Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.

Abstract: A class of acetamidine derivatives of general formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR.sup.3 wherein X is oxygen, C(O).sub.m wherein m is 1 or 2, S(O).sub.n wherein n is 0, 1 or 2, or a group NR.sup.4 wherein R.sup.4 is hydrogen or C.sub.1-6 alkyl; and R.sup.3 is hydrogen, C.sub.1-6 alkyl, or a group NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl, provided that R.sup.3 is not NR.sup.5 R.sup.6 when X is oxygen or S(O).sub.n; R.sup.1a and R.sup.1b are independently selected from hydrogen and halo; R.sup.2 is a C.sub.1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R.sup.2 being optionally substituted by one or more groups independently selected from halo; N.sub.3 ; nitro; CF.sub.3 ; ZR.sup.7 wherein Z is oxygen, C(O).sub.m' wherein m' is 1 or 2, S(O).sub.n' wherein n' is 0, 1 or 2, or a group NR.sup.8 wherein R.sup.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.

Abstract: The present invention provides a novel carbamazepine hydrazide compound suitable for covalent attachment to a polymer particle reagent, having the general formula ##STR1## The present invention provides a novel carbamazepine acid compound suitable for attachment to proteins for the production of carbamazepine immunogens. The carbamazepine antigen of the present invention has the following general structure: ##STR2## where X is C.dbd.O, CH.sub.2 or SO.sub.2 ; Y is C.dbd.O, CH.sub.2, SO.sub.2 ; R is an alkyl and P is a protein or a hapten.

Abstract: Products prepared by reacting polyisocyanates with alkenyl or alkynyl compounds; then with perfluoroalkyl iodides & dehydroiodinating the product.

Abstract: A retroviral protease inhibiting compound of the formula A--X--B is disclosed. Also disclosed are a composition and method for inhibiting a retroviral protease and for treating an HIV infection. Also disclosed are processes and intermediates useful for the preparation of the retroviral protease inhibitors.

Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.

Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.

Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.

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

Abstract: 2-?4-Biphenyloxymethylene!anilides of the formula I ##STR1## where the indices and the substituents have the following meanings: R, R.sup.1 and R.sup.2 are cyano, nitro, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylamino, dialkylamino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl(alkylamino), alkenyl, alkenyloxy, alkynyl, alkynyloxy, cycloalkyl or C(R.sup.a).dbd.NOR.sub.b ;R.sup.a and R.sup.b are hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;m is 1, 2, 3, 4 or 5;n is 0, 1 or 2;R.sup.3 is nitro, cyano, halogen,n is 0, 1 or 2,unsubst. or subst. alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy oralkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylcarbonylamino, alkylcarbonyl(alkylamino), C(R.sup.a).dbd.NOR.sub.b oro is 0, 1, 2, 3 or 4;R.sup.4 is hydrogen,unsubst. or subst.

Abstract: Vinyl carbamate compounds are prepared by reacting appropriate secondary amines with carbon dioxide and acetylenically unsaturated compounds in the presence of a compound of a metal from the platinum group, in particular a ruthenium compound, with either one of the two process steps (a) and (b) or, preferably, both being carried out:(a) the acetylene compound is reinjected during the reaction;(b) the reaction is carried out in the presence of a tertiary amine.

Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.7 and R.sub.8 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkoxycarbonyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a phenyl group with either two or three substituents of the following formula: ##STR2## wherein the positions of substitution are R.sub.2,R.sub.3 -, R.sub.2,R.sub.4 -, R.sub.2,R.sub.5 -, R.sub.2,R.sub.6 -, R.sub.3,R.sub.4 -, R.sub.3,R.sub.5 -, and R.sub.2,R.sub.4,R.sub.6 - and R.sub.2 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.3 is methyl, ethyl, fluoro, chloro, methoxy or trifluoromethyl; R.sub.4 is methyl, fluoro, bromo, methoxy or cyano; R.sub.5 is methyl, fluoro, chloro, methoxy, cyano or trifluoromethyl; R.sub.

Abstract: Described herein are compounds of Formula (XX) and Formula (XXIV), shown below, and processes of making same. ##STR1## wherein p is 0 ##STR2## wherein p is 1, and Y is chlorine or bromine.

Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.

Abstract: .beta.-Hydroxyamines and .beta.-hydroxycarbamates are synthesized from olefin substrates by means on a catalyzed asymmetric addition reaction. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. Carbamates are employed as an oxidant nitrogen source for the production of .beta.-hydroxysulfonamides. Excellent yields and enantiomeric efficiencies are achieved with co-solvents containing a 50/50 (v/v) mixtures of water and organic solvent. The performance of the reaction is further enhanced by omitting the addition silver or mercurial salts conventionally employed in asymmetric aminohydroxylation additions to olefins performed in neat or substantially neat solvents. .beta.

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

Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.

Abstract: A photothermographic element comprising a support bearing at least one heat-developable, photosensitive, image-forming photothermographic emulsion layer comprising:(a) a photosensitive silver halide;(b) a non-photosensitive, reducible source of silver;(c) a chromogenic leuco dye reducing agent; and(d) a binder;wherein the chromogenic leuco dye reducing agent is a chromogenic leuco redox-dye-releasing compound of the general formula: ##STR1## wherein: (i) Cp is a coupler group;(ii) N--D is a photographic developer group; and(iii) R.sup.1 is a --C(O)--NH--A--Dye group wherein Dye represents the chromophore of a thermally mobile dye; and A represents a single bond or a divalent linking group of the formula --X--R.sup.5 --L--, wherein R.sup.5 is a divalent hydrocarbon chain containing up to 12 carbon atoms, L is a single bond or a divalent group that binds the chromophore of the thermally mobile dye to R.sup.5, and X represents a single bond or an --SO.sub.2 -- group.

Abstract: A process is described for the preparation of aromatic carbamates in which an organic carbonate in a stoichiometric quantity or in a quantity higher than the stoichiometric value is reacted with an aromatic amine operating in the presence of a carbamation catalyst, wherein this catalyst is selected from N,N-substituted carbamate complexes of zinc or copper.The process gives high yields and selectivity in the useful reaction product.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain proteasome inhibitors. The structure of the inhibitors are also disclosed.

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

Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.

Abstract: The synthesis of paclitaxel obtained from the semi-synthesis of taxol using a protected baccatin III backbone which is esterified with a suitably protected side chain acid, thereby producing an intermediate which may be acylated and deprotected to produce paclitaxel.

Abstract: Polyurethane elastomers exhibiting improved green strength while maintaining short demold times are prepared from ultra-low unsaturation polyoxypropylene polyols containing up to 20 weight percent internal random oxyethylene moieties. The elastomers adsorb less than 10 weight percent water at 0.degree. C. The internal polyoxyethylene moiety-containing polyoxypropylene polyols may be used to prepare ultra-low unsaturation polyoxyethylene capped polyols which are haze-free and which may be used to prepare haze-free 4,4'-MDI prepolymers. Multidisperse blends of monodisperse internal oxyethylene moiety-containing polyoxypropylene polyols of ultra-low unsaturation provide yet further improvements in elastomer processing.

Abstract: A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl;Y is a direct bond or lower alkylene; andR.sub.1, R.sub.2, R.sub.3, R.sub.4 are as defined herein. The compounds are advantageously used as Tachykinin antagonists in the treatment of respiratory diseases, ophthalmic diseases and inflammatory diseases, for example.

Abstract: N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities.

Abstract: The present invention relates to blocked polyisocyanates containing at least one isocyanate group which is reversibly blocked with a monofunctional blocking agent for isocyanate groups and at least one isocyanate group in the form of a urea group, which may be converted to a thermally stable hydantoin group. The present invention also relates to one-component coating compositions containing these blocked polyisocyanates and compounds containing isocyanate-reactive groups.

Abstract: Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.

Abstract: Allophanate-modified MDI which is a storage stable liquid at 25.degree. C. is produced by reacting a monoisocyanate and an organic material having at least two hydroxyl groups and a molecular weight of from about 60 to about 6,000 to form a urethane. The urethane is then reacted with and isomeric mixture of MDI in an amount such that the product isocyanate will have an NCO content of from about 12 to about 30%. The isomeric mixture of MDI is composed of 4,4'-diphenylmethane diisocyanate containing from 0 to about 60% by weight 2,4'-MDI and less than 6% by weight of the 2,2'-MDI. This allophanate-modified MDI is further reacted with an organic isocyanate-reactive material to produce an allophanate-modified MDI prepolymer containing urethane, urea and/or biuret groups having an NCO content which is generally from about 5 to about 29% by weight. The prepolymers of this invention are particularly useful in reaction injection molding processes because they give molded articles having improved flex modulus.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aromatic or heteroaromatic radical, a hydroxy group that is aliphatically, araliphatically or heteroarylaliphatically etherified or protected by a hydroxy-protecting group, or an aliphatically etherified mercapto group, andR.sub.2 is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical, orR.sub.1 and R.sub.2 together form a divalent aliphatic radical,R.sub.3 is free or aliphatically, araliphatically or aromatically esterified carboxy, formyl or hydroxymethyl,R.sub.4 is hydrogen, an aliphatic or araliphatic radical or an amino-protecting group, andR.sub.5 is hydrogen or an aliphatic radical,and the salts thereof can be used as intermediates in the preparation of medicinal active ingredients.

Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.

Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.

Abstract: 2-fluoro-cyclopropylamine is prepared in an advantageous manner by reacting an N-vinyl compound with a carbene of type FXC: (where X=chlorine or bromine) to give the corresponding cyclopropylamine derivative, replacing the radical X in this derivative by hydrogen, by reduction, and finally eliminating the other substituents on the hydrogen atom.

Abstract: The invention relates to the compounds of formula (I) wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); and X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical.

Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.

Abstract: Amino acid-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent and a medicament containing themBenzoylguanidines of the formula I ##STR1## in which the radicals R(1) to R(5) have the meanings given in the description, are described. They are prepared by reacting a compound of the formula II ##STR2## in which R(1) to R(5) and L have the meanings given in the description, with guanidine. The compound I is suitable for the preparation of cardiovascular medicaments.

Abstract: Disclosed herein is a process for producing a (2S,5S)-2,5-diamino-1,6-diphenyl-3-hexanone derivative represented by the formula (1): ##STR1## wherein R.sup.1 means a lower alkylcarbonyl group, a halogen-substituted lower alkylcarbonyl group, an arylcarbonyl group or a lower alkoxycarbonyl group, and R.sup.2 and R.sup.3 are identical with or different from each other and denote individually an aryl group or an alkoxy-substituted aryl group, which comprises subjecting a (2S)-2,5-diamino-1,6-diphenyl-4-hexen-3-one derivative represented by the formula (2): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the same meaning as defined above, to a hydrogenation reaction in the presence of a transition metal-containing catalyst.

Abstract: Compounds of formula (I), and salts and prodrugs thereof wherein X, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7 and R.sup.8 are defined herein, are tachykinin receptor antagonists.

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

Abstract: The invention provides the preparation procedure for N-substituted derivatives of N-methyl-3-(p-trifluoromethylphenoxy)-3 -phenylpropylamine having the general formula (I), where R is hydrogen and the group of the general formula (II), in which R.sub.1 is aryl, alkylaryl and alkyl group with C.sub.1 to C.sub.4 atoms, and n is 0 and 1, and also covers the compounds of the general formula (I), where R is the group of the formula (II), in which R.sub.1 is aryl and alkylaryl group, and n is 0 and 1.According to this invention by condensation of N-substituted derivatives of N-methyl-3-phenyl-3-hydroxypropylamine (XV), where R.sub.1 is benzyl and p-nitrobenzyl group and n is 0, and p-trifluoromethylchlorbenzene (XVI) prepared N-substituted derivatives of N-methyl-3-(p-trifluoromethylphenoxy)-3 -phenylpropylamine (I), where R is the group of the formula (II), in which n and R are the same as in the compound (XV), which by the reaction with chloroformic acid esther (XVII), where R.sub.

Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.

Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein Q is optionally substituted phenyl or naphthyl;X and Y are each H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or X and Y are together .dbd.O;Z is O or S;R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl (C.sub.1-4 alkyl), C.sub.2-6 alkenyl, COC.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;R.sup.2 is substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.p optionally substituted by oxo;R.sup.3 is H [or C.sub.1-6 alkyl];R.sup.4 is H, C.sub.1-6 alkyl or phenyl; andR.sup.5 is optionally substituted (CH.sub.2).sub.

Abstract: A method of treatment or prophylaxis of angina in mammals, such as humans, which comprises the administration to the sufferer of an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a solvate of any of the foregoing: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, A and B are herein defined.

Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.

Abstract: Novel carbodiimides and/or oligomeric polycarbodiimides containing terminal isocyanate, urethane and/or urea groups are obtainable, for example, by condensation of 1,3-bis(1-methyl-1-isocyanatoethyl)benzene with elimination of carbon dioxide followed, if desired, by reaction of all or some of the free isocyanate groups of the resultant (poly)carbodiimides with aliphatic, cycloaliphatic or araliphatic amines, alcohols and/or alkoxypolyoxyalkylene alcohols, and are used as stabilizers against hydrolytic degradation of polyaddition and polycondensation products containing ester groups.

Abstract: This invention relates to ortho substituted phenyl compounds as inhibitors of prostaglandin synthase, to pharmaceutical compositions comprising such compounds and to methods of using such compounds as antiinflammatory and antipyretic agents.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heteroeyelylearbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl:and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.

Abstract: Allophanate-modified MDI which is a storage stable liquid at 25.degree. C. is produced in two steps. First, a monoisocyanate is reacted with an organic material having about 1.8 or more hydroxyl groups and a molecular weight of from about 60 to about 6,000 to form the urethane. The urethane is then reacted with an isomeric mixture of MDI in an amount such that the resultant isocyanate will have an NCO content of from about 3 to about 28%. The isomeric mixture of diphenylmethane diisocyanate contains from about 0 to about 60% by weight 2,4'-diphenylmethane diisocyanate, less than 6% by weight 2,2'-MDI and the remainder 4,4'-MDI. The prepolymers of this invention are particularly useful in reaction injection molding processes because molded articles having improved flex modulus are obtained.

Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.