Abstract: The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein R1 to R4 are, independent from each other, a hydrogen atom or an optionally substituted alkyl group; E1 is —NR4—; and E2 is an oxygen atom or —NR10—; Q is the group —X—Y-Q?, wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C?O, NHC(?), and C(?O)NH, and Q? is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.

Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.

Abstract: Certain cyclic compounds are presented as well as their use for inhibiting paramyxovirus neuraminidase.

Abstract: The present invention relates to a process for the preparation of 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, the enantiomers and its salts, characterised in that 5-(4-fluorophenyl)pyridine-3-carbaldehyde is reacted directly with aminomethylchroman or its salts under reducing conditions to give 2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chroman, and the latter is, if desired, converted into one of its physiologically acceptable salts by treatment with an acid.

Abstract: Disclosed are NK1 antagonists having the formula: Also disclosed are methods for treating a number of physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough, using the compounds of formula (I).

Abstract: The present invention provides a novel bioactive substance having an antitumor activity and a process for producing it, and a medical use thereof. Namely, it provides a 12-membered ring macrolide compound represented by the following formula obtained from the incubation solution of Streptomyces sp. Mer.

Abstract: Compounds of general formula I: R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C?6? alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

Abstract: Compounds of the general formula (I) are described wherein R1 and R2, which may be the same or different, is each a hydrogen atom or a CF3, CF2H or CFH2 group, provided that when one of R1 and R2 is a hydrogen atom, then the other is a CF3, CF2H or CFH2 group, and the salts, solvates or hydrates thereof. Compounds of the invention are potent MMP inhibitors which advantageously do not cause tendonitis in a relevant animal model. Compounds of the invention may be expected to be of use in medicine, especially where the avoidance of side effects, such as joint pain, is desired.

Abstract: The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention provides compounds that block calcium channels having the Formula I shown below. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.

Abstract: The invention provides a compound of formula (I): wherein R1, R2, R3, R4, R5, N, X and Y are as defined in the specification, processes, for their preparation, pharmaceutical compositions containing them, and their use in therapy, especially for the treatment of chemokine receptor related diseases and conditions.

Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the treatment of various disorders.

Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7 and R8 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.

Abstract: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Abstract: Hindered amines substituted on the N-atom with an —O-E-OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O-E moieties.

Abstract: This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.

Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1-C6 alkoxy, C1-C4 alkenyloxy, amino, C1-C4 alkylamino, or di-(C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.

Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) 1

Abstract: A compound of the formula: in which R1 is optionally substituted phenyl, optionally substituted naphthyl, optionally substituted bicyclic heterocyclic group, optionally substituted lower alkenyl or optionally substituted lower alkynyl, and R2 is carboxy or protected carboxy, or a salt thereof, useful for treating and/or preventing MMP- or TNF-&agr; mediated diseases.

Abstract: The invention relates to processes for the preparation of a key intermediate in the synthesis of a GARFT inhibitor of formula (Ia) containing a 4-methyl-substituted thiophene core: 1

Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract: Compounds of the invention, for example compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).

Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: Compounds are provided which are antagonists of the calcium sensing receptor, and have the general formula 1

Abstract: The present application describes modulators of chemokine receptor activity of formula (I): 1

Abstract: The invention relates to novel substituted pyrimidone derivatives which bind to integrin receptors, to their preparation and to their use.

Abstract: The present invention relates to a class of compounds represented by the Formula I 1

Abstract: The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Abstract: This invention is directed to compounds of formula I: 1

Abstract: A cyclic amidine derivative represented by the formula: 1

Abstract: Compounds of formula (I) 1

Abstract: The invention relates to thiophene carboxanmides of formula (I). wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general formula (I): 1

Abstract: The invention relates to compounds of the general formula (I): 1

Abstract: Compounds of general formula I 1

Abstract: Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof. (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus.

Abstract: of the formula (IV): 1

Abstract: The present invention relates to the synthesis and biological application of piperidinoyl carboxylic acid integrin antagonists affinity moiety of IFormula (I): 1

Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.

Abstract: A invention relates to N auroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.

Abstract: The present invention relates to alkyne compounds of general formula I 1

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.

Abstract: The invention provides compounds of formula (I), in which m, n, X, Y, R1, R2 and R3 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; and their use in therapy.

Abstract: The subject invention relates to 4-phenyl-piperidine derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by an opioid receptor. The subject also particularly relates to using such derivatives to treat certain disease states, disorders and conditions, for example irritable bowel syndrome, drug addiction or dependency, including alcohol addiction, depression, anxiety, schizophrenia, anxiety, schizophrenia and eating disorders, among numerous other disease states, disorders and conditions as more fully described herein.

Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-26alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R4, —Alk—NR5R6, 1-R6-4-piperidinyl, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar—, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloa