Abstract: The present invention provides a novel benzazepine derivative represented by formula: 1

Abstract: This invention relates to a novel class of heterocyclic compounds that bind chemokine receptors, inhibiting the binding of their natural ligands thereby. These compounds result in protective effects against infection by HIV through binding to chemokine receptors, including CXCR4 and CCR5, thus inhibiting the subsequent binding by these chemokines.

Abstract: The invention relates to method of preventing or treating a disease related to the 5-HT2C receptor and the 5-HT6 receptor, comprising administering to a human or animal subject in need thereof a 5-HT2C receptor agonist and a 5-HT6 receptor antagonist in sufficient amounts to provide a therapeutic effect. The invention also relates to a pharmaceutical composition comprising an effective amount of a combination of a 5-HT2C receptor agonist and a 5-HT6 receptor antagonist, and optionally a pharmaceutically acceptable carrier.

Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.

Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I:

Abstract: The invention relates to novel compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.

Abstract: The invention provides compounds of formula (I): wherein: R2 and R3 independently represent various substituents; R1 and R4 independently represent H, F, Cl, Br, Cl1-2alkyl, C1alkoxy, OH, CN, or NO2; B represents a sulfur atom or a —CH2-group; t represents 3 or 4; and A represents an optionally substituted 5- or 6-membered aromatic heterocyclic ring, or an optionally substituted bicyclic heterocyclic ring system in which at least the ring bound to the group B in Formula (I) is aromatic; or a salt thereof.

Abstract: The present invention provides a medicinal composition comprising (1) a pharmacologically active substance, (2) a drug absorbefacient and (3) a taurine compound or a polyamine. A taurine compound has an efect of suppressing or preventing damage of the intestinal mucous membrane, and therefore adding the taurine compound to a medicinal composition containing a pharmacologically active substance and a drug absorbefacient makes it possible to suppress or prevent damage of the intestinal mucosa. A polyamine improves the absorbability of pharmacologically active substances, and therefore adding the polyamine to a medicinal composition containing a pharmacologically active substance and a drug absorbefacient makes it possible to decrease the dose of the drug absorbefacient, thereby suppressing or preventing damage of the intestinal mucosa.

Abstract: Compounds of the formula I 1

Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists especially urotensin II antagonists.

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism, infection and cell proliferation. The subject compounds contain a fused heterobicyclic ring.

Abstract: The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3-7C) methyl, benzyl or m-phenyl benzyl.

Abstract: The invention relates to novel benzazepines and related heterocyclic derivatives (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as orexin receptor antagonists.

Abstract: Novel compounds (I) 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 Ar is a group of formula a) or b).

Abstract: The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis.

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

Abstract: Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH2, O and N-alkyl, Z is either S or —CH═CH—, R1 and R2 are independently selected from H, F, Cl, Br and alkyl, R3 is selected from OH, O-alkyl and NR4R5, R4 and R5 are each independently H or alkyl, or together are —(CH2)q—, p is 0, 1, 2, 3 or 4, and q is 4 or 5, are new. They are agonists at the asopressin V2 receptor and are useful as antidiuretics and pro-coagulants.

Abstract: The present invention relates to novel compounds of Formula (I): 1

Abstract: Tetrahydroisoquinoline analogs are provided which are modulators of chemokine receptor activity. The tetrahdroisoquinoline analogs thereof have the structure wherein R1, R2, R3, R3a, X1, X2, X3, X4, m, n and p are as described herein.

Abstract: The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.

Abstract: There is disclosed a compound having the formula or a pharmaceutically acceptable salt thereof, wherein: R1a, R1b and R1c are independently fluorine or hydrogen; R2 is C1 to C12 alkyl being straight or branched chain, saturated or unsaturated, mono-substituted or unsubstituted, said substituents being selected from piperidine, pyrroliding, morpholine, thiomorpholine and cycloalkyl of 3 to 7 carbon atoms; a cycloalkyl of 3 to 9 carbon atoms; a cycloalkyl of 3 to 9 carbon atoms having a C1 to C6 alkyl substituent; a polycycloalkyl of 2 to 3 rings having 7 to 12 carbons; and phenyl or phenyl substituted with halogen, hydroxy, C1 to C6 alkoxy, C1 to C6 alkyl, nitro, methylene dioxy or trifluoromethyl; and R3 is a moiety selected from: (I), (II) or a pyrrolidin-3-yl moiety of the formula (III). The compounds are disclosed for use as muscarinic antagonists with M3 selectivity.

Abstract: A variety of small, guanidino group-containing molecules capable of acting as MC4-R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4-R mediated diseases and may be formulated into pharmaceutical formulations and compositions.

Abstract: A compound selected from those of formula (I): 1

Abstract: The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.

Abstract: A melanin-concentrating hormone antagonist comprising a compound of the formula: 1

Abstract: Compounds of Formula I and their salts having affinity for dopamine receptors, in particular the D3 Receptor, and thus potential in the treatment of conditions wherein modulation of the D3 receptor is beneficial, e.g., as antipsychotic agents.

Abstract: The present invention provides compounds of Formula I: 1

Abstract: 4,4′-diaminodiphenylsulphone is a bactericide and anti-inflammatory agent. It is known to have therapeutic activity against leprosy, dermatitis herpetiformis, actinomycotic mycetoma, asthma, malaria, rheumatoid arthritis, Kaposiis sarcoma, pneumocystis carinii (pneumonia), subcorneal pustular dermatosis and cystic acne, in patients in need of such therapy. It is also known to have therapeutic activity against memory loss in patients in need of such therapy, including patients suffering from Alzheimer disease and related neurodegenerative disorders. Donepezil hydrochloride (donepezil) is an acetylcholinesterase inhibitor that is currently used for the symptomatic treatment of Alzheimer disease in patients in need of such therapy. It has now been found that combinations of 4,4′-diaminodiphenylsulphone and cholinesterase inhibitors unexpectedly show synergistic effects in the prevention and/or treatment of dementia.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof:

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: 1

Abstract: The present invention provides a composition for neurotrophic action which comprises a compound of the formula: 1

Abstract: The present application describes to novel bicyclic hydroxamates derivatives of formula I: 1

Abstract: The invention relates to compounds which are represented by the formula wherein R1, R2, R3, R4, X and Y are as defined in the specification, as well as pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds and to a process for their preparation. The compounds possess affinity towards metabotropic glutamate receptors and are therefore useful in the treatment or prevention of acute and/or chronic neurological disorders.

Abstract: The present invention relates to methods of treating various CNS and other disorders by adminstering fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, by administering compounds of the formula 1

Abstract: This invention relates generally to a novel class of bicyclic heterocyclic compounds of the Formula (I): 1

Abstract: New derivatives of benzazepine, particularly of benzofuro[3a,3,2,ef][2]benzazepin of the general formula (I) 1

Abstract: The object of the present invention is to provide a prophylactic and/or therapeutic drug for obesity and obesity-associated diseasestor diabetes with a reduced risk for central side effects and high universality in usage. Another object of the present invention is to provide a pharmaceutical composition comprising a compound of the following formula: wherein Ar represents phenyl which may be substituted and/or condensed; n represents an integer of 1 to 10; R represents hydrogen or a hydrocarbon group which may be substituted, which may not be the same in its n occurrences; R may be bound to either Ar or a substituent for Ar; Y represents an amino group which may be subsituted or a nitrogen-containing saturated heterocyclic group which may be substituted, or a salt thereof, which can be used for a thermogenic agent, an antiobesity agent, a lipolytic agent, or a prophylactic and/or treating drug for obesity-associated diseases.

Abstract: A compound of the formulae (I) or (II): 1

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: Compounds of formula (I) 1

Abstract: Compounds represented by the formula: 1

Abstract: The invention relates to the use of selective phosphodiesterase 2 (PDE 2) inhibitors for producing pharmaceuticals for improving perception, concentration, learning and/or memory.

Abstract: The invention relates to compounds which are represented by the formula 1

Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I 1

Abstract: Compounds of formula (I) 1

Abstract: A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR1; R1 is H, C1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R1 is —(CH2)h-aryl, —COR1-1, —COOR1-2, —CO—(CH2)h—COR1-1, C1-6 alkyl sulfonyl, —SO2—(CH2)h-aryl, or —(CO)i-Het; R2 is H, C1-6 alkyl, —(CH2)h-aryl, or halo; R3 and R4 are independently H or halo; R5 is H, C1-12 alkyl optionally substituted with one or more halo, C3-12 cycloalkyl, C1-6 alkoxy; m and n taken together are 1 or 2. The compounds are useful antimicrobial agents.

Abstract: The invention discloses that anandamide is an endogenous ligand for vanilloid receptors, and especially the vanilloid receptor VR1. Other structurally related lipids, such as AM404, 1-arachidonylglycerol, and 2-arachidonylglycerol, are identified having vanilloid receptor activity as well. Methods of treating individuals suffering from, or at risk of suffering from, diseases and disorders associated with abnormal vanilloid receptor function are provided, as are methods of designing and identifying vanilloid receptor agonists and antagonists.

Abstract: The present invention relates to a novel urea derivative represented by the following formula (I), which is useful as an anti-cancer agent: 1

Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human &agr;2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the &agr;2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.