Abstract: Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.

Abstract: Certain novel aryl sulfonyl fluorides, their preparation, and their use in inhibiting serine proteases with chymotrypsin-like and elastase-like specificity.

Abstract: Compounds having the formula ##STR1## in which R is hydrogen, cyano or --COOR.sub.2 ; R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and Z is ##STR2## in which A is halogen, B is halogen or hydrogen and Y is nitrogen or --CH--, are herbicides.

Abstract: A method for converting ether groups such as alkyl or aryl ether groups including hydroquinone ether groups to hydroxyl groups and ester groups such as alkyl or aryl ester groups to carboxylic acid groups which comprises reacting a compound including at least one ether and/or ester group with a 2-halo-1,3,2-benzodioxaborole to form an intermediate and hydrolyzing the intermediate such as by quenching it into water to form the desired final product.

Abstract: This invention relates to dihydropyridazinone compounds having a cyclopropylmethoxyethyl group in the 6-substituent. These compounds are vasodilators and .beta.-adrenoceptor antagonists. A particular compound of the invention is 6-[4-[3-[2-hydroxy-3-[4-(2-(cyclopropylmethoxy) ethyl)phenoxy]propylamino]propionamido]phenyl]-5-methyl-4,5-dihydro-3 (2H)-pyridazinone.

Abstract: The synthesis of 5,6-dioxy substituted quinazolinediones is described. The novel quinazolinediones are useful as cardiotonic agents.

Abstract: A glycinamide derivative of the general formula I: ##STR1## wherein: R is a linear or ramified alkyl group C.sub.5 -C.sub.18, a linear or ramified alkenyl group C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9, C.sub.10, C.sub.11, C.sub.12, C.sub.13, C.sub.14, C.sub.15, C.sub.16, C.sub.17 or C.sub.18, a linear or ramified alkynyl group C.sub.4 -C.sub.10, a linear or ramified acyl group C.sub.4 -C.sub.18, a linear or ramified alkyl group C.sub.1 -C.sub.10, substituted by a phenoxy group, by a hydroxy radical, by an acetoxy radical, by a carboxy radical, by a linear or ramified alkoxycarbonyl group C.sub.1 -C.sub.4, by a carbonyl radical, by a carboxaldehyde group, by an acetal or cetal group, by one or more phenyl groups, by one or more phenyl groups substituted by a halogen atom such as fluorine, chlorine or bromine,R.sub.1 represents hydrogen, a linear or ramified alkyl group C.sub.1, C.sub.2, C.sub.3, C.sub.4, C.sub.5, C.sub.6, C.sub.7, C.sub.8, C.sub.9 or C.sub.10, a linear or ramified acyl group C.sub.1 -C.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: Derivatives having the general formula: ##STR1## in which the various radicals A,B,X,R.sub.1, R.sub.2, R.sub.3 and n have indicated definitions. These compounds have in particular enkephalinase-inhibiting, antalgic, antidepressive, antidiarrhea and hypotensive activities.

Abstract: The present invention relates to an improved process for the manufacture of (3S)-3,4-trans-disubstituted azetidinones of the formula ##STR1## in which R.sub.1 represents hydrogen or lower alkyl,R.sub.2 represents hydrogen or a hydroxy-protecting group,Y represents the group --S(.dbd.O)--R.sub.3 or --S(.dbd.O).sub.2 --R.sub.3 wherein R.sub.3 represents an organic radical bonded to the sulphur atom by a carbon atom that is not bonded to hydrogen, or the group --C(.dbd.O)--O--R.sub.3 ' wherein R.sub.3 ' represents an organic radical bonded to the oxygen atom of the carboxy group by a carbon atom that is not bonded to hydrogen, or a carboxy-protecting group, andR.sub.4 represents hydrogen or an amino-protecting group R.sub.4 '.The process according to the invention is carried out under particularly favorable reaction conditions and yields compounds (I) in particularly high yields.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl- lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

Abstract: This invention relates to herbicidal quinoxalinyloxy ethers, herbicidal compositions containing said ethers, and methods of using said compounds as herbicides.

Abstract: A method for the treatment or prophylaxis of cardiac disorders in a mammal, comprising administering to such mammal a short-acting .beta.-blocking compound of the formula: ##STR1## wherein X is an ester-containing group; R may be lower alkyl, aralkyl or an ester-containing group; R.sub.1 may be lower alkyl; and Ar may be substituted or unsubstituted aromatic; or a pharmaceutically acceptable salt thereof. Novel compounds possessing short acting .beta.-adrenergic blocking activity are also disclosed.

Abstract: A compound of formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl;R.sup.2 is hydrogen or halogen;R.sup.3 is hydrogen or methyl;R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H or an ester or amide derivative thereof, O(CH.sub.2).sub.b M or --CO.sub.2 H or an ester or amide derivative thereofwhereina is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring; R.sup.5 is C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted by carboxy or esters and amides thereof; or phenyl optionally substituted by C.sub.1-6 alkyl, halogen, alkoxy or trifluoromethyl;R.sup.8 is hydrogen or C.sub.1-6 alkyl or R.sup.8 together withR.sup.5 form a carbocyclic ring; andn is 1 or 2.Processes for preparing these compounds and their use in therapy is also described.

Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl,R.sup.2 is hydrogen or halogen,R.sup.3 is hydrogen or methyl.R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H, --O(CH.sub.2).sub.b M, --CO.sub.2 H or an esteror amide derivative thereof in whicha is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## in which R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring, and n is 1 or 2; a process for preparing such a compound and its use in medicine and agriculture.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: The invention relates to compounds of the general formula (X) ##STR1## wherein R is as a removable protecting substituent of the amido group a phenyl group or a benzyl group substituted by one or more alkoxy group(s) having 1-4 carbon atoms andR.sup.1 stands for a hydrogen atom or an alkyl group having 1-4 carbon atoms and a process for the preparation thereof.The compounds of the general formula (X) can be prepared from the starting materials of the general formula (V), wherein R and R.sup.1 are as stated above and Z is an alkyl group having 1-4 carbon atoms.The compounds of the general formula (X) are useful pharmaceutical intermediates which can be used in the preparation of known antibiotics (e.g. Thienamycin and PS-5).

Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.

Abstract: There are prepared compounds of the formula: ##STR1## wherein X is the group >C.dbd.O or >CH(OH), Y is the group ##STR2## R.sub.2 is hydrogen or C.sub.1 to C.sub.6 alkyl, R.sub.3 is hydrogen or a hydroxy group and R.sub.1 is the adamantyl group or a saturated or single unsaturated C.sub.3 to C.sub.16 cycloalkyl group where the C.sub.3 to C.sub.16 cycloalkyl group can be substituted by a C.sub.1 -C.sub.4 alkyl group or a halogen atom and their salts. The compounds are useful in dilating the peripheral blood vessels and in lowering blood pressure.

Abstract: A process for producing a compound of the formula ##STR1## wherein A is aryl or alkyl, R.sub.1 is an aromatic radical and R.sub.2 is hydrogen, alkyl, aryl, cyano, --COOalkyl or --COOaryl, which process comprises reacting 1 mol of an aromatic nitrile of the formula R.sub.1 --CN (II) with 1 mol of an acetic ester of the formula (X)(R.sub.2)CH--COOA (III) in which X is halogen, in the presence of zinc, in an inert organic solvent and at a temperature of less than 80.degree. C.; hydrolyzing in an alkaline medium the formed reaction product; and then isolating the compound of the formula I.The compounds of the formula I are valuable intermediates for producing heterocyclic compounds.

Abstract: The invention relates to compounds and salts of compounds which are diaminopimelyl peptides, N-acetoxypropionyl or N-t-butoxycarbonyl-amino-acid - (.alpha.-OBzl) glutamic acid peptides or N-acylated derivatives of (.alpha.-OBzl) glytamic acid or of (.alpha.-OBzl) aminoadipic acid.The compounds and their salts are starting materials for the preparation of pharmacologically active peptides.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: New acyl derivatives of p-aminophenol and esters of same useful as pharmacologically active ingredients and process for their preparation.

Abstract: N-substituted amino acids are described which when coupled with 1,2,3,4-tetrahydroisoquinolines result in substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids as anti-hypertensive agents. The novel intermediates are in turn prepared by reacting an amino acid such as alanine with 2-bromo-4-phenyl butanoic acid or an ester thereof.

Abstract: The present invention consists of chelating agents for the treatment of iron overload and methods of using these agents in mammals such as mice and rats. These agents or compositions comprise diesters of dicarboxylic acids, which are phenolic derived and otherwise resemble ethylene and propylenediamine diacetic acids.The acids are known as: HBED [N,N'-bis(2-hydroxybenzyl)ethylenediamine N,N-diacetic acid]; EHPG [ethylenediamine N,N'-bis(2-hydroxyphenylacetic acid)]; HBPD [N,N'- bis(2-hydoxybenzyl)propylenediamine-N,N'-diacetic acid]; HBHPD [N,N'- bis(2-hydroxybenzyl)-2-hydroxy-1,3-propylenediamine-N,N'-diacetic acid].Mineral acid addition salts are also included in the spirit of this invention. Such salts as sulfuric, hydrochloric and nitric may be utilized.In activity it has been found that the odd-numbered carbon atom esters, such a dimethyl and dipentyl, specially of HBED, are of highest activity, as well as the dipentyl ester of the HBPD.

Abstract: The present specification provides novel analogs of carbacyclin (CBA.sub.2), 6a-carba-prostacyclin (6a-carba-PGI.sub.2), which have pronounced prostacyclin-like pharmacological activity, e.g., as platelet anti-aggregatory agents. Specifically the novel chemical analogs of CBA.sub.2 are those substituted by fluoro (C-5), alkyl (C-9), interphenylene (C-5), methano (C-6a,9), and an additional (olefinic) valence bond (C-6a,9). Further provided are benzindene analogs of CBA.sub.2 and substituted forms thereof, i.e., 9-deoxy-2', 9-methano (or 2', 9-methano)-3-oxa-4,5,6-trinor-3,7-(1',3'-interphenylene)-PGF.sub.1 compounds. Also provided are a variety of novel chemical intermediates, e.g., substituted bicyclo[3.3.0]octane intermediates, and chemical process utilizing such intermediates which are useful in the preparation of the novel CBA.sub.2 analogs.

Abstract: Acyloxyketone substituted imino and amino acids of the formula ##STR1## are disclosed. These compounds are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.

Abstract: There is disclosed a polyprenylcarboxylic acid amide of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl group, R.sup.2 represents a hydrogen atom or a group of the formula: --COOR.sup.4 in which R.sup.4 represents a lower alkyl group, R.sup.3 represents a hydrogen atom or an OH group and n represents an integer of 1 to 6.

Abstract: Herbicidal and fungicidal compounds of the formula ##STR1## wherein R.sup.1 is (a) a phenyl group optionally substituted by one or more halogen atoms, cyano groups, alkoxy groups, methylene- or ethylene-dioxy groups, alkyl groups, or haloalkyl groups (e.g. trifluoromethyl groups); or (b) a heteroaromatic group optionally substituted by one or more alkyl groups, haloalkyl groups or halogen atoms X is a 5-membered heteroaromatic radical linked by a ring nitrogen atom to the carbon atom bearing Y, and optionally substituted by one or more alkyl groups, and Y is a CN group; a --CSNH.sub.2 group; a --CO.sub.2 R.sup.4 group wherein R.sup.4 is an esterifying radical, for example an alkyl radical; or an amide group --CONR.sup.5 R.sup.6 wherein each of R.sup.5 and R.sup.6 may be a hydrogen atom or an alkyl radical (e.g. an alkyl radical of 1 to 6 carbon atoms).

Abstract: 3-Amino-4-substituted phenoxy alkanoic (alkenoic) acid esters, derivatives thereof, and the use thereof for the control of weeds.

Abstract: Compounds of the general formula ##STR1## wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C.sub.1-4 alkoxycarbonyl, amido, C.sub.1-4 alkylamido, C.sub.1-4 alkoxy, C.sub.2-4 alkenyl, cyano, aminomethyl, or methylsulphonyl; Y is a group of formula ##STR2## where R.sup.1 is hydrogen or methyl; R.sup.2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR.sup.3 or --NR.sup.4 R.sup.5 where R.sup.3, R.sup.4 and R.sup.5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R.sup.3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, e.g.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: Novel compounds of the following formula: ##STR1##

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: For the preparation of polyfunctional organic compounds having at least one functional group of medium nucleophilic character selectively blocked by a tertiary butyl group, the corresponding unblocked compound is dissolved in a solution of concentrated sulfuric acid in an organic ether, and excess liquid isobutene is added to the solution at a temperature of not more than 5.degree. C.

Abstract: New 3-N-acyl derivatives of 3-amino-2-hydroxy-4-phenylbutanoic acid are provided, which exhibit analgesic activity and are affective to enhance the morphine analgesia.

Abstract: Disclosed is a process for the stereocontrolled total synthesis of thienamycin from acetone dicarboxylate via intermediate II: ##STR1## wherein R is a readily removable carboxyl protecting group.

Abstract: A short-acting .beta.-blocking compound of the formula ##STR1## wherein Ar may be substituted or unsubstituted aromatic, Y may be a straight or branched carbon chain or aralkyl, R may be lower alkyl, lower alkenyl, lower alkynyl, aryl or aralkyl, and x is an integer from 1 to about 3; or a pharmaceutically acceptable salt thereof.

Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.

Abstract: Fluorinated alkenylene diamine compounds are inhibitors of ornithine decarboxylase enzyme in vivo and have the following formula: ##STR1## wherein: R.sub.a represents hydrogen or R.sub.2, where R.sub.2 is as defined below;R.sub.b represents hydrogen or, when R.sub.a is hydrogen, R.sub.2, where R.sub.2 is as defined below;R.sub.c represents hydrogen or --COR.sub.3, where R.sub.3 is as defined below;R.sub.1 represents hydrogen or C.sub.1 --C.sub.6 alkyl;each R.sub.2, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from a carboxy moiety of an L-aminocarboxylic acid;R.sub.3 represents hydroxy, or, when R.sub.a and R.sub.b are both hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;R.sub.4 and R.sub.

Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: wherein Y is ClCH.sub.2, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR1## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.

Abstract: Diphenyl ethers of the formula ##STR1## where Z.sup.1, Z.sup.2 and Z.sup.3 independently of one another are each hyrogen, halogen, nitro, cyano, carboxyl, alkyl of 1 to 4 carbon atoms, or haloalkyl, alkoxy, haloalkoxy, alkylmercapto, haloalkylmercapto, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or haloalkylsulfonyl where alkyl is in each case of 1 to 4 carbon atoms, Y is hydrogen, halogen, cyano or nitro and Q is --CO--NA--OR.sup.1, where A is hydrogen, alkyl of 1 to 4 carbon atoms, a metal ion or an unsubstituted or substituted ammonium ion and R.sup.1 is carboxyalkyl, alkoxycarbonylalkyl or carbamylalkyl of not more than 10 carbon atoms, herbicides which contain these diphenyl ethers as active ingredients, and methods of controlling undesirable plant growth using these active ingredients.

Abstract: Compounds of the general formula ##STR1## wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C.sub.1-4 alkoxycarbonyl, amido, C.sub.1-4 alkylamido C.sub.1-4 alkoxy, C.sub.2-4 alkenyl, cyano, aminomethyl or methylsulphonyl; R.sup.a and R.sup.b, which may be the same or different, each represents a hydrogen or alkali metal (e.g. sodium or lithium) atom or a C.sub.1-4 (e.g. ethyl) group; m is 0 or 1; Y is a group of formula:--NH--CH.sub.2 --CO--or a group of formula: ##STR2## where R.sup.1 is hydrogen or methyl;R.sup.2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; andZ is --OR.sup.3 or --NR.sup.4 R.sup.5 where R.sup.3, R.sup.4 and R.sup.5 are each hydrogen or alkyl of 1 to 4 carbon atoms (i.e. methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, or t-butyl) and R.sup.

Abstract: Phenylacetic acid amide compounds of the formula ##STR1## in which R.sub.1 is hydrogen, lower alkyl, lower alkoxy, halogen having an atomic number of not more than 35 or trifluoromethyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen having an atomic number of not more than 35 or trifluoromethyl, R.sub.3 is hydrogen, lower alkyl, lower alkoxy or halogen having an atomic number of not more than 35 and R.sub.4 is hydrogen, lower alkyl, lower alkoxy or halogen having an atomic number of not more than 35, and in which R.sub.5 is a radical of aliphatic character containing the group R.sub.6, R.sub.6 and R.sub.7 are each hydrogen or together are a divalent aliphatic radical and the group of the formula --C(.dbd.O)--R.sub.8 (Ia) is a carboxyl group, which can be functionally modified, and their salts are useful as anti-inflammatory agents.

Abstract: Phenylacetic acid amide compounds of the formula ##STR1## in which R.sub.1 is hydrogen, lower alkyl, lower alkoxy, halogen having an atomic number of not more than 35 or trifluoromethyl, R.sub.2 is hydrogen, lower alkyl, lower alkoxy, halogen having an atomic number of not more than 35 or trifluoromethyl, R.sub.3 is hydrogen, lower alkyl, lower alkoxy or halogen having an atomic number of not more than 35 and R.sub.4 is hydrogen, lower alkyl, lower alkoxy or halogen having an atomic number of not more than 35, and in which R.sub.5 is a radical of aliphatic character containing the group R.sub.6, R.sub.6 and R.sub.7 are each hydrogen or together are a divalent aliphatic radical and the group of the formula --C(.dbd.O)--R.sub.8 (Ia) is a carboxyl group, which can be functionally modified, and their salts are useful as anti-inflammatory agents.

Abstract: The present specification provides novel analogs of carbacyclin (CBA.sub.2), 6a-carba-prostacyclin (6a-carba-PGI.sub.2), which have pronounced prostacyclin-like pharmacological activity, e.g., as platelet antiaggregatory agents. Specifically the novel chemical analogs of CBA.sub.2 are those substituted by fluoro (C-5), alkyl (C-9), interphenylene (C-5), and methano (C-6a,9). Further provided are benzindene analogs of CBA.sub.2 and substituted forms thereof, i.e., 9-deoxy-2',9-methano (or 2',9-metheno)-3-oxa-4,5,6-trinor-3,7-(1',3'-interphenylene)-PGF.sub.1 compounds. Also provided are a variety of novel chemical intermediates, e.g., substituted bicyclo[3.3.0]octane intermediates, and chemical process utilizing such intermediates which are useful in the preparation of the novel CBA.sub.2 analogs.

Abstract: The invention relates to new 16-amino-18,19,20-trinor-prostaglandin derivatives of general formula I, having at C-17 a substituted or unsubstituted phenyl group, wherein C-15 and C-16 may have either S or R configuration, Y stands for a hydrogen atom or a lower alkyl group, W stands for a hydrogen atom, halogen atom, hydroxy group, lower alkyl or alkoxy group, and their acid addition salts. These compounds can be prepared by removing the ester group and the p-nitrobenzyloxycarbonyl protective group of a 9.alpha.,11.alpha.

Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.

Abstract: A novel derivative of dihydroxybenzoic acid represented by the formula (I) ##STR1## wherein R represents ##STR2## or a salt or an ester thereof which has specific pharmacological activities, a method for preparing thereof and a pharmaceutical composition comprising thereof as an active ingredient are provided.

Abstract: A compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, an acyl group or an alkoxycarbonyl group; X.sup.1 represents an alkylene group having 3 to 6 carbon atoms, a 1,4-cyclohexylene group, or a 1,4-phenylene group, the alkylene group may be substituted by an alkyl group having 1 to 6 carbon atoms, and the 1,4-phenylene group may be substituted by 1 or 2 substituents selected from halogen atoms and alkoxy groups having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom or a hydroxyl group and R.sup.3 represents hydrogen atom, or R.sup.2 and R.sup.3 together may form an oxo group (.dbd.O), and when X.sup.1 is other than the 1,4-phenylene group, R.sup.2 represents a hydrogen atom and R.sup.3 represents a bond between the carbon atoms to which R.sup.3 is bonded and that carbon atom of X.sup.1 which is adjacent to said carbon atom; X.sup.