Abstract: The present invention is related to rosuvastatin zinc salt of the Formula (I), process for preparation thereof and medicinal products containing said salt. Rosuvastatin zinc salt according to the present invention is prepared by reacting rosuvastatin with a zinc alcoholate, zinc enolate or an inorganic or organic zinc salt and isolating the thus obtained rosuvastatin zinc salt (2:1).

Abstract: The invention refers to a novel process for the preparation of {2-[-(?-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetic acid, which comprises hydrolyzing an N,N-disubstituted {2-[-(?-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetamide, wherein said substituents are selected from alkyl groups having 1 to 4 carbon atoms optionally substituted by a phenyl group, alkenyl groups having 2 to 4 carbon atoms or cyclohexyl groups, or the substituents together with the adjacent nitrogen atom of the acetoamido group, form a morpholino group.

Abstract: The invention refers to a novel process for the preparation of cetirizine of formula (I) as well as to novel {2-[4-(&agr;-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}acetamides of formula II, wherein R1 and R2 represent, independently, a C1-4 alkyl group optionally substituted by a phenyl group, a C2-4 alkenyl group or a cyclohexyl group, or R1 and R2 form together with the adjacent nitrogen atom a morpholino group. According to the novel process, an acetamide of formula (II) is hydrolized, if desired in the presence of a phase transfer catalyst, to obtain cetirizine.

Abstract: The invention relates to a new process for the preparation of amlodipine besylate of the Formula ##STR1## Amlodipine besylate of the Formula I is a valuable known blood pressure decreasing antianginal agent.The advantage of the process of the present invention is that it can be carried out in a simple way with high yields and there is no need to isolate the amlodipine base.

Abstract: This invention relates to a new and improved process for the preparation of 6,7-dichloro-1,5-dihydroimidazo[2,1-b]-quinazolin-2[3H]-one of formula ##STR1## (anagrelide), a valuable blood platelet antiaggregative compound. According to the process of the invention the compound of formula (I) is prepared by subjecting a new 2-cyanoiminoquinazoline derivative of the general formula ##STR2## wherein R stands for cyano or a group of the formula COOR.sup.1, in the latter R.sup.1 representing lower alkyl optionally carrying a phenyl substituent, to thermal cyclization in an acidic medium.The invention also relates to new 2-cyanoiminoquinazo-lines of the general formula (III) used for the production of anagrelide and to the preparation of the said compounds.The invention provides an advantageous process for the preparation of anagrelide which is devoid of the drawbacks of the hitherto known processes and renders possible the production of the compound of the formula (I) on industrial scale, too.

Abstract: The invention relates to a process for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitro-phenyl)-pyridine-3,5-dicarbo xylate of the Formula I ##STR1## which comprises a) reacting a compound of the general Formula II ##STR2## (wherein n is 1 or 3; if n is 1, then R stands for a group of the Formula (a) ##STR3## and if n is 3, then R represents hydrogen) with methyl acetoacetate of the Formula IIICH.sub.3 --CO--CH.sub.2 --COOCH.sub.3 (III)and optionally with an amino compound of the general Formula IV ##STR4## (wherein Z is a group of the Formula (c), ##STR5## k is 1 and both symbols p are 0; or Z stands for a C.sub.

Abstract: The invention is directed to processes for the preparation of dimethyl-1,4-dihydro-2,6-dimethyl-4-(2'-nitrophenyl)-pyridine-3,5-dicarbox ylate by reacting 1-methoxy-1-(2'-nitrophenyl)-N-(2'-nitrophenyl)methylene methanamie or 1-(2'-nitrophenyl)-N,N'-bis-(2'-nitrophenyl) methylene methanediamine with methyl acetoacetate in the presence of an amine compound or by reacting the monomeric or trimeric from of 2-nitrobenzaldimine with methyl acetoacetate.

Abstract: The present invention relates to a process for the preparation of regulated release solid pharmaceutical compositions comprising 4-(2'-nitro-phenyl)-2,6-dimethyl-3,5-dimethoxycarbonyl-1,4-dihydro-pyridin e (referred to further on as "nifedipine") as active ingredient which comprises admixing a solution or solutions of 1 part by weight of nifedipine, 0.1-1.5 parts by weight of one or more hydrophilizing agent(s) and 0.05-1.5 parts by weight of one or more retarding agent(s) formed with one or more identical or different solvent(s) completely or partly and applying the solution(s) thus obtained simultaneously or in succession onto an inert carrier, drying and sieving the product thus obtained and subsequently admixing the same with suitable conventional auxiliary agents and compressing the mixture thus obtained to tablets in a known manner and coating the tablets or filling the mixture into capsules.

Abstract: The invention relates to new dihydropyrimidothiazine derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same and new intermediates useful in the preparation of the said dihydropyrimidothiazine derivatives.The new dihydropyrimidothiazine derivatives of the general formula I, ##STR1## wherein R.sup.1 represents C.sub.1-6 alkoxy, amino or phenylamino,R.sup.2 stands for C.sub.1-6 alkyl or phenyl,R.sup.3 represents hydrogen or C.sub.1-6 alkyl, andR.sup.4 denotes C.sub.1-11 alkyl or phenyl optionally bearing one or more identical or different substituent/s/ selected from halogen, nitro, amino, di-(C.sub.1-6 alkyl)-amino, C.sub.1-6 alkyl, C.sub.1-6 alkoxy and hydroxy,and pharmaceutically acceptable acid addition salts thereof exert valuable antianginal and/or antiinflammatory effect/s/ and are useful in therapy.

Abstract: The invention relates to optically active 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]dioxaz ocine of the Formula ##STR1## and pharmaceutically acceptable acid additional salts thereof. The enantiomers are especially active against Parkinsion's disease.The optically active enantiomers are prepared by(a) resolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxa zocine with a optically active organic acid and separating the enantiomers; or(b) dissolving the racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxa zocine in an organic solvent, crystallizing and isolating one of the enantiomers, optionally dissolving additional racemic 2-chloro-12-(3-dimethylamino-2-methylpropyl)-12H-dibenzo[d,g][1,3,6]-dioxa zocine in the mother liquor obtained and crystallizing and isolating the other enantiomer, and, if desired, repeating the whole process.

Abstract: The invention relates to new quinoline derivatives of the general Formula I ##STR1## (wherein X stands for hydrogen, halogen or lower alkoxy;n is an integer of 1, 2 or 3;R.sup.1 represents hydrogen andR.sup.2 represents hydroxy-lower alkyl or lower alkoxy-lower alkyl or a group of the general formula IV, ##STR2## wherein Z stands for --O--, --S--, --NH-- or --N(lower alkyl)--; the dotted lines represent optional bonds; andm is 0 or 1; orR.sup.1 and R.sup.2 together with the adjacent nitrogen atom, they are attached to, form a 5- or 6-membered heterocyclic group which may optionally contain a further oxygen, nitrogen or sulfur heteroatom and may be optionally substituted),and pharmaceutically acceptable acid addition salts thereof. The new compounds of the present invention exhibit radiosensitizing effect, make hypoxial cells highly sensitive towards radiation and may be used in radiation therapy.