Abstract: The present invention further relates to a method of inhibiting MRP1 in a mammal which comprises administering to a mammal in need thereof an effective amount of a compound of formula (I).

Abstract: Provided are chromophores of the formula Q—(—L—Z)x, wherein x is 2 or 3, wherein Q is selected from the group consisting of wherein L is wherein R is an alkyl group having 1 to 20 carbon atoms, and wherein Z is selected from the group consisting of

Abstract: Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and urea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of a variety of conditions including viral diseases and neoplastic diseases.

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

Abstract: Compounds of formula (I) in which the substituents as defined in the description are useful for preventing and treating gastrointestinal disorders.

Abstract: The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.

Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.

Abstract: A benzimidazole derivative or its medically acceptable salt, represented by the following formula (1), that is a human chymase activity inhibitor capable of being applied clinically: 1

Abstract: A process for preparing (1R,3S)-3-(9-chloro-3-methyl-4-oxo-5H-(isoxazoloquinolin-5-yl))cyclohexanecarboxylic acid and esters thereof, as represented by formulas II and III, wherein R is a lower alkyl groups, and A and B are N or O, provided that when A is N, B is O, or when A is O, B is N: Formula (III) and Formula (II).

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

Abstract: The present invention relates to a compounds of formula I, wherein A is olefin, diol, or acetonide; which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.

Abstract: The present invention relates to a compound of formula (I), which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.

Abstract: 1

Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.

Abstract: The invention relates to a substituted 4-trifluoromethyl carbostyril according to formula (I) and is characterised in that the 4-trifluoromethyl carbostyril is provided with an absorption maximum between 350 and 420 nm and a luminescence maximum between 430 and 900 nm. The molecule can be substituted with groups that are useful for complexing metal ions and/or for binding the molecule to relevant groups of a target molecule or a solid supporting material. The carbostyril as described above can inter alia serve as an antenna molecule of a lanthanide complex. Said complexes can be templates and can be brought into contact with a directly bound or free colour molecule which absorbs in the rant of 580-710 nm. Luminescence effects and decay periods can be measured after the contact with a relevant analyte.

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

Abstract: Substituted aza-oxindole derivatives useful as cyclin dependent kinase 11 inhibitors, for preventing/reducing the severity of epithelial cytotoxicity side-effects (e.g., alopecia, plantar-palmar syndrome, mucositis) induced by chemoptherapy and/or radiation therapy in a patient receiving such therapy.

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

Abstract: Disclosed are novel compounds of formula (I): 1

Abstract: The present invention is drawn to pyrrolopyridinium derivatives having a new structural skeleton, preferably containing an intramolecular hemiacetal, which is clearly different from any known Advanced Glycation Endproduct (AGE) and which, when present in an organism, has a bioactivity unlike the conventional AGE. The present invention provides pyrrolopyridinium derivatives and pharmaceutically acceptable salts thereof, an antibody prepared from said derivatives as a hapten, a method for the diagnosis of diabetes, diabetic complications, renal failure, dialysis-related complications, amyloidosis, aging, diseases accompanied by aging, etc. using said derivatives or an antibody prepared therefrom and a method for evaluating effectiveness of pharmaceuticals used to treat diabetes, diabetes-related diseases, dialysis-related complications, aging, diseases accompanied by aging, etc.

Abstract: Compounds of the formula 1 1

Abstract: 1 Compounds of formula (1), in which the substituents as defined in the description are useful for preventing and treating gastrointestinal disorders.

Abstract: Compounds of formula (1), in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.

Abstract: The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II) wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions associated with gonadotropin releasing hormone (GnRH). The compounds of the invention are antagonists of GnRH, useful in the treatment of the infertility, prostate cancer, benign prostate hyperplasia (BPH) and as contraceptives.

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 provides a process of a compound of the formula (I): 1

Abstract: This invention concerns the use of compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dotted line is an optional bond; n is 1 or 2; R1 is hydrogen; halo; formyl; C1-4alkyl optionally substituted with hydroxy, C1-4alkyloxy, C1-4alkylcarbonyloxy, imidazolyl, thiazolyl or oxazolyl; or a radical of formula —X—COOR5, —X—CONR6R7 or —X—COR10 wherein —X—is a direct bond, C1-4alkanediyl or C2-6alkenediyl; R5 is hydrogen, C1-12alkyl, Ar, Het, C1-6alkyl substituted with C1-4alkyloxy, aryl or heteroaryl; R6 and R7 each independently are hydrogen or C1-4alkyl; R2 is hydrogen, halo, C1-4alkyl, hydroxyC1-4alkyl, C1-4alkyloxycarbonyl, carboxyl, formyl or phenyl; R3 is hydrogen, C1-4alkyl or C1-4alkyloxy; R4 is hydrogen, halo, C1-4alkyl, C1-4alkyloxy or haloC1-4alkyl; Z is —CH2—, —CH2—CH2—, —CH═CH—, —CHOH—CH

Abstract: Compounds of formula I are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.

Abstract: 1

Abstract: The invention relates to substituted or unsubstituted benzodioxinothiophenes, their preparation and their use for preparing electrically conductive oligomers or polymers, also oligomers or polymers comprising these thiophene derivatives as repeating unit.

Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.

Abstract: This invention provides a serotonin 5-HT3 receptor partial activator which has a serotonin 5-HT3 receptor activating action, in addition to its serotonin 5-HT3 receptor antagonism, and does not cause constipation as a side effect.

Abstract: Methods of preparing compounds of Formula I 1

Abstract: The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II) 1

Abstract: Disclosed are novel compounds of formula (I): 1

Abstract: Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators and induce cytokine biosynthesis, including interferon and/or tumor biosynthesis, necrosis factor, and inhibit the T-helper-type 2 immune response. The compounds are further useful in the treatment of viral and neoplastic diseases.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, X, Y, A, B and C are as defined herein.

Abstract: These compounds function as antiviral agents, they induce biosynthesis of interferon, and they inhibit tumor formation in animal models. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.

Abstract: The present invention relates to a compound of formula (I) which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.

Abstract: There is disclosed a compound of the formula (A): wherein W is C—G or C—G′ (G is optionally esterified carboxyl; and G′ is halogen); X is oxygen, optionally oxidized sulfur or —(CH2)q—, (q is 0 to 5); R is optionally substituted amino or heterocyclic group; the ring B is optionally substituted nitrogen-containing 5- to 7-membered ring; L is hydrogen, optionally substituted hydrocarbon residue, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl provided that, when W is C—G, L is hydrogen, optionally substituted acyl, optionally substituted carbamoyl, optionally substituted alkoxycarbonyl, optionally substituted thiocarbamoyl or optionally substituted sulfonyl; n is 0 or 1; the ring A may have a substituent. A process for producing the compound (A) and a pharmaceutical composition containing the compound (A) are also disclosed.

Abstract: Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.

Abstract: The present invention relates to a compound of formula (I), which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.

Abstract: Compounds of formula I 1

Abstract: This invention provides compounds of formula 1, having the structure 1

Abstract: The present invention relates to the method of treating leukemia, lymphoma or inhibiting the proliferation of cells with a compound of formula I.

Abstract: The present invention relates to 6-substituted 1,2,4a,5a,8a,8b-hexahydro- and 1,2,3,4,4a,5a,8a,8b-octahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyrid-8(7H)-one derivatives of the general formula (I) and their salts in which the radicals R1, R2, R3, R4, B and A are each as defined in the description, to processes for their preparation and to their use for controlling endoparasites.

Abstract: The present invention relates to the use of 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives of the general formula (I) and salts thereof, in which the radicals R1 to R5 have the meaning given in the description, and to novel 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3′,4′:4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives and processes for their preparation.

Abstract: The invention relates to the use of quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in position 7 by a 1-aminomethyl-2-oxa-7-azabicyclo[3.3.0]oct-7-yl radical, and of their salts for the therapy of Helicobacter pylori infections and associated gastroduodenal disorders.