Abstract: The present invention relates to substituted piperazine derivatives of general formula 1

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1

Abstract: The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives showing superior antioxidant activity compared to the known antioxidant compounds, their pharmaceutically acceptable salt, and pharmaceutical compositions containing them. It can be usefully used in treating neurodegerative diseases such as aging, cancer, diabetes, ischemic stroke, Parkin's disease, dementia and Huntinton's disease.

Abstract: The present invention relates to a compound selected from those of formula (I): 1

Abstract: The present invention provides a method of treating or preventing a novelty-seeking disorder such as pathological gambling, attention deficit disorder with hyperactivity disorder, substance addiction, drug addiction, alcohol addiction and sex addiction. using a compound which is a dopamine D4 receptor ligand, or a pharmaceutically acceptable salt thereof.

Abstract: The invention provides compounds of Formula (I): 1

Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula 1

Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted indan derivatives having the formula I 1

Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl, CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

Abstract: The present invention relates to a compound represented by formula (1): wherein Q, which may have a substituent, represents an aryl group, a heterocyclic group, a diarylmethyl group, or an aralkyl group; R, which may have a substituent, represents a bicyclic nitrogen-containing heterocyclic group or a phenyl group; and Z represents a C1-C3 alkylene group, a C2-C4 alkenylene group, a C1-C3 alkylene group having one hydroxyl group, a carbonyl moiety, a C1-C2 alkylene group containing one carbonyl moiety at one end or an intermediate position of the carbon chain, or an oxalyl group; or salts thereof and a piperazine-cyclodextrin complex combined with a water-soluble cyclodextrin derivative. The complex exhibits enhanced water solubility, excellent stability, and low topical stimulation and is useful as a therapeutic agent for circulatory diseases and diseases of the brain region.

Abstract: Disclosed are compounds of the formula: 1

Abstract: The present invention provides pharmaceutically active compounds useful for the treatment of diseases or disorders of the central nervous system.

Abstract: The present invention relates to a novel 4′-methanesulfonyl-biphenyl derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor.

Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

Abstract: The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): 1

Abstract: The present invention relates to a novel process for the preparation of a compound of formula I: 1

Abstract: The invention provides substituted phenyl compounds of general formula wherein R1, T, U and Ar are as 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: The treatment of addictive disorders, psychoactive substance use disorders, intoxication disorders, inhalation disorders, alcohol addiction, tobacco addiction, and nicotine addiction using a heterocyclic amine, a phenylazacycloalkane, a cabergoline, or an aromatic bicyclic amine active agent, or a pharmaceutically acceptable derivative or salt of any said active agent is described herein.

Abstract: The invention relates to therapeutic benzamide compounds of formula (I) wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present invention also provides pharmaceutical compositions, processes for the preparation of compounds of formula (I) and their use in the treatment of conditions mediated by ApoB-100 regulation.

Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted indan derivatives of the formula I as (R)-enantiomers, (S)-enantiomers, or racemates in the form of a free base or pharmaceutically acceptable salts or solvates thereof. The present invention further relates to a process for the preparation of the compounds, to pharmaceutical compositions containing the compounds and to methods of treatment of 5-hydroxytryptamine-mediated disorders comprising administering the compounds.

Abstract: The present invention therefore provides, in a first aspect, a compound of formula (I) or a salt thereof: in which the group D is selected from a group of formula (A), (B) or (C) below: in which P is a monocyclic, bicyclic or tricyclic alicyclic ring containing up to 20 carbon atoms in the ring(s); A is a single bond, a C1-6alkylene or a C2-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more fluorine atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, amino, alkylamino or dialkylamino, SR11 where R11 is hydrogen or C1-6alkyl or R1 is aryl, arylC1-6alkyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulfur; n is 0, 1, 2 or 3; and R2 is hydrogen, C1-6alkyl, aryl, arylC1-6alkyl or C3-6cycloalkyl; or in which Ra is an alkyl group containing 1 to 20 carbon atoms o

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): 1

Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: R1, R2, R3 R4 and R5, R6, R7, and R8 represent organic and/or inorganic substituents as defined herein, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

Abstract: A method for treating Attention Deficit/Hyperactivity Disorder (ADHD) in humans and the symptoms associated therewith, inattentiveness, and hyperactivity with impulsivity, using eltoprazine and related compounds is provided.

Abstract: Sulfohydroxamic acid diarylamines and derivatives thereof; compositions made from them; and methods of using them.

Abstract: A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: wherein R1 to R4 independently represent H, halogen, OH, alkoxy, optionally substituted alkyl, aryl, or aralkyl group, R5 represents H, optionally substituted alkyl, aryl, or aralkyl group, E1 represents O, S, or —NR6, where R6 represents H, an optionally substituted alkyl, aryl, or aralkyl group, E2 represents O, S, or —NR7, where R7 represents H, an optionally substituted alkyl, aryl, or aralkyl group, A represents CH, C(OH), or N, X represents H, halogen, alkoxy, or an optionally substituted alkyl group, and Q represents an optionally substituted phenyl group, phenoxy, phenylmethyl, or cycloalkyloxy group, where when E1 represents O or S, E2 does not represent O or S, which has an action of suppressing the cytotoxic Ca2+ overload and lipid peroxidation and effective for pharmaceutical preparation for the alleviation and treatment of symptoms due to ischemic diseases, etc.

Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula wherein: X is a moiety selected from the group of: n is selected from the integers 1 through 5; R1 is optionally substituted aryl or mono or bicyclic heteroaryl, with a proviso that heteroaryl is not thiadiazole; R2 is H or alkyl; R3 is H, COR5, COOR5, and CONR5R6; R4 is H, alkyl, alkenyl, alkynyl, aryl, mono or bicyclic heteroaryl, aralkyl, and mono or bicyclic heteroaralkyl, wherein the aryl or heteroaryl groups are optionally substituted; R5 and R6 are H, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, adamantyl, and noradamantyl or R5 and R6 taken together may form a 5-7 membered azacyclic ring, optionally containing an additional heteroatom selected from O, S, or NR4; when R5 or R6 are chosen from cycloalkyl or cycloalkenyl, the cyclic group may optionally

Abstract: A series of aryl piperazine compounds of the formula: 1

Abstract: Described herein is a compound of the formula wherein Ar′ is a mono or bicyclic aromatic or heteroaromatic radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is —(C═O)—; or a pharmaceutically acceptable salt racemate, optical isomer or solvat

Abstract: A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.

Abstract: New substituted 4-phenyl N-alkyl)-piperazine and 4-phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bind at the dotted line; R1 is CF3, OSO2CF3, OSO2CH3, SOR7, SO2R7, COR7, CN, OR3, NO2, CONHR3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, and NH2; R3 and R4 are independently H or a C1-C4 alkyl; R5 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or —(CH2)—R6; R6 is a C3-C6 cycloalkyl, 2-tetrahydrofurane, or 3-tetrahydrofurane; R7 is a C1-C3 alkyl, CF3, or N(R4)2, and pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

Abstract: The present invention is directed to novel 1-(N-phenylaminoalkyl)piperazine derivatives substituted at the position 2 of the phenyl ring. Pharmaceutical compositions comprising the compounds of the invention also are contemplated. The compounds of the present invention also are contemplated for use in treating neuromuscular dysfunction of the lower urinary tract in a mammal.

Abstract: Novel compounds of the formula I in which X, Y, R1, R2 and R3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

Abstract: The invention provides compounds of general formula 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: A method of treating Mild Cognitive Impairment has been discovered. The treatment method comprises administering an effective amount of a serotonergic agent, including, but not limited to dexnorfenfluramine. The agent can be any serotonergic agonist, partial agonist, serotonin reuptake inhibitor, or combinations of these agents. The treatment method also encompasses combinations of serotonergic agents and non-steroidal anti-inflammatory agents. The treatment method may also delay the onset of Mild Cognitive Impairment, dementia, or both.

Abstract: A compound having agonist activity to the 5-HT4 receptor for use as a medicament and the use of said compound in the manufacture of a medicament for use in therapeutic or prophylactic treatment of disorders involving bronchocontraction of a human or animal body is described, as well as methods of treatment, wherein said compounds are administered. Further, a compound having antagonist activity to the 5-HT2a receptor for use as a medicament and the use of said compound in the manufacture of a medicament for use in therapeutic or prophylactic treatment or disorders involving bronchocontraction of a human or animal body is described, as well as methods of treatment, wherein said compounds are administered.

Abstract: A method for potentiating the action of a serotonin reuptake inhibitor in increasing the availability of serotonin, norepinephrin and dopamine in the brain, comprising administering to a patient in need of such treatment a serotonin reuptake inhibitor in combination with an effective amount of a compound of the formula 1

Abstract: This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula 1

Abstract: Provided, among other things, is a method of decreasing intraocular pressure or improving ocular accommodation in an animal, including a human, comprising administering an intraocular pressure decreasing or ocular accommodation improving amount of a compound of the formula I:

Abstract: Compound of formula (I): which is useful as a TXA2 and 5-HT2 receptor antagonist and pharmaceutical compositions containing the same.

Abstract: The present invention relates to novel N-substituted azaheterocyclic compounds of the general formula 1

Abstract: This invention is directed toward a method of preparing a topical composition comprising ciprofloxacin and hydrocortisone. The method involves dispersing hydrocortisone with lecithin for greater than 45 minutes prior to combining hydrocortisone with the balance of the composition.

Abstract: Compounds of general formula (1) are described: 1

Abstract: The present invention relates to a piperazine compound of the formula wherein R1 and R2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R3, R4 and R5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R6 and R7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R8 and R9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds.

Abstract: This invention relates to the use of a compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined in the disclosure, for treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.

Abstract: An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.

Abstract: Benzamides 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: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be arom

Abstract: A method of reducing, treating or preventing drug-mediated respiratory depression, muscle rigidity, or nausea/vomiting in an animal, incident to the administration to said animal of a mixed delta/mu opioid agonist or a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a delta receptor agonist compound. Preferred examples of such delta receptor agonist compound include diarylmethyl piperazine compounds and diarylmethyl piperidine compounds, and pharmaceutical compositions thereof, having utility in medical therapy for reducing respiratory depression associated with certain analgesics, such as mu opiates.

Abstract: Provided, among other things, is a method of treating, ameliorating or preventing certain fibrotic diseases or other indications in an animal, including a human, comprising administering an effective amount of a compound of the formula I: