Abstract: Novel aminoalkylphenols, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the aminoalkylphenols or compositions thereof are disclosed.

Abstract: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with indoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.

Abstract: A compound of formula (IA) or the pharmaceutically acceptable acid addition salts thereof wherein: R1, R2, R3, R4 and R5 are the same or different and represent hydrogen, halogen, C1-C6alkyl, C1-C4-alkoxy, C1-C4akylthio, hydroxy, 1 amino, mono(C1-C6) alkylamino, di(C1-C6)alkylamino, cyano, nitro, trifluoromethyl or trifluoromethoxy; R6 is hydrogen or C1-C6alkyl; W is nitrogen, COH, or CH; Y and Z independently represent nitrogen or CH; and A represents an alkylene group of from 2-5 carbon atoms optionally substituted with one or more alkyl groups having from one to four carbon atoms. The compounds of the invention demonstrate high affinity and selectivity in binding to the D4 receptor subtype.

Abstract: This invention relates to compounds of Formula I 1

Abstract: Substituted heterocyclic compounds for treating multidrug resistance are disclosed. Compositions and methods of use for the substituted heterocyclic compounds are disclosed.

Abstract: This invention provides a compound of the formula (I): 1

Abstract: The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof; as antifungals; their processes for preparation, composition containing them and their use as a medicine.

Abstract: Substituted heterocyclic compounds for treating multidrug resistance are disclosed. Compositions and methods of use for the substituted heterocyclic compounds are disclosed.

Abstract: Substituted acyclic compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent.

Abstract: A use for agents that disrupt actin cytoskeletal organization is provided. In the instant invention, agents that disrupt actin cytoskeletal organization are found to upregulate endothelial cell Nitric Oxide Synthase activity. As a result, agents that disrupt actin cytoskeletal organization are useful in treating or preventing conditions that result from the abnormally low expression and/or activity of endothelial cell Nitric Oxide Synthase. Such conditions include pulmonary hypertension, ischemic stroke, impotence, heart failure, hypoxia-induced conditions, insulin deficiency, progressive renal disease, gastric or esophageal motility syndrome, etc. Subjects thought to benefit mostly from such treatments include nonhyperlipidemics and nonhypercholesterolemics, but not necessarily exclude hyperlipidemics and hypercholesterolemics.

Abstract: Novel sulphonamide derivatives having CNS activity, processes for their preparation and their use as medicaments are disclosed.

Abstract: Substituted bicyclic compounds for treating multidrug resistance are disclosed. Compositions and methods of use for the substituted bicyclic compounds are disclosed.

Abstract: Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.

Abstract: Sulfonylcarboxamide derivatives of formula I, their physiologically acceptable salts and/or physiologically functional derivatives, methods of making these compounds, their use for preparing medicines for the prevention and treatment of hyperlipidemia and arteriosclerotic disorders.

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: The invention provides a method of treatment or prophylaxis of obesity, comprising administering to a patient in need of such treatment a therapeutically effective amount of an aryl sulfonamide compound of formula (I) or formula (II) wherein the substituents are as described in the specification.

Abstract: The present invention provides sustained-release derivatives of hydroxylated analogs of substituted 1-[2[bis(aryl)methoxy]ethyl]-piperazines and -homopiperazines, pharmaceutical compositions comprising the same, and a method of using such sustained-release derivatives to bind the dopamine transporter to achieve a desired effect, such as antagonism of dopamine reuptake inhibitors, such as cocaine, or dopamine releasers or norepinephrine and/or serotonin reuptake inhibitors, such as methamphetamine.

Abstract: The present invention relates to a process for preparing 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen-2-ol compounds useful as an estrogen agonist.

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: The present invention provides novel compounds of the general formula: 1

Abstract: The present invention comprises unsubstituted and substituted piperazine-containing compounds having alkanoyl, alkylsulfonyl, alkylamido or alkoxycarbonyl substituents, and having the formula A, which inhibit prenyl-protein transferases. In particular, the invention relates to prenyl-protein transferase inhibitors which are efficacious in vivo as inhibitors of geranylgeranyl-protein transferase type I (GGTase-I) and that inhibit the cellular processing of both the H-Ras protein and the K4B-Ras protein. Such therapeutic compounds are useful in the treatment of cancer.

Abstract: The invention concerns compounds of formula (I) wherein R1, R2, R3, R4 and R5 are as defined herein. Said compounds are useful in therapy as antithrombotic agents.

Abstract: Disclosed are compounds of the formula: 1

Abstract: The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—, —C═C—, —(CH═CH)2—, —C≡C—CH═CH—, —CH═CH—C≡C—, phenylene or the like, and W is or and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.

Abstract: The present invention comprises piperazine/piperazinone-containing compounds having multicyclic ring system substituents on one of the piperazine/piperazinone nitrogens, which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.

Abstract: Novel compounds which are inhibitors of the binding of fibrinogen to the Gp iib/iiia platelet receptors, and which can be used therapeutically as antithrombotic agents.

Abstract: A compound of formula I, 1

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 CNS disorders.

Abstract: Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R1, R2 and R3 are each, independently, hydrogen, halogen, CF3, alkyl, alkoxy, MeSO2, or together can form a 5-7 membered carbocyclic or heterocyclic ring; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, alkylaryl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, or alkoxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is carbon or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.

Abstract: The present invention provides novel compounds of the general formula: wherein R1 and R2 are H, OH, F, Cl, Br, I, 1 to 6 carbon alkyl or alkenyl, 1 to 6 carbon alkoxy, aryl, OR5, nitro, amino, CF3 or R1 and R2 are taken together to form a fused ring at the 2,3- or 3,4-positions providing a fused phenyl group or a benzodioxane group, or a 4- or 7-substituted indole group, or a 4- or 5- or 8-substituted quinoline group; R3 represents a group selected from hydrogen, a 1 to 6 carbon alkyl, a 1 to 4 carbon alkoxy or a halogen; R4 represents a group selected from hydrogen, 1 to 6 carbon alkyl or R5; R5 is CH2Ph in which the phenyl ring can be optionally substituted by a group selected from OMe, halogen, CF3; X is selected from a group represented by N, CR4, CHR4 and CHCH; A is selected from a group represented by N, NH, CH and CH2; B is selected from a group represented by ═O, ═S, H and H2; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and m

Abstract: Compounds of the Formula (I) wherein R2, Y, X and n are as defined in the specification which compounds are useful in the treatment of disorders associated with serotonergic neuron-related diseases.

Abstract: The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor.

Abstract: New 4-(1-piperazinyl)benzoic acid derivatives of the formula (I) are described. Also described is methods for making these compounds and their use as therapeutic agents. In particular, the compounds find use in the treatment of diabetes.

Abstract: The invention relates to compound of formula (I): 1

Abstract: Arylalkylpiperazine compounds (1) wherein B is aryl or optionally substituted aryl; R1 is hydroxy; R2 and R3 are the same or different and are independently selected from hydrogen or C1-3 alkyl; m is 0, 1 or 2; D is a linking chain of atoms which may be optionally substituted and which contains from 1 to 8 atoms in the chain; E is a phenolic antioxidant group or a corresponding amino derivative thereof wherein the phenolic hydroxyl is replaced by amino, are disclosed. The compounds have both free radical scavenging activity and block excitatory amino acid activity. Some compounds of the present invention also display an affinity for voltage-sensitive sodium channels.

Abstract: The invention relates to a group of new piperazine and piperidine compounds having interesting pharmacological properties. It has been found that compounds of formula (a) wherein A represents a heterocyclic group of 5-7 ring atoms wherein 1-3 heteroatoms from the group O, N and S are present; R1 is hydrogen or fluoro; R2 is C1-4-alkyl, C1-4-alkoxy or an oxo group, and p is 0, 1 or 2; Z represents carbon or nitrogen, and the dotted line is a single bond when Z is nitrogen, and a single or double bond when Z is carbon; R3 and R4 independently are hydrogen or C1-4-alkyl; n has the value 1 or 2; R5 is halogen, hydroxy, C1-4-alkoxy or C1-4-alkyl, and q is 0, 1, 2 or 3; Y is phenyl, furanyl or thienyl, which groups may be substituted with 1-3 substituents of the group hydroxy, halogen, C1-4-alkoxy, C1-4-alkyl, cyano, aminocarbonyl, mono- or di-C1-4-alkylaminocarbonyl; and salts thereof show high affinity for both the dopamine D2 and serotonin 5-HT1A receptors.

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R5 is hydrogen or C1-C6 alkyl; and R represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.

Abstract: Novel piperazine and piperidine derivative compounds having interesting and advantageous pharmacological properties. The disdosed compounds have the general formula (a) and salts thereof. These compounds have high affinity for both the dopamine D2 receptors and serotonine 5-HT1A receptors, rendering them useful for the treatment of CNS-disorders, in particular schizophrenia.

Abstract: This invention relates to compounds of the formula where X is halogen, R1 is H or a C1-C3 alkyl, R2 is H or OH and R3 is one of in which A is a single bond or a —CO(CH2)p—NH— group, R4 is H or —C(═NR5)NHR′5, R5 and R′5 are each H or a C1-C6 alkyl group, R6 is H or a C1-C3 alkyl group, m is 0, 1 or 2; n is 2, 3 or 4; p is 1, 2 or 3; plus their acid addition salts. The invention likewise relates to the method for their preparation and their therapeutic applications.