Abstract: The present invention provides a purified retinoid compound characterized by a molecular mass of about 320 daltons and an atomic composition of C.sub.20 H.sub.32 O.sub.3. The present invention also provides a purified retinoid compound having the structure: ##STR1## wherein the configuration of the C7, C9, and C11 double bond independently is Z or E and the absolute configuration at C13 and C14 is independently R or S; wherein R1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acyl halide, amide, nitrile, or amine; R2 and R3 are independently hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R2 and R3, or R1 and R2 are replaced by a 13,14-oxirane or a 14,15-oxirane group, respectively.

Abstract: 1-substituted, 2-substituted 1H-imidazo?4,5-c!-quinolin-4-amines are disclosed. These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.

Abstract: A process of making certain compounds using a phase transfer catalyst that permits the recovery and recycle of the phase transfer catalyst.

Abstract: The invention provides novel labelled boronic acid conjugates of formula ##STR1## (wherein V is a reporter moiety; W.sup.2 is a bond or an organic linker moiety;W.sup.1 is a *SO.sub.2 NR.sup.2, *CON.sup.2 or *CH.sub.2 N.sym.R.sup.2 .sub.2 group bound at the *-marked atom to the phenyl ring;R.sup.1 is hydrogen or an electron withdrawing substituent group; andeach R.sup.2 independently is hydrogen or an optionally hydroxylated and optionally C.sub.1-6 -alkoxylated C.sub.1-6 -alkyl group) and salts thereof, e.g. for use in assays for cis-diols such as glycated blood proteins, having enhanced water-solubility and storage stability.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

Abstract: 1-substituted, 2-substituted 1H-imidazo[4,5-c]-quinolin-4-amines are disclosed. These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.

Abstract: A ganglioside GM3 derivative containing fluorine atoms in a ceramide portion thereof, represented by the formula: ##STR1## in which m is an integer of at least 2, n is an integer of 0 to 7 provided that m is larger than n, and R represents an alkyl group or a fluoroalkyl group is disclosed.

Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, -N(alkoxycarbonyl)-,-N(acyl)- or --S--or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.

Abstract: A new and practical method for synthesizing heterocyclic polyhydroxylated alkaloids using enzymatic aldol condensation and catalytic intramolecular reductive amination is disclosed.

Abstract: Novel multi-azido formals, acetals and ketals are disclosed, having the following generic formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently selected from H, CH.sub.3, and CH.sub.2 N.sub.3, and methods of preparation of these compounds.

Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.

Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.

Abstract: Provided by the present invention is a process for the biocatalytic synthesis of optically pure sphingosines from achiral starting material. The stereoisomers of sphingosine are prepared from chiral arene diols using stereospecific reaction techniques to obtain the desired sphingosine or derivative thereof.

Abstract: Provided by the present invention is a process for the biocatalytic synthesis of optically pure sphingosines from achiral starting material. The stereoisomers of sphingosine are prepared from chiral arene diols using stereospecific reaction techniques to obtain the desired sphingosine or derivative thereof.

Abstract: A process of making poly(glycidyl azide) and 3,6 -dioxadecyl thiocyanate using a phase transfer catalyst that permits the recovery and recycle of the phase transfer catalyst.

Abstract: The present invention provides an improved method of carrying out cationic polymerization of cyclic ether monomers substituted with high-energy, electron-withdrawing pendant groups (e.g., BAMO and NMMO). Such cyclic ether monomers are polymerized with an initiator precursor (i.e., an alcohol) and boron trifluoride tetrahydrofuranate (BF.sub.3 .cndot.THF). It has been discovered that when boron trifluoride tetrahydrofuranate is used as a catalyst in the cationic polymerization of cyclic ether monomers substituted with high-energy, electron-withdrawing pendant groups (e.g., BAMO and NMMO), polymers are produced that have improved functionality and low poly-dispersity. The polymers formed using the method of the present invention are useful for forming cross-linked elastomers which, in turn, are useful for forming elastomeric binders for high-energy compositions, such as propellants, explosives, gasifiers or the like.

Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein R.sup.4 represents:(i) when B represents a closed ring, a group of the general formula: ##STR2## wherein U represents an oxygen atom or a sulfur atom; or (ii) when B represents a divalent group, a group of the general formula: ##STR3## wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8, n, m, p and q are as defined in the specification, and exclusing certain compounds as defined in the specification, depending on whether A represents a single bond or a group. The compounds are useful for the prevention and/or treatment of diseases induced by leukotrienes, 5.alpha.-reductase, phospholipase and aldose reductase in mammals, especially human beings.

Abstract: The invention relates to substituted 5-oxo-di-benzo[a,d]cyclohepta-1,4-dienes of the formula (I) ##STR1## processes for their preparation and their use as retroviral agents.

Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.

Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein A represents a single bond or a group as defined in the specification;B represents(i) a substituted or unsubstituted carbocyclic ring of 4 to 8 members being unreplaced or optionally having one, two or three carbon atom(s) replaced by oxygen, nitrogen and/or sulfur atom(s); or(ii) a divalent group of formula: ##STR2## T represents oxygen or sulfur; R.sup.1 represents a group of general formula: ##STR3## or (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s);R.sup.2 represents hydrogen or a straight or branched alkyl group of from 1 to 6 carbon atom(s);R.sup.' represents hydrogen, a halogen atom, a hydroxy group, a nitro group or a group --COOR.sup.7 ;R.sup.

Abstract: A process for for producing a (2R,3S)-cyclohexylnorstatine or a salt thereof is disclosed, which comprises the steps of: enantioselectively hydrogenating a 4-cyclohexyl-2-halogeno-3-oxobutyric acid ester in the presence of a ruthenium-phosphine complex to produce a 4-cyclohexyl-2-halogeno-(3R)-hydroxybutyric acid ester (2); epoxidizing the compound (2) in the presence of a base to produce a 4-cyclohexyl-(2S,3R)-epoxybutyric acid ester (3); reacting the compound (3) with a lower trialkylsilyl azide in the presence of a Lewis acid to produce a (3S)-azide-4-cyclohexyl-(2S)-substituted butyric acid ester (4); subjecting the compound (4) to hydrogenolysis to produce a (2S,3S)-cyclohexylnorstatine derivative (5); and inverting the configuration at the 2-position of the compound (5).

Abstract: The invention concerns a process of preparation of the polyazido alcohols by reaction of a polysubstituted oxirane having in position .beta. a nucleofuge group with a metal nitride, characterized in that the reaction is performed in an aqueous medium.The oxirane formula is: ##STR1## in which X represents a nucleofuge substituent, R1 represents an atom of hydrogen, a lower alkyl group substituted or not by a halogen, an aryl group possibly substituted, R2 and R3 represent an atom of hydrogen, a lower alkyl radical possibly substituted, an aryl group possibly substituted, R4 represents an atom of hydrogen, a lower alkyl group possibly substituted, an aryl group possibly substituted by an alkoxy group. Application to the preparation of polyamino alcohols, ureas, polyazidothiols and binding compositions for propergols.

Abstract: Described is a process for converting an alcohol to an azide with S.sub.N 2 inversion using a phosphoryl azide, e.g. diphenylphosphoryl azide (DPPA). Good yields of azide in high enantiomeric excess can be achieved specifically for benzylic alcohols and alpha-hydroxy alkyl esters. The process is carried at preferably room temperature in an inert dry aprotic solvent, e.g. toluene, and in the presence of a proton acceptor, e.g. 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) to afford high yields of high enantiomeric purities.

Abstract: The present invention relates to cyclopentane heptanoic or cyclopentane heptenoic acid, 2-hydrocarbyl sulfonamidomethyl, and derivatives thereof, useful as therapeutic agents. In particular, the therapeutic agents of this invention are useful as ocular hypotensives.

Abstract: Glycidyl azide polymers, which are used as binders in composite explosive and propellant compositions, include hydroxyl groups which react with the isocyanate curing agent normally used in such compositions. Since the functionality of available linear glycidyl azide polymers is less than two, triols and/or triisocyanates are needed to crosslink the chains to form a matrix. A glycidyl azide polymer with increased functionality (higher than two) and reactivity obviates the need for triols and triisocyanates in the compositions. Moreover, a glycidyl azide polymer with primary hydroxyl groups would give faster curing reactions at lower temperatures without gassing problems, eliminating the need for a catalyst. Examples of glycidyl azide polymer having increased functionality have one of the formulae: ##STR1## wherein R is ##STR2## wherein m and n are different from zero, and m+n is 4 to 60.

Abstract: The present invention provides novel 2-aliphatic or arylaliphatic cyclopentane heptanoic and heptenoic acid derivatives including at least one azido substituent. In particular 2-aliphatic or arylaliphatic cyclopentane heptenyloic and cyclopentane heptanoic acids and esters thereof, substituted at the 3 and/or 5 position of the cyclopentane ring with radicals selected from the group consisting of hydroxy, azido and mixtures thereof, are disclosed. These azido compounds are useful as ocular hypotensives and are intermediates for the preparation of other compounds useful as ocular hypotensives.

Abstract: A new and practical method for synthesizing heterocyclic polyhydroxylated alkaloids using enzymatic aldol condensation and catalytic intramolecular reductive amination is disclosed.

Abstract: 2-Azido-2,2-difluoroethanol is useful in the preparation of energetic placizers for explosives and propellants. Ethyl 2-bromo-2,2-difluoroacetate reacts with sodium azide to produce ethyl 2-azido-2,2-difluoroacetate which then reacts with sodium borohydride in water to produce the 2-azido-2,2-difluoroethanol.

Abstract: Glycidyl azide polymers, which are used as binders in composite explosive and propellant compositions, include hydroxyl groups which react with the isocyanate curing agent normally used in such compositions. Since the functionality of available linear glycidyl azide polymers is less than two, triols and/or triisocyanates are needed to crosslink the chains to form a matrix. A glycidyl azide polymer with increased functionality (higher than two) and reactivity obviates the need for triols and triisocyanates in the compositions. Moreover, a glycidyl azide polymer with primary hydroxyl groups would give faster curing reactions at lower temperatures without gassing problems, eliminating the need for a catalyst. Examples of glycidyl azide polymer having increased functionality have one of the formulae: ##STR1## wherein R is ##STR2## wherein m and n are different from zero, and m+n is 4 to 60.

Abstract: Novel multi-azido formals, acetals and ketals are disclosed, having the following generic formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently selected from H, CH.sub.3, and CH.sub.2 N.sub.3, and methods of preparation of these compounds.

Abstract: Epichlorohydrin is polymerized with an active hydrogen-containing initiator and the resulting secondary hydroxyl-containing polyepichlorohydrin is further reacted to produce a hydroxyl-terminated polyepichlorohydrin product having chains terminating in a primary hydroxyl group, said polyepichlorohydrin product being reactable with an inorganic azide to produce a poly(glycidyl azide) product useful as a binder for solid rocket propellants.

Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.

Abstract: 1,2-dihydropyrido[3,4-b]pyrazines are provided which possess antimitotic activity. The compounds have the structure: ##STR1## wherein R is a lower alkyl group and OR.sub.1 is a member selected from the group consisting of aryl-alkyl ethers having from seven to about 20 carbon atoms, alkyl carbamates having from one to about 12 carbon atoms, the alkyl portion of which may be substituted with a halogen atom, e.g., chlorine, fluorine, bromine or iodine; aryl-alkyl carbamates having from about seven to about 20 carbon atoms, aryl carbamates having from about six to about 20 carbon atoms, aryl-alkyl esters having from about 7 to about 20 carbon atoms, aryl esters having from about six to about 20 carbon atoms, alkylthiocarbamates having from about one to about 12 carbon atoms, aryl-alkylthiocarbamates having from about seven to about 20 carbon atoms, and arylthiocarbamates having from about six to about 20 carbon atoms.

Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 means a hydrogen atom,their salts with physiologically compatible bases, their cyclodextrin clathrates, processes for their preparation, and their use as medicinal agents.

Abstract: A method for the preparation of chiral 2-amino-1,3-diols is disclosed. The method involves four steps including performance of an aldol condensation with a chiral oxazolidinone on an aldehyde, treating the aldol condensation product with an alkali metal azide, treating the product with a borohydride reagent and reducing the azide to an amine.

Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.

Abstract: Novel trisubstituted phenyl analogs are now found to have activity as for the treatment of congestive heart failure.

Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.

Abstract: .beta.-substituted polyfluoropropionate salts, derivatives and copolymers and processes for the preparation thereof.

Abstract: This present invention provides an improved method for producing N-L-aspartyl-D-alanine fenchyl ester or N-L-aspartyl-methylalanine fenchyl ester and new compositions of fenchol derivatives which are intermediate compositions in the preparation of the above described fenchyl esters.

Abstract: A method of making a product comprising poly(glycidyl azide) by reacting polyepichlorohydrin and alkali and/or alkaline earth metal azides in the presence of certain quaternary amine compounds.