Abstract: Compounds are described which inhibit mitogen activated protein kinase-activated protein kinase-2 (MK-2). Methods of using such compounds for the inhibition of MK-2, and for the prevention or treatment of a disease or disorder that is mediated by TNF&agr;, are described, where the method involves administering to the subject an MK-2 inhibiting compound of the present invention. Therapeutic compositions, pharmaceutical compositions and kits which contain the present MK-2 inhibiting compounds are also described.

Abstract: The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant &agr;7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant &agr;7 nicotinic receptor agonist.

Abstract: The present invention includes novel retinoid compounds that have selectivity as RXR agonists on one or more isoforms of RXR, currently, RXR&agr;, RXR&bgr;, or RXR&ggr;. The present compounds, and pharmaceutical compositions incorporating these compounds, therefore, are effective in treating conditions mediated by RXRs. Among other physiological responses, the compounds of the present invention reduce blood glucose and maintain body weight, and, thus, are useful for the treatment of diabetes (NIDDIM) and obesity.

Abstract: Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases.

Abstract: The invention relates to 3,5-diamino-1,2,4-triazoles as kinase inhibitors, the production thereof and the use of the same as a medicament for treating cancer, for example solid tumours and leukaemia, auto-immune diseases such as psoriasis, alopecia and multiple sclerosis, alopecia induced by chemotherapeutic agents and mucositis, cardiovascular diseases such as stenoses, arterioscleroses, and restenoses, infectious diseases such as those caused by unicellular parasites such as trypanosome, toxoplasma or plasmodium, or by fungi, nephrological diseases such as glomerulonephritis, chronic neurodegenerative diseases such as Huntington's disease, amyotropic lateral sclerosis, Parkinson's disease, AIDS dementia and Alzheimer's disease, acute neurodegenerative diseases such as cerebral ischemia and neurotrauma, and viral infections such as cytomegalovirus infections, herpes, hepatitis B and C, and HIV diseases.

Abstract: The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters.

Abstract: The invention provides certain thiazolopyrimidine compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof; processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention is directed to a compound represented by the following formula (1) and to a process for producing a compound (5) from the compound (1).

Abstract: The invention relates to novel isoxazolo pyrimidinones of general formula (I), a method for producing the same and the pharmaceutical use thereof.

Abstract: The invention provides certain thiazolopyrimidine compounds of formula (1) or a pharmaceutically acceptable salt or solvate thereof: in which: A is a group of formula (a) or (b): processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The invention relates to pharmaceutically acceptable compounds of formula I, wherein the radicals have the significances given in the description. Compounds of formula I are useful against tumor diseases.

Abstract: 5-Halogen-6-phenyl-7-fluoroalkylamino-triazolopyrimidines of formula I: (I) in which R1 is hydrogen, fluoro, alkyl, alkenyl, alkynyl, alkadienyl, where the carbon chains of these radicals may be unsubstituted or substituted as defined in the description; R2 is hydrogen, alkyl, alkenyl, alkynyl, alkadienyl, where these radicals may be unsubstituted or substituted; R3 is fluoroalkyl or fluoroalkenyl; X is halogen; n is 0 or an integer from 1 to 4; L each independently is halogen, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy. Processes for their preparation, compositions containing them and to their use for combating phytopathogenic fungi.

Abstract: The invention provides compositions and methods for improved hybridization analysis utilizing DNA, RNA, PNA and chimeric oligomers in which one or more purine bases are substituted by a pyrazolo[5,4-d]pyrimidine or by a 7-deazapurine purine analogue. Reduced self-aggregation and reduced fluorescence quenching are obtained when the oligomers are used in various methods involving hybridization. Methods of synthesis, as well as novel synthetic precursors, are also provided.

Abstract: There is disclosed the use of a compound of formula (I) wherein R1, R2, R3, Ar and X are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which antagonism of the CX3CR1 receptor is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed, together with processes for their preparation. The compounds of the formulae (I) and (Ia) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyclinating disease and pain.

Abstract: Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed small molecules which interact with the N-terminal binding pocket with an affinity which is greater than ADP and different from the ansamycin antibiotics for at least one species of the HSP90 family. Moreover, these small molecules can be designed to be soluble in aqueous media, thus providing a further advantage over the use of ansamycin antibiotics. Pharmaceutical compositions can be formulated containing a pharmaceutically acceptable carrier and a molecule that includes a binding moiety which binds to the N-terminal pocket of at least one member of the HSP90 family of proteins. Such binding moieties were found to have antiproliferative activity against tumor cells which are dependent on proteins requiring chaperones of the HSP90 family for their function.

Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.

Abstract: An inhibitor of NF-&kgr;B comprising as an active ingredient an indan derivative represented by the general formula (I) or a salt thereof.

Abstract: Compounds of formula I 1

Abstract: The invention relates to novel triazolopyrimidines of the formula 1

Abstract: Certain thienopyrrolyl and furanopyrrolyl compounds are disclosed as useful to treat or prevent disorders and conditions mediated by the histamine H4 receptor, including allergic rhinitis.

Abstract: Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: The invention relates to a process for the preparation of [7-(3-chloro-4-methoxybenzylamino)-1-methyl-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl-methoxy]acetic acid and intermediates thereof.

Abstract: This invention provides compounds defined by Formula I 1

Abstract: This invention provides bicyclic heterocycles that are useful for treating cell proliferative disorders, such as cancer and restenosis, as well as angiogenesis and atherosclerosis. We have now discovered a group of bicyclic compounds that are potent inhibitors of cyclin-dependent kinases (cdks), growth factor-mediated kinases, and non-receptor kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability for clinical use.

Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula 1

Abstract: Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR an FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Abstract: This invention provides compounds defined by Formula I 1

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Abstract: A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, 1

Abstract: Compounds having the formula 1

Abstract: Compounds of formula (I) 1

Abstract: The present application is directed to pyrazolopyrimidine and furopyrimnidine analogs of the formula (I) 1

Abstract: The present invention provides a compound of formula (I): 1

Abstract: An amide compound given by formula [I]: 1

Abstract: Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: 1

Abstract: Compounds having the formula 1

Abstract: This invention discloses pyrimidine compounds, and pharmaceutically acceptable salts, solvates and prodrugs thereof, useful in therapeutically and/or prophylactically treating patients with cancer by inhibiting receptor tyrosine kinases and/or dihydrofolate reductase and/or thymidylate synthase. The compounds, and methods of using these compounds, are disclosed.

Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: 1

Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): 1

Abstract: Novel pyrimidine derivatives of formula I as well as possible isomers and mixtures of isomers thereof. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms and insecticidal attack.

Abstract: The invention provides methods for treating female sexual dysfunctions by administering to a female individual a therapeutically effective amount of at least one compound that donates, transfers or release nitrogen monoxide, that induces the production of endogenous endothelium-derived relaxing factor, that stimulates endogenous synthesis of nitrogen monoxide, or that is a substrate for nitric oxide synthase. The methods may further comprise administering a therapeutically effective amount of a phosphodiesterase inhibitor and/or a nitrosated and/or nitrosylated phosphodiesterase inhibitor.

Abstract: Compounds are provided having a piperazine or homopiperazine ring which are useful in the treatment of thrombosis.

Abstract: The invention relates to novel isoxazolo pyrimidinones of general formula (I), a method for producing the same and the pharmaceutical use thereof.

Abstract: The present invention describes novel isoxazolo[1,5-a]pyrimidines of formula: wherein R is an aromatic or heteroaromatic ring, or pharmaceutically acceptable salt form thereof, which are useful as CRF antagonists.

Abstract: The present invention relates to a method of treating disorders of the Central Nervous System (CNS) and other disorders in a mammal, including a human, by administering to the mammal a CNS-penetrant &agr;7 nicotinic receptor agonist. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier and a CNS-penetrant &agr;7 nicotinic receptor agonist.

Abstract: The present invention describes novel isoxazolo[1,5-a]pyrimidines of formula: 1

Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: 1

Abstract: Disclosed are novel compounds having the formula 1

Abstract: Nucleoside analogues or base analogues having structure (1), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or alkenyl or alkoxy or aryl or a reporter moiety; where necessary (i.e. when Y and/or W is N or CR6 where R6 is not O) a double bond is present between Y and W or W and W, and Q is H or a sugar or a sugar analogue or a nucleic acid backbone or backbone analogue.

Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.