Abstract: Novel 1,3-dioxolane compounds useful as antifungal and antiallergy agents and represented by the formula ##STR1## wherein Ar is thienyl, pyridyl, biphenyl, phenyl or phenyl substituted by one or more of halo, nitro, cyano, lower alkyl, lower alkoxy or perhalo(lower)alkyl; Y is CH or N;Q is ##STR2## W is --NR.sub.5 --, --O--, --S(O).sub.n --; X is NO.sub.2, NR.sub.6 R.sub.7 or COR.sub.8 ;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl or (C.sub.2 -C.sub.6) alkanoyl; R.sub.6 and R.sub.7 are independently hydrogen, lower alkyl, phenyl or phenyl substituted by one or more of halo, perhalo loweralkyl, (C.sub.2 -C.sub.6)alkanoyl lower alkyl, lower alkoxy or 2-loweralkyl-3-oxo-1,2,4-trirazol-4-yl or R.sub.6 and R.sub.7 taken together with the nitrogen atom in NR.sub.6 R.sub.7 form substituted or unsubstituted heterocyclyl, said heterocyclyl substituents being (C.sub.2 -C.sub.
Type:
Grant
Filed:
December 24, 1986
Date of Patent:
November 29, 1988
Assignee:
Schering Corporation
Inventors:
Anil K. Saksena, Alan B. Cooper, Henry Guzik, Viyoor M. Girijavallabhan, Ashit K. Ganguly
Abstract: A sustained release theophylline containing oral dosage formulation comprising theophylline containing micropellets coated with from about 0.5% to about 2% by weight of a pharmaceutically acceptable water-insoluble film former, preferably ethyl cellulose and having first order release. The formulation is an improvement over theophylline containing micropellets coated with two film formers which have zero order release. The oral dosage formulation has superior non-fasting release and absorption characteristics when compared to the zero order release formulation.
Type:
Grant
Filed:
May 18, 1987
Date of Patent:
November 22, 1988
Assignee:
Schering Corporation
Inventors:
Richard Chang, Robert P. Giannini, Charles Hsaio
Abstract: An oil-in-water cream or lotion emulsion formulation containing clotrimazole having improved antifungal properties containing various amounts of clotrimazole, petrolatum, cetearyl alcohol, propylene glycol, and ceteth-20, with or without other additional ingredients.
Abstract: A multi-step stereospecific process for preparing (3S,4R,5R)-1-(allyloxycarbonyl)-methyl-3-(1-hydroxyethyl)-4-beta-naphthoxy thiocarbonylthio-2-azetidinones, stereoisomers thereof or hydroxy protected analogs thereof from anhydropenicillin. The azetidinones are intermediates useful for producing penems which are a known group of antibacterial compounds. The process involves protecting the hydroxy group of anhydropenicillin with a readily removable hydroxy protecting group, then converting the resulting compound by ozonolysis followed by reaction with a trialklyl phosphite, then hydrolysis to remove the methylidene group at the 2-position of anhydropenicillin. The resulting compound is converted to the unprotected 4-beta-naphthoxy thiocarbonylthio derivative by reaction with allyl alcohol and HCl followed by reaction with O-2-napththalenylcarbonochloridothioate, or to the protected compound by reaction with silver imidazolate and allyl alcohol followed by reaction with O-2-naphthalenylcarbonochloridothioate.
Abstract: A compound represented by formula I ##STR1## wherein R is hydrogen, or ##STR2## wherein R.sup.1 is N-acylamino, N-alkylamino, N,N-dialkylamino, N-acyl-N-hydroxylamino, nitroso or the pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
August 27, 1986
Date of Patent:
July 30, 1988
Assignee:
Schering Corporation
Inventors:
Ashit K. Ganguly, Olga Sarre, Viyyoor M. Girijavallabhan
Abstract: The antibiotic 7273 complex is elaborated by the microorganism, Dactylosporangium vescum ATCC 39499. The novel 7-chloro-4a-hydroxy-8-methoxytetracycline isolated from antibiotic 7273 complex is active against gram-positive and gram-negative aerobes.
Type:
Grant
Filed:
August 9, 1985
Date of Patent:
June 21, 1988
Assignee:
Schering Corporation
Inventors:
Mahesh G. Patel, Ann C. Horan, Joseph A. Marquez, George H. Miller, Richard W. Vaughan
Abstract: Disclosed are 6-(1'hydroxyethyl)-2-(azacycloalkyl)penem-3-carboxylic acids and salts or metabolizable esters thereof having an absolute stereochemistry of 5R,6S,8R. The compounds are useful and potent antibacterial agents and can be formulated into a variety of forms suitable for oral, parenteral or topical use.
Type:
Grant
Filed:
December 6, 1982
Date of Patent:
May 10, 1988
Assignee:
Schering Corporation
Inventors:
Ashit K. Ganguly, Viyyoor M. Girijavallabhan, Adriano Afonso, Jay Weinstein
Abstract: Actinomadura melliaura nov. sp. (ATCC 39691) produces four novel compounds which we have designated AT 2433 A.sub.1, AT 2433 A.sub.2, AT 2433 B.sub.1 and AT 2433 B.sub.2. The novel compounds or pharmaceutically acceptable salts thereof exhibit antibacterial and antitumor activity.
Type:
Grant
Filed:
September 17, 1984
Date of Patent:
May 10, 1988
Assignee:
Schering Corporation
Inventors:
Ann C. Horan, Jerzy Golik, James A. Matson, Mahesh G. Patel
Abstract: A multistep process is disclosed for preparing azetidinone intermediates used in the making penems and carbapenems wherein intermediates containing ##STR1## R' is independently hydrogen or 1, 2 or 3 of lower alkyl or lower alkoxy, preferably hydrogen, wherein R" is methyl, ethyl, a phenyl or alkyl, preferably ethyl, as a readily removable nitrogen protecting group are made.
Abstract: A process for the conversion of aristeromycin into cyclaradine via. The stereoselective reduction of a 3',5'-di-O-protected-2'-keto derivative of aristeromycin is disclosed.
Type:
Grant
Filed:
May 20, 1986
Date of Patent:
April 26, 1988
Assignee:
Schering Corporation
Inventors:
Tattanahali L. Nagabhushan, Doris P. Schumacher
Abstract: Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-trizazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiopenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.
Abstract: 2-Alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-2-(1H-azolyl(C.sub.1 -C.sub.2)alkyl)benzo[b]thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-3-hydroxy-2-(1H-1-imidazolylmethyl)-4-,5-,6- and 7-halobenzo[b]thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions comprising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed.
Abstract: A topical albuterol composition having superior transdermal flux containing various amounts of albuterol, 1-dodecyl-azacycloheptan-2-one and urea in a non-aqueous environment. The enhancement observed in albuterol skin penetration indicates that a therapeutically effective amount of albuterol can be delivered through skin using these formulations. The compositions can be administered topically as a cream, lotion or via a transdermal device.