Abstract: The present invention pertains to a method for designing inhibitors of enzyme human immunodeficiency virus type 1 reverse transcriptase which comprises the steps of:(a) providing a three dimensional model of the receptor site in the prepolymerization complex of the p66 subunit of enzyme human immunodeficiency virus type 1 reverse transcriptase and a known nonnucleoside inhibitor;(b) locating the conserved residues in the p66 subunit which constitute the nonnucleoside inhibitor binding pocket; and(c) designing a new nonnucleoside inhibitor which possesses complementary structural features and binding forces to the residues in the p66 subunit nonnucleoside inhibitor binding pocket.

Abstract: Compounds of the invention have the formula ##STR1## The compounds have fibrinogen receptor antagonist activity.

Abstract: Thiadiazabicyclodecanes of formula (I) wherein, Z is oxygen or sulfur; R is an optional substituent and W is an optionally condensed or substituted phenyl radical and the salts, complexes and stereisomers thereof, have good selective pre- and post-emergence herbicidal properties.

Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## wherein: A is ##STR2## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.

Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.

Abstract: A flame retardant organic silicon and phosphorus containing compound is produced by reacting a silicon halides compound with an organic phosphorus compound to produce an organic silicon and phosphorus halides compound which is then reacted with an organic compound to produce an organic silicon and phosphorus containing compound. This organic silicon and phosphorus containing compound is incorporated in an otherwise more flammable organic material under reaction conditions and in an amount sufficient to reduce the combustibility of the otherwise more flammable organic material. The organic silicon and phosphorus containing compound may also be utilized as coating agents, adhesives, surfactants, insecticides, hydraulic fluid and other uses.

Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: A mixture of silicon and phosphorus are heated and reacted with halide to produce silicon tetrahalides, silicon-phosphorus halide and phosphorus trihalides compositions. These compositions are reacted with any suitable organic, inorganic-organic and/or inorganic compound to produce novel organic silicon-phosphorus containing compositions. These compositions may be utilized as flame retardants, coating agents, adhesives and many other uses.

Abstract: Disclosed us a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula 1.0.Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, Schizophrenia, and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment.

Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.

Abstract: In the formulae, R.sup.1, R.sup.2, and R.sup.3 independently represent lower alkyl or aryl, and R.sup.4 represents lower alkyl.The present invention relates to a process for producing an indolocarbazole derivative represented by Formula (II), comprising the acidic treatment of a silylated indolocarbazole derivative represented by Formula (VI).

Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## are useful as ACE and NEP inhibitors and those wherein A is ##STR3## are useful as ACE inhibitors. Methods of preparation and intermediates are also disclosed.

Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.

Abstract: The present invention relates to the discovery of new C-terminal boronic acid dipeptide inhibitors of trypsin-like enzymes such as thrombin and pharmaceutical compositions thereof.

Abstract: An N-substituted polyamideimide essentially composed of identical or different repeating units of the formula I ##STR1## where R.sup.1 is one of the following tetravalent aromatic radicals ##STR2## and X is a bond or one of the following linkers ##STR3## where R.sup.2 and R.sup.4 are each, independently of one another, one of the following divalent aromatic radicals ##STR4## and where X has the abovementioned meanings and where R.sup.3 is hydrogen or a monovalent radical such as C.sub.1 -C.sub.6 -alkyl or phenyl, and the C.sub.1 -C.sub.6 -alkyl-, C.sub.1 -C.sub.6 -alkoxy-, aryl- or halogen-substituted derivatives thereof, and precursors (monomers) therefor, are described.

Abstract: Novel compounds of formula (I) and salts, solvates and hydrates thereof, processes for their preparation and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R is hydrogen, C.sub.1-6 alkyl or optionally substituted benzyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2 is C.sub.3-6 alkyl; R.sub.3 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.3 is a group ##STR2## where R.sub.7 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl and R.sub.8 is hydrogen or alkyl; and R.sub.4 is --CH.sub.2 --(CH.sub.2).sub.n OR.sub.5 or --CH.sub.2 --(CH.sub.2).sub.n OCOR.sub.6 or --CH(R.sub.9)COR.sub.10, where n is an integer from 1 to 6; R.sub.5, R.sub.6 and R.sub.9 are hydrogen or C.sub.1-6 alkyl; and R.sub.10 is hydroxy or --O--C.sub.1-6 alkyl or --NR.sub.5 R.sub.6 (where R.sub.5 and R.sub.

Abstract: Novel cyclic N,N,N' and N,N,N',N'-substituted organyloxysilyl-functional silanes are prepared by reacting an aminopropyl silane with carbon disulfide and heating the dithiocarbamate.

Abstract: Novel compositions of phosphoroustriscaprolactams, including tris(caprolactyl)phosphite which may be produced in accordance with the methods disclosed, finding particular utility as catalysts for esterification and other condensation reactions.

Abstract: A silane compound having the following formula, wherein R.sup.1 and R.sup.2 are each monovalent hydrocarbon radicals having 1 to 4 carbon atoms and n is an integer of 0, 1 or 2: ##STR1## which is manufactured by reacting 1-allyl-.epsilon.-caprolactam of the following formula: ##STR2## with a hydrogen silane of the following formula:HSiR.sup.1.sub.n (OR.sup.2).sub.3-nin the presence of a platinum-containing catalyst. The silane compound is useful as a surface treatment agent for imparting a moisture-repelling property to the surface of various materials.

Abstract: An improved process for preparing trialkylsilyl ester and acid halide derivatives of carboxylic acids is provided along with novel trialkylsilyl ester intermediates of 2-(2-furyl)-2-methoximinoacetic acid.

Abstract: Novel substituted imidazo-fused 7-member ring heterocycles of the formulae (I) and (Ia), which are useful as angiotensin II antagonists, are disclosed.

Abstract: A process for the condensation of imides and alcohols or amines to ester acyl lactams, ester amide acyl lactams or amide acyl lactams by reacting a polyol or polyamine in the liquid phase with an acyl lactam compound is disclosed.

Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.

Abstract: An improved process for preparing trialkylsilyl ester and acid halide derivatives of carboxylic acids is provided along with novel trialkylsilyl ester intermediates of 2-(2-furyl)-2-methoximinoacetic acid.

Abstract: Novel cyclic N,N,N' and N,N,N',N'-substituted organyloxysilyl-functional silanes are prepared by reacting an aminopropyl silane with carbon disulfide and heating the dithiocarbamate.

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 process of producing a silanic or siloxanic compound containing at least one cycloalkyl ring by the hydrogenation of a corresponding compound containing at least one aromatic ring, in the presence of a Raney nickel catalyst having a granulometry comprised essentially between 10 and 150 micrometers and a surface area of at least 80 m.sup.2 /g.

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: A novel class of 5, 6 or 7 member heterocycles which belong to the 3-isoxazolidinone, 2H-1,2-oxazin-3 (4H)-one and 3-isoxazepinone series of compounds and which are substituted at the 4-carbon by a benzylidene radical. The compounds have utility as analgesic agents, immunomodulating agents, anti-inflammatory agents and anti-pyretic agents and they may be combined with excipients to provide formuations which are useful in treating arthritis and conditions generally associated with that disease.

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: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable composition containing them, and their use as broad spectrum herbicides.

Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## , R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.

Abstract: An organophosphorus compound having the formula: ##STR1## wherein X is ##STR2## Z is an oxygen atom or a sulfur atom, and each of R.sub.1 and R.sub.2 is an alkyl group which may be substituted by halogen, alkoxy or alkylthio. The compound is useful as an insecticide, miticide, nematicide or soil pesticide.

Abstract: Compounds of formula (I): ##STR1## (wherein A is an alkylene group substituted by an optionally substituted amino or heterocyclic group and optionally interrupted by an oxygen or sulfur atom, R.sup.2 is various organic groups, B is C.sub.1 -C.sub.2 alkylene and Y is sulfur or methylene) and pharmaceutically acceptable salts and esters thereof are valuable hypotensive agents which may be prepared by a condensation reaction of the corresponding compound having an amino group in place of the group A--CH(COOH)--NH--.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, alkyl, aralkyl, aralkoxy-alkyl, hydroxy-alkyl, amino-alkyl, acylamino-alkyl, monoalkylamino-alkyl, dialkylamino-alkyl, alkoxycarbonylamino-alkyl, halo-alkyl, carboxy-alkyl, alkoxycarbonyl-alkyl, alkoxy or aralkoxy; R.sup.2 and R.sup.3 each represent hydrogen, alkyl or aralkyl; R.sup.4 and R.sup.5 each represent hydrogen or R.sup.4 and R.sup.5 together represent oxo; and X represents an oxygen atom or the group --NR.sup.6 -- in which R.sup.6 represents hydrogen, alkyl or aralkyl or --(CH.sub.2).sub.n -- in which n stands for zero, 1 or 2,and racemates, enantiomers, diastereoisomers or pharmaceutically acceptable salts thereof have antihypertensive activity and can be used as medicaments in the form of pharmaceutical preparations. They can be prepared according to known methods.Compounds useful as starting materials for producing the compounds of formula I are also provided.

Abstract: The invention is directed to N-silylpropyl-N'-acyl ureas and their production from an alkali cyanate, a 3-halopropylsilane and in a given case, a cyclic acidamide. By heating the compounds of the invention the blocked isocyanate function can be set free.

Abstract: A composition containing lactam functional materials, which are useful in the preparation of nylon block polymers, selected from the group consisting of: ##STR1## wherein, Q is ##STR2## with Y=C.sub.3 -C.sub.11 alkylene; b is an integer equal to 2 or more;R.sub.1 is an alkyl, aryl, aralkyl, alkyloxy, halogen, aryloxy, or aralkyloxy group;Z is a segment of: (1) a polyether, provided said polyether is not solely polyarylene polyether; (2) a polyester containing polyether or polymeric hydrocarbon segments (3) a hydrocarbon; (4) a polysiloxane; or (5) combinations thereof.

Abstract: The invention concerns a simple process for preparing an ester acyllactam and/or esteramide acyllactam by the catalytic condensation of imide and alcohol, characterized in that a polyol and an acyllactam compound are reacted in the liquid state in the presencce of a halide, carboxylate or acetylacetonate from beryllium, magnesium, calcium, strontium, barium, boron, aluminium, zinc or cadmium.The invention is important for the preparation of compounds which may be used in the preparation of nylon block copolymers, more in particular in RIM-nylon systems (Reaction Injection Moulding), since when the compounds obtained according to the present invention are used in a RIM system, a very fast lactam polymerization takes place, and it therefore also relates to the preparation of nylon block copolymers.