Abstract: The present invention relates to a method of preparing a 1-nitro-3-substituted-3-amino-2-propanol diastereomer represented by Structural Formula I: In Structural Formula I, R is an amine protecting group, and R1 is an amino acid side-chain, a protected amino acid side-chain, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group, a substituted or unsubstituted aralkyl or a substituted or unsubstituted heteroaralkyl group. The method involves contacting a 1-nitro-3-substituted-3-amino-2-propanone with a reducing agent to form a mixture of 1-nitro-3-substituted-3-amino-2-propanol diastereomers. The 1-nitro-3-substituted-3-amino-2-propanol diastereomers are then separated by simulated moving bed chromatography to obtain one or more 1-nitro-3-substituted-3-amino-2-propanol diastereomer.

Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.

Abstract: Process for preparing optically active &bgr;-amino alcohols represented by a general formula (2): Ra—C*H(OH)—C*H(Rb)—Rc wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, Rb is one member selected from among groups represented by the following general formulae; (3) R1CO(R2)N—, and (4) R1CO(R1′CO)N—, and C* is an asymmetric carbon atom, characterized by reacting a racemic &agr;-aminocarbonyl compound represented by the general formula (1): Ra—CO—CH(Rb)—Rc, with hydrogen in the presence of an optically active transition metal compound represented by a general formula (7): MaXY(Px)m(Nx)n wherein Ma represents a metal atom belonging to VIII-group of the periodic law, X and Y represent each independently hydrogen, halogeno, Px represents a phosphine ligand, Nx represents an amine ligand, at least one of Px and Nx is optically active, and m and n each independently represent 0 or an integer of 1 th

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: A halogenating agent of the formula (1) and a method of halogenating hydroxyl group wherein R1 and R2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or allyl; X is chlorine atom or bromine atom; and Y is chlorine ion, bromine ion, dichlorophosphate ion, dibromophosphate ion, chlorosulfonate ion, bromosulfonate ion, chlorooxalate ion or bromooxalate ion.

Abstract: Organic photoprecursors of amines are provided for use in photosensitive imaging systems, finding particular application in the preparation of lithographic printing plates. Said photoprecursors generate free amines on exposure to long wavelength UV or visible radiation, have high solubility in organic solvents, and include photolabile 2-nitrobenzyl functional groups. Methods for the synthesis of the photoprecursors are described, and the use of the said photoprecursors for the production of printing plates using both positive working and negative working techniques are discussed.

Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solvent

Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have the formula: where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: N-(4-carbamimidoyl-phenyl)-glycine derivatives have the formula: 1

Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: The invention provides an improved process for preparing compounds of formula (I)

Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, inducing osteoporosis; gingival disease including gingivitis and periodontists; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: A halogenating agent of the formula (1) and a method of halogenating hydroxyl group wherein R1 and R2 are the same or different and are each ethyl, propyl, isopropyl, butyl, isobutyl or allyl; X is chlorine atom or bromine atom; and Y is chlorine ion, bromine ion, dichlorophosphate ion, dibromophosphate ion, chlorosulfonate ion, bromosulfonate ion, chlorooxalate ion or bromooxalate ion.

Abstract: The compounds of formula I ##STR1## wherein: a) X is O, andY is OC.sub.1 -C.sub.4 alkyl; orb) X is O or S, andY is NHCH.sub.3have fungicidal properties and can be used in plant protection for controlling and preventing disease infestation.

Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 and [sic] CHCH.sub.2 CH.sub.3 ;R.sup.1 is hydrogen and [sic] alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl and [sic] alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sup.4 and R.sup.5 are as defined in the specification.

Abstract: A method for the inhibition of the binding of .alpha..sub.4 .beta..sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which .alpha..sub.4 .beta..sub.1 is involved.

Abstract: Phenylcarbamates of the formula I ##STR1## where the substituents and the index have the following meanings: R is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2;R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and, in the event that X is NR.sup.a, additionally hydrogen;X is a direct bond, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.2 is hydrogen,substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl;R.sup.3 and R.sup.4 independently of one another are hydrogen, cyano, nitro, hydroxyl, amino, halogen, hetaryloxy, hetarylthio, hetarylamino or N-hetaryl-N-alkylamino, andR.sup.5 is one of the groups mentioned under R.sup.3 or a group CR.sup.d .dbd.NOR.sup.e ;processes and intermediates for their preparation, and their use.

Abstract: Cyanoiminooxime ethers of the formula I ##STR1## wherein X is NOCH.sub.3, CHOCH.sub.3 or CHCH.sub.3 ;Y is O or NZ where Z is hydrogen or alkyl;R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.2 is cyano, nitro, halogen, alkyl, trifluoromethyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, alkyl, haloalkyl, alkoxy or cycloalkyl;R.sup.4 is hydrogen, orunsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl or hetaryl,or a salt thereof, their preparation, intermediates for their preparation, and their use for controlling harmful fungi and animal pests.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: Briefly, in one aspect, the present invention provides compositions of open-chain, .alpha.-branched fluoroalkylcarbonyl fluorides, and derivatives thereof.

Abstract: Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R.sup.1= halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3= H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, hydroxy-C.sub.1 -C.sub.6 -alkyl;R.sup.4= H, halogen, CN, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl orR.sup.3 +R.sup.4 =chemical bond;Y=--O--, --S--, --O--CO--, --O--SO.sub.2 -- or chemical bond;Y'=--O-- or --S--;R.sup.5= unsubst. or subst. C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl; C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, unsubst. or subst. phenyl or phenyl-C.sub.1 -C.sub.6 -alkyl, or, if Y is --O--, --S-- or a chemical bond, is (C.sub.1 -C.sub.6 -alkyl)carbonyl or (C.sub.1 -C.sub.6 -alkoxy)carbonyl; or, if Y is a chemical bond, is hydrogen or halogen;R.sup.5 '=R.sup.5, H or (C.sub.1 -C.sub.6 -haloalkyl)carbonyl;R.sup.6= H, C.sub.1 -C.

Abstract: An .alpha.-hydrazino acid derivative of general formula (I) is described, wherein R.sub.1, R.sub.2, R.sub.3 are hydrogen or a carbon radical, such that when R.sub.2 and R.sub.3 are different, C* is an asymmetric carbon of L, D or DL configuration, and R.sub.4 and R.sub.5 are a protecting group, characterized in that R.sub.4 is a benzyl ArCH.sub.2 radical of formula (a), wherein Ar is a phenyl radical or phenyl substituted by one or more X groups; X being hydrogen, halogen, a nitro or alkyl radical; and in that R.sub.5 is a Y--O--CO group, where Y is a carbon radical different from R.sub.4.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: A dye mixture, which comprises as component (A) a dye of formula as component (B) a dye of formula ##STR1## and/or as component (C) a dye of formula ##STR2## wherein D, X and Y are as defined in the specification. These dyes are particularly suitable for dyeing polyester fiber textile material.

Abstract: A process for the preparation of N-carboxyalkyl-3-fluoro-4-dialkylaminoanilines, which comprises reacting, in a first step, 2-chloro-4,5-difluoronitrobenzene of the formula (I) ##STR1## with a secondary amine of the formula (II) HNR.sup.1 R.sup.2, in which R.sup.1 and R.sup.2, independently of one another, are identical or different and are an alkyl radical having from 1 to 10 carbon atoms or, together with the N atom to which they are bonded, form a ring having from 5 to 7 members, in the presence of a water-soluble amine which forms hydrofluorides and hydrochlorides which are liquid at the reaction temperature and work-up temperature or soluble in the reaction mixture, in the presence or absence of a solvent at -10 to 120.degree. C., reducing, in a second step, the reaction mixture containing the 2-chloro-4-dialkylamino-5-fluoronitrobenzene using hydrogen at from 30 to 150.degree. C.

Abstract: A process for production of l-alkylthiomethanediphosphonic acid compound or 1-arylthiomethanediphosphonic acid compound characterized by removing a thiolate byproduct as an insoluble salt, in the condensation represented by the following formula: ##STR1## wherein R'.sub.1 represents a linear or branched alkyl group having 1 to 6 carbon atoms, R.sub.2 represents an alkyl or aryl group, R.sub.1 represents a pharmaceutically allowable cation, hydrogen atom, or linear or branched alkyl group having 1 to 6 carbon atoms. The present invention significantly improves the yield compared with conventional methods, and simplifies the purification process at the same time, thus is extremely useful in an economical and industrial points of view.

Abstract: There is provided a 3-(3-aryloxyphenyl)-1-(substituted methyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.

Abstract: The invention provided methods and compositions for oligonucleotide synthesis and labeling. The subject compounds have either rigid ring or long linear linker structures and provide enhanced coupling efficiencies over prior art labeling reagents because of lack of stereo hindering and/or provide more convenient and cost-effective syntheses. These novel linkers also contain a base labile structure which provides: labeling at 3' end with regular solid supports, cleaving under mild conditions, and achieving higher yield because of the complete cleavage and higher purity because the mild conditions will not bring down the impurities on the solid support. When used in a solid support pre-attached with either a nucleotide for unlabeled oligonucleotide synthesis, or a label for 3' end labeled oligonucleotide synthesis, or an alternate structure to use as an universal support, these linkers provide solid supports requiring only mild cleavage conditions.

Abstract: Enzymatically cleavable chemiluminescent 1,2-dioxetane compounds capable of producing light energy when decomposed, substantially stable at room temperature before a bond by which an enzymatically cleavable labile substituent thereof is intentionally cleaved, are disclosed. These compounds can be represented by the formula: ##STR1## wherein: X and X.sup.1 each represent, individually, hydrogen, a hydroxyl group, a halo substituent, an unsubstituted lower alkyl group, a hydroxy (lower) alkyl group, a halo (lower) alkyl group, a phenyl group, a halophenyl group, an alkoxyphenyl group, a hydroxyalkoxy group, a cyano group or an amide group, with at least one of X and X.sup.1 being other than hydrogen; andR.sub.1 and R.sub.2, individually or together, represent an organic substituent that does not interfere with the production of light when the dioxetane compound is enzymatically cleaved and that satisfies the valence of the dioxetane compound's 4-carbon atom, with the provisos that if R.sup.1 and R.sub.

Abstract: Substituted phthalimidocinnamic acid derivatives I ##STR1## wherein the variables are as defined in the description are useful as herbicides and for the desiccation and/or defoliation of plants.

Abstract: Aromatic amides of poly(oxyalkylene) carbamates having the formula: ##STR1## or a fuel-soluble salt thereof; wherein A, R.sub.1 -R.sub.10, x, y, and z are as defined herein.

Abstract: A liquid crystal compound of the formula (1) ##STR1## wherein R is a linear alkyl group having 6 to 12 carbon atoms,both X and Y are hydrogen atoms or one of X and Y is a fluorine atom and the other is a hydrogen atom,A is --CF.sub.3 or --C.sub.2 F.sub.5,m is an integer of 2 to 4,n is an integer of 2 to 4, andC* is an asymmetric carbon,having a ferrielectric phase in its phase sequence, or a ferrielectric liquid crystal composition containing the liquid crystal compound of the formula (1) having a ferrielectric phase, may be injected between substrates provided with nonlinear active elements, such as thin film transistors or diodes formed on each pixel, to form an active matrix liquid crystal display device.

Abstract: There are described new amino acid amide derivatives, some of which are known, of the formula (I) ##STR1## in which R.sup.1 to R.sup.8 have the meaning given in the description, and a process for their preparation. The amino acid amide derivatives of the formula (I) are used for the preparation of pesticides.

Abstract: The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.

Abstract: N-arylmethylene ethylenediaminetriacetate, N-arylmethylene iminodiacetate or N,N'-diarylmethylene ethylenediaminediacetate type compounds and their use in combatting oxidative stress, and pharmaceutical and cosmetic compositions comprising said compounds. The invention also concerns a process for the preparation of said compounds.

Abstract: This invention is directed to a method for making an iodopropargyl carbamate in an aqueous reaction medium so as to yield a more pure and stable, e.g., U.V. resistant, product in a high yield, free from environmental hazards posed by using non-aqueous solvents as the reaction medium.

Abstract: Novel tricyclic triazolo derivatives and pharmaceutically acceptable salts thereof, which are useful as anti-inflammation agents, anti-allergy agents or anti-PAF agents as well as processes for producing the same are disclosed. The triazolo derivatives of the present invention are represented by the formula (I): ##STR1## ?wherein R.sup.1 represents hydrogen, lower alkyl or C.sub.3 -C.sub.5 cycloalkyl; R.sup.2 and R.sup.3 respectively represent hydrogen, lower alkyl, lower alkoxy or halogen; W represents C.dbd.O or CR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 respectively represents hydrogen or lower alkyl); A represents C.sub.1 -C.sub.5 straight or branched saturated or unsaturated alkylene which may contain one or more hetero atoms; l represents 0 to 2, n represents 1 to 3, . . . represents single bond or double bond; Y represents N or C; Z represents C(B)Ar.sup.1 Ar.sup.2 (wherein B represents hydrogen, hydroxy or methoxy, Ar.sup.1 and Ar.sup.

Abstract: There are disclosed (+)2-benzoyl-3-[prop-2(S)-yl)amino] acrylate derivatives of following the formula and a method for the preparation of the same; ##STR1## wherein X is a halogen; X.sub.1 and X.sub.2 are independently selected from a halogen and a nitro; and R and R.sub.1 each is an alkyl group containing 1 to 4 carbon atoms.

Abstract: The present invention relates to benzoquinazoline thymidylate synthase inhibitors, processes for preparing them and pharmaceutical formulations containing them.

Abstract: An N-substituted phenylcarbamic acid derivative represented by the general formula (I): ##STR1## [wherein R.sup.1 is H, a (C.sub.1-6)alkyl group, a halo(C.sub.1-6)alkyl group, a (C.sub.1-6)alkoxy(C.sub.1-6)alkyl group, a (C.sub.2-6)alkenyl group, a (C.sub.2-6)alkynyl group or a halo(C.sub.1-6)alkoxy(C.sub.1-6)alkyl group, R.sup.2 is H, a (C.sub.1-6)alkyl group, a halo(C.sub.1-6)alkyl group, a (C.sub.1-6)alkoxy(C.sub.1-6)alkyl group, a (C.sub.2-6)alkenyl group, a (C.sub.2-6)alkynyl group, a halo(C.sub.1-6)alkoxy(C.sub.1-6)alkyl group or a cyano(C.sub.1-6)alkyl group, R.sup.3 is a (C.sub.1-6)alkyl group or a halo(C.sub.1-6)alkyl group, each of R.sup.4 and R.sup.5 is a specific group, and Y is O or S] which is very effective in controlling powdery mildew, scab, late blight and gray mold; a process for producing said derivative; an agricultural and horticultural fungicide containing said derivative as an active ingredient; an intermediate of said derivative; and a process for producing the intermediate.

Abstract: Pyrimido[4,5-g]quinazoline quinone derivatives were synthesized as anthranone-like reductive alkylating agents. Like many naturally-occurring antibiotics, these quinone derivatives are designed to afford an alkylating quinone methide species upon reduction and leaving group elimination. Kinetic studies of pyrimido[4,5-g]quinazoline hydroquinones provided evidence of quinone methide intermediates able to trap nucleophiles (alkylation) and protons. The rate of quinone methide formation is determined by the hydroquinone free energy. Thus, a linear free energy relationship for quinone methide formation was obtained by plotting rates of quinone methide formation, as the log, versus the quinone reduction potential. The pyrimido[4-5-g]quinazoline quinone methides fall on this free energy plot, showing that these species are formed by the same mechanism as the other structurally-diverse quinone methides previously studied in this research group.

Abstract: The invention relates to caged compounds for the study of biological processes, where the caged compound has a photoremoveable .alpha.-carboxy-substituted o-nitrobenzyl group. Covalent attachment of the substituted o-nitrobenzyl to a parent compound yields a caged compound with biological and/or physical properties that are significantly altered from the original properties of the parent compound. Illumination of the caged compounds to cleave the photoremoveable group yields the parent compound with its original properties restored.

Abstract: N-arylmethylene ethylenediaminetriacetate, N-arylmethylene iminodiacetate or N,N'-diarylmethylene ethylenediaminediacetate type compounds and their use in combatting oxidative stress, and pharmaceutical and cosmetic compositions comprising said compounds. The invention also concerns a process for the preparation of said compounds.

Abstract: The invention relates to novel asymmetrically substituted diaminodicarboxylic acid derivatives of the formula ##STR1##

Abstract: Polylactone aromatic esters having the formula: ##STR1## wherein R.sub.1 is a hydrocarbyl group having a sufficient number of carbon atoms to render the compound soluble in hydrocarbons boiling in the gasoline or diesel fuel range;R.sub.2 is an alkylene group of about 2 to 5 carbon atoms;R.sub.3 and R.sub.4 are each independently hydrogen, hydroxy, nitro, amino, N-alkylamino having 1 to 6 carbon atoms in the alkyl group, or N,N-dialkylamino having 1 to 6 carbon atoms in each alkyl group, provided that R.sub.3 and R.sub.4 may not both be hydrogen;and x is an integer from 1 to 25.The polylactone aromatic esters of formula I are useful as fuel additives for the prevention and control of engine deposits.

Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.

Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.

Abstract: A process for the preparation of 2-chloro-4,5-difluorobenzoic acid and 2,4,5-trifluorobenzoic acid as well as synthetic intermediates useful in and prepared according thereto, comprising reacting a nitrobenzene having the formula ##STR1## wherein X is chloro or fluoro, with an appropriate carbanion to form a compound having the formula ##STR2## wherein one of Y and Z is chloro and the other is nitro, and R is a radical selected from the group consisting of --CCl.sub.3, --CH.sub.2 NO.sub.2, --CH(NO.sub.2)R.sup.1, --CH(CO.sub.2 R.sup.1).sub.2, --CH(C(O)R.sup.2).sub.2, --CH(CN)CO.sub.2 R.sup.1, --CH(CO.sub.2 R.sup.1)COR.sup.2 and --COR.sup.2 where R.sup.1 is alkyl or arylalkyl and R.sup.2 is alkyl, aryl or arylalkyl and, where appearing more than once in such a radical, R.sup.1 and R.sup.2 may be the same or different at each occurrence.