Abstract: Disclosed is the novel bacteriophage TG1, TG1 derivatives, and the corresponding genome or nucleic acid components of such bacteriophages and derivatives of such genome, which are useful as DNA cloning vectors into organisms, such as bacteria, for example, Streptomyces cattleya NRRL 8057; portions of such phage genome are additionally useful as adjuncts in recombinant DNA cloning procedures, for example: (1) to permit the maintenance of cloned DNA in the host, either in an integrated state or as an autonomous element; (2) to serve as promoters for increasing expression of endogenous or foreign genes wherein said promoters are ligated to such genes or otherwise serve as promoters; and (3) to serve as regulatory elements for achieving control over endogenous and foreign gene expression; as cloning vectors, TG1, its deletion mutants, and other derivatives serve for the amplification and transfer of DNA sequences (genes) coding for useful functions, for example, genes necessary for the production of the antibioti
Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine;R is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl;R.sup.1 is hydrogen; straight or branched C.sub.1-8 alkyl; aryl; aryl substituted with up to two members selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halo, and mono- or di-C.sub.1-3 alkyl substituted amino; heteroaryl; formyl C.sub.2-4 alkenyl; or C.sub.2-4 alkenyl; andR.sup.2 is straight or branched C.sub.
Abstract: This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the 6-amino nitrogen moiety of the penicillin (or ring analogue thereof) nucleus represents a mono- or polycyclic N-containing heterocyclic group;X is S, SO, CH.sub.2, or O; m is 0, 1 or 2;R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkyl, heterocyclylalkenyl, aralkenyl, aralkyl, --NR.sub.2, COOR, CONR.sub.2, --OR, or CN;R.sup.2 is H, or lower alkoxyl.
Abstract: Antimicrobial compounds of the formula: ##STR1## where R is a heterocyclic radical selected from the group consisting of thienyl; furanyl; pyrrolyl; isoxazolyl; oxazolyl; isothiazolyl, thiazolyl; pyrazolyl; imidazolyl; pyridazinyl; pyrimidinyl; pyrazinyl; pyridinyl; and N-oxides thereof; andn is 0 to 4.
Type:
Grant
Filed:
December 22, 1981
Date of Patent:
January 29, 1985
Assignee:
Merck & Co., Inc.
Inventors:
John E. Engelhart, Marshall R. Angeles, Michael J. D'Errico
Abstract: Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.
Abstract: Disclosed are azabicyclo[2.1.0] antibiotics (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics. ##STR1## Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Abstract: 4-Amino-3-hydroxy-2,4-(disubstituted)pentanoic acids of the formula: ##STR1## useful as intermediates in preparing antibacterial compounds, are synthesized enantiospecifically by acylation of a chiral enolate with an optically active acylating agent. The resulting product is reduced stereospecifically to afford a protected form of the desired product, which contains three adjacent asymmetric centers of known configuration.
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Abstract: Antimicrobial compounds of the formula: ##STR1## wherein: Hal is bromine or chlorine; andR is halo; mono- or di-substituted mono- or diloweralkylamino wherein the loweralkyl substituents are hydroxy or loweralkanoyloxy; 4-morpholino; thiocyano; mercapto; straight or branched chain C.sub.1-8 alkylthio; mono- or di-substituted loweralkylthio wherein the substituents are hydroxy, amino, loweralkanoylamino, or loweralkoxycarbonyl; arylthio; loweralkylsulfoxy; or loweralkylsulfonyl; andR.sup.1 is C.sub.6-12 alkyl;are useful in various agricultural and industrial applications.
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperalaosteronism.
Type:
Grant
Filed:
November 4, 1982
Date of Patent:
October 30, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Daniel F. Veber, Joshua S. Boger, Mark G. Bock
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Abstract: Disclosed is a process for preparing antibiotic 1-oxadethiacephalosporins via diazo-species I: ##STR1## wherein: A is acyl; R.sup.1 is H or OCH.sub.3 ; and R.sup.2 is a protecting group.
Abstract: Renin inhibitory peptides of the formula ##STR1## and analogs thereof inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.
Abstract: A method of controlling Corbicula in aqueous systems comprising treating said systems with a cationic polymer. A preferred polymer is a poly (quaternary ammonium) compound having the recurring structure:[DMDAAX.sup..crclbar. ]where DMDAAX.sup..crclbar. is a polymer unit resulting from monomeric dimethyldiallylammonium X.sup..crclbar. ; and X.sup..crclbar. is an anion; said polymer preferably having a weight average molecular weight of from about 200,000 to 400,000.
Abstract: Disclosed is the novel bacteriophage TG1, TG1 derivatives, and the corresponding genome or nucleic acid components of such bacteriophages and derivatives of such genome, which are useful as DNA cloning vectors into organisms, such as bacteria, for example, Streptomyces cattleya NRRL 8057; portions of such phage genome are additionally useful as adjuncts in recombinant DNA cloning procedures, for example: (1) to permit the maintenance of cloned DNA in the host, either in an integrated state or as an autonomous element; (2) to serve as promoters for increasing expression of endogenous or foreign genes wherein said promoters are ligated to such genes or otherwise serve as promoters; and (3) to serve as regulatory elements for achieving control over endogenous and foreign gene expression; as cloning vectors, TG1, its deletion mutants, and other derivatives serve for the amplification and transfer of DNA sequences (genes) coding for useful functions, for example, genes necessary for the production of the antibioti
Abstract: Novel substituted pyrazinyl-1,2,4-oxadiazoles and processes for preparing the same. The compounds are useful in the treatment of edema and hypertension.
Type:
Grant
Filed:
September 1, 1982
Date of Patent:
June 12, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Mark G. Bock, Edward J. Cragoe, Jr., Robert L. Smith
Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
Type:
Grant
Filed:
June 25, 1982
Date of Patent:
May 15, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams