Abstract: The present disclosure relates to the preparation of ketal compounds from glycerol and levulinic acid and esters, and uses thereof.

Abstract: A process for the production of glycerol acetals of aldehydes selected from the group consisting of isobutyraldehyde, 2-ethylhexyl aldehyde, furfuryl aldehyde and benzaldehyde, in which glycerol is reacted with one or more of those aldehydes in the absence of organic solvents and in the presence of phosphoric acid as catalyst, the molar ratio of glycerol to aldehyde(s) being between 1:1 to 1:1.2.

Abstract: The present invention is to provide manufacturing intermediates which can be led to useful ?-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: wherein R1 and R2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R6—O— or R7—N(R8)—; where R6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R7 and R8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R4 and R5 represent the same groups as R7 and R8, respectively, and R4 and R5 optionally form a ring together; and X represents —O— or —N(R9)—, where R9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R4 or R5, and

Abstract: To provide a curable composition which gives a cured fluorinated product excellent in transparency, light resistance (particularly against a short wavelength light having a wavelength of from 200 to 500 nm) and heat resistance, and having a controlled volume particularly thickness. A curable composition which contains a perfluorocyclic polyene having alicyclic structures which comprise carbon atoms and which may contain an oxygen atom and having at least two carbon-carbon double bonds, at least one of which is a polymerizable carbon-carbon double bond in which at least one of the two carbon atoms forming the polymerizable carbon-carbon double bond is a carbon atom forming the alicyclic structure, and a polymerization initiator; a cured fluorinated product obtained by curing the curable composition; an optical material made of the cured fluorinated product; and a light emitting device encapsulated with the cured fluorinated product in a light-transmitting manner.

Abstract: In the case of the materials according to the invention, the charge carrier mobility in the correspondingly prepared films is achieved if the molecules are composed in such a way that side chains—consisting of conjugated aromatic or heteroaromatic systems—are attached in direct conjugation to a central aromatic or heteroaromatic ring so that the total molecule acquires an octupolar structure. This octupolar structure permits an effective ?-? interaction of the molecules with one another in a manner such that stacking of a plurality of molecules along an imaginary axis (central ring) can take place and various stacks from among these stacks can interact with one another by intermeshing of the side chains. The electronic properties of the materials are determined both by the arrangement of the molecules in a layer and by the molecular design.

Abstract: Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R1 is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3? are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocarbonyl, whereas R3 and R3? do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.

Abstract: A novel method for the preparation of a compound of formula (I) from an N—protected-D-mannosamine. A compound of formula (I) is a useful intermediate for the preparation of kiftnensine, a potent and selective mannosidase inhibitor. The method includes protecting the hydroxyl group at the C-6 position of an N—protected-D-mannosamine, to give a 6—O—protected—N—protected-D-mannosamine; reducing the C-1 anomeric carbon atom of the 6—O—protected—N—protected-D-mannosamine to give a 6—O—protected—N—protected-D-mannitol; protecting the four hydroxyl groups of the 6—O—protected—N—protected-D-mannitol; and removing the nitrogen atom protecting group and optionally removing the C-6 oxygen atom protecting group to give the compound of formula (I): where R1 and R2 are each independently protecting groups which, together with the oxygen atoms to which they are attached, form a 5-, 6-, 7- or 8-membered ring; and R3 is hydrogen or a protecting group.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: Fatty acid amide hydrolase inhibitors of the Formula: 1

Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Compounds that are dual aP2/k-FABP inhibitors are provided having the formula 1

Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I)

Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NR′ wherein R′ is H or loweralkyl, R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.

Abstract: A compound of the Formula (I): wherein Z, R1, R, and Ar2 are as defined in the specification. This invention also relates to sulfonamide compounds of the Formula (I) that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use, and methods for preparing the compounds.

Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NR′ wherein R′ is H or loweralkyl; R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of:  wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.

Abstract: A method of efficiently removing the protective group from a protected hydroxyl or amino group with an allyl derivative by one step reaction under neutral conditions. A protected hydroxyl or amino group is converted into a free hydroxyl or amino group in one-step by adding a reducing agent to an allyl derivative in the presence of nickel dichlorobis (diphenylphospino) propane.

Abstract: The present invention provides Wondonin A of general formula (I), which is extracted from a two-sponge association of phylum Porifera (sponge) and has antiangiogenic activity, and a process for preparing the same. Wondonin A has no cytotoxicity, but has an inhibitory activity against angiogenesis which is one of the crucial mechanisms of cancer cell metastasis, thus, it can be applied not only as an anticancer drug but also as a therapeutic agent of angiogenesis-associated diseases such as cardiac ischemia, rheumatoid arthritis, and diabetes mellitus.

Abstract: The present invention relates to a novel acyclic chiral derivatives of Hibiscus acid of formula I, 1

Abstract: The invention provides a process for covalently coupling organic compounds which comprises reacting an aromatic ring compound having a halogen or halogen-like substituent at a coupling position with a diboron derivative in the presence of a Group VIII metal catalyst and a suitabIe base. The invention also provides useful arylboron intermediates.

Abstract: The present invention concerns novel 7-deoxy taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.

Abstract: The present invention relates to novel benzopyranyl guanidine derivatives of the formula 1, process for preparation therof and pharmaceutical use of the benzopyranyl guanidine derivatives. The benzopyranyl guanidine derivatives of the present invention can be used for protecting heart, neuronal cell or brain damage, preserving organs, and also the benzopyranyl guanidine derivatives are pharmacologically useful for inhibiting NO generation, and for suppressing lipid peroxidation, angiogenesis or restenosis. Wherein R1, R2, R3, R4, R5, R6, n and * are each defined in specification.

Abstract: Omapatrilat (I) is a potent inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) both in vitro and in vivo and is currently undergoing large scale clinical trials as an anti-hypertensive. Omapatrilat may be synthesized using the S-stereoisomer of a racemic mixture. The racemic mixture may be prepared from a hydantoin (III). The hydantoin may be prepared from a novel dinitrile compound (IV): The dinitrile may be produced by reacting a monoacetal with a non-carbonate ammonium salt and an alkali cyanide.

Abstract: A quaternary ammonium cholinergic agent is complexed with a multivalent anion, or with multiple monovalent anions. The complex may be administered orally to a patient to treat pain, or for some other purpose. Numerous modifications are contemplated, including modifications to the ring structure of the compound, substitution and functionalization of the ring. Other contemplated modifications include the use of different anions, including various monovalent and polyvalent anions, and both organic and inorganic anions. The compounds have utility as cholinergic agents, and especially in the treatment of mysasthenia gravis, chest pain, and carpal tunnel syndrome.

Abstract: Polymerisable optically active compounds have the general formula: ##STR1## where: W.sup.1 denotes a polymerisable residue,S.sup.1 denotes a spacer unit,Y.sup.1 denotes a single bond, or one of the groups --O--, --COO--, --OOC--, --OCOO--, --S--, --CONH-- or --NHCO--,M denotes a divalent mesogenic group, andR.sup.1 and R.sup.2 denote straight chain, branched or cyclic alkyl groups with up to 8 carbon atom.

Abstract: The present invention is directed to a synthetic route for preparing endothelium receptor antagonists of formulae (7B) and (7A) and to the chiral intermediates ##STR1##

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: Monomers with cyclic carbonate groups of the formula I are suitable for the production of photosensitive recording materials, for example for the production of offset printing plates ##STR1## in which A means an (n+m)-valent hydrocarbon residue with 3 to 30 C atoms, which may be OH-substituted and may contain up to 8 ether bridges,R means H or methyl;n means an integer from 1 to 5;m means an integer from 1 to 3, providing that n+m is at least 3.

Abstract: Polyol ether derivatives, a method for producing the polyol ether derivatives, and a working fluid composition for a refrigerating machine containing a hydrofluorocarbon and a refrigeration oil containing the polyol ether derivatives as a base oil.

Abstract: Novel taxoids are provided having enhanced water solubility and/or improved pharmacological properties as compared to paclitaxel. The subject taxoids comprise a functional group attached to a paclitaxel at the C-2' and/or C-7 position by a linking group. Functional groups present in the subject taxoids may be hydrophilic chains, groups capable of in vivo conversion to hydrophilic chains, targeting moieties capable of specifically binding with cellular receptors and water soluble polymers of at least 5 kD. The subject taxoids find use in the treatment of hosts suffering from a cellular proliferative disease.

Abstract: The amide derivative of the present invention is one represented by the following general formula (I) and the dermatologic preparation of the present invention is one containing said amide derivative. ##STR1## wherein R.sup.1 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.2 represents a straight-chain or branched, saturated or unsaturated hydrocarbon group carrying 3 to 39 carbon atoms; R.sup.3 represents a group containing at least one group represented by the formula: ##STR2## wherein R.sup.4 and R.sup.5 each represents a hydrogen atom or a straight-chain or branched or cyclic, saturated or unsaturated hydrocarbon group, or R.sup.4 and R.sup.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: Dioxacycloalkane compounds of the formula ?1! ##STR1## wherein A is ##STR2## wherein W is ##STR3## X is --CO-- or --SO.sub.2 --; Y is --CH.sub.2 --, --O-- or --NR.sup.25 --; and R.sup.1 is an aralkyl which may be substituted by lower alkoxy;R.sup.2 is a hydrogen atom or a lower alkyl;R.sup.3 is --(CH.sub.2)d-SR.sup.26 or ##STR4## R.sup.4 and R.sup.5 are each a hydrogen atom or a lower alkyl; and E is --C(R.sup.29)(R.sup.30)-- or --CH.sub.2 CH.sub.2 --, pharmaceutically acceptable salts thereof, intermediates for producing said compounds, and methods for producing said intermediates. The compounds of the formula ?1! have a strong inhibitory activity against renin and show continuous hypotensive action by oral administration. They are useful as hypotensive agents or therapeutic agents for heart failure.

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: The amide derivative of the present invention is one represented by the following general formula (II) and the dermatologic preparation of the present invention is one containing said amide derivative. ##STR1## wherein R.sup.11 represents a straight-chain or branched hydrocarbon group carrying 10 to 40 carbon atoms; R.sup.12 represents a straight-chain or branched hydrocarbon group carrying 1 to 39 carbon atoms; R.sup.13 represents a hydrogen atom or a hydrocarbon group carrying 1 to 6 carbon atoms; and R.sup.14 represents a hydrogen atom or a hydrocarbon group having a straight-chain, branched or cyclic structure and carrying 1 to 40 carbon atoms which may contain an oxygen atom.

Abstract: The present invention relates to novel 7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates which may be used to prepare a final anti-thrombotic, anti-vasospastic product, and to methods for preparing the same.

Abstract: Novel water soluble carbodiimides, and intermediates or derivatives thereof, such as isoureas or isothioureas, are described. A particularly preferred embodiment is bis[4-(2,2-dimethyl-1,3-dioxolyl)methyl] carbodiimide (BDDC), which can be synthesized efficiently from 1,2-isopropylideneglycerol (solketal). The isoureas are effective esterifying agents. The corresponding N-protected amino acid tert-butyl, benzyl, isopropyl, ethyl, and methyl esters can be synthesized in high yield under neutral conditions, with no urea residue after simply washing with aqueous acid. Amino acid couplings utilizing carbodiimide embodiments give peptides in good yield, free of carbodiimide by-products, after washing with dilute acid, while racemization-free peptides are also obtained.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: Compounds of formula I or a pharmaceutically acceptable salt thereof: ##STR1## in which formula R.sub.1 represents an aliphatic hydrocarbyl group; Ar represents a substituted or unsubstituted aromatic nucleus;X represents --SO.sub.2 -- or --CO-- andR.sub.2 and R.sub.3 which may be identical or different represent moieties of formula (a), (b), (c), (d), (e), (f), (g), (h) or (i): ##STR2## wherein B represents the residue of a nucleoside base of formula (A), (G), (C), (H) or (T): ##STR3## provided that when R.sub.2 and R.sub.3 both represent an unsubstituted moiety of formula (a) B represents the residue of a nucleoside base which is of formula (A), (G), (C) or (H) are of value for their antiviral activity.

Abstract: Water-insoluble iodinated esters of the formula (I) ##STR1## useful in X-ray and ultrasound imaging, are disclosed.

Abstract: The present invention provides two basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogs to taxol. Both the intermediates and analogs to taxol may prove to be valuable anticancer agents.

Abstract: Azines of formula (I): ##STR1## in which R and R' either are identical and represent an alkyl radical containing 1 to 4 carbon atoms or an alkenyl radical containing 3 to 5 carbon atoms, or together form a radical of formula (II):--CHR.sub.1 --(CR.sub.2 R.sub.3).sub.n --CHR.sub.4 -- (II)in which R.sub.1, R.sub.2, R.sub.3 and R.sub.4, identical or different, represent a hydrogen atom or an alkyl radical containing 1 to 4 carbon atoms and n represents 0 or 1, in their different stereoisomer forms, their preparation process and their use.

Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.

Abstract: Described is a process for preparing chiral compounds of the formula ##STR1## wherein X.sup.1 and X.sup.2 are independently F or Cl, and Y is Cl, Br or I, comprising reacting a triol of the formula ##STR2## wherein X.sup.1 and X.sup.2 are as defined above, with acetone in the presence of a catalyst, then with a halogen selected from Cl.sub.2, Br.sub.2 or I.sub.2, or N-bromosuccinimide or N-iodosuccinimide.

Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.

Abstract: Water insoluble iodinated esters of formula (I), in which R.sup.1 is a substituted or unsubstituted C.sub.1-20 aliphatic, C.sub.7-20 araliphatic or C.sub.6-20 aryl group or a C.sub.1-20 heterocyclic group having one or more hereto atoms selected from O, S and N; R.sup.2 is hydrogen or a substituted or unsubstituted C.sub.1-6 aliphatic, C.sub.6-10 aryl or C.sub.7-20 araliphatic group; and R.sup.3 is a group as defined above for R.sup.1, which may be the same as or different from R.sup.1, or R.sup.2 and R.sup.3 together represent a substituted or unsubstituted C.sub.1-4 alkylene group, the molecule containing at least one iodine atom and being metabolisable to products which are soluble in body fluids and are physiologically acceptable. The esters are useful in X-ray and ultrasound imaging, especially liver and spleen imaging.

Abstract: Methine dyes with a polyketo group I ##STR1## where A is ##STR2## R.sup.1 is a 5- or 6-membered cycloaliphatic radical which contains one or two hetero atoms from the group --NR.sup.4 --, --O-- and --S-- and which may be fused to an isoaromatic or heteroaromatic group, R.sup.2 and R.sup.3 are identical or different C.sub.1 -C.sub.10 -alkyl groups or together one of the radicals R.sup.1, and m and n are identical or different integers from 0 to 3, are useful as drugs, for producing singlet oxygen, as sensitizers in electrophotographic layers and for photopolymerizations and as laser light sensitive dyes in optical recording media; also novel triketo- and tetraketomethine dyes.

Abstract: A process for the preparation of mono-fatty acid or hydroxymono-fatty acid esters of isopropylidene derivatives of a polyglycerol is disclosed. A C6-C22 fatty acid or -hydroxy fatty acid is reacted with isopropylideneglycerol glycidyl ether or diisopropylidenetriglycerol glycidyl ether in a molar ratio of 0.5:1 to 1:0.5 at temperatures of 373473 K. in the presence of a catalyst. The monoisopropylidenediglycerol mono-fatty acid ester or monoisopropylidenediglycerol hydroxy mono-fatty acid ester or diisopropylidenetetraglycerol mono-fatty acid ester or diisopropylidenetetraglycerol hydroxy mono-fatty acid ester obtained is optionally purified by distillation, fractional distillation and/or ion exchange.

Abstract: A method is provided for preparing carboxylic acid intermediates of the structure ##STR1## wherein an aldehyde of the structure ##STR2## is prepared and subjected to a Horner-Emmons reaction to form the ester of the structure ##STR3## and the ester is hydrogenated to the carboxylic acid which may be used in making the final anti-thrombotic--anti-vasospastic compounds.