Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.

Abstract: An increase in the disastereoselectivity resulting from the reaction of a phosphinic acid ester of the formula ##STR1## with the halo ester of the formula ##STR2## is achieved by carrying out the reaction in the presence of 4-methylmorpholine, diazabicyclooctane, quinuclidine, 1-methylpyrolidine, or cinchonidine. After removal of the R.sub.3 protecting group and fractional crystallization, the resulting desired diastereomeric pair can be resolved, and the desired isomer can be coupled to 4-substituted L-proline to give compounds possessing angiotensin converting enzyme inhibition activity. In particular, the process is useful in producing the antihypertensive agent fosinopril sodium in increased yields.

Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.

Abstract: A method is disclosed for the sulfurization of a phosphorus containing compound, which comprises: solubilizing the phosphorous containing compound and then contacting the phosphorous containing compound, with a sulfur containing compound of the solution formula: ##STR1## wherein, B is selected from the group consisting of --CH.sub.2 --, --C(O)-- or --C(S)--;Q is a non-interfering moiety or radical; andm and n, same or different, are selected from the group consisting of zero or one.

Abstract: A novel triphenylphosphonium salts of chloromethyl pyrrolidone having the formula: ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 may be the same or different and may be hydrogen, lower alkyl, lower alkoxy, lower alkenyl, lower cycloalkyl, and lower carboalkoxy, phenyl, substituted phenyl, naphthyl, and substituted naphthyl, R.sub.4 is lower alkyl or phenyl and X is an anion. The compounds are useful in Wittig-type reactions and as phase transfer catalysts. A method for preparing the inventive compound is also disclosed.

Abstract: Novel derivatives of monophosphoryl lipid A and a process for their preparation are provided. The derivatives contain one or more free groups, such as an amine, on a side chain attached to the primary hydroxyl groups of the monophosphoryl lipid A nucleus through an ester group. The derivatives provide a convenient method for coupling the lipid A through coupling agents to various biologically active materials, substrates, and the like, wherein the immunostimulant properties of lipid A are desired.

Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## according to claim 1. These compounds are useful for the treatment or prophylaxis of calcium metabolism disturbance or disease.

Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) or (II): ##STR1## wherein position 5 of the polyhydronaphthyl ring is singly or doubly bonded to oxygen or incorporated into a C.sub.3-7 carbocyclic ring.

Abstract: Novel nucleophilic tertiary organophosphines and the specific cleavage of peptide bonds by nucleophilic tertiary organophosphines. This invention is of particular utility in providing chemical agents for use in the cleavage of proteins and the determination of the amino acid sequence of proteins.

Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein W is selected from the group consisting of methyl and phenyl optionally substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and phenyl; r, n, m and a are integers such that the expression r+(n+1)m+a is also an integer and has a value of 3 to 20; r is greater than or equal to 2; n is greater than or equal to 2; m is greater than or equal to zero and a is greater than or equal to zero; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Q is a bivalent radical selected from --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer 2-12 and the moiety --(CHR.sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.

Abstract: Compounds of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 is cycloalkyl of 5 to 7 carbon atoms; aryl of 6 to 10 carbon atoms unsubstituted or substituted by straight or branched chain alkyl of 1 to 4 carbon atoms, halo or trifluoromethyl; or ##STR2## wherein A is oxygen, sulfur or NR.sup.5, wherein R.sup.5 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo, and R.sup.6 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo;R.sup.2 is straight or branched chain alkyl of 1 to 4 carbon atoms or cycloalkyl of 5 to 7 carbon atoms; andR.sup.3 and R.sup.4 are the same or different and each is hydrogen; straight or branched chain alkyl of 1 to 8 carbon atoms unsubstituted or substituted by hydroxy, acyloxy of 2 to 5 carbon atoms, carboxyl or carbamoyl;are useful for treating pain, inflammation and fever in humans and animals.

Abstract: The invention relates to novel compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkoxycarbonyl, phenylsulfonyl, phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, nitro, lower alkoxy, mono (or di or tri)halo(lower)alkyl and lower alkyl, phenylcarbamoyl, lower alkylsulfonyl, benzoyl or thienylsulfonyl;R.sup.2 is phenylsulfonyl or phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy and mono(or di or tri)halo(lower)alkyl,R.sup.3 is carboxy(lower)alkyl, lower alkyl substituted with carboxy and 1 to 3 halogen atom(s), esterified carboxy(lower)alkyl, carbamoyl(lower)alkyl, lower alkylsulfonylcarbamoyl(lower)alkyl, phenylsulfonylcarbamoyl(lower)alkyl, carboxyphenyl, esterified carboxyphenyl, carboxy, esterified carboxy, hydroxy(lower)alkyl, sulfino(lower)alkyl, phosphono(lower)alkyl, di(lower)alkoxyphosphoryl(lower)alkyl or halo(lower)alkyl,R.sup.

Abstract: Oligonucleotide functionalizing reagents are disclosed which are useful in introducing sulfhydryl, amino and additional hydroxyl groups into oligonucleotides. The reagents are substantially linear in structure, at one end provided with a phosphoramidite moiety, at an opposing end provided with a sulfhydryl, amino or hydroxyl moiety, the two ends linked through a hydrophilic spacer chain. Methods of using and synthesizing the novel reagents are disclosed as well.

Abstract: The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-meth

Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by stuctural formulae (I) and (II): ##STR1## wherein A is O, S(O).sub.n or N--R.sub.13.

Abstract: Compounds of formula (I): ##STR1## (wherein: l is 2-4; A and B are oxygen or sulfur; one of R.sup.1 and R.sup.2 represents a long chain alkyl, alkylcarbamoyl or aliphatic acyl group and the other of R.sup.1 and R.sup.2 represents a group of formula (III) or (II.sub.f): ##STR2## in which E represents a single bond, a bivalent heterocyclic group or a group of formula --CO--, --COO-- or --CONR.sup.6 --, where R.sup.6 is hydrogen or an imino-protecting group; m is 0-3; n is 0-10; q is 0 or 1; R.sup.4 is optionally protected hydroxy, mercapto group or carboxy; Q is an amino or nitrogen-containing heterocyclic group;R.sub.f.sup.4 R.sub.f.sup.5 and R.sub.f.sup.6 are independently selected from the group consisting of hydrogen atoms and C.sub.1 -C.sub.6 alkyl groups, or R.sub.f.sup.4 and R.sub.f.sup.5 or R.sub.f.sup.4, R.sub.f.sup.5 and R.sub.f.sup.

Abstract: Hypotensive activity is exhibited by compounds having the formulas ##STR1##

Abstract: Novel alkoxycarbonylalkylalkylphospholipids and alkylaminocarbonylalkylphospholipids of the formula ##STR1## wherein A.sup.1 is a bivalent radical of the formula --C.sub.m H.sub.2m --wherein m is an integer having a value from 0 to 20, inclusive; A.sup.2 is a bivalent radical of the formula --C.sub.p H.sub.2p --wherein p is an integer having a value from 2 to 6, inclusive; X is a bivalent radial of the formula --O--or --N(R)--wherein R is selected from the group consisting of hydrogen, alkyl radicals having up to 6 carbon atoms, inclusive and phenyl radicals of the formula: ##STR2## where Z and a are as difined in the specification; Y is ##STR3## wherein R.sup.1 is an anlkyl radicals having up to 6 carbon atoms, inclusive and R.sup.2 and R.sup.3 are independently alkyl radicals having up to 6 carbon atoms, inclusive, or taken together with R.sup.1 and the nitrogen atom to which they are attached form a group of the formula ##STR4## wherein r is 0 or 1, and W is oxygen, CH.sub.2, sulfur or N(R.sup.

Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.

Abstract: Aromatically substituted azacycloalkylalkanediphosphonic acids of the formula ##STR1## in which R represents an aromatically substituted azacycloaliphatyl radical that is bonded to the group alk by way of a nitrogen atom and that optionally contains an additional nitrogen atom, and alk represents a divalent aliphatic radical, and their salts, can be used for the treatment of illnesses that can be attributed to calcium metabolism disorders. They are manufactured, for example, by reacting a compound of the formulaR--alk--X.sub.3 (IV)in which X.sub.3 represents carboxy, carbamoyl or cyano, with phosphorus acid and phosphorus trichloride and in an intermediate of the formula ##STR2## obtained by starting from compounds of the formula IV in which X.sub.3 represents cyano or carbamoyl and by working up by hydrolysis, or in a salt thereof, replacing the amino group by hydroxy by treatment with nitrous acid.

Abstract: This invention relates to a process for producing phosphonitrile oligomers containing maleimido phenoxy groups.

Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts wherein Z completes a cycloalkyl ring, a substituted cycloalkyl ring, a cycloalkenyl ring, a substituted cycloalkenyl ring or a saturated heteroalkyl ring; R.sub.2 is lower alkyl, aralkyl or aminoalkyl and X is an amino or imino acid. The compounds possess angiotensin converting enzyme inhibition activity.

Abstract: The invention provides azetidinones of the formula ##STR1## where R.sub.4 is hydrogen, amino or protected amino; R.sup.0 is H when R.sub.4 is amino or protected amino, or C.sub.1 -C.sub.4 alkyl when R.sub.4 is H; R.sub.1 is H, CH.sub.3, --CH.sub.2 --.sub.n Y where Y is OH, protected OH, --CH.sub.2 OH, protected --CH.sub.2 OH, halogen, COOH or protected COOH; n is 1 or 2; --CH.sub.2 --C(O)SR.sub.1 ' where R.sub.1 ' is e.g., C.sub.1 -C.sub.4 alkyl; R.sub.2 is H or protecting group and R.sub.3 is e.g., alkyl or phenyl. The azetidinones obtained are useful intermediates to carbapenems and carbacephems and monocyclic antibacterials, e.g., .alpha.-(dialkylphosphono)-[[3.beta.-[2-(2-aminothiazol-4-yl)-2-(syn)metho xyiminoacetylamino]azetidin-2-one-1-yl]]acetic acid and pharmaceutically acceptable salts thereof.

Abstract: The present invention discloses a new class of calcium chelating compounds which have a decreased affinity for calcium following illumination. These new compounds contain a photolabile nitrobenzyl derivative coupled to a tetracarboxylate Ca.sup.2+ chelating parent compound having the octacoordinate chelating groups characteristic of EGTA or BAPTA. However unlike EGTA or BAPTA-like compounds, in which the two halves of the chelator are linked by a simple 1,2-ethanediyl moiety, the compounds of the present invention modify the stereochemical conformation of this linkage by adding bulky substituents or incorporating the linkage into a carbocyclic or heterocyclic ring. In a first form, the new compounds are comprised of a BAPTA-like chelator coupled to a single 2-nitrobenzyl derivative, which in turn is a photochemical precursor of a 2-nitrosobenzophenone.

Abstract: Described are phosphatidyl compounds of the formula I ##STR1## in which R.sup.1 represents C.sub.3-14 -alkanoyl, benzoyl, the acyl radical of an .alpha.-aminocarboxylic acid that is other than glycine, L-alanine and derivatives thereof having a substituted amino group, and of which the .alpha.-amino group may be substituted by lower alkanoyl, lower alkoxycarbonyl or by benzyloxycarbonyl, or the acyl radical of a .beta.-aminocarboxylic acid or an .alpha.- or .beta.-hydroxycarboxylic acid,T represents a group NH that is unsubstituted or is substituted by lower alkyl, or oxygen,Y represents dimethylene that is unsubstituted or is substituted by free, etherified or amidated carboxy,W represents hydrogen, andZ represents a 1,2-dihydroxyethyl, 2-hydroxyethyl or hydroxymethyl group, in which at least one of the hydroxy groups is esterified by an aliphatic C.sub.8-30 -carboxylic acid or is etherified by an aliphaticC.sub.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 denote alkyl, OH, CF.sub.3 or cyanoethyl, A preferably denotes --COOH, R.sub.3 denotes inter alia alkoxycarbonylalkoxy, fairly high-molecular (>C.sub.12) alkoxy, alkylcarbonylalkoxy or nitrobenzyloxy, are valuable herbicides and growth regulators.

Abstract: Disclosed are nadimido-substituted cyclophosphazene derivatives and thermosets thereof. The thermosets are useful as high temperature, flame resistant matrices for composites and as metal adhesives.

Abstract: The present invention is concerned with the phosphonic acids of formula I ##STR1## wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di-esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl, 2-carboxyperhydroindolyl, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents B--X--D wherein B represents a direct bond, or straight chain or branched lower alkylene; X represents O, S, SO, SO.sub.2, CO--NR.sub.b, R.sub.b N--CO or N--Ra; Ra represents hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl; R.sub.

Abstract: This invention is directed to orally active antihypertensive agents of the formula ##STR1## wherein R.sub.1 is certain alkyl or aralkyl groups.

Abstract: Novel compounds useful as dopamine receptor agonists for the treatment of various diseases of the central nervous system such as Parkinson's disease and related disorders having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is selected from the group consisting of hydrocarbyl radicals; ##STR2## where X is S or O: and pharmaceutically acceptable salts thereof. Also disclosed is a method for inducing a dopaminergic response in a patient by adminstering a pharmacologically-effective amount of one of the foregoing compounds.

Abstract: Phosphorus containing compounds of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid and A is ##STR2## These compounds possess angiotensin converting enzyme activity and are thus useful as hypertensive agents.

Abstract: A compound provided by the present invention, of the formula ##STR1## wherein R.sup.1 is C.sub.14-20 alkyl; R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-5 alkyl, or ##STR2## represents a cyclic ammonio group; and A is C.sub.2-5 alkylene, and a pharmaceutically acceptable salt thereof, are useful as a anti-tumor agent.

Abstract: An electrolyte for electrolytic capacitor containing within an aprotic solvent a fluorocomplex acid salt of a N-heterocyclic compound as solute.An electrolyte for electrolytic capacitor according to the invention may conveniently be prepared by adding to an aqueous solution of fluorocomplex acid salt an equivalent amount of N-heterocyclic compound for reaction with subsequent dryness at reduced pressure to obtain an anhydrous salt which is then added to the aprotic solvent to prepare the resultant electrolyte having desired conductivity.

Abstract: Compounds of the general formula ##STR1## wherein two of the residues R.sup.1, R.sup.2 and R.sup.3 represent C.sub.10-30 -alkyl residues with at least 8 C-atoms in a straight chain, at least one of these residues being substituted by at least 2 C.sub.1-3 -alkyl residues and the sum of the C-atoms in the two residues being greater than 20; and the third residue is a residue --P(O)(O.sup.-)OR.sup.4 in which R.sup.4 represents a lower-alkyl or C.sub.5-7 -cycloalkyl residue which is substituted by a quaternary ammonium group or a C.sub.5-7 -cycloalkyl residue which contains a di-(lower-alkyl)-substituted nitrogen atom,are useful for the manufacture of colloidal solution systems. The compounds of formula I can be prepared starting from glycerol derivatives as described in more detail in the specification.

Abstract: The subject invention pertains to a novel class of fire- and heat-resistant bisimide resins prepared by thermal polymerization of maleimido or citraconimido substituted 1-[(dialkoxyphosphonyl)methyl]-2-4 and -2,6-diaminobenzenes. Typical polymer precursors have the chemical structure: ##STR1## wherein R is alkyl, substituted alkyl or aryl, and R.sup.1 is hydrogen or lower alkyl.The polymer precursors are prepared by reacting 1-[(diorganooxyphosphonyl)methyl]-2-4- and -2,6-diaminobenzenes with maleic anhydride or citraconic anhydride in a mole ratio 1:2. Chain extension of the monomers is achieved by reacting the mono-N-maleimido derivatives of 1-[(diorganooxyphosphonyl)methyl]-2,4 and -2,6-diaminobenzenes with aryl tetracarboxylic dianhydrides, such as benzophenone tetracarboxylic dianhydride, or aryl diisocyanates, such as methylenebis(4-phenylisocyanate), in a mole ratio 2:1.

Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.

Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another or also together, signify hydrogen atoms or lower alkyl radicals, whereby R.sub.1 and X or R.sub.3 and Y or R.sub.4 and Z, together with the nitrogen atom to which they are attached, can form a five- or six-membered ring, X and Y, which can be the same or different, represent a straight-chained or branched alkylene chain with up to 6 carbon atoms which can optionally be substituted by aromatic or heteroaromatic radicals, Z is a straight-chained or branched alkylene chain with up to 6 carbon atoms, which can be interrupted by heteroatoms and can optionally also be substituted by aromatic or heteroaromatic radicals, n is 0, 1 or 2 and A is a hydrogen atom or a hydroxyl group, and the pharmacologically acceptable salts thereof.

Abstract: This invention relates to a new class of organic chemical compounds. More particularly, this invention is concerned with amido and hydrazido derivatives of N-phosphinothioylmethylglycine esters. This class of compounds has been found to be useful as herbicides.

Abstract: A novel phospholipid of the formula: ##STR1## wherein R.sup.1 is an alkyl group of 10 to 24 carbon atoms, R.sup.2 is a cyclic imide group and A.sup.+ is a cyclic ammonio group and a salt thereof have platelet activating factor inhibiting activity and are useful for prevention and treatment of circulatory disorders and allergic bronchial asthma.

Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more o-diaminophosphinyl derivatives of oximes, and methods and composition for inhibiting the activity of urease through use of such compounds.

Abstract: Oxime N-alkyl-N-.alpha.-(alkylthio-phosphorothio)acyl carbamates represented the structure: ##STR1## wherein the R represents various imino radicals, Q is oxygen or sulfur and the numbered R groups represent various alkyl substituents, which exhibit superior insecticidal and miticidal activity.

Abstract: Amine-containing dispersants, such as succinimides, Mannich Bases and Viscosity-index improvers are reacted with fluorophosphoric acid. The reaction of the dispersant with the fluorophosphoric acid passivates the dispersant to fluorocarbon compositions used as seals, for example in automobile engines.

Abstract: A process for producing a water-soluble dicarboxylic acid imide compound which comprises adding a primary amine compound to an aqueous solution of a water-soluble salt of a dicarboxylic acid compound containing at least one dicarboxylic acid unit capable of forming a 5-membered cyclic acid imide linkage and heating the mixture to introduce an acid imide linkage into the molecule.

Abstract: Amino-phosphonates are prepared by reacting an enamine with a phosphite ester, for example, according to the equation ##STR1## where OR' is an alcohol moiety and NR.sub.2 is an amino moiety, both R and R' being preferably hydrocarbon such as alkyl or R.sub.2 is part of a ring structure. These compounds have many uses, for example, as corrosion inhibitors, scale inhibitors, fuel stabilizers, etc. In addition, amino-phosphonates can be converted to alpha, beta - unsaturated phosphonates according to the equation ##STR2## which are useful in forming flame retardant polymers and copolymers.

Abstract: Angiotensin converted enzyme inhibitor activity if exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is hydrogen, aryl, or heteroaryl; R.sub.2 is hydrogen, amino, alkanoylamino, arylcarbonylamino, or heteroarylcarbonylamino;R.sub.3 is hydrogen, alkyl, or aminoalkyl;R.sub.4 and R.sub.5 are the same or different and each is hydrogen, alkyl, halogen, aryl, arylalkyl, hydroxy, alkoxy, alkylthio, aryloxy, arylthio, or cycloalkyl, or R.sub.4 and R.sub.5 taken together are oxo, ethylenedithio or propylenedithio;one of R.sub.6 and R.sub.7 is ##STR2## and the other is hydrogen, alkyl or arylalkyl; R.sub.8 is hydrogen, alkl or aryl;R.sub.9 is hydrogen or alkyl;n is 0 or an integer of 1 to 8;m is 0 or 1; andA is --(CH.sub.2).sub.p --wherein p is 0 or 1, --NH--, or --O--.

Abstract: The present invention encompasses a method for determining ligands in test samples comprising intermixing with the test sample a ligand analog-irreversible enzyme inhibitor conjugate and a binding protein bindable to the ligand and the ligand analog-irreversible enzyme inhibitor conjugate and wherein the amount of ligand analog-irreversible enzyme inhibitor conjugate bound by the binding protein is related to the amount of ligand in the test sample, said binding protein inactivating the irreversible enzyme inhibitor when bound to the ligand analog portion of the conjugate; intermixing an enzyme which is irreversibly inhibited by the ligand analog-irreversible enzyme inhibitor conjugate unbound by the binding protein; and intermixing substrate to the enzyme and monitoring the enzyme substrate reaction.The invention also includes ligand analog-irreversible enzyme inhibitor conjugates useful as reagents in practicing the method.

Abstract: 4-Aminophenoxy cyclotriphosphazenes are reacted with maleic anhydride to produce maleamic acids which are converted to the maleimides. The maleimides are polymerized. By selection of starting materials (e.g. hexakis amino or trisaminophenoxy-trisphenoxy-cyclotriphosphazenes), selection of molar proportions of reactants, use of mixtures of anhydrides and use of dianhydrides as bridging groups a variety of maleimides and polymers are produced. The polymers have high limiting oxygen indices, high char yields and other useful heat and fire resistant properties making them useful as, for example, impregnants of fabrics.

Abstract: Novel anilide derivatives of the formulaZ--ArwhereinZ is a heterocyclic ring system attached to Ar through a ring nitrogen atom in Z, andAr is a substituted phenyl ring, exhibit good control of broadleaf weeds and safety to important crops at low application rates.

Abstract: A method is provided for inhibiting onset of or treating migraine headache by administering an ACE inhibitor, such as captopril, alone or in combination with a calcium channel blocker such as diltiazem or nifedipine, over a prolonged period of treatment.