Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula

Abstract: Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scented candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.

Abstract: Hindered amine compounds which are substituted by a long hydrocarbon chain are useful in a number of applications where the solubility or compatibility afforded by said substitution is needed. This is seen particularly for example with white, dyed, dipped, unscented and/or scented candle wax which is effectively stabilized against discoloration and fading by the incorporation therein of a long chain hindered amine alone or in combination with a UV absorber and/or an antioxidant.

Abstract: Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound.

Abstract: One embodiment of the present invention is a compound represented by the Structural Formula (I): 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: 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: The invention relates to novel inhibitors of human tryptase which are used in the pharmaceutical industry for the production of medicaments.

Abstract: The invention provides conjugates of fatty alcohols and pharmaceutical agents useful in treating cancer, viruses, psychiatric disorders. Compositions, pharmaceutical preparations, and methods of preparation of the fatty alcohols-pharmaceutical agent conjugates are provided.

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: This invention relates to piperidine derivatives having antitumor activity and useful as pharmaceuticals such as an antitumor agent.

Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.

Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: The subject invention involves novel acyl isothiocyanate resins of formula (I) and processes for making them: (a) starting with a phenyl carboxy resin, treating the resin with any reagent that converts the carboxy to an acyl halide, followed by treatment with tetranikylammonium thiocyanate or an alkali metal salt thereof, to provide the acyl isothiocyanate resin. The subject invention also involves processes for making guanidine compounds and related cyclized compounds using an acyl isothiocyanate resin, comprising the following steps: (b) reacting the acyl isothiocyanate resin with a primary amine; (c) reacting the product from Step (b) with a sulfur activating agent and ammonia or a primary or secondary amine; (d) treating the product from Step (c) with a strong base or medium strength acid to cleave product from the resin, providing the guanidine compound or/and the related cyclized compound.

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

Abstract: Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidaseactivity are also described.

Abstract: Hindered amines substituted on the N-atom with an hydroxy-substituted alkoxy moiety are particularly effective in stabilizing organic polymer compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not otherwise attainable.

Abstract: This invention relates to compounds of formula (I): wherein: Y is Ar or NR1R2; R1 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), or R″R′NC(S); R2 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R3 is H, C2-6alkenyl, C2-6alkynyl, Het, Ar or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R′, CO2NR′2, N(C═NH)NH2, Het or Ar; R4 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R5 is  Ar-C0-6alkyl, Het-C0-6alkyl, adamantyl-C(O)—, Ar-C(O)—, Het-C(O)— or; R6 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), R″R′NC(S), or R″OC(O)NR′CH(R*)C(O); R7 is C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C0-6alkoxy, Het-C0-6alkoxy, or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R&p

Abstract: The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These can then be reacted with building blocks to form the amine compounds of the invention. This invention further provides libraries or monocyclic, bicyclic and oligomeric amine compounds. Also provided are methods for preparing monocyclic, bicyclic and oligomeric amine compounds and libraries thereof. The present invention also provides pharmaceutical compositions of the monocyclic, bicyclic and oligomeric amine compounds.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.

Abstract: Substituted cyanoenamines of the general formula I 1

Abstract: The present invention relates to a process for the production of salts of cyclic amidines of the general formula (I) The processes described hitherto as prior art enable salts of the compound (I) to be produced only at low yields. As a result of protecting &ohgr;-amino-&agr;-amino acids selectively at the &ohgr;-amino function, oxidative decarboxylation of the latter protected compounds by means of halogen derivatives, and subsequent cyclisation of the oxidatively decarboxylated substances with the addition of acid, according to the invention salts of the compound (I) are achieved in better yields.

Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.

Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.

Abstract: A novel 4-acylamino-2,2,6,6-tetramethylpiperidine derivatives and antioxidants comprising the same. The 4-acylamino-2,2,6,6-tetramethylpiperidine derivatives are represented by formula (A): wherein R1 represents a hydrogen atom, a hydroxyl group, an oxyradical group, an aliphatic group, an acyl group, an aliphatic oxy group or an acyloxy group; and R2 represents an aliphatic group having at least 3 carbon atoms and at least two hydroxyl groups.

Abstract: Partially or completely blocked polyisocyanates having an built-in HALS stabilizer.

Abstract: Novel phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity as well as anti-viral activity. These novel compounds can be incorporated within contraceptive compositions to provide for spermicidal or sperm-immobilizing activity.

Abstract: The invention concerns a compound of formula (I), ##STR1## wherein, for example: R.sup.1 is of the formula --NHC(.dbd.O) (1-4C) alkyl; R.sup.2 and R.sup.3 are hydrogen or fluoro; R.sup.4 and R.sup.5 are hydrogen or methyl; >A--B-- is of the formula >C.dbd.CH--, >CHCH.sub.2, or >C(OH)CH.sub.2 -- (> represents two single bonds); D is O, S, SO, SO.sub.2 or --NR.sup.7 ; wherein R.sup.7 is hydrogen, R.sup.10 CO--, R.sup.10 SO.sub.2 --, R.sup.a OC(R.sup.b).dbd.CH(C.dbd.O)--, R.sup.c C(.dbd.O)C(.dbd.O)--, R.sup.d N.dbd.C(R.sup.e)C(.dbd.O)--, R.sup.f NHC(R.sup.g).dbd.CHC(.dbd.O)-- or R.sup.14 CH(R.sup.13)(CH.sub.2).sub.m --; wherein R.sup.10 is (1-6 C)alkyl [optionally substituted by, for example, hydroxy or (1-6 C)alkanoyl], R.sup.11 C(O)O(1-6 C)alkyl or R.sup.12 O--; wherein R.sup.11 is optionally substituted (1-6 C)alkyl; R.sup.12 is optionally substituted (1-6 C)alkyl; R.sup.a, R.sup.b, R.sup.c, R.sup.d, R.sup.e, R.sup.f, R.sup.g are (1-6 C)alkyl; m is 0 or 1; R.sup.13 is cyano; R.sup.

Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

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: Novel enzyme-inhibitory compounds are disclosed. The subject invention further pertains to methods and compositions for the inhibition of bacteria, viruses, parasites, and other pathogens.

Abstract: The invention relates to a process for reducing the dimerization of piperidines of the formula I ##STR1## where R.sup.1 to R.sup.4 are C.sub.1 - to C.sub.6 -alkyl, R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 together are a CH.sub.2 chain having 2 to 5 carbon atoms, which comprises adding to the piperidine from 0.001 to 0.2% by weight of a reducing agent of the formula MXH.sub.4-m Y.sub.m, where M is an alkali metal, NR.sub.4, where R are identical or different C.sub.1 -C.sub.4 -alkyl groups, or an equivalent of an alkaline earth metal or an equivalent of zinc, X is boron or aluminum, Y is H or CN and m is 0 or 1. The invention also relates to a mixture of piperidines of the formula I, from 0.001 to 0.2% by weight of a reducing agent and from 1 to 1000 ppm of dimers of the piperidines of the formula I, and to the preparation of hindered amine light stabilizers therefrom.

Abstract: A method for improving light fastness of an image, which comprises releasing or forming an image forming dye or a precursor thereof corresponding or counter-corresponding to silver development and allowing an image formed by transferring said image forming dye or precursor thereof to coexist with a compound represented by general formula (I) in an image forming material ##STR1## The symbols in formula (I) are defined in the description. Also disclosed is an image forming material for use in the method.

Abstract: A process for purifying crude piperidines of the formula I ##STR1## where R.sup.1 to R.sup.4 are C.sub.1 -C.sub.6 -alkyl, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 together are a CH.sub.2 -chain of 2 to 5 carbons, which comprises, in a first step, removing high-boiling substances and, if present, water from the crude piperidines by distillation; in a second step, adding from 0.01 to 5% by weight, based on the product of the first step, as a reducing agent; and, in a third step, isolating the piperidines by distillation.

Abstract: Piperidine antioxidants and compositions therewith for preventing the fading of artificial hair dye are described herein.

Abstract: N-monosubstituted 4-aminopiperidine is prepared by a process comprising, in a single stage, continuously passing a 4-oxopiperidine and a primary amine over a metal hydrogenation catalyst under a hydrogen partial pressure of 1-500 bar at a LHSV of up to 1 hr.sup.-1.

Abstract: Selected derivatives of 1-oxyl-2,2,6,6-tetramethyl-4-aminopiperidine are surprisingly effective as inhibitors to prevent the premature polymerization of acrylic and methacrylic acids, their esters, their amides, vinyl acetate and acrylonitrile in the presence of water.

Abstract: 4-Acylaminopiperidine N-oxides IaA.sup.1 B.sup.1 (Ia)where A.sup.1 is hydrogen or an organic radical and B.sup.1 is a radical IIa ##STR1## where R.sup.1 -R.sup.4 are each C.sub.1 -C.sub.4 -alkyl and R.sup.1 and R.sup.2, on the one hand, and R.sup.3 and R.sup.4, on the other hand, may furthermore be bonded to form a 5-membered or 6-membered ring,R.sup.5 is H or C.sub.1 14 C.sub.4 -alkyl andR.sup.6 is H or C.sub.1 -C.sub.18 -alkyl,are used for stabilizing organic materials against the harmful effect of free radicals, particularly in the distillation of monomers which undergo free radical polymerization, especially styrene.

Abstract: A process for acetylating diamines having a sterically hindered amino function and a further, sterically unhindered amino function where the acetylation takes place at the sterically unhindered amino function is provided comprises reacting the diamine with ketene. A preferred diamine is 4-amino-2,2,6,6-tetramethylpiperidine (TAD).

Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.

Abstract: A description is given, as an alternative to known processes, of a process for preparing 4-amino-2,2,6,6-tetramethylpiperidine (TAD) of the formula (I) ##STR1## which comprises the steps of reacting without catalysis, in a first step, 2,2,6,6-tetramethylpiperidine-4-one(TAA) of the formula II ##STR2## with TAD to form 2,2,6,6-tetramethyl4?(2,2,6,6tetramethyl-4-piperidylidene)- amino!piperidine (imine III) of the formula III below ##STR3## and of reacting, in a further step, the imine (III) with ammonia and hydrogen in the presence of a hydrogenation catalyst to give 2 mol equivalents of TAD.

Abstract: A method for the treatment of mammalian tissue injured or at risk of injury during sepsis or shock including the administration to a mammal a diazeniumdiolate which releases a therapeutically effective amount of nitric oxide sufficient to protect the tissue from sepsis- or shock-induced injury.

Abstract: The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.

Abstract: An environmentally friendly process is described for the preparation of 4-acyl-amino-2,2,6,6-tetramethylpiperidine-N-oxyl by the carbonate-mediated hydrogen peroxide oxidation of 4-acylamino-2,2,6,6-tetramethylpiperidine. The reaction can also be run in the absence of any catalyst.

Abstract: Novel oligomeric compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, are disclosed as stabilisers for protecting organic material against oxidative, thermal or light-induced degradation.

Abstract: A process for the continuous preparation of 4-amino-2,2,6,6-tetramethylpiperidine (TAD), comprising: passing triacetoneamine, ammonia and hydrogen over a catalyst of at least two layers in a reactor, wherein at least one catalyst layer comprises at least one element of the 4th, 5th, or 6th row of the 8th transition group of the Periodic Table or combinations of these metal elements on a suitable support, where the catalyst content with respect to each individual catalytically active element changes independently from the reactor inlet to the reactor outlet.

Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: Described herein are compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom andY is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH andY is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.