Hoechst Roussel Pharmaceuticals

Hoechst Marion Roussel

Denise M Flanagan

Lawrence L Martin

Raymond W Kosley, Jr

Peter A Nemoto

Joseph F Payack

David G Wettlaufer

Gert U Kuerzel

Richard C Allen

There are disclosed neuroprotective compounds having the formula ##STR1## wherein the moieties are defined in the specification, and processes for making them.

(1H-indol-1-yl)-2-(amino)acetamides and related

Novel 2-(4-piperidinyl)-1H-pyrido[4,3-b]indol-1-ones and related compounds, intermediates and processes for the preparation thereof, and methods of treating psychoses employing compounds and compositions thereof are disclosed.

2-(4-piperidinyl)-1H-pyrido[4,3-b]indol-1-ones and related compounds

There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

1-aminoacetamidopyrroles and 1-amino acetamido-2-(substituted) pyrroles

There are disclosed compounds having the formula ##STR1## wherein the variables are defined in the specification, and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.

(1H-indol-1-yl)-2-(amino)acetamide derivatives and preparation thereof

There is disclosed a process for the preparation of 1-aminoacetamidopyrroles and 1-amino-2-(substituted)-pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias which comprises treating a 1-phthalimidopyrrole of the formula ##STR2## with a base to yield a 1-aminopyrrole of the formula ##STR3## which is reacted with a compound of the formula ##STR4## to obtain the compound of Formula (I).

Process for preparing 1-aminoacetamidopyrroles

There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

1-amino-2-(substituted)pyrroles and related compounds

There are disclosed compounds having the formula ##STR1## wherein X, Y, Z and R.sub.1 -R.sub.6 are defined in the specification and pharmaceutically acceptable addition salts thereof, or where applicable, the optical or geometrical isomers or racemic mixtures thereof, intermediates in the process for making the compounds, a process for making the compounds and pharmaceutical compositions and method of use as neuroprotective agents.

A compound of the formula ##STR1## wherein R.sup.1 is hydrogen, loweralkyl, phenyl, phenyl substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups, phenylloweralkyl or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; R.sup.2 is loweralkyl, furanylloweralkyl, thienylloweralkyl, pyrrolylloweralkyl, pyridinylloweralkyl, phenylloweralkyl, or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; X is hydrogen, loweralkyl, loweralkoxy, halogen, or trifluoromethyl; m is 0 or 1; n is 1 or 2; an optical isomer thereof or a salt thereof.

2-(4-piperidinyl)-1H-pyrido[4,3-b]-indol-1-ones and related compounds

2-(4-pyrrlidinyl)-1H-pyrido[4,3-b]indol-1-ones and related compounds

There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted) pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

There are disclosed compounds having the formula ##STR1## wherein X is hydrogen, chloro, bromo, fluoro, hydroxy, loweralkoxy, arylloweralkoxy, acyloxy, loweralkylaminocarbonyloxy, diloweralkylaminocarbonyloxy, amino, loweralkylamino, diloweralkylamino, acylamino, loweralkyl or trifluoromethyl;

(1H-indol-1-yl)-2-(amino) acetamides and related

A compound of the formula ##STR1## wherein R.sup.1 is hydrogen, loweralkyl, phenyl, phenyl substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups, phenylloweralkyl or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; R.sup.2 is loweralkyl, furanylloweralkyl, thienylloweralkyl, pyrrolylloweralkyl, pyridinylloweralkyl, phenylloweralkyl, or phenylloweralkyl in which the phenyl group is substituted by one or more loweralkyl, loweralkoxy, halogen, or trifluoromethyl groups; X is hydrogen, loweralkyl, loweralkoxy, halogen, or trifluoromethyl; m is 0, 1 or 2; n is 1 or 2; an optical isomer thereof or a salt thereof.

2-(4-piperidinyl)-1H-pyrido[4,3-B]indol-1-ones and related compounds

There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)-pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

1-aminoacetamidopyrroles and 1-aminoacetamido-2-(substituted)pyrroles

This invention relates to compounds of the formula ##STR1## where X is --NH, oxygen, N-loweralkyl, or N-arylloweralkyl; R.sub.1 is hydrogen, loweralkyl, cycloalkyl, aryl, arylloweralkyl, loweralkylene, haloloweralkyl, heteroaryl selected from the group consisting of thienyl, furanyl, pyrrolyl and pyridinyl; heteroarylloweralkyl, heterocyclic selected from piperidinyl, piperazinyl, pyrrolidinyl; or heterocyclicloweralkyl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkyl or arylloweralkyl; R.sub.4 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, arylloweralkyl, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl or loweralkoxycarbonyl; Y is hydrogen, loweralkyl or loweralkoxy, and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful in the treatment of memory impairment characterized by a cholinergic deficit such as that associated with electroshock-induced amnesia and Alzheimer's disease and other senile dementia.

Method of preparing .alpha.-oxopyrrolo[2,3-b]indole acetic acids and

There are disclosed various compounds of the formula below, ##STR1## where the parameters R.sub.1 and R.sub.2 are as defined in the specification, which compounds are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.

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Bridgewater, NJ, United States of America

Denise M Flanagan