Abstract: The present invention provides inhibitors of kynureninase having the formula ##STR1## where X is CHOH, S, SO.sub.2, SO, SONH, PO.sub.2 H or PONH.sub.2, R.sub.A and R.sub.B, independently of one another, are H, a halogen, CF.sub.3 or a small alkyl group having one to three carbon atoms; A is a H or an acetyl group; R.sub.1 is H, NH.sub.2, NR.sub.6 R.sub.7, NO.sub.2, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms, wherein: R.sub.6 and R.sub.7, independently of one another, are H, a formyl group or a small alkyl group having from one to three carbon atoms with the exception that only one of R.sub.6 or R.sub.7 can be a formyl group; R.sub.2 is OH, H, halogen, CF.sub.3 or a small alkyl group having from one to three carbon atoms; and R.sub.3, R.sub.4 and R.sub.5, independently of one another, are H, halogen, CF.sub.3, NO.sub.2, NH.sub.2, or small alkyl group having from one to three carbon atoms. In particular, compounds of this formula in which X is CHOH, S or SO.sub.

Abstract: A composition comprising a compound of the formula: ##STR1## wherein: X is H or OH;Y is a group capable of hydrogen bonding to amino, guanidino, or imidazole function, or a group comprising an acidic hydrogen atom, a protected acidic group, or an anion;E is N or CR.sub.1, wherein R.sub.1 is H, OH, CN, F, Cl, Br, or I;A.sub.4, A.sub.5, and A.sub.6 are each independently N, CH, CR.sub.40 or CZ wherein R.sub.40 is R.sub.43, OR.sub.43, SR.sub.43, S(O)R.sub.43, S(O).sub.2 R.sub.43, or NR.sub.43 R.sub.44 wherein R.sub.43 comprises an alkyl of 1 to 3 carbon atoms, an acyl of 2 to 3 carbon atoms, or an alkyl of 1 to 3 carbon atoms substituted with an acyl of 2 to 3 carbon atoms, and R.sub.44 is H or an alkyl of 1 to 2 carbon atoms, and Z is a group capable of hydrogen bonding to carboxyl, or a group comprising a basic heteroatom, a protected basic heteroatom, or a cation.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:x is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --C(O)--, --O--, --NR.sup.1 -- or --(S).sub.q --;Y is --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O) (OR.sup.2) (R.sup.3);R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl;R.sup.3 is --(O).sub.t R.sup.4 ;R.sup.1, R.sup.2 and R.sup.4 are each independently hydrogen, alkyl, aryl or aralkyl;m and n are each independently 0 or an integer from 1 to 5;p and t are each independently 0 or 1; andq is an integer from 1 to 2.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: A is a bond or --OCH.sub.2 --, where the oxygen is linked to R.sup.1 ;B is --CH.sub.2 -- or when R.sup.3 is hydrogen, B may be --CH.sub.2 O-- where the oxygen is linked to the phenyl ring;R.sup.1 is an aryl group;R.sup.2 is hydrogen or lower alkyl;R.sup.3 is hydrogen; or R.sup.2 and R.sup.3 together form the group --CH.sub.2 CH.sub.2 --; andR.sup.4 is --SO.sub.3 H, --P(O.sub.2 H)R.sup.5, --P(O.sub.2 R.sup.5')R.sup.5, --PO.sub.3 H.sub.2, --PO.sub.3 HR.sup.5' or --PO.sub.3 (R.sup.5').sub.2 where R.sup.5 and R.sup.5' are independently lower alkyl. These compounds are beta.sub.3 adrenergic receptor agonists and are useful, for example, in the treatment of diabetes, obesity, achalasia, and gastrointestinal diseases.

Abstract: Substituted 2-aminoalk-3-enoic acid derivative of formula I ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon radical that is substituted by hydroxy, and R.sub.2 is free or esterified carboxy, and their salts exhibit NMDA-antagonistic properties and are useful as active ingredients of anticonvulsive medicaments.

Abstract: A phenylalanine-glycine derivative of the general formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described.The novel conjugate of the phenylalanine-glycine derivative and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered singly or as a mixture with phenylalanine.

Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: The invention relates to a process for the enantioselective preparation of L-phosphinothricin (L-Ptc) and derivatives of the formula I ##STR1## in which R.sup.1 is H, (C.sub.1 -C.sub.6)-alkyl, (C.sub.1 -C.sub.4)-haloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl or (subst.) phenyl-(C.sub.1 -C.sub.4)-alkyl, R.sup.2 is hydrogen, formyl, [(C.sub.1 -C.sub.6)alkyl]carbonyl, [(C.sub.1 -C.sub.6)alkoxy]carbonyl, (subst.) benzyloxycarbonyl, (C.sub.1 -C.sub.6)-alkylsulfonyl or (subst.) (C.sub.6 -C.sub.10)-arylsulfonyl, and R.sup.3 is OH, NH.sub.2 or (C.sub.1 -C.sub.6)-alkoxy, or their salts with acids or bases.

Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.

Abstract: Derivatives of 2-amino-1,2,3,4-tetrahydronaphthalene and their use in therapeutic field are described.The compounds are particularly useful in the treatment of arterial hypertension, cardiac decompensation and renal failure, in the treatment of peripheral arteriopathies and in cerebrovascular insufficiency.

Abstract: The present invention pertains to antagonists of excitatory amino acid neurotransmitter receptor antagonists, their method of preparation as well as compositions containing them which have the general formula: ##STR1## wherein n and m independently are 0, 1, 2, or 3; R.sub.1 is selected from the group consisting of hydrogen and R.sub.2 ; R.sub.2 is selected from the group consisting of hydrogen, halogen, halomethyl, nitro, amino, alkoxy, hydroxyl, hydroxymethyl, C.sub.1 to C.sub.6 lower alkyl, C.sub.7 to C.sub.12 higher alkyl, aryl and aralkyl, wherein if R.sub.2 is hydrogen, R.sub.1 is not hydrogen; R.sub.3 is selected from the group consisting of hydrogen and C.sub.1 to C.sub.6 lower alkyl; the stereoisomers thereof in their resolved or racemic form, and pharmaceutically acceptable salts thereof.

Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts possibly in the form of complexes, esters and amides thereof, represented by the formula: ##STR1##

Abstract: Novel compounds of formula I ##STR1## wherein R is selected from butyl, diethoxymethyl, cyclohexylmethyl, cyclohex-3-enylmethyl, benzyl, 4-chlorobenzyl, 4-methylbenzyl and 4-methoxybenzyl, R.sub.1 is selected from hydrogen and hydroxy, R.sub.2 is selected from hydrogen, chlorobenzyl, dichlorobenzyl, .alpha.-cyclopropyl-dichloro-benzyl, dichlorophenyl-2-hydroxy-ethyl, dimethylbenzyl, trimethoxybenzyl, methylenedioxybenzyl, chlorophenylethyl, dichlorophenylethyl, chloro-iodo-phenylethyl, dimethoxyphenylethyl, methylenedioxyphenylethyl, trimethoxyphenylethyl, 3-phenylprop-2-yl, 3-phenyl-3-hydroxy-prop-2-yl, dichlorophenylpropyl, dichlorophenyl-3-hydroxyprop-2-yl, dichlorophenylbutyl and quinolin-4-ylmethyl, and R.sub.3 is selected from hydrogen and methyl, and salts thereof, have GABA.sub.B -antagonistic properties and can be used for the treatment of diseases responsive to GABA.sub.B -antagonists.

Abstract: A cycloalkyl phosphorus compound is obtained by the catalytic hydrogenation of a substituted or unsubstituted aryl phosphonic acid using a heterogeneous catalyst which is a Group VIII metal on carbon. The hydrogenation is preferably effected in water. The catalyst can be ruthenium or carbon. When phenylphosphonic acid is used as the starting material, a yield of about 95% of essentially pure cyclohexylphosphonic acid can be obtained.

Abstract: N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I ##STR1## wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms,R.sub.1 is hydrogen or hydroxy,R.sub.2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, andR.sub.3 is hydrogen, lower alkyl or a group R.sub.2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.

Abstract: The ampholytes are extracted from the reaction solution with a liquid cation exchanger which is immiscible with the acidic aqueous reaction solution, where the cation exchanger is dissolved in at least one organic solvent which is immiscible with water and forms an organic phase with the organic solvent. Subsequently the organic phase which is loaded with the ampholyte is separated from the reaction solution, and then the ampholytes are back-extracted from the organic phase with aqueous solvents. The product losses in the process are low, and the residual salt content is very low.

Abstract: The present invention is directed to a new class of beta-ketone, beta oxime and beta hydrazine phosphonate NMDA antagonists.

Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.

Abstract: Substituted 2-aminoalk-3-enoic acid derivative of formula I ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon radical that is substituted by optionally acylated or aliphatically or araliphatically etherified hydroxy, by halogen, by optionally acylated and/or aliphatically substituted amino or by an aza-, diaza-, azoxa- or oxa-cycloaliphatic radical, or is an oxacycloaliphatic hydrocarbon radical bonded via a carbon atom, or is an optionally aliphatically N-substituted or N-acylated azacycloaliphatic hydrocarbon radical, and R.sub.2 is free or esterified carboxy, and their salts exhibit NMDA-antagonistic properties and are useful as active ingredients of anticonvulsive medicaments.

Abstract: P-substituted aminoalkylphosphinic acids of the formula ##STR1## wherein R denotes an optionally fluorinated methyl group, R.sub.1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.sub.2 and R.sub.3 denote hydrogen or R.sub.2 denotes hydroxy, lower alkoxy or halogen and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together represent an oxo group, and their pharmaceutically acceptable salts are active as GABA.sub.B.sup.- agonists and can be used in the treatment of spinal spasticity, multiple sclerosis and cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain. They can be manufactured by methods known per se and suitable such methods are described.

Abstract: Nucleosidyl phosphite-borane compounds of the formula: ##STR1## wherein: Nucleoside is a natural or synthetic nucleoside connected to the phosphorus atom via a hydroxyl oxygen; each X is independently selected from O and BHR.sub.3 R.sub.4 ;R.sub.1 is selected from H, alkyl, aryl, alkyaryl, monovalent metal ions, and ammonium cation; R.sub.2 is selected from OR.sub.1 and N(R.sub.5).sub.2, wherein R.sub.5 is independently selected from H, C.sub.1 -C.sub.10 linear or branched alkyl or aryl; R.sub.3 is selected from H, CN, COOH, carboxyl salts, COOR.sub.6 and CONHR.sub.6, wherein R.sub.6 is selected from H, C.sub.1 -C.sub.10 alkyl, alkylaryl and aryl; R.sub.4 is selected from H and C.sub.1 -C.sub.10 alky; and n is 1 to 2.

Abstract: An unexpectedly more potent isomer of 2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a known excitatory amino acid antagonist, pharmaceutical compositions including this isomer and methods of using this isomer to antagonize excitatory amino acid receptors.

Abstract: A compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, alkenyl or phenylalkyl; or R.sup.1 and R.sup.2 taken together are --CH.sub.2 CH.sub.2 --, --CH.sub.2 C(R.sup.6)(R.sup.7)CH.sub.2 -- or --CH.sub.2 C(R.sup.8)(R.sup.9)--C(R.sup.10)(R.sup.11)CH.sub.2 --, where R.sup.6, R.sup.8 and R.sup.10 are, independently, hydrogen, alkyl of 1 to 6 carbon atoms or hydroxyl and R.sup.7, R.sup.9 and R.sup.11 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; A is alkylene or alkenylene; X is CO.sub.2 R.sup.3 in which R.sup.3 is hydrogen or alkyl, P(O)(OR.sup.4)(OR.sup.5) in which R.sup.4 and R.sup.5 are, independently, hydrogen or alkyl, 3,5-dioxo-1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl; or a pharmaceutically acceptable salt thereof are useful as neuroprotectants.

Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.

Abstract: A photographic processing composition containing at one compoud represented by formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, an aliphatic group, or an aromatic group, L.sub.1 and L.sub.2 each represents a divalent bonding group including an alkylene group and/or an arylene group; X represents a ##STR2## group (wherein R.sub.a, R.sub.b and R.sub.c each represents a hydrogen atom, an aliphatic group or an aromatic group, and R.sub.d represents an aliphatic group or an aromatic group); and Y represents a carboxy group, a hydroxy group, a phosphono group, a sulfo group or a salt thereof. The processing composition does not produce precipitate or sludge even when contaminated by metallic ions. A processing method using the processing composition is also disclosed.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## wherein m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or 4;Y.sup.1 and Y.sup.2 are H or halogen;R.sup.2, R.sup.3 and R.sup.4 may be the same or different and are independently H, metal ion, C.sub.1 to C.sub.8 alkyl or C.sub.3 to C.sub.12 alkenyl;X is O, S, NH or NCH.sub.2 R.sup.15 wherein R.sup.15 is H or C.sub.1 to C.sub.5 alkyl; andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein;and when m is o, X is other than S; and if m is o and X is 0, then n is 1, 2, 3 or 4; including all stereoisomers thereof.

Abstract: Novel phosphorus containing compounds are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.

Abstract: The present invention relates to a synergistic antimicrobial compound (mafenide-phosphanilate) having especially high activity for topical prophylaxis and therapy of burn wound infections. The invention further relates to anti-microbial pharmaceutical compositions and a method for treating microbial infection. More particularly, the invention relates to the effective unexpectedly improved treatment of burn wounds involving Pseudomonas and Proteus bacteria.

Abstract: Compounds of the formula I ##STR1## wherein either R.sub.1 is halogen, R.sub.1 ' is halogen or hydrogen and R.sub.2 and R.sub.2 ' denote hydrogen or R.sub.1 and R.sub.1 ' represent hydrogen, R.sub.2 is an aliphatic or aromatic radical and R.sub.2 ' is hydroxy or R.sub.2 and R.sub.2 ' together represent oxo, and wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms or, if R.sub.1 and R.sub.1 ' denote hydrogen, R.sub.2 represents an aromatic radical and R.sub.2 ' is hydroxy, R represents methyl, and their salts are useful as nootropics, antidepressants and/or anxiolytics. The can be manufacture by replacing any group R.sub.5 by hydrogen and/or converting any group Z.sub.0 into amino in a compound of formula II ##STR2## in which R, R.sub.1, R.sub.1 ', R.sub.2 and R.sub.2 ' have their previous significances, Z represents a protected or latent amino group Z.sub.0 and R.sub.4 denotes hydrogen or a hyddroxy-protective group R.sub.

Abstract: A class of phosphono-hydroisoquinoline compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phosphono-hydroisoquinoline compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of Formula I: ##STR1## wherein each of R.sup.1 through R.sup.4 is hydrido, wherein each of Z.sup.1 and Z.sup.2 is hydroxyl, wherein W is a single bond connecting the phosphorus atom with the aromatic ring and wherein the A ring is aromatic. Also disclosed are two classes of intermediate compounds having a fully unsaturated A ring, which intermediate compounds are useful in methods to make product compounds of Formula I.

Abstract: The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.

Abstract: The present invention is novel substituted .alpha.-amino acids, pharmaceutical compositions, method of use, and preparations therefore having utility for treating disorders which benefit from blockade of aspartate and glutamate receptors.

Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.

Abstract: The invention relates to a process for the preparation of compounds of the formula ##STR1## in which Q is substituted or unsubstituted C.sub.1 -C.sub.6 alkyl, A is a direct bond or a bridging member, s is the number 1 or 2, Z is a radical of the formula --CH.sub.2 CH.sub.2 OH, --CH.dbd.CH.sub.2 or --CH.sub.2 CH.sub.2 --Y, and Y is a leaving group, and the benzene or napthalene nucleus I can be further substituted, which comprises reacting compounds of the formula ##STR2## with compounds of the formulaQ--OH (3)in which A, s, Z and Q are as defined under formula (1), in the presence of hydrogenation catalysts, and then carrying out further conversion reactions where appropriate.The compounds obtained by the process according to the invention are suitable as intermediates for the preparation of reactive dyes.

Abstract: This invention relates to lubricating compositions containing hydroxyalkane phosphonic acids and derivatives thereof. More specifically, this invention relates to hydroxylakane phosphonic acids which can be reacted to form salts with basic materials, including overbased detergents, dispersants and amines. These materials can be particularly useful in lubricating compositions.The hydroxyalkane phosphonic acid is represented by the following formula: ##STR1## wherein X is oxygen, sulfur or a secondary amino group, n is an integer from 1 to 8, Y is hydrogen or a phosphonic acid group and R is an alkyl group having from 1 to about 100 carbon atoms.

Abstract: A large number of customary processes for separating amino acids fails when very polar hydrophilic amino acids with isoelectric points (IEP) which are close to one another are to be fractionated. Mixtures of L-glutamic acid (IEP=3.24) and L-phosphinothricin (IEP=2.6) produced by enzymatic transaminations of the corresponding .alpha.-keto acid have been difficult to separate to date. The invention relates to a process for separating L-phosphinothricin and L-glutamic acid, which comprises carrying out the separation as liquid/liquid extraction with two non-miscible aqueous phases as phase system, where the phase former contained in the phase system is a combination of at least two different water-soluble polymers or of at least one water-soluble salt and one water-soluble polymer, and the extraction is carried out by multistage countercurrent partition on the van Dijck principle.

Abstract: Phosphite-borane compounds of the formula ##STR1## wherein: each R.sub.1 is independently selected from: H; C.sub.1 -C.sub.10 alkyl; alkylaryl; aralkyl; aryl; monovalent metal ions; nucleosides; and quaternary ammonium ions, (R.sub.4).sub.4 N.sup.+, in which the substituents R.sub.4 of the ammonium nitrogen atom are H or C.sub.1 -C.sub.10 alkyl;R.sub.2 is H or C.sub.1 -C.sub.10 alkyl; andR.sub.3 is CNCH.sub.2 CH.sub.3.sup.+ BF.sub.4.sup.-, COOH, carboxyl salts, COOR.sub.5, or CONHR.sub.5, wherein R.sub.5 is C.sub.1 -C.sub.10 alkyl, alkylaryl, aralkyl, or aryl;with the proviso that if at least one of the R.sub.1 substituents is H, nucleoside, monovalent metal ion, or quaternary ammonium ion, then R.sub.3 may also be CN. The phosphorous-boron adducts of the invention are bioactive in character, variously exhibiting anti-tumor, anti-inflammatory, and hypolipidemic activity.

Abstract: Unsaturated aminodicarboxylic acid derivatives of formula I ##STR1## wherein A is a divalent aliphatic hydrocarbon radical containing 2 carbon atoms and R.sub.1 and R.sub.2 are each independently of the other free or esterified carboxyl groups, and salts thereof, have a pronounced and selective antagonistic action against N-methyl-D-aspartic acid (NMDA)-sensitive excitatory amino acid receptors. These compounds are prepared, for example, by converting, in a formula of formula II ##STR2## wherein Z.sub.1 and Z.sub.2 are hydroxy or protected hydroxy and Z.sub.3 is protected amino, Z.sub.3 into amino and, if present, converting protected hydroxyl groups Z.sub.1 and/or Z.sub.2 into hydroxy and, if desired, converting a resultant compound into another compound of formula I, resolving a resultant mixture of isomers into the individual components and separating the desired preferred isomer and/or converting a resultant free compound into a salt or a resultant salt into the corresponding free compound.

Abstract: A process for preparing a carboxyalkyl-substituted hydroxylamine represented by formula (I) ##STR1## where L represents an alkylene group; A represents a hydrogen atom, a sulfo group, a carboxy group, a phosphono group, a trialkylammonio group, a hydroxy group, an amino group, an acyl group, a carbamoyl group, a sulfamoyl group, an alkoxycarbonyl group, or a cyano group; and R.sub.1, R.sub.2, and R.sub.3, which may be the same or different, each represent a hydrogen atom, an alkyl group, or an aryl group; which comprises: reacting an .alpha.,.beta.-unsaturated carboxylic acid represented by formula (II) as an alkylating agent ##STR2## where R'.sub.1, R'.sub.2, and R'.sub.3, which may be the same or different, each represent the same group as defined for R.sub.1, R.sub.2, and R.sub.

Abstract: A phosphorylated derivative of L-dopa of the formula ##STR1## wherein when X is ##STR2## wherein Z is --CH.sub.2, N, S or a linkage other than oxygen which renders the phosphate group resistant to hydrolysis by phosphatase enzymes in tissues and biological fluids,then Y is OQ, wherein Q is H or an alkyl with one to twelve carbon atoms, orwherein X is OQ, then Y is ##STR3## wherein R' is hydrogen or a pharmaceutically acceptable cation and R is a moiety which increases hydropobicity. The phosphorylated derivative of L-dopa is useful as an agent to increase the melanin content in mammalian skin and hair.

Abstract: Rhizocticines of the formula ##STR1## in which X represents hydrogen or a hydrophobic amino acid radical and Y represents a basic amino acid radical, the C2 atoms of the amino acid radicals having the L-configuration, and protected derivatives and salts thereof.The compounds are obtained from culture broths of Bacillus subtilis or synthetically and have especially fungicidal action.

Abstract: The present invention is directed to a new class of 4-(oxoalkyl)phosphono, 4(oxime alkyl)phosphono, or 4-(hydrazine alkyl)phosphono, 2-piperazine carboxylic derivatives that are useful as NMDA antagonists

Abstract: Cyclic 1-one-2-ene-3-ol compounds substituted in 2-position by an aroyl or heteroaroyl group bearing a hydrocarbylsulfonyloxy or hydrocarbylsulfonylamino substituent exhibiting herbicidal activity.

Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.

Abstract: The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.

Abstract: The invention relates to rhodium complexes of the formula[A--O--(CH.sub.2 CH.sub.2 O).sub.n --A].sup.2+ 2X.sup.- (Ia)and[A--O--(CH.sub.2 CH.sub.2 O).sub.m --CH.sub.3 ].sup.+ X.sup.-(Ib)in whichn=5-1,000,m=5-250,X.sup.- denotes a tetrafluoroborate, hexafluorophosphate or per-chlorate anion,A denotes a radical of the formula ##STR1## (en).sub.2 denotes two molecules of a monoolefin or one molecule of a diolefinAr denotes phenyl or phenyl which is substituted by one or two alkyl groups having 1 or 2 carbon atoms andR.sup.1 denotes an arylene or alkylene bridge,and their use for the preparation of L-phosphinothricin and its derivatives by enantioselective catalytic hydrogenation of 2,3-dehydrophosphinothricin (derivatives).

Abstract: The present invention describes a class of dyes for use in staining cell samples and methods of making such dyes. A preferred class of dyes known as detergent dyes which possess the ability to stain cells in whole blood and are only slowly leached or lost from the stained cells over time are described. The present invention has application, for example, to blood typing for the determination of the presence of blood group antigens A, B, AB, O, and D (Rh.sub.o) and antibodies to such antigens.

Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.0 and R.sup.

Abstract: Sulfonamide derivatives of the formula I ##STR1## where R.sup.1 is a C.sub.1 -C.sub.4 -alkyl or phenyl group which may be substituted by halogen, trifluoromethyl or C.sub.1 -C.sub.4 -alkyl, R.sup.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl, A is a group CHOR.sup.3 C.dbd.O, C.dbd.S or C.dbd.N--OR.sup.4, R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl phenyl, benzyl or C.sub.1 -C.sub.4 -acyl, R.sup.4 is hydrogen or methyl, B may be methylene or ethylene in the m or p position or, of A is not carbonyl, may be methyleneoxy, the oxygen atom being bonded to the aromatic, and E is a carboxyl, phosphonic acid or sulfo radical, their physiologically acceptable salts, esters with C.sub.1 -C.sub.4 -alcohols or amides or the tetrazol-5-yl radical, their preparation and their use as drugs.