Abstract: Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.

Abstract: Disclosed is use of andrographolide derivative as shown by general formula 1 in manufacture of medicaments for anti-hepatitis C virus, and preventing and treating immunological liver damage caused by virus infection and different chemical liver damage.

Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not to, those associated with cognitive deficits or schizophrenic symptoms.

Abstract: Disclosed is use of andrographolide derivative as shown by general formula 1 in manufacture of medicaments for anti-hepatitis C virus, and preventing and treating immunological liver damage caused by virus infection and different chemical liver damage.

Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases, gastrointestinal diseases and respiratory diseases.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

Abstract: The present invention relates to enaminocarbonyl compounds with the formula I. The present invention also relates to the use of compounds with the formula I for the modification of the taste of a product and/or preparation for oral administration.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: The present invention relates to new phosphodiesterase inhibitors, more specifically soft PDE4 inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new soft PDE4 inhibitors compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including inflammatory diseases.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: The present invention relates to a process for preparing enaminocarbonyl compounds by reacting compounds of the formula (II) with compounds of the formula (III) in which the A, R1, R2 and Z radicals are each as defined in the description, in the presence of a Brønsted acid.

Abstract: The present invention relates to a process for the preparation of enaminocarbonyl compounds of the formula (I) where compounds of the formula (II) are reacted in the presence of a Brønsted acid to give compounds of the formula (I), and A, R1 and Z are as defined in the description, and also corresponding starting compounds which are used in the process according to the invention.

Abstract: Disclosed are novel active compound combinations comprising at least one substituted enaminocarbonyl compound and azadirachtin, which combinations are highly suitable for controlling animal pests such as insects and unwanted acarids. Methods of controlling insects and acarids are also disclosed.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.

Abstract: The invention relates to the use of at least one compound selected from the class of the enaminocarbonyl compounds for enhancing plants' intrinsic defences and/or for improving plant growth and/or for enhancing the resistance of plants to plant diseases which are caused by fungi, bacteria, viruses, MLOs (mycoplasma-like organisms) and/or RLOs (rickettsia-like organisms), and/or for enhancing the resistance of plants to abiotic stress factors.

Abstract: The present application relates to novel substituted enaminothiocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.

Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.

Abstract: The present invention relates to a novel solid form of 4-[[(6-chloropyridin-3-yl)methyl](2,2-difluoroethyl)amino]furan-2(5H)-one, to processes for its preparation and to its use in agrochemical preparations.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: Process for the preparation of 4-aminobut-2-enolide compounds of the formula (I): comprising reaction of a 4-alkoxyfuran-2(5H)-one compound or 4-arylalkoxyfuran-2(5H)-one compound of the formula (II) with an amine of the formula (III) in which R1, R2 and A have the definitions given in the description, in the presence of a Brønstedt acid.

Abstract: The present invention relates to a defined crystalline modification of the compound of the formula (I), to processes for its preparation and to its use in agrochemical preparations.

Abstract: Process for the preparation of 4-aminobut-2-enolide compounds of the formula (I): comprising reaction of a 4-(methylamino)furan-2(5H)-one compound of the formula (II) with an amine of the formula (III) in which R1 and A have the definitions mentioned in the description, optionally in the presence of a Brønstedt acid.

Abstract: The invention relates to a new co-crystal of 4-{[(6-chloropyrid-3-yl)methyl](2,2-difluoroethyl)amino} furan-2(5H)-one with benzoic acid, to processes for the preparation thereof and use thereof.

Abstract: The invention relates to a new co-crystal of 4-{[(6-chloropyrid-3-yl)methyl](2,2-difluoroethyl)amino}furan-2(5H)-one with oxalic acid, and also to processes for preparation thereof and use.

Abstract: The invention relates to a new co-crystal of 4-{[(6-chloropyrid-3-yl)methyl](2,2-difluoroethyl)amino}furan-2(5H)-one (I) with salicylic acid, and also to processes for preparation thereof and use thereof.

Abstract: Process for preparing 2,2-difluoroethylamine derivatives, wherein compounds of the general formula (IV) are reduced to the corresponding 2,2-difluoroethylamine derivatives of the general formula (III), where the A radical is as defined in the description:

Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.

Abstract: This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.

Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.

Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.

Abstract: The present invention relates to a process for the preparation of enaminocarbonyl compounds of the formula (I) where compounds of the formula (II) are reacted in the presence of a Brønsted acid to give compounds of the formula (I), and A, R1 and Z are as defined in the description, and also corresponding starting compounds which are used in the process according to the invention.

Abstract: The present invention relates to a process for preparing enaminocarbonyl compounds by reacting compounds of the formula (II) with compounds of the formula (III) in which the A, R1, R2 and Z radicals are each as defined in the description, in the presence of a Brønsted acid.

Abstract: The present invention relates to enaminocarbonyl compounds with the formula I, in which X denotes O or CH2, Y denotes N and each of R1 and R2 denotes hydrogen, or Y denotes a CH and either R1 or R2 denotes a C1-4 alkyl, and the remaining R1 or R2 denotes hydrogen, selected (for Y denoting CH and R1 or R2 denoting a C1-4 alkyl) from a group encompassing a mixture of R and S enantiomers enriched in either enantiomer R or enantiomer S, enantiomer R and enantiomer S. The present invention also relates to the use of compounds with the formula I, in which X denotes O or CH2, Y denotes a CH and either R1 or R2 is selected from a group encompassing hydrogen and a C1-4 alkyl, and the remaining R1 or R2 denotes hydrogen, for the modification of the taste of a product and/or preparation for oral administration.

Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.

Abstract: Process for the preparation of 4-aminobut-2-enolide compounds of the formula (I): comprising reaction of a 4-alkoxyfuran-2(5H)-one compound or 4-arylalkoxyfuran-2(5H)-one compound of the formula (II) with an amine of the formula (III) in which R1, R2 and A have the definitions given in the description, in the presence of a Brønstedt acid.

Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

Abstract: Process for the preparation of 4-aminobut-2-enolide compounds of the formula (I): comprising reaction of a 4-(methylamino)furan-2(5H)-one compound of the formula (II) with an amine of the formula (III) in which R1 and A have the definitions mentioned in the description, optionally in the presence of a Brønstedt acid.

Abstract: The present application relates to novel substituted enaminothiocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: Disclosed is a composition for agricultural use, which is used for controlling or preventing plant diseases caused by plant pathogens. The composition for agricultural use contains a compound represented by formula (1), a salt thereof or a hydrate of the compound or the salt. (1) [In the formula, Z represents an oxygen atom, a sulfur atom or NRZ; and E represents a furyl group, a thienyl group, a pyrrolyl group, a tetrazolyl group, a thiazolyl group, a pyrazolyl group, a phenyl group or the like.

Abstract: In the quorum sensing antagonist blocking the communication in bacteria, the method for preventing biofilm formation using this quorum sensing antagonist and the method for reducing the bacterial contamination, the quorum sensing antagonist contains the homoserine lactone moiety and sulfanylethanoyl group, and has a similar chemical structure to that of the autoinducer which is produced by bacteria as a signal, whereby the quorum sensing antagonist can inhibit the formation of biofilm and reduce the bacterial contamination as well.

Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.

Abstract: The present application relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

Abstract: The present invention relates to a process for preparing 4-aminobut-2-enolides and also corresponding intermediates and starting compounds which are passed through or used in the process according to the invention.

Abstract: Process for preparing 2,2-difluoroethylamine derivatives, wherein compounds of the general formula (IV) are reduced to the corresponding 2,2-difluoroethylamine derivatives of the general formula (III), where the A radical is as defined in the description: