Abstract: The present invention relates to new compounds of formula (I), (I) wherein the meaning of R1 is hydrogen atom, C1-C5 acyl group, benzoyl group or R2—COOR3 group, Y is hydrogen atom or alkali ion, R2 is C1-C4 straight or branched alkylidene group and R3 is hydrogen atom, C1-C4 alkyl group or alkali ion, and/or stereoisomers and/or diastereomers and/or pharmaceutically acceptable salts and/or hydrates and/or solvates thereof, which are suitable for the treatment of pain of acute and chronic inflammation origin as well as postoperative pain and dysmenorrhea. The invention also relates to the process of the synthesis of compounds of formula (I) as well as the pharmaceutical composition containing the same and the use for treatment of pain, inflammation and disorders associated with inflammation.

Abstract: Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof—wherein the meaning of R is 3?-pyridyl or 2?-amino-ethylidene group—from compounds of formula (II)—wherein the meaning of R is as described above—or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.

Abstract: The present invention relates to new compounds of formula (I), (I) wherein the meaning of R1 is hydrogen atom, C1-C5 acyl group, benzoyl group or R2—COOR3 group, Y is hydrogen atom or alkali ion, R2 is C1-C4 straight or branched alkylidene group and R3 is hydrogen atom, C1-C4 alkyl group or alkali ion, and/or stereoisomers and/or diastereomers and/or pharmaceutically acceptable salts and/or hydrates and/or solvates thereof, which are suitable for the treatment of pain of acute and chronic inflammation origin as well as postoperative pain and dysmenorrhea. The invention also relates to the process of the synthesis of compounds of formula (I) as well as the pharmaceutical composition containing the same and the use for treatment of pain, inflammation and disorders associated with inflammation.

Abstract: The invention relates to new N-hydroxy-4-(3-phenyl-5-methyl-isoxazole-4-yl)-benzenesulfonamide solvates of formula (I). wherein n represents 0 or 1 mol, [solvate] represents water, C1-C4 alcohol, C1-C4 alkylester of C1-C3 carboxylic acid or dioxane, and the mixture of solvated (wherein n=1) and solvat-free forms (wherein n=0). Furthermore, the invention relates their process for production and use for the treatment of osteoarthritis and rheumatoid arthritis and surgical and primary dysmenorrheal pains, based on anti-inflammatory and analgesic pharmacological model experiments.

Abstract: The object of the present invention are new desloratadine salts of formula I wherein the meaning of X is an acid residue and the meaning of n is 1 or 2, and formula II wherein the meaning of X is a pK <3.5 acid residue.

Abstract: Process for the synthesis of high purity 2-substituted-1-(hydroxy-ethylidene)-1,1-bisphosphonic acid of formula (I), the salts and hydrates thereof—wherein the meaning of R is 3?-pyridyl or 2?-amino-ethylidene group—from compounds of formula (II)—wherein the meaning of R is as described above—or salts and hydrates thereof with phosphorous acid in the presence of methanesulfonic acid using phosphorus pentoxide as reagent and in given case the obtained acid is converted into a salt with base.

Abstract: The object of the present invention are new desloratadine salts of formula I wherein the meaning of X is an acid residue and the meaning of n is 1 or 2, and formula II wherein the meaning of X is a pK<3.5 acid residue.

Abstract: A Process is disclosed for preparing a compound of the Formula (I) which comprises the steps of: (a) detritylating a compound of the Formula (III)  with 0.1 to 1 equivalent of potassium hydroxide in a C1 to C4 straight chain alcohol solvent to obtain a reaction mixture containing the compound of the Formula (I), (b) changing the C1 to C4 straight chain alcohol solvent in the reaction mixture to an aprotic solvent or a weakly protic solvent, and (c) following step (b) crystallizing out the compound of the Formula (I) from the reaction mixture.

Abstract: The invention relates to a novel process of amalodipine benzenesulphonate of formula (I) by reacting a new 2-[/2-carboxy-benzoyl)-aminoethoxy/methyl/]-4-(2-chlorophenyl)-3-ethoxycarbonyl-5-methoxycarbonyl-6-methyl-1,4-di-hydropyridine derivative of general formula (II) wherein X represents hydrogen or alkali metal or alkali earth metal or quaternary ammonium—with benzenesulphonic acid.

Abstract: The invention relates to a process for the synthesis of losartan potassium of formula (I), chemical name: 2-n-butyl-4-chloro-1-[(2′-(tetrazol-5-yl)-1,1′biphenyl-4-yl)-methyl]-imidazol-5-methanol potassium, starting from 2-n-butyl-4-chloro-1-[(2′-(2-triphenylmetyl-2H-tetrazol-5-yl)-1,1′-biphenyl-4-yl)-methyl]-1H-imidazol-4-methanol of formula (III). According to the process the compound of formula (III) is reacted in an alcohol of formula (VI),—wherein the meaning of R is C1-C4 straight chain alkyl group—with 0.1-1 equivalent of potassium hydroxide. The final product of formula (I) is isolated after crystallizing out by changing the solvent to an aprotic or weakly protic solvent (I).

Abstract: The present invention relates to a proccss for preparing cis-(1S)-N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphtalenami ne and its acid addition salts wherein N-methyl-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-naphtalene-1-en]-amine -N-oxide is hydrogenated in an inert solvent in the presence of a catalyst, then the resulting mixture is treated with alcanolic solution of a mineral acid, the resulting cis-racemic acid addition salt is converted to the free base by known methods, resolved and the resulting cis-(+)-base of formula (II) is converted to an acid addition salt. N-methyl-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-naphtalene-1-en]amine- N-oxide is also disclosed.

Abstract: Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.

Abstract: Novel acrylic acid salts of formula ##STR1## wherein R represents a hydrogen or a halogen atom, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group,M represents a cation derived from bismuth, zinc or a pharmaceutically acceptable organic base,X represents an inorganic anion,n is an integer of from 0 to 2,m is an integer of from 1 to 3,p is 0 or 1, andr is an integer of from 0 to 6having cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.

Abstract: The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or a C.sub.1-4 acylamino group; andR.sup.1 is hydrogen or a carboxyl-protective group or E and/or Z configuration as well as their salts.The compounds according to the invention show a cytoprotecive effect and in addition, a valuable anti-inflammatory action. Their toxicity is low.

Abstract: The invention relates to novel butenoic acid derivatives of the general formula (Ia) having E-configuration ##STR1## as well as to their Z-izomers of the general formula ##STR2## wherein R stands for a (-)-menthyl or a (+)-menthyl group. as well as pharmaceutical compositions containing these compounds.The novel butenoic acid derivatives of the general formulae (Ia) and (Ib) possess valuable pharmacological properties, mainly gastric cytoprotective effect.

Abstract: The present invention relates to a compound of the formula (I) ##STR1## wherein R.sup.1 stands for methyl or a group of the formula R.sup.3 --NH--(CH.sub.2).sub.4 --wherein R.sup.3 is hydrogen or a protective group being compatible with the peptide bond,R.sup.2 represents hydrogen, a protective group being compatible with the peptide bond or a cation derived from an organic or inorganic basethe pharmaceutically acceptable salts and diastereomers thereof.The compounds of the invention are useful for inhibiting the effect of the angiotensin converting ensime and they can be used in the therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.

Abstract: The invention relates to a novel process for the preparation of 1-[3-mercapto-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid through the N-acylation of L-proline.According to the process of the invention L-proline is acylated with a 3-halogen-2-methylpropionyl chloride of the formula III ##STR1## wherein Hal is a halogen atom, preferably chlorine or bromine, the obtained 1-[3-halogen-(2S)-methylpropionyl]-pyrrolidine-(2S)-carboxylic acid, wherein Hal is as stated above, is reacted with an alkali thiosulfate or alkali trithiocarbonate and the reaction product is hydrolized with an acid.The process of the invention is very economical as compared with the known processes. The desired product is prepared from methacrylic acid in 4 reaction steps with a total yield of 25 percent and from L-proline in 2 reaction steps with a total yield of 30 percent.

Abstract: Keys which are used in a keyboard of a miniaturized data processing device include an upper surface which is provided with a downwardly-extending wall running transversely to the movement of the finger when operating the keys. The downwardly-extending wall, which is formed, for example, by a groove disposed in the upper surface, serves as a support for the tip of a user's fingernail when operating the keys. Such keys make possible an accurate operation even if the keys are disposed closely side by side in a miniaturized key board and the fingernail is fashionably long.

Abstract: The keyboard for the computer portion of a combined electronic digital watch - computer device is hinged so as to be foldable into either a useable mode or a non-accessable mode, and the individual keys include triggers extending upwardly from the bottom of an elongated depression formed by surrounding side walls, the triggers being positioned eccentrically within the depression.