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: The present invention relates to novel heteroaryl-diazabicycloalkanes which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 3; q is 0 to 4; —A—B— represents —(CH2)r—, —(CH2)t—O—, —(CH2)t—S(═O)u— or —(CH2)t—NR3—; r is 2 to 4; t is 1 to 3; u is 0 to 2; X1 is O, S, NR3 or a direct bond; R1 and R4 are C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6, NR7R8 or substituted C1-4alkyl; R2 is aryl, Het1, C3-7cycloalkyl, cyano, optionally substituted C1-6alkyl, —C(═Q)—X2—R15; R3 is hydrogen or C1-4alkyl; R15 is hydrogen, optionally substituted C1-6alkyl, C3-7cycloalkyl, aryl; where X2 is a direct bond, R15 may also be halo or Het1; where X2 is NR5, R15 may also be hydroxy; where X2 is C(═O)—NH—NH or NH—NH—C(&bo

Abstract: A compound of formula (I): wherein A is an optionally substituted heterocyclic group, R is a lower alkoxy; Z is C═O or CH2; and B is benzazapinyl, which may be optionally substituted, or a salt thereof, that possesses vasopressin antagonistic activity and is useful as a vasopressin antagonist.

Abstract: Compounds of formula (I) 1

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

Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

Abstract: 1

Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1

Abstract: Disclosed are novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein n, m, X, R1, R2, R3, R4, R5, R6, and R7 are defined more fully in the description. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.

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

Abstract: Compounds of formula (I) 1

Abstract: Benzoazepines of the following formula wherein R1, R1a, R2, R9k, L, Q, X, Y and Z are as described herein, and analogs thereof are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.

Abstract: A benzoheterocyclic derivative of the following formula [1]: 1

Abstract: Disclosed are thiazolobenzoheterocycles of the general formula Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them.

Abstract: The invention relates to nitro- and cyano-1,2,4,5-tetrahydro-heterocycloazepinyl pyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.

Abstract: Certain novel substituted piperidine compounds 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. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.

Abstract: Compounds of formula I 1

Abstract: 4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine compounds or salts thereof and pharmaceutical compositions containing 4,4-difluoro-2,3,4,5-tetrahydro-1H-1-benzoazepine compounds, or salts thereof, and a pharmaceutically acceptable carrier. The chemical structure of these compounds is characterized by a difluoro group on a ring carbon atom adjacent to an azepine ring carbon atom substituted with a methylidene group. Pharmaceutical compositions containing these compounds are particularly useful as oxytocin antagonists and are effective in inhibiting threatened premature birth or abortion and precesarean birth, and are effective as a remedy for dysmenorrhea and other such conditions.

Abstract: A benzoheterocyclic derivative of the following formula [1]: and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.

Abstract: Hydroxamic acids having the formula 1

Abstract: The invention relates to a compound represented by the general formula (1), 1

Abstract: A pyridine alcohol derivative represented by General Formula III 1

Abstract: A compound represented by the formula (I) or its salt and herbicidal and desiccant use thereof: wherein X, Y are independently hydrogen, halogen, cyano, nito, or (C1-6)haloalkyl; Z is oxygen or sulfur; and

Abstract: This invention relates to a compound of the Formula I

Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids

Abstract: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: wherein R1, R2, R3 and R4 are independently selected from the group consisting of H, halo, OH, C1-6alkyl, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl and others; R5 is selected from the group consisting of SO2Ar, C(O)Ar, Ar and CH2Ar; R6 and R7 are independently selected from the group consisting of H, C1-6alkyl, optionally substituted phenyl and optionally substituted benzyl; ————— represents a single or double bond; n is selected from an integer of from 1-3; X is selected from the group consisting of CR17 and N; Z is selected from the group consisting of C, CH and N, provided that when ————— is a double bond, Z is C and when ————— is a single bond, Z is selected from CH and N; Ar is an optionally substituted aromatic group selected from the group consisting of phenyl, pyridyl, thienyl,

Abstract: A new process for preparing substituted 7-aminocarbonyl-3-oxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepines is disclosed.

Abstract: The present invention relates to compounds of formulas (IA), (IB), and (IC): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.

Abstract: This invention is to provide a compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted 5- to 6-membered ring: C is a divalent group of the formula: ##STR2## wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R.sup.2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.

Abstract: There are described compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the description, Q is heterocyclyl boned via a ring nitrogen atom and having the formula IA ##STR2## wherein R.sub.3 and R.sub.4 and m and n are as defined in the description, the ring marked A is a heterocyclyl having 5 to 9 ring atoms and having at least one saturated bond, it being possible for a further ring hetero atom selected from O and S to be present in addition to the bonding nitrogen atom, the ring system marked B is a free or benzo-, thieno-, furo-, pyrrolo- or dihydropyrrolo-fused carbocyclic ring having from 5 to 9 carbon atoms that is fused to the ring A and may be unsaturated, partially saturated or fully saturated, and the bond marked by a parallel dotted line between the ring systems marked A and B is either a single bond or a double bond, and a salt thereof where at least one salt-forming group is present.

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:X--CO--CH.sub.2 --Z (I)whereinX is a monocyclic or polycyclic aromatic group,Z is of a linear, cyclic or bicyclic, aromatic or aliphatic moiety containing a nitrogen atom;and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

Abstract: This invention relates to substituted benzamido-heterocyclic compounds of general formula (I) having an alkoxy substituent at the C2 position of the benzamido group and various substituents at positions C4 and C5, being optionally substituted on the N atom of the heterocyclic system, and where the unsaturated ring of the heterocyclic system is a 5,6, 7 or 8-membered ring. Also to the use of these compounds as anticonvulsants in certain medical conditions, and to processes for making them.

Abstract: Novel benzazepine derivative of the formula [1]: ##STR1## wherein R.sup.1 is H or halogen, A is lower alkylene, R.sup.2 and R.sup.3 are the same or different and each H, lower alkoxy, lower alkyl having optionally a lower alkoxy substituent, etc., or R.sup.2 and R.sup.3 may combine together with the nitrogen to which they bond to form a 5- to 7-membered saturated heterocyclic group which may optionally be substituted by a lower alkyl, etc., R.sup.4 is H, lower alkyl, OH, etc., R.sup.5 is --NHR.sup.6 (R.sup.6 is lower alkyl) or pyrrolidinyl, or a salt thereof, which show excellent anti-vasopressin activity, oxytocin antagonistic activity and vasopressin agonistic activity, and are useful as a vasopressin antagonist, a vasopressin agonist and an oxytocin antagonist.

Abstract: A benzoheterocyclic derivative of the following formula [1]: ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.

Abstract: The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor.

Abstract: The present invention relates to phenethanolamine derivatives of formula (I) wherein R.sup.1 represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R.sup.2 represents hydrogen or C.sub.1-6 -alkyl; R.sup.3 represents a group (A) where the ring is substituted by one to four further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; or R.sup.3 represents a group (B) where the aromatic ring is optionally substituted by up to three further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; R.sup.4 represents hydrogen, or C.sub.1-6 -alkyl; R.sup.5 represents ZCH.sub.2 CO.sub.2 H wherein Z represents a bond, or O; Y represents (CH.sub.2).sub.

Abstract: A compound of the formula ##STR1## wherein a, V, X, Y, Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined above, useful in (a) the treatment of myelosuppression including suppression associated with cancer chemotherapy as well as activation of the immune system for the treatment of cancer or (b) prevention and treatment of viral, fungal, bacterial and parasitic infectious diseases.

Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: Compounds of the formula and compounds of the formula ##STR1## or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.

Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a method for using these compounds.

Abstract: This invention provides new condensed furan compounds which exhibit excellent 2,3-oxidosqualene cyclase inhibition and high-density lipoprotein-cholesterol elevating activities.This invention also provides a therapeutic and prophylactic agent for hyperlipidemia, hypercholesterolemia and atherosclerosis.

Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds of formula I ##STR1## and to pharmaceutical formulations comprising these compounds and methods of treatment comprising administering these compounds to a subject in need of treatment. The novel oxadiazole compounds, such as (.+-.)-3-butyloxy-4-(1-azabicyclo[2.2.2]octyl-3-oxy)-1,2,5-oxadiazole, are useful in treating central nervous system disorders caused by malfunctioning of the muscarinic cholinergic system.

Abstract: Acetic acid derivatives of the formula ##STR1## wherein L, M, T and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell--cell adhesion, and are manufactured by cleaving protecting groups in the corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitrites.

Abstract: Phenyloxazolidinone compound of formula (I)or a pharmaceutically acceptable salt thereof characterized by a bicyclic thiazine or oxazine substituent. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.

Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.

Abstract: Compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form a seven-membered ring containing one optionally substituted nitrogen atom;D.sup.1 to D.sup.4 form a substituted six membered ring, optionally containing up to two nitrogen atoms;R is preferably at least one acid containing substituent;R* is is one or more groups chosen from H, Q-C.sub.1-6 alkyl, Q-C.sub.1-6 oxoalkyl, Q-C.sub.2-6 alkenyl, Q-C.sub.3-4 oxoalkenyl, Q-C.sub.3-4 oxoalkynyl, Q-C.sub.2-4 alkynyl, C.sub.3-6 cycloalkyl, Ar or Het;Q is H, C.sub.3-6 cycloalkyl, Het or Ar;R.sup.6 is preferably a basic nitrogen containing substituent; are inhibitors of platelet aggregation.

Abstract: The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic chiral catalyst to produce a stereoisomerically or regioselectively enriched product.