Abstract: Compounds of the formula wherein R, R1, COOR2, R3–R7, alk, and X have meaning as defined, such being useful as dual inhibitors of angiotensin converting enzyme and neutral endopeptidase, as well as inhibitors of endothelin converting enzyme.

Abstract: A process for preparing 2-{1-[2-(4-chlorophenoxy)propoxyimino]-butyl}-3-hydroxy-5-(tetrahydrothiopyran-3-yl)cyclohex-2-enone lithium salt by reacting the corresponding acid 2-{1-[2-(4-chlorophenoxy)-propoxyimino]butyl}-3-hydroxy-5-(tetrahydrothiopyran-3-yl)-cyclohex-2-enone and lithium hydroxide and the isolation of the lithium salt are described. Here, it is advantageous to use a solvent mixture which comprises methanol and at least one aromatic hydrocarbon and to remove at least some of the solvent prior to the isolation. It is particularly preferred to dissolve the acid in an aromatic hydrocarbon, preferably toluene, and to use a methanolic lithium hydroxide solution. The product, which can be obtained in a more efficient manner by this process, furthermore has considerable advantages with respect to formulation.

Abstract: The invention relates to novel 2-(N,N-di(het)arylamino)-thiophene derivatives of formula (I), wherein R1, R2, R3, R4 and R5 are, independently each of other, each a monofunctional (het)aryl system and wherein R1 can also be a bifunctional (het)arylene system, R3 can also be a group R8, except when R1 is a bifunctional (het)arylene system, R8 representing chemical bond or a bifunctional (het)arylene system, R4 can also mean R10, R10 representing a chemical bond or a bifunctional (het)arylene system, or R4 can be one of the following groups (II) and (III), R9 representing a chemical bond or a bifunctional (het)arylene system and R5 can also be H or (IV).

Abstract: This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substituted deriviatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.

Abstract: Compounds of the formulae IA and Ib. in which X, R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel antiarrhythmic active compounds, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.

Abstract: Aminocycloalkyl compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of local analgesia and anesthesia.

Abstract: The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.

Abstract: Compounds of formula (I): wherein: X is a group of formula (A) or (B): and R1, R2, R3, R4, n, x, y and z are as defined within are described. Processes for their preparation and their use in the treatment of disorders mediated by the neuropeptide Y5 receptor in a warm-blooded animal, such as a human being are also described.

Abstract: Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.

Abstract: In accordance with the present invention, there are provided thermosetting resin compositions with a reduced propensity to shrink in volume upon cure and methods of use therefor. The compositions of the present invention include compounds having aromatic, rigid-rod like spacer groups between the crosslinkable moieties. As such, these compounds impart a degree of liquid crystal-like character to the thermosetting resin composition which results in lower shrinkage upon cure. This effect follows from the well-known expansion that occurs when liquid crystal-like materials pass from a nematic liquid crystal-like state to an isotropic state. Further provided by the present invention are low shrinkage die attach pastes and methods of use therefor.

Abstract: An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a ?-chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the ?-chloro vinyl carbonyl compound in

Abstract: A one-step process for the preparation of a substituted thioxanthone, such as carboxymethoxythioxanthone, in high yields and as a single isomer. The substituted aryl compound is reacted with mercaptobenzoic acid or dithiobisbenzoic acid in the presence of sulphuric acid.

Abstract: A method is disclosed for the preparation of benzo[b]thiophenecarbodithioic esters of the formula: wherein R is alkyl, R1 is hydrogen, halogen, or alkyl, R2, R3, R4, and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, alkylthio, trifluoromethyl, cyano, and aryl, wherein said method comprises reacting an equivalent of an S-thiol ester of the formula: with one-third of an equivalent of P2S5, 2 equivalents of at least one alkali metal carbonate, about 2.5 mole percent of a phase transfer catalyst, and a catalytic amount of water in hot toluene.

Abstract: A method for the preparation of a compound of formula (II) wherein R1 and R2 are independently H, alkyl, alkoxy, oxoalkyl, alkenyl, aryl or arylalkyl whether unsubstituted or substituted, optionally interrupted by one or more hetero atoms, straight chain or branched chain, hydrophilic, hydrophobic or fluorophilic; R3, R4, R5 and R6 are independently or all hydrogen or halogen; provided that at least two of the R3, R4, R5 and R6 are halogens.

Abstract: Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.

Abstract: This invention relates to the identification of a novel class of therapeutic agents which selectively target and kill tumor cells and certain other types of diseased cells, and to compositions comprising lipoic acid derivatives which poison the pyruvate dehydrogenase complex specifically in such cells. This invention also provides for methods of using therapeutically effective amounts of the lipoic acid derivatives for the treatment of cancer and other diseases. The lipoic acid derivatives described herein have a wide range of preventive and therapeutic applications.

Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: An E-isomeric fulleropyrrolidine compound of formula (I): is disclosed. Also disclosed is a method for preparing and polymers prepared from such a compound.

Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: The present invention provides compounds of the formula: wherein X?CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.