Abstract: The invention relates to siloxane polymers comprising a central polysiloxane polymer block B with organofunctional radicals bonded terminally or laterally to the polymer block and based on IPDI and UV/Vis chromophores or derivatives, in particular UV chromophores, which are covalently bonded via a hydrophobic or hydrophilic linker group Q1?, Q2?, and compositions comprising these siloxanes. Also disclosed are processes for their preparation and their use.

Abstract: Novel Fostriecin (or FST) derivatives represented by formula (I), the pharmaceutical compositions and preparation methods thereof. The pharmaceutical uses of these compounds, especially the use for the preparation of pharmaceutical compositions for treating tumor, inhibiting cell over growth, or lowering myocardial infarction and the injury to cells.

Abstract: Antitumoral compounds obtained from a porifera, of the family Raspailiidae, genus Lithoplocamia, species lithistoides, and derivatives thereof are provided.

Abstract: Antitumoral compounds obtained from a porifera, of the family Raspailiidae, genus Lithoplocamia, species lithistoides, and derivatives thereof are provided.

Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.

Abstract: Novel Fostriecin (or FST) derivatives represented by formula (I), the pharmaceutical compositions and preparation methods thereof. The pharmaceutical uses of these compounds, especially the use for the preparation of pharmaceutical compositions for treating tumor, inhibiting cell over growth, or lowering myocardial infarction and the injury to cells.

Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (

Abstract: A nematic liquid crystal compound represented by any one of formulas (a-1) to (a-6): in formulas (a-1) to (a-6), Ra and Rb are each independently hydrogen or alkyl having 1 to 10 carbons, provided that in the alkyl, —CH2- may be replaced by —O—, —(CH2)2- may be replaced by —CH?CH—, and hydrogen may be replaced by a halogen; ring A1 and ring A2 are each independently trans-1,4-cyclohexylene or 1,4-phenylene, provided that in these rings hydrogen may be replaced by a halogen, and in the case where the ring is trans-1,4-cyclohexylene, —CH2- may be replaced by —O—, and —CH2CH— may be replaced by —CH?C—; and Z1 and Z2 are each independently a single bond, —COO—, —OCO—, —OCH2-, —CH2O— or —CH2CH2-, provided that in formula (a-3), in the case where ring A2 is trans-1,4-cyclohexylene, Z2 is a single bond, —COO—, —OCO—, —OCH2- or —CH2O—, in the case where Ra is —C3H7, Rb is —OC2H5, and Z2 is a single bond, ring A2 is trans-1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, 2-fluoro- 1,4-phenylene, 3-fluoro-1,4-phenylene, 2-f

Abstract: Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.

Abstract: Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.

Abstract: A recording layer including a novel dye for a high density optical recording medium, employing short wavelength laser source with a wavelength not longer than 530 nm for recording high density information and reproduction/playback of the high density information recordings, is provided.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I).

Abstract: Leptomycin-type compounds according to formula I wherein R0, R1, R2, R10, R11, R12, R13, R14, and m are as defined herein, exhibit anti-tumor activity.

Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula VI, or a salt thereof, wherein R1, R2, R3 and R? are as defined in the specification, and processes of manufacturing this compound including intermediates.

Abstract: Leptomycin derivatives having a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody are disclosed. The therapeutic use of such leptomycin derivative conjugates is also described; such conjugates have therapeutic use because they can deliver cytotoxic leptomycin derivatives to a specific cell population in a targeted fashion.

Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, wherein n is 1 or 2; m is 0, 1, 2, 3 or 4; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, hydroxy, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula (

Abstract: Leptomycin-type compounds according to Formula I wherein R0, R1, R2, R10, R11, R12, R13, R14, and m are as defined herein, exhibit anti-tumor activity.

Abstract: The present invention relates to a dinaphthyl ethylene derivative of formula (I), a process for preparing it, a film prepared from it useful in the manufacure of an organic light emitting device (OLED), an OLED including the film, and the use of the dinaphthyl ethylene derivative in the manufacture of an OLED. Wherein R1 to R16 are defined as in the specification.

Abstract: Compounds which mimic the chemical and/or biological activity of discodermolide are provided and intermediates useful in their preparation.

Abstract: Autoinducer compounds which enhance gene expression in a wide variety of microorganisms, therapeutic compositions and therapeutic methods wherein gene expression within microorganisms is regulated are disclosed.

Abstract: This invention provides various biquinone and trimeric quinone derivatives. The invention also provides a method for synthesis of a multi-quinone compound including reacting a hydroxyquinone anion with a first quinone possessing a first directing group at a C-2 of the first quinone and a second directing group at a C-3 of the first quinone and obtaining a biquinone having one of the first and second directing groups at a C-3 of a first quinone monomer and a hydroxyl group at a C-3′ of a second quinone monomer. The biquinone can be further reacted to obtain various biquinone derivatives or with a second hydroxyquinone anion to obtain trimeric quinone derivatives, including trimeric naphthoquinone derivatives. The biquinones and trimeric quinones of this invention demonstrate antiviral activity and can be used to treat viral infections, particularly HIV infections.

Abstract: of the formula (IV): 1

Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.

Abstract: A compound of the formula (I) wherein R1 is a protecting group for N&agr;, R2 is a protecting group for NG, and R3 is aryl, and wherein the compound of formula (I) is a trypsin substrate such that trypsin cleaves the O—C single bond, which liberates R3—OH; a diagnostic device comprising same; a method for preparing the diagnostic device; and a method of using the diagnostic device to detect levels of urinary trypsin inhibitor in a biological sample; and a diagnostic kit for detecting levels of urinary trypsin inhibitor in a biological sample.

Abstract: The present invention relates to a class of compounds represented by the Formula I.

Abstract: The application concerns a compound of formula I: 1

Abstract: This invention features a 5,6-dihydro-2-pyrone compound of formula (I), wherein R1 is H, OH, or C2˜C5 alkoxyl; and R2 is 2-phenyl ethyl, 2-phenyl ethenyl, 2-heteroaryl ethyl, or 2-heteroaryl ethenyl; in which the phenyl or the heteroaryl is optionally mono-, di-, or tri-substituted with R3, R4, or R5; each of R3, R4, and R5, independently, is Cl, F, Br, I, CN, C1˜C5 alkyl, C1˜C5 alkoxyl, C3˜C5 alkenyloxy, C4˜C6 cycloalkoxyl, C4˜C8 cycloalkyl alkoxyl, C3˜C5 alkoxy alkoxyl, or C1˜C4 alkoxy carbonyl.

Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”) , apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.

Abstract: The invention concerns compounds of formula (I) wherein: A represents R1 or (O)R1 where R1 represents an alkyl group comprising 1 to 30 carbon atoms, linear or branched, saturated or unsaturated, capable of being partly or totally substituted by Hal where Hal represents —Cl,—Br, or —F, and of being interrupted by one or several units selected among —O—,—S—,—C(O)—,—NR3C(O)—, —Ph(R4)n— and —CH2—CH2—O)n′—, wherein R3 represents or —CH2)n″—CH where n″=0 to 17; R4 represents, —CH3,—CH2H5,—C3H7 and n=0 to 4 and n′=1, 2, or 3, or R1 represents a cyclanic radical with diterpene or triterpene root; and R2 represents a C1−C11 linear or branched alkyl group.

Abstract: The present invention relates to new compounds of the formula (I) 1

Abstract: There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): wherein R1 represents a hydrogen atom or an alkyl group of 1 to 5 carbons; R2 represents hydrogen, —CO—R5 or —SO2R6; R3 represents hydrogen, an alkyl group of 1 to 5 carbons, etc.; and R4 is a substituent attached to the 4-carbon, 5-carbon, 6-carbon or 7 carbon of the benzofuran ring; and their salts. The compounds are useful as therapeutic agent for hypertriglyceridemia, lipid metabolism enhancers, or prophylactic and/or therapeutic agents for arteriosclerosis.

Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.

Abstract: 2-Phenylpyran-4-one derivatives of formula (I): wherein: R1 represents an alkyl or —NR4R5 group, wherein R4 and R5 each independently represents a hydrogen atom or an alkyl group; R2 represents an alkyl, C3-C7 cycloalkyl, pyridyl, thienyl, naphthyl, tetrahydronaphthyl or indanyl group, or a phenyl group which may be unsubstituted or substituted by one or more halogen atoms or alkyl, trifluoromethyl, hydroxy, alkoxy, methylthio, amino, mono- or dialkylamino, hydroxalkyl or hydroxycarbonyl groups; R3 represents a methyl, hydroxymethyl, alkoxymethyl, C3-C7 cycloalkoxymethyl, benzyloxymethyl, hydroxycarbonyl, nitrile, trifluoromethyl or difluoromethyl group or a CH2—R6 group wherein R6 represents an alkyl group; and X represents a single bond, an oxygen atom, a sulfur atom or a methylene group; or pharmaceutically acceptable salts thereof, processes for their production and synthetic intermediates used in said processes, pharmaceutical compositions containing them and their use

Abstract: A more practical synthesis for preparing discodermolide and structurally related analogues, novel compounds useful in the process and novel compounds prepared by the process.

Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

Abstract: The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions comprising compounds of Formula I as well as methods of treating cyclooxygenase-2 mediated diseases comprising administering to a patient in need of such treatment a non-toxic therapeutically effective amount of a compound of Formula I.

Abstract: The invention encompasses the novel compounds of Formula I, which are useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: The subject invention provides novel compositions of biologically active discodermolide compounds which can advantageously be used for immunomodulation and/or treating cancer. The compounds of the subject invention have utility for use in the treatment of cancer, as tubulin polymerizers and as microtubule stabilization agents. The present invention also pertains to the identification of regions of the discodermolide molecule which are responsible for certain aspects of the bioactivity of discodermolide compounds.

Abstract: Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.

Abstract: A compound selected from the group consisting of a 5,6-dihydro-&agr;-pyrone of formula (I): wherein bond a is oriented either or ; X is O or NH; R1 is selected from the group consisting of: a group R3(O)C— wherein R3 is selected from the group consisting of: (i) a group of formula R4—CH═CH— wherein R4 is C1-C20 alkyl, C2-C20 alkenyl, an aryl group, or a 5- or 6-membered unsaturated heterocyclic ring containing one or two O, N or S atoms, (ii) C2-C20 alkyl; and (iii) an aryl group or a substituent which is a fused ring system of formula (1) or (2):  wherein each of R′ and R″, which are the same or different and may occupy any position on ring a or ring b of said fused ring system, is H or C1-C6 alkyl; a group ArCH2— wherein Ar is an aryl group; and a group R5O—CH2— wherein R5 is C1-C6 alkyl optionally interrupted by one or two O atoms; and R2 is CH3 or, when R1 is a group of formula (A) as defined below, R2 i

Abstract: The invention relates to novel 3-aryl-5-halogeno-pyrone derivatives of the formula (I) ##STR1## in which A, D, G, X, Y, Z and n are each as defined in the description,to a plurality of processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.

Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.

Abstract: A prodrug of the general formula FTLi-(PRT)m, where m is an integer from 1 to 5; FTLi is a ras inhibitor such as a farnesyltransferase inhibitor compound, such as Ia, Ib, Ic; and PRT represents m protecting groups or a precursor thereof, such as compound XVI, which are capable of being cleaved from the ras inhibitor by the action of a enzyme.

Abstract: This invention relates to novel haloenol lactone compounds. These compounds have the following general structure: ##STR1## in which Ar is an aryl group and Y is a haloenol lactone moiety. The compounds of the invention are useful for the specific measurement of particular isoenzymes of glutathione S-transferase. Measurement of glutathione S-transferase isoenzymes has importance in diagnostic medicine. The compounds of the invention are also useful for treatment of drug resistance in cancer and for preventing herbicide resistance in plants.

Abstract: The manufacture and use of compounds of the formula ##STR1## wherein Y is O or S, R.sub.1 is hydrogen or alkyl, and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are hydrogen or various substituent groups, and pharmaceutically acceptable acid addition salts thereof. The compounds have activity as inhibitors of the IL-I or other agonist-induced proteoglycan degradation in bovine nasal cartilage and pharmaceutical compositions containing such compounds are described to treat conditions advantageously affected by such inhibition including arthritis.

Abstract: This invention relates to phenyl amidine alkanoic acids and lactones having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.

Abstract: The inventive Oxalylamino-benzofuran- and benzothienyl-derivatives are prepared by reacting the appropriate amino substituted benzofuranes and benzothiophenes with oxalic acid derivatives. The inventive compounds are suitable for the prevention and treatment of acute and chronic inflammatory processes, particularly of the airways.

Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.