Sterling Drug Inc.

Sterling Winthrop Inc.

Eastman-Kodak Company

Sanofi

Nahosystems L.l.c.

Sol J Daum

Robert L Clarke

Edward R Bacon

Carl R Illig

Kimberly G Estep

Kurt A Josef

Brent D Douty

George Y Lesher

Baldev Singh

Paul P Spara

Philip E Shaw

John L Toner

Robert W Lee

Edward J Baker

Michael Reuman

Haruo Yamamoto

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.

6-substituted pyrazolo[3,4-d]pyrimidin-4-ones and compositions and

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;

2,4,6-triiodo-5-substituted-amino-isophthalate esters useful as x-ray

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;

Compositions of iodophenyl sulfonates for X-ray visualization of the

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; and R.sup.5 is H, alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl; are useful as contrast agents in x-ray imaging compositions and methods.

Polyiodinated aroyloxy esters

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;

Compositions of iodophenyl esters and iodophenyl sulfonates and

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

Compositions of iodophenyl esters and iodophenyl sulfonates in

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;

Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;

Iodinated aroyloxy esters

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

Compositions of iodophenyl esters for X-ray visualization of the

Iodinated aroyloxy carboxamides

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.

Pyridinyl-quinolone compounds, their preparation and use

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.

1-ethyl-6-fluoro-1,4-dihydro-

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.

Aminocyclitol antibiotics, pharmaceutical compositions and method of

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.

2-Hydroxy gentamicin compounds

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.

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Albany, NY, United States of America

Sol J Daum