Abstract: The novel antibiotic, oxanosine, having the structure ##STR1## inhibits the growth of Gram-negative bacteria and has antiviral and carcinostatic activity. It is produced by cultivation of an oxanosine-producing microorganism of the genus Streptomyces, preferably Streptomyces capreolus MG265-CF3, ATCC No. 31963.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Potent antibacterial agents of the formula ##STR1## wherein R is methyl, ethyl or isopropyl, and their pharmaceutically acceptable salts, physiologically hydrolyzable esters and solvates, and processes for their preparation, are described.

Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Four new antibiotics which are denominated istamycin A, istamycin B, istamycin A.sub.o and istamycin B.sub.o, and which are useful as antibacterial agents, are produced by fermentation of a new microorganism, Streptomyces tenjimariensis.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anti-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the corresponding 3-methylcephem. The 6- or 7-side-chain of these products may be cleaved to give the corresponding 6-amino (penams) or 7-amino (cephams and cephems) compounds, and the latter may be reacylated to produce different 6-acyl-2-carbamoyloxymethyl penams, 7-acyl-3-carbamoyloxy cephams and 7-acyl-3-methylcephems. The substituent groups may be removed from the (substituted)-2-carbamoyloxypenams or the (substituted)-3-carbamoyloxycephams to give the corresponding free 2-carbamoyloxymethylpenams or 3-carbamoyloxycephams, respectively.

Abstract: Histamine H.sub.2 -antagonists of the formula ##STR1## wherein p is 1 or 2; R.sup.1 is hydroxy, amino, substituted amino or a 5- to 9-membered fully saturated nitrogen-containing heterocyclic ring attached via its nitrogen atom; m is an integer of from 0 to 2; n is an integer of from 2 to 4; Z is sulfur, oxygen or methylene; and A is an optionally substituted phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl, thiadiazolyl, oxadiazolyl, furyl, thienyl or pyridyl ring; and nontoxic pharmaceutically acceptable salts, hydrates, solvates or N-oxides thereof are novel anit-ulcer agents. Intermediates and processes for their preparation are disclosed.

Abstract: An improved process for the preparation of 1-N-[.omega.-amino-.alpha.-hydroxyalkanoyl]aminoglycoside antibiotics comprises acylating a polysilylated aminoglycoside antibiotic in a substantially anhydrous organic solvent with an acylating derivative of an .omega.-amino-.alpha.-hydroxyalkanoic acid.

Abstract: Enhanced antiulcer activity is obtained in warm-blooded animals by the concomitant administration of the histamine H.sub.2 -receptor antagonist, etintidine, and the pepsin complexing agent, pepstatin. Concomitant administration of the two entities reduces the amount of etintidine necessary for effective treatment, thereby decreasing its side effect liability.

Abstract: Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the corresponding 3-methylcephem. The 6- or 7-side-chain of these products may be cleaved to give the corresponding 6-amino (penams) or 7-amino (cephams and cephems) compounds, and the latter may be reacylated to produce different 6-acyl-2-carbamoyloxymethyl penams, 7-acyl-3-carbamoyloxy cephams and 7-acyl-3-methylcephems. The substituent groups may be removed from the (substituted)-2-carbamoyloxypenams or the (substituted)-3-carbamoyloxycephams to give the corresponding free 2-carbamoyloxymethylpenams or 3-carbamoyloxycephams, respectively.

Abstract: A method of producing analgesia by the simultaneous or sequential administration of butorphanol and zomepirac and compositions comprising butorphanol and zomepirac which provide enhanced (synergistic) analgetic potencies.

Abstract: A stable, microcrystalline form of cisplatin, a process for its preparation, and stable, sterile dry-mix formulations thereof which are more rapidly reconstituted with sterile water to produce solutions suitable for intravenous administration to man than are similar formulations containing "regular" cisplatin. The microcrystalline cisplatin and dry-mix formulations thereof are prepared without the use of lyophilization.

Abstract: The known antibiotic, nocardicin, is produced by submerged aerobic cultivation of Microtetraspora caesia sp. nov. ATCC 31724 or 31725.

Abstract: Penicillin sulfoxide esters are reacted with an isocyanate to produce the corresponding (substituted)-2-carbamoyloxymethylpenam, the corresponding (substituted)-3-carbamoyloxycepham or the corresponding 3-methylcephem. The 6- or 7-side-chain of these products may be cleaved to give the corresponding 6-amino (penams) or 7-amino (cephams and cephems) compounds, and the latter may be reacylated to produce different 6-acyl-2-carbamoyloxymethyl penams, 7-acyl-3-carbamoyloxy cephams and 7-acyl-3-methylcephems. The substituent groups may be removed from the (substituted-2-carbamoyloxypenams or the (substituted)-3-carbamoyloxycephams to give the corresponding free 2-carbamoyloxymethylpenams or 3-carbamoyloxycephams, respectively.

Abstract: A stable, microcrystalline form of cisplatin, a process for its preparation, and stable, sterile dry-mix formulations thereof which are more rapidly reconstituted with sterile water to produce solutions suitable for intravenous administration to man than are similar formulations containing "regular" cisplatin. The microcrystalline cisplatin and dry-mix formulations thereof are prepared without the use of lyophilization.

Abstract: Four new antibiotics which are denominated istamycin A, istamycin B, istamycin A.sub.o and istamycin B.sub.o, and which are useful as antibacterial agents, are produced by fermentation of a new microorganism, Streptomyces tenjimariensis.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, hydroxy, cyano, (lower)alkyl, (lower)alkoxy, halogen or amino; n is 2 or 3; X is NR.sup.3 or CHR.sup.3 ; R.sup.3 is cyano, nitro, SO.sub.2 Ar; or SO.sub.2 (lower)alkyl; R.sup.12 is hydrogen or (CH.sub.2).sub.p NR.sup.13 R.sup.14 ; p is an integer of from 1 to 4, inclusive; R.sup.13 and R.sup.14 each are independently hydrogen or (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents independently selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is a straight or branched chain alkynyl group containing from 3 to 9 carbon atoms, inclusive; R.sup.2 is hydrogen, hydroxy, cyano, (lower)alkyl, (lower)alkoxy, halogen or amino; n is 2 or 3; X is NR.sup.3 or CHR.sup.3 ; R.sup.3 is cyano, nitro, SO.sub.2 Ar; or SO.sub.2 (lower)alkyl; R.sup.12 is hydrogen or (CH.sub.2).sub.p NR.sup.13 R.sup.14 ; p is an integer of from 1 to 4, inclusive; R.sup.13 and R.sup.14 each are independently hydrogen or (lower)alkyl; and Ar is phenyl or phenyl containing 1 or 2 substituents independently selected from halogen and (lower)alkyl; and nontoxic, pharmaceutically acceptable salts thereof, are potent anti-ulcer agents.