Abstract: The invention relates to fluorescent dyes (fluorophores) based on polymethines for use in optical measurement and detection procedures, in particular those employing fluorescence, for example in medicine, in pharmacology and in the biological, materials and environmental sciences.

Abstract: The invention includes pharmaceutically active 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 treating or prophylaxis of undesired thrombosis.

Abstract: The invention relates to vitamin D derivatives of general formula I, 1

Abstract: This invention provides methods for the solution-phase synthesis of arylbenzoxazoles. The methods involve condensation of aminophenols with benzaldehydes to form a Schiff base. The Schiff base is then induced to undergo oxidative cyclization in the presence of DDQ. The resulting arylbenzoxazoles can be separated from the reduced DDQ byproduct by treatment of reaction mixture with a strongly basic ion exchange resin.

Abstract: The use of compounds of the formula I in which R1 and R2 are identical or different, electron-withdrawing radicals chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl and optionally substituted aminocarbonyl, R3 is a hydrogen atom, a C1-C20-alkyl radical or a C3-C20-cycloalkyl radical or a radical of the formula —CH2—CH2—SO3—M+, where M+ is a cation, X is the divalent radical of oxygen, sulfur or the radical where R3 is as defined above, is the divalent radical of the formula II or III, which forms a fused system with the radical of the formula I where R4 can be bonded one or more times to the benzylidene ring I or naphthylidene ring II, and is hydrogen, alkyl, cycloalkyl, alkyloxy, cycloalkyloxy, alkoxycarbonyl, mono- or dialkylaminocarbonyl, alkylamino, dialkylamino, each having up to 20 carbon atoms, and also cyano, amino and SO3—M+, where M+ is a cation,

Abstract: The present invention provides a process for preparation of optically active azabicyclo heptanone derivatives using lactamases that will react with racemic −lactam of formula (I) to give a single enantiomer of lactam (III) and the corresponding ring opened compound of formula (IV) in an enantiomerically pure form.

Abstract: Cyanine dye bioconjugates useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologues. The compounds may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350-1300 nm, the exact range being dependent upon the particular dye. Use of dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.

Abstract: The invention concerns sterically shielded, stabilized fluorescent dyes based on symmetrical or unsymmetrical 3-spirocyanines and their utilization as marker-molecules in analytical procedures. The fluorescent dyes according to the invention are characterized by a strongly reduced proneness towards aggregation due to the insertion of bulky spiro-substituents and thus enable to reach a high degree of coupling to the target molecule without a significant loss of fluorescence due to self quenching effects. They therefor exhibit a high quantum yield and are thus excellently suitable as fluorescent dyes, especially as NIR-fluorescent dyes, for the coupling or binding to biological and non-biological target molecules used in analytical methods. The analytical methods comprise all methods in which fluorescence-optical methods are used to detect biological and non-biological molecules.

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

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:

Abstract: A compound of the following formula or a pharmacologically acceptable salt thereof: 1

Abstract: The present invention relates to substituted pyrazolyl derivatives, compositions comprising such, intermediates, methods of making substituted pyrazolyl derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Abstract: The present invention relates to peptidomimetic compounds which inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The compounds of this invention have a bridged bicyclic moiety at the P2 position. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.

Abstract: Provided are processes and chemical intermediates useful for preparing a compound of the formula I 1

Abstract: The present invention relates to substituted indazole derivatives, compositions comprising such, intermediates, methods of making substituted indazolel derivatives, and methods for treating cancer, inflammation, and inflammation-associated disorders, such as arthritis.

Abstract: The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract: The invention is directed to inhibition of p38-a kinase using compounds of the formula 1

Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

Abstract: There are disclosed compounds of the formula 1

Abstract: The present invention relates to novel 1

Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Orohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

Abstract: This invention relates generally to a novel class of fused heterocyclic compounds of the Formula (I) or Formula (II): 1

Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are 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: Use of a compound of formula (I): wherein X is optionally substituted aminoalkyl, optionally substituted alkylene or an interactive group; Y and Z may be the same or different and are selected from N, O, S and C(R′) wherein R′ is hydrogen, optionally substituted alkyl or optionally substituted alkenyl; ---- is a double bond unless the attached Y or Z group is O or S in which case it is a single bond; and R1 to R11 may be the same or different and are selected from hydrogen, a sterically hindering group and an electron donating group; or any two of R1 to R11, Y, Z, NH and R′ may together with the carbon atoms to which they are attached form an optionally substituted ring which may contain heteroatoms, provided that at least one of R1 to R11 is an electron donating group and that when X is NCH3, Y and Z are N and R1, R2 and R4 to R11 are hydrogen, then R3 is not OH or OCH2CH3; and salts thereof, pharmaceutically acceptable derivatives thereof, pro-drugs thereof and/or tau

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: 1

Abstract: Non-peptide acetamide derivatives of Formula I are specific NK1 antagonists, 1

Abstract: Disclosed are novel compounds having the formula 1

Abstract: The invention provides an asymmetric cyanine dye compound having the structure including substituted forms thereof, wherein, at least one of R1 and R2 is linking group, X is O, S, or Se, and n ranges from 0 to 2. The invention further provides reporter-quencher dye pairs comprising the asymmetric cyanine dyes, dye-labelled polynucleotides incorporating the asymmetric cyanine dyes, and hybridization detection methods utilizing the dye-labelled polynucleotides.

Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4al

Abstract: The present application relates to the use of the carboxylic acid derivatives of general formula

Abstract: A process for preparing 7-(pyrazol-3-yl)benzoxazoles of the formula I 1

Abstract: Compounds of formula (I): 1

Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably,  and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.

Abstract: Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.

Abstract: Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably,  and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.

Abstract: A process is provided for preparing chiral diol sulfones of the structure 1

Abstract: An organic electroluminescent compound of the formula (I) 1

Abstract: This invention relates to compounds of Formula I 1

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

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

Abstract: Substituted (4-bromopyrazol-3-yl)benzazoles I and their salts where R1=H, C1-C4-alkyl, C1-C4-haloalkyl; R2=CN, Cl-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-haloalkylthio, C1-C4-alkylsulfinyl, C1-C4-haloalkylsulfinyl, C1-C4-alkylsulfonyl, C1-C4-haloalkylsulfonyl; R4=H, halogen; R5=H, CN, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Z=—N═C(XR6)—O— or —N═C(XR6)—S—, attached to &agr; via the nitrogen, oxygen or sulfur; X=a chemical bond, oxygen, sulfur, —S(O)—, —SO2—, —NH— or —N(R7)—; R6, R7=Cl-C6-alkyl, Cl-C6-haloalkyl, cyano-Cl-C4-alkyl, hydroxy-C1-C4-alkyl, C3-C6-alkenyl, cyano-C3-C6-alkenyl, C3-C6-haloalkenyl, C3-C6-alkynyl, cyano-C3-C6-alkynyl, C3-C6-haloalkynyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-haloalkoxy-C1-C4-alkyl, C3-C4-alkenyloxy-C1-C4-alkyl, C3-C4-alkynyloxy-C1-C4-alkyl,

Abstract: Acetonides are obtained in a one-step reaction of a carboxylic acid halide, a 1,2-aminoalcohol, and 2-alkoxypropene or 2,2-dialkoxypropane in an ether solvent and in the presence of an inorganic base. Acetonides are also obtained in a two-step reaction scheme in which an acid halide and 1,2-aminoalcohol are reacted in an ether solvent in the presence of LiOH to form a hydroxyamide, which is then reacted with 2-alkoxypropene or 2,2-dialkoxypropane in the presence of acid to form the acetonide. The acetonides resulting from the one-step and two-step protocols can be further reacted with an allylating agent such as an allyl halide in the presence of a strong base to provide the corresponding allyl acetonide. The acetonides and allyl acetonides can serve as intermediates in the production of certain HIV protease inhibitors which are useful for treating HIV infection and AIDS.

Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers 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-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, 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 C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or 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 ea

Abstract: The present invention provides a novel sulfonamide derivative of general formula (I) useful as an inhibitor of matrix metalloproteinase (MMP), its isomers, pharmaceutically acceptable salts thereof and a process for preparing the same. Since the sulfonamide derivatives of the present invention selectively inhibit MMP activity in vitro, the MMP inhibitors comprising the sulfonamide derivatives as an effective ingredient can be practically applied for the prevention and treatment of all sorts of diseases caused by overexpression and overactivation of MMP.

Abstract: Compounds of formula: in which R represents a CR1R2, C═C(R5)SO2R6 or C═C(R7)SO2alk radical, their preparation and the pharmaceutical compositions containing them.

Abstract: The present invention relates to novel 2-aminobenzoxazole derivative compounds of the following formula: 1

Abstract: The present invention encompasses novel sulfonylphenylpyrazole compounds useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: A symmetric cyanine of the formula: 1