Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract: Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.

Abstract: Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Abstract: A compound having the following formula I: where R1 is an alkyl group or an alkenyl group, X represents R2 is selected from the group consisting of a halogen (o, m, p) group such as F, Cl, Br or I, —NH2, —NO2 and a hydrogen group, R3 is a hydrogen group or OH. The compound has pharmacologically ?2-adrenergic/5-HT2A antagonist activity, 5-HT re-uptake activity, and anti-oxidant activity. The compound is produced by preparing 4-epoxy isoeugenol, mixing piperazine dissolved in methanol with the 4-epoxy isoeugenol to reflux at 100° C. for approximately 2 to approximately 6 hours, removing the methanol, passing the mixture through a silica gel column chromatography after the removing step, eluting the passed mixture with n-hexane and ethyl acetate, drying the eluted mixture, and crystallizing the dried mixture with methanol.

Abstract: This invention relates to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.

Abstract: A process for the monomethylation of nitrogenous heterocycles having at least one nitrogen atom bonded to a hydrogen atom by reacting the nitrogenous heterocycle with dimethyl carbonate at a temperature of between 100° and 200° C. and a pressure of between 0.93×105 Pa and 1.07×105 Pa while methanol produced during the reaction is distilled off as it is formed.

Abstract: The present invention relates to a compound selected from those of formula (I): wherein: R1 represents alkyl, R2 represents hydroxy, alkoxy, or amino, n represents an integer from 1 to 12 inclusive, R3 represents: hydrogen, optionally substituted alkyl, cycloalkyl, pyrimidinyl or optionally substituted phenyl, its isomers, and addition salts thereof with a pharmaceutically acceptable acid or base, medicinal products containing the same are useful in the prevention or treatment of acute and chronic cell ischaemia.

Abstract: Described herein is a series of aryl piperazine compounds of the formula: wherein Ar′ is a mono or bicyclic aryl or heteroaryl 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-C5)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-C5)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is —(C═O)—, —CHOH— or —CH2—; or a pharmac

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: 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: 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 medicine having the following basic structure, for the alleviation or treatment of symptoms derived from ischemic diseases and seizures, epilepsy, and migraine, having a powerful action in suppressing cytotoxic Ca2+ overload and free from side-effects: wherein Z═C, CH, or N, X═O or CH2, E and Y═H, OH, a halogen, alkoxy, alkyl, or a halogen-substituted alkyl.

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

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: The present invention is directed to an N-phenyl-N′-phenylpropylpiperazine derivative represented by formula (1): (wherein R1 represents a lower alkyl group; R2 represents a lower alkoxy group; and R3 represents a cyano group, a carboxyl group, or an indolecarbonyl group); a medicament; and to a process for producing the derivative. The compound of the present invention is endowed with potent &agr;1-adrenoceptor blocking activity, and thus is useful for the prevention or treatment of hypertension, congestive heart failure, myocardinal ischemia, arrhythmia, angina pectoris, and urinary obstruction and pollakiuria caused by benign prostatic hyperplasia.

Abstract: Piperazine derivatives of formula (I) wherein Z, X, n, Ar and i have the meanings defined herein are usefull in the treatment of pathologies associated with insulin-resistance syndrome.

Abstract: This invention relates to a series of substituted piperazines of Formula II, as well as enantiomers thereof These compounds are useful in the manufacture of pharmaceutical compositions.

Abstract: A hydroquinone compound is represented by the following formula or a pharmacologically acceptable salt thereof with W, R, R1-4, and B1-2 defined herein.

Abstract: Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally through employment of a tether moiety. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.

Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof, wherein: X, Y and Z are the same or different and represent optionally substituted carbon or nitrogen; R1 and R2 independently represent organic or inorganic substituents; R3 and R4 are variables independently representing inorganic or organic substituents; A represents C1-C4 alkylene; and R5, R6, and R7 independently represent hydrogen or C1-C6 alkyl, which compounds bind selectively with high affinity to the dopamine D4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.

Abstract: A process for preparing a 1-aryl-4-(arylethyl)piperazine of the formula (I) by reacting a 1-arylpiperazine of the formula (II) with an aromatic olefin of the formula (III) Ar′CR1═CHR2  (III) in an inert solvent in the presence of at least one basic catalyst, where in the formulae (I) to (III) Ar and Ar′ independently of one another are an aryl radical, selected from the group of the fused and unfused C6-C22-aromatics and the fused or unfused C5-C22-heteroaromatics which have at least one nitrogen, oxygen or sulfur atom in the ring; and R1 and R2 independently of one another are a hydrogen atom, a C1-C8-alkyl radical or an aryl radical Ar.

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 hydroquinone derivative useful as an intraocular pressure lowering, anti-hypertensive and radical scavenging agent represented by the following formula 1

Abstract: A monohydrate of an aminobenzenesulfonic acid derivative represented by the following formula (I), for example, 2-(1-piperazinyl)-5-methylbenzenesulfonic acid, is substantially free from weight change due to moisture absorption and can be weighed accurately in manufacturing a pharmaceutical composition for the treatment of heart diseases comprising said monohydrate.

Abstract: A series of aryl piperazine compounds of the formula: or the pharmaceutically acceptable salts thereof, 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: 4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) wherein one of X and Y is CH2, and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute a 3-7-membered ring; R8 is hydrogen or alkyl

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where X, W, Z, A, G, R1, R2, R3, R4, R5, R5′ and k have the meanings described in the specification. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof Also described are pharmaceutical compositions comprising these compounds, and methods of treating or preventing metalloprotease-related maladies using the compounds or the pharmaceutical compositions.

Abstract: A compound of the formula: is disclosed. This compound is useful in methods of protecting a subject of of protecting biological materials from radiation damage.

Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.4, R.sup.23, R.sup.24, R.sup.25 and R.sup.26 are defined as in the specification.These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and antagonists.

Abstract: Di- and tri-Methoxybenzyl substituted piperazines and piperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopamine antagonists and antipsychotic agents.

Abstract: Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable addition salts thereof, wherein: X, Y and Z are the same or different and represent optionally substituted carbon or nitrogen;R.sub.1 and R.sub.2 independently represent organic or inorganic substituents;R.sub.3 and R.sub.4 are variables independently representing inorganic or organic substituents;A represents C.sub.1 -C.sub.4 alkylene; andR.sub.5, R.sub.6, and R.sub.7 independently represent hydrogen or C.sub.1 -C.sub.6 alkyl,which compounds bind selectively with high affinity to the dopamine D.sub.4 receptor subtype and are therefore of use in treatment of various neuropsychological disorders.

Abstract: Compounds of formula (I) wherein: R.sub.1 is --(CR.sub.4 R.sub.5).sub.n C(O)O(CR.sub.4 R.sub.5).sub.m R.sub.6, --(CR.sub.4 R.sub.5).sub.n C(O)NR.sub.4 (CR.sub.4 R.sub.5).sub.m R.sub.6, (CR.sub.4 R.sub.5).sub.n O(CR.sub.4 R.sub.5).sub.m R.sub.6, or --(CR.sub.4 R.sub.5).sub.r R.sub.6 : W is alkynyl or 2 carbon atoms; R.sub.3 is H or R.sub.7 ; Z is C(O)R.sub.13, (CH.sub.2).sub.0-1 C(O)OR.sub.13, (CH.sub.2).sub.0-1 C(O)NR.sub.10 R.sub.13, (CH.sub.2).sub.0-1 C(R.sub.8 R.sub.8)OR.sub.8, --NHC(O)R.sub.7, (CH.sub.2).sub.0-1 NR.sub.10 R.sub.13, NH[C(O)C(O)OR.sub.8 ], CH.sub.2 NH[C(O)CNR.sub.10 R.sub.13 ], CH.sub.2 S(O).sub.q R.sub.7, CH[S(O).sub.q R.sub.7 ].sub.2, dithiolane, (tetrazol-5-yl), thiazol-2-yl, [1,2,4]thiadiazol-5-yl, [1,3,4]oxadiazol-2-yl, imidazol-2-yl, oxazol-2-yl, or (3- or 5-oxadiazolyl[1,2,4]; R.sub.7 is --(CR.sub.4 R.sub.5).sub.q R.sub.11 or C.sub.1-6 alkyl wherein the R.sub.11 or C.sub.

Abstract: A monohydrate of an aminobenzenesulfonic acid derivative represented by the following formula (I), for example, 2-(1-piperazinyl)-5-methylbenzenesulfonic acid, is substantially free from weight change due to moisture absorption and can be weighed accurately in manufacturing a pharmaceutical composition for the treatment of heart diseases comprising said monohydrate.

Abstract: Substituted piperazines and piperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopamine antagonists and antipsychotic agents.

Abstract: Compounds corresponding to the general formula (I): ##STR1## in which X represents a hydrogen atom, a hydroxyl group, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom, a hydroxyl group or a methoxy group and salts and bases thereof. The compounds may exists in the form of a pure enantiomer or as a mixture of enantiomers. Additionally, the compounds of formula (I) are useful for the treatment of diseases associated with serotoninergic receptors, particularly anxiety and/or depression.

Abstract: This invention encompasses compounds of formula (I) and the pharmaceutically ##STR1## acceptable salts thereof, wherein W,X,Y,A,T,R.sub.1 -R.sub.4,B,Ar,n and m are described herein and are useful in treating feeding disorders and certain cardiovascular diseases due to the binding of these compounds to human Neuropeptide Y1 receptors.

Abstract: A compound of formula (I): ##STR1## In which: R.sub.1 represents linear or branched (C.sub.1 -C.sub.6) alkyl,X represents oxygen or sulfur,R.sub.2 represents optionally substituted alkyl, alkoxy, optionally substituted phenyl, optionally substituted cycloalkyl, 4-(2,3-dithiacyclopent-1-yl)butyl, pyridyl or optionally substituted amino or any one of the groups as defined in the description,R.sub.3 represents hydrogen or cycloalkyl, formyl, optionally substituted phenyl, pyridyl or optionally substituted alkyl,the isomers thereof, the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal compounds containing them are useful for the treatment of chronic or cellular ischemia.

Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.

Abstract: The salts of S(+) 2-(3-benzoylphenyl)propionic acid and of R(-) 2-(3-benzoylphenyl)propionic acid with an organic base such as D-lysine, L-lysine, L-arginine, (R) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol and (S) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol, the process for their preparation and the corresponding pharmaceutical compositions containing said salts are described.

Abstract: Fused benzo compounds of formula I are provided, wherein A is a 2 to 6 membered hydrocarbon spacer group, B is a polar divalent group selected from a group (a); U is C, N or CH; X is a divalent 3-4 membered chain optionally comprising one or more heteroatoms; R.sup.1 is an aliphatic hydrocarbon group, arylalkyl or diphenylalkyl; R.sup.2 and R.sup.3 are hydrogen or alkyl or together form an ethylene or propylene bridge; R.sup.4, R.sup.5 and R.sup.6 are hydrogen or substituents; R.sup.7 and R.sup.8 are hydrogen or substituents including --COOR.sup.9 and --CONR.sup.10 R.sup.11 ; are 5-HT.sub.1A receptor ligands useful in the treatment of CNS disorders. Pharmaceutical compositions comprising the compounds and their use for the manufacture of a pharmaceutical preparation are also provided.

Abstract: Alkyl derivatives of trazodone endowed with pharmacological activity, pharmaceutical compositions containing them, process for preparing them and intermediate compounds useful in their preparation are disclosed.

Abstract: Alkyl derivatives of trazodone endowed with pharmacological activity, pharmaceutical compositions containing them, process for preparing them and intermediate compounds useful in their preparation.

Abstract: The compound of the formula (I) or its salt or a medicament containing the same ##STR1## wherein, A and B represent a carbonyl group or sulfonyl group, m and p are different and represent 0 or 1,R.sup.1 and R.sup.2 may be the same or different from each other and represent a hydrogen atom, an unsubstituted or substituted alkyl group, an unsubstituted or substituted aryl group, an unsubstituted or substituted aralkyl group, an unsubstituted or substituted heterocyclic group containing nitrogen or an unsubstituted or substituted heterocyclic group containing oxygen, or R.sup.1 and R.sup.2, taken together with the nitrogen atom to which they are linked, may form an unsubstituted or substituted heterocyclic group, provided that when B is a sulfonyl group, R.sup.

Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;Ar and Ar' independently are a thienyl group; a substituted or unsubstituted phenyl group; or an imidazolyl group; it also being possible for Ar' to be a benzothienyl group which is unsubstituted or substituted by a halogen; a naphthyl group which is unsubstituted or substituted by a halogen; a biphenyl group; or a substituted or unsubstituted indolyl;X is hydrogen;X' is hydrogen or a hydroxyl group or is joined to X" below to form a carbon-carbon bond, or X and X' together form an oxo group or a dialkylaminoalkoxyimino group of the formula .dbd.N--O--(CH.sub.2).sub.p --Am, in which p is 2 or 3 and Am is a dialkylamino group;Y is a nitrogen atom or a group C(X"), in which X" is hydrogen or forms a carbon-carbon bond with X';Q is hydrogen, a C.sub.1 -C.sub.4 alkyl group or an aminoalkyl group of the formula --(CH.sub.2).sub.

Abstract: A compound represented by formula (I): ##STR1## wherein Q represents an aryl group, a heterocyclic group, a diarylmethyl group, an aralkyl group composed of an aryl group and an alkylene group, an alkyl group or a cycloalkyl group, in which the aryl group, heterocyclic group, and the aryl moiety of the diarylmethyl group and aralkyl group may be substituted with one or more substituents; R represents a bicyclic, substituted, nitrogen-containing heterocyclic group or a substituted phenyl group, in which the nitrogen-containing heterocyclic group is composed of a 5-membered, substituted, aromatic or saturated ring containing one or two nitrogen atoms and a 6-membered ring; and Z represents an alkylene group, an alkenylene group, an alkylene group, a carbonyl group, an alkylene group containing a carbonyl group or an oxalyl group, or a salt thereof.

Abstract: The present invention relates to substituted piperazine derivatives (herein referred to as compounds or compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.

Abstract: Compounds of the formula ##STR1## and their salts with mineral or organic acids are useful as neurokinin receptor antagonists. Methods of preparing the compounds, especially pure STEREO ISOMERS thereof, are provided.

Abstract: Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.

Abstract: An arylamide derivative of formula (1), a salt thereof and a therapeutic agent for hyperlipemia which comprises the derivative or salt: ##STR1## wherein Ar represents a group ##STR2## a naphthyl group, a pyridinyl group, a furyl group, a thienyl group, a quinolyl group or an indolyl group; Y represents a group ##STR3## and Q represents --O-- or a single bond, Z represents an alkylene group, and R.sup.4 represents a hydroxyl group, an alkoxy group or a group --NH(CH.sub.2).sub.m COOH.

Abstract: Compounds of formula: ##STR1## in which X represents a hydrogen atom, a C.sub.1 -C.sub.3 alkoxy group or a cyclopropylmethoxy group and Y represents a hydrogen atom or a methoxy group, are useful in the therapy of conditions.