Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.

Abstract: Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.

Abstract: Compounds of formula (I): [in which: X is a group of formula >CR1R2 or >SO2; Y is a group of formula >NH or >CR1R2; Z is a group of formula >C?O or >CH2 or a direct bond; R1 is hydrogen and R2 is hydrogen, carboxy or hydroxy; or R1 and R2 together represent an oxo group, a methylenedioxy group or a hydroxyimino group; R3 is hydrogen or lower alkyl; R4 represents two hydrogen atoms, or an oxo or hydroxyimino group; R5 is hydrogen, lower alkyl or halogen; R6 is hydrogen, lower alkoxy or carboxy; R7 and R8 are each hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts and esters thereof can be used for the treatment or prophylaxis of acute or chronic neurodegenerative diseases or conditions such as Alzheimer's Disease, Parkinson's Disease, Huntington's Chorea, Multiple Sclerosis or the sequelae to acute ischaemic events such as heart attack, stroke or head injury and for protection against ischaemic damage to tissues of peripheral organs.

Abstract: [Problem] An agent for treating eye and mouth dryness, which does not accompanies undesirable actions is provided. [Means for Resolution] Administration of the compound A made it possible to accelerate tear and salivary fluid secretion without accompanying sweating and its sustained release administration enabled acceleration of lacrimal gland and salivary gland cell growth as well.

Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).

Abstract: The invention relates to the use of compounds which exhibit an affinity for the ?-opioid receptor of at least 100 nM (Ki value, human) and an affinity for the ORL-1 receptor, wherein the ratio between the affinities ORL1/? defined as 1/[Ki(ORL1)/Ki(?)] is from 0.1 to 30, for the treatment of pain.

Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3 and R4 are as described herein. The compounds exhibit anticancer activity.

Abstract: This invention relates to the compounds of formula (I) shown below. Each variable in formula (I) is defined in the specification. These compounds can be used to treat hepatitis C virus infection.

Abstract: The instant invention relates to the use of compounds that are effective as selective opiate receptor modulators for the manufacture of a pharmaceutical for the diagnosis, prophylaxis and/or the treatment of neuropathy, the clinical pictures and symptoms associated therewith, and related disorders, and to pharmaceutical compositions, comprising one or more of said modulator compounds.

Abstract: Spirocyclic cyclohexane compounds, methods for their production, pharmaceutical compositions containing these compounds, and the use of these spirocyclic cyclohexane compounds for treating conditions associated with the nociceptin/ORL1 receptor system, e.g. pain, drug withdrawal, anxiety, etc.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: The present invention relates to spirocyclic cyclohexane compounds, to methods for their production, to pharmaceutical compositions containing these compounds, to methods of treatment using such compounds and to the use of such spirocyclic cyclohexarie compounds for producing pharmaceutical compositions.

Abstract: Disclosed herein are novel spiro beta-lactone/gamma lactams for use in treating bacterial infections and cancer. The compounds are characterized by a terminal electron-withdrawing group such as a nitro group. Screening data shows antimicrobial activity against various bacterial cell lines, particularly gram-positive bacteria, and anti-cancer activity.

Abstract: Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borne virus, anti-HSV and anti-Hepatitis C virus activity.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.

Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.

Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties.

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula I: or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.

Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (22) listed in the disclosure.

Abstract: An inhibitor of the renin-angiotensin system is useful for the treatment or prevention of the lipodystrophy syndrome, e.g. in AIDS patients also receiving anti-retroviral therapy.

Abstract: The invention relates to novel active compound combinations having very good insecticidal and acaricidal properties and containing (a) cyclic ketoenols having the formula ?in which the groups W, X, Y, Z, A, B, D, and G have the meanings given in the disclosure, and (b) the active compounds (1) to (23) listed in the disclosure. maintaining device useful in producing polyurethane foams.

Abstract: 2-pyrrolidinone derivatives which have in position 4 at least one substituent are described herein. Methods of treating polygltamine disorders such as Huntington's disease, dentorubropallidoluysian atrophy (DRPLA), spinal and bulbar muscular atrophy (SBMA), and spinocerebellar ataxias with 2-pyrrolidinone derivatives are also descibed.

Abstract: The present application describes novel spiro-cyclic ?-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), and/or aggrecanase inhibitors.

Abstract: The invention concerns 1-H-3-arylpyrrolidine-2,4-dione derivatives of formula (I), in which A, B, G, X, Y and Z are as defined in the description, methods of preparing them and intermediates used in their preparation. The compounds of formula (I) are suitable for use as pest-control agents.

Abstract: This invention relates to a process for making spiro isobenzofuranone compounds by coupling of an aminopyrazine fragment with a spirolactone piece.

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.

Abstract: Disclosed is a novel class of substituted imidazole compounds, pharmaceutical compositions containing them and uses of these compounds in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, these compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial. These imidazoles compounds have the formula I wherein R1, R2, R3, R4, R5, R6, A, X, Y and Z are as defined in the specification.

Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: Compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, synergistic compositions comprising amounts of at least two therapeutic agents selected from the group consisting of a renin inhibitor, an angiotensin I converting enzyme inhibitor and an angiotensin II antagonist, which inhibitors and antagonists are present in amounts sufficient to cause synergistic therapeutic effects such as lowering blood pressure and treating congestive heart failure in a mammal.

Abstract: Compound with an indole linked through an aliphatic ring system to an aromatic moiety are useful in treating conditions associated with enhanced P38? kinase activity.

Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: The invention concerns novel mikanolide derivatives, their preparation method and their therapeutic uses, in particular as anti-cancer and anti-viral agents.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: Trifluoromethyl-substituted spirocyclic ketoenols of the formula (I) are provided wherein Het represents one of the groups and G, V, W, X, Y, and Z are as defined in the specification. Also provides are processes for the preparation of the compounds. The compounds of formula (I) find use as pesticides.

Abstract: This invention provides compounds of the formula I: wherein: R1 and R2 are independently H, OH, OAc, alkylaryl, alkylheteroaryl, 1-propynyl, 3-propynyl, and substituted alkyl, O(alkyl), aryl, or heteroaryl; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2C(CH3)2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to C(CH3)2, C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is optionally substituted benzene ring; five or six membered heterocyclic ring; 4 or 7-substituted indole or a substituted benzothiophene; or pharmaceutically acceptable salt t

Abstract: The present invention provides a compound of Formula I or Formula II: 1

Abstract: The present invention relates to a &bgr;;3 adrenergic receptor agonist of formula I: (1); or a pharmaceutical salt thereof; which is useful for treating Type II diabetes and/or obesity.

Abstract: A process produces an optically active amine or its salt and includes the steps of reacting a ketone of Formula (1a): 1

Abstract: Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.

Abstract: A compound represented by the following formula (I) or a salt thereof and a medicament such as an angiogenesis inhibitor and an antitumor agent which comprises said compound or a physiologically acceptable salt thereof as an active ingredient.

Abstract: Spiro[9,10-dihydroanthracene]-9,3′-pyrrolidine (SPAN) and derivatives thereof are provided as selective serotonin receptor antagonists. The compounds are selective, high affinity antagonists of 5-HT2 serotonin receptors. The compounds are useful as antidepressant and antianxiety agents.

Abstract: The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.

Abstract: The present invention provides illudin analogs of the general formula (I): 1

Abstract: The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.

Abstract: There is provided substantially crystalline forms of 4-({3-[7-(3,3-dimethyl-2-oxobutyl)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]propyl}amino)benzo-nitrile; 2-{7-[3-(4-cyanoanilino)propyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate; tert-butyl 2-{7-[4-(4-cyanophenyl)butyl]-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl}ethylcarbamate; or tert-butyl 2-{7-[(2S)-3-(4-cyanophenoxy)-2-hydroxypropyl]-9-oxa-3,7-diazabicyclo-[3.3.1]non-3-yl}ethylcarbamate and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of cardiac arrhythmias.

Abstract: The present invention relates to spirobenzofuran lactam derivatives of the formula I 1

Abstract: The present invention relates to implantable surgical medical devices having coatings comprising one or more compounds that inhibit TNF-&agr; converting enzyme (TACE), more particularly, stents having coatings comprising TACE inhibitors.

Abstract: The invention relates to indole derivatives of formula (I) or (II) for use as inflammation modulators, especially having an inhibitory effect on protein kinases. Formula (I), wherein n=0 or 1, R1=R2=3-indole, R3═COOH— or a ketone, X═O or NH; with the proviso that if n=0, R4═OH and R5=3-indole; and if n=1, R4 together with R5 represents an indole ring system condensed to the structure in the 2,3 position and X═NH. Formula (II), wherein R1=R2=3-indole, X═O, CH2 or a carbonyl group; X═O, a carbonyl group NH or >C═N(R′)2 with R′═CH3 or C2H5. The novel indole derivatives isolated from Melassezia are especially useful as substances for producing a medicament for the treatment of inflammatory or proliferative diseases, especially of the skin, but also of other organ systems.