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: A label assembly includes machine readable indicia on the underside of the backing strip for verifying correspondence between identifying indicia on the label and the contents of a container before and/or during and/or after labeling of the container and is made by feeding a label layer/backing layer laminate web along a travel path and printing machine readable indicia on the underside of the backing layer and printing identifying indicia on the label layer.
Abstract: New compositions using particular .beta..sub.2 agonists and vehicle materials have been prepared and are useful for producing a topical anti-inflammatory effect in mammals. The selected .beta..sub.2 agonists have previously not been known to exhibit topical anti-inflammatory activity. The compositions can be for example in the form of sprays, ointments, creams, gels, lotions, and suppositories, all of which are to be applied to the mammal topically, as opposed to systemically.
Abstract: New compositions using particular .beta..sub.2 agonists and vehicle materials have been prepared and are useful for producing a topical anti-inflammatory effect in mammals. The selected .beta..sub.2 agonists have previously not been known to exhibit topical antiinflammatory activity. The compositions can be for example in the form of sprays, ointments, creams, gels, lotions, and suppositories, all of which are to be applied to the mammal topically, as opposed to systemically.
Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.
Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula ##STR2## .
Abstract: This invention relates to the conjoint use of asparagine or aspartic acid polymers, e.g. poly-l-asparagine or poly-l-aspartic acid polymers, or copolymers thereof, with aminoglycoside antibiotics to inhibit the nephrotoxicity associated with aminoglycoside antibiotics.
Type:
Grant
Filed:
April 29, 1983
Date of Patent:
July 2, 1985
Assignee:
Bristol-Myers Company
Inventors:
Patricia D. Williams, Girard H. Hottendorf
Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones of the general formula ##STR1## are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers. A preferred compound, 1-amino-2-[3-(3-piperidinomethylphenoxy)propylamino]cyclobutene-3,4-dione, is prepared by treating an intermediate, 1-methoxy-2-[3-(3-piperidinomethylphenoxy)propylamino]cyclobutene-3,4-dion e, with ammonia.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 is a straight or branched chain alkyl, alkenyl or alkynyl containing from 1 to 4 carbon atoms, and ##STR2## is a quaternary ammonio group as described herein, and nontoxic pharmaceutically acceptable salts, physiologically hydrolyzable esters and solvates thereof, as well as processes for their preparation, are disclosed. The compounds in which R.sup.1 is hydrogen are potent antibacterial agents.
Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.
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 anti-ulcer agents. Intermediates and processes for their preparation are disclosed.
Abstract: Histamine H.sub.2 -antagonists of the formula: ##STR1## wherein m is an integer of from 0 to 2 inclusive;n is an integer of from 2 to 5 inclusive;Z is oxygen, sulfur or methylene; andA is ##STR2## in which R.sup.1 is hydrogen, (lower)alkyl, or (lower)alkoxy, and R.sup.2 is ##STR3## in which q is an integer of from 1 to 4 inclusive, and R.sup.3 and R.sup.4 each are independently, (lower)alkyl, (lower)-alkoxy(lower)alkyl in which the (lower)alkoxy moiety is at least two carbon atoms removed from the nitrogen atom, cyclo(lower)alkyl, or phenyl(lower)alkyl; provided that R.sup.3 and R.sup.4 may not both be cyclo(lower)alkyl; or R.sup.3 and R.sup.4, taken together with the nitrogen atom to which they are attached, may be pyrrolidino, methylpyrrolidino, dimethylpyrrolidino, morpholino, thiomorpholino, piperidino, methylpiperidino, dimethylpiperidino, N-methylpiperazino, 1,2,3,6-tetrahydropyridyl, homopiperidino, heptamethyleneimino, octamethyleneimino, or 3-azabicyclo[3.2.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or a conventional amino-protecting group, R.sup.2 is a straight or branched chain alkyl group containing from 1 to 4 carbon atoms, allyl, 2-butenyl, 3-butenyl, propargyl, 2-butynyl, 3-butynyl, cycloalkyl containing from 3 to 6 carbon atoms or a group of the formula ##STR2## in which R.sup.3 and R.sup.4 each are independently hydrogen, methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the carbon atom to which they are attached, may be a cycloalkylidene ring containing from 3 to 6 carbon atoms or a substituted cyclobutylidene ring of the formula ##STR3## wherein X is halogen, hydroxy or (lower)alkoxy, and R.sup.5 and R.sup.