Abstract: A cyclic iminocarboxylic acid derivative of the formula: ##STR1## or a salt thereof, wherein X.sup.1 and X.sup.2 are each hydrogen, halogen, lower alkoxy, lower alkyl, trifluoromethyl, nitro, amino, alkylamino, aralkylamino, acetylamino or ethoxycarbonylamino, Y is --CO-- or --SO.sub.2 --, Z is --CH.sub.2 -- or --S--, and R is hydrogen or lower alkyl. Such compounds are useful as antihypertensive agents.

Abstract: Novel antibacterially-active analogs of the antibiotics nodusmicin and nargenicin A.sub.1. These compounds are prepared by selectively blocking active hydroxyl groups at the 9, 11 and 18 positions of nodusmicin, and the 11 and 18 positions of nargenicin A.sub.1. Antibacterially-active compounds can be used in various environments to control or eradicate susceptible bacteria. The techniques for such use are well known in the art.

Abstract: The present invention relates to the 3-[N-(2-mercapto-propionyl-amino-acetyl)]-tetrahydro-thiazolyl-4-carboxyli c acid and pharmaceutical compositions containing it, endowed with a marked inhibitory activity of the angiotensin converting enzyme (ACE).

Abstract: Thiazolidine derivatives of the general formula: ##STR1## [wherein R.sup.1 is alkyl, cycloalkyl, phenylalkyl, phenyl, a five- or six-membered heterocyclic group including one or two hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur or a group of the formula ##STR2## (where R.sup.3 and R.sup.4 are the same or different and each is lower alkyl or R.sup.3 and R.sup.4 are combined to each other either directly or as interrupted by a hetero-atom selected from the group consisting of nitrogen, oxygen and sulfur to form a five- or six-membered ring); R.sup.2 means a bond or a lower alkylene group; L.sup.1 and L.sup.2 are the same or different and each is lower alkyl or L.sup.1 and L.sup.2 are combined to form an alkylene group, provided that when R.sup.1 is other than alkyl, L.sup.1 and L.sup.2 may further be hydrogen, respectively] are novel compounds and useful as, for example, remedies for diabetes, hyperlipemia and so on of mammals including human beings.

Abstract: The present specification provides novel analogs of khellin. These analogs are all useful as antiatherosclerotic agents. Particularly, the present specification provides 4-methoxy, 9-methoxy, or 4,9-dimethoxy-6,7-dihydro-7,7-disubstituted-5H-furo[3,2-g][1]benzopyran-5- ones.

Abstract: Derivatives of 4-thiazolidinecarboxylic acid which have the general formula ##STR1## are useful in compositions as antihypertensive agents.

Abstract: To separate the racemate (R,S)-cysteine, the racemate is condensed in an inert solvent with an enantiomerically enantiomeric monosaccharide of the group of aldoses having 4 to 7 carbon atoms to form the corresponding 2-substituted thiazolidin-4-carboxylic acid and the mixture of diastereomers obtained separated from each other. Subsequently, the isolated unitary diastereomers are reacted in an inert solvent with a carbonyl reagent to split the ring and the enantiomerically pure cysteine in each case is isolated as such or as the corresponding cystine.

Abstract: Compounds of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein m is 0 to 3;n is 1 to 5;R.sub.1 is hydrogen, or C.sub.1-6 alkyl;R.sub.2 is hydrogen, C.sub.1-4 alkyl, --(CH.sub.2).sub.p --NH.sub.2wherein p is 1 to 4, or --NHCOR, wherein R.sub.5 is C.sub.1-4 alkyl;R.sub.3 is hydrogen or C.sub.1-6 alkyl;R.sub.4 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or CF.sub.3 ; and X is CH.sub.2 or S.having useful pharmacological activity, compositions containing them, and a process for their preparation.

Abstract: This invention relates to the new thiazolidine and pyrrolidine compounds represented by the following general formula ##STR1## wherein p1 Q.sup.1 and Q.sup.2 are methylene or sulfur atom; Z is alkylene containing 1 to 3 carbon atoms;R.sup.1 is hydrogen, alkyl, aryl or heterocycle;R.sup.2 is hydrogen, alkyl, acyl, aryl, heterocycle or mercapto radical;R.sup.3 is hydrogen or alkyl;R.sup.4 is hydrogen, alkyl, aryl, pyrroridine ring formed with R.sup.3, or thiazolidine ring formed with R.sup.3 ;R.sup.5 is hydroxy or amino, which may be substituted by alkyl or aryl.The compounds of this invention are synthesized by the condensation of sulfur-containing acyl thiazolidine carboxylic acid or sulfur-containing acyl pyrrolidine carboxylic acid with amino acid.The compounds of this invention are useful for antihypertensive agent.

Abstract: This invention relates to an antihypertensive agent comprising N-(mercaptoacyl)amino acid and probenecid.The concomitant effect of probenecid and N-(mercaptoacyl)amino acid was observed to reduce the effective dose of N-(mercaptoacyl)amino acid and to prolong the duration time of the effect.

Abstract: The invention relates to novel 7-acylamino-3-vinylcephalosporanic acid derivatives of antimicrobial activity, and to methods of preparation thereof from novel intermediate compounds of the formula: ##STR1## in which R.sub.C is amino or a group of the formula: ##STR2## wherein R.sup.8 is aryl,A.sup.12 is lower alkylene having a group of the formula: .dbd.N.about.OR.sup.4, wherein R.sup.4 is hydrogen, cyclo(lower) alkenyl, lower alkynyl, lower alkenyl, lower alkenyl substituted by carboxy or a protected carboxy group, lower alkyl, or lower alkyl substituted by one or more substituent(s) selected from carboxy, a protected carboxy group, amino, a protected amino group, cyano, phosphono, a protected phosphono group and a heterocyclic group which may have suitable substituent(s),R.sup.a is a protected amino group,R.sup.b is a protected carboxy group,R.sup.c and R.sup.d are combined to form oxo or a protected oxo group, and X.sup.1 is halogen, andR.sup.

Abstract: Derivatives of 4-thiazolidinecarboxylic acid which have the general formula ##STR1## are useful in compositions as antihypertensive agents.

Abstract: The novel compounds of the formula I are useful selective herbicides for postemergence application in crops of cereals, maize and rice.In formula I, ##STR1## A is an unsubstituted or substituted amino group, Q is a C.sub.2 -C.sub.6 alkylene bridge, Y is an oxygen or sulfur atom or an unsubstituted or substituted nitrogen atom, and Z is an unsubstituted or substituted phenyl, naphthyl or heterocyclic radical, which phenyl radical, containing the bridge member Y, can additionally carry one to four further substituents.

Abstract: Disulfide compounds which have the general formula ##STR1## and salts thereof used for reducing blood pressure and for preventing or relieving diabetic complications, processes for manufacturing thereof, compositions comprising them and pharmaceutically acceptable excipients, and administering methods are mentioned.

Abstract: Compounds of the general formula I ##STR1## where B.sup.2 and B.sup.2 independently of one another are hydrogen, C.sub.1 -C.sub.6 -alkyl which may or may not be interrupted by oxygen or sulfur and is unsubstituted by hydroxyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylmercapto, cyano, phenylmercapto (which is unsubstituted by chorine or methyl), unsubstituted or substituted carbamoyl or a carboxylic acid ester group, benzyl or phenylethyl which are unsubstituted or substituted in the ring by chlorine, bromine, methyl, ethyl, methoxy or ethoxy, phenyl which is unsubstituted or substituted by chlorine, bromine, hydroxyl, methoxy, ethoxy, methyl, C.sub.1 -C.sub.4 -alkylmercapto, C.sub.1 -C.sub.4 -alkanoylamino or amino, unsubstituted or substituted carbamoyl or a carboxylic acid ester group,B.sup.2 may in addition be cyano, C.sub.2 -C.sub.4 -alkanoyl, benzoyl which is unsubstituted or substituted by chlorine, methyl, methoxy or ethoxy, C.sub.1 -C.sub.

Abstract: The invention relates to urea compounds which are useful as antihypertensives.

Abstract: A novel thiazolidine derivative having the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring selected from the group consisting of morpholino, piperazino, piperidino and pyrrolidino, or said heterocyclic ring substituted with 1 or 2 methyl groups, and the pharmaceutically acceptable salts thereof are useful immunomodulators.

Abstract: Derivatives of 4-thiazolidinecarboxylic acid which have the general formula ##STR1## are useful in compositions as antihypertensive agents.

Abstract: There are disclosed substituted phosphonamides and related compounds which are useful as converting enzyme inhibitors and as antihypertensives.

Abstract: This disclosure describes novel [4R]-3-(.omega.-aroylpropionyl)-4-thiazolidinecarboxylic acids and esters and the cationic salts thereof which are useful as hypotensive agents in mammals.

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: A process is disclosed wherein an optically active N-mercaptoalkanoylamino acid is prepared by(1) reacting an optically active .beta.-hydroxyalkanoic acid, with a halogenating reagent to prepare an optically active .beta.-haloalkanoyl halide(2) reacting the .beta.-haloalkanoyl halide with an amino acid to produce an optically active N-.beta.-haloalkanoylamino acid and(3) reacting the N-.beta.-haloalkanoylamino acid with a reagent capable of converting the halogen into the thiol group, the configuration of the formulas (II), (III), (IV), (V), and (VI) being retained in all the optically active compounds throughout the process to prepare the compound represented by formula (I). The product of the present invention, for example, N-(3-mercapto-2-D-methylpropanoyl)-L-proline inhibits the enzymatic conversion of angiotensin I into angiotensin II and therefore is useful for relieving angiotensin-related hypertension.

Abstract: Novel antibacterially-active esters of antibiotic nodusmicin. Activity is demonstrated against Staphylococcus aureus, Streptococcus pyogenes, and Sarcina lutea. Thus, these esters can be used in various known environments, using well-known procedures, to eradicate or control susceptible microbes.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids, and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: Novel antibiotic U-61,732 producible in a fermentation under controlled conditions using a biologically pure culture of the microorganism Saccharopolyspora hirsuta strain 367, NRRL 12045. This antibiotic is active against gram-positive bacteria, for example, Staphylococcus aureus. Also disclosed are the 11-acyl esters of U-61,732. Thus, these compounds can be used in various environments to eradicate or control such bacteria.

Abstract: Disulfide compounds which have the general formula ##STR1## and salts thereof used for reducing blood pressure and for preventing or relieving diabetic complications, processes for manufacturing thereof, compositions comprising them and pharmaceutically acceptable excipients, and administering methods are mentioned.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)oxy]alkanoi c and cycloalkanoic acid and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: These compounds have been found to be effective in reducing herbicidal injury to direct-seeded rice caused by 2-chloro-2',6'-diethyl-N-(butoxymethyl)acetanilide.

Abstract: Compounds having the formula ##STR1## wherein: R.sub.1 is hydrogen, alkyl, aryl or arylalkyl;R.sub.2 is hydrogen and R.sub.3 is hydrogen, hydroxy, alkoxy or halogen, or together R.sub.2 and R.sub.3 can be .dbd.Q or --X--(CH.sub.2).sub.t --X-- wherein X is oxygen or sulfur and t is 2 or 3;R.sub.4 is hydrogen or alkyl;R.sub.5 is hydrogen, alkyl or trifluoromethyl;R.sub.6 is alkyl of 1 to 20 carbon atoms, aryl, arylalkyl or a 5- or 6-membered heterocyclic group having 1 to 2 nitrogen, sulfur or oxygen atoms in the ring;R.sub.7 is aryl;m is 0, 1 or 2; andn is 1 or 2have useful hypotensive activity.

Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of a cyclic polyether compound and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.

Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of an alkylene oxide derivative and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)-oxy]alkano ic and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: There are provided compounds of the formula: ##STR1## wherein R is a heteroaroyl group containing a nitrogen, sulfur or oxygen atom which may be substituted with a lower alkyl group, an aralkyl group, an acyl group or a halogen atom; or a cycloalkanoyl group which may be substituted with a lower alkyl group, a lower alkenyl group, a halogen atom, a halogeno-lower alkenyl group, a phenyl group, a halogenophenyl group, a lower alkoxyphenyl group, a lower alkylphenyl group, a formyl group, a hydroxy group, an amino group, a carboxyl group, an aminomethyl group or an oxo group, its non toxic salt and a process for producing them. These compounds are useful as antitumor agents and immunosuppressants.

Abstract: The invention relates to new phosphoryl aminoacid derivatives and related compounds which are useful as antihypertensives.

Abstract: The invention relates to the testing of humans or other animals, such as horses, cattle or dogs, for allergic reaction or hypersensitivity to penicillins. The tests can be used both to predict and to diagnose allergy. The invention comprises new materials for use in minor determinant mixture (MDM) compositions and lyophilized, storage-stable MDM compositions and novel test methods employing such materials.The new MDM materials are N-penicilloyl amines of an aliphatic amine or .alpha.-aminoacid having the following molecular structure: ##STR1## wherein: R.sub.1 =a side chain which defines the type of penicillin--e.g., where R.sub.1 = ##STR2## the new material is a derivative of benzylpenicillin; and R.sub.2 is an alkyl group of C.sub.2 -C.sub.6 length, preferably ethyl or propyl, or an aminoacid residue as described herein.

Abstract: The invention relates to novel [(5,6,9a-substituted-3-oxo-1,2,9,9a-tetrahydro-3H-fluoren-7-yl)-oxy]alkano ic and cycloalkanoic acids and their analogs, esters, salts and derivatives. These compounds are synthesized by methods selected from a number of synthetic routes depending on the particular structure, choice of intermediate or preferred reaction sequence. The compounds are useful in the treatment and prevention of injury to the brain and spinal chord due to accidents, ischemic stroke and hydrocephalus; compositions for such uses are also disclosed.

Abstract: This disclosure describes novel 4-[(monosubstituted-alkyl)amino]benzoic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.

Abstract: Hydroxamic acid derivatives of certain mercaptoacyl amino acids inhibit the conversion of angiotensin I to angiotensin II in mammals and are useful for the treatment of hypertension.

Abstract: 2-Substituted-N-(3-substituted phenyl)thiazolidine-, tetrahydro-2H-1,3-thiazine-, and benzothiazoline-3-carbothioamides, useful as insecticides.

Abstract: Compounds having the formula ##STR1## wherein: R.sub.1 is hydrogen, alkyl, aryl or arylalkyl;R.sub.2 is hydrogen and R.sub.3 is hydrogen, hydroxy, alkoxy or halogen, or together R.sub.2 and R.sub.3 can be .dbd.O or --X--(CH.sub.2).sub.t --X-- wherein X is oxygen or sulfur and t is 2 or 3;R.sub.4 is hydrogen or alkyl;R.sub.5 is hydrogen, alkyl or trifluoromethyl;R.sub.6 is alkyl of 1 to 20 carbon atoms, aryl, arylalkyl or a 5- or 6-membered heterocyclic group having 1 or 2 nitrogen, sulfur or oxygen atoms in the ring;R.sub.7 is aryl;m is 0, 1 or 2; andn is 1 or 2have useful hypotensive activity.

Abstract: New substituted derivatives of thiazolidine-, thiazane and related carboxylic acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.

Abstract: Pyrazole derivatives of the formula ##STR1## wherein R.sup.1 is H or Cl; R.sup.2 is 1-methyl-4-piperidyloxy-carbonyl, 2-(4-phenylpiperazino)-ethoxycarbonyl, benzoxazol-2-yl, benzthiazol-2-yl, tetrazol-5-yl or 3-R.sup.3 -4-R.sup.4 -thiazolidin-2-yl; R.sup.3 is H, alkanoyl of 1-7 carbon atoms or benzoyl; and R.sup.4 is H or COOH,or a physiologically acceptable salt thereof;possess valuable pharmacological activities.

Abstract: Acylated phenylaminotetrahydro-2-furanones of the formula I disclosed herein, which have a systemic action, are suggested as novel microbicides. They can be used in the form of pesticidal compositions in particular for combating phytopathogenic fungi, or for preventing fungus infections on cultivated plants.

Abstract: This disclosure describes novel 4-[(carboxyl- and sulfamyl-substituted alkyl)amino]benzoic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.

Abstract: The invention relates to the testing of humans or other animals, such as horses, cattle or dogs, for allergic reaction or hypersensitivity to penicillins. The tests can be used both to predict and to diagnose allergy. The invention comprises new penicilloyl-polylysine (PPL) preparations, new materials for use in minor determinant mixture (MDM) compositions and novel test methods employing such materials.The new PPL preparations comprise homogeneous, high purity, maximally coupled, .alpha.-diastereoisomeric, penicilloyl conjugates of low molecular weight PPLs. The PPL materials of the invention have the molecular structure in accordance with the following generic formula: ##STR1## wherein: R is selected from the group consisting of H and penicilloyl groups or similar groups derived from cephaolosporins or other .beta.-lactam antibiotics; andn is an integer of from 4 to 10,at least about 66% and up to 100% of the R groups are other than hydrogen.

Abstract: This disclosure describes novel 4-(aralkyl- and heteroarylalkylamino)phenyl compounds useful as hypolipidemic and antiatherosclerotic agents.

Abstract: Monocyclic .beta.-lactam antibiotics of the formula ##STR1## wherein R is amino or acylamino, e.g., phenylacetylamino, phenylglycylamino and 2-[4-(3-amino-3-carboxypropoxy)phenyl]-2-hydroximinoacetylamino; R.sub.1 is H or ester forming group; R.sub.2 is H, --OCH.sub.3, --SCH.sub.3, or --CH.sub.3 ; and R.sub.3 is H or acetoxy; are useful antibacterials for controlling .beta.-lactamase producing gram-negative bacteria and other pathogens. Intermediates useful in the preparation of the antibiotics and a novel process for preparing 4.alpha.-acetoxy substituted azetidin-2-ones are provided.

Abstract: 2,4-Disubstituted-5-thiazolecarboxylic acids and derivatives thereof have been found to reduce herbicidal injury of corn, rice and sorghum plants due to the application thereto of acetamide herbicides.

Abstract: Hypolipidemic and anti-atherosclerotic 2- or 3-(monosubstituted-amino) phenyl compounds of the formulae: ##STR1## wherein R.sub.1 is a saturated or unsaturated hydrocarbon radical of 8-19 carbon atoms which may be branched or unbranched and which may contain one or more radicals selected from the group consisting of saturated or unsaturated cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl; J is ##STR2## wherein Z is inter alia hydrogen, loweralkyl, hydroxy, loweralkoxy and loweralkoxyalkoxy, or J is carboxyloweralkyl, carboxyloweralkenyl, carboxyloweralkynyl, carboalkoxyloweralkyl, carboalkoxyloweralkenyl or carboalkoxyloweralkynyl.