Abstract: Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## ?wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, Y is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!.

Abstract: A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.

Abstract: A class of 1,2,3,6-tetrahydropyridine derivatives, substituted in the 4-position by a fused bicyclic heteroaromatic moiety and in the 1-position by an optionally substituted benzyl moiety, are ligands for dopamine receptor subtypes within the body, in particular the D.sub.4 subtype, and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia or depression.

Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.

Abstract: The object of this invention is to provide novel buprenorphine analgesic analogues represented by following formula(I) and their non-toxic pharmaceutically acceptable salts. ##STR1## wherein R.sub.1 is hydrogen atom, methyl, ethyl, cyclopropyl or cyclobutyl; andR.sub.2 is cyclopropyl or cyclobutyl.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract: This application relates to a process for preparing quinacridones whereby the corresponding dihydroquinacridone is oxidized by subjecting a paste containing the dihydroquinacridone and an oxidizing agent to a high shear force mixing step.

Abstract: New camptothecin derivatives of the general formula (1): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.2 represents a hydrogen or a C.sub.1 -C.sub.6 alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, C.sub.2 -C.sub.6 acyloxy or methoxyethoxymethoxy group, R.sup.4 represents a hydrogen or halogen atom, and R.sup.5 represents a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 unsaturated alkyl, alkylthioalkyl, alkoxyalkyl, pyridyl or substituted phenyl group, with the proviso that all of the R.sup.2, R.sup.3 and R.sup.4 substituents should not be a hydrogen atom, and a process for preparing the new camptothecin derivatives by subjecting the camptothecin derivatives of the general formula (2): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.

Abstract: A series of 4-O & 5-aminomethylation of synthetic capsaicin derivatives selectively reveal antagonist activity on capsaicin-sensitive sensory neurons, and inhibit its innervating atrium, airway, and ileum smooth muscles in vitro. The compound of this invention has the following formula ##STR1## wherein R is a member selected from the group consisting of ##STR2## wherein R.sub.1 is a member selected from the group consisting of C.sub.1-12 alkyl, C.sub.1-12 alkenyl, C.sub.1-12 alkylene, and C.sub.1-12 alkenylene, andwherein R.sub.2 is a member selected from the group consisting of H, C.sub.1-3 alkylene-NR.sub.1 R.sub.1, and C.sub.1-6 alkenylene-NR.sub.1 R.sub.1.

Abstract: 9-Amino camptothecin of formula (I) ##STR1## is prepared by: 1) reducing a compound of formula (II): ##STR2## wherein Hal is 10- or 12-halogen, in a single step to the 9-amino-camptothecin of formula (I) or, alternatively, 2a) reductively removing the Hal group from a compound of formula (II) so obtaining the compound of formula (III): ##STR3## and 2b) reducing the compound of formula (III) so obtaining the 9-amino camptothecin of formula (I); the said steps 1 and 2a) and, optionally, step 2b) each being carried out in the presence of a catalytic amount of a compound of formula PdL.sub.2 wherein L is acetate or halogen and, additionally, in the presence of an ammonium formate as a hydrogen source. The 9-amino camptothecin of formula (I) is useful as inhibitor of the enzyme topoisomerase I. It is useful in the treatment of cancers, in particular leukaemia, colon and rectal tumours.

Abstract: An N-?2-(1-hydroxyethyl)-3-oxopropyl!amine compound of the formula ?III!: ##STR1## wherein Ring B represents a benzene ring which may be substituted; W represents oxygen atom or sulfur atom; Y represents oxygen atom, sulfur atom or N R.sup.0, R.sup.0 represents hydrogen atom or a substituent; Z represents a substituted methylene group which contains at least one chiral center; R.sup.5 represents an aralkyloxycarbonyl group or an alkoxycarbonyl group; R.sup.6 represents hydrogen atom, an aralkyl group, an acyloxy group, a tri-substituted silyloxy group or an alkoxy group; or both of R.sup.5 and R.sup.6 bond at their termini and combine with the adjacent nitrogen atom to form phthalimido group, and a process thereof are disclosed. Said compound ?III! is useful as a starting compound of .beta.-lactam antibacterial agents.

Abstract: The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (A) or (B) wherein X, W, Z, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.

Abstract: A process for producing 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester having a high purity from 1,4-cyclohexanedione-2,5-di(carboxylic acid alkyl ester) at high yields for a short period of time; a process for producing quinacridone of which the byproduct content is small, from the above 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester; and a process for producing quinacridone of which the particle diameter is adjusted as desired, from the above 2,5-di(arylamino)-3,6-dihydroterephthalic acid dialkyl ester without adding a step of forming a pigment.

Abstract: Compounds of the formula ##STR1## in all possible racemic, enantiomeric and diastereoisomeric forms and their non-toxic, pharmaceutically acceptable salts with acids and bases having antagonistic properties for angiotensin II receptors and a process and novel intermediates for their properties.

Abstract: Method for the preparation of 1,3-oxazolidin 5-carboxylic acid having the general formula (I) ##STR1## from a product having the general formula (II) ##STR2## In the general formulas (I) and (II), Ar is an aryl radical, R.sub.1 is a benzoyl radical or a radical R.sub.2 --O--CO-- wherein R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, Ph is an optionally substituted phenyl radical, X is the residue of an optically active organic base or an alkoxy radical optionally substituted by a phenyl radical. The acids of formulas (I) and (II) are particularly useful in preparing taxol, Taxotere or analogs thereof which have remarkable antitumor and antileukemia properties.

Abstract: Novel methods for the preparation of sidechain-bearing taxanes, comprising the preparation of an oxazoline compound, coupling the oxazoline compound with a taxane having a hydroxyl group directly bonded at C-13 thereof to form an oxazoline sidechain-bearing taxane, and opening the oxazoline ring of the oxazoline sidechain-bearing taxane so formed. Novel compounds prepared by the methods of the present invention are also provided.

Abstract: The present invention relates to new camptothecin derivatives which display antitumor activity. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.

Abstract: The invention relates to new azatrioxaspiroalkenes of the formula (I) ##STR1## in which Ar.sup.1 and Ar.sup.2 are identical or different and independently of one another in each case represent optionally substituted aryl, to processes for their preparation, to new intermediates, and to the use of the azatrioxaspiroalkenes of the formula (I) as pesticides.

Abstract: Quinoline-3-carboxamides I ##STR1## where R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, and the organic radicals may be substituted or unsubstituted;R.sup.2 is hydrogen, hydroxyl, alkoxy, alkenyloxy, dialkylamino, alkyl, alkenyl, alkynyl, cycloalkyl, and the organic radicals may be substituted or unsubstituted;orR.sup.1, R.sup.2 together denote an alkylene chain of 4 to 7 members and which may be interrupted by oxygen, sulfur or N-methyl;R.sup.3 -R.sup.6 are hydrogen, alkyl, alkoxy, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, halogen, cyano or nitro;X is oxygen or sulfur;with the proviso that R.sup.2 is not hydrogen, C.sub.1 -C.sub.3 -alkyl, n-butyl, 3-methylbutyl, cyclohexyl, hexyl, heptyl, octyl, 2-chlorobenzyl, 3-(dimethylamino)propyl, 3-(diethylamino)propyl, 2-morpholinoethyl or 2-(3,4-dimethoxyphenyl)ethyl when R.sup.1 and R.sup.3 to R.sup.6 are hydrogen and X is oxygen, and that R.sup.2 is not benzyl when R.sup.1 is methyl, R.sup.3 to R.sup.6 are hydrogen and X is oxygen, and that R.

Abstract: A process for producing isatoic anhydrides of the formula (II): ##STR1## which comprises reacting an anthranilic acid of formula (I): ##STR2## or a salt thereof with phosgene using a mixed solvent of water and an organic solvent miscible with water and inert to the reaction; conducting the reaction in the coexistence of an alkylpyridinium salt in an aqueous solvent; or using a mixed solvent of water and a specific amount of an organic solvent substantially immiscible with water and inert to the reaction.