Abstract: 4-Benzoylpyrazoles of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR10, —OCOR10, —OSO2R10, —S(O)nR10, —SO2OR10, —SO2NR3R10, —NR10SO2R10 or —NR10COR; Q is a pyrazole of the formula II,  which is attached in position 4 and, Substituted 4-benzoylpyralozoles.

Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

Abstract: Epoxysuccinamide derivatives of the formula (1): wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, or aralkyl; R2 is alkyl, alkenyl, alkynyl, aryl, or aralkyl; R3 is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl; X is —O— or —NR4— (R4 is hydrogen, alkyl, aryl, aralkyl, heterocyclic, or heterocyclic-alkyl); Y1 is OR5, SR6, or NR7R8; and Y2 is hydrogen or alkyl. The compounds are useful as remedies for bone diseases and arthritis.

Abstract: Novel spiropyran compounds, particularly with photochromic properties, are disclosed, as well as photochromic compositions and ophthalmic articles (e.g. lenses) containing said compounds. The photochromes have been designed so as to have a high colorability, a high sensitivity to activating radiation breaking the pyran ring, to be entirely or practically free from coloration in a non activated (non exposed) state, to have an intense coloration following activation and a high coverage of the visible spectrum in combination with at least one other photochrome, and to have high rates of coloration/decoloration. The spiropyrans are easily produced and photochemically stable, and are, e.g., of formula (i), wherein L=(a);(b).

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

Abstract: New taxoids of general formula (I): their preparation and pharmaceutical compositions containing them. The new products of general formula (I) in which Z represents a radical of general formula (II): display noteworthy antitumour and antileukaemic properties.

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

Abstract: A compound of the following formula: or a salt thereof, wherein A is hydrogen, halo, hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, furanyl or thienyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

Abstract: The present invention concerns novel 7-ethers of taxane derivatives, their use as antitumor agents and pharmaceutical compositions containing the novel compounds.

Abstract: Compounds of the formula ##STR1## wherein A and X are independently oxygen or sulphur;R.sup.6 is H, halogen, alkyl, alkoxy, alkylthio, cyano, or nitro;Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, or --CH.sub.2 SO.sub.2 --;Q is a substituted or unsubstituted phenyl or aromatic heterocyclic group:useful for the inhibition of the replication of HIV-1, in vitro and in vivo.

Abstract: Biologically-active, water soluble, 3-substituted trioxanes of the formula ##STR1## wherein R represents a COOH-- substituted aryl group, a substituted or unsubstituted heteroaryl group or an alkyl group, and C.sub.12 -(p-carboxy)benzyloxy trioxanes of formula ##STR2## wherein R represents a substituted or unsubstituted alkyl, alkenyl, aryl or heteroaryl group and methods for their use as antiparasitic agents, particularly for the treatment of malaria.

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 application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: This invention relates to a novel oxirane carboxylic acid derivative and thereof manufacturing method. Based on thereof mechanism to inhibit the CPT I, oxirane carboxylic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and less side effects.

Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.

Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.

Abstract: The present invention relates to a group of polyheterocyclic compounds covered by the following formula: ##STR1## wherein each of X.sub.1, X.sub.2, X.sub.3, and X.sub.4, independently, is O, S, NH, or N(C.sub.1-6 alkyl), but one of them must be O, NH, or N(C.sub.1-6 alkyl); each of R.sub.1, R.sub.2, R.sub.5, and R.sub.6, independently, is H or a substituent (e.g., halogen, CN, NO.sub.2, or C.sub.1-4 haloalkyl), but at least one of them must be a substituent; each of R.sub.3 and R.sub.4, independently, is H, C.sub.1-6 alkyl, CHO, CH.sub.2 OH, or CH.sub.2 NH.sub.2 ; and each of m and n, independently, is 0 or 1.

Abstract: Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.

Abstract: The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines 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.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, 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.

Abstract: A process for preparing oxiranemethane derivatives which are useful as intermediates for preparing aspartyl protease inhibitors comprising the steps of activating an aminodiol, acylating the aminodiol and reacting the acylated aminodiol with a base to form an epoxy compound.

Abstract: Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.

Abstract: A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.

Abstract: In accordance with the present invention, there are provided derivatives of chemotherapeutic agents (e.g., paclitaxel), which serve as bifunctional agents. Invention derivatives retain the antitumor activity of the parent compound, and, coupled with the electron affinic substituents thereon, produce compounds which show a strong capability for radiosensitizing tumor cells growing in vitro. It is expected that a single drug which combines the properties of a radiosensitizer with chemotherapeutic activity will offer significant advantages not only to patients, but also to radiotherapists seeking improved modes of treatment. The combination of antitumor properties with electron-affinic function produces novel radiosensitizers, a second generation of drugs which are more powerful to fight cancers. Bifunctional agents with the dual properties of tubulin assembly and electron affinity will make the compounds useful not only as radiosensitizers, but also as cytotoxins.

Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks. The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.

Abstract: The present invention provides an ozonide reducing agent for use in the ozonolysis reaction of an organic compound, the ozonide reducing agent finding wide applications, and being safe and inexpensive from a commercial viewpoint and easy to treat for disposal.The ozonide reducing agent of the invention is a compound wherein sulfur has, at both ends of its molecule, a hydrocarbon residue substituted by a polar functional group.

Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.

Abstract: Intermediate compounds represented as formula (I) useful for the synthesis of 16-phenoxy-prostatrienoic acid derivatives and a preparing method thereof are disclosed. ##STR1## wherein R is tetrahydropyranyl, tetrahydrofuranyl, 2-ethoxyethyl, t-butyldimethylsilyl, triisopropylsilyl or triethylsilyl group; R.sup.1 and R.sup.2 are independently hydrogen or ester-forming group; P is hydrogen, trimethylsilyl or tri-n-butyltin; and wavy line means epi-stereoisomeric mixture.

Abstract: The present invention provides paclitaxel derivatives of formula I ##STR1## and pharmaceutical compositions.

Abstract: Compounds of the formula ##STR1## wherein: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification,Y is alkylene of 3 to 9 carbon atoms,R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle chosen from benzoxazolyl, benzathiazolyl, thiadiazolyl, imidazolyl, dihydroimidazolyl, oxazolyl, thiazolyl, oxadiazolyl, pyrazolyl, oxazolinyl, isoxazolyl, isothiazolyl, furyl, triazolyl, thiophenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl or any of the above substituted with alkyl, alkoxyalkyl, cycloalkyl, halo alkyl, hydroxyalkyl, alkoxy, hydroxy, halo, furyl, thienyl, fluoroalkyl;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines 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.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, 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.

Abstract: The present invention concerns antitumor compounds. More particularly, the invention provides novel taxane derivatives, pharmaceutical compositions thereof, and their use as antitumor agents.

Abstract: The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.

Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.

Abstract: The invention is drawn to a compound having the following formula ##STR1## in which X.sup.1 and X.sup.2, which may be the same or different, represent hydrogen or a hydroxy-protecting group, X.sup.4 is hydrogen, A is selected from --COOAlkyl and CH.sub.2 OH, and B is a hydroxy group, or A and B, when taken together, represent an oxo group. These compounds are useful as intermediates in the production of 19-nor vitamin D derivatives.

Abstract: Intermediate compounds represented as formula (I) useful for the synthesis of 16-phenoxy-prostatrienoic acid derivatives and a preparing method thereof are disclosed. ##STR1## wherein R is tetrahydropyranyl, tetrahydrofuranyl, 2-ethoxyethyl, 3-t-butyldimethylsilyl triisopropylsilyl or triethylsilyl group; R.sup.1 and R.sup.2 are independently hydrogen or ester-forming group; P is hydrogen, trimethylsilyl or tri-n-butyltin; and wavy line means epistereoisomeric mixture.

Abstract: A process for making a dialkyl carbonate which comprises reacting urea with a first alcohol in a carbamate reactor at a temperature and pressure sufficient to convert said urea to an alkyl carbamate; and reacting the alkyl carbamate with a second alcohol in the presence of a dialkyl isocyanato alkoxy tin catalyst or derivatives in a carbonate reactor at a temperature and pressure sufficient to convert the alkyl carbamate to a dialkyl carbonate, wherein the molar ratio of alkyl carbamate to second alcohol is in the range between about 2:1 to about 10:1 and wherein dialkyl carbonate is present within the carbonate reactor in an amount between about 1 to about 3 weight %, based on total alkyl carbamate and second alcohol content, and wherein the second alcohol is either the same as or different from the first alcohol or a mixture of alcohols.

Abstract: This invention relates to taxoids of general formula (I), their preparation and the pharmaceutical compositions which contain them. The products of general formula (I) have notable antitumoral properties. In the general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl or alkoxyacetyl radical,R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, andR.sub.3 represents an alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, optionally substituted aryl (with the exception of unsubstituted phenyl) or heterocyclyl radical.

Abstract: The invention describes intermediates for use in the synthesis of 1.alpha.-hydroxy-19-nor-vitamin D compounds. The intermediates have the following formula: ##STR1## The disclosed process includes (a) the construction of a 5,8-diol-6-yne intermediate by joining ring-A and ring-C/D portions of the desired end product via the condensation of an acetylenic derivative containing the C/D-ring portion of the desired end product with a cyclic dihydroxy ketone representing the A-ring of the desired end product; (b) the partial reduction of the 6,7 acetylenic triple bond linkage between the A and C/D ring portions to obtain a 5,8-diol-6-ene intermediate; and (c) the reductive removal of the 5,8-oxygen functions to generate the required 5,7-diene end product from which the desired 7-trans(7E)-isomer is purified directly, or after optional double bond isomerization of the 7-cis(7Z)-isomer employing a novel thiophenol-promoted isomerization step.

Abstract: The present invention relates to a novel 2-aminothiazolecarboxamide derivative represented by the following general formula (I): ##STR1## in which R.sup.1 -R.sup.5 are defined herein, which is a fungicidal agent useful for controlling phytopathogenic organisms. In addition, the present invention also relates to a process for preparing the novel 2-aminothiazolecarboxamide derivative of formula (I) and use of the compound of formula (I) as an agent for controlling phytopathogenic organisms.

Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.

Abstract: R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

Abstract: The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and method for treatment of certain cancers with these new compounds.

Abstract: A composition of polymer molecules effective to bind, with substantially uniform binding affinity, to a single-stranded polynucleotide containing a target sequence of bases. The polymer molecules are composed of a sequence of base-pairing moieties effective to hydrogen bond to corresponding, complementary bases in the target sequence, under selected binding conditions, and a predominantly uncharged, achiral backbone supporting the base-pairing moieties at positions and in orientations which allow hydrogen bonding between the pairing moieties of the polymer and the corresponding complementary bases in the target sequence. The composition has diagnostic uses, in a solid-support assay system, and therapeutic uses involving inhibition or inactivation of target polynucleotides.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines 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.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, 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.

Abstract: The present invention relates to novel (tetrahydro-3-furanyl)methylamino derivatives of the following formula (1): ##STR1## wherein the variables are defined in the specification, which are useful as insecticides.

Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.