Abstract: A process for preparing (1R,2S,4R)-(−)-2-[(2′-[N,N-dimethylamino}-ethoxy)]-2-[phenyl]-1,7,7-tri-[methyl]-bicyclo [2.2.1]heptane and pharmaceutically acceptable acid addition salts thereof with higher yields and higher grades of purity.

Abstract: The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical compositions containing the above derivatives, and a process for the preparations of the novel compounds.

Abstract: The new compound of Formula (I) and salts thereof possess valuable anxiolytic properties.

Abstract: The invention relates to new 1-[2-(substituted vinyl)]-3,4-dihydro-5H-2,3-benzodiazepine derivatives, a process for the preparation thereof and pharmaceutical compositions comprising them. The new 1-[2-(substituted vinyl)]-3,4-dihidro-5H-2,3-benzodiazepine derivatives according to the invention correspond to the general formula (I), ##STR1## wherein the variables are hereinbelow defined: The new compounds according to the invention affect the central nervous system and can be used to advantage in the therapy.

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: The present invention is directed to an acid amide of the formula ##STR1## wherein R.sup.1 represents hydrogen or nitro,R.sup.2 and R.sup.3 stand for, independently from each other, hydrogen, lower alkyl or lower alkenyl each optionally carrying a substituent selected from the group consisting of halogen, hydroxy, lower alkoxy, di(lower alkyl)amino, phenyl-lower alkoxycarbonyl and a 5- to 6-membered saturated hetero-ring selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino; orR.sup.2 and R.sup.3 form, together with the adjacent nitrogen atom, a 6-membered saturated heterocyclic group selected from the group consisting of piperidino, pyrrolidino, piperazino and morpholino, said heterocyclic group optionally carrying a hydroxy or a hydroxy-lower alkyl group; or apharmaceutically acceptable salt thereof; process of making and pharmaceutical compositions and methods of treating.

Abstract: The invention relates to anxiolytic pharmaceutical compositions comprising as active ingredient 1-sytrylisoquinoline derivatives of general formula (I), whereinn is 1, 2, 3 or 4;R may be the same or different and represent(s) hydrogen, lower alkyl, lower alkoxy or hydroxy, or two substituents R attached to adjacent carbon atoms may form together an alkylenedioxy group;R.sup.1 represents hydrogen or lower alkyl, andAr stands for an optionally substituted aryl or heteroaryl,Some of the compounds of general formula (I) is known, but the majority thereof has not so far described in the literature.The invention also encompasses the preparation of the new compounds of general formula (I), which comprises reacting a compound of general formula (II) with an aldehyde or general formula (III) in the presence of a condensing agent or an acidic catalyst.

Abstract: Derivatives of 2,3-benzodiazepine are substituted by one or two halogen atom(s) and have the general formula ##STR1## These derivatives are non-competitive AMPA antagonists and are used in pharmaceutical compositions.

Abstract: A pharmaceutical composition that is suitable for inhalation is disclosed, thus ensuring an effective treatment of the lungs. For this purpose, an aerosol composition is believed to be suited. The aerosol preparation comprises a stabilized suspension of sodium cromoglycate from which the active substance is favorably absorbed in the lungs after inhalation. In the aerosol preparation, 1 to 4% by mass of sodium cromoglycate is suspended in a mixture of propellants comprising 0.3 to 2.0% by mass of a dispersing agent consisting of oleyl oleate.

Abstract: The invention relates to oral solid pharmaceutical composition containing as active ingredient gemfibrozil and conventional pharmaceutical auxiliary agents comprising as surfactant bis-(2-ethyl-hexyl)-sodium-sulfosuccinate in an amount of 0.05-0.5% by weight relative to gemfibrozil content of the composition.The pharmaceutical compositions according to the present invention contain a relatively small amount of a surfactant, provide uniform dissolution of the active ingredient among the different batches and the standard deviation of the dissolution rate is low.

Abstract: This invention relates to new oxaindene derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same.The compounds according to the invention are characterized by the general formula (1) ##STR1## wherein R.sup.1 represents lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or lower C.sub.3-6 cycloalkyl,R.sup.2 stands for hydrogen, lower C.sub.1-4 alkyl or lower C.sub.3-6 cycloalkyl,R.sup.3 stands for hydrogen, lower C.sub.1-4 alkyl, lower C.sub.1-4 alkoxy or benzyloxy,X denotes hydrogen, an aliphatic C.sub.1-4 -acyl or benzoyl or naphthoyl group, optionally substituted by 1 or more nitro or C.sub.1-4 -alkoxy group(s) or a group of the formula R.sup.5 R.sup.6 N--R.sup.7 --, wherein R.sup.7 represents lower C.sub.1-4 alkylene and R.sup.5 and R.sup.6 each represent lower C.sub.1-4 alkyl, or R.sup.5 and R.sup.

Abstract: The invention refers to a pharmaceutical composition, a process for the preparation thereof and a novel medical use of bicycloheptane derivatives. The pharmaceutical compositions of the invention comprise a bicycloheptane derivative of the formula I ##STR1## wherein said derivative is as defined in the specification herein. The pharmaceutical compositions of the invention are suitable for the treatment of diseases and disorders that are connected with the influence on the cholecystokinin system, especially for preventing the spastic contraction of the gallbladder.

Abstract: The invention relates to a process for the preparation of racemic or optically active epibatidine of the Formula XIV ##STR1## which comprises subjecting racemic or optically active epi-epibatidine-of the Formula XIII ##STR2## to epimerization in the presence base. The advantage of the process is that readily available starting materials are used and the procedure is suitable for industrial scale productions too.Epibatidine is a known highly affective analgesic active ingredient.

Abstract: The invention relates to a novel diffusion-osmotic controlled drug-release pharmaceutical composition containing a one-layer tablet core including a polymeric film-coat, a therapeutically active agent and a hydrophilic polymer; if desired, a two-layer tablet core including active agent and hydrophilic polymer in the first layer thereof and a hydrophilic polymer in the second layer thereof; at least one bore on the part of film-coat in contact with the core or core layer containing the active agent; and, if desired, containing one or more bore(s) in the part thereof in contact with the second layer containing the hydrophilic polymer, which comprises an ammonium methacrylate copolymer as coating material and hydroxypropyl-methylcellulose as hydrophilic polymer. The composition according to the invention is useful for preparing controlled drug-release tablets containing as active agents e.g. .beta.-adrenergic inhibitors (e.g. propranolol) calcium-antagonists (e.g.

Abstract: The invention relates to novel, pharmaceutically active trisubstituted cycloalkane derivatives, a process for the preparation thereof and pharmaceutical compositions comprising the same. The invention also encompasses the use of the said cycloalkane derivatives for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The compounds according to the invention are characterized by the general formula (I), ##STR1## wherein R represents hydrogen, C.sub.1-4 alkyl or hydroxyl,R.sup.1 stands for C.sub.1-12 alkyl,R.sup.2 and R.sup.3 each represents hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, orR.sup.2 and R.sup.3 together with the adjacent nitrogen atom form a 4- to 7-membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which latter may carry a phenyl, benzyl or C.sub.1-4 alkyl substituent,R.sup.4 and R.sup.5 each stands for hydrogen, halogen or C.sub.

Abstract: A pharmaceutical ointment is disclosed containing to 10 percent by mass of micronized piroxicam, 15 to 30 percent by mass of hydrophobic carrier(s), 60 to 75 percent by mass of water, 0.1 to 10 percent by mass of additive(s), and 2 to 5 percent by mass of emulsifiers selected from (i) a poly(ethylene glycol) alkyl or alkenyl ether and (ii) a sorbitane ester of a fatty acid or an oleic acid in a mass ratio of 3:1 to 1:3. The ointment is free from skin irritative action and has local antiphlogistic activity. In addition, a process for preparing he pharmaceutical ointment is provided.

Abstract: Novel basic ether of general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen or C.sub.1-4 alkoxy, or together they represent a 3,4-methylenedioxy group,R stands for C.sub.1-8 alkyl,R.sup.3 represents hydrogen, C.sub.1-4 alkyl or hydroxy,A is a valency bond or methylene group,R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1-12 alkyl or C.sub.1-12 alkenyl, orR.sup.4 and R.sup.5 form together with the adjacent nitrogen atom 1-pyrrolidinyl, 1-piperidinyl, morpholino or 1-piperazinyl groups, stereo and optically active isomers and their possible mixtures, acid-addition salts and quaternary ammonium derivatives thereof. The basic ethers have antiulceric and anxiolytic activities.

Abstract: The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR.sup.3, whereinp is 0, 1, or 2, andR.sup.3 is alkyl, alkenyl, or phenyl-, which may have halogen or nitro substituents, or phenyl optionally substituted;or NR.sup.4 R.sup.5 whereinR.sup.4 and R.sup.5 are hydrogen, alkyl, alkenyl, phenyl-alkyl, or di-alkyl-amino-alkyl;R.sup.1 and R.sup.2 are hydrogen or alkyl, ortogether form a group (CH.sub.2)n--Y--(CH.sub.2)m, wherein Y is CH.sub.2, or NR.sup.6, wherein R.sup.6 is phenyl-alkyl,n and m are 0 or 1 to 5;Z is NR.sup.7 R.sup.8, whereinR.sup.7 and R.sup.8 each are hydrogen, alkenyl, cycloalkyl, adamantayl, or phenyl-alkyl, which may have one or more substituents ortogether form a group of (CH.sub.2)j--W--(CH.sub.2)k, wherein j and k each are 1 to 3, and W is oxygen, CH.sub.2, CHOH, or NR.sup.10 , wherein R.sup.10 is hydrogen, alkoxycarbonyl, or alkyl, which latter may be substituted.or SR.sup.9, whereinR.sup.

Abstract: Process for the preparation of 8 -[4 -[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7,9-d ione (buspiron) of the Formula I ##STR1## and the hydrochlorides thereof having high purity by continuously adding a solution of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-but-2 -inyl]-8-aza-spiro[4.5]decane-7,9-dione of the formula II ##STR2## formed with an inert organic solvent having a concentration of at least 40% by weight to a suspension of a hydrogenation catalyst in an inert organic solvent and optionally converting the 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]decane-7 ,9-dione thus obtained into the hydrochloride thereof.

Abstract: The invention relates to racemic or optically active 1,3,4-benzotriazepin-5(4H)-one derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said compounds for the treatment of diseases and for the preparation of pharmaceutical compositions containing the said compounds as active agent.The new compounds according to the invention correspond to the general formula (I), ##STR1## wherein R.sup.1 represents hydrogen or straight or branched chain C.sub.1-4 alkyl optionally carrying a pyridyl or a phenyl substituent;R.sup.2 stands for cyanoimino;R.sup.3 denotes hydrogen or straight or branched chain C.sub.1-4 alkyl;R.sup.4 stands for C.sub.1-4 alkyl; andthe dotted line does not represent a valency bond; orR.sup.2 stands for a group of the formula R.sup.9 R.sup.10 N, whereinR.sup.9 and R.sup.10 are independently hydrogen or straight or branched chain C.sub.1-10 alkyl, orR.sup.9 R.sup.10 N together form a 5- to 7-membered heterocyclic group; orR.sup.9 R.