Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.

Abstract: Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula: or a pharmaceutically acceptable acid addition salt thereof, in which R1 is alkyl, alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy; alkoxy; dialkylamino; alkanoyloxy; alkanoyloxyaryl; alkoxyalkanoyl; alkoxycarbonyl; dialkylcarbamoyloxy; or aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nitro, or alkanoyloxy. These analogues can be administered, either alone or concurrently with known medications, to treat the above-described diseases.

Abstract: The invention relates method of combating undesired plant growth at a locus, comprising application to the locus of an effective amount of at least one compound of formula (I): wherein R1, R3, A, X, Z and m have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and to novel compounds of formula I as well as to herbicidal compositions containing such compounds as active ingredients.

Abstract: The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.

Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.

Abstract: Compositions comprising novel chemical libraries are prepared. The compositions of the present invention are useful as antibacterial and other pharmaceutical agents and as intermediates for preparation of other pharmaceutical agents. In addition, compounds of the present invention are useful as research reagents.

Abstract: The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: 1

Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.

Abstract: The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Ar′ and Ar are independently optionally substituted aryl or optionally substituted heteroaryl, provided that the ring structure of said optionally substituted heteroaryl comprises not more than two nitrogen atoms; and R11 is hydrogen; or alkyl, cycloalkyl, aryl or heteroaryl, each of which is optionally substituted. The present invention also relates to the discovery that compounds having Formula V are activators of caspases and inducers of apoptosis. Therefore, the compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.

Abstract: Zinc-complex photoiniators and applications therefore are disclosed. The zinc-complex photoinitiators of the present invention include various pendent groups which serve to protect the compound from hydrolysis. In this manner, the stability of the photoinitiator is increased. The photoinitiators of the present invention can be used in many different processes and applications. For example, the photoinitiators are well suited for use in photocurable inks as used in ink jet printers or on a printing press.

Abstract: The present invention relates to a fungicide containing a novel benzoylpyridine derivative or its salt. The present invention provides a fungicide containing a benzoylpyridine derivative represented by the formula (I) or its salt: wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group; n is 1, 2, 3 or 4; R1 is a substitutable alkyl group; R2 is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.

Abstract: A compound of the formula (I) wherein A is O, S, CHR1 or NR2, R1 and R2 are H, lower alkyl, X1 and X2 are H, halogen, nitro, cyano, etc., Y1 is H, lower alkyl, Z1 and Z2 are H, halogen, cyano, hydroxy, lower alkyl, etc., and n is an integer of 2 to 4, a pharmaceutically acceptable salt thereof, a process for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and an intermediate therefor. The compounds (I) of the present invention show a potent PDE IV inhibitory activity as well as an excellent bronchodilating activity, and hence, they are widely useful as a PDE IV inhibitor in the treatment or prophylaxis of allergic inflammatory diseases or organ inflammatory diseases, especially in the treatment or prophylaxis of pulmonary diseases accompanied by airway obstruction such as asthma.

Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions as well as for wounds healing.

Abstract: Compounds of formula (I) wherein the substituents R1, R2, R3 and R4, and the suffixes n and m are as defined in claim 1, and agrochemically acceptable salts and all stereoisomers and tautomers of such compounds are suitable for use as herbicides.

Abstract: The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein Ar1, Ar2, and R1-R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract: This invention pertains to the discovery of a novel family of thiolesters and uses thereof. Also provided for are viricidal compounds and pharmaceutical formulations comprising these novel thiolesters. The invention also provides thiolester-inactivated viruses and thiolester-complexed viral proteins.

Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: 1

Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.

Abstract: The present invention provides formulae for fluorescent compounds that have a number of properties which make them uniquely suited for use in sensors of analytes such as saccharides. The advantageous fluorescent properties include favorable excitation wavelengths, emission wavelengths, fluorescence lifetimes, and photostability. Additional advantageous properties include enhanced aqueous solubility, as well as temperature and pH sensitivity. The compound comprises an aryl or a substituted phenyl botonic acid that acts as a substrate recognition component, a fluorescence switch component, and a fluorophore. Fluorescent compounds are described that are excited at wavelengths greater than 400 nm and emit at wavelengths greater than 450 nm, which is advantageous for optical transmission through skin. The fluorophore is typically selected from transition metal-ligand complexes and thiazine, oxazine, oxazone, or oxazine-one as well as anthracene compounds.

Abstract: Compounds are provided having the formula: wherein A, Q, and X are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such compounds alone or in combination with other antidiabetic agents such as metformin, glyburide, troglitazone and/or insulin.

Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: Disclosed are pyridine amido derivatives of the formula wherein X, Y, and R1 to R6 are as defined herein. These compounds are selective MAO-B inhibitors and are useful in treating diseases such as, for example, Alzheimer's and senile dementia. Also disclosed are pharmaceutical compositions containing such compounds and a method of preparing such compounds.

Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors.

Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.

Abstract: The present invention relates to a fungicide containing a novel benzoylpyridine derivaitive or its salt. The present invention provides a fungicide containing a benzoylpyridine derivative represented by formula (I) or its salt: wherein X is a halogen atom, a nitro group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cyclo(alkoxy group, a hydroxyl group, a substitutable hydrocarbon group, a substitutable alkylthio group, a cyano group, a carboxyl group which may he esterified or amidated, or at substitutable amino group; n is 1, 2, 3 or 4; R1 is a substitutable alkyl group, R2 is a substitutable alkyl group, it substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; and m is 1, 2, 3 or 4, provided that when m is at least 2, R2 may contain an oxygen atom to form a condensed ring.

Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.

Abstract: This invention relates to new aryl ureas and methods for their synthesis. The inventive compounds are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.

Abstract: The present invention provides a compound containing at least one sulfhydryl group and at least one NO donor group, wherein said compound contains one or more protected sulfhydryl groups linked to at least one aromatic ring or a heteroaromatic ring with a nitrogen in the ring structure, which ring is substituted by one or more substitutes bearing at least one terminal —ONO2 group. The present invention further provides pharmaceutical compositions comprising one or more of said compounds as an active ingredient.

Abstract: An unsaturated derivative at the 4-position of 6-tert-butyl-1,1-dimethylindane corresponding to the following formula: in which: X represents: a divalent radical of formula: and Y represents a divalent radical of following formula: R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue selected from the group consisting of residues deriving from glucose, galactose, mannose and glucuronic acid or an amino acid residue deriving from lysine, glycine and aspartic acid, r′ and r″, which are identical or different, represent H, low

Abstract: A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula: in which each An is nitrogen or CRn(n=1 to 5), with the proviso that at least one of the ring members is nitrogen and that two nitrogen atoms are not bonded directly to one another; R1 to R5, if present, independently of one another; C1-4-alkyl or aryl, one of the substituents R1 to R5 being a group of the formula —OR, in which R is an optionally substituted aromatic or heteroaromatic radical; R6 is hydrogen or C1-4-alkyl; and R7 is an optionally substituted aromatic or heteroaromatic radical. The amides are obtained from the corresponding heteroaromatic halogen compounds, the corresponding aromatic amines and carbon monoxide in the presence of palladium diphosphine complex. Compounds of this class (Formula I) are important herbicides.

Abstract: Compositions, methods, and kits for dyeing at least one keratin fiber, comprising at least one specific cationic compound and at least one compound chosen from specific aldehydes, specific ketones, quinones, diiminoisoindoline derivatives, and 3-aminoisoindolone derivatives, with the proviso that the inventive compositions do not comprise an oxidizing agent.

Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions as well as for wounds healing.

Abstract: Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof.

Abstract: In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors.

Abstract: The invention relates to a combination of a nicotinamide derivative and tiotropium or a derivative thereof, compositions containing it and the uses of, such a combination. The combination according to the present invention is useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: This invention relates to new RAR selective retinoid agonists of formula I 1

Abstract: Compounds having the formula (I), 1

Abstract: Disclosed are pyridine amido derivatives of the formula 1

Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: Patients susceptible to or suffering from central nervous system disorders are treated by administering effective amounts of aryl substituted aliphatic amine compounds, aryl substituted olefinic amine compounds or aryl substituted acetylenic amine compounds. A representative compound is (E)-N-methyl-5-(3-pyridinyl)-4-penten-2-amine.

Abstract: The invention concerns a condensation method for at least a carbonyl compound bearing at least an electroattractive group on an aromatic derivative bearing at least a hydroxyl function, characterised in that the electroattractive group present on the carbonyl compound is selected among fluoroalkyl derivatives, esters including orthoesters and nitriles and said condensation is carried out in a basic medium.

Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.

Abstract: Peptide analogs formed by replacing one or more, but not all, amino acids of a peptide chain with 1,2-dihydro-3(6H)-pyridinone, display an unusually strong tendency to assume a &bgr;-strand conformation and to enter into &bgr;-sheet-like interactions with peptides and other peptide analogs that engage in &bgr;-sheet-like interactions with peptides. The peptide analogs of this invention therefore have utility has &bgr;-strand mimics offering advantages over native peptides as well as &bgr;-strand mimics of the prior art.

Abstract: A method of synthesizing a compound having the formula: 1

Abstract: 1

Abstract: Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: 1