Abstract: This invention relates in general to certain substituted substituted 1,1,4-1l6-trioxo[1,2]thiazepan-4-ylamides of formula I as defined herein which are protease inhibitors.

Abstract: This invention relates to new 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivatives of formula (1) having anticonvulsant activity which are useful as therapeutic agents for the treatment or prevention of epilepsy and other neurological disorders. The invention also concerns processes for preparing these derivatives and novel intermediates used in the preparation of these derivatives.

Abstract: The present invention relates to quinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: Processes to prepare 5-cyanovaleric acid or its ester are provided, by carbonylation of a pentenenitrile, wherein pentenenitrile is reacted with carbon monoxide and water and/or an alcohol in the presence of a catalyst system. The catalyst system contains: (a) a metal of Group VIII or a compound thereof and (b) a bidentate phosphine, arsine and/or stibine ligand, wherein the bidentate ligand has the general formula (I): R1R2-M1-R-M2-R3R4??(I) ?wherein M1 and M2 are independently P, As or Sb, R is a divalent organic bridging group, which bridging group comprises a chain of 3 to 5 atoms directly connecting the 2 phosphorus atoms, which chain consists of carbon atoms and optionally a nitrogen, oxygen or sulphur atom or a silano or dialkylsilicon group, which alkyl groups independently comprise from 1 to 4 carbon atoms, and R1–R4 represent the same or different optionally substituted tertiary alkyl groups, (c) an acid having a pKa less than 3, as measured at 18° C. in an aqueous solution.

Abstract: The present invention relates to triaryl-oxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, G, and W are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.

Abstract: An amine ether of formula (A) wherein a is 1 or 2; and when a is 1, E is E?; when a is 2, E is L; E? is C1-C36 alkyl; C3-C18 alkenyl; C2-C18 alkinyl; C5-C18 cycloalkyl; C5-C18 cycloalkenyl; a radical of a saturated or unsaturated aliphatic bicyclic or tricyclic hydrocarbon of 7 to 12 carbon atoms; C2-C7alkyl or C3-C7alkenyl substituted by halogen; C7-C15aralkyl or C7-C15 aralkyl substituted by C1-C4 alkyl or phenyl; or E? is a radical of formula (VII) as explained in claim 1; T? is tertiary C4-C18alkyl or phenyl, each of which are unsubstituted or substituted by halogen, OH, COOR21 or C(O)—R22; or T? is C5-C12cycloalkyl; C5-C12cacloalkyl which is interrupted by at least one O or —NR18—; a polycyclic alkyl radical having 7-18 carbon atoms, or the same radical which is interrupted by at least one O or —NR18—; or T? is —C(G1)(G2)—T?; or C1-C18alkyl or C5-C12cycloalkyl substituted by F(I)T? is hydrogen, halogen, NO2, cyano, or is a monovalent organic radical comprising 1-50 carbon atoms; or T? and T? together for

Abstract: The present invention relates to N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein ring X is a 5-7 membered heterocyclic ring, and wherein A, Y, B, and G are as defined in the specification; and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.

Abstract: A process for distillative removal of ammonia from solutions (I) which include a lactam and ammonia comprises effecting said removal in a distillation apparatus (a) at an absolute pressure of less than 10 bar.

Abstract: The present invention is to provide a technology to establish a new cycle-based organic chemical industry, which may be called a polymer cascade (polymer reflux industry) wherein the polymer substances shall not remain the final products, but still give birth to synthetic materials as raw materials for chemical industry and produce useful organic compounds.

Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.

Abstract: Template-fixed &bgr;-hairpin peptidomimetics of the general formulae (I) and (II) wherein Z, Z1 and Z2 are template-fixed chains of 8 to 16 &agr;-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms and cancer cells. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials or as medicaments to treat or prevent infections or diseases related to such infections and/or cancer. These &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

Abstract: This invention relates to new 2-oxo-piperidinyl- and 2-oxo-azepanyl alkanoic acid derivatives of formula (1) having anticonvulsant activity which are useful as therapeutic agents for the treatment or prevention of epilepsy and other neurological disorders. The invention also concerns processes for preparing these derivatives and novel intermediates used in the preparation of these derivatives.

Abstract: Processes to prepare 5-cyanovaleric acid or its ester are provided, by carbonylation of a pentenenitrile, wherein pentenenitrile is reacted with carbon monoxide and water and/or an alcohol in the presence of a catalyst system. The catalyst system contains: (a) a metal of Group VIII or a compound thereof, (b) a certain bidentate phosphine, arsine and/or stibine ligand, and (c) an acid having a pKa less than 3, as measured at 18° C. in an aqueous solution. &egr;-caprolactam is also prepared by reduction of 5-cyanovaleric acid or ester obtained above to 6-aminocaproic acid or ester, and then cyclisation of the 6-aminocaproic acid or ester to &egr;-caprolactam.

Abstract: A method of storing and transporting N-vinyl-&egr;-caprolactam is provided wherein the N-vinyl-&egr;-caprolactam is kept in the liquid phase.

Abstract: It is an object of the present invention to provide a method of continuously producing a lactam in high-temperature high-pressure water, and the present invention relates to a method for producing a lactam characterized by selectively synthesizing the lactam without bringing about hydrolysis by introducing an oxime into flowing high-temperature high-pressure water, wherein the lactam is continuously synthesized at a high rate from the oxime in water at a high temperature of at least 250° C. and a high pressure of at least 12 MPa.

Abstract: The present invention is directed to pharmaceutical compositions containing active compounds, which inhibit the activity of the chemokines, MIP-1&agr; and RANTES. It also is directed to methods of treating inflammatory and immunoregulatory disorders and diseases using these pharmaceutical compositions.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: A process for preparing N-alkenyl-amides by reacting the corresponding NH-amides with acetylenes in the liquid phase in the presence of basic alkali metal compounds and of a cocatalyst comprises using as the cocatalyst diols of the general formula (I) where X is branched or unbranched alkylene selected from the group consisting of where R1 to R6 are independently hydrogen or C1- to C4-alkyl; or branched or unbranched cyclic alkylene of 3 to 14 carbon atoms including 3 to 12 ring carbon atoms, their monoalkenyl ethers, their dialkenyl ethers or mixtures thereof.

Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I), 1

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: A process of producing an aliphatic aldehyde-acid (e.g., adipaldehyde-acid) and/or an aliphatic dicarboxylic acid (e.g., adipic acid) comprising oxidizing a cyclic ketone (e.g., cyclohexanone) with molecular oxygen in the presence of a fixed catalyst which comprises a composite of a carrier and at least one metal element belonging to the groups 4 to 11 of the Periodic Table supported on the carrier and has an acid amount of 0.06 mmol/g or more per unit weight of the carrier.

Abstract: A process for preparing N-alkenyl-amides by reacting the corresponding NH-amides with acetylenes in the liquid phase in the presence of basic alkali metal compounds and of a cocatalyst comprises using as the cocatalyst compounds of the general formulae (Ia) and/or (Ib) R1O—(CH2CH2CH2CH2O)n—H  (Ia): R1O—(CH2CH2CH2CH2O)n—R2,  (Ib): where n is 1, 2 or 3 and R1 and R2 are independently C1- to C6-alkyl or C2- to C6-alkenyl, or together a butenyl unit.

Abstract: The invention relates to a method for purifying lactames, especially lactames obtained by cyclization hydrolysis of an aminoalkylnitrile, and more particularly, to the purification of &egr;-caprolactame obtained by cyclization hydrolysis of the aminocapronitrile. This crystallisation process can either be carried out directly on the cyclization reaction medium after removal of the volatile components or on a medium that has been subjected to different treatments or on a caprolactame extracted from the reaction medium, for example by distillation.

Abstract: Certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of serine proteases, are prepared in various embodiments using Grignard reagents and alkyllithium reagents and various aldehydes to make oxadiazole, thiadiazole and triazole peptoid alcohols, which are then oxidized to the desired keto products.

Abstract: Methods of making low molecular weight methylene acceptors are provided. The methylene acceptors are prepared by reacting a polyhydric phenol with an aromatic olefinic compound in the presence of an acid catalyst, and then further reacting the products of the first reaction with an N-methylol lactam derivative. Derivatives made by the above method, as well as rubber compositions using these derivatives are also provided.

Abstract: A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an &agr;,&bgr;-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is used relative to the substrate as compared with the amount in a conventional process. An optically active amide is produced by asymmetric hydrogenation of an &agr;,&bgr;-unsaturated amide derivative in the presence of a transition metal complex containing a specific phosphine-phosphorane compound.

Abstract: The invention provides an N-alkenyllactam having at least a 6-membered lactam ring, stabilized by phenothiazine and/or derivatives thereof, and a process for the stabilization of N-alkenyllactams.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.

Abstract: Sulfonamide lactams of the following formula wherein X, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R7 and R8 are as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.

Abstract: Piperidine derivatives of the formula I and their physiologically acceptable salts in which X, Y, Z, R1, R2, R3 and R4 are as defined in claim 1 can be as excitatory amino acid antagonists for combating neurodegenerative disorders including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease and Huntington's disease, cerebral ischaemias, infarcts and psychosis.

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

Abstract: Compounds, compositions and methods are disclosed useful for enhancing penetration of a pharmacologically active substances across skin or tissue membranes. Compounds for use in such compositions and methods are highly water-soluble N-substituted polyalkylene oxide derivatives of cyclic amides.

Abstract: Novel compounds of the following general formula or salts thereof. wherein Ring M is a heterocyclic ring having —N═C<, —CO—N< or —CS—N< as the partial structure —X{overscore (— — — — — — — — —)} Y<; Ra and Rb are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.

Abstract: The invention relates to a process for the cyclizing hydrolysis of an aminonitrile compound into a lactam in the presence of a catalyst. The invention relates more particularly to a process for the cyclizing hydrolysis of an aminonitrile compound in the presence of a macroporous particulate catalyst obtained by deposition/impregnation of an oxygenated compound onto a macroporous support such as alumina. The invention applies in particular to the preparation of &egr;-caprolactam by cyclizing hydrolysis of aminocapronitrile.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.

Abstract: The present invention relates to compounds of the formula 1

Abstract: A method of storing and transporting N-vinyl-&egr;-caprolactam is provided wherein the N-vinyl-&egr;-caprolactam is kept in the liquid phase.

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: A process is provided for stabilizing and/or lowering the color number of alkenyl compounds containing a divalent or trivalent heteroatom in the &agr;-position to the double bond, wherein an oxidizing agent is added to the alkenyl compounds.

Abstract: This invention relates to a composition containing (a) a component selected from the group of a mono- or poly- vinyl substituted mono- or poly-ether, a mono- or poly- vinyl substituted lactam, or a mixture thereof contained in an acidic medium and (b) an aliphatic, primary or secondary mono- or poly-amine at a concentration sufficient to adjust the pH of the composition above

Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

Abstract: Processes to prepare 5-cyanovaleric acid or its ester is provided, by carbonylation of a pentenenitrile, wherein pentenenitrile is reacted with carbon monoxide and water and/or an alcohol in the presence of a catalyst system containing

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.

Abstract: Free-flowing flakes of vinyl caprolactam monomer usable below its melting point of 34° C. without developing coloration.

Abstract: A nitroaromatic compound is used to enhance the solubility of a nitroxyl compound in an aromatic hydrocarbon solvent.

Abstract: The invention provides an N-alkenyllactam having at least a 6-membered lactam ring, stabilized by phenothiazine and/or derivatives thereof, and a process for the stabilization of N-alkenyllactams.