Abstract: The present invention relates to a pharmaceutical composition with broad-spectrum of activity against class A, class C and D enzymes comprising an antibiotic and a pharmaceutically effective amount of a compound of Formula (I), compounds of Formula (I), the use of a therapeutically effective amount of one or more compounds of Formula (I) as a broad-spectrum beta-lactamase inhibitor and the use of such a pharmaceutical composition for the treatment of an infection in humans or animals caused by bacteria.

Abstract: The present invention relates to a compound of Formula (I) in particular compounds of formula (Ia), the use of a therapeutically effective amount of one or more compounds of formula (I) or (Ia) as a broad-spectrum antibiotic and the use of a pharmaceutical composition comprising said compounds for the treatment of bacterial infections in humans or animals.

Abstract: The present invention relates to the pharmaceutical dosage forms which enable a controlled and/or a targeted delivery of an active substance to the selected regions of gastrointestinal tract of humans or animals. The pharmaceutical dosage forms preferably comprises the active substance N-(2(2-phthalimidoethoxy)-acetyl)-L-alanyl-D-glutamic acid (designated as LK 423). Methods of treatment of chronic inflammatory diseases of gastrointestinal tract of humans and/or animals by using the pharmaceutical dosage forms of the invention are disclosed.

Abstract: The invention relates to a pharmaceutical composition comprising an ethylene derivatives of tricyclic carbapenems of the general Formula (I) in the form of pure diastereoisomers and in the form of pure geometric isomers or a salt, ester or amide derivate thereof and an antibiotic and the use of this composition as a broad band spectrum ?-lactamase inhibitor.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a new method for the treatment of psychostimulant addiction, in particular cocaine addiction, or pharmaceutically acceptable acid addition salts thereof, with a therapeutically effective amount of 9,10-didehydro-N-methyl-N-(2-propy-nyl)-6-methyl-8?-aminomethylergo-line in the form of free base or in the form of pharmaceutically acceptable addition salt, in particular the bimaleate salt, as well as pharmaceutical compositions containing said compound. In literature, the compound is also known under code LEK-8829. More particularly, present invention relates to a novel method of treatment for reduction of abstinence symptoms after cocaine withdrawal and for suppression the symptoms of craving for cocaine withdrawal and for suppression the symptoms of craving for cocaine reinforcement, and to the use of said active substance for the preparation of the pharmaceutical composition for the treatment of cocaine addiction.

Abstract: The present invention concerns novel azolidine compounds of Formula (I) wherein X denotes S, NH, CH2 or O, Y and W denotes each independently S or O, Q denotes CH or N, n and m are an integer from 0 to 2, and R1 and R2 denote independently from each other hydrogen, optionally substituted aryl, optionally substituted heterocyclyl, or an optionally substituted (C1-10) aliphatic group, R3 denotes hydrogen, lower alkyl, halogen, lower alkoxy, nitro, and R4 and R5 denote independently from each other hydrogen, halogen or alkyl, with the proviso that if one of R1 and R2 is hydrogen then the respective other one of R1 and R2 does not denote substituted or unsubstituted 2-furyland their salts, that are useful as pharmaceutical agents, e.g. as antibacterial agents, and to pharmaceutical compositions comprising such compounds.

Abstract: A novel process for the preparation of 1?-hydroxy-2?-substituted cyclohexyl azetidin-2-one compound of formula 2, which is important intermediate in the synthesis of trinems, is described by epoxide ring opening of (3S,4R)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-4-[(1?R,2?S,3?R)-1?,2?-epoxycyclohexan-3?-yl]azetidin-2-one of formula 1 with the nucleophile compound of formula RYH, where nucleophile may act as solvent itself if the nucleophile is in the liquid form, in a suitable solvent and in the presence of a suitable catalyst from the group of salt of trifluoromethane sulfonic acid, preferably ytterbium (III) trifluoromethanesulfonate, stannous (II) trifluoromethanesulfonate or dysprosium (III) trifluoromethanesulfonate, under a) ultrasonic irradiation or b) under microwave irradiation of the reaction mixture following by isolation and purification of the desired compound.

Abstract: A novel crystalline form of the substrate known under the chemical name 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfiny]-1H-benzimidazole, and having the generic name omeprazole, hereinafter referred to as omeprozole form C, is disclosed. Further, a process for the preparation of omeprazole form C, a pharmaceutical formulation containing omeprazole form C in admixture with pharmaceutically acceptable excipients and the use of omeprazole form C for treatment of gastrointestinal disorders are disclosed.

Abstract: The invention is related to novel substituted diazaheterocycles useful as effective antihypercholesterolemic agents, methods of their preparation, and pharmaceutical compositions containing them.

Abstract: The present invention relates to the use of certain aza-phenylalanine compounds of formula (I) wherein R1 denotes amino, alkylamino, dialkylamino, amidino, alkylamidino, N-hydroxyamidino, or N-alkoxyamidino, Y denotes sulfonyl or carbonyl and R2 and R4 independently represent various organic residues, in the treatment or prevention of cardiac arrhythmia and/or in treatment or prevention of diseases in association with ischemic heart conditions.

Abstract: The compounds of the formula I and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombin inhibitors.

Abstract: The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.

Abstract: A novel crystalline form of the substrate known under the chemical name 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfiny]-1H-benzimidazole, and having the generic name omeprazole, hereinafter referred to as omeprozole form C, is disclosed. Further, a process for the preparation of omeprazole form C, a pharmaceutical formulation containing omeprazole form C in admixture with pharmaceutically acceptable excipients and the use of omeprazole form C for treatment of gastrointestinal disorders are disclosed.

Abstract: The present invention belongs to the field of pharmaceutical industry and relates to a new method for the treatment of psychostimulant addiction, in particular cocaine addiction, or pharmaceutically acceptable acid addition salts thereof, with a therapeutically effective amount of 9,10-didehydro-N-methyl-N-(2-propy-nyl)-6-methyl-8?-aminomethylergo-line in the form of free base or in the form of pharmaceutically acceptable addition salt, in particular the bimaleate salt, as well as pharmaceutical compositions containing said compound. In literature, the compound is also known under code LEK-8829. More particularly, present invention relates to a novel method of treatment for reduction of abstinence symptoms after cocaine withdrawal and for suppression the symptoms of craving for cocaine withdrawal and for suppression the symptoms of craving for cocaine reinforcement, and to the use of said active substance for the preparation of the pharmaceutical composition for the treatment of cocaine addiction.

Abstract: A novel crystalline form of the substrate known under the chemical name 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfiny] -1H-benzimidazole, and having the generic name omeprazole, hereinafter referred to as omeprozole form C, is disclosed. Further, a process for the preparation of omeprazole form C, a pharmaceutical formulation containing omeprazole form C in admixture with pharmaceutically acceptable excipients and the use of omeprazole form C for treatment of gastrointestinal disorders are disclosed.

Abstract: The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.

Abstract: Heterocyclic acyldipeptides of the formula I ##STR1## wherein Z represents an oxygen or sulphur atom or a --CH.sub.2 -group;R.sub.1, R.sub.2 and R.sub.3 individually represent hydrogen or certain organic groups;R.sub.4 and R.sub.5, which are identical or different, represent an OR.sub.6 or NHR.sub.6 group, wherein R.sub.6 is hydrogen or certain organic groups;Y represents a --CH.sub.2 --, .dbd.CH-- or .dbd.N-- group;A represents a --(CH.sub.2).sub.3 -- group when Y is --CH.sub.2 --, the two rings being transcondensed, or a ##STR2## wherein R.sub.7 represents H, F, Br, Cl, nitro, or certain organic groups when Y is .dbd.CH-- or .dbd.N--; and their pharmaceutically acceptable salts are provided. These heterocyclic acyldipeptides and their salts are useful as active compounds in medicaments having immunostimulatory and antitumor activity.

Abstract: N-acyldipeptides of formula I ##STR1## wherein R represents a rest of formula ##STR2## and R.sub.4, Y, m, n and Z have the meaning as defined in the description, R.sub.1 represents hydrogen, a 1-10 C. alkyl, an optionally substituted methyl or benzyl,R.sub.2 represents a --CO--A group,wherein A has the meanings as defined in the description,R.sub.3 represents a --(CH.sub.2).sub.p --CO--W group,wherein p and W have the meaning as defined in the description.

Abstract: There are described novel trans-2-acylaminocyclohexyloxyacyldipeptides of formula I ##STR1## wherein R.sub.1 represents --CO--R.sub.6, --SO.sub.2 --R.sub.7 or ##STR2## R.sub.6 is C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.18 alkoxy, R.sub.7 is C.sub.1 -C.sub.18 alkyl or an optionally substituted phenyl group,Y is .dbd.O, .dbd.S or .dbd.NH;R.sub.2 =R.sub.3 and represent --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 represents --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, a straight or branched chain C.sub.1 -C.sub.18 alkyl group or benzyl group;R.sub.5 represents --OR.sub.9 or --NHR.sub.9,and novel (1R,2R)- and (1S,2S)-trans-2-acylaminocyclohexyloxyacetyldipeptides of the formulas Ia and Ib ##STR3## wherein R.sub.1 is --CO--R.sub.6, R.sub.6 is C.sub.1 -C.sub.18 alkyl,R.sub.2 is --H,R.sub.3 is --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 is --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, C.sub.1 -C.sub.18 alkyl or benzyl,R.sub.5 is --OR.