Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, are useful in the treatment of systolic heart failure including congestive heart failure.

Abstract: The present invention provides compounds of the formula: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.

Abstract: The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

Abstract: The present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).

Abstract: A heteroaryl derivative having the formula (I).

Abstract: The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of treating pain using these compounds and pharmaceutical compositions including these compounds.

Abstract: The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.

Abstract: The invention is concerned with novel heteroarylacetamides of formula (I) R—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb) ??(I) wherein Ra to Re are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.

Abstract: The invention provides compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein Ar1 represents a group (II), (III), (IV) or (V), and A, Ar2, n, R1, R2, R3, R4 and R5 are as defined in the specification; a process for their preparation; pharmaceutical compositions containing them; and their use in therapy.

Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.

Abstract: Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; CI1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono- or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a —S—, —N(R5aR5b), R10a—O—C(?O)—, N(R5aR5b)—C(?O)—, R10a—C(?O)—NR5b1', R10b—C(?O)—O—; and R8 and/or R9 may also be

Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.

Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: The present invention relates to Radiolabeled Compounds and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.

Abstract: This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.

Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.

Abstract: The present invention relates to aryl-3-[(het)aryl-piperidin-4-yl]-thioureas, processes for the production thereof and the use thereof for the production of pharmaceutical agents for the treatment of diseases and indications which are connected with the EP2 receptor.

Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.

Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: This application relates to a compound of formula I (or a pro-drug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor (I).

Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

Abstract: The present invention provides a compound having p38 MAP kinase inhibitory activity. Because of having p38 MAP kinase inhibitory activity, the compounds represented by the formula (I): wherein each symbol is as defined in the description, salts thereof, N-oxides thereof, solvates thereof, or prodrugs thereof are useful in preventing and/or treating diseases that are supposedly caused or deteriorated by abnormal production of cytokines including inflammatory cytokines or chemokines, or by overresponse thereto, namely cytokine-mediated diseases such as inflammatory diseases, respiratory diseases, cardiovascular diseases and bone diseases.

Abstract: The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis, including methods of preparing and intermediates thereof.

Abstract: The present invention relates to amide compounds of general formula I wherein the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Abstract: Compounds of the formula (I): or a pharmaceutically-acceptable salt or pro-drug thereof: wherein R1 is selected for example from hydrogen, halogen, optionally substituted methyl; R2 and R3 are independently selected from hydrogen, fluoro, chloro and trifluoromethyl; R4 and R5 are independently selected, for example, from hydrogen, methyl, optionally substituted (2-4C)alkyl, C(O)R6 or R4 and R5 together with the nitrogen to which they are attached form an optionally substituted 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring or an optionally substituted imidazole ring. Methods for making the compounds of formula (I), compositions containing them and their use as antibacterial agents are also described.

Abstract: A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Q2 is a single bond or the like; Q3 is a group in which Q5 is an alkylene group having 1 to 8 carbon atoms, or the like; and T0 and T1 are carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof.

Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.

Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.

Abstract: Certain substituted benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.

Abstract: This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.

Abstract: The present invention relates to 6-(4-{[(benzylsulfonyl)amino]carbonyl}piperidin-1-yl)-5-cyano-2-methylnicotinic acid isopropyl ester, form II, to a process for preparing such compound, to its utility as P2Y12 inhibitor and as anti-thrombotic agent etc, its use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing it.

Abstract: The present invention relates to 6-(4-{[(benzylsulfonyl)amino]carbonyl}piperidin-1-yl)-5-cyano-2-methylnicotinic acid ethyl ester, form I and II, to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-thrombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.

Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian Factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.

Abstract: Compounds of formula (I) in which R1, R2, R3 and R4, have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.

Abstract: The present invention relates to novel piperidine derivatives having effect of inhibiting acetylcholinesterase and aggregation of ?-amyloid, Alzheimer's disease-induced protein, and treatment for Alzheimer's disease containing the same, the piperidine derivatives represented by Formula 3.

Abstract: A process for preparing 10,11-dihydro-5H-dibenzo[a,d]cyclohept-5-enes (e.g. loratadine) by reacting a dibenzozuberone with an aliphatic ketone in the presence of low valent titanium.

Abstract: (S)-(?)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperi-dine represented by the formula (IV): wherein * represents an asymmetric carbon.

Abstract: Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine [sic], morpholine [sic], piperidine [sic], —NR5R6 and ?and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl [sic], pyridyl [sic], pyrimidyl [sic] and pyridazyl [sic], it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by by [sic] a maximum of two R8 radicals

Abstract: The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression

Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: Compounds having a selective N-type calcium channel antagonistic activity are provided. Dihydropyridine derivatives represented by the following formula: analogs thereof and pharmaceutically acceptable salts thereof have an activity of selectively inhibiting the action of N-type calcium channel, and they are used as therapeutic agents for various diseases relating to N-type calcium channel.

Abstract: The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression.

Abstract: The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.

Abstract: Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided.

Abstract: The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.

Abstract: The present invention relates to compounds of formula I: which are antagonists of 5-HT6 receptor.