Ciba-Geigy Corporation

Max Wilhelm

Franz Ostermayer

Herbert Schroter

Kurt Eichenberger

Angelo Storni

Raymond Bernasconi

Karl Schenker

Dieter Beck

The invention relates to a method of lowering intraocular pressure by a topical application of 2-tert-butylamino-1-(3,5-diisobutyryloxyphenyl)-ethanol or an acid addition salt thereof onto the eye of a mammalian species including man, especially as a conservative and/or curative medical treatment of ocular hypertension and pathological states associated therewith, in the first line glaucoma. The invention also relates to ophthalmic preparations for the topical application comprising an effective amount of the above-identified compounds in combination with a pharmaceutically acceptable carrier, and a method for producing themselves by non-chemical means.

Method of lowering intraocular pressure with ibuterol

Compounds selected from the group consisting of amines of the formula I ##STR1## in which R.sub.1 and R.sub.2 stand for a member selected from lower alkyl, lower alkenyl, cycloalkyl having 4 to 7 ring members, phenyl-lower alkyl, phenyl-lower alkyl substituted in the phenyl residue by a member selected from lower alkyl, lower alkoxy, halogen and trifluoromethyl, lower alkylene, oxa-lower alkylene, aza-lower alkylene and thia-lower alkylene, and one of R.sub.1 and R.sub.2 stands for hydrogen and the other has the above meanings, Ph stands for a member selected from meta- and para-phenylene and meta- and para-phenylene substituted by a member selected from lower alkyl, lower alkenyl, lower alkinyl, mercapto-lower alkyl, hydroxy-lower alkyl, phenyl, cyano, hydrogen, halogen, lower alkoxy, lower alkenyloxy, lower alkinyloxy, mono-, di and trihalogeno-lower alkyl, cycloalkyl having 5 to 7 ring members and phenoxy, and R.sub.3 stands for a member selected from lower alkyl and cycloalkyl having 5 to 7 ring member, and their condensation product with aldehydes and ketones, and their salts are useful as agents for the inhibition of the cardiac .beta.-receptors.

Pharmaceutical composition for inhibiting and blocking cardioselective

Piperidines of the formula ##STR1## in which R.sub.1 stands for optionally substituted aryl, R.sub.2 for hydrogen, lower alkyl, lower alkenyl, acyl or .alpha.-aryl-lower alkyl, R.sub.3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R.sub.4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.

1-Substituted-4-(2-oxo-hexahydro-1-pyrimidinyl)-piperidine

Pharmaceutical piperidine derivatives

9-(2-A-3-R-propyl)-9,10-dihydro-9,10-ethano-anthracenes containing the nucleus of the formula ##STR1## wherein R denotes a secondary or tertiary amino group and A denotes a free, etherified or acylated hydroxyl group, their pharmaceutically acceptable salts are useful as psychotropics, especially as anti-depressants.

Pharmaceutical preparation using

Compounds selected from the group consisting of amines of the formula I ##STR1## in which R.sub.1 and R.sub.2 stand for a member selected from lower alkyl, lower alkenyl, cycloalkyl having 4 to 7 ring members, phenyl-lower alkyl, phenyl-lower alkyl substituted in the phenyl residue by a member selected from lower alkyl, lower alkoxy, halogen and trifluoromethyl, lower alkylene, oxa-lower alkylene, aza-lower alkylene and thia-lower alkylene, and one of R.sub.1 and R.sub.2 stands for hydrogen and the other has the above meanings, Ph stands for a member selected from meta- and para-phenylene and meta- and para-phenylene substituted by a member selected from lower alkyl, lower alkenyl, lower alkinyl, mercapto-lower alkyl, hydroxy-lower alkyl, phenyl, cyano, hydrogen, halogen, lower alkoxy, lower alkenyloxy, lower alkinyloxy, mono-, di and trihalogeno-lower alkyl, cycloalkyl having 5 to 7 ring members and phenoxy, and R.sub.3 stands for a member selected from lower alkyl and cycloalkyl having 5 to 7 ring members, and their condensation product with aldehydes and ketones, and their salts are useful as agents for the inhibition of the cardiac .beta.-receptors.

Cycloalkylureido phenoxy propanolamines

9-(2-A-3-R-propyl)-9,10-dihydro-9,10-ethanoanthracenes containing the nucleus of the formula ##STR1## wherein R denotes a secondary or tertiary amino group and A denotes a free, etherified or acylated hydroxyl group, their pharmaceutically acceptable salts are useful as psychotropics, especially as anti-depressants.

9-(2-Hydroxy-3-amino-propyl)-9,10-dihydro-9,10-ethano-anthracenes and

Piperidines of the formula ##SPC1## In which R.sub.1 stands for optionally substituted aryl, R.sub.2 for hydrogen, lower alkyl, lower alkenyl, acyl or .alpha.-aryl-lower alkyl, R.sub.3 for a free or substituted hydroxyl group, alk for lower alkylene which separates the two nitrogen atoms by 2 or 3 carbon atoms, R.sub.4 represents hydrogen or lower alkyl and n represents an integer from 1 to 4, and their salts as well as processes for their manufacture and pharmaceutical compositions comprising such compounds, and a process for lowering the blood pressure wherein such compositions are administered to a warm-blooded host.

1-Substituted-4-(2-oxo-1-imidazolidinyl) piperidines

Compounds selected from the group consisting of amines of the formula I ##EQU1## in which R.sub.1 and R.sub.2 stand for a member selected from lower alkyl, lower alkenyl, cycloalkyl having 4 to 7 ring members, phenyl-lower alkyl, phenyl-lower alkyl substituted in the phenyl residue by a member selected from lower alkyl, lower alkoxy, halogen and trifluoromethyl, lower alkylene, oxalower alkylene, aza-lower alkylene and thia-lower alkylene, and one of R.sub.1 and R.sub.2 stands for hydrogen and the other has the above meanings, Ph stands for a member selected from meta- and para-phenylene and meta- and para-phenylene substituted by a member selected from lower alkyl, lower alkenyl, lower alkinyl, mercapto-lower alkyl, hydroxy-lower alkyl, phenyl, cyano, hydrogen, halogen, lower alkoxy, lower alkenyloxy, lower alkinyloxy, mono-, di and trihalogeno-lower alkyl, cycloalkyl having 5 to 7 ring members and phenoxy, and R.sub.3 stands for a member selected from lower alkyl and cycloalkyl having 5 to 7 ring members, and their condensation product with aldehydes and ketones, and their salts are useful as agents for the inhibition of the cardiac .beta.-receptors.

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Watchung, NJ, United States of America

Max Wilhelm