Abstract: The invention is directed to physiologically active compounds of general formula (I): 1

Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.

Abstract: The invention provides compounds having formula (I), wherein W is OH, or derivatives of the carboxylic acid, and Q is a heterocyclo-condensed ortho-phenylene residue. These compounds are useful as MEK inhibitors, particularly in the treatment of proliferative diseases such as cancer.

Abstract: Disclosed is a material for a light emitting device excellent in color purity, good in light emitting characteristics and excellent in stability, which consists of a compound represented by the following general formula (I): L&Parenopenst;A)m  (I) wherein A represents a heterocyclic group in which two or more aromatic heterocycles are condensed; m represents an integer of 2 or more, and the heterocyclic groups represented by A may be the same or different; and L represents a connecting group.

Abstract: A sulfur-containing unsaturated carboxylate compound comprising a sulfur-containing substituent and at least two &agr;,&bgr;-unsaturated carboxylic acid residues, which are each attached to a secondary or tertiary carbon atom via an oxygen atom; a polymerizable composition comprising the sulfur-containing unsaturated carboxylate compound; a cured product prepared by polymerizing the polymerizable composition; an optical component consisting of the cured product; and novel intermediate compounds for preparation of the above carboxylate.

Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic.

Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Abstract: This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: A compound represented by the general formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof, and their medical applications. These compounds inhibit the action of chemokines such as MIP-1&agr; and/or MCP-1 on target cells, and are useful as therapeutic and/or preventative drugs in diseases, such as atherosclerosis, rheumatoid arthritis, and the like where blood monocytes and lymphocytes infiltrate into tissues.

Abstract: This invention involves compounds having the following structure: 1

Abstract: A heterocyclic compound corresponding to formula (I) 1

Abstract: Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.

Abstract: This invention involves compounds having the following structure: as described in the Claims; and enantiomers, optical isomers, stereoisomers, diastereomers, tautomers, addition salts, biohydrolyzable amides and esters thereof, as well as pharmaceutical compositions comprising such novel compounds. The invention also relates to the use of such compounds for preventing or treating disorders modulated by alpha-2 adrenoceptors.

Abstract: The present invention relates to a practical and efficient way to synthesize the compound for the endothelin receptor antagonist involving a Grignard addition and a cyclization reaction to give a desired compound of the general formula shown below: 1

Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ar represents substituted or unsubstituted aryl, wherein the optional substituents are selected from alkyl, hydroxy or alkoxy or, if attached to adjacent carbon atoms any two substituents together with the carbon atoms to which they are attached may form a fused heterocyclic ring of five to six atoms wherein one, two or three of the said atoms are oxygen or nitrogen; A represents a C1-4 n-alkylene group wherein each carbon is optionally substituted by 1 or 2 C1-6 alkyl groups; R1 represents hydrogen, alkyl, alkenyl or cycloalkyl; one or two of of the group of R2, R3 and R4 represents nitro the remaining members of the group of R2, R3 and R4 represent hydrogen; X represents a —CO—NH— moiety; and Z represents C2-4 n-alkylene group wherein each carbon is optionally substituted 1 or 2 C1-6 alkyl groups; a process for preparing such compounds, pharmaceutical compositions comprising such compounds and the use of such compo

Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benz[cd]indolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

Abstract: This invention involves compounds having the following structure: 1

Abstract: A metal coordination compound suitable as an organic material for a luminescent device is represented by the following formula (1): 1

Abstract: The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods.

Abstract: A compound of the formula wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2)— (R2 is H or a substituent group), Z is —N═ or —C(R3)═ (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention provides compounds of formula (I): 1

Abstract: The invention relates to anti-tumour-effective compounds of formula (I), wherein the radicals have the meanings given in the description.

Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents.

Abstract: The invention provides peptide synthons having protected functional groups for attachment of desired moieties (e.g. functional molecules or probes). Also provided are peptide conjugates prepared from such synthons, and synthon and conjugate preparation methods including procedures for identifying the optimum probe attachment site. Biosensors are provided having environmentally sensitive dyes that can locate specific biomolecules within living cells and detect chemical and physiological changes in those biomolecules as the living cell is moving, metabolizing and reacting to its environment. Methods are included for detecting GTP activation of a Rho GTPase protein using polypeptide biosensors. When the biosensor binds GTP-activated Rho GTPase protein, the environmentally sensitive dye emits a signal of a different lifetime, intensity or wavelength than when not bound.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhance reactivity.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: Compounds of formula I in which R1, R2, R3 and A have the meaning set forth in the specification, are selective cyclic nucleotide phosphodiesterase (PDE) inhibitors useful as therapeutics in human and veterinary medicine. They are distinguished by low toxicity, good enteral absorption (high bioavailability), a wide therapeutic breadth and absence of significant side effects.

Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE III inhibition.

Abstract: The invention concerns compounds of formula (1) wherein: R represents a chain (A) or (B); R1 is methyl or ethyl; R2 is either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R3 and R4, identical or different, are either an optionally substituted aromatic or an optionally substituted heteroaromatic ring; R′ represents a hydrogen atom or a —CO—alk radical, their optical isomers, their salts, their preparation and medicines containing them.

Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: Compounds of the formula (i) have therapeutic utility via inhibition of TNF or phosphodiesterase.

Abstract: The present invention relates to pharmaceutical compositions containing, as active ingredient, a compound of formula: 1

Abstract: Protecting groups derived from a halogenated coumarin group, a quinoline-2-one group, a xanthene group, a thioxanthene group, a selenoxanthene group, or an anthracene group are described. The protecting groups is photolabile and can be removed by irradiating the group with light, such as flash photolysis with ultraviolet radiation or pulsed infrared radiation.

Abstract: The present invention relates to compounds of Formula (I) 1

Abstract: A compound of the formula: 1

Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.

Abstract: The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary tract incontinence, and methods for preparing the compounds of Formula (I).

Abstract: Selected amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically inhibiting retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.

Abstract: A cyanine dye having the formula 1

Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eac

Abstract: Compounds are useful for enhancing synaptic responses mediated by AMPA receptors are disclosed, as are methods for the preparation thereof and methods for their use for treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number of excitatory synapses or in the number of AMPA receptors. The invention compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors and for improving memory encoding.

Abstract: The invention relates to a process for preparing chlorobenzoxazoles of the formula (I), in which R1, R2 and R4 are as defined in claim 1 and in case (a) R3=H, halogen, CN, NO2, C1-C5-alkyl, C1-C5-alkoxy, aryl or aryloxy, where each of the 4 lastmentioned radicals is unsubstituted or substituted, or in case (b) R3=chlorine, which comprises reacting benzoxazoles of the formula (II), in which R1, R2 and R4 are as defined in formula (I) and R3 in case (a) is as defined in formula (I) and R3 in case (b) is hydrogen, in the presence of an acidic catalyst with a chlorinating agent to give the monochlorination product (I) or in case (b) with an excess of the chlorinating agent to give the dichlorination product (I) in which R3=chlorine.

Abstract: A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhanced reactivity.

Abstract: Substituted Pyrazol-3-ylbenzazoles I salts thereof, and their use as herbicides or for the desiccation/defoliation of plants.