Abstract: A multistep process for producing 8-chloro-6-(2-fluorophenyl)-1-methyl-4-H-imidazo?1,5a!?1,4! benzodiazepine (midazolam) comprises treating a compound of Formula II with a lower alkyl dithiol to produce a compound of Formula III, wherein n=2 or 3, converting the compound of Formula III to a compound of Formula VII, and then treating the compound of Formula VII with a deprotecting agent, thereby producing midazolam. Novel intermediate compounds are also disclosed.

Abstract: A process for the asymmetric hydrogenation of a compound of the formula ##STR1## wherein each R, independently, is alkyl, arylmethyl, aryl, alkoxy, arylmethoxy or aryloxy or both R's, taken together, are methylene, ethylene or 1,2-phenylene and n is 1,2 or 3,or of a salt thereof to a compound of the formula ##STR2## in the form of an (S) or (R) enantiomer, wherein R and n have the significances given above, using an optically active ruthenium-diphosphine complex as catalyst, is described. The preparation of the compounds of formula II, as well as the compounds of formula II, which form a further object of the invention, are also described.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6 ', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Benzazepine derivatives represented by the following general formula (I) useful as arginine vasopressin antagonists or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and difluorobenzazepinone derivatives represented by the following general formulae (II) and (III) which are useful as production intermediates of the compound (I).

Abstract: A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive.

Abstract: Provided are brefeldin A derivatives of the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 is H and the other of R.sub.1 and R.sub.2 is a substituent group having 1 to 12 carbon atoms containing a basic nitrogen atom or a quaternary ammonium group, or a salt thereof. These derivatives exhibit good antitumor activity, and are administrable to human patients without the problems associated with brefeldin A.

Abstract: Novel piperidine-triazine compounds of the formula (Ia) and (Ib) suitable for use as light stabilisers, heat stabilisers and oxidation stabilisers for organic materials. The meanings of R.sub.1, R.sub.2, R.sub.3, G.sub.1, G.sub.2, L.sub.1, L.sub.2, m and n are defined in the text.

Abstract: Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q is a single bond or ##STR3## and Z, A, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.6 are as defined herein.

Abstract: A novel process for preparing clonidine derivatives has been discovered which is shorter, less expensive and safer than previously known methods. A new thiourea complex has also been discovered which can be directly cyclized to produce the corresponding heterocyclic product.

Abstract: There is provided a 1-(3-heterocyclylphenyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.

Abstract: Novel process for the preparation of 2,2,6,6-tetramethyl-4-piperidyloxy-1,3,5-triazines, based on the reaction of cyanuric chloride with C.sub.1 -C.sub.4 alkanols or with sodium or potassium C.sub.1 -C.sub.4 alkoxides and subsequent reaction with 2,2,6,6-tetramethyl-4-piperidinols in the presence of a transesterification catalyst.The various reactions can be carried out in the same reactor, without isolation of the intermediates.

Abstract: Compounds structurally related to ethacrynic acid are described. The compounds are useful for controlling intraocular pressure. Unlike ethacrynic acid, the compounds of the present invention are capable of effectively penetrating the cornea. Methods of controlling intraocular pressure via topical application of one or more of the compounds to the eye and topical ophthalmic compositions useful in the treatment of glaucoma are also described.

Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation, and uses of the pharmaceutical products based on these compounds. The substituted benzenesulfonylureas and -thioureas are of the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 E, and y are as defined in the specification. The compounds of formula I have antiarrhythmic activity.

Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: ##STR1## wherein R.sup.22 and R.sup.23 are allyl.

Abstract: The invention relates to new amino acid derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, wherein group R.sup.5 is ##STR2## and R.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, Z, t and u have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: N.sub.1 -(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: ##STR1## These compounds have patent antibacterial activities against a wide variety of infectious bacteria and are useful as antibacterial agents by oral or parenteral administration.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Disclosed is a method of combating Pneumocystis carinii Pneumonia in a subject in need of such treatment. The method comprises administering to to the subject an effective Pneumocystis carinii-combating amount of a bis-benzimidazole compound such as bis[5-(2-imidazolyl)-2-benzimidazolyl]methane, 1,4-bis[5-2-imidazolyl)-2-benzimidazolyl]butane, or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations for carrying out the method and novel compounds are also disclosed, along with methods of combating Giardia lamblia.

Abstract: Thrombin inhibitors are provided which have the formula ##STR1## wherein Z is a thrombin inhibitor substructure containing distal and proximal binding site residues; andR.sup.1 is cyano, hydroxyl, alkoxy, amino, aminoalkyl or nitro.

Abstract: The present invention relates to water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: 1) R.sup.1 and R.sup.2 represent independently, hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl;ii) R.sup.1 represents hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R.sup.2 represents --COR.sup.3,wherein:R.sup.3 represents hydrogen, lower alkyl, perhalo-lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy or lower alkoxy lower alkyl; oriii) R.sup.1 and R.sup.2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) ##STR2## wherein: Y represents O, S, SO, SO.sub.2, CH.sub.2 or NR.sup.4wherein:R.sup.

Abstract: The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl;Alk.sup.1 is a bivalent C.sub.

Abstract: Aminoketone-substituted coumarin sensitizers having tethered tertiary amino groups are described which have extremely good photosensitivity. The sensitizers of the instant invention have the formula: ##STR1## wherein R.sub.1 and R.sub.2 each represent an alkyl group having 1 to 6 carbon atoms, and R.sub.3 and R.sub.4 each represent hydrogen; or at least one of R.sub.1 and R.sub.3 or R.sub.2 and R.sub.4 together represent an alkylene group having 2 to 4 carbon atoms,R.sub.5 represents an alkyl group having 1 to 6 carbon atoms or H,R.sub.6 represents an alkylene group having 1 to 6 carbon atoms, andR.sub.7 and R.sub.8 each independently represent an alkyl group having 1 to 6 carbon atoms, both of R.sub.7 and R.sub.8 taken together represent an alkylene group having 4 to 6 carbon atoms, or R.sub.5 or R.sub.6 taken together with R.sub.7 or R.sub.8 represent a five, six, or seven membered heterocyclic ring group.

Abstract: Polymeric compounds comprising subunits of the following formulas ##STR1## wherein R.sub.1, X, x, y, z, x', y' and z' are as defined in the application. The polymeric compounds are capable of stimulating the immune response system of animals, including humans. The polymeric compounds are useful also in the manufacture of medicaments, including vaccines, for the prophalaxis and treatment of conditions requiring an enhanced immune response.

Abstract: Disclosed are a benzothiazolesulfonamide derivative represented by the formula (I) or a pharmaceutically acceptable acid addition salt thereof ##STR1## wherein A represents a lower alkylene group which is unsubstituted or substituted; R.sup.1 represents a hydrogen atom or a lower alkyl group; each of R.sup.2 and R.sup.3 independently represents a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 are bonded together to form a lower alkylene group which is unsubstituted or substituted; and R.sup.4 represents a hydrogen atom, a lower alkyl group, an amidino group, or a phenyl-substituted lower alkyl group, wherein the lower alkyl group is substituted or unsubstituted, and the phenyl group is unsubstituted or substituted with a lower alkyl group, a lower alkoxy group, a halogen atom or a methylenedioxy group;a method for preparing the same; and a pharmaceutical composition comprising the same.

Abstract: Novel piperidine-triazine compounds of the formula (Ia) and (Ib) suitable for use as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials. The meanings of R.sub.1, R.sub.2, R.sub.3, G.sub.1, G.sub.2, L.sub.1, L.sub.2, m and n are defined in the text.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.

Abstract: There are disclosed preparation and compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl or taken together are a --CH.sub.2 -- group to form a cyclopropane ring.X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are hydrogen or alkyl,p and q are independently either 0 or 1;R.sup.3 is alkyl, alkenyl, cycloalkyl, alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10 whereinR.sup.9 and R.sup.10 are hydrogen or alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, adamantyl, aryl, benzyl, diphenylmethyl, norbornyl, or taken together with the nitrogen to form 4 to 8 atom heterocyclic group, ##STR3## optionally substituted with alkyl groups; Ar is aromaticR.sup.4 is hydrogen or methyl;Z is --O--, --NH--, --N(lower alkyl), --S--, --SO--, --SO.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, CO, CO.sub.2, O.sub.2 C, --N.dbd.N--, --CH.dbd.N--, or --N.dbd.CH--,and n and m are 0, 1 or 2.

Abstract: Nitroinimo compound as intermediate for insecticides and pharmaceauticals of the formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different from each other and denote lower alkyl of 1 to 4 carbon atoms.

Abstract: New carbamazepine hapten analogues are described comprising:(A) an active ester group;(B) a carbamazepine nucleus; and(C) a linking chain (i) linking the carboxamide group of the carbamazepine nucleus to the active ester group, said linking chain having about 4 to about 40 atoms consisting of:(1) alkylene groups; and(2) 5 to 7 membered heterocyclic ring groups, each group being joined into the linking group through chemical groups selected from(a) esters,(b) amides,(c) hetero atoms selected from --0--, --S--, and --NR--; wherein R represents hydrogen or C.sub.1 to C.sub.6 alkyl; and(d) carbonyl groups.The carbamazepine-active ester analogues are useful in preparing labeled carbamazepines. The labeled carbamazepines are useful in immunoassay elements and processes for the detection of carbamazepine drugs, for example, in body fluids.

Abstract: Disclosed is a fused pyrimidine of the formula [I] ##STR1## wherein R.sup.1, R.sup.2, and R.sup.

Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.

Abstract: The present invention relates to novel substituted guanidine and amidine compounds, their preparation and their use in the kill and control of fungal organisms which infest plants.

Abstract: Amino-substituted benzoylguanidines, process for their preparation, their use as a medicament and medicament containing themBenzoylguanidines of the formula I ##STR1## are described in which R(1) or R(2) is an amino group --NR(3)R(4), where R(3) and R(4) are H or (cyclo)alkyl or R(3) is phenyl-(CH.sub.2).sub.p -- where p=0, 1, 2, 3 or 4, or phenyl, or R(3) and R(4) can also together be a methylene chain, and in which the other substituent R(1) or R(2) in each case is H, F, Cl, alkyl, alkoxy, CF.sub.3, C.sub.m F.sub.2m+1 --CH.sub.2 --, benzyl or phenoxy, and their pharmaceutically tolerable salts.The compounds according to the invention have very good antiarrhythmic properties, as occur, for example, in the case of oxygen deficiency symptoms.

Abstract: Compounds of formula I ##STR1## wherein Y, Z, S, S', m, n and R.sub.1 -R.sub.4 are as defined in the description, have valuable pharmaceutical properties and are effective especially against protozoal infections. They are prepared in a manner known per se.

Abstract: Disclosed is a sulfonamide derivative represented by following formula (I) and a medicine for the treatment of asthma comprising the sulfonamide derivative as an active ingredient which exhibits bronchodilation effect. ##STR1## wherein X represents a quinoline residue represented by formula (II) or an isoquinoline residue represented by formula (III) ##STR2## where R.sup.1 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, or ##STR3## where R.sup.2 is a hydrogen atom or a hydroxyl group, and wherein: when X is quinoline residue (II), n is zero or 1, in which,when n is zero, R.sup.4 is an unsubstituted or substituted diazacycloalkyl group, andwhen n is 1, R.sup.3 is a hydrogen atom or a lower alkyl group and R.sup.4 is an unsubstituted or substituted aralkylamino group or an unsubstituted or substituted diazacycloalkyl group; andwhen X is isoquinoline residue (III), n is 1, in which, R.sup.3 is a hydrogen atom or a lower alkyl group and R.sup.

Abstract: Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein X is S or --CH.sub.2 --; m is 0, 1 or 2 when X is --S-- or m is 0 when X is --CH.sub.2 --; n is 1, 2 or 3; R.sup.1 and R.sup.2 are independently H, lower alkyl, cyclo-alkyl, aryl, heteroaryl or heteroarylalkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 5- to 8-membered ring which may optionally contain an additional N, O or S atom in the ring; R.sup.3 is heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.

Abstract: Glycol aldehyde and lactic acid derivatives and their sulfur analogs of the formula I ##STR1## where R.sup.1 to R.sup.3 have the meanings given in the specification, X is oxygen, sulfur or a single bond, and Y is a C.sub.2 -C.sub.4 -alkylene or C.sub.2 -C.sub.4 -alkenylene chain where in each case a methylene group may be substituted by an oxo group (.dbd.O), environmentally compatible salts of the compounds I, methods of preparing the compounds I, and their use as herbicides.

Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.

Abstract: This invention concerns compounds of the formula I: ##STR1## wherein R.sup.1 is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)-alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R.sup.2 is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R.sup.6 is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R.sup.3 and R.sup.4 are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R.sup.5 is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.

Abstract: There are provided alkyl esters of 5-heterocyclic-pyridine-2,3-dicarboxylic acids useful as intermediates for the preparation of highly effective 5-heterocyclic-2-(2-imidazolin-2-yl)pyridine herbicidal agents and methods for the preparation thereof.

Abstract: The present invention relates to the derivatives of formula: ##STR1## as well as to their addition salts and to their use in therapy, in particular for the treatment of cardiovascular diseases, especially for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.

Abstract: The present invention relates to a novel method for stabilizing synthetic thermoplastic materials against thermal degradation, which comprises incorporating in said materials one or more compounds of the formula (I) ##STR1## in which R.sub.1 is unsubstituted or substituted phenyl, n is e.g. 1, 2 or 3, and, when n is 1, R.sub.2 is e.g. --COR.sub.3, --COOR.sub.4 or --CO-N(R.sub.5)R.sub.6 in which R.sub.3 is e.g. C.sub.4 -C.sub.17 alkyl, R.sub.4 is e.g. C.sub.4 -C.sub.18 alkyl, cyclohexyl or t-butylcyclohexyl, R.sub.5 and R.sub.6 which can be identical or different are e.g. C.sub.2 -C.sub.8 alkyl or cyclohexyl, and, when n is 2, R.sub.2 is e.g. --CO--R.sub.10 --OC, --COO-R.sub.11 --OOC-- or --CONH--R.sub.12 --NHCO- in which R.sub.10 is e.g. C.sub.2 -C.sub.8 alkylene, R.sub.11 is e.g. C.sub.4 -C.sub.6 alkylene and R.sub.12 is e.g. C.sub.4 -C.sub.6 alkylene, and, when n is 3, R.sub.2 is e.g. benzenetricarbonyl.Several compounds of the formula (I) are new.

Abstract: The imidazo[1,2-b]pyridazine compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterocyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.n (n=0 to 2), Alk is a straight or branched chain alkylene group containing 1-10 carbon atoms and optionally having substituent(s), or their pharmaceutically acceptable salts which possess antiallergic, anti-inflammatory and anti-PAF activities, and their production and use.

Abstract: A process is described for the preparation of compounds of the formula ##STR1## in which W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH-- or --CH.sub.2 Ch.sub.2 --Y is a saturated heterocyclic amino group, andR.sup.2 is substituted or unsubstituted phenyl-, thienyl- or naphthyl-alkyl, or cinnamyl,and their salts and solvates.The process comprises hydrolysing a corresponding ester, amide, nitrile or ortho-ester. The starting materials are preferably prepared by reducing the corresponding cyclopentanone and hydrolysis can take place simultaneously with reduction.

Abstract: Compounds of the formula ##STR1## in which R.sup.1, R.sup.2, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 have the following meaningsR.sup.1 and R.sup.2 designate optionally substituted aryl, or an optionally substituted heterocyclic radical which contain 1 or 2 five-, six- or seven-membered rings at least one of which contains 1, 2 or 3 hetero atoms from the series comprising O, N and S which has a C.dbd.C in conjugation with the C.dbd.C bond in the five-membered ring of III,X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 designate O, S, NR.sup.5, or X.sup.1 and Y.sup.1 or X.sup.2 and Y.sup.2 in each case form parts of a fused-on heterocyclic five-membered or six-membered ring,processes for their preparation and their use as dyestuffs and pigments.

Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.

Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p -, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p - or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p - (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.

Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.

Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.