Abstract: There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.

Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.

Abstract: The present invention provides certain alpha-amino acids and derivatives thereof, such as, but not limited to, esters, amides and salts. These derivatives may comprise such representative side groups as a phenyl, pyridyl, piperidinyl, tetrahydropyranyl, tetrahydrothiopyranyl, or thienyl group. The present invention further provides a method for synthesizing alpha-amino acids and derivatives thereof via a modified Ugi type reaction using an aldehyde, ammonium formate and a C1-C5 alkyl isocyanide. The compounds provided by this method are useful in the development of new pharmaceuticals for the treatment of human diseases.

Abstract: Described herein are compounds that are useful as caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CN, CHN2, R, or CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, or an aralkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; and R3 is hydrogen, an optionally substituted aryl group, an optionally substituted aralkyl group, or an optionally substituted C1-6 aliphatic group, R4 is an optionally substituted group selected from an aryl group or a heterocyclyl group, or R3 and R4 taken together with the nitrogen to which they are attached optionally form a substituted or unsubstituted monocyclic, bicyclic or tricyclic ring.

Abstract: The present invention relates to a method for reacting amines of the general formula (I) 1

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is adminstered to a patient in need of such treatment.

Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.

Abstract: The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin sensitizer, and a medicament comprising the compound as an active ingredient. That is, the present invention provides a carboxylic acid compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them.

Abstract: Vinylic hindered amine light stabilizers as novel polylmerizable light stabilizers are disclosed and have the general formula (I): wherein: R1 is C1 to C8: alkyl, alkoxy, alkyl phenyl, hydroxy alkyl (all linear and branched), allyl, acyl, cycloalkyl (cyclopentyl, cyclohexyl or curnyl: linear and branched); R2 is hydrogen and methyl, R3 is vinyl, C1-C4 vinyl alkyl [H2C═C(R4)C1-C4], R4 is H, C1-C4 alky and alkyl phenyl and R5 is H, C1-C4 alkyl, X is O, NH, C1-C8 alkyloxy and alkylamino: (linear or branched).

Abstract: One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

Abstract: A process for making enantiomerically enriched 4-piperidinylglycine having the formula (I), said process comprising (a) combining N-protected glycine ester with 4-piperidone to form didehydroamino acid ester; (b) reducing the didehydroamino acid ester with hydrogen gas in the presence of a rhodium catalyst selected from the group consisting of (R,R)-BPE-Rh; (S,S)-BPE-Rh; (R,R)-DuPHOS-Rh; (S,S)-DuPHOS-Rh; and combinations thereof; whereby a protected compound is formed; and (c) removing the protecting groups from the protected compound, whereby the 4-piperidinylglyeine having the formula (I) is formed, wherein X− is an anion wherein X is independently a halogen; and “*” designates an asymmetric carbon having (R)- or (S)-configuration. The process of the invention yields an enantiomerically enriched (R)-4-piperidineglycine or (S)-4-piperidineglycine.

Abstract: A one-pot process for the preparation of functional alkoxyamines of the general formula (I), 1

Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.

Abstract: Compounds of formula wherein A is an unsubstituted or substituted aromatic or non-aromatic, monocyclic or bicyclic heterocyclic radical wherein a ring nitrogen atom may have been replaced by a group R1 is hydrogen or C1-C3alkyl; R2 is hydrogen or C1-C3alkyl; R3 is hydrogen an unsubstituted or substituted C1-C6alkyl, C3-C6cycloalkyl, C2-C6alkenyl or C2-C6alkynyl group, or C(═O)—R5, R5 is C1-C4alkyl, C1-C4alkoxy, an unsubstituted or substituted phenyl, phenoxy or benzyloxy group, or N(R6)2, each R6, independently of the other, is hydrogen, C1-C4alkyl or unsubstituted or substituted phenyl, X is CH—NO2, N—CN or N—NO2 and n is from 1 to 3, in free form or in salt form, and, where appropriate, tautomers of those compounds and the salts thereof, can be used as agrochemical active ingredients and can be prepared in a manner known per se

Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: The invention relates to bifunctional tryptase inhibitors of formula (I) wherein H1 and H2 comprise a Q group and L is a linker of formula and the conformation of the H1, H2 and L groups is such that the groups are separated by a distance of from 20 to 45 Å. Pharmaceutical compositions and crystal forms of the compounds are described in addition to methods for producing and identifying such compounds, as well as the use of such compounds in methods of treating allergic and inflammatory diseases.

Abstract: The present invention relates to novel processes for the preparation of optically active 3-aminocarboxylic acids and their esters, in particular processes for the preparation of optically active compounds of the formula IA or IB 1

Abstract: The present invention relates to nitric oxide-releasing amidine- and enamine-derived diazeniumdiolates, compositions comprising such compounds, methods of using such compounds and compositions, and to a method for the preparation of nitric oxide-releasing amidine and enamine derived diazeniumdiolates via the direct reaction of nitric oxide with amidines and enamines, and to a method of converting amines into such compounds.

Abstract: Compounds and methods of preparing compounds of the formula: RZ—CO—CRaRb—(CRcRd)n—NH—(Y)m—CO—A  (I) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, wherein the substitution pattern on the phenylene group is an ortho, meta, or para substitution pattern and one or more of the hydrogens of the phenylene group may be substituted by a hydrocarbyl group or a functional group; Z is —O— or —NG—, wherein G is H, C1-C12 alkyl or the radical R; wherein R is wherein R1 is hydrogen, C1-C18 alkyl, O, OH, CH2CN, C1-C18 alkoxy, C1-C18 hydroxyalkoxy, C5-C12 cycloalkoxy, C5-C12 hydroxycycloalkoxy, C3-C6 alkenyl, C1-C18 alkynyl, C7-C9 phenylalkyl, unsubstituted or substituted on the phenyl with 1, 2 or 3 C1-C4 alkyl

Abstract: The invention relates to novel inhibitors of human tryptase which are used in the pharmaceutical industry for the production of medicaments.

Abstract: Novel hindered amine light stabilizers of the formula wherein R1 is C1 to C8 alkyl, alkoxy, alkylphenyl, hydroxy alkyl, allyl, acyl, or cycloalkyl; R2 is hydrogen or methyl; R3 is vinyl or C1-4 alkyl vinyl; R4 is hydrogen, C1-4 alkyl or alkyl phenyl; R5 is hydrogen or C1-4 alkyl; and X is O, NH, C1-8 linear or branched chain or alkylamino, are prepared from the corresponding 1-unsubstituted, 4-XH-substituted piperidines by first reaction with a carbonyl compound and subsequent reaction with a vinyl group-containing acyl chloride.

Abstract: Compounds of formula (I) are matrix metalloprotemase inhibitors wherein X represents a carboxylic acid group —COOH, or a hydroxamic acid group —CONHOH;R2 represents a radical of formula (II): R3—(ALK)m—(Q)p—(ALK)n.

Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.

Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.

Abstract: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation.

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: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives.

Abstract: A photochromic grey coloring 2H-naphtho[1,2-b]pyran of formula (1) wherein R1 is selected from mono-, di- or poly-substituted aryl groups, mono-, di- or poly-substituted naphthyl groups and mono-, di- or poly-substituted heteroaryl groups, wherein at least one substituent is a nitrogen containing group, including amino, C1-C20 and C6-C20 alkylamino, C1-C20 and C6-C20 dialkylamino, C2-C20 dialkenylamino, C2-C20 or C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, tetra (C1-C10 linear or branched alkyl) guanidino and cyclic-amino groups and at least one of R7 and R9, which may be the same or different, is selected from C1-C20 N alkylamino C1-C20 N-alkylamido, C1-C20 N,N-dialkylamido, amido, nitro, amino, C1-C20 alkylamino, C1-C20 dialkylamino, C2-C20 dialkenylamino, C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, or cyclicamino groups.

Abstract: Trisubstituted pyrroles are useful in the control of coccidiosis in poultry.

Abstract: The present invention relates to solenopsin alkaloid derivatives which are trans-2,6-disubstituted piperidines according to the structure: wherein R1 and R2 are selected from a C1 to C20 saturated or unsaturated linear, cyclic or branch-chained substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted aromatic group, or an ester group. In certain preferred embodiments, where R1 or R2 contains an unsaturated group, such as an alkenyl group, the double bond in the alkenyl group preferably is found in the hydrocarbon chain between the carbon atom bonded to the piperidine ring and the adjacent carbon atom (&agr; and &bgr; carbons).

Abstract: A composition having the formula: wherein R is a linear alkyl, branched alkyl, cycloalkyl, polycyclic alkyl, alkylaminoalkyl, or alkyloxyalkyl group having 1 to 20 carbon atoms and at least one primary, secondary, or tertiary amino functional group. The composition is effective as a catalyst in the production of polyurethanes.

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: A poly(oxyalkylene)pyridyl or piperidyl ether having the formula: wherein A is a nitrogen-containing ring selected from the group consisting of 3-pyridyl, 4-pyridyl, 3-piperidyl and 4-piperidyl; R1 and R2 are independently hydrogen or lower alkyl and each R1 and R2 is independently selected in each —O—CHR1—CHR2— unit; R3 is hydrogen, alkyl having 1 to about 100 carbon atoms, phenyl, aralkyl having about 7 to about 100 carbon atoms or alkaryl having about 7 to about 100 carbon atoms; n is an integer from about 5 to about 100; and x is an integer from 0 to 4. The poly(oxyalkylene)pyridyl and piperidyl ethers of the present invention are useful as fuel additives for the prevention and control of engine deposits.

Abstract: A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.

Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.

Abstract: Diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating agents are disclosed.

Abstract: This invention provides a convenient, new, one step process for the preparation of 2-(trihaloacetyl)-3-(substituted amino)-2-propenoates and related derivatives thereof by reaction of carbonyl compounds substituted with a trihaloacetyl group with an acetal in the presence of an organic acid. The resulting propenoates are useful as intermediates for the construction of trihalomethyl substituted heterocyclic compounds for use in pharmaceutical and agricultural applications.

Abstract: At least one of a Rh catalyst, a Pd catalyst or a Ru catalyst is used as a catalyst in preparing the salt of &ggr;-(piperidyl)-butyric acid (2) by hydrogenating the salt of &ggr;-(pyridyl)butyric acid (1) [preferably the salt of &ggr;-(pyridyl)butyric acid (1) obtained in the undermentioned steps (a) and (b) and containing not more than 3% by weight of salt of bis(pyridylethyl)acetic acid (3)] in a solvent in the presence of a catalyst: (a) reacting the vinylpyridine (4) with the diester of malonic acid (5) in the presence of a base to give the 2-(pyridylethyl)malonic acid diester (6), and (b) hydrolyzing and decarboxylating the 2-(pyridylethyl)malonic acid diester (6) obtained in the step (a) in an acidic aqueous solution to give the salt of &ggr;-(pyridyl)butyric acid (1).

Abstract: (Meth)acrylate functional compound which is the reaction product of a cyclic secondary amine and a poly(meth)acrylate having at least three acrylate or methacrylate groups, useful for radiation curable coating or ink composition having low viscosity, low volatility, and high cure rate under radiation. Process of preparing a coating or ink composition using such compound. Radiation cured coating or ink based on such composition. Coated or printed article having such a cured coating or ink based on such composition.

Abstract: A poly(oxyalkylene)pyridyl or piperidyl ester having the formula: ##STR1## or a fuel-soluble salt thereof; wherein A is a nitrogen-containing ring selected from the group consisting of 3-pyridyl, 4-pyridyl, 3-piperidyl and 4-piperidyl; R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and each R.sub.1 and R.sub.2 is independently selected in each --O--CHR.sub.1 --CHR.sub.2 -- unit; R.sub.3 is hydrogen, alkyl having 1 to about 100 carbon atoms, phenyl, aralkyl having about 7 to about 100 carbon atoms or alkaryl having about 7 to about 100 carbon atoms; x is an integer from 0 to 4; and n is an integer from about 5 to about 100.The poly(oxyalkylene)pyridyl and piperidyl esters of the present invention are useful as fuel additives for the prevention and control of engine deposits.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The present invention relates to a process for the reduction of an azetidinone-carboxylic acid to an azetidine-alcohol.

Abstract: A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.

Abstract: The invention relates to intermediates and processes for producing benzothiophenes employing hydroxylamines.

Abstract: The present invention provides certain novel compounds, compositions, and a method of treating a mammal by blocking its adenosine receptors comprising administering at least one compound of the present invention. Examples of the present inventive compounds include certain flavonoids of formulae (I) and (II), wherein R.sub.1 to R.sub.4 are as defined in the description, and M is --CH(OH)--CH(R.sub.2)-- or --C(OH).dbd.C(R.sub.2)-- and R.sub.1, R.sub.2 are as defined in the description; or dihydropyridines of formula (III), wherein R.sub.2 to R.sub.6 are as defined in the description; or pyridines of formula (IV), wherein R.sub.2 to R.sub.6 are as defined in the description, or triazoloquinazolines of formula (V), wherein R.sub.1 and R.sub.2 are as defined in the description; and their derivatives, or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides novel heteroaryl compounds having the general formula (I): ##STR1## their pharmaceutical compositions to be used as human and veterinary medicine, particularly in the treatment of dermatological, rheumatic, respiratory, cardiovascular and ophthalmologic conditions, and their use in cosmetic compositions.

Abstract: A description is given of compounds of formula 1 ##STR1## and of compounds of formula 2 ##STR2## wherein X, Y and Z and the radicals R.sup.1 and also m and n have the meanings claimed in claim 1.The cited compounds are advantageously used e.g. for stabilizing organic material against the damaging effect of light, oxygen and/or heat.

Abstract: The invention relates to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): ##STR1## in which: the Z-Y entity represents an N--CH.sub.2, C.dbd.CH or CH--CH.sub.2 group;R.sup.1 represents a hydrogen, fluorine, bromine or iodine atom or a hydroxyl, methoxy, nitrile or nitro group;R.sup.2 represents a hydrogen or bromine atom or a hydroxyl, methoxy, nitrile or nitro group;the R.sub.1 and R.sub.2 substituents both being situated on the same ring of the naphthamide unit or each being situated on one of the rings;R.sup.3 and R.sup.4 can be identical or different and each independently represent a hydrogen or chlorine atom or a methoxy or methyl group or an electron-withdrawing group.The invention also relates to their therapeutic applications as partial agonists of the dopamine D.sub.3 receptor.The invention applies more particularly to the treatment of neuropsychiatric conditions involving the dopamine D.sub.

Abstract: A fluorine-containing polyether compound, a lubricant, and a magnetic recording medium comprising the lubricant.