Abstract: The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl;R.sup.2 and R.sup.3 together form --A.sup.2 --X.sup.2 --A.sup.3 -- which defines a ring having 5 or 6 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio or imino;Ar is optionally substituted phenylene;R.sup.4 is (1-4C)alkyl, fluoro-(2-4C)alkyl or optionally substituted phenyl or a heterocyclic moiety;R.sup.5 is hydrogen or (1-4C)alkyl; andR.sup.6 is hydrogen, halogeno, trifluoromethyl, (1-4C)alkyl or (1-4C)alkoxy;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.

Abstract: A purification method of intermediates for the preparation of Diltiazem which consists of the crystallization of a mixture enantiomerically enriched in (2S,3S)-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H) -one is described.

Abstract: Polycyclic diamines, incorporating a basic framework similar to [3.3.3]propellane, and derivatives of the basic polycyclic diamines and a process for preparing same are provided. The diamines are prepared by subjecting bispyridine compounds to electroreductive coupling in an acidic solution. The polycyclic diamines and derivatives thereof are useful as chain extenders, crosslinking agents and curatives in various polymer systems.

Abstract: Halo-displacement reaction products of aliphatic hydroxy compounds and chloro- or bromo-substituted aromatic nitrogen-heterocyclic compounds are conducted under alkaline conditions in the presence of a phase transfer catalyst, in the substantial absence of water inorganic salts other than those formed in the reaction. The method is particularly useful for the preparation of substituted chlorotriazines. In a preferred embodiment, the reagents constitute at least about 25% by weight of the organic phase of the reaction mixture.

Abstract: Polycyclic diamines, incorporating a basic framework similar to [3.3.3]propellane, and derivatives of the basic polycyclic diamines and a process for preparing same are provided. The diamines are prepared by subjecting bispyridine compounds to electroreductive coupling in an acidic solution. The polycyclic diamines and derivatives thereof are useful as chain extenders, crosslinking agents and curatives in various polymer systems.

Abstract: A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a linking structure comprising an alkyl chain containing two nitrogen atoms. This linking structure is represented by ##STR1## [wherein A is --(CH.sub.2).sub.n --, --CO-- or --O--(CH.sub.2).sub.m --; each of R.sup.1 and R.sup.2 is independently a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.1 and R.sup.2 may be so linked with each other as to make an alkylene chain and thus form a heterocyclic structure; R.sup.5 is a halogen atom, a hydroxyl group, a lower alkyloxycarbonyl group, a lower alkyloxy group which may be substituted by a lower alkyloxy group, or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.5 may be so linked with R.sup.1 as to make an alkylene chain and thus form a heterocyclic structure; n is 0, 1, 2 or 3 (when R.sup.5 is the hydroxyl group, n.noteq.

Abstract: Substituted quinazolinones and pyridopyrimidines of structural formula 1 ##STR1## are angiotensin II antagonists useful in the treatment of disorders related to the renin-angiotensin system (RAS) such as hypertension, congestive heart failure, ocular hypertension and certain CNS disorders.

Abstract: Benzamide derivatives of the following formula (I) ##STR1## [wherein R.sup.1 : ##STR2## B, D: hydrogen atom, etc. E: pyridyl group, etc.n: integer from 0 to 2R.sup.2 : R.sup.3 R.sup.4 N-- etc.(R.sup.3,R.sup.4 : optionally substituted C.sub.6 -C.sub.14 aryl group, etc.)A; ##STR3## --CH.sub.2 --, --N.dbd.N--, --CH.dbd.N--, --N.dbd.CH--, --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --].Optical antipodes thereof or pharmaceutically acceptable salts thereof, show excellent PAF antagonism and are effective for therapy and prophylaxis of diseases caused by PAF (bronchial asthma, nephritis, shocks, cardiac infarction, cerebral hemorrhage, ulcer, DIC, autoimmune diseases, thrombosis, etc.).

Abstract: This invention relates to a process for preparing synergistic derivatives of formula (I), in which Y is hydrogen or dimethylamino, from pristinamycin I.sub.A or from virginiamycin, via a Mannich base, followed by elimination of the amine introduced.

Abstract: Amelinic compounds of general formula (I) ##STR1## obtained by condensation of 1 mol of cyanuric acid halide with 2 mols of an amine and subsequent hydrolysis of the intermediate thus obtained. Compounds of general formula (I) are used, in particular, as flame retardant additives for polymers.

Abstract: This invention relates to intermediates and processes thereto, for the preparation of 5,6-dihydropyrro[2,3-d] pyrimidines which are useful for the treatment of susceptible neoplasms.

Abstract: The invention concerns a heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted quinoxalinyl or a hydrogenated derivative thereofX.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 4 to 7 ring atoms, wherein A.sup.2 and A.sup.3, which may be the same or different, each is (1-4C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.

Abstract: The present invention relates to bisguanidine derivatives of the formula I ##STR1## where R.sup.1 and R.sup.2 are each, independently of one another, hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, haloalkenyl; or cycloalkyl which has 5-12 carbon atoms in the ring and may be substituted, or benzyl which may be substituted, with the proviso that only one of R.sup.1 and R.sup.2 can be hydrogen; orR.sup.1 and R.sup.2 are, together with the atoms which they substitute, a heterocyclic ring which may be substituted;X is CH.sub.2, O, a single bond, NH, N-alkyl or N-benzyl whose phenyl ring may be substituted,n is 5 to 8,and their plant-compatible acid addition salts and their metal complexes and fungicides containing these compounds.

Abstract: The invention concerns a heterocyclic cyclic ether of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 and R.sup.2 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the oxygen atom to which A.sup.2 is attached and with the carbon atom to which A.sup.3 is attached, defines a ring having 5 to 7 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino, and which ring may bear one, two or three substituents; andR.sup.

Abstract: The present invention involves, in addition to many unique substituted sapphyrins, a novel method for synthesizing sapphyrins with good efficiency and high yield. An improved 9-step synthesis of substituted sapphyrins, e.g., the two C.sub.2 symmetric sapphyrins, compounds 2 and 4 of FIG. 1C, is described herein. This synthesis involves as an important step the condensation between a tripyrrane diacid and a diformyl bipyrrole. The key tripyrrane component is prepared in three high-yield steps from readily available pyrrolic precursors and the bipyrrole portion is prepared in four steps from ethyl 3-methyl-4-methylpyrrole-2-carboxylate in roughly 33% yield overall.

Abstract: A compound with immunosuppressive properties having formula (I), in which R.sup.1 represents a heterocyclic ring system, a combined heterocyclic ring system and homocyclic ring system, or an ethoxycarbonylmethyl group. R.sup.2 and R.sup.3 represent hydrogen or lower alkyl groups.

Abstract: Compounds of formula I, and pharmaceutically acceptable salts thereof, ##STR1## in which R1 is hydrogen (1-6C)alkyl or (1-4C)alkanoyl;A is --N.dbd.CQ--O--, N.dbd.CQ--NR.sup.8 --, --N.dbd.CQ--CH.dbd.N--or --N.dbd.CH--CQ.dbd.N--;Q is 2-furyl;R.sup.8 is hydrogen or C1-4C)alkyl;and R.sup.2 has any of the meanings given in the specification, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H.sub.2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H.sub.2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H.sub.2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.

Abstract: A compound of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, halogen, nitro, amino, protected amino, hydroxyamino, lower alkyl, hydroxy, protected hydroxy, sulfamoyl, carboxy, protected carboxy, mercapto, optionally substituted heterocyclic-carbonyl, optionally substituted heterocyclic-(lower)alkyl, lower alkylthio, hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.3 is aryl which may have suitable substituent(s), andA is lower alkylene,or pharmaceutically acceptable salts thereof.

Abstract: .alpha.-Fluoro-substituted N-acryloylamino acid derivatives of the formula ##STR1## are used to make polymers optionally for chromatographic resolution of racemates into their enantiomers. The fluorine atom improves performance in many instances.