Abstract: What is claimed is a process for preparing macropolycyclic polyamines of the formula ##STR1## where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description. These compounds are prepared by a novel improved process by reacting a cyclic amine of the formula ##STR2## with a compound of the formula X--A.sup.2 --Y or X--A.sup.3 --Y where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description and X and Y are a leaving group.

Abstract: The invention relates to novel (1,3,4)-oxadiazine derivatives of formula (I), to a process and intermediates for their preparation, and to their usefulness as pesticides, in particular as anthelminthics, insecticides, acaricides, and nematicides.

Abstract: The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.

Abstract: Compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form a seven-membered ring containing one optionally substituted nitrogen atom and one heteroatom selected from oxygen and nitrogen;D.sup.1 to D.sup.4 form a substituted six membered ring, optionally containing up to two nitrogen atoms;R is preferably at least one acid containing substituent;R* is is one or more groups chosen from H, Q-C.sub.1-6 alkyl, Q-C.sub.1-6 oxoalkyl, Q-C.sub.2-6 alkenyl, Q-C.sub.3-4 oxoalkenyl, Q-C.sub.3-4 oxoalkynyl, Q-C.sub.2-4 alkynyl, C.sub.3-6 cycloalkyl, Ar or Het;Q is H, C.sub.3-6 cycloalkyl, Het or Ar;R.sup.6 is preferably a basic nitrogen containing substituent;are inhibitors of platelet aggregation.

Abstract: An improved synthesis for preparing a tetraamido-macrocyclic ligand, such as 5,6-Benzo-3,8,11,13-tetraoxo-2,2,9,9-tetramethyl-12,12-diethyl-1,4,7,10 -tetraazacyclotridecane, H.sub.4, in greatly improved yield and in a commercially viable manner, comprising the steps of dissolving a quantity of a 1,2-bis(2-aminoalkanamido)benzene in a solution comprised of ethyl acetate and methylene chloride to yield a first reaction solution; dissolving a quantity of a malonyl dihalide in an ethyl acetate solution to yield a second reaction solution; adding the first reaction solution and the second reaction solution to a reaction vessel containing a third reaction solution comprised of refluxing ethyl acetate solution and an acid scavenger to form a reaction mixture; and isolating a solid product comprised of the tetraamido-macrocycle directly from the reaction mixture by filtration.

Abstract: 9,10-DIAZATRICYCLO[4,4,1,1.sup.2,5 ]DECANE (la) AND 2,7-DIAZATRICYCLO[4,4,0,0.sup.3,8 ]DECANE (1b) DERIVATIVES HAVING ANALGESIC ACTIVITY.

Abstract: Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH.sub.2, CH--halogen, CH--N.sub.3, or C.dbd.CH.sub.2 ;Q and U are independently selected from: O, S, and CH(R.sub.a) wherein R.sub.a is hydrogen, OH, halogen, N.sub.3, NH.sub.2, SH, carboxyl, C.sub.1-6 alkyl or R.sub.a is CH.sub.2 (R.sub.b) wherein R.sub.b is hydrogen, OH, SH, NH.sub.2, C.sub.1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond;Z is selected from: O, a C.sub.1-6 alkoxy, a C.sub.1-6 thioalkyl, a C.sub.1-6 aminoalkyl, (CH.sub.2).sub.m wherein m is 0 or an integer, and N(R.sub.c).sub.2 wherein both R.sub.c are independently hydrogen or a C.sub.1-6 alkyl; andR2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.

Abstract: The novel compounds of the present invention are .beta.-octafluoro-meso-tetraarylporphyrins of formula (I) and their metallic complexes of formula (II): ##STR1## .beta.-octafluoro-meso-tetraaryl porphyrins are synthesized by reacting 3,4-difluoropyrrole with an aromatic aldehyde in the presence of boron trifluoride etherate, followed by oxidation. The difluoropyrrole used in this reaction is produced by reacting 3,3,4,4-tetrafluoropyrroline or its corresponding salt, 3,3,4,4-tetrafluoropyrrolidinium salt, with a base such as potassium tert-butoxide. The metalloporphyrins of the present invention are synthesized by deprontonating .beta.-octafluoro-meso-tetraarylporphyrin ligands and treating said ligands with metal ions.

Abstract: A pyrimidine of formula (I) ##STR1## and its pharmaceutically acceptable acid addition salts are useful as analgesics, as anticonvulsants or in the treatment of irritable bowel syndrome or bipolar disorder.

Abstract: The present invention relates to novel pyrazine compounds and their use in the regulation of haematopoiesis, in particular in the stimulation of haematopoiesis, and in the treatment of bacterial, viral and fungal diseases.

Abstract: The present invention is relative to 1,2-dialkynylated compounds, especially dialkynyl-1,2-diones, a method of their production and their use as synthetic structural units to produce NIR dyes, pigments, thermostable polymers, charge-transfer complexes, heterocycles or pharmaceuticals.

Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R' represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.1 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; X represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.

Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I) ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester, acyloxyamide, or imide thereof. Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: The synthesis of novel compound (I) is described: 5-bromo-2-iodopyrimidine may be used for the synthesis of a range of chemical compounds both known and novel. The synthesis of a number of novel liquid crystalline compounds is described.

Abstract: Disclosed are enantiomers diastereomers, salts, solvates, hydrates and mixtures thereof, of formula I: ##STR1## The core moiety is non-cyclic or at least one five- to seven-membered ring, n is an integer from about 4 to about 16, R.sub.1 and R.sub.2 are hydrogen, halogen or C.sub.1-12 alkyl or alkenyl, and (CH.sub.2).sub.n may be substituted by a hydroxyl, halogen, oxygen, a (C.sub.1-4) alkyl group or a dimethylamino group. The compounds and pharmaceutical composition thereof are useful in methods for treating an individual having a disease or treatment-induced toxicity, mediated by second messenger activity.

Abstract: The present invention relates to novel affinity ligand-matrix conjugates comprising a ligand with the general formula (a) ##STR1## which ligand is attached to a support matrix in position (A), optionally through a spacer arm interposed between the matrix and ligand. The invention furthermore relates to these novel affinity ligand-matrix conjugates and the preparation and use thereof in the purification of proteinaceous materials such as e.g. immunoglobulins, insulins, Factor VII, or human Growth Hormone or analogues, derivatives and fragments thereof and precursors.

Abstract: The invention relates to new porphyrin complex compounds, pharmaceutical agents that contain the latter, and the use of porphyrin complexes for the production of agents for photodynamic therapy and MRI diagnosis.

Abstract: A process for the preparation of tetraazamacrocycles of general formula (I) ##STR1## wherein n, p and q can independently be 0 or 1, comprising the following steps:a): condensation of polyamines with a glyoxal derivative;b): condensation of the resulting compound with an alkylating agent;c): oxidation of the resulting compound with an oxidizing agent, to give a mixture of oxidated products which is submitted tod): hydrolysis in acid aqueous solution, to give the compound of formula (I).

Abstract: The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.Compounds of the formula (I): ##STR1## wherein R.sup.1 to R.sup.10 and X are as defined in the Specification and useful as hypolipidemic compounds.

Abstract: The invention also discloses compounds and pharmaceutically acceptable salts having the generic formula (2) ##STR1## wherein X and Y may be the same or different and are selected from the group consisting of OH and NH.sub.2 ; wherein Z is one of either nitrogen or carbon and Q is one of either nitrogen or carbon but when Z equal nitrogen, Q does not equal nitrogen and when Q equals nitrogen, Z does not equal nitrogen; wherein A is selected from the group consisting of nitrogen, carbon and sulfur and B equals carbon when A is selected from the group consisting of sulfur, carbon, and nitrogen, B equals nitrogen when A equals carbon and B equals sulfur when A equals carbon; wherein R.sub.3 is one of either hydrogen or methyl except where Z is nitrogen wherein R.sub.3 is zero; wherein R.sub.4 is one of either a hydrogen or a first lower alkyl group except when A equals sulfur wherein R.sub.4 is zero; wherein R.sub.