Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.

Abstract: The invention relates to N-sulfonyl derivatives of formulae (I) and (I)' ##STR1## to their preparation, and to pharmaceutical compositions in which they are present. The compounds of formulae (I) and (I)' have an affinity for the vasopressin and ocytocin receptors.

Abstract: The invention relates to new optically active amino acid derivatives of the general formula (I) ##STR1## in which n, R, R.sub.1, R.sub.2, R.sub.3, X and A have the meaning given in the description, which amino acid derivatives contain sulphoxide or sulphone groups, to two basic synthetic routes for the preparation from sulphur-containing amino acids, to the polymerization of these monomers and to the use of the polymers as optically active adsorbents for chromatographic resolution of racemates to give the enantiomers.

Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.

Abstract: Process for the diastereoselective reductive pinacol coupling of homochiral .alpha.-aminoaldehydesA process for the preparation of optically pure symmetrical compounds of the formula I ##STR1## is described in which R.sup.1, R.sup.2 and R.sup.3 are explained in the description, with simultaneous control of the four centers of chirality marked by *.

Abstract: Novel mercaptosulfide matrix metalloproteinase inhibitors of the Formula I, ##STR1## wherein: n is 0 or 1;R.sup.1 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH(lower alkyl); andR.sup.2 is selected from the group consisting of hydrogen, lower alkyl, amino lower alkyl, carbamoyl lower alkyl, PhtN(lower alkyl), TsNH (lower alkyl); orR.sup.1 and R.sup.2 together are --CH.sub.2 --CH.sub.2 --CH.sub.2 --;R.sup.3 is selected from the group consisting of hydrogen, lower alkyl, aralkyl and heteroaralkyl; andR.sup.4 is selected from the group consisting of hydrogen, lower alkyl, amino lower-alkyl, guanyl lower-alkyl, imidazoylalkyl, aralkyl and 2-indolylmethyl; andR.sup.5 is selected from the group consisting of lower alkyl, aralkyl and --CH(R.sup.6)--C(O)NH.sub.2,whereinR.sup.

Abstract: The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.

Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.

Abstract: Compounds characterized generally as alkylaminoalkyl-terminated .beta.-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is methyl; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein q is two or three; wherein r is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl containing moiety; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.12 and R.sup.13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

Abstract: The present invention is directed to branched amidoamine additives useful in oleaginous compositions formed by (a) reacting a first nitrogen-containing compound (e.g., ammonia or an organic amine) with an alpha, betaunsaturated compound of the formula: ##STR1## wherein W.sup.1 is sulfur or oxygen, Y is --OR.sup.4, --SR.sup.4, or --NR.sup.4 (R.sup.5), and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen or substituted or unsubstituted hydrocarbyl, to form a first adduct containing unreacted --C(W.sup.1)--Y groups; (b) reacting the first adduct with a polyamine (e.g., a polyalkylene polyamine) to form a second adduct containing unreacted --NH-- group (preferably primary amine groups) and comprising a branched amido-amine oligomer; and (c) reacting the second adduct with mixtures of an aldehyde and a long chain hydrocarbyl substituted hydroxy aromatic compound.

Abstract: The present invention relates to compounds exhibiting central nervous system (CNS) activity which are useful in the treatment of epilepsy and other CNS disorders. The compounds of this invention have the following general formula: ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: meso-DTA and method for its use in reducing disulfide bonds.

Abstract: The invention is directed to a pesticide composition comprising free flowing, essentially spherical, water-dispersible granules wherein said water-dispersible granules are from about 150 to about 850 microns in diameter; wherein said granules contain up to about 8.0% by weight moisture; wherein each individual water-dispersible granule is an aggregation of individual spherical microcapsules which contain at least one water-insoluble pesticide within a polymeric shell wall; and wherein said water-dispersible granule disintegrates upon contact with water to release said individual microcapsules.The invention also relates to dry flowable pesticidal formulations of the above water-dispersible granules, together with formulation adjuvants.The invention is further directed to a process for preparing a water-dispersible granule by spary drying an aqueous suspension comprising discrete microcapsules containing at least one water-insoluble pesticide within a polymeric shell wall suspended in an aqueous liquid.

Abstract: The invention relates to new optically active sulphur-containing amino acid derivatives, a process for their preparation, their polymerisation to give optically active polymers and the use of these optically active polymers as adsorbents for chromatographic separation of racemates into enantiomers.

Abstract: Oxamides useful as dye intermediates have the formula ##STR1## where R.sup.1 and R.sup.2 are independently of each other hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,X is hydroxyl, nitro or a radical of the formula --NR.sup.3 R.sup.4, where R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkanoyl and R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl or phenyl,Z is C.sub.2 -C.sub.8 -alkylene, substituted or unsubstituted phenylene or substituted or unsubstituted naphthylene, or X--Z and R.sup.1 are, together with the nitrogen atom joining them together, the radical of the formula ##STR2## where R.sup.3 is as defined above,L is a bridge member andY is vinyl or a radical of the formula --C.sub.2 H.sub.4 --A, where A is hydroxyl or a group which is detachable under alkaline reaction conditions.

Abstract: Alkylamino-mercaptoalkylamides have the formula ##STR1## where in A represents the divalent radical --(CH.sub.2).sub.n --, wherein n is a whole number ranging from 2 to 5, or the divalent radical --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --,m is 0, 1 or 2,R.sub.1 represents hydrogen or linear or branched lower alkyl having 1-5 carbon atoms,R.sub.2 and R.sub.3, each independently, represent hydrogen or a linear or branched lower alkyl having 1-4 carbon atoms with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously and the salts of the compound of formula I as well as the corresponding disulfides with the exclusion of the disulfide in which A.dbd.--(CH.sub.2).sub.2 --, m.dbd.0, R.sub.1 and R.sub.2 .dbd.H and R.sub.3 .dbd.--C.sub.2 H.sub.5. The compound of formula I is used as a reducing agent in a cosmetic composition for the permanent deformation of hair.

Abstract: A process for preparing p-nitroaromatic amides is provided which comprises contacting an amide and nitrobenzene in the presence of a suitable solvent system, and reacting the amide and nitrobenzene in the presence of a suitable base and a controlled amount of protic material at a suitable temperature in a confined reaction zone. The p-nitroaromatic amides of the invention can be reduced to p-aminoaromatic amides. In one embodiment, the p-aminoaromatic amide is further reacted with ammonia under conditions which produce the corresponding p-aminoaromatic amine and the amide starting material which can be recycled or with water in the presence of a suitable basic or acidic catalyst under conditions which produce the corresponding p-aminoaromatic amine and the acid or salt thereof corresponding to the amide starting material. In another embodiment, the p-aminoaromatic amine is reductively alkylated to produce alkylated p-aminoaromatic amine.

Abstract: A composition, test device and method of determining the presence or concentration of ketone bodies, and specifically D-.beta.-hydroxybutyrate, in a test sample are disclosed. The test device includes a test pad comprising a suitable carrier matrix incorporating an indicator reagent composition capable of interacting with D-.beta.-hydroxybutyrate to produce a detectable or measurable response. In addition, a new and improved indicator reagent composition, comprising a) an indicator dye that is responsive to thiols, such as a substituted isobenzothiazolone, Ellman's reagent or a derivative of Ellman's reagent: b) D-.beta.-hydroxybutyrate dehydrogenase; c) lipoamide dehydrogenase; d) D,L-lipoamide; and e) nicotinamide adenine dinucleotide, is incorporated into the carrier matrix to provide an accurate and sensitive assay of a test sample for D-.beta.-hydroxybutyrate (DHBA) in particular, and for ketone bodies in general.

Abstract: Disclosed herein are novel unsymmetrical dithiol ketals which are useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.

Abstract: Compounds characterized generally as cyclopropyl alanine aryl/alkylsulfide/sulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronapthylmethyl and chloronaphthylmethyl; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is cyclopropylmethyl wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.

Abstract: Compounds characterized generally as ethynyl alanine aryl/alkylsulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl-containing moeity; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.

Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together, and R.sup.3 and R.sup.4 taken together, independently represent a polymethylene chain leaving 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having from 1 to 4 carbon atoms and R.sup.5 to R.sup.8 are independently hydrogen, hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 complete a trimethylene ring, R.sup.5 and R.sup.7 are each hydrogen and R.sup.6 and R.sup.8 are alkyl such as methyl. The compounds have microbiological activity.

Abstract: Compounds characterized generally as .beta.-alanineamide aryl/alkylsulfide/sulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from methyl and ethyl; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.

Abstract: Amide-thiolate ligands having improved metal chelate formation kinetics are disclosed. The ligands include a tertiary amine strategically located to facilitate rapid formation of an amine-amide-thiolate intermediate complex, followed by transfer of the metal to a thermodynamically stable amide-thiolate complex. The amide-thiolate ligands of the present invention may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.

Abstract: A composition of matter including an onium salt and a method of forming images. The onium salt has a chromophore which absorbs ultraviolet radiation, an S, Se, As, N or P atom which is free of substituents exhibiting a higher energy occupied molecular orbital than the chromophore; an insulating group which links the chromophore to the S, Se, As, N or P atom of the salt and substantially prevents .pi. resonance from the chromophore through the S, Se, As, N or P atom; and an anion. The onium salt is capable of forming a Bronsted acid upon exposure to ultraviolet radiation in the presence of a proton source. In the method of forming images, the onium salt is exposed to ultraviolet radiation in the presence of a proton source, to convert said onium salt to a Bronsted acid.

Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.

Abstract: Aromatic compounds absorbing UVB and/or UVA, substituted with an amide function, selected from the group consisting of ##STR1## whose variable substituents are as defined in the specification, e.g. ##STR2## are useful as photoprotective agents or tanning accelerators.

Abstract: Fungicidal compounds of the formula (I): ##STR1## in which A and B are independently H, fluoro, chloro, bromo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halo(C.sub.1-4)alkyl provided that both are not H; D and E are independently H or fluoro; R.sup.1 is H, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is CC.sub.1-4 alkyl, C.sub.1-4 alkoxy or optionally substituted phenyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached join to form a morpholine, piperidine, pyrrolidine or azetidine ring which is optionally substituted with C.sub.1-4 alkyl; R.sup.3 is H; R.sup.4 is trichloromethyl, C.sub.2-8 alkyl (optionally substituted with halogen, C.sub.1-8 alkoxy or R'S(O) in which R' is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl and n is 0, 1 or 2), cyclopropyl (optionally substituted with halogen or C.sub.1-4 alkyl), C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, C.sub.1-8 alkoxy, mono- or di(C.sub.1-4)alkyl- amino or the group, R"ON.dbd.C(CN) in which R" is C.sub.1-4 alkyl, or R.sup.

Abstract: Compounds characterized generally as being propargyl-terminated aryl/alkylsulfonyl-terminated amino diol derivatives having a cycloalkylalkyl group at the P2 substitution site are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is propargyl or a propargyl-containing moiety.

Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.

Abstract: A novel disulfide compound is presented which can be readily led to 5-amino-2-chloro-4-fluoro-thiophenol in good yield.

Abstract: Compounds characterized generally as di-propargyl-containing aryl/alkylsulfonyl-terminated amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, nethyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylnethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein each of R.sup.5 and R.sup.8 is independently propargyl or a propargyl-containing moiety; and wherein R.sup.7 is cyclohexylmethyl.

Abstract: Novel thiol-terminated hydroxyamides, and processes for their preparation and use are provided. These hydroxyamide compounds may be prepared by the reaction of a mercapto-functional alkyl ester, such as methylmercaptopropionate, with a molar excess of an alcohol-substituted amine, such as a b-hydroxyalkyl amine. The thiol-terminated hydroxyamides are useful as polymerization chain transfer agents, particularly when it is desirable to form polymers or oligomers containing functional hydroxyamide end groups. By chain terminating such polymers or oligomers with reactive hydroxyamide end groups the polymers or oligomers can be further reacted with acid-containing monomers or polymers to form block or graft copolymers.

Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.

Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.

Abstract: A compound of the formula ##STR1## in which R.sup.1 and R.sup.2 taken together, and R.sup.3 and R.sup.4 taken together, independently represent a polymethylene chain having 3 or 4 carbon atoms, or a polymethylene chain having 3 or 4 carbon atoms substituted by at least one lower alkyl radical having from 1 to 4 carbon atoms, and R.sup.5 to R.sup.8 are independently hydrogen, hydrocarbyl or substituted hydrocarbyl. Typically R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 complete a trimethylene ring, R.sup.5 and R.sup.7 are each hydrogen and R.sup.6 and R.sup.8 are alkyl such as methyl. The compounds have microbiological activity.

Abstract: Compounds of formula: ##STR1## in which R.sub.1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R.sub.8)--COOR.sub.4, (c) a chain --CH.sub.2 --CO--NR.sub.5 R.sub.6 or (d) a phenylalkyl radical, R.sub.2 is a methylene or ethylene radical or a radical --CH(R.sub.7)--, R.sub.3 is a 1- or 2-naphthyl radical, 2- or 3-indolyl or phenylamino radical in which the phenyl ring is optionally substituted on the understanding that, when R.sub.3 is 1- or 2-naphthyl or 2- or 3-indolyl radical, R.sub.7 cannot represent a benzyl, alkylthioalkyl or phenyl radical, as well as, when R.sub.2 is a radical --CH(R.sub.7)--, their racemates and their stereoisomers, and medicinal products containing them.

Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.

Abstract: A bifunctional coupling agent for joining a sulfhydryl-containing protein or peptide and a metallic radionuclide comprising a sulfhydryl selective electrophile, a chelator containing at least one protected thiol and a organic linking radical which serves to join said electrophile and said chelator is disclosed. A radiodiagnostic precursor comprising an antibody or antibody fragment and the specified bifunctional coupling agent bound to a sulfhydryl group on the antibody or antibody fragment is also disclosed.

Abstract: This invention relates to novel compounds of the formula [I], which are useful for treatment of various diseases such as immunodeficiency and autoimmune diseases caused by immune disorders, processes for preparing the compounds and compositions containing the compounds as active ingredients.

Abstract: Anchimeric chelates are disclosed which are capable of rapidly forming stable chelates with radionuclide metals at or below physiological temperature. Bifunctional anchimeric chelates having these same properties are also disclosed which are useful for radiolabeling target specific molecules such as monoclonal antibodies and fragments thereof.

Abstract: A composition, test device and method of determining the presence or concentration of ketone bodies, and specifically D-.beta.-hydroxybutyrate, in a test sample are disclosed. The test device includes a test pad comprising a suitable carrier matrix incorporating an indicator reagent composition capable of interacting with D-.beta.-hydroxybutyrate to produce a detectable or measurable response. In addition, a new and improved indicator reagent composition, comprising a) an indicator dye that is responsive to thiols, such as a substituted isobenzothiazolone, Ellman's reagent or a derivative of Ellman's reagent; b) D-.beta.-hydroxybutyrate dehydrogenase; c) lipoamide dehydrogenase; d) D,L-lipoamide; and e) nicotinamide adenine dinucleotide, is incorporated into the carrier matrix to provide an accurate and sensitive assay of a test sample for D-.beta.-hydroxybutyrate (DHBA) in particular, and for ketone bodies in general.

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: Non-peptidyl compounds characterized generally as aralkyl-N-terminal amino hydroxy .beta.-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 is hydroxy; wherein R.sub.7 is isobutyl or ethyl; and wherein each of R.sub.8 and R.sub.9 is hydrido; or a pharmaceutically-acceptable salt thereof.

Abstract: Compounds, compositions and methods are described for treating a CNS disorder such as a cognitive disorder, epilepsy, depression, Parkinson's disease, Alzheimer's disease, a neurodegenerative disease or neurotoxic injury. Compound of interest are 2-amino-4,5-methyleneadipic acid compounds and derivatives defined by the formula I: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, ##STR2## with each of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein each of X and Y is independently selected from hydroxyl, alkoxy, alkylthio, amino and ##STR3## with each of R.sup.6 and R.sup.7 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein any of R.sup.1 through R.sup.