Hoechst Roussel Pharmaceuticals

Hoechst Marion Roussel

American Hoechst Corporation

Hoechst-roussel Incorporated

Lawrence L Martin

Manfred Worm

Denise M Flanagan

Charles A Crichlow

Joseph F Payack

Linda L Setescak

Peter A Nemoto

Richard C Effland

Joseph T Klein

Raymond W Kosley, Jr

Helen H Ong

David G Wettlaufer

Gert U Kuerzel

Richard C Allen

Mark G Palermo

Susan J Scott

Vernon B Anderson

Gregory M Shutske

Grover C Helsley

Kevin J Kapples

Brian S Freed

John D Tomer, Iv

R Richard Hamer

Salvatore M Brucato

John I White

Brian J Duffy

Larry A Davis

Victor J Bauer

Charles A Crishlow

There are disclosed various compounds of the formula below, ##STR1## where R, R.sub.1, W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such as Alzheimer's disease, as modulators of neurotransmitter functions such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antienmtics, and for the treatment of personality disorders such as obsessive compulsive disorder.

Substituted pyridylamino indoles

This invention relates to compounds of the formula wherein X, Y, Z, m, n and p are as defined within, pharmaceutical compositions containing these compounds and to their use as antipsychotic agents, particularly in the treatment of schizophrenia. Depot derivatives of the compounds are useful for providing long acting effects of the compounds.

Antipsychotic agents, compositions and method of use

This invention relates to compounds of the formula ##STR1## wherein X, Y, Z, m, n and p are as defined within, pharmaceutical compositions containing these compounds and to their use as antipsychotic agents, particularly in the treatment of schizophrenia. Depot derivatives of the compounds are useful for providing long acting effects of the compounds.

This invention relates to N-hydroxy-dibenz�b,e!oxepinalkylamines, N-hydroxy-dibenz�b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R.sup.1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R.sup.2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.

N-hydroxy-dibenz�b,e!oxepinalkylamines,

This application relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, m and n are as defined in the specification which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants, anxiolytics, atypical antipsychotics, antiemetics, and for the treatment of personality disorders such as obsessive compulsive disorders. Certain of the compounds are also useful as glycine partial agonists.

Substituted aminothienopyridines, pharmaceutical composition and use

Antipsychotic agents, composition and method of use

N-hydroxy-dibenz �b,e!oxepinalkylamines, N-hydroxy-dibenz

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

This invention relates to substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo[b]thiophenes and 1,2-benzisothiazoles of the formula ##STR1## wherein Q is S, N or NR.sub.2 ;

Substituted pyridinylamino-1H-indoles, 1H-indazoles, 2H-indazoles, benzo [b

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.

Growing community of inventors

Lebanon, NJ, United States of America

Lawrence L Martin