Abstract: The invention relates to novel glyoxylic acid amides, to a plurality of processes for their preparation and to their use for controlliing pests.

Abstract: A process for the increasing the conversion of raw materials into DMAc by increasing the temperature at which the reaction occurs. The higher temperature is achieved by installing a pressure control valve in the dimethyl amine recycle line returning to the scrubber column. This raises back pressure on reactor and reactor column. The higher pressure raises the temperature in reactor vessel. Higher temperature increases the reaction rate and efficiency. The implementation of this invention greatly increases the capacity of existing equipment without adding large amounts of capital to expand conventional methods.

Abstract: The present invention provides an inexpensive one-step method for preparing an aromatic carboxamide, such as a phenyl substituted carboxamide) by reacting an aromatic amine (e.g. a phenylamine) and a carboxylic acid (e.g. an alkanoic acid or ester thereof) in the presence of a boron containing compound (e.g. boronic acid or boric acid) and, optionally, a chelating agent (e.g. a 2-pyridinylamine).

Abstract: The use of a compound of the formula (I): wherein: ring C is phenyl or carbon-linked heteroaryl selected from pyridyl, pyrazinyl, pyrimidinyl and pyridazinyl; and wherein said phenyl or heteroaryl is substituted as defined herein; A—B is selected from NHCO, OCH2, SCH2, NHCH2, trans-vinylene, and ethynylene; R1 is linked to ring C at a carbon ortho to the position of A—B attachment and is defined herein; n is 1 or 2; R2 and R3 are alkyl, haloalkyl or together from cycloalkyl or halocycloalkyl as defined herein; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Salts and esters of compounds of formula (I) are also described.

Abstract: Compounds of the formula R2.[(AO)n.R3]m, where R2 is a residue of a group having at least m active hydrogen atoms derived from hydroxyl and/or amino and/or amido groups, AO is alkyleneoxy, n is 2 to 200; R3 includes residue(s) of alkenyl succinic acids and optionally other acids, and m is 2 to 10, but when m is 2 there are other restrictions in the definitions, are disclosed as useful thickeners and/or dispersants in aqueous systems. The use of such materials as thickeners is also disclosed.

Abstract: There is provided a process for producing an N-acyl amino acid amide, comprising a condensation reaction of an N-acyl amino acid with an amine and/or an ammonia, preferably a primary amine, a secondary amine and/or an ammonia under dehydration in the presence of a boron compound as the catalyst under coexistence of an alcohol as the auxiliary solvent, at a high yield for a short time. A medium for hylotropic dehydration such as hydrocarbon compounds may be used in the reaction.

Abstract: A process for producing a saturated aliphatic carboxylic acid amide, comprising reacting a saturated aliphatic carboxylic acid with ammonia to thereby obtain a saturated aliphatic ammonium carboxylate and subjecting the saturated aliphatic ammonium carboxylate to a dehydration reaction for obtaining a saturated aliphatic carboxylic acid amide, wherein the dehydration reaction of the saturated aliphatic ammonium carboxylate is conducted while supplying water to a reaction system in which the dehydration reaction is carried out. Preferably, water is continuously supplied to the reaction system so that the production of the saturated aliphatic carboxylic acid amide is carried out in a continuous manner and the amount of water present in a steady state ranges from 20 to 70 mol per 100 mol of a total of the saturated aliphatic carboxylic acid, the ammonia, the saturated aliphatic ammonium carboxylate, the saturated aliphatic carboxylic acid amide and the water.

Abstract: A compound of the formula wherein R1 and R2 are H, a hydrocarbon group or a heterocyclic group, or R1 and R2 are combinedly a spiro ring; R3 is a hydrocarbon group, a substituted amino group, a substituted hydroxyl group or a heterocyclic group; R4 is H or alkyl; ring A is a substituted benzene ring; m and n denote 1 to 4; {overscore (.........)} means a single or double bond or a salt, a process of producing thereof and a composition having a binding affinity for melatonin receptor.

Abstract: The present invention provides a novel single step process for the production of amides from amines comprising reaction of amines with an acylating agent comprising of a carboxylic acid in a molar ratio of 1:3 to 1:10 in the presence of reusable natural montmorillonite/metal ion-exchanged clay catalysts, in a suitable solvent medium at a temperature in the range of 30-160° C. for a period of 0.02 to 6 hrs, and recovering the corresponding amides by a conventional simple work-up procedure.

Abstract: A process is disclosed for preparing di- or oligoamide alkoxylates. Diamides are prepared from carboxylic acids or carboxylic acid alkyl esters and di-, oligo-, or polyamines and are alkoxylated as a melt directly after their preparation, without any further intermediate preparation process.

Abstract: The present invention provides a method for producing a mass-coded combinatorial library comprising a set of compounds having the general formula X(Y)n, where X is a scaffold, each Y is, independently, a peripheral moiety, and n is an integer greater than 1. The method comprises selecting a peripheral moiety precursor subset from a peripheral moiety precursor set. The subset includes a sufficient number of peripheral moiety precursors that at least about 50 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors in the subset exist. The subset of peripheral moiety precursors is selected so that at least about 90% of all possible combinations of n peripheral moieties derived from the subset have a molecular mass sum which is distinct from the molecular mass sums of all of the other combinations of n peripheral moieties. The method further comprises contacting the peripheral moiety precursor subset with a scaffold precursor which has n reactive groups.

Abstract: Benzamides of the formula I: wherein R1 and R2 independently of one another are each alkyl having 1-6 C atoms, or R1 and R2 together are alkylene, and their salts, are suitable as intermediates in the synthesis of drugs.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: A process for producing an aromatic polyamide which comprises:(a) a dicarboxylic acid component which consists of 30-100 mol % of terephthalic acid and optionally 0-70 mol % of at least one dicarboxylic acid other than terephthalic acid, and(b) a diamine component which consists of 50-100 mol % of an aliphatic alkylenediamine of 4-25 carbons and optionally 0-50 mol % of at least one alicyclic diamine of 3-25 carbons, said process comprising a first step of performing melt reaction of said dicarboxylic acid with said diamine, thereby giving a low molecular weight condensate having an intrinsic viscosity [.eta.] of 0.05-0.6 dl/g, a second step of subjecting it to solid phase polymerization, thereby giving an aromatic polyamide precursor having an intrinsic viscosity [.eta.] of 0.5-1.0 dl/g, and a third step of subjecting it to melt polymerization, thereby giving an aromatic polyamide having a desired intrinsic viscosity [.eta.] of 0.8-2.5 dl/g.

Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.

Abstract: A process for preparing cocondensates of aspartic acid and amines by heating aspartic acid and amines in the presence of acidic catalysts comprises supplying the feed region of the extruder with particulate aspartic acid and a downstream metering zone with at least one amine and at least one acidic catalyst, condensing the resulting mixture to such an extent by heating that the downstream end of the extruder discharges a precondensate which contains at least 20-95% by weight of the starting aspartic acid in condensed form, and then completing the condensation of the precondensate. The cocondensates are useful as incrustation inhibitors in detergents.

Abstract: A method for preparing carbamoylmethylurea derivatives of the formula (I): ##STR1## characterized by reacting a compound of the formula (II): ##STR2## with a compound of the formula (III): ##STR3##

Abstract: The invention relates to a carbamide of the general formulaR.sub.1 --CO--NH--C(R.sub.2)(R.sub.3)--X--Ywhich is protected by a temporary protective group and whereinR.sub.1 --CO means a carbonyl residue which can be provided as a unit for the chain of a peptide, and can have one or a plurality of amino acid residues;R2 and R3 mean resides of the carbamide which do not participate in their function, whereby R2 and R3 can be identical or different, but are different when one of the two residues means a hydrogen atom;X means an oxygen atom or a sulphur atom, andY means a protective group for X.The invention further relates to a process for producing the protected carbamide and to utilisation of the protected carbamide.The protected carbamide according to the invention can also be linked to a carrier material.

Abstract: The invention relates to a process for the preparation of highly concentrated free-flowing and pumpable aqueous solutions of betaines by quaternization of a compound which contains tertiary amine nitrogen with a .omega.-halo carboxylic acid characterized in that 0.5-5% by weight of the final product, of a viscosity-reducing compound such as an alkali or alkaline earth metal citric acid salt is added to the reaction mixture before or during the quaternization reaction.

Abstract: This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.

Abstract: A process for preparing .alpha.-(N,N-dialkylamino) carboxamides of the formula I ##STR1## where the substituents have the stated meanings, comprises reacting the corresponding free acids with primary or secondary amines in the presence of anhydrides of an alkanephosphonic acid.

Abstract: Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, restenosis, rheumatoid arthritis, wounds, cancer, angiogenesis and shock.

Abstract: The present invention relates to polyisocyanates containingi) 0.5 to 10 wt. % of amide and/or imide structural units (calculated as --CO--N.dbd., MW=42),ii) 5 to 20 wt. % of isocyanate groups (calculated as --NCO, MW=42) blocked with blocking agents which are monofunctional in the context of the isocyanate addition reaction andiii) 0 to 30 wt. % of chemically incorporated urethane groups (calculated as --NH--CO--O--, MW=59) obtained from the reaction of isocyanate groups with the hydroxyl groups of organic polyhydroxyl compounds.The present invention also relates to a process for the production of these lacquer polyisocyanates, their use as a binder for stoving lacquers optionally in combination with organic polyhydroxyl compounds and to their use as a binder component containing free hydroxyl groups and optionally blocked isocyanate groups by reacting and/or blending the polyisocyanates with organic polyhydroxyl compounds having a molecular weight of 62 to 350.

Abstract: The present invention relates to compounds selected from the group consisting of:(i) the compounds of the formula ##STR1## in which: R is a hydrogen atom, a group OH, a group OCH.sub.3 or a group CH.sub.2 OH,*C, in the case where R is not a hydrogen atom, is an asymmetric carbon atom of (R,S), (R) or (S) configuration, and**C is an asymmetric carbon atom of (R,S) or (R) configuration; and(ii) their addition salts.It further relates to the method of preparing these compounds, to their use in therapeutics and in the field of analysis, and to intermediates.

Abstract: The present invention relates to derivatives of 2,2,3,3-tetramethylcyclopropane carboxylic acid (TMCA) of general formula (I), ##STR1## wherein R is lower alkyl group (C.sub.1 -C.sub.6), an aryl group, an aralkyl group or an amide of general formula (II), ##STR2## where R.sub.1 and R.sub.2 are the same or different and may be hydrogen, a alkyl group (C.sub.1 -C.sub.6), an aryl group or an aralkyl group, and n=0-3, to their racemic mixtures and the D and L enantiomers. The invention also relates to processes for the preparation of said compounds and for pharmaceutical preparations comprising the same. The new compounds show improved activity against epilepsy.

Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.

Abstract: Alkylbenzoylguanidines of the formula I ##STR1## in which A, R.sup.1, R.sup.2 and R.sup.3 have the given meanings, and their physiologically harmless salts exhibit antiarrhythmic properties and act as inhibitor of the cellular Na.sup.+ /H.sup.+ antiporter.

Abstract: A method for synthesizing a halogen-containing condensation product, the method comprising the step of:reacting a compound represented by Formula (I) with a compound represented by Formula (II) or (III) in the presence of a halogenating agent whereby dehydration condensation and halogenation are carried out, ##STR1##

Abstract: A process for preparing polymeric amides is disclosed. The process comprises sequentially reacting a hydrocarbon polymer functionalized (e.g., via the Koch reaction) to contain acid, ester, thioacid and/or thioester groups with a heavy polyamine to form a partially derivatized product in which at least about 85% of the functional groups are converted to heavy (thio)amide groups, and then reacting the partially derivatized product with an excess of light amine to complete the derivatization by converting substantially all of the remaining functional groups to light (thio)amide groups. Products of the foregoing process are also disclosed, which products are useful as additives in fuels and in lubricants.

Abstract: The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.

Abstract: Cyclopropanecarboxylic acid amides ##STR1## wherein R represents hydrogen, straight-chain or branched C.sub.1 -C.sub.4 -Alkyl, optionally substituted aryl or optionally substituted aralkyl,can be prepared directly from the corresponding cyclopropanecarboxylic acid by reaction with ammonia under pressure in a suitable organic solvent.

Abstract: Nitrogen mustard pro-drugs of the formula ##STR1## are disclosed where R is the residue of an .alpha.-amino acid RNH.sub.2 and M is a disubstituted amino "mustard" group, useful in antibody directed enzyme pro-drug therapy in the treatment of cancer.

Abstract: The present invention relates to a one-step process for preparing amido-carboxylic acid esters having the amide nitrogen positioned between two carbonyl carbons by reacting a carboxylic acid or carboxylic acid ester with a monohydric alcohol and either a lactam, amino-carboxylic acid or a polymeric amino-carboxylic acid. In this process, amidation, esterification, alcoholysis, and hydrolysis reactions occur simultaneously.

Abstract: The present invention relates to a process for the preparation of hydroxycarboxylic acid amides of the general formula (1): ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen, halogen, cyano, a linear or branched alkyl, alkenyl, alkynyl or alkoxy group having 1 to 12 carbon atoms, an aralkyl group having 7 to 12 carbon atoms, a cycloalkyl group having 6 to 12 carbon atoms or an aryl group having 6 to 12 carbon atoms, R.sup.3 is hydrogen or a linear or branched alkyl group having 1 to 4 carbon atoms, R.sup.4 is hydrogen or a linear or branched alkyl group having 1 to 6 carbon atoms, or R.sup.3 and R.sup.4, together with the carbon atom to which they are attached, form a five- or six-membered cycloalkane ring, and n is an integer from 1 to 12, wherein an aniline of the general formula (2) ##STR2## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.

Abstract: A process for the production of of general formula I diethylenetriaminepentacarboxylic acid monoamide derivatives ##STR1## in which E.sup.1, E.sup.2 and Z have varying meanings.

Abstract: A method for amidation of carboxylic acids using a supported transition metal catalyst. The amides prepared by this inventive method are available in high-yield and excellent purity, without catalytic residue.

Abstract: Process for the of aromatic carboxamides from aromatic carboxylic acids and ureaProcess for the preparation of aromatic carboxamides of the formula (I) ##STR1## in which R.sub.1, R.sub.2, and R.sub.3 are identical or different and are hydrogen, fluorine, chlorine or bromine atoms, or are alkyl(C.sub.1 -C.sub.4), hydroxyl or nitro groups, or R.sub.1 and R.sub.2 form an aromatic ring of 5 or 6 ring members, which ring may be substituted by fluorine, chlorine or bromine atoms or by alkyl(C.sub.1 -C.sub.4), hydroxyl or nitro groups, which involves reacting aromatic carboxylic acids of the formula (II) ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 are as defined above with urea in an inert organic solvent with the addition of a catalytic amount of phosphorous acid.

Abstract: An .alpha.-amino acid amide is prepared by reaction of an N.sup..alpha. -aryloxycarbonylamino acid with a compound containing a free amino group. This process makes it possible readily to prepare peptides, by direct reaction between the carboxyl group of the N.sup..alpha. -aryloxycarbonyl derivative of an amino acid and the free amino group of a second amino acid or of a peptide fragment, without requiring protection of the carboxyl function of the second amino acid or of the peptide fragment, nor a coupling agent nor a deprotection step.

Abstract: The present invention is drawn to a process for forming an amide bond linkage comprising reacting a carboxylic acid and an amine in a two-phase mixture of water and an organic solvent selected from an oxygenated organic solvent or an aromatic solvent in the presence of a coupling reagent and an additive. This process is useful for making ubiquitous amides and polypeptides having various biological activities.

Abstract: The dispersants are formed by reacting (a) at least one dispersant having at least one primary or secondary amino group and/or at least one hydroxyl group, with (b) at least one polyolefinic compound substituted at each terminal position by a succinic group. Suitable substances for use as reactant (b) include compounds derived from at least one telechelic compound having up to 5000 carbon atoms and at least two terminal methylene groups by reaction with maleic anhydride or the like. The products are deemed to be effective dispersant/detergents for use in fuels and lubricants. In fuels the products are deemed to exhibit the property of inhibiting and/or reducing deposit formation such as intake valve deposits. In crankcase lubricants, the products are deemed to provide desirable viscosity index improving properties.

Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.

Abstract: Acylamides or amine acylate salts of arylalkanolamines are prepared by reacting an arylisonitrosoalkanone with hydrogen and a carboxylic acid, carboxylic acid anhydride or carboxylic acid ester or mixture thereof in the presence of a transition metal catalyst; optionally the product is converted to the corresponding arylalkanolamine hydrochloride salt by reaction of the acylamide or amine acylate salt of the arylalkanolamine with hydrogen chloride in a C.sub.1 -C.sub.3 alkyl alcohol.

Abstract: Diamidopolyamines are prepared by reacting glutamic acid with two moles, per mole of glutamic acid, of a defined class of diamines, including oxyethyelene diamines, oxypropylenediamines, oxyethylene/propylene diamines, oxypropylene triamines, 1,2-diaminocyclohexane and isophorone diamine, whereby each of the carboxyl groups of the glutamic acid will react with an amine group of the amine reactant to thereby provide primary amine terminated amidopolyamines containing, internally, the unreacted primary amine group of the glutamic acid.

Abstract: Acylamides or amine acylate salts of arylalkanolamines are prepared by reacting an arylisonitrosoalkanone with hydrogen and a carboxylic acid, carboxylic acid anhydride or carboxylic acid ester or mixture thereof in the presence of a transition metal catalyst; optionally the product is converted to the corresponding arylalkanolamine hydrochloride salt by reaction of the acylamide or amine acylate salt of the arylalkanolamine with hydrogen chloride in a C.sub.1 -C.sub.3 alkyl alcohol.

Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methy1-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.

Abstract: Optionally substituted p-aminophenol compounds, easily converted into the N-acylated derivatives thereof, are prepared by hydrogenating the corresponding nitrobenzene, in solution in a saturated aliphatic monocarboxylic acid, notably acetic acid, in the presence of an effective amount of a protonic acid.

Abstract: Improved additives/detergents for lubricant and fuel compositions are obtained by condensing a hydroxyalkyl or hydroxyaryl compound with an amine compound. The condensates according to the present invention are produced by the acid catalyzed condensation of the amine reactant with the hydroxy reactant.

Abstract: An additive for fuels and lubricating oils with detergent, dispersant and anti-rust properties is described, consisting essentially of the product of condensing a mixture of alkenylsuccinic acids or anhydrides of formula (I) ##STR1## where m and n, mutually independently, represent 0 or a whole number between 1 and 10 and are such that their sum is 9 or 10, and >R is >O or (--OH, --OH), with triethylenetetramine of formula (II)H.sub.2 N--(CH.sub.2 --CH.sub.2 --NH).sub.3 --H (II).

Abstract: Surfactant composition prepared by reacting dicarboxylic acids and esters thereof, such as adipic acid, diethyl oxalate, etc.; a polyoxyalkyleneamine residue, such as an alkylene glycol diamine bottoms product, and fatty acids and esters thereof, such as tallow acid or coconut acid, are described. These nonionic surfactant compositions are useful for preparing surfactant bars, or other molded or shaped articles such as toys.

Abstract: Intermediates of Formula ##STR1## where R is a methylthio, methylsulfoxy, methylsulfonyl or a nitro group; andX1 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenyl or phenylalkyl(1-6C), where the phenyl ring may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX1 together with X2 is an oxygen atom or an alkylene having from two to five Carbon atoms; orX1 together with X2 and R4 is a chain of formula ##STR2## where p is 3 or 4 and q is 1 or 2; and X2 is hydrogen, 1-6 C alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl or phenyl which may be substituted by one or two halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; orX2 together with R4 is ##STR3## where n is 1 or 2; m is 0 or 1; X is hydrogen, halogen, 1-3 C alkyl, 1-3 C alkoxy or nitro; andX3 is hydrogen or --CO--R4 where R4 is hydrogen, 1-6 alkyl, 1-6 C haloalkyl, 3-6 C cycloalkyl, phenylalkyl(1-6C) or phenyl where the phenyl ring may be substituted by one or two halogen, 1-3 alkyl, 1-3 alkoxy or nitro; andX4 is --OH, fluorine,