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: Novel .alpha.-phenyl-2-(aza)benzothiazolylthioglycolic acids, derivatives thereof and pharmacologically acceptable salts thereof are disclosed, as well as their use as intermediates in the preparation of 2-substituted-3-hydroxy-thiazolo[2,3-b]-benzothiazolium salts, 2-substituted-thiazolo[2,3-b]benzothiazol-3(2H)-one mesoionic didehydro derivatives, 2-substituted-thiazolo[2',3'-2,3]thiazolo[5,4-b]pyridin-3(2H)-one mesoionic didehydro derivatives and related compounds, and their use as modulators of the immune response.

Abstract: There are disclosed compounds having the formula ##STR1## wherein X is a group selected from ##STR2## Y represents a single or double bond; R.sup.1 is hydrogen or lower alkyl;n is an integer 2-4;n' is an integer 1-2; andR is 2-pyrimidinyl, 2-pyridinyl, 2-pyrazinyl, halo-substituted 2-pyrazinyl, 5-tetrazolyl, phenyl or phenyl substituted by halo, lower alkyl or lower alkoxy;and the pharmacologically acceptable salts thereof, which exhibit anti-hypertensive activity.

Abstract: There are disclosed compounds of the formula ##STR1## wherein X is --O--, --S-- or ##STR2## Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR3## m is 1-3; A is O or NR.sup.2 ;B is OR.sup.2 ; SR.sup.2 or N(R.sup.2).sub.2 ;R.sup.1 is hydrogen, loweralkyl, loweralkoxy or halo;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.

Abstract: A method for the elaboration of large quantities of Bordetella pertussis protective antigens useful in the production of acellular vaccines for prevention of whooping cough.

Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, trifluoromethyl or halo;R.sup.2 is hydrogen, trifluoromethyl or halo; andR.sup.3 is hydrogen, nitro or carboxy;which possess lipoxygenase and cyclo-oxygenase inhibitory activity, making them useful as anti-inflammatory agents and which also possess analgesic activity.

Abstract: The invention concerns benzoquinolizines of general 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 hydrogen or lower alkyl and R.sup.4 represents a heterocyclic radical attached to the SO.sub.2 group through a carbon atom of the heterocyclic ring. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.

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: There are disclosed compounds of the formula ##STR1## wherein X is O, S or NHR.sup.3, wherein R.sup.3 is hydrogen, lower alkyl or cycloalkyl;R is loweralkyl, loweralkoxy, aralkoxy of up to 10 carbon atoms or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are, independently, hydrogen, lower alkyl, cycloalkyl or aminoalkyl; or R is alkoxymethyl or hydroxymethyl;n is one of the integers 2, 3 or 4;R.sup.1 and R.sup.2 are, independently, hydrogen, halo, nitro, cyano, SCH.sub.3, or NR.sup.6 R.sup.7, NHCOR.sup.6, COOR.sup.6, OR.sup.6 or SO.sub.2 NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 are independently hydrogen or loweralkyl;and their activity as anticonvulsants, having use in the treatment of epileptic conditions.

Abstract: Compounds of the formula: ##STR1## wherein A is ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, lower cycloalkyl, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, loweralkyl-sulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro;X and Y are each, independently, hydrogen or ##STR3## wherein R.sup.1 is hydrogen or lower alkyl;R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a heterocyclic moiety selected from 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl, with the proviso that one of X and Y is always hydrogen;n is 1-4;and the pharmacologically acceptable salts thereof, which are intermediates in preparing H.sub.

Abstract: The invention concerns pharmaceutical compositions containing a novel oxazole derivative, calcium oxaprozin. The formulations may be for oral or other use. The oral formulations are more palatable than those containing oxaprozin itself.

Abstract: Fused carbocyclic ring derivatives of pyridine which contain a nitrile or thioamide group on the carbocyclic ring e.g. 8-cyano or thiocarboxamido-5,6,7,8-tetrahydroquinolines are prepared by a process in which a sodium, potassium, lithium or magnesium halide derivative of the pyridine compound is treated with a compound RaRbNCN wherein Ra and Rb are the same or different and represent alkyl, cycloalkyl, or aralkyl, or Ra and Rb are joined to form a heterocyclic ring with the nitrogen, and the product is treated with a proton source to obtain the nitrile which is optionally treated with a sulphurizing agent to form the thioamide. The nitriles or thioamides may be isolated as their acid addition salts.

Abstract: There are disclosed compounds of the formula ##STR1## wherein X is OR.sup.2, SR.sup.2, N(R.sup.2).sub.2 or halo;W is --CH.sub.2 --, ##STR2## Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, ##STR3## m is 0-6; n is 0-6;p is 1-3;A is O or S;B is OR.sup.2, SR.sup.2 or N(R.sup.2).sub.2 ;R.sup.1 is hydrogen, loweralkyl, loweralkoxy or halo;R.sup.2 is hydrogen or loweralkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like.

Abstract: The invention concerns benzoquinolizines of general formula ##STR1## and their pharmaceutically acceptable acid addition salts. In formula (I), R represents hydrogen or lower alkyl, 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 and R.sup.4 which may be the same or different each represents lower alkyl, halo(lower)alkyl or aryl and A represents a lower alkylene group having 1 to 3 carbon atoms in the chain between the two N atoms. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.

Abstract: The invention provides a sustained release pharmaceutical composition comprising a mixture of micronized indoramin or a pharmaceutically acceptable salt thereof, a water-channelling agent, a wetting agent and a disintegrant, the mixture being in the form of a non-compressed pellet and having an enteric coat or a sustained release coat permeable to gastrointestinal juices. Sustained release capsules are also provided comprising a plurality of the aforementioned pellets.

Abstract: .alpha.-Mercaptobenzylacetic acid derivatives of imidazole-containing compounds and analogues thereof, and their use as immunomodulating agents are disclosed.

Abstract: Compounds of the formula: ##STR1## wherein B is a moiety having the formula: ##STR2## R is mono- or dihalo, amino, nitro, cyano, hydroxy, trifluoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, cycloalkyl of 4-7 carbon atoms, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, lower alkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro.X is SO.sub.2, SO, S or C.dbd.O; andA is amine selected from the group ##STR3## , wherein R.sup.1 is hydrogen or R.sup.2 CH.sub.2 wherein R.sup.2 is mono- or diloweralkylamino, mono- or di-N-lower alkylaminoloweralkyl, (2-furyl)methylamino, benzylamino, lowercycloalkylamino, 1-pyrrolidinyl, 1-piperidinyl, 1-hexahydroazepinyl, 1-octahydroazocinyl, 3-thiazolidinyl, 4-morpholinyl or 4-thiomorpholinyl; R.sup.3 is hydrogen or (1-piperidinyl)methyl with the proviso that when R.sup.

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: 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: There are disclosed mammalian vaccine compositions comprising an inactivated whole or subunit vaccine or toxoid and an adjuvant having the formula ##STR1## wherein R is hydrogen or lower alkyl, R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, R.sub.2 is hydrogen, chloro or nitro, n is 1 or 2 and pharmaceutically acceptable salts thereof.