Patents by Inventor Sol J. Daum
Sol J. Daum has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5977118Abstract: 6-Substituted pyrazolo[3,4-d]pyrimidin-4-one derivatives, pharmaceutical compositions containing them and methods for effecting c-GMP-phosphodiesterase inhibition and for treating heart failure and/or hypertension.Type: GrantFiled: March 26, 1997Date of Patent: November 2, 1999Assignee: SanofiInventors: Edward R. Bacon, Sol J. Daum, Baldev Singh
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Patent number: 5670136Abstract: Compounds having the structure: ##STR1## wherein Q is ##STR2## n is an integer from 0 to 20; R.sup.1 is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido;R.sup.6 is alkyl, cycloalkyl, aryl, or aralkyl; andR.sup.7 is H or --COR.sup.6 are useful as contrast agents in medical diagnostic x-ray imaging compositions and methods.Type: GrantFiled: January 16, 1996Date of Patent: September 23, 1997Assignee: NahoSystems L.L.C.Inventors: Edward R. Bacon, Sol J. Daum, Kimberly G. Estep
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Patent number: 5468466Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract wherein ##STR2## Z=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=C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene, lower-alkoxy-carbonyloxy;n=1-5;y=0-4; andw=1-4in an aqueous pharmaceutically acceptable carrier.Type: GrantFiled: February 1, 1994Date of Patent: November 21, 1995Assignee: Sterling Winthrop, Inc.Inventors: Edward R. Bacon, Sol J. Daum, Kimberly G. Estep, Kurt A. Josef, Brent D. Douty, Carl R. Illig
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Patent number: 5466433Abstract: Compounds having the structure ##STR1## wherein Z--COO).sub.m is the residue of a polyiodinated aromatic acid; m is 1, 2, 3 or 4;n is an integer from 1 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy or acylamino; andR.sup.5 is H, alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;are useful as contrast agents in x-ray imaging compositions and methods.Type: GrantFiled: June 20, 1994Date of Patent: November 14, 1995Assignee: Eastman Kodak CompanyInventors: Edward R. Bacon, Sol J. Daum, Paul P. Spara
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Patent number: 5385722Abstract: Disclosed are contrast agents of the formula ##STR1## wherein ##STR2## Z is H, halo, C.sub.5 -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 is C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, each of which may be optionally substituted with lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy;n is 1-5;y is 0-4; andw is 1-4;in a pharmaceutically acceptable carrier comprising a cellulose derivative.Type: GrantFiled: April 18, 1994Date of Patent: January 31, 1995Assignee: Sterling Winthrop Inc.Inventors: Edward J. Baker, Robert W. Lee, Edward R. Bacon, Sol J. Daum, Kimberly G. Estep, Kurt A. Josef, Brent D. Douty, Carl R. Illig, John L. Toner
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Patent number: 5372800Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract whereinX= ##STR2## Z=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=C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy,n is 1-5;y is 0-4; andw is 1-4.Type: GrantFiled: February 4, 1994Date of Patent: December 13, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Sol J. Daum, Kimberly G. Estep, Kurt A. Josef, Brent D. Douty, Carl R. Illig
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Patent number: 5336484Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a polymeric material capable of forming a coating on the gastrointestinal tract and an x-ray producing agent of the formula ##STR1## and methods for their use in diagnostic radiology of the gastrointestinal tract wherein ##STR2## Z=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=C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy,n is 1-5;y is 0-4; andw is 1-4.Type: GrantFiled: March 31, 1993Date of Patent: August 9, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Sol J. Daum, Kimberly G. Estep, Kurt A. Josef, Brent D. Douty, Carl R. Illig
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Patent number: 5322679Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;n is an integer from 1 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy or acylamino; andR.sup.5 is alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;are useful as contrast agents in x-ray imaging compositions and methods.Type: GrantFiled: December 16, 1992Date of Patent: June 21, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Sol J. Daum, Paul P. Spara
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Patent number: 5318769Abstract: Disclosed are contrast agents of the formula ##STR1## contained in aqueous compositions and methods for their use in diagnostic radiology of the gastrointestinal tract whereinX= ##STR2## Z=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=C.sub.1 -C.sub.25 alkyl, cycloalkyl, aryl, or halo-lower-alkyl, optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl, lower-alkenyl, lower-alkynyl, lower-alkylene, lower-alkoxy-carbonyloxy;n=1-5;y=0-4; andw=1-4in an aqueous pharmaceutically acceptable carrier.Type: GrantFiled: March 31, 1993Date of Patent: June 7, 1994Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Sol J. Daum, Kimberly G. Estep, Kurt A. Josef, Brent D. Douty, Carl R. Illig
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Patent number: 5260478Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;n is an integer from 0 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently a substituent as defined for R.sup.1 and R.sup.2 above, halogen, hydroxy or acylamino;and R.sup.5 and R.sup.6 are independently H, alkyl, cycloalkyl, aryl, aralkyl, alkoxy, alkoxyalkyl, or acetamidoalkyl;or R.sup.5 and R.sup.6, taken together with the nitrogen atom to which they are attached, represent a 4 to 7-membered nitrogen containing ring, are useful as contrast agents in x-ray imaging compositions and methods.Type: GrantFiled: December 8, 1992Date of Patent: November 9, 1993Assignee: Sterling Winthrop Inc.Inventors: Edward R. Bacon, Sol J. Daum, Carl R. Illig
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Patent number: 5169853Abstract: Fluorinated 1- cyclopropyl-7-(substituted-pyridinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxy lic acids of the formula ##STR1## wherein R is hydrogen, R' and R" are hydrogen or fluoro, and Z is 3- or 4-pyridinyl substituted by alkyl groups or substituted alkyl groups, are superior antibacterial agents. They are prepared via a coupling reaction between the corresponding esters (R=alkyl) having a halo group in the 7-position and a substituted (trialkylstannyl)-pyridine.Type: GrantFiled: September 9, 1991Date of Patent: December 8, 1992Assignee: Sterling Drug Inc.Inventors: George Y. Lesher, Baldev Singh, Michael Reuman, Sol J. Daum
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Patent number: 4698350Abstract: 1-Ethyl-6-fluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinoline carboxylic acid (Win 52,522) or salt thereof, a highly potent antibacterial agent, is prepared by nitrating the corresponding 6-desfluoro compound (Win 35,439) to produce the corresponding 6-nitro compound, reducing the latter compound to produce the corresponding 6-amino compound and converting the 6-amino via its diazonium salt to said 6-fluoro compound (Win 52,522). Comparative in vitro and in vivo antibacterial test data are provided to demonstrate the uniqueness of Win 52,522 as a highly potent antibacterial agent having a broad spectrum of antimicrobial activity.Type: GrantFiled: September 17, 1984Date of Patent: October 6, 1987Assignee: Sterling Drug Inc.Inventors: Sol J. Daum, George Y. Lesher
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Patent number: 4396609Abstract: Aminocyclitol analogs of gentamicin C.sub.1, C.sub.2 and C.sub.1a and the corresponding compounds acylated on the 1-, 3- and 2'-amino groups with an .omega.-amino-.alpha.-hydroxy-lower-alkanoyl group are prepared by culturing a nutrient medium containing carbohydrates, a source of assimilable nitrogen, essential salts and an added aminocyclitol with a mutant of Micromonospora purpurea and acylating the product with an ester of an .omega.-(N-benzyloxycarbonyl)amino-.alpha.-hydroxy-lower-alkanoic acid followed by catalytic hydrogenolysis of the benzyloxycarbonyl group.Type: GrantFiled: September 6, 1977Date of Patent: August 2, 1983Assignee: Sterling Drug Inc.Inventors: Sol J. Daum, Robert L. Clarke
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Patent number: 4387219Abstract: 2-Hydroxygentamicins B, B.sub.1 and A.sub.3 and 2-hydroxy antibiotics JI-20A and JI-20B are prepared as fermentation products by culturing a nutrient medium containing carbohydrates, a source of assimilable nitrogen, essential salts and D-streptamine with a mutant of Micromonospora purpurea, and isolating the said fermentation products from the nutrient medium; the fermentation products are acylated with an ester of an .omega.-(N-benzyloxycarbonyl)amino-.alpha.-hydroxy-lower-alkanoic acid, after first blocking the 6'-and/or 2'-amine group with an amine-protecting group, followed by catalytic hydrogenolysis of the benzyloxycarbonyl group and removal of the amine-protecting groups to prepare the 1-N-(.omega.-amino-.alpha.-hydroxy-lower-alkanoyl) derivatives.Type: GrantFiled: November 24, 1980Date of Patent: June 7, 1983Assignee: Sterling Drug Inc.Inventors: Haruo Yamamoto, Sol J. Daum
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Patent number: 4281130Abstract: Compounds of tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substituent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.Type: GrantFiled: October 26, 1979Date of Patent: July 28, 1981Assignee: Sterling Drug Inc.Inventors: Robert L. Clarke, Sol J. Daum
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Patent number: 4233449Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substitutent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.Type: GrantFiled: October 26, 1979Date of Patent: November 11, 1980Assignee: Sterling Drug Inc.Inventors: Robert L. G. Clarke, Sol J. Daum
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Patent number: 4233448Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substitutent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.Type: GrantFiled: October 26, 1979Date of Patent: November 11, 1980Assignee: Sterling Drug Inc.Inventors: Robert L. Clarke, Sol J. Daum
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Patent number: 4214084Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substituent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.Type: GrantFiled: May 24, 1979Date of Patent: July 22, 1980Assignee: Sterling Drug Inc.Inventors: Robert L. Clarke, Sol J. Daum
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Patent number: 4179567Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substiutent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.Type: GrantFiled: April 10, 1978Date of Patent: December 18, 1979Assignee: Sterling Drug Inc.Inventors: Robert L. Clarke, Sol J. Daum
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Patent number: 4072692Abstract: Trans-4-(8-hydroxyoctyl)-5-octyl-1,3-dithiolane-2-thione, useful as a hypocholesteremic and hypotriglyceridemic agent, is prepared by treatment of the epoxide of oleyl alcohol with carbon disulfide and an alkali metal hydroxide in a lower-alkanol.Type: GrantFiled: October 15, 1976Date of Patent: February 7, 1978Assignee: Sterling Drug Inc.Inventor: Sol J. Daum