Abstract: A method for prevention or treating myocarditis, dilated cardiomyopathy and heart failure comprising administering to a patient in need of such treatment a NF-&kgr;B inhibitor in a therapeutically effective amount, wherein said NF-&kgr;B inhibitor is a benzoquinone derivative represented by the following formula (I): wherein R1, R2 and R3 are each independently a hydrogen atom, an alkyl group having 1 to 5 carbons or an alkoxy group having 1 to 5 carbons; R4 is a hydrogen atom, a hydroxymethyl group, an alkyl group, or a carboxyl group which is optionally esterified or amidated; Z is and n is an integer from 0 to 6, or its hydroquinone form, or a pharmaceutically acceptable salt thereof, is provided.

Abstract: A substituted benzoic acid derivative which is represented by the following formula (I) and has an NF-&kgr;B inhibiting action (in the formula, R3, R4 and R5 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an alkoxy group having 1 to 6 carbon(s); R9 and R10 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an acyl group having 2 to 11 carbons); R2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted heterocyclic group; and X represents a carboxyl group which may be esterified or amidated).

Abstract: Compounds useful as surface coating agents, including compounds of the formula: 1

Abstract: A cyclic compound comprising m units of formula Ia and n units of formula (Ib) joined together to form a ring, wherein Y is a divalent bridging group which may be the same or different in each unit; R0 is H, a C1-C6 alkyl or a metal or ammonium cation; R5 is H or a C1-C6 alkyl; and j is 1 or 2; R3 is hydrogen, a hydrocarbyl or a hetero-substituted hydrocarbyl group; each of R1, R2 and R4, which may be the same or different, is hydroxyl, hydrogen, hydrocarbyl or hetero-substituted hydrocarbyl, with the proviso that at least one of R1, R2, R4 is hydroxyl, and m+n is 4 to 20, m is 1-8 and n is at least 3; and with the proviso that at least one of the conditions a) to e) below is satisfied: (a) the cyclic compound comprises at least one formula (Ia) unit in the form of a carboxylate anion, (b) the caclic compound comprises at least one formula (Ia) unit in the form of an alkaline earth metal or alkali metal carboxylate salt, (c) the cyclic compound comprises at least 2 units of formula (Ia) (d) the cyclic co

Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.

Abstract: The invention disclosed herein relates to linear compounds in the form of oligomers or polymers containing unsubstituted or substituted phenol units and unsubstituted or substituted salicylic acid units. These compounds are useful as additives for lubricants and fuels. Metal salts of these compounds are useful as lubricant additives. The process for making these compounds involves reacting phenol units and salicylic acid units in an organic solvent.

Abstract: Novel molecular compounds containing carboxylic acid derivatives represented by general formula (I) or (II) as the constituent compound and exhibiting excellent performances in various technical fields including selective separation of useful substances, chemical stabilization, nonvolatilization, prolongation of release and powderization, wherein X is (CH2)n or p-phenylene; n is 0, 1, 2 or 3; R1 to R8 and R13 to R20 are each hydrogen, C1-C6 alkyl, C2-C4 alkenyl, phenyl optionally substituted with C1-C6 alkyl, halogeno or C1-C6 alkoxy; and R9 to R12 and R21 to R24 are each hydrogen, C1-C6 alkyl, C2-C4 alkenyl, C11-C12 aralkyl or an alkali metal.

Abstract: A cyclic compound comprising m units of the formula Ia.

Abstract: A cyclic compound comprising m units of the formula Ia.

Abstract: A cyclic compound comprising m units of the formula Ia. and n units of the formula (Ib) joined together to form a ring, wherein Y and y2 are divalent bridging groups which may be the same or different in each unit; Ro is H or (C1-C6) alkyl or is a metal or amnmonium cation; R5 is H or (C1-C60) alkyl or OH group; j is 1 or 2; R3 is hydrogen, a hydrocarbyl or a hetero-substituted hydrocarbyl group; each of R1, R2 and R4, which may be the same or different, is hydroxyl, hydrogen, hydrocarbyl or hetero-substituted hydrocarbyl, with the provisos that i) at least one of R1, R2, R4 is hydroxyl, and m +n is 4 to 20, m is 1-8 and n is at least 3, and ii) in formula Ia at least one OH group is in the meta or para position to the COORo group and/or at least one R5 group is OH.

Abstract: A process for preparing an alkyl phenylglycolic acid is disclosed. It follows the sequence of condensing a substituted acetaldehyde with mandelic acid to provide a 5-phenyl-1,3-dioxolan-4-one, which is condensed with an alkyl ketone or aldehyde to provide a 5-(1-hydroxyalkyl)-5-phenyl-1,3-dioxolan-4-one, which is dehydrated to a 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one. The 5-(1-alkenyl)-5-phenyl-1,3-dioxolan-4-one may be hydrolyzed and reduced to an &agr;-alkylphenylglycolic acid or the hydrolysis and reduction steps may be reversed. The process enables the production of single enantiomers of cyclohexylphenylglycolic acid (CHPGA). An analogous process for racemic CHPGA is disclosed employing racemic mandelic acid and acetone. Novel intermediates in the process are also disclosed.

Abstract: A method for treating symptoms, diseases and conditions in extra-reproductive tract tissues that are responsive to treatment with estrogen, using triarylethanes of formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; wherein R3 is an anionic substituent; m is an integer from 1 to 4; and n is an integer from 0 to 4; and wherein R2 is either H or —OH. Each of R1 and R2 can be either meta or para to its respective phenyl ethyl linkage. Compounds having the formula (I) wherein R1 is —O(CH2)mR3 or —(CH2)nR3; R3 is an anionic substituent; m is 1, 2, 3 or 4; n is 0, 1, 2, 3 or 4; R2 is H or —OH; and wherein each of R1 and R2 is independently meta or para to its respective phenyl ethyl linkage are also provided, with the proviso that R2 is not para —OH when m is 1 and R3 is —COOH.

Abstract: An oxidation free process for converting a hydroxy substituted aromatic to an aromatic diacid which comprises reacting a hydroxy substituted aromatic with excess basic salt in the presence of carbon dioxide at disproportionation/isomerization reaction conditions.

Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells.

Abstract: A series of phloroglucide derivatives are synthesized, which possess potent antibacterial activities. They include unsymmetrical phloroglucide analogs, phloroglucides attached to cephalosporins at the C-3′ position, and 7-(phloroglucidamido)cephalosporins.

Abstract: A phloroglucide derivative having the following formula: ##STR1## wherein Q is halogen; X is CH.sub.2 or C.dbd.O; Y is cephalosporin having a formula of ##STR2## wherein Ph is phenyl, Ac is acetoxy, or pharmaceutically acceptable salts thereof, and an antibacterial pharmaceutical composition derived thereof.

Abstract: A process for the preparation of optically active phenylcyclohexylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)-- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.

Abstract: A universal linker for solid-phase nucleic acid synthesis that is cleaved under conditions orthogonal to those used during the synthesis and deprotection of nucleic acids such as dsDNA or RNA fragments is disclosed. The invention includes compounds of the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of OH, OR.sub.2 and an amino functionalized support and n is an integer ranging from about 1 to about 1000 or more preferably from about 1 to about 100 or greater and R.sub.2 is an alkyl (C.sub.1-20) or greater.

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.

Abstract: An improved method for the preparation of functionalized substituted bisphenol compound is provided. In particular, there is provided a method of making a functionalized substituted bisphenol compound of the formula: ##STR1## which comprises heating a mixture comprising a 2,6-dimethylphenol and levulinic acid in the presence of an effective amount of a macroreticular ion-exchange resin, optionally with removal of the water of reaction.

Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## wherein the substituents are defined in the specification.

Abstract: The reaction product of a hydroxyaromatic compound, at least some of the units of which are hydrocarbyl-substituted, a carboxy-substituted aldehyde, and an aldehyde other than a carboxy-substituted aldehyde, provides an additive for lubricants as well as an intermediate for further reaction with amines, alcohols, or neutralization to form a salt.

Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.

Abstract: Novel benzoic acid derivatives have the formula: ##STR1## wherein --X-- represents C.sub.1 to C.sub.6 alkylene, C.sub.2 to C.sub.6 alkenylene or a divalent moiety having the structure --(CH.sub.2).sub.m --Z-- in which m is an integer from 0 to 3 and Z represents --O--, --S-- or --NH--;--Y-- represents a direct bond, C1 to C.sub.6 alkylene, C.sub.2 to C.sub.6 alkenylene or a divalent moiety having the structure --(CH.sub.2).sub.m --Z--(CH.sub.2).sub.n in which m and n are each, independently, an integer from 0 to 3 and --Z-- represents --O--, --S-- or --NH--;R represents a 5- or 6-membered carbocyclic or heterocyclic ring or a carbocyclic or heterocyclic fused ring system containing up to 10 members in the ring, which carbocyclic, heterocyclic or fused ring system may be saturated or unsaturated and may contain up to two substituents selected from lower alkyl, methoxy, halo and trifluoromethyl; andR.sup.1 and R.sup.

Abstract: Compounds having the Formula I:R.sup.1 R.sup.2 C(OR.sup.3)--Ar.sup.1 --X--Ar.sup.2 --C(Ar.sup.3).dbd.CHCO.sub.2 H Iare inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.

Abstract: New substituted phenoxyisobutyric acids and esters that can be used as medicaments and correspond to the formula: ##STR1## wherein X, A, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and Z are as defined in the description.Those compounds and their physiologically tolerable salts can be used therapeutically.

Abstract: Disclosed is a polyoxyalkylene derivative which is useful for a carboxyl group-containing polyurethane resin, can easily introduce a carboxyl group into a polyurethane resin skeleton, and has a low melting point or is in a liquid state at normal temperature. The polyoxyalkylene derivative is represented by formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or an alkyl group having from 1 to 3 carbon atoms; R.sub.2 represents an alkylene group having from 1 to 6 carbon atoms or an arylene group having from 6 to 8 carbon atoms; A represents an alkylene group having from 4 to 7 carbon atoms; B represents an alkylene group having from 2 to 6 carbon atoms; l represents from 0 to 2; m represents from 0.1 to 35; n represents from 0.1 to 50; and 0.5<(m+n)<50.

Abstract: A novel phenylalkanoic acid derivative represented by the following formula ##STR1## wherein n is an integer of 1-2, X is a halogen atom, alkoxyl group or nitro group, R is a hydrogen atom or alkyl group, and Z is a hydrogen atom or acyl group,a method for producing said derivative, a method for separating the optical isomers of said derivative from each other, as well as an anti-inflammatory drug, analgesic drug or preparation for external use each containing said derivative.

Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein: R.sup.1 and R.sup.2 are each alkyl;n is an integer of from 1 to 4;x is oxygen or --(CH.sub.2).sub.m --;m is an integer of from 1 to 3;y is oxygen or sulfur; andp is an integer of from 1 to 4.These compounds are inhibitors of COX-I and/or COX-II, and are useful for the treatment of inflammation-associated disorders.The present invention also provides pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for treating inflammation-associated disorders in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: A color developer is provided comprising a polyvalent metal salt of a salicylic derivative. The salicylic derivative is made up of ring-substituted salicylic compounds having one, two and three styrene units bonded to salicylic core where at least 25% of the salicylic derivatives are polyvalent metal salts.

Abstract: Phenyl acetylenic acetals and thioacetals and their use in the treatment of allergy, asthma, inflammation, arthritis, hyperproliferative skin disease, psoriasis or contact dermatitis are disclosed. Also disclosed are intermediates useful for producing said phenyl acetylenic acetals and thioacetals.

Abstract: Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.

Abstract: Allene compounds have the formula:(CH.sub.2 .dbd.C.dbd.CH--O).sub.n --R--(A).sub.m (I)in which R is a substituted or unsubstituted mono- or polyvalent benzene, naphthalene, anthracene, azobenzene, bisphenol or polyphenyl (containing 2 to 10 benzene rings connected in line) nucleus, or a group--Ph--R.sup.1 --Ph-- (II)(in which each group Ph is a phenylene, halophenylene, alkylphenylene, cyanophenylene or alkoxyphenylene group, and the chain R.sup.1 linking the two group Ph is a C.sub.1 -C.sub.6 aliphatic hydrocarbon or an alicyclic hydrocarbon group, the chain optionally being interrupted by one or more oxygen atoms); A is a carboxyl or sulphonyl group or a group --CH.dbd.C.dbd.CH.sub.2 ; n is an integer of from 1 to 10; m is 0, 1, 2 or 3; and the sum of m and n is equal to the valence of the group R.They may be prepared by isomerization of corresponding propargyloxy compounds.

Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.

Abstract: A color-developing sheet using, as a color developer, polyvalent-metal-modified products of salicylic acid compounds composed mainly of a 3,5-di(.alpha.-methylbenzyl)salicylic acid derivative obtained by reacting a salicylic acid ester with an .alpha.-methylbenzyl halide in the presence of an acid catalyst and hydrolyzing the reaction product.Said color-developing sheet has excellent color developability at low temperatures and gives a color of excellent water resistance.

Abstract: The invention relates to a process for the preparation of optically active .alpha.-hydroxycarboxylic acids characterised in that carbamates are first reacted in the presence of a selective base and of a chelate-forming diamine to give a carbanion complex compound, this is then dia- or enantioselectively deprotonated, then substituted with CO.sub.2 and, as a final step, the heterocyclic protective group is eliminated.

Abstract: Novel diphenyl acetic acid derivatives of the formula I are described, ##STR1## in which R is C.sub.3 -C.sub.18 -2-alkenyl, C.sub.3 -C.sub.8 -2-alkynyl or phenyl-C.sub.1 -C.sub.4 alkyl, each of which is unsubstituted or substituted by phenyl, R.sub.1 is hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl or phenyl-C.sub.1 -C.sub.4 alkyl, R.sub.2 is --OR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 is hydrogen, C.sub.1 -C.sub.18 alkyl or (--CH.sub.2 --).sub.n G, R.sub.5 and R.sub.6 independently of one another are hydrogen, C.sub.1 -C.sub.12 alkyl or phenyl-C.sub.1 -C.sub.4 alkyl, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 independently of one another are hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, with the proviso that at least one of the radicals R.sub.7, R.sub.8, R.sub.9 or R.sub.10 is hydrogen, R.sub.11 is hydrogen, C.sub.1 -C.sub.18 alkoxy, C.sub.5 -C.sub.8 cycloalkoxy, phenyl-C.sub.1 -C.sub.4 alkoxy or C.sub. 3 -C.sub.

Abstract: Nonsteroidal estrogenic triarylethylene carboxylic acids of the formula ##STR1## wherein R is (CH.sub.2).sub.m O or (CH.sub.2).sub.n, where m is an integer from 1 to 4 and n is an integer from 0 to 4, X is hydrogen or hydroxyl, Y is methyl, ethyl, chlorine, or bromine, and wherein the RCOOH and X moieties are either meta or para to the phenyl ethylene linkage. Examples of active compounds include 4-hydroxytamoxifen acid, 3-hydroxytamoxifen acid, 4-[1-(p-hydroxyphenyl)-2-phenyl-1-butenyl]benzoic acid and 4-[1-(p-hydroxyphenyl)-2-phenyl-1-butenyl]phenylacetic acid. Compositions containing these triarylethylene carboxylic acids can be administered to patients to alleviate medical conditions associated with a deficiency of estrogen, including osteoporosis, premenstrual syndrome, vasomotor symptoms associated with menopause, atrophic vaginitis, Kraurosis vulvae, female hypogonadism, primary ovarian failure, excessive hair growth and prThe U.S.

Abstract: A novel fluorine-containing aromatic compound of the formula: ##STR1## wherein X is ##STR2## in which R.sub.f is a perfluoroalkyl group having 1 to 10 carbon atoms,R.sub.f ' is a perfluoroalkyl group having 1 to 12 carbon atoms,p is an integer of 1 to 3,q is an integer of 0 to 3,r is 0 or 1,s is an integer of 0 to 5and t is an integer of 0 to 5,Y is X, a hydrogen atom, an alkyl group having 1 to 8 carbon atoms or a fluoroalkyl group having 1 to 8 carbon atoms, andeach A is independently ##STR3## in which D is an amino, carboxyl, hydroxyl, methyl or haloformyl group, and n is an integer of 1 or 2, or ##STR4## can be used to derive various compounds, some of which are useful for preparing a fluorine-containing epoxy compound of polyimide with good properties.

Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.

Abstract: Novel salts of 1-adamantamine are formed by reacting non-steroidal anti-inflammatory carboxylic acids with 1-adamantamine. Formulations of 1-adamantamine hydrochloride and non-steroidal anti-inflammatory carboxylic acids are also described.

Abstract: The invention provides a process for the preparation of cyclopentanediol derivatives of the general formula ##STR1## in which n represents an integer from 0 to 5; each R represents a halogen atom, nitro, cyano, hydroxyl, alkyl, haloalkyl, alkoxy, haloalkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, carboxyl, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, alkylamido, cycloalkyl or phenyl group; and R.sup.1, R.sup.2 and R.sup.3 independently represent a hydrogen atom or an alkyl group; which comprises reacting a cyclopentanol derivative of the general formula ##STR2## with a reducing agent. The invention also provides the cyclopentanol derivative intermediates of formula II per se and a process for their preparation. Compounds of formulae I and II are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.

Abstract: The invention provides a process for the preparation of fungicidally active cyclopentene derivatives of the general formula ##STR1## cyclopentane derivatives of the general formula ##STR2## and cyclohexane derivatives of the general formula ##STR3## in which n, R, R.sup.1, R.sup.2, R.sup.5, X and Y are as herein defined. Compounds of formula II and III are also provided which are useful as intermediates in the preparation of certain fungicidally active cyclopentane derivatives.

Abstract: The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl, R.sup.2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R.sup.3 denotes hydrogen or (C.sub.1 -C.sub.4)-alkyl, and Y.sup.1 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy or --O--(CH.sub.2).sub.n --COOH (with n=1 to 6), with one of these radicals being --O--(CH.sub.2).sub.n --COOH, or Y.sup.1, Y.sup.2 and Y.sup.5 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl or (C.sub.1 -C.sub.4)-alkoxy, Y.sup.3 denotes hydrogen or (C.sub.1 -C.sub.8)-alkoxy and Y.sup.4 denotes --(CH.sub.2).sub.n --COOH or --NH--CO--(CH.sub.2).sub.n --COOH (with n=1 to 6).

Abstract: Compounds of the formula I ##STR1## can be prepared by various process steps from 2-(4-methylphenyl)-2-hexafluoroisopropanol.Hexafluoroisopropyl-containing monomers are important starting compounds in the preparation of linear polycarboxamides and polycarboximides.

Abstract: The new aromatic ethers of the formulae ##STR1## can be used for the preparation of plastics which, in turn, can be processed further to give moulded articles, films, foils and filaments. The plastics prepared from the new aromatic ethers are distinguished by exceptional dimensional stability under heat.

Abstract: Acids, esters, amides and salts of benzhydryl compounds are antidotes for thiocarbamate and acetamide herbicides. These antidote compounds are especially effective to safen acetamide herbicides used to control grassy weeds and broadleaf weeds in rice, sorghum, corn and wheat.

Abstract: A process for producing an optically active carboxylic acid represented by formula (I): ##STR1## wherein R.sup.1, and R.sup.2, and R.sup.3 each represents a hydrogen atom, an alkyl group, an alkenyl group, or a phenyl or naphthyl group which may have a substituent, provided that all of R.sup.1, R.sup.2, and R.sup.3 are not simultaneously a hydrogen atom; when R.sup.1 and R.sup.2 are simultaneously a hydrogen atom, then R.sup.3 is not a methyl group; and that when R.sup.3 is a hydrogen atom, then R.sup.1 and R.sup.2 are each a group other then a hydrogen atom,is disclosed, comprising asymmetrically hydrogenating an .alpha.,.beta.-unsaturated carboxylic acid represented by formula (II): ##STR2## wherein R.sup.1, R.sup.2, and R.sup.3 are the same as defined above, in the presence of a ruthenium-optically active phosphine complex as a catalyst.

Abstract: The invention relates to new compounds of the formula ##STR1## in which R.sup.1 denotes (C.sub.1 -C.sub.8)-alkyl or optionally substituted (C.sub.6 -C.sub.14)-aryl, R.sup.2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off with weak acid or base, R.sup.3 denotes hydrogen or (C.sub.1 -C.sub.4)-alkyl, and Y.sup.1 -Y.sup.9 denote identical or different radicals hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy or -O-(CH.sub.2).sub.n -COOH (with n=1 to 6), one of these radicals being -O-(CH.sub.2).sub.n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.