Abstract: The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic and/or basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.

Abstract: Immunomodulatory macrocyclic compounds having the formula ##STR1## and pharmaceutically acceptable salts, esters, amides and prodrugs thereof, wherein X is a group having the formula ##STR2## as well as pharmaceutical compositions containing the same.

Abstract: A method and system for use in treating a patient with FK 506 to prevent an adverse immune response, either a rejection of a transplanted organ or an attack on the patient's body by its own immune system caused by an autoimmune disease, without unduly suppressing the ability of the patient's immune system to combat infection. The method employs an expert system to provide non-numerical information concerning the course of action to be taken with respect to a patient's FK 506 treatment, at a given time, including, in particular, an instruction on whether the FK 506 dosage being administered to the patient should be changed, and if so how. That instruction is determined by the expert system through analysis of standardized characterizations assigned to standardized patient examination criteria provided to the expert system. The method also determines the actual numerical FK 506 dosage the patient should receive at a given time.

Abstract: The invention includes a water-soluble oxygen carrier. The oxygen carrier includes a meso-.alpha.,.alpha.,.alpha.,.alpha.-tetrakis(o-propanoylamino)phenylporph yrin, in which the 3-carbons of the propanoyl groups are each covalently bound to an amine nitrogen, and iron or cobalt is bound to the pyrrole nitrogens of the porphyrin. The oxygen carrier also includes a ligand L for protecting the open face of the porphyrin from .mu.-oxo dimer formation.

Abstract: A compound of the structure ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are each, independently, hydrogen or ##STR2## with the proviso that R.sup.1, R.sup.2, and R.sup.3 are not all hydrogen; R.sup.4 is --(CH.sub.2).sub.m X(CH.sub.2).sub.n CO.sub.2 R.sup.5 or ##STR3## R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, mono-, di-, or tri-hydroxyalkyl, aralkyl, or aryl; ##STR4## R.sup.7, R.sup.8, R.sup.9, and R.sup.10 are each, independently, hydrogen or alkyl;Y is CH or N:m is 0-4; n is 0-4; p is 0-4;with the proviso that m and n are not both 0 when X is O or S;or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, by virtue of its antitumor activity useful in treating tumors, and by virtue of its antifungal activity is useful in treating fungal infections.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: A method and system for use in treating a patient with FK 506 to prevent an adverse immune response, either a rejection of a transplanted organ or an attack on the patient's body by its own immune system caused by an autoimmune disease, without unduly suppressing the ability of the patient's immune system to combat infection. The method employs an expert system to provide non-numerical information concerning the course of action to be taken with respect to a patient's FK 506 treatment, at a given time, including, in particular, an instruction on whether the FK 506 dosage being administered to the patient should be changed, and if so how. That instruction is determined by the expert system through analysis of standardized characterizations assigned to standardized patient examination criteria provided to the expert system. The method also employs a means for determining the actual numerical FK 506 dosage the patient should receive at a given time.

Abstract: Method for preparing (dialkylamino-2 alkyl)sulphonyl-26 pristinamycin II.sub.B having general formula (I) ##STR1## by oxidation of (dialkylamino-2 alkyl)thio-26 pristinamycin II.sub.B with 3,5 to 20 of hydrogenperoxide equivalent, in the presence of alcaline metal tungstate, in a 2-phase medium, at a temperature between 10.degree. and 25.degree. C.

Abstract: Preparation of (dialkylamino-2 alkyl) sulphinyl-26 pristinamycin II.sub.B by oxidation of (dialkylamino-2 alkyl)thitinamycin II.sub.B, by hydrogen peroxide in the presence of sodium tungstate, in alcoholic medium.

Abstract: Polycyclic compounds (I) can be prepared in accordance with the following reaction formula: ##STR1## wherein R.sub.1 -R.sub.8 each represents a hydrogen atom, a hydroxyl group, an alkoxyl group or a substituted or unsubstituted benzyloxy group or neighboring two groups of R.sub.1 -R.sub.

Abstract: A Streptogramine derivative of formula (I) is disclosed, wherein the symbol Y is a hydrogen atom, a methyl amino or dimethylamino radical, or a protected methylamino radical, and the symbol R represents a methyl or ethyl radical.

Abstract: This invention relates to a process for preparing synergistic derivatives of formula (I), in which Y is hydrogen or dimethylamino, from pristinamycin I.sub.A or from virginiamycin, via a Mannich base, followed by elimination of the amine introduced.

Abstract: Bicyclic derivatives of the formula ##STR1## wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7a, R.sup.7b, and R.sup.8 are as defined in the specification. These compounds are antimicrobially active.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: Alkylidene macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by derivitization at C-9 or C-22. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Abstract: Alkyl and alkenyl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and derivitization at C-17. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: Dicarbonyloxy, carbonyloxy, carbanilate, and dihydroxy derivatives of Virginiamycin M.sub.1 are useful antibiotics and effectively bind gastrin and brain CCK receptors.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms which is optionally unsaturated, aralkyl of 7-10 carbon atoms, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, hydroxy, cyano, halo, nitro, carbalkoxy of 2-7 carbon atoms, trifluoromethyl, amino, or a carboxylic acid;or a pharmaceutically acceptable salt thereof when R.sup.2 is hydrogen, which are useful in the treatment of transplantation rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, or fungal infections.

Abstract: Disclosed are cyclic hexapeptides of the formula: ##STR1## These compounds are antagonists of oxytocin and are useful in the treatment of preterm labor and dysmenorrhea, and for stoppage of labor prepatory to Caesarian delivery. Also disclosed are pharmaceutical compositions containing the compounds of formula I and methods of preparing these compounds.

Abstract: A compound of the structure ##STR1## where R.sup.1, R.sup.2, and R.sup.3 are each, independently, hydrogen or ##STR2## with the proviso that R.sup.1, R.sup.2, and R.sup.3 are not all hydrogen; R.sup.4 is --(CH.sub.2).sub.m X(CH.sub.2).sub.n CO.sub.2 R.sup.5 or ##STR3## R.sup.5 and R.sup.6 are each, independently, alkyl, aralkyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid;X is ##STR4## R.sup.7 and R.sup.8 are each, independently, hydrogen or alkyl; Y is CH or N;m is 0-4; n is 0-4;with the proviso that m and n are not both 0 when X is O or S;or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppresive activity is useful in treating transplantation rejection, host vs.

Abstract: Aminomacrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by incorporation of a nitrogen substituent at C-3" and/or C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: A composition comprising a chelating compound which is a macrocyclic compound containing at least two coordinating centers in the ring, at least one of which is a neutral base moiety, and an organic acid containing at least one alkyl or alkenyl group containing 8 or more carbon atoms. The macrocyclic compound contains at least 10 ring atoms and especially at least 12 ring atoms. The neutral base moiety is typically a nitrogen moiety. Preferably there are at least four coordinating centers at least two of which are neutral base moities. The acid can be an alkyl or alkenyl substituted acid for example a long chain carboxylic acid. The composition can be used as an extractant system for the selective extraction of metals from an aqueous phase into an organic phase.

Abstract: A fused thiophene compound of the formula: ##STR1## or a pharmaceutically acceptable acid addition salt thereof. In the above formula, one of E.sup.1, E.sup.2 and E.sup.3 is sulfur atom and other two of them are C--R.sup.1 and C--R.sup.2 respectively. R.sup.1 and R.sup.2 are the same or different and each is hydrogen, halogen, nitro, amino, cyano, hydroxyl, formyl, alkyl, alkoxy, haloalkyl, arylalkyl, acyl, alkoxyalkyl, acyloxyalkyl, hydroxyalkyl, acyloxyalkanoyl, alkoxyalkanoyl, hydroxyalkanoyl, aryloxyalkanoyl, haloalkanoyl, alkylthio, alkylsulfinyl, alkylsulfonyl, arylthio, arylsulfinyl, arylsulfonyl, hydroxysulfonyl, halosulfonyl, sulfamoyl, substituted sulfamoyl, carboxyl, acylamino, alkoxycharbonyl, carbamoyl, substituted carbamoyl or substituted amino. D is --CH.sub.2 -- or --S(O).sub.m -- (m is 0, 1 or 2). Q is straight or branched chain alkylene. T is primary amino, secondary amino or tertiary amino.

Abstract: Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.

Abstract: Described is a new immunosuppressant, L-687,795, a C-13, C-15, C-31 trisdemethylated, ring rearranged derivative of L-683,590, produced under fermentation conditions utilizing the microorganism, Actinoplanacete sp. (Merck Culture Collection MA 6559) ATCC No. 53771. The macrolide immunosuppressant is useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow and heart transplants.

Abstract: This invention relates to novel 3,4,5,6-tetrahydro-2H-1,7,4-benzodioxazonines and their pharmaceutically acceptable salts. The compounds of the invention are cardiovascular agents and especially Class III antiarrhythmic agents.

Abstract: Novel didemnin compounds named didemnin X and didemnin Y have been isolated from the Caribbean tunicate Trididemnum solidum. These compounds have cytotoxic activity and, therefore, are useful as antitumor drugs.

Abstract: Aromatic hydrocarbons which are monosubstituted by straight-chain or branched C.sub.1 -C.sub.12 -alkyl or by C.sub.3 -C.sub.8 -cycloalkyl can be chlorinated in the presence of Friedel-Crafts Catalysts in liquid phase on the aromatic ring if 1,6-benzothiazocins are used as co-catalysts. This makes it possible to obtain a higher proportion of p-isomers.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sub.c is carboxy, esterified carboxy or amidated carboxy; R.sub.2 is hydrogen or lower alkyl or joins with R.sub.a and R.sub.b and the atoms therebetween to form a fused ring ##STR2## and either R.sub.a is methyl and R.sub.b is ##STR3## or R.sub.2 and R.sub.b and the atoms therebetween form a group ##STR4## wherein R.sub.3 and R.sub.4 are either both hydrogen, or together are propylene, butylene, or with the two atoms to which they are attached form a benzene ring. Methods of manufacture and use thereof in the production of angiotensin converting enzyme inhibitors are disclosed.

Abstract: Reagents useful in the preparation of 5'-biotinylated oligonucleotides are disclosed.

Abstract: Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No.

Abstract: There is described a process for the preparation of therapeutically useful pristinamycin II.sub.B sulphone derivatives.Also disclosed are compounds of general formula (I) in which n is equal to 2 in the form of their B isomers, and certain novel compounds of general formula (I) in which n is equal to 2.

Abstract: The invention provides new synergistin derivatives of formula ##STR1## in which Y is hydrogen or dimethylamino and R is a 3- or 4-quinuclidinyl radical, the isomers thereof and their mixtures, and their salts, also the preparation thereof. These compounds may be made by reaction of the corresponding 5-methylene compounds with the appropriate mercaptoquinuclidine. The products of formula (I), optionally combined with pristinamycin II.sub.A or a derivative of pristinamycin II.sub.B of the formula ##STR2## are useful as antimicrobials.

Abstract: Pristinamycin II.sub.

Abstract: Virginiamycin M.sub.1 having the Formula: ##STR1## and virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## Virginiamycin M.sub.1 and the analogs I-IV are antagonists of cholecystokinin (CCK) and gastrin. Cholecystokinin antagonists are useful as analgesics and in the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite regulatory systems in animals, especially humans. Gastrin antagonists are useful in blocking the receptors for gastrin in humans and may function as agents for the treatment of ulcers, tumors or other gastrointestinal disorders. The compounds of Formulae I-IV are also antibiotics and are useful as antimicrobial agents in animals including man and are useful as food additives to promote feed utilization in animals. Virginiamycin M.sub.1 and the analogs of Formula I, III, and IV are produced by the controlled aerobic fermentation of a strain of Streptomyces olivaceus, ATCC No.

Abstract: Pristinamycin II.sub.B derivatives of formula: ##STR1## in which R denotes a nitrogen-containing 4 to 7-membered heterocyclic ring optionally substituted by alkyl; or alkyl (2 to 4 C) substituted by 1 or 2 phenyl, cycloalkylamino or N-alkyl-N-cycloalkylamino (3 to 6 ring atoms), alkylamino, dialkylamino or dialkylcarbamoyloxy radicals (the dialkylamino moieties of these 2 latter radicals being capable of forming a 4 to 7-membered cyclic ring optionally substituted by alkyl) or substituted by 1 or 2 nitrogen-containing 4 to 7 membered heterocyclic rings, optionally substituted by alkyl, at least one of the above substituents being a nitrogen-containing substituent capable of forming salts and n is 1 or 2, all the alkyls being linear or branched and containing (unless stated otherwise) 1 to 10 carbon atoms, their isomers, their salts and their preparation. These compounds, optionally in combination with known synergistins or synergistins of formula: ##STR2## are useful as antimicrobial agents.