Abstract: The invention provides a novel bleaching composition comprising:(a) an oxidatively stable bleach activator having the structure ##STR1## wherein Y.sub.1, Y.sub.3 and Y.sub.4 each represents a bridging group, i.e., zero, one, two or three carbon containing nodes for substitution, while Y.sub.2 is a bridging group of at least one carbon containing node for substitution, each said node containing a C(R), C(R.sub.1)(R.sub.2), or a C(R).sub.2 unit and each R substituent is the same or different from the remaining R substituents and is selected from the group consisting of H, alkyl, cycloalkyl, cycloalkenyl, alkenyl, aryl, alkynyl, alkylaryl, halogen, alkoxy, or phenoxy, CH.sub.2 CF.sub.3, CF.sub.3 and combinations thereof, or form a substituted or unsubstituted benzene ring of which two carbon atoms in the ring form notes in the Y unit, or together with a paired R substituent bound to the same carbon atom form a cycloalkyl or cycloalkenyl ring, which may include an atom other than carbon, e.g.

Abstract: A process for the isolation of cyclosporin A comprising the steps of: adding a lower alkanol solvent to a culture fluid of a mutant of Tolypocladium inflatum to form a mixture, filtering the mixture to form an extract, transferring the extract to methylene chloride as a solvent therefor, and column chromatographing the resultant product on silica gel.

Abstract: Dendroamide derivatives are disclosed which are useful in cancer therapy, especially in treating multidrug resistant cells.

Abstract: Compounds having utility as light absorbing compounds, especially in the area of photodynamic therapy. Such compounds have the formula: ##STR1## where z is .dbd.O or NR.sub.14 ; R.sub.14 is alkyl or substituted alkyl; R.sub.1 is an amino acid group, a polyamine group, a polyether group or OR.sub.13 where R.sub.13 is alkyl; R.sub.4 through R.sub.11 are --H, --OH alkyl, alkoxy, alkenyl, alkylene, aryl, or aryloxy, or a carbonyl containing group, wherein carbon containing groups may be substituted with carbonyl, hydroxy, phosphoro, carboxy, halo, sulfo, amino and ether substituents, provided that; R.sub.4 may be taken together with R.sub.7 to form .dbd.O; R.sub.8 may be taken together with R.sub.9 to form .dbd.O; R.sub.10 may be taken together with R.sub.11 to form .dbd.O; and R.sub.4 and R.sub.7 may together form a chemical bond and R.sub.8 and R.sub.11 may together form a chemical bond; and R.sub.12 is hydrogen or lower alkyl; provided that if one z is O, the other z is --NR.sub.14.

Abstract: A robust chelate complex is provided having the formula: ##STR1## wherein M is a metal, preferably a transition metal; Z is an anionic donor atom, at least three of which are nitrogen and the other is preferably nitrogen or oxygen; L.sub.1 is a labile ligand;Ch.sub.1, Ch.sub.2 and Ch.sub.3 are oxidation resistant chelate groups which are the same or different and which form 5 or 6 membered rings with the metal, and Ch.sub.4 is a chelate group having the structure ##STR2## wherein R.sub.1 and R.sub.2 are the same or different and are preferably selected from the group consisting of hydrogen, halogen, methyl, and CF.sub.3 or when linked, a five or six membered ring cyclo substituent. The complex provides a stable, long-lived oxidation catalyst or catalyst activator.

Abstract: The present invention relates to N-heterocyclic-containing macrocyclic hydroxyethylamine protease inhibitor compounds, compositions and methods for inhibiting retroviral proteases.

Abstract: Macrocycle compounds of precise molecular geometry are disclosed and claimed, useful for a variety of purposes including membranes, molecular recognition and any other purpose where specific molecular macrogeometry is important. Most preferably, the macrocycles are of the imide class, formed by way of reactions of diamines with .alpha.-anhydride, .omega.-nitro compounds, followed by cyclization with an acid chloride.

Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.

Abstract: A compound according to the formula: ##STR1## and conjugates thereof.

Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.

Abstract: Compounds of formula (I): ##STR1## as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption diseases, such as osteoporosis.

Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has anexcellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Abstract: Disclosed herein are cyclic oligomers comprising substituted or unsubstituted m-phenylene isophthalamide, complexes of these oligomers with selected metal salts, novel methods for their preparation, and polymerization of the cyclic oligomers to linear aramids. The aramids are useful, for example, as fibers for fire resistant clothing. Amino-finctional cyclic oligomers may be reacted with polyfunctional acyl halides to produce polyamides.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The invention is directed to a novel compound of formula ##STR1## in which R is a hydroxyl, alkyloxy, phenylalkyloxy or --NH--CH.sub.2 --COOH radical, R' and R" are identical and are each a hydroxy or methoxy radical and R'" represents a hydrogen, bromine, chlorine or iodine atom or a nitro radical. The invention is also directed to the salts of said compounds and their use.

Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R1, R2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.

Abstract: The present invention relates to heat-curable, cyclic isocyanate addition productsi) which are the reaction products of a polyisocyanate having two or more isocyanate groups with a compound containing two or more isocyanate-reactive groups andii) in which at least 10% by weight of the reaction products are in the form of cyclic groups containing urea and/or urethane groups.The present invention also relates to a process for the preparation of these cyclic isocyanate addition products and to the products obtained by curing these compositions at elevated temperatures, e.g., coatings, adhesives, molded articles, elastomers and foams.

Abstract: Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.

Abstract: A benzolactam derivative represented by the following formula (I): ##STR1## wherein n represents an integer of from 1 to 3; R.sup.1 represents a straight- or branched-chain alkyl group or an aralkyl group; R.sup.2 represents a straight- or branched-chain alkyl group; R.sup.3 and R.sup.4 independently represent a hydrogen atom or a straight- or branched-chain alkyl group, and when R.sup.3 and R.sup.4 are adjacent each other on the phenyl group, they may be combined to form a cycloalkyl ring together with two carbon atoms of the phenyl group to which R.sup.3 and R.sup.4 bind, and said cycloalkyl ring may optionally have one or more substituents; and a anti-retroviral agent comprising the same as an active ingredient.

Abstract: This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR.sup.1.sub.2 Y;each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract: A compound (I) is prepared by reaction of at least one (meth) acrylate (II) with a heterocyclic alcohol (III), in the presence of at least one catalyst chosen from the chelates of calcium with 1,3-dicarbonyl compounds, such as calcium acetylacetonate. ##STR1## R.sup.1 =H, CH.sub.3 ; A, B=C.sub.2 -C.sub.5 alkylene; R.sup.2 =C.sub.1 -C.sub.4 alkyl.

Abstract: The present invention provides novel cyclic tetrapeptides useful in the treatment or prevention of protozoal diseases; in particular, the novel compounds are active against the causative pathogens in malaria, toxoplasmosis, and coccidiosis.

Abstract: A compound (I) is prepared by reacting at least one (meth)acrylate (II) with a heterocyclic alcohol (III), in the presence of a catalyst consisting of a mixture formed (a) of at least one magnesium alkoxide and (b) of a component chosen from the chelates of calcium with 1,3-dicarbonyl compounds, dialkyltin oxides, dialkyltin alkoxides and dialkyltin diesters. ##STR1## R=C.sub.1 -C.sub.4 alkyl. R.sup.1 =H, CH.sub.3 ; A, B=straight or branched C.sub.2 -C.sub.5 hydrocarbon chain; R.sup.2 =C.sub.1 -C.sub.4 alkyl.

Abstract: There are disclosed certain novel compounds identified as heterocyclic-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such heterocyclic-fused lactams as the active ingredient thereof are also disclosed.

Abstract: The invention relates to bisquaternary ammonium compounds of the formula (I) ##STR1## and their preparation, where: R.sup.1, R.sup.2, R.sup.3 are, for example, identical or different (C.sub.1 -C.sub.12)alkyl which can also contain oxygen atoms or N--R.sup.4 moieties, where R.sup.4 is (C.sub.1 -C.sub.4)alkyl, in the chain and A is a chlorine, bromine, iodine atom or a OSO.sub.3 R.sup.5 radical, where R.sup.5 is (C.sub.1 -C.sub.4) alkyl or aryl.

Abstract: The subject invention provides chiral receptor molecules having the structure: ##STR1## wherein A has the structure: ##STR2## and R.sub.1 and R.sub.2 are independently the same or different and are H, F, alkyl, aryl, etc.; X is CH.sub.2 or NH; Y is C.dbd.O or SO.sub.2 ; and n is 0 to about 3; which are useful for the purification of enantiomers of amino acid derivatives and other compounds. The subject invention also provides methods of preparing said receptor molecules.

Abstract: The present invention relates to a composition having the general formula: ##STR1## wherein each of A, B, C, X, Y, and Z is independently O, NH, N(CH.sub.2).sub.m CH.sub.3, N(C.dbd.O) (CH.sub.2).sub.m CH.sub.3, CH.sub.2, S, or Se; each of R.sub.1, R.sub.2, and R.sub.3 is independently phenyl, 4-hydroxyphenyl, pyridyl, pyrrolyl, indolyl, naphthyl, thiophenyl, (C.dbd.O) (CH.sub.2).sub.p CH.sub.3, NH(C.dbd.O) (CH.sub.2).sub.p CH.sub.3, OH, COOH, NH.sub.2, or SH; and m, n, and p are integers between 0 and 5. The composition is a chiral receptor molecule useful for the purification of enantiomers of derivatives of amino acids and of compounds able to form hydrogen bonds. The preparation of the composition involves coupling a trifunctional aromatic molecule with three protected chiral molecules at the three aromatic groups, cleaving protecting groups, and joining adjacent chiral groups by multiple lactamizations.

Abstract: Described is a process for producing (meth)acrylates with Formula (I) ##STR1## with R.sub.1 is H or CH.sub.3, and A and B are each independently unbranched or branched alkylene groups with 2 to 5 C atoms, comprising the step of reacting a (meth)acrylate of the Formula (II), ##STR2## wherein R.sub.2 is alkyl especially with 1 to 4 C atoms and R.sub.1 is as defined above, with an alcohol of the Formula (III) ##STR3## wherein A and B are as defined above in the presence of an alkali earth catalyst or alkaline earth metal catalyst or a mixture thereof.

Abstract: The present invention provides an efficient process of reacting a bis-indolyl acid of the Formula (II): ##STR1## wherein R.sup.1 is a hydrogen or C.sub.1 -C.sub.4 alkyl and R, X, and Y are optional substitutions; to produce a bis-indolyloxallic acid of the Formula (III): ##STR2## Compounds of the Formula (III) are readily converted to the bis-indolylmaleimides.

Abstract: Macrocyclic chelating agents, optionally possessing more than one macrocyclic ring having at least two peptide linkages within the macrocyclic skeleton. The chelating agents are used for the preparation of paramagnetic metal chelates for use as MRI contrast agents.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract: This invention relates to a method of inhibiting platelet aggregation using 1,4-diazocine compounds which are mimics of the peptide sequence Arg--Gly--Asp.

Abstract: Compounds having the structure below ##STR1## and pharmaceutically acceptable salts thereof exhibit vasopressin antagonistic activity, vasodilating activity, hypotensive activity, activity for inhibiting saccharide release in the liver, activity for inhibiting growth of mesagium cells, water diuretic activity, platelet agglutination inhibitory activity, oxytocin antagonistic activity and the like, and are useful in treating or preventing hypertension, heart failure, renal insufficiency, edema, ascites, vasopressin parasecretion syndrome, hepatocirrhosis, hyponatremia, hypokalemia, diabetic or circulation disorder, oxytocin related diseases and the like.

Abstract: The present invention relates to 1,3,6-Trialkylhexahydro-1,3,6-triazocine-2-on represented by the formula (1): ##STR1## wherein R is a C.sub.1 .about.C.sub.8 alkyl group and a preparation process of the compound comprising reacting N,N',N"-trialkyldiethylenetriamine represented by the formula (2): ##STR2## wherein R is a C.sub.1 .about.C.sub.8 alkyl group, with urea, phosgene or carbon dioxide.

Abstract: The invention relates to dimeric 2-(2'-hydroxyphenyl)benzotriazoles of the formula I ##STR1## in which p is 0 or 1; is C.sub.1 -C.sub.12 alkylene;R.sub.1 and R'.sub.1, independently of one another, are hydrogen, halogen, C.sub.1 -C.sub.18 aklyl, C.sub.1 -C.sub.18 alkoxy or --CN;R.sub.2 and R'.sub.2, independently of one another, are hydrogen or C.sub.1 -C.sub.18 alkyl or together are C.sub.2 -C.sub.12 alkylene or C.sub.2 -C.sub.12 hydroxyalkylene; andR.sub.3 and R'.sub.3, independently of one another, are hydrogen, halogen, C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.18 alkoxy.The compounds of formula I are highly suitable for the stabilization of organic material against the harmful effects of heat, oxygen and light, in particular UV radiation.

Abstract: Novel piperidine-triazine compounds of the formula (I) useful as light stabilizers, heat stabilizers and antioxidants for organic materials.The meanings of R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2, X.sub.3, Y.sub.1, Y.sub.2, M and N are defined in the text.

Abstract: The invention relates to macrocyclic rare earth complexes which consist of at least one rare earth salt complexed by a macrocyclic compound of formula (I): ##STR1## in which: the bivalent radicals A, B, C and D, which are identical or different, are hydrocarbon chains optionally containing one or more heteroatoms, at least one of said radicals containing at least one molecular unit or essentially consisting of a molecular unit possessing a triplet energy greater than the energy of the emission level of the complexed rare earth ion, at least one of said radicals consisting of a substituted or unsubstituted nitrogen-containing heterocyclic system in which at least one of the nitrogen atoms carries an oxy group, and it being possible for one of the radicals C or D not to exist; andX.sub.1 and X.sub.2, which are identical or different, are hydrogen or a hydrocarbon chain (CH.sub.2).sub.

Abstract: Cyclodextrin catenanes capable of forming inclusion complexes and a method of preparing them are disclosed. The catenanes comprise one or two per-2,6- di-O-alkyl-.beta.-cyclodextrin macrocycles wherein each per-2,6-di-O-alkyl-.beta.-cyclodextrin macrocycle is interpenetrated by another macrocycle. Such modified cyclodextrins may be used for the electrochemical and optical sensing of small organic molecules, especially small aromatic molecules.

Abstract: The invention includes a water-soluble oxygen carrier. The oxygen carrier includes a meso-.alpha.,.alpha.,.alpha.,.alpha.-tetrakis(o-propanoylamino)phenylporph yrin, in which the 3-carbons of the propanoyl groups are each covalently bound to an amine nitrogen, and iron or cobalt is bound to the pyrrole nitrogens of the porphyrin. The oxygen carrier also includes a ligand L for protecting the open face of the porphyrin from .mu.-oxo dimer formation.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: The present invention relates to a composition having the general formula: ##STR1## wherein each of A, B, C, X, Y, and Z is independently O, NH, N(CH.sub.2).sub.m CH.sub.3 ], N(C.dbd.O) (CH.sub.2).sub.m CH.sub.3 ], CH.sub.2, S, or Se; each of R.sub.1, R.sub.2, and R.sub.3 is independently phenyl, 4-hydroxyphenyl, pyridyl, pyrrolyl, indolyl, naphthyl, thiophenyl, (C.dbd.O) (CH.sub.2).sub.p CH.sub.3, NH(C.dbd.O) (CH.sub.2).sub.p CH.sub.3 ], OH, COOH, NH.sub.2, or SH; and m, n, and p are integers between 0 and 5. The composition is a chiral receptor molecule useful for the purification of enantiomers of derivatives of amino acids and of compounds able to form hydrogen bonds. The preparation of the composition involves coupling a trifunctional aromatic molecule with three protected chiral molecules at the three aromatic groups, cleaving protecting groups, and joining adjacent chiral groups by multiple lactamizations.

Abstract: Compositions which are immunologically crossreactive with antibodies are provided, together with preparative and therapeutic methods therefor. The compositions preferably comprise a plurality of covalently bound synthetic compounds, at least one of which is individually crossreactive with at least one complementarity determining region (CDR) of the antibody. Preferred processes for preparing the immunologically crossreactive compounds comprise identifying chemical functionality such as hydroxyl groups in the CDR which participates in at least one immunological binding phenomena, determining the three-dimensional positioning of the chemical functionality, and synthesizing a compound which comprises substantially the same chemical functionality as the CDR and which has at least one conformation wherein the three-dimensional positioning of the chemical functionality is substantially identical to the three-dimensional positioning of the chemical functionality of the CDR.

Abstract: The present invention relates to novel tetramethylpiperidine compounds of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, R.sub.2 and R.sub.3 are e.g. --(CH.sub.2).sub.2 --, R.sub.4 is e.g. --CO--, --COCO-- or --COCH.sub.2 CO--, n is e.g. 1 and R.sub.5 is e.g. hydrogen or allyl.These compounds are suitable for use as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.

Abstract: This invention relates to a process for preparing synergistic derivatives of formula (I), in which Y is hydrogen or dimethylamino, from pristinamycin I.sub.A or from virginiamycin, via a Mannich base, followed by elimination of the amine introduced.

Abstract: Macrocyclic oxamides may be made easily, in good yield and in one step by reacting an oxalic compound, such as oxalic acid or oxalic esters, with a diamine, where the amine groups are separated by at least five atoms. The oxalic compounds may include, but are not limited to such materials as dimethyl oxalate and diethyl oxalate. The diamines may include, but are not limited to such materials as alkylenediamines; polyalkylene glycol diamines; alkyl-bis-(aminoalkyl)amines; imino bis-(alkyl)amines; and N,N' bis-(aminoalkyl)-N,N'-dialkylalkylenediamines and bis-(aminoalkyl)piperazines; and mixtures thereof. The macrocyclic oxamides made by this process may be used to selectively separate metal ions from solution, or complexed together with a metal ion act as a catalyst.

Abstract: A method for reducing adverse effects of neurotoxic injury, which comprises administering to a patient susceptible to neurotoxic injury an effective amount, sufficient to reduce the injury, of a compound having an indolactam V ring system. Particularly preferred are compounds having ring stereochemistry as indicated in the following formula: ##STR1## The indicated substituents show preferred locations of substituents; preferred substituents are defined in the specification.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.

Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.