Abstract: Compounds, 1,3-dihydro-1-{1-?piperidin-4-yl!piperidin-4-yl}-2H-benzimidazol-2-ones and 1,3-dihydro-1-{4-amino-1-cyclohexyl}-2H-benzimidazol-2-ones and derivatives thereof, their preparation, method of use and pharmaceutical compositions are described. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).

Abstract: The present invention includes novel compounds or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

Abstract: Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.

Abstract: Provision of a succinamic acid compound of the formula (1) ##STR1## wherein R.sup.1 is an alkyl or a lower alkenyl and R.sup.2 is an optionally esterified carboxyl, a pharmaceutically acceptable salt thereof, an agent for the prophylaxis and/or treatment of the complications of diabetes, comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, an aldose reductase inhibitor comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, and a method for producing the succinamic acid compound or a pharmaceutically acceptable salt thereof. The novel succinamic acid compounds of the formula (1) of the present invention and pharmaceutically acceptable salts thereof have a strong aldose reductase activity-inhibitory in mammals such as human, and show superior safety.

Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium as catalyst comprises adding to the reactiona) at least one water-soluble complexing ligand andb) sufficient water for the reaction mixture to form an aqueous phase.The reaction of the invention proceeds chemoselectively so that even electrophilic groups such as esters or nitriles do not have an adverse effect on the course of the reaction.The use according to the invention of a water-soluble complexing ligand in an aqueous phase enables polycyclic aromatic compounds to be prepared in very good yields and at the same time very high purity, in particular without contamination by the complexing ligands.

Abstract: Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.

Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.

Abstract: A quinazoline derivative represented by formula(I) or a pharmaceutically acceptable salt thereof is useful for the treatment of peptic ulcer, wherein: ##STR1## R.sub.1 and R.sub.2 are each hydrogen or a C.sub.1 -C.sub.4 alkyl group; R.sub.3 is hydrogen or a halogen;R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9, which may be the same or different, are each hydrogen, a C.sub.1 -C.sub.4 alkyl group, a cyclopropyl group, or a C.sub.1 -C.sub.4 alkyl group substituted with a halogen; andR.sub.10 is a methoxy group.

Abstract: The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumour diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,R is one or more substituents selected from halogen, alkyl, trifluoromethyl and alkoxy; andR.sub.1 and R.sub.2 are each independently of the other alkyl, or phenyl that is unsubstituted or substituted by halogen, trifluoromethyl, alkyl or by alkoxy, it also being possible for one of the two radicals R.sub.1 and R.sub.2 to be hydrogen, or R.sub.1 and R.sub.2 together form an alkylene chain having from 2 to 5 carbon atoms that is unsubstituted or substituted by alkyl; or salts thereof. Compounds of formula I inhibit protein kinases, for example the tyrosine protein kinase of the receptor for the epidermal growth factor, EGF.

Abstract: Optically active carboxamide derivatives having analgesic activity and being useful as an analgesic agent. The compounds have a general formula: ##STR1## (in the above formula, R.sup.1 represents a hydrogen or halogen atom;R.sup.2 represents a halogen atom;R.sup.3 represents a pyrrolidino or piperidino group;Y represents a methylene or carbonyl group; andn is an integer of 1 or 2) and pharmacologically acceptable salts thereof.

Abstract: A bioavailable crystalline form of cefuroxime axetil, obtained by treating known crystalline or amorphous cefuroxime axetil with water or with a water-miscible organic solvent or with a mixture thereof at a temperature of between +20.degree. C. and +100.degree. C., followed by cooling and separating the crystalline product by known methods.

Abstract: The invention relates to new 1-H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A and B together with the carbon atom to which they are bonded represent a substituted cycle,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents 0, 1, 2 or 3,G is defined in the claims,to processes for their preparation, and to their use as pesticides.

Abstract: The present invention encompasses structures of the Formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: X is oxygen, H.sub.2, or sulfur;Y is oxygen or sulfur;W is alkyl, arylalkyl, or heteroarylalkyl, each of which is optionally substituted; orW is aryl or heteroaryl; ##STR2## wherein: Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C--R.sub.a, whereeach R.sub.a independently is hydrogen, an inorganic substitutent or an optionally substituted aromatic group;n is 1, 2 or 3; andR.sub.b is hydrogen, alkyl, or an optionally substituted aromatic group,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.

Abstract: The invention relates to new labelled fibrinogen receptor antagonists which have an affinity for the receptor which is comparable to or greater than that of .sup.125 I-fibrinogen and whose binding is not disrupted by foreign proteins.

Abstract: The manufacture of 5-dichloroacetyl-3,3,6-trimethyl-9-oxo-1,5-diazabicyclo?4.3.0!-nonane I by the reaction of 3,3,6-trimethyl-9-oxo-1,5-diaza-bicyclo?4.3.0!nonane II with dichloroacetyl chloride in the presence of a solvent and a base, whereina) this reaction is carried out in a two-phase system comprising a virtually water-insoluble organic solvent and water, and sodium or potassium hydroxide acting as the base is metered in at a rate corresponding to the rate of consumption of the dichloroacetyl chloride such that the aqueous phase exhibits a pH of from 7 to 9, andb) the resulting product is separated.

Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.

Abstract: Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.

Abstract: Compounds of formula (I), wherein R is an oxygen or sulphur atom or an NH or N-alk radical, and each of R.sub.1 and R.sub.2, which are the same or different, is a hydrogen or halogen atom or an alkyl, alkoxy, amino, acylamino, --NH--CO--NH--Ar,--N.dbd.CH--N(alk)alk', nitro, cyano, phenyl, imidazolyl or SO.sub.3 H radical, the preparation thereof, and drugs containing such compounds, are disclosed.

Abstract: Isobenzofurandiones are obtained in particularly advantageous manner by the dehydrogenation of tetrahydroisobenzofurandiones in the presence of catalysts at elevated temperature by a process in which distilled tetrahydro-isobenzofurandiones are heated to temperatures of between 120.degree. and 300.degree. C. in the presence of supported palladium and/or platinum catalysts and in the presence of maleic acid derivatives in a trickle-phase or liquid-phase procedure, the temperature in the liquid-phase procedure being increased at a rate of 0.6.degree. to 3.degree. C. per minute above 80.degree. to 110.degree. C.

Abstract: A method of synthesizing an indole derivative of the tryptamine type particularly .?.melatonine,.!. .Iadd.melatonin .Iaddend.comprising the steps of 1) reacting potassium phthalimide and 1,3-di-bromopropane to obtain 3-bromopropylphthalimide; 2) reacting 3-bromopropylphthalimide with sodium acetoacetic ester in ethanol to obtain ethyl-2-acetyl-5-phthalimidopentanoate; 3) reacting the product from step 2) with diazo-p-anisidine to obtain 2-carboxyethyl-3-(2-phthalimidoethyl)-5-methoxy-indole; 4) reacting the 2-carboxyethyl-3-(2-phthalimidoethyl)-5-methoxy-indole with 2N/NaOH and then 20% H.sub.2 SO.sub.4 to obtain impure 5-methoxytriptamine, which is purified by means of hexamethyldisilazane. The mono and disubstituted derivatives are obtained and the monosubstituted derivative is hydrolyzed with aqueous methanol and then recrystallized from ethanol. The N-acetyl derivative is prepared by reaction with acetic anhydride. .?.Melatonine.!. .Iadd.Melatonin .Iaddend.