Abstract: The invention relates to compounds of the formula I in which the radicals have the stated meanings, their stereoisomeric forms and their physiologically tolerated salts and process for their preparation. The compounds are suitable for the treatment of metabohlic disorders such as type 2 diabetes.

Abstract: The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.

Abstract: The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I: where R1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is saturated, unsaturated or aromatic and optionally fused to other ring structures to give a fused ring system and the heterocycle has a total of 1 to 4 N, O and/or S atoms in the ring structures and is optionally monosubstituted, disubstituted or trisubstituted by one or more of the groups -A, —OR4, —N(R4)2, —NO2, —CN, Hal, —COOR4, —CON(R4)2, —COR4, ?O; R2 is a phenyl group which is optionally monosubstituted, disubstituted, trisubstituted, tetrasubstituted or pentasubstituted by one or more of the groups Hal, -A, —O-A, —NO2 or —CN, or is a thienyl group which is optionally monosubstituted or disubstituted by one or more of the groups Hal, -A, —O-A, -NO2, —CN or thienyl; R3 is H, -A, —CO-A, —C(R4)2R2, —C(R4)2-pyridinediyl-R2; R4 is H or -A; A is C1-C6-alkyl, where 1 to 7 hydrogen atoms are optionally replaced by fluor

Abstract: A radioactive iodine-labeled compound represented by the following formula wherein X represents a radioactive iodine atom which may substitute at an arbitrary position on the benzene ring (preferably 123I, 125I and the like.), n represents an integer of 1 to 3, R1 and R2 each independently represent a substituted or unsubstituted alkyl group, Y represents an alkylene group having 1 to 6 carbon atoms (preferably methylene group), M represents a counter ion, and m represents the number of ions required to neutralize the charge of the molecule. A radioactive iodine-labeled compound that can selectively accumulate in tumor cells or tumor tissue and a scintillation imaging agent containing the compound are provided.

Abstract: The invention relates to a group of novel piperazine and piperidine derivatives of the formula wherein Y is hydrogen, halogen, alkyl (1-3C), or CN, CF3, OCF3, SCF3, alkoxy(1-3C), amino or mono- or dialkyl(1-3C) substituted amino or hydroxy, X is O, S, SO or SO2, ---Z represents —C, ?C or —N, R1 and R2 independently represent hydrogen or alkyl (1-3C), Q is benzyl or 2-, 3- or 4-pyridylmethyl, wich groups may be substited with one or more more substituents from the group halogen, nitro, cyano, amino, mono- or di (1-3C)alkylamino, (1-3C) alkoxy, CF3, OCF3, SCF3, (1-4C)-alkyl, (1-3C)alkylsulfonyl or hydroxy, and salts and prodrugs thereof.

Abstract: The present invention relates to new compounds of general formula having thrombin-inhibiting activity. Exemplary are: 1-Methyl-2-[4-(N-hydroxyamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-ethoxycarbonylethyl)-amide, and 1-Methyl-2-[4-(N-methoxycarbonylamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amide.

Abstract: The invention provides novel compounds of formula (I) wherein all variables are as defined in the specification, that are useful as inhibitors of aspartyl proteases.

Abstract: The present invention relates to 4-pyridyl- and 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1: in which the variables have the meanings indicated in the description. The compounds according to the invention have immunomodulating and/or cytokine release-inhibiting action and are therefore utilizable for the treatment of disorders which are connected with a disturbance of the immune system.

Abstract: The present invention relates to benzoxazole compounds represented by the following formula (I): wherein R1 to R4 may be the same or different from each other, and each represent a hydrogen atom, alkyl group having 1 to 6 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, halogen atom, nitro group, cyano group, R12S(O)n, alkoxycarbonyl group having 1 to 4 carbon atoms, amino group, —NHCOR11 or carbonyl group, where R11 and R12 each represent an alkyl group having 1 to 6 carbon atoms, and n is an integer of 0 to 2, A represents a single bond, CHR5—Y, CR5?CR6, CR5R7—CHR6 or CHR5, where R5 represents a hydrogen atom, hydroxyl group, halogen atom or alkyl group, R6 and R7 each represent a hydrogen atom, hydroxyl group, alkyl group, halogen atom or substituted sulfonyloxy group, Y represents O, S or NH, and W represents a substituted or unsubstituted benzene ring or hetero ring, and processes for preparing the same.

Abstract: The present invention relates to novel heterocyclic compounds of formula (I) where A, R1, R2, Y, Z, and n are defined in the disclosure, to processes for their preparation, and to their use as crop protection agents, in particular for controlling animal pests.

Abstract: This application is directed to compounds of the formula wherein j is 1; k is 0 or 1; m is 1, 2 or 3; n is 1 or 2; W1 and W2 are independently —O— or —S(═O)t—, where t is 0, 1, or 2; Y is ═C(R1a)—, where R1a is a member selected from the group consisting of H; F; Cl; CN; NO2; —(C1-C4) alkyl; —(C2-C4) alkynyl; fluorinated-(C1-C3) alkyl; fluorinated-(C1-C3) alkoxy; —OR16; and —C(═O)NR22aR22b; R22a and R22b are defined as set forth in the specification; —RA and RB are each a member independently selected from the group consisting of H; F; CF3; —(C1-C4) alkyl; —(C3-C7) cycloalkyl; phenyl; and benzyl; wherein said cycloalkyl, phenyl, and benzyl moieties are each independently substituted with 0 to 3 substituents R10, which is defined as set forth in the specification; R16 and R17 are defined as set forth in the specification; —RC and RD have the same meaning as defined above for RA and RB except that one

Abstract: A radioactive iodine-labeled compound represented by the following formula 1

Abstract: This invention relates to improved azole derivatives of formula (I): where B is O or S; Het is a heterocycle selected from a number of specified heterocycles and R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are each selected from specified groups; provided that at least one of R6 and R10 is not hydrogen; and to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.

Abstract: The present application relates to novel heterocyclic compounds of formula (I) 1

Abstract: The present invention relates to compounds of the general formula I 1

Abstract: Organic compounds having the formulas I and II are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.

Abstract: Disclosed are compounds of formula (I) 1

Abstract: The present invention relates to a process for preparation of amino substituted benzothiazole derivatives of formula I 1

Abstract: The present invention relates to new cyanine dyes according to the formula (I), wherein A1 and A2 are each independently O, S, or N, and R is H or a carbohydrate that may contain a hetero atom, and m is 0 to 5, and n is 0 to 5.

Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are as described within. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they may be used in the treatment of diseases, related to this receptor.

Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Abstract: A new class of alpha-cyanomethine and alpha-cyanopolymethine dyes is provided having moieties which serve for the covalent attachment to biological substrates and resulting in the fluorescent labeling of the substrates. The labeled substrates are useful in analytical techniques for the detection and measurement of biological and clinical compounds of interest. Of particular interest is a class of methine molecules which are non-fluorescent in buffer solutions but intensely fluoresce when they enter a cell.

Abstract: The present invention relates to a method for the manufacture of asymmetric cyanine dyes of general formula (Ia, Ib, Ic, Id), whereby the dye is produced by carrying out a solid phase condensation reaction.

Abstract: The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.

Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyridine- or 1,4-dihydropyridine-based compounds and pharmaceutical compositions comprising these compounds.

Abstract: Organic compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R1 and R2 in structure I join together to form a 5 to 7 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group in structures I and II.

Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.

Abstract: Chemiluminescent heteroaryl substituted benzothiazole 1,2-dioxetane compounds capable of producing light energy when decomposed are provided. These chemiluminescent compounds are represented by the general formula: The heteroaryl substituent Y can be, for example, a pyridyl group or a benzothiazolyl group. The heteroaryl substituted benzothiazole compounds are substantially stable at room temperature. Kits including the heteroaryl substituted dioxetane compounds as well as methods for using these compounds for detecting the presence of one or more analytes in a sample are also provided.

Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.

Abstract: This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: The present invention relates to compounds of the formula wherein R1, A and R are as described within. The compounds of the present invention have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have an affinity to the A2A-receptor and are therefore useful in the treatment of diseases related to this receptor.

Abstract: The invention relates to novel 2-benzimidazolyl-, 2-benzoxazolyl- and 2-benzothiazolyl hydrazones that are derived from 2-formylpyridine, 2-acylpyridines, acetyldiazines and acetyl(iso)quinolines. The invention also relates to a novel method for producing 2-benzimidazolyl-, 2-benzoxazolyl- and 2-benzothiazolyl hydrazones and to their use as useful anti-cancer therapeutic agents. The novel compounds are also active against multidrug-resistant cancer cells.

Abstract: This invention relates to compounds represented by the general formula [I]   wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to 4-pyridyl- und 2,4-pyrimidinyl-substituted pyrrole derivatives and their use in pharmacy, of the formula 1 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

Abstract: Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: 1

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of arteriosclerosis.

Abstract: Minor groove binding molecules are covalently bound to oligonucleotides which in their base sequence are complementary to a target sequence of single stranded or double stranded DNA, RNA or hybrids thereof. The covalently bound oligonucleotide minor groove binder conjugates strogly bind to the target sequence of the complementary strand.

Abstract: Compounds of Formula I: wherein Ar, Y, m, and Z are as defined in the specification, are useful antipsychotic and antidepressant agents demonstrating potent inhibition of 5-HT reuptake and dopamine D2 receptor antagonism.

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: Organic compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R1 and R2 in structure I join together to form a 5 to 7 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group in structures I and II.

Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments

Abstract: The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives.

Abstract: Disclosed are new organometallic complex molecules having light-emitting and electron-transporting characteristics. Also disclosed is organic EL (electroluminescent) devices using these organometallic complex molecules as electron-transporting materials. The organometallic complex molecules are used to form a light-emitting layer with or without doping of another light-emitting material. The organometallic complex molecules can also be used in an electron-transporting layer of the organic EL device. The organic EL devices incorporating the organometallic complex molecules have high thermal stability.

Abstract: 2-(Benzaryl)pyridines I and salts thereof where n=zero, 1; R1=H, CN, NO2, NH2, OH, SH, SO2—OH, SO2—Cl, SO2—NH2, halogen, optionally halogenated alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl; R2, R3=H, halogen; R4=CN, OH, halogen, alkoxy or optionally substituted benzyloxy; X=—Y—C(ZR5)═N— where the nitrogen is attached to &agr; or &bgr; and Y=—O—, —S—, —N(R6)—; Z=a chemical bond, —O—, —S—, —S(O)—, —SO2—, —N(R7)—; R5, R6, R7=H, optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or 3- to 7-membered heterocyclyl; or R5=H, CN, SH, NH2, halogen, —CH2—CH(halogen)-R8, —CH═CH—R8 or —CH═C(halogen)-R8 (R8=COOH, alkoxycarbonyl, alkylthiocarbonyl, CONH2, alkylaminocarbonyl or dialkylamino