Abstract: The present invention relates to quinobenzoxazines analogs having the general formula: and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R1, R3, R4 and R5 are substituents. The present invention also relates to methods for using such compounds.

Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.

Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.

Abstract: The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and R1 to R10 are as described in the specification.

Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.

Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12?, R13?, X and Y are as defined in the specification.

Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12?, R13?, X and Y are as defined in the specification.

Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.

Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12,, R13,, X and Y are as defined in the specification.

Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.

Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Abstract: The present invention relates to novel isoxazoline-indole derivatives according to Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, with a binding affinity towards dopamine receptors, in particular towards dopamine D2 and/or D3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT1A receptor, pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production, wherein the variables are further defined in the application.

Abstract: This invention relates to compounds of formula I wherein R1 and R2 are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of formula I are adenosine receptor ligands with good affinity to the A2A-receptor and a high selectivity to the A1- and A3 receptors. These compounds are useful, inter alia, in treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.

Abstract: The invention relates to novel amino alcohols of the general formula (I) where X, R1, R2, R3, R4, R5 and R6 are each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.

Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.

Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Abstract: The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors using pharmaceutical compositions comprising compounds of Formula (I)

Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

Abstract: The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N—R10R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceuti

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 a method for the preparation of a carboxylic imide having the general formula R1—(CO)—(NR3)—(CO)—R2 , ??(I) wherein a carboxylic anhydride having the general formula R1—(CO)—O—(CO)—R2 ??(II) is reacted with urea or a urea derivative of the form (R3HN)—(CO)—(NR3H) in a solvent. In particular, the method can be used for the preparation of thalidomide.

Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.

Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2–6 ?, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0–3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0–4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0–2 wherein the sum of l and k is 0–3; Ar is an aryl group substituted with 0–5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; a

Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.

Abstract: The present invention discloses compounds of formula I wherein Ar, X, R1 and R11 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: Disclosed are novel heterocyclic compounds having the structure which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes.

Abstract: The process consists in condensing (2-methyl-6,7,8,9-tetrahydro-4 H-pyrido-[1,2-a]pyrimidin-3-yl)-acetaldehyd with 6-fluoro-3-piperidinyl)-1,2-benzisoxazole to yield the intermediate enamine, 3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]vinyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2,-a]pyrimidin-4 -one followed by reduction of such an enamine.

Abstract: The invention is directed to compounds of the formula and the pharmaceutically acceptable salts thereof wherein Ar1 is indole, benzimidazole, or benzotriazole, optionally substituted with lower alkyl (1–4C), halo, or lower alkoxy (1–4C); X1 is CO or an isostere thereof; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl; n is 0 or 1; Z is CH or N; X2 is CH, CH2 or an isostere thereof; and Ar2 consists of one or two phenyl moieties directly coupled to X2 and optionally substituted by halo, nitro, alkyl (1–6C), CN or CF3, or by RCO, COOR, CONR2, NR2, OR or SR, wherein R is H or alkyl (1–6C) or by phenyl, itself optionally substituted by the foregoing substituents; with the proviso that if Z is N, X1 is CO, and Ar1 is indole, Ar1 must be coupled to X1 through the 2-, 5-, 6- or 7-position. These compounds are useful in the treatment of conditions associated with inflammation.

Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.

Abstract: The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV), and to methods for their production and their therapeutic utility.

Abstract: The present invention relates to heteroaromate OSC inhibitors. 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: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight. The compounds according to the invention have surprisingly been shown to have a serotonine (5-HT) reuptake inhibitor activity in combination with additional ?2-adrenoceptor antagonist activity and show a strong anti-depressant activity without being sedative.

Abstract: Novel compounds represented by the following formula (I) that act as a ligand to sigma receptor/binding cite and a medicament comprising the same as an active ingredient: wherein X represents an alkyl group, an aryl group, a heterocyclic group or the like; Q represents a group represented by —CH2—, —CO—, —O—, —CH(OR7)— or the like wherein R7 represents a hydrogen atom, an alkyl group or the like; n represents an integer of from 0 to 5; R1 and R2 each represent a hydrogen atom, an alkyl group or the like; B represents either of the following groups: wherein R3, R4, R5, and R6 each represent a hydrogen atom, a halogen atom, an alkoxyl group or the like; m represents 1 or 2; and the ring of: represents an aromatic heterocyclic ring.

Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein: represents (i) a saturated 3 to 6 membered carbocycle, optionally substituted by one or more alkyl groups, (ii) indanyl or (iii) a saturated 4 to 6 membered heterocyclic ring; R1 represents R3Z1-Het- or R4N(R5)—C(?O)—NH—Ar1—; L1 represents an —R6—R7— linkage; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; L2 represents an alkylene linkage; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (?4?1).

Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous system

Abstract: The present invention provides novel amino benzothiazole compounds, compositions comprising these compounds and methods of using these compounds as neuroprotectants. In particular, the compounds described in the present invention are useful for treating stroke and neuropathic pain.

Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Abstract: Pyrrolidine compounds of Formula (I), (wherein R1, R2, R3, R4, R5, R6a, R6b, R7 and R8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

Abstract: The invention encompasses a series of benzothiazole compounds which inhibit HIV entry and are useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for using these compounds.

Abstract: Disclosed is a compound represented by Structural Formula (I): R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl group. Z1 is ?O, ?S, ?NOR11. R is represented by a Structural Formula selected from (II)–(VII): The variables in Structural Formulas (II)–(VII) are described herein.

Abstract: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.

Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.

Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula to a person in need of such treatment.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.