Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: pharmaceutical compositions containing them, to their medicinal use, and to their preparations. The compounds of the invention are particularly useful in the treatment or alleviation of inflammation and inflammation associated disorders, such as, for example, rheumatoid arthritis and osteoarthritis, and in the relief of pain, such as, for example, pain associated with surgery or trauma, in mammals, preferably felines and canines.

Abstract: The present invention relates to a compound of the formula I 1

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

Abstract: According to the present invention, fused imidazole derivatives of the general formula: 1

Abstract: The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1

Abstract: This invention relates to novel pyridazinone derivatives of formula I wherein R1-R4, R7, R8 and X1 are as defined in the summary and pharmaceutically acceptable salts and solvates thereof, methods to inhibit or modulate Human Immunodeficiency Virus (HIV) reverse transcriptase with compounds of formula I, pharmaceutical compositions containing of formula I admixed with at least one solvent, carrier or excipient and processes to prepare compounds of formula I.

Abstract: This invention relates to pharmaceutical compositions and kits comprising pyridazinone compounds and cyclooxygenase-2 inhibitors, therapeutic methods of treatment or prevention of certain complications arising from diabetes mellitus in mammals and therapeutic methods of treatment or prevention of cardiac tissue ischemia in mammals.

Abstract: The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1

Abstract: The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1

Abstract: The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1

Abstract: Compounds of the formula (I) below, or pharmacologically acceptable salts, esters or other derivatives thereof: 1

Abstract: A method of altering specificity of cyclooxygenase-inhibiting compounds that have a COOH moiety by changing the various COOH containing compounds, such as indomethacin, into ester derivatives or into secondary amide derivatives.

Abstract: Compounds of the formula I 1

Abstract: This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.

Abstract: The present invention relates to a &bgr;;3 adrenergic receptor agonist of formula I: (I); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.

Abstract: This invention relates to compounds of the formula (I) in which R1, R2, R3, X and Q are as defined above and their use as PDE IV inhibitors.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain.

Abstract: Disclosed compounds of the formula (I) 1

Abstract: This invention relates to compounds represented by the general formula [I] 1

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein: R1, R2, and R3 are each independently in each occurrence aryl or heteroaryl; R4 is —COOH or tetrazolyl; A, B, m, n, and r are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and processes for their preparation.

Abstract: The present invention relates to the use of certain benzimidazoles for preparing a pharmaceutical composition for the treatment of systemic inflammatory response syndrome and particularly sepsis.

Abstract: Objects of the invention are to provide compounds having excellent activity against interleukin-1&bgr; production and also medicines comprising them as effective ingredients. Pyridazin-3-one derivatives represented by the following formula (1): wherein Ar1 represents a substituted or unsubstituted aromatic group, Ar2 represents a phenyl group having a substituent at least at the 4-position thereof, R1 represents a linear or branched alkyl group, an alkyl group having a cyclic structure, a substituted or unsubstituted phenyl group or a substituted or unsubstituted phenyl(lower alkyl) group, and R2 represents a cyano group, a carboxyl group, a (lower alkoxy)carbonyl group, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted carbamoyl group, or salts thereof; and medicines comprising them as effective ingredients.

Abstract: 1

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

Abstract: Compounds of the formula I 1

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

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, n, and Ar are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract: The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have similar or superior lipid peroxidation (LPO) inhibition activity to the reference compounds. While showing lower toxicity and better water solubility, they also effectively inhibit the cerebral neuronal cell death caused by ROS and show neuroprotective effects against ischemic neuronal degeneration.

Abstract: Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1, 2 and R3 are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.

Abstract: The present invention relates to aminoalkyl-substituted aromatic bicyclic compounds of formula I, 1

Abstract: The present invention relates to cyclooxygenase-2 (COX-2) selective inhibitors of formula I: 1

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: This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.

Abstract: Stasis is treated or prevented in all or any part or parts of the stomach of a patient, especially a human patient, in need of such treatment, where said stasis results from hypomotility in the stomach, particularly gastric hypomotility with delayed emptying of the liquid and/or solid contents of the stomach. Gastric or gastrointestinal disorders are also treated which are characterized by one or more symptoms selected from pain, nausea, vomiting, heartburn, postprandial discomfort, indigestion and gastroesophageal reflux. Such treatment or prevention is achieved by administering to the patient a therapeutically effective amount of an inhibitor of phosphodiesterase-4 (PDE4), including isozyme subtypes thereof, sufficient to treat or prevent such hypomotility or gastric or gastrointestinal disorder in said patient.

Abstract: Medicinal compositions for colorectal cancer to be administered to the large intestine by taking advantage of preparations disintegrating in the large intestine, characterized by containing a cyclooxygenase inhibitor and an HMG-CoA reductase inhibitor. These compositions are appropriate for inhibiting the postoperative liver metastasis and recurrence of colorectal cancer.

Abstract: Quinolylpropylpiperidine derivatives of general formula (I) are described, and are useful as antimicrobial agents. Their preparation is also described.

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: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.

Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula VIII: wherein Z1 is N or C—R9, Z2 is N or CH, and Z3 is N or C—Rx, provided that one of Z1 and Z3 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and Rx, R1, R2, R2′, R3, and R9 are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: Disclosed are substituted benzimidazole compounds of formula(I): 1

Abstract: Compounds of general formula (I), wherein R1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl; each phenyl ring and heteroaromatic ring optionally and independently being further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.

Abstract: The present invention provides a compound of the formula (I):   wherein A ring, B ring and C ring are each independently optionally substituted aromatic carbocycle or optionally substituted 5- or 6-membered heterocycle which may fuse with benzene ring, W1, W2 and/or W3 represents a bond when A ring, B ring and/or C ring is optionally substituted 5-membered heterocycle, X is —O—, —NR1— wherein R1 is hydrogen, lower alkyl etc. or the like, Y is hydrogen, lower alkyl, lower alkenyl or the like, one of V1 and V2 is a bond, and the other is a bond, —O— or the like, and a pharmaceutical composition comprising the same.

Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and a selective COX-2 inhibitor, a prodrug thereof or a pharmaceutically acceptable salt of said selective COX-2 inhibitor or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy and diabetic cardiomyopathy.

Abstract: The present application describes aryl sulfonyls of formula I: 1

Abstract: Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A1 antagonist.