Abstract: The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar.sup.1 --A.sup.1 ; Ar and Ar.sup.1 are the same or different aryl groups (including heteroaryl) which are optionally substituted, e.g. by one or more substituents commonly used in pharmaceutical chemistry; A and A.sup.1 are the same or different alkylene groups having one or two carbon atoms linking Ar or Ar.sup.1 to N and optionally substituted by lower alkyl and/or optionally substituted aryl, B is an alkylene group of 3 or 4 carbon atoms, which may be substituted by lower alkyl; D.sup.1 represents halogen, CH.sub.3, CR.sup.1 R.sup.2 NH.sub.2, SO.sub.3 H or SO.sub.2 NR.sup.6 R.sup.7 where R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and R.sup.6 and R.sup.7 are each hydrogen, lower alkyl or aralkyl of 7 to 12 carbon atoms or R.sup.6 and R.sup.

Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and -B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.

Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2 and R, R.sup.1, R.sup.2 and R.sup.2 have specified meanings. The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are useful for the treatment of CNS disorders e.g. anxiety, as antihypertensives and in treating anorexia.

Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein Ar is an optionally substituted aryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optionally substituted aryl;A represents a group of formula --XR.sup.3 whereinX is (i) a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q --or (ii) a group of formula --(CHR.sup.6).sub.r --O--(CHR.sup.7).sub.qin which formulae: Y represents --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 providing that p and q do not both represent 0, 1 or 2 and the other is zero; R.sup.6, R.sup.7 and R.sup.8 independently represent hydrogen or lower alkyl, and R.sup.

Abstract: The invention concerns compounds of formula ##STR1## or salts thereof; wherein:.alpha. and .beta. together represent a bond and additionally when B is an electron withdrawing group .alpha. can also represent OH and .beta. can represent hydrogen;Ar is an optionally substituted aryl or heteroaryl radical;R represents hydrogen or an optionally substituted alkyl or aralkyl group;R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen and saturated or unsaturated, cyclic or acyclic aliphatic hydrocarbon residues optionally substituted by one or more groups selected from halogen, OH, carboxy, CN, alkoxy, alkylthio, aryloxy, alkoxycarbonyl, amino, substituted amino, and optioanlly substituted aryl or heteroaryl;A represents a group of formula --XR.sup.3 wherein X is a group of formula --(CHR.sup.6).sub.p --Y--(CHR.sup.7).sub.q -- in which formula: Y represents --O--, --S--, NR.sup.8 or a direct bond, p and q each represent 0, 1 or 2 R.sup.6, R.sup.7 and R.sup.

Abstract: The preparation of compounds having the formula I ##STR1## where R.sup.1 is --CN, --CO--N(CH.sub.3).sub.2 or --CS--N(CH.sub.3).sub.2 and R.sup.2 is hydrogen, methyl or a removable protecting group is carried out by condensing a compound having the formula ##STR2## where M is lithium, sodium, potassium or halomagnesium and R.sup.3 is methyl or a removable protecting group in a solvent comprising 80-100% of one or more hydrocarbons and 0-20% of one or more ethers.The solvent enables less inconvenient reaction temperatures to be used and higher yields to be obtained. Compounds (I) are new per se where R.sup.1 is --CS--N(CH.sub.3).sub.2. Compounds (I) are chemical intermediates for preparing N,N-dimethyl-2-(1-hydroxycyclohexyl)-2-(4-hydroxyphenyl or 4-methoxyphenyl) ethylamine and pharmaceutically acceptable salts thereof. These end products are antidepressants.

Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 which is optionally present represents single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is 0 or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.

Abstract: N'-Acyl-N-alkyl-1,3-diaminopropanes of formulaR.sup.1 CONH(CH.sub.2).sub.3 NHR.sup.2(where R.sup.1 is R- or RNH where R is a substituted or unsubstituted hydrocarbon group and R.sup.2 is alkyl) are prepared by selectively acylating N-alkyl-1,3-diaminopropanes. In the process a N-alkyl-1,3-aminopropane is reacted with an aldehyde to form a hexahydropyrimidine, the hexahydropyrimidine is acylated and the acylated hexahydropyrimidine is then hydrolyzed to give the product.

Abstract: The invention provides a method of relieving inflammation in a mammal inflicted with an imflammatory disease which method comprises treating said mammal with a therapeutically effective amount of a compound of formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, loweralkyl, cycloloweralkyl, loweralkoxy, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, loweralkoxycarbonyl, aryl or aralkyl or 7-12 carbon atoms, or R.sup.1 and R.sup.2 taken together, or R.sup.2 and R.sup.3 taken together form a5,6, or 7 membered ring with the carbon atoms to which they are attached, which ring may be saturated or unsaturated and unsubstituted or substituted by loweralkyl or loweralkoxy, R.sup.

Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and -B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.

Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is alkyl; R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene, R.sup.2 and R.sup.3 complete a 5-norbornen-2-yl moiety; X is --CO.sub.2 --, --OCO--, --OCO.sub.2 --, --N(R.sup.7)CO--, --NHNHCO--, --ON(R.sup.7)CO--, --CON(R.sup.7)--, --N(R.sup.7)CO.sub.2 --, --OCON(R.sup.7)-- or --N(R.sup.7)CON(R.sup.8)--, wherein R.sup.7 and R.sup.8 are, independently, hydrogen, alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are halo, alkyl alkoxy, cyano, nitro or perhalomethyl; R.sup.4 is hydrogen or alkyl; R.sup.5 is hydrogen, alkyl, hydroxyalkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; R.sup.

Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substitutent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.

Abstract: The invention concerns a new stable crystal form of anhydrous, crystalline 1,4-dihydro-2-(imidazol-1-ylmethyl)-6-methyl-4-(3-nitrophenyl)pyridine)-3, 5-dicarboxylic acid 3-ethyl 5-methyl diester hydrochloride, "having a melting point greater than about 215.degree. C., an infra red spectrum (nujolmull) having sharp peaks at 3195 cm.sup.-1, 3100 cm.sup.-1, 2735 cm.sup.-1 and 2625 cm.sup.-1 and an x-ray powder diffraction pattern with specific peaks occurring at 2.theta.=12.3.degree. and 44.5.degree..

Abstract: Aroyl ureas and carbamic acid derivatives of formulaA--CO--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including optionally substituted phenylW is O or SY is NH or S andB is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.

Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is O or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.

Abstract: Piperidine derivatives of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein A represents an aromatic radical selected from ##STR2## wherein R.sup.3 is hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy or halogen; X.sup.1 -X.sup.2 represents CH.sub.2 --CH, NR.sup.4 --CH, O--CH, S--CH, CH.sub.2 --N, O--N, S--N, NR.sup.4 --N, CH--NR.sup.4 or N--NR.sup.4 [where R.sup.4 is hydrogen, (C.sub.1-4)alkyl, phenyl or phenyl(C.sub.1-4)alkyl] or ##STR3## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen, halogen, trifluoromethyl, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, hydroxy, nitro, amino, (C.sub.1-4)alkylamino, di(C.sub.1-4)alkyl-amino, (C.sub.2-4)alkanoylamino, mercapto or (C.sub.1-4)alkylthio and R.sup.1 and R.sup.2 are independently hydrogen, (C.sub.1-4)alkyl or (C.sub.1-4)alkylphenyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent pyrrolidino or piperidino possess 5-HT.sub.3 -antagonistic activity.

Abstract: Novel ethers of formula ##STR1## their heteroaromatic N-oxides, and the pharmaceutically acceptable acid additions of the compounds of formula (I) and their N-oxides possess 5-HT.sub.3 -antagonistic activity. In the formula ##STR2## represents an optionally substituted heteroaryl group containing a hetero atom X and --B represents a saturated azabicyclic ring such as quinuclidyl or tropanyl.

Abstract: The invention concerns a compound formula II ##STR1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are the same or different and represent hydrogen, or loweralkyl, cycloalkyl or lower aralkyl, any of which radicals may be substituted by lower alkyl, lower alkoxy or CF.sub.3 or phenyl radicals which may be substituted by lower alkyl or CF.sub.3 or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered saturated ring R.sup.4 and R.sup.5 may also represent lower alkoxy, or cycloalkoxy, n is 1, 2, or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different with the provisos that (1) when R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are all hydrogen, R.sup.6 R.sup.7 are not both hydrogen, (2) when R.sup.1 and R.sup.3 are both phenyl and when R.sup.1 is methyl and R.sup.4 is methyl then R.sup.6 and R.sup.7 are not both methyl, and (3) when R.sup.1 is hydrogen or methyl, R.sup.

Abstract: The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; n is 1,2,3,4 or 5; R.sup.1 hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; R.sup.2 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl or 2- or 3-pyrazinyl; R.sup.3 and R.sup.4 are, independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.

Abstract: Pyridyl ethers of formula ##STR1## [where R is hydrogen, or 1 to 4 hydroxy, alkyl, alkoxy, amino, alkylamino, dialkylamino, halogen, trifluoromethyl, phenyl, halophenyl, alkyphenyl, alkoxyphenyl, carboxy, carboxamide, nitro, thiol or alkylthio substituents and B is quinuclidyl or tyopanyl] are useful for the treatment of conditions which respond to antagonism of 5 - HT.sub.3 receptors e.g. the treatment of migraine, emesis, anxiety, gastro-intestinal disorders and psychotic disorders.