereof are useful as antiviral agents.Type: GrantFiled: December 30, 1992Date of Patent: November 15, 1994Assignee: Sterling Winthrop Inc.Inventor: Guy D. Diana
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Patent number: 5360793Abstract: This invention is an antacid composition capable of forming a floating gelatinous mass when contacted with aqueous acid and consisting essentially of, as active ingredients, xanthan gum; an effective acid neutralizing amount of hexitol stabilized aluminum hydroxide and a gas producing material capable of producing a non-toxic gas when contacted with aqueous acid which may be formulated as a solid, powder, tablet or suspension.Type: GrantFiled: May 24, 1993Date of Patent: November 1, 1994Assignee: Sterling Winthrop Inc.Inventor: William J. Brooks
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Patent number: 5356903Abstract: Compounds of formula ##STR1## wherein; R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 X where X is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro;Z is NR.sub.5 or CR.sub.6 R.sub.7 ;R.sub.5 is hydrogen, aryl, arylthio, arylsulfonyl, lower-alkyl, cycloalkyl, heterocycloalkyl, amino-lower-alkyl, lower-alkylamino-lower-alkyl, dilower-alkylamino-lower-alkyl, lower-alkoxy, hydroxy or NR.sub.8 R.sub.9 ;R.sub.6 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro or lower-alkylsulfonyl;R.sub.7 is hydrogen, cyano, lower-alkoxycarbonyl, lower-alkanoyl, nitro, aryl, or lower-alkylsulfonyl;R.sub.8 is hydrogen, lower-alkyl, aryl, heterocycloalkyl, carbamyl, alkanoyl, aroyl, hydroxy-lower-alkyl; andR.sub.9 is hydrogen, lower-alkyl or lower-alkanoyl or pharmaceutically acceptable acid addition salts thereof are useful as anticancer agents.Type: GrantFiled: April 22, 1993Date of Patent: October 18, 1994Assignee: Sterling Winthrop Inc.Inventors: Michael A. Eissenstat, Gee-Hong Kuo
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Patent number: 5349068Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 is alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, alkoxyalkyl or hydroxyalkoxy;Y is alkylene of 3 to 9 carbon atoms,R.sub.2 and R.sub.3 independently are hydrogen, alkyl, alkoxy, halo, trifluoromethyl and nitro;R.sub.4 is alkoxy, hydroxy, halomethyl, dihalomethyl, trihalomethyl, cycloalkyl, alkoxycarbonyl, hydroxyalkyl, alkoxyalkyl, alkanecarbonyloxyalkyl, cyano, 2,2,2-trifluoroethyl, (4-methylphenyl)sulfonyloxymethyl, N.dbd.Q or CON.dbd.Q, where N.dbd.Q is amino, alkylamino or dialkylamino; or pharmaceutically acceptable acid-addition salts thereof are useful as antiviral agents.Type: GrantFiled: April 15, 1992Date of Patent: September 20, 1994Assignee: Sterling Winthrop Inc.Inventors: Guy D. Diana, Theodore J. Nitz
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Patent number: 5340589Abstract: Low solubility drug coated bead compositions, capsules filled therewith and method of preparation thereof, especially wherein the low solubility drug is an antiandrogenic steroid and most especially wherein the antiandrogenic steroid is (5.alpha.,17.alpha.)-1'-(methylsulfonyl)- 1'-H-pregn-20-yno[3,2-c]pyrazol-17-ol, are disclosed.Type: GrantFiled: May 12, 1993Date of Patent: August 23, 1994Assignee: Sterling Winthrop Inc.Inventors: Gregg Stetsko, Kuei-Tu Chang
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Patent number: 5334399Abstract: A lactose-hydrolyzed fluid milk comprising fluid milk, the normal lactose content of which has been reduced by at least about 70% by lactase hydrolysis, having incorporated therein from about 0.01 to about 0.15% by weight of potassium chloride, a process for its preparation and a method of suppressing perceived sweetness of lactose-hydrolyzed milk by incorporating therein potassium chloride.Type: GrantFiled: February 27, 1992Date of Patent: August 2, 1994Assignee: Sterling Winthrop Inc.Inventors: Robert G. Flynn, Abraham I. Bakal, Margaret A. Snyder
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Patent number: 5334595Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Y where Y is hydroxy, chloro, lower-alkylamino or dilower-alkylaminoR.sub.3 and R.sub.4 are each independently hydrogen or fluoro;R.sub.5 is hydrogen, lower-alkyl or(a) phenyl, 2-pyridyl, 4-pyridyl, 1-naphthyl or such groups substituted with one or more, the same or different, lower-alkyl, fluoro, hydroxy, or lower-alkoxy;(b) cycloalkyl or cycloalkyl substituted with amino, lower-alkylamino, dilower-alkylamino, formamido, acetamido, lower-alkyl, hydroxy, lower-alkoxy, trifluoromethyl, carboxy, lower-alkoxycarbonyl or halo, or cycloalkyl having a phenyl ring fused thereto;(c) A saturated heterocyclic 5- or 6-membered ring containing oxygen and/or nitrogen or such ring substituted with lower-alkyl; or(d) (CH.sub.2).sub.Type: GrantFiled: October 23, 1992Date of Patent: August 2, 1994Assignee: Sterling Winthrop Inc.Inventor: Mark P. Wentland
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Patent number: 5330759Abstract: Soft capsules coated with an enteric coating comprising a 1:1 copolymer of methacrylic acid and methyl or ethyl acrylate or methyl or ethyl methacrylate and a plasticizer without need for a subcoating and optionally additionally coated with a protective coating comprising hydroxypropyl methylcellulose or hydroxypropyl cellulose or a mixture thereof and a plasticizer and method of preparation thereof are disclosed.Type: GrantFiled: August 26, 1992Date of Patent: July 19, 1994Assignee: Sterling Winthrop Inc.Inventors: Shrikant N. Pagay, Gregg Stetsko
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Patent number: 5330760Abstract: A solid effervescent antacid formulation comprising as primary ingredients from about 35 to about 53 percent by weight of calcium carbonate, from about 0 to about 14 percent by weight of magnesium carbonate, from about 3.5 to about 7 percent by weight of a bicarbonate salt, from about 3.5 to about 7 percent by weight of malic acid and from about 21 to about 35 percent by weight of a bulking agent.Type: GrantFiled: August 27, 1992Date of Patent: July 19, 1994Assignee: Sterling Winthrop Inc.Inventor: William C. Walton
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Patent number: 5330992Abstract: Compounds of formula ##STR1## wherein R.sub.1 is hydrogen, lower-alkyl, or trifluoromethyl;R.sub.2 is lower-alkyl, trifluoromethyl or CH.sub.2 Z where Z is hydroxy, chloro, lower-alkylamino or dilower-alkylamino;R.sub.3 and R.sub.4 are each individually hydrogen or fluoro; andAr is phenyl, an aromatic 5- or 6-membered heterocycle or any of these substituted at one or more positions with lower-alkyl, fluoro, chloro, hydroxy, amino, lower-alkylamino, dilower-alkylamino, carboxy, sulfonamido, lower alkylsulfonamido, methylenedioxy, trifluoroacetamido, lower-alkanoylamino, or carbamoyl; and their pharmaceutically acceptable acid addition salts are useful as anticancer agents.Type: GrantFiled: October 23, 1992Date of Patent: July 19, 1994Assignee: Sterling Winthrop Inc.Inventors: Michael A. Eissenstat, John D. Weaver, III, Gee-Hong Kuo, Mark P. Wentland
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Patent number: 5294612Abstract: Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclylcarboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.Type: GrantFiled: March 30, 1992Date of Patent: March 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Baldev Singh, George Y. Lesher, deceased
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Patent number: 5292736Abstract: Compounds of the formula ##STR1## wherein Alk is lower-alkylene;R.sub.1 is hydrogen, lower-alkyl, Ar or ArCOO;R.sub.2 is hydrogen or lower-alkyl;R.sub.3 and R.sub.4 are the same or different hydrogen, fluoro, chloro, bromo, hydroxy, lower-alkoxy, lower-alkyl, or trifluoromethyl;Ar is phenyl, naphthyl, anthryl, 2-phenylethenyl or a 5- or 6-membered monocyclic or 9- or 10-membered bicyclic fused aromatic heterocyclic ring containing carbon and one or two heteroatoms independently selected from oxygen, nitrogen and sulfur, or such carbocyclic or heterocyclic rings substituted with from 1 to about 3 of lower-alkoxy, lower-alkyl, lower-alkylthio, lower-alkyl sulfinyl, lower-alkyl sulfonyl, hydroxy, cyano, amino, lower-alkylamino, dilower-alkylamino or halo;or pharmaceutically acceptable acid addition salts thereof are useful as analgesics and in the treatment of glaucoma.Type: GrantFiled: February 26, 1993Date of Patent: March 8, 1994Assignee: Sterling Winthrop Inc.Inventors: Virendra Kumar, Susan J. Ward