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Treatment of effect of chemicals with their ultradilute stereoisomers
A method of treating an effect of a chemical agent, which agent is characterized by one or more chiral centres, by administering a dilution or an ultra-high...
2-pyridinylcycloalkylcarboxamide derivatives as fungicides
A compound of general formula (I): ##STR00001## A process for preparing this compound. A compound of general formula (II): ##STR00002## A fungicide...
The invention is concerned with novel indazole derivatives of formula (I) ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X and Y...
2-pyridinylethylcarboxamide derivatives and their use as fungicides
A compound of general formula (I) ##STR00001## A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A...
Chelating agents and highly luminescent and stable chelates and their use
This invention relates to a group of novel chelating agents, novel chelates, biomolecules labeled with said chelates or chelating agents as well as solid...
Certain chemical entities, compositions, and methods
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions...
N-substituted piperidines and their use as pharmaceuticals
The present invention relates to inhibitors of 11-.beta. hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and...
Amide substituted indazoles as poly(ADP-ribose)polymerase(PARP) inhibitors
The present invention relates to compounds of formula I: ##STR00001## and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are...
The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a...
Compounds of Formula I ##STR00001## wherein R.sup.1, A, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, n, m, q and r are as described in the specification,...
Carbamic acid compounds comprising a bicyclic heteroaryl group as HDAC
This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is...
Injectable liquid formulation of paracetamol
The invention relates to a novel injectable liquid formulation of paracetamol, comprising an aqueous solvent, a buffer agent with a pKa between 4.5 and 6.5, an...
Caspase inhibitors and uses thereof
The present invention provides a compound of formula I: ##STR00001## wherein: X is --OR.sup.1 or --N(R.sup.5).sub.2, Y is halo, trifluorophenoxy, or...
Modulators of cellular adhesion
The present invention provides compounds having formula (I): ##STR00001## and pharmaceutically acceptable derivatives thereof, wherein R.sub.1-R.sub.4, n, p,...
Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which...
Carbonylamino-derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) ##STR00001## wherein n, m, t, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L, Q, X, Y and ...
Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors
The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R.sup.1, q, A, B, X.sub.1, X.sub.2, X.sub.3, X.sub.4, X.sub.5...
An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio...
6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and
2-quinoxalinones as poly(ADP-ribose) polymerase...
The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and...
Spirocyclic heterocyclic derivatives and methods of their use
Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain...
Compositions and methods for enhancing brain function
Compositions and methods are provided that enhance cognition in a human to which the composition is orally administered. Remarkably, clinical studies have...
Unsaturated heterocyclic derivatives
This invention relates to compounds of the general formula: ##STR00001## in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or...
(2S)-2-[1-(2-Chloro-6-cyano-phenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-[(- 1R)-2-hydroxy-1-methyl-ethoxy]-N-(5-methylpyrazin-2-yl)propanamide or a ...
Mnk1 or Mnk2 inhibitors
The present invention relates to the use of pyrazolopyrimidine compounds for the production of pharmaceutical compositions for the prophylaxis and/or treatment...
Substituted pyrazinone amides useful for activation of glucokinase
The present invention provides compounds of Formula (I) ##STR00001## that act as glucokinase activators; pharmaceutical compositions thereof; and methods of...
Piperidine compounds for use in the treatment of bacterial infections
Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing...
Thio-substituted arylmethanesulfinyl derivatives
The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present...
Heterocyclic derivatives and their use as stearoyl-CoA desaturase
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal...
Piperidine and piperazine derivatives
Compounds of general formula (I) ##STR00001## in which R.sup.1, m, X, n, Y and R.sup.3 have any of the meanings given in the specification, have affinity for...
Aminoquinoline derivatives and their use as adenosine A3 ligands
The present invention relates to an adenosine A.sub.3 receptor ligand of the general formula (I).
Derivatives of 4-piperazin-1-yl-4-benzo[B]thiophene suitable for the
treatment of CNS disorders
A heterocyclic compound or a salt thereof represented by the formula (1): where R.sup.2 represents a hydrogen atom or a lower alkyl group; A represents a lower...
Methods of treatment of chronic pain using eszopiclone
The invention relates to the use of eszopiclone for the treatment of low-level, chronic pain and fatigue associated with pain.
3,9-diazabicyclo[3.3.1]nonane derivatives and their use as monoamine
neurotransmitter re-uptake inhibitors
3,9-diazabicyclo[3.3.1]nonane derivatives, useful as monoamine neurotransmitter re-uptake inhibitors. Also, use of these compounds in a method for therapy and...
Pyrazine compounds and uses as PI3K inhibitors
The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or...
Endothelin receptor antagonists
This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The...
1,2-disubstituted heterocyclic compounds
1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions,...
Substituted diketopiperazines and their use as oxytocin antagonists
Compounds of formula (1) ##STR00001## wherein R.sub.1 is 2-indanyl, R.sub.2 is 1-methylpropyl, R.sub.3 is 2-methyl-1,3-oxazol-4-yl and R.sub.4 and R.sub.5...
2-oxo-3-benzylbenzoxazol-2-one derivatives and related compounds as Met
kinase inhibitors for the treatment of...
Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to...
Derivatives and analogs of N-ethylquinolones and N-ethylazaquinolones
Bicyclic nitrogen containing compounds and their use as antibacterials.
7-cycloalkylaminoquinolones as GSK-3 inhibitors
Provided herein are aminoquinolones of formula I and compositions containing the compounds, wherein formula I is ##STR00001## The compounds and compositions...
9-substituted-5-carboxy-oxadiazino-quinolone derivatives, their
preparation and their application as...
A subject of the invention is the compounds of formula (I): ##STR00001## wherein R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, R'.sub.4, R.sub.5, R.sub.6 and...
The invention relates to benzoindazole derivatives according to general Formula I ##STR00001## or a pharmaceutically acceptable salt thereof. The compounds...
Dual pharmacophores--PDE4-muscarinic antagonistics
The present invention relates to novel compounds of Formula (I) ##STR00001## and their use in the treatment of respiratory diseases, including...
The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I ##STR00001## or a...
The invention is concerned with novel heterocyclyl compounds of formula (I) ##STR00001## wherein A, X, Y.sup.1, Y.sup.2, Y.sup.3, R.sup.3, R.sup.4, R.sup.5,...
A compound (2S)-2-[1-(2,6-dichlorophenyl)pyrazolo[4,5-e]pyrimidin-4-yl]oxy-3-(3-hydr- oxyazetidin-1-yl)-N-(5-methylpyrazin-2-yl)propanamide is useful in the ...
Indole carboxamides as IKK2 inhibitors
The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): ##STR00001## ...
Pyrrolo[3,2-D] pyrimidines as DPP-IV inhibitors for the treatment of
The present invention relates to substituted pyrrolo[3,2-d]pyrimidines of formula (I), wherein R1 and R2 are defined as in claim 1, including the tautomers,...
Substituted aniline derivatives
The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
Triazolopyridazine protein kinase modulators
The present disclosure relates to triazolopyridazine protein kinase modulators of Formula (I), methods of using these compounds to treat diseases mediated by...