Hoechst Roussel Pharmaceuticals

Hoechst Marion Roussel

Hoechst Aktiengesellschaft

Aventis Pharmaceuticals Inc.

Gerard J O'Malley

Mark G Palermo

Raymond W Kosley, Jr

Robert J Cherill

Helen H Ong

Michael C Merriman

Eugen Uhlmann

Anuschirwan Peyman

Richard C Allen

Irvin Winkler

Matthias Helsberg

Bettina Spahl

John I White

Udo Hedtmann

Novel spiro&lsqb;cyclopent&lsqb;b&rsqb;indole-piperidines&rsqb;, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro&lsqb;cyclopent&lsqb;b&rsqb;indole-piperidines&rsqb; and intermediates, or compositions thereof are disclosed.

Spiro&lsqb;cyclopent&lsqb;b&rsqb;indole-piperidines&rsqb;

Novel spiro[cyclopent[b]indole-piperidines], intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro[cyclopent[b]indole-piperidines] and intermediates, or compositions thereof are disclosed.

Spiro[cyclopent[b]indole-piperidines]

This application relates to compounds of the formula ##STR1## wherein R.sup.1,X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.

Substituted 3-(aminoalklamino)-1,2-benzisoxazoles and related compounds

The invention relates to compounds of the formula I ##STR1## where R.sup.1 is H, alkyl, acyl, aryl, or a phosphate residue; R.sup.2 is H, OH, alkoxy, NH.sub.2, or halogen; B is a base customary in nucleotide chemistry; a is O or CH.sub.2 ; n is an integer from 1 to 100; W=O, S or Se; V=O, S, or NH; Y=O, S, NH, or CH.sub.2 ; Y'=O, S, NH, or alkylene; X=OH or SH; U=OH, SH, SeH, alkyl, alkoxy, aryl, aryloxy, or amine, and Z=OH, SH, SeH, an optionally substituted radical from the group comprising alkyl, aryl, heteroaryl, alkoxy, or amino, or a group which favors intracellular uptake or serves as the label of a DNA probe or attacks the target nucleic acid during hybridization, where if Z=OH, SH, CH.sub.3, or OC.sub.2 H.sub.5, at least one of the groups X, Y, Y', V, or W is not OH or O or R.sup.1 is not H; a process for their preparation and their use as inhibitors of gene expression, as probes for detecting nucleic acids and as aids in molecular biology.

Oligonucleotide analogs, their preparation and use

This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful or the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.

Substituted 3-(aminoalkylamino)-1, 2-benzisoxazoles and related compounds

Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.

Carbamoyloxylabdanes

Carbamoyloxlabdanes

Novel spiro�cyclopent�b!indole-piperidines!, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the spiro�cyclopent�b!indole-piperidines! and intermediates, or compositions thereof are disclosed.

Spiro�cyclopent�b!indole-piperidines!

This application relates to compounds of the formula ##STR1## wherein R.sup.1, X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.

Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds

These are disclosed novel 2-(piperidin-4-yl, pyridin-4-yl and tetrahydropyridin-4-yl)benzofuran-7-ol and carbamate derivatives of the formula ##STR1## where the substituents are as defined in the specification, which are useful as acetylcholinesterase inhibitors and as such may be useful for the treatment of Alzheimer's disease and other senile dementias.

2-(piperidin-4-yl, pyridin-4-yl and tetrahydropyridin-4-yl)

The present invention relates to novel oligonucleotide analogs with valuable physical, biological and pharmacological properties, and a process for their preparation.

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Newtown, PA, United States of America

Gerard J O'Malley