Abstract: The invention concerns benzoquinolizines of formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents methyl or ethyl, A represents a direct bond between the S and N atoms or a lower alkylene group having 1 to 3 carbon atoms in the chain between the S and N atoms, R.sup.4 and R.sup.5 each independently represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or together with the nitrogen atom to which they are attached represent a five or six membered heterocyclic ring. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity and can be incorporated into pharmaceutical compositions.
Abstract: Morpholine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts possess analgesic and/or opiate antagonistic activity. In the formula R.sup.1 represents lower alkyl; R.sup.2 represents hydrogen, lower alkyl or (lower)alkoxymethyl; R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R.sup.4 represents a lower alkenyl or lower alkynyl group containing at least 3 carbon atoms and in which there is no unsaturated bond in the 1-position.
Abstract: The invention concerns benzoquinolizines of formula ##STR1## and their pharmaceutically acceptable acid addition salts. In the formula, R.sup.1 and R.sup.2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents methyl or ethyl and R.sup.4 represents halo(lower)alkyl. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity and can be incorporated into pharmaceutical compositions.
Abstract: Pharmaceutical compositions containing meptazinol or a pharmaceutically acceptable acid addition salt thereof and ibuprofen or a pharmaceutically acceptable salt thereof are useful in treating pain in mammals.
Abstract: Novel N-(4-pyridyl)acetamide derivatives having the formula ##STR1## [where R.sup.1 and R.sup.2 are aryl or heteroarly (optionally linked together by a lower alkylene bridge) or one of R.sup.1 and R.sup.2 is aryl or heteroaryl and the other of R.sup.1 and R.sup.2 is lower alkyl or ar(lower)alkyl, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl] and their nontoxic acid addition salts are described. They are chemical intermediates for the preparation of 4-pyridinamine derivatives having the formula ##STR2## which show CNS activity and may be used as antidepressant drugs.
Abstract: The invention concerns a new anti-inflammatory agent calcium oxaprozin, its preparation and use in pharmaceutical formulations. Calcium oxaprozin is more palatable than oxaprozin itself.
Abstract: m-Hydroxyphenyl substituted compounds of formula ##STR1## where R is an organic radical and R.sup.1 is hydroen or an organic radical are prepared by dehydrohalogenating a compound of formula ##STR2## (where X is chlorine or bromine, and R and R.sup.1 have the above meanings). Preferred novel starting materials of formula (II) are of the formula ##STR3## (where R.sup.1 and X are as above, n is 2,3 or 4, R.sup.2 is hydrogen or lower alkyl and R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl(lower)alkyl or aryl(lower)alkyl).
Abstract: The invention concerns benzoquinolizines of formula ##STR1## and their acid addition salts. In the formula R.sup.7 is lower alkyl or a phenyl or naphthyl radical optionally substituted with specified substituents and R.sup.8 is methyl or ethyl. The compounds possess high .alpha..sub.2 (presynaptic) adrenoceptor antagonistic activity and a good .alpha..sub.2 /.alpha..sub.1 antagonistic selectivity.
Abstract: 2,3,4,10-Tetrahydro-3,3-dimethyl-10-phenylpyrimido[1,2-a]indol-10-ol and the pharmaceutically acceptable acid addition salts thereof are useful in treatment or preventing obesity in mammals. The compounds may be administered in pharmaceutical compositions, optionally with one or more vitamins.
Abstract: Thiazolotriazine derivatives having the formula I ##STR1## their pharmaceutically acceptable salts, pharmaceutically acceptable triazolotriazinium compounds containing the cation having formula II ##STR2## and their zwitterionic forms and pharmaceutically acceptable acid addition salts [where A is hydroxy whilst B is hydrogen or A and B together represent a direct bond; R.sup.1 is aryl; R.sup.2 and R.sup.3 are independently lower alkyl or ar(lower)alkyl] are novel compounds useful as anti-cancer agents.
Abstract: The invention concerns compounds of formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Ar represents an optionally substituted indolyl group; A represents a straight or branched chain alkylene or oxoalkylene group, each having 2-4 carbon atoms and R represents an optionally substituted aryl (including heteroaryl) group, which possess anti-hypertensive and psychotropic activity, and are useful in the treatment of high blood pressure or as anti-depressants.
Abstract: Guanidines of formula ##STR1## and their pharmaceutically acceptable acid addition salts, (wherein R.sup.1 and R.sup.2 each represents lower alkyl or trifluoromethyl and R.sup.3 and R.sup.4 each represents hydrogen or lower alkyl or R.sup.3 and R.sup.4 together represent dimethylene or trimethylene) are useful in treating or preventing diarrhoea in mammals or poultry. The compound, if desired, may be administered with one or more antimicrobial, adsorbent, anti-emetic, parasympatholytic or antihistaminic agents.
Abstract: The invention provides a compound of the formula I ##STR1## wherein Y is a heterocyclic radical of formula ##STR2## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkoxy, halogen, formyl, phenyl, phenylalkyl, halophenyl, or acetal [CH(OR.sup.4).sub.2 where R.sup.4 is lower alkyl or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, the dotted lines in formula V represent an optional double bond in one of the indicated positions, A is a saturated or unsaturated alkylene radical having from 1 to 6 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and R.sup.3 is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms and Z.sup.- is an anion, and acid addition salts thereof, with the provisos that (1) when more than one R.sup.1 radical is present in the molecule then the R.sup.
Abstract: The invention provides novel thiomorpholines of the formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts wherein n represents 0 or 1, R.sup.1 represents (lower)alkyl, R.sup.2 represents hydrogen or (lower)alkyl, R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R.sup.4 represents hydrogen, hydroxy, acyloxy or a protected hydroxy group, with the proviso that when n is 0, R.sup.4 is other than hydrogen. The compounds in which n is 0 and R.sup.4 is lower alkoxy, hydroxy or acyloxy are analgesics and/or opiate antagonists and the compounds in which n is 1 and R.sup.4 is hydrogen are hypotensives or anti-hypertensives. The other compounds of formula (I) are intermediates for the pharmacologically active compounds.
Abstract: The invention concerns 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 defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.
Abstract: The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinum radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
Abstract: The invention relates to a pharmaceutical composition comprising an anti-ulcer effective amount of a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl, or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or lower alkoxy, R.sup.2 represents hydrogen, chlorine or trifluoromethyl and n is 1 or 2, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable carrier.A method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula I is also disclosed. Some compounds of formula I are novel and within the scope of the invention.
Abstract: The invention concerns novel compounds of formula IX--A--S--Y (I)wherein X is a radical selected from imidazolyl, pyridyl, quinolyl, tetrahydropyridyl or piperidyl any of which may be substituted and Y is any of the above radicals or a pyridinium radical, A is alkylene of 1-6 carbon atoms. Most of the compounds are anti-ulcer agents but some have anti-hypertensive activity, e.g. where X is quinolyl. Methods of treating ulcers and anti-ulcer compositions are also described.
Abstract: Morpholine derivatives of the formula ##STR1## and their acid addition salts, wherein n represents 1, 2 or 3, R.sup.3 is alkyl of 1 to 10 carbon atoms, R.sup.4 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cyclo (lower)alkylmethyl and OR.sup.5 is hydroxy, acyloxy or a protected hydroxy group possess analgesic and/or opiate antagonistic activity or are useful as intermediates for other compounds of formula I possessing such activity.