Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.