Abstract: Process for racemization of amino acids by use of a ketone and an organic acid such as acetic acid. In particular, a process for resolution of free .alpha.-amino acids with in situ racemization. The resolution of 4-hydroxyphenylglycine and 3,4-dihydroxyphenylglycine with 3-bromocamphor-9-sulphonic acid with in situ racemization are specifically mentioned.

Abstract: The invention relates to a process for the preparation of DL-.beta.-aryl-amino acids of the general Formula ##STR1## wherein R, R.sub.1 and R.sub.2 stand for hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro or C.sub.1-4 dialkylamino; wherebyin the case of monosubstituted derivatives R and R.sub.1 are hydrogen and R.sub.2 has the same meaning as stated above and can be attached to position 2, 3 or 4 related to the methylene group;in the case of disubstituted derivatives R is hydrogen and R.sub.1 and R.sub.2 have the same meaning as stated above and are attached to positions 2,3; 2,4; 2,5; 2,6; 3,4 or 3,5 related to the methylene group;in the case of trisubstituted derivatives R, R.sub.1 and R.sub.2 have the same meaning as stated above and are attached to positions 2,3,4; 2,3,5; 2,3,6; 3,4,5 or 3,4,6 related to the methylene group.

Abstract: The racemization of optically active aminoacids (including their N-acyl derivatives) by heating with carboxylic acids takes place particularly readily with carboxylic acids of low volatility. Only catalytic quantities of acid are needed; it is advantageous to use equimolar quantities or an excess, which serves as a diluent. A reaction mixture from an enzymatic racemate resolution can be heated directly for the purpose of racemization, after separation of the L-aminoacid and the water.

Abstract: There are described new optically active 3,4-bis-(diphenylphosphino)-pyrrolidines of the formula ##STR1## wherein Ph is a phenyl group and R is hydrogen, an alkyl group, an arylalkyl group or an acyl group, rhodium complexes containing a compound of formula (I) as its chiral ligands, said rhodium complexes having the formula[RH(en).sub.2 A].sup.+ X.sup.- (II),where (en).sub.2 is two molecules of a monoolefin or one molecule of a diolefin, A is an optically active compound of formula (I) and X.sup.- is a tetrafluoroborate, hexafluorophosphate or a perchlorate ion, and use of the rhodium complexes as catalysts for the homogeneous asymmetric hydrogenation of unsubstituted or .beta.-substituted .alpha.-acylamino-acrylic acids.

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

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: Disclosed herein is a process for producing an N-acyl-substituted or unsubstituted phenylalanine comprising hydrolyzing a 2-substituted-4-substituted or unsubstituted benzylidene-5-oxazolone with alkali, adjusting pH of the reaction solution containing its hydrolysis product with acid at 5-9 and reducing the resultant reaction solution catalytically in the presence of a palladium or platinum reducing catalyst.In accordance with the process of the present invention, time duration required for effecting the reduction can be shortened markedly in comparison with the reduction in an aqueous strong alkaline solution. Moreover, the catalyst recovered after completion of the reduction can be used repeatedly without any additional treatment and without any observed lowering in its activity. Accordingly, the reduction using the recovered catalyst may proceed in practically the same time as in the case of using a fresh catalyst.

Abstract: In the production of a .beta.-phenylserine by reacting glycine with a benzaldehyde in the presence of an alkali and treating the product with an acid, a novel process which comprises carrying out the reaction in a mixed solvent composed of water and a hydrophobic organic solvent. The presence of a phase transfer catalyst or a surface-active agent in this reaction system promotes the reaction and the .beta.-phenylserine can be obtained in a high yield.

Abstract: Disclosed herein are new aldose reductase inhibitors of the formula ##STR1## wherein n is an integer from 1 to 5 and X is a chalcogen, and methods of preparation. The derivatives are useful for treating or preventing diabetic complications.

Abstract: Process for producing hydroxyalkylaminoacetic acids having the general formula (I):R--CHOH--CHR.sub.1 --NR.sub.2 --CH.sub.2 --COOH (I)in which:R represents a hydrogen atom, a C.sub.1 -C.sub.18 -alkyl group, with straight or ramified chain, or a phenyl group possibly substituted by one or more radicals (preferably one or two) selected from the group comprising: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alcoxy or halogeno radicals;R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group;R.sub.2 represents a C.sub.1 -C.sub.18 -alkyl group or R.sub.3 --CHOH--CHR.sub.4 --group in which R.sub.3 identical to R represents a hydrogen atom or a C.sub.1 -C.sub.18 -alkyl group with straight or ramified chain, and R.sub.4 is identical to R.sub.1, according to which glyoxal is reacted hot upon a secondary hydroxylated amine having the general formula (III): ##STR1## in which R, R.sub.1 and R.sub.2 have the meaning as given above.

Abstract: (3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.

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: .alpha.-Alkylated, acyclic .alpha.-aminocarboxylic acids of the formula ##STR1## where * represents a center of asymmetry, R.sup.1 is a lower alkyl, allyl, benzyl or substituted benzyl group and R.sup.2 is a lower alkyl, methoxymethyl, lower alkylmercaptoethyl, phenyl, phenyl substituted with alkyl or alkoxy, benzyl, or benzyl substituted with alkyl, alkoxy or halo are produced by an enantio-selective plural step process from the corresponding .alpha.-aminocarboxylic acid monomethyl or monoethyl amide. A particular advantage of the new process is that there can be produced from one educt-enantiomer, i.e. from an (S)- or an (R)-.alpha.-aminocarboxylic acid, selectively depending on the reaction conditions used the two enantiomeric forms of the desired .alpha.-alkyl-.alpha.-aminocarboxylic acid.

Abstract: P-oxybenzoic acid derivatives of formula (1) ##STR1## wherein R.sup.1 is hydrogen, or straight or branched alkyl of one to four carbon atoms;n is 1 or 2;X is ##STR2## and R.sup.2 is --OH or --NHCH.sub.2 COOH; and non-toxic pharmaceutically acceptable salts thereof.The compounds exhibit a hypolipemic effect. They may be prepared by methods known in themselves from the corresponding ester or acid halide compounds, wherein optionally the secondary alcohol group may be oxidized to a keto group.

Abstract: 1-Oxo-2-phenyl-2-(2-alkylaminoethyl)-1,2,3,4-tetrahydronaphthalenes of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and are each hydrogen, halogen, trifluoromethyl, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy, R.sup.3 is C.sub.1 -C.sub.6 -alkyl and R.sup.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl or benzyl, or R.sup.3 and R.sup.4 together may furthermore be a C.sub.2 -C.sub.5 -alkylene chain, and their salts with physiologically tolerated acids, and their preparation, are described.The novel compounds are useful active compounds for treating disorders.

Abstract: A process for producing racemic or optically active threo- or erythro-3-(3,4-dihydroxyphenyl)serine which comprises phthaloylating the amine group of a racemic or optically active threo- or erythro-3-(3,4-dihydroxyphenyl)serine derivative to yield a racemic or optically active threo- or erythro-N-phthaloyl-3-(3,4-dihydroxyphenyl)serine derivative and removing the phthaloyl group from the racemic or optically active threo- or erythro-N-phthaloyl-3-(3,4-dihydroxyphenyl)-serine to yield the racemic or optically active threo- or erythro-3-(3,4-dihydroxyphenyl)serine.

Abstract: A multi-step process is described for preparing a methoxytrifluoromethylnaphthoic acid compound of formula ##STR1## from 1,5-dimethylnaphthalene and for preparing novel intermediate compounds of formula ##STR2## where X is chlorine or fluorine. Methoxytrifluoromethylnaphthoic acid is useful for preparing biologically active compounds such as naphthyl thioamide derivatives which inhibit aldose reductase activity.

Abstract: A multi-step process is described for preparing a methoxytrifluoromethylnaphthoic acid of formula ##STR1## from 1-methyl-5-naphthoic acid and for preparing novel intermediate compounds of formula ##STR2## where X is chlorine or fluorine. Methoxytrifluoromethylnaphthoic acid is useful for preparing biologically active compounds such as naphthyl thioamide derivatives which inhibit aldose reductase activity.

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: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in preparing substituted peptide compounds which possess hypotensive and analgesic activity.

Abstract: Chiral N-protected, N-substituted .alpha.-amino acids are described. These compounds are prepared by condensation of an N-protected .alpha.-amino acid with an aldehyde followed by the selective reductive cleavage of an oxazolidinone intermediate.

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

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: Novel radioactive stilbene derivatives marked with iodine 125 or 131 of the formula ##STR1## wherein each A and B are both hydrogen or together form a double bond and R is the remainder of amino acid of the formula R--NH.sub.2 or a derivative thereof possessing an iodine acceptor group and marked with iodine 125 or 131 and their preparation and antigens obtained therefrom and a process for preparing said antigens.

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: .alpha.-(S)-amino acid..alpha.-phenylethanesulfonate compounds and methods of optical resolution of .alpha.-amino acids and .alpha.-phenylethanesulfonic acids are described.

Abstract: A material having a use as a detergent in a motor fuel composition is the reaction product of an aldehyde, a phenoxy acid, and a mono- or diamine, wherein the aldehyde includes a hydrocarbon radical having from 1 to about 10 carbon atoms and the phenoxy acid has the following formula: ##STR1## wherein R is any hydrocarbon radical or oxygen-containing hydrocarbon radical of from 1 to about 36 carbon atoms with the carbon atom adjacent to the carboxylic acid functional group having at least one active hydrogen atom, and x varies from about 1 to 3. The monoamine useful in forming the reaction product has the formula: ##STR2## wherein X, X.sup.1 and X.sup.2 can be any hydrocarbon radical having from about 6 to about 36 carbon atoms, and wherein X.sup.1 and X.sup.2 can be a hydrogen atom. The diamine has the formula: ##STR3## wherein z varies from about 1 to 3, R.sup.1 is any hydrocarbon radical or oxygen substituted hydrocarbon radical having from about 6 to 36 carbon atoms and R.sup.

Abstract: Serine derivatives are synthesized by the condensation of an alkali metal salt of a glycine derivative and a carbonyl compound in the presence of a phase transfer catalyst.

Abstract: A manufacturing method is described for the preparation of optically active 1-(6-methoxy-2-naphthyl)-2-(alkoxycarbonyl)amino-1-propanone, its derivatives and their halo analogs. The optically active 1-(6-methoxy-2-naphthyl)-2-(alkoxycarbonyl)amino-1-propanone, its derivatives and their halo analogs are useful intermediates in the preparation of 2-(6-methoxy-2-naphthyl)propionic acid, which is useful as pharmaceutical, e.g. antiinflammatory, analgesic and anti-pyretic agents.

Abstract: The invention relates to crystallized 2-dimethylamino-2-parahydroxyphenyl sodium acetate, anhydrous or with 2 molecules of water. The process for preparation thereof comprises heating parahydroxy mandelic acid in dimethylformamide in the presence of a catalytic quantity of a strong acid, such reaction being followed by a sodium hydroxide neutralization. Said product is applied to the production of parahydroxybenzyl cyanide by reacting it with 2-hydroxy isobutyronitrile.

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

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

Abstract: (3-Aminopropoxy)bibenzyl derivatives are prepared and found useful as pharmaceutical agents, particularly as inhibitors of platelet aggregation.

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: A process for producing efficiently and economically without using strong acids nor strong bases, .alpha.-amino acids from .alpha.-amino acid amides by hydrolyzing .alpha.-amino acid amides in an aqueous medium in the presence of ammonia. If necessary, the resultant hydrolyzate liquid from which .alpha.-amino acid has been removed may be reused.

Abstract: Aminoacid and peptide derivatives of the formula:A--NH--R.sub.1 --CO].sub.x [NH--R.sub.2 --CO].sub.y NH--R.sub.4 --COOHin which A, R.sub.1, R.sub.2, x and y have the meanings specified in claim 1 for formula I, and R4 is a residue of an .alpha.-aminoacid which, when A is 4-allyloxy-3-chloro-phenylacetyl and x and y are 0, contains at least 2 carbon atoms, and their physiologically acceptable salts and lower alkyl ester.These compounds and 4-allyloxy-3-chloro-phenylacetylglycine have anti-inflammatory activity and pharmaceutical compositions containing them are described.

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

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: Aqueous solutions of sodium salts of .alpha.-aminocarboxylic acids practically free of foreign salts are produced by saponifying the corresponding hydantoin at a temperature between 110.degree. C. and 180.degree. C. with a mixture, in each case based on the hydantoin, of 1 equivalent of sodium hydroxide and 2 equivalents of calcium oxide or hydroxide, separating off the precipitated calcium carbonate after the end of the saponification and concentrating the aqueous sodium salt solution remaining to drive off the ammonia contained therein.

Abstract: Novel 1-fluoromethyl-substituted alkyl amines are disclosed. The novel compounds have biological activity including decarboxylase inhibition.

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: 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: (1R,cis)-Oxyimino-substituted cyclopropanecarboxylic acids are prepared via a (1R,4R,5S)-4-acetoxy-6,6-dimethyl-2-oxo-3-oxabicyclo [3.1.0]hexane intermediate.

Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.

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.