Ayerst, Mckenna & Harrison, Inc.

American Home Products Corporation

Andre A Asselin

Leslie G Humber

Thomas A Dobson

Christopher A Demerson

Ivo L Jirkovsky

Gervais Dionne

Amedeo Failli

Clara Revesz

Danilo A Crosilla

Jean A Gauthier

Katherine Voith

Francois T Bruderlein

Herein is disclosed bicyclic-substituted aminoethanol derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for treating hypertension in a mammal.

Bicyclo-heterocyclic nitrogen substituted aminoethanol derivatives

5(Indolyl) and 5(2,3-dihydroindolyl) substituted aminoethanols and their

1,2,3,7,8,12b-Hexahydrobenzo[6,7]cyclohepta[1,2,3-de]isoquinoline derivatives, characterized by having two adjacent oxy substituents at positions 4 and 5 or at positions 5 and 6, are disclosed. Thus, the substituent at position 5 is lower alkoxy or hydroxy and the substituents at positions 4 and 6 are different and are hydrogen or hydroxy. The derivatives are neuroleptic agents, free of extrapyramidal side effects. Methods for the preparation and for the use of the derivatives also are disclosed.

Dioxy hexahydrobenzo[6,7]cyclohepta[1,2,3-de]isoquinoline derivatives

5-Indolyl substituted aminoethanols

7,8,9,10-Tetrahydrobenzo[h]quinolin-9-amine derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 each independently is hydrogen or lower alkyl, or R.sup.1 and R.sup.2 together form a chain of the formula --(CH.sub.2).sub.n -- where n is the integer 4, 5 or 6, are useful for treating depression.

7,8,9,10-Tetrahydrobenzo[h]quinolin-9-amine derivatives and compositions

This invention discloses novel imidazo[2,1-a]pyrrolo[2,1-c][1,4]benzodiazepine derivatives, processes for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful as antiobesity agents to reduce food intake in a mammal.

Imidazo[2,1-a]pyrrolo[2,1-c][1,4]benzodiazepine derivatives, methods of

Herein is disclosed compounds of the formula ##STR1## in which R.sup.1,R.sup.2,R.sup.3,R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.

6,7,8,9-Tetrahydro-1H-benz(g)indol-8-amine derivatives

Herein is disclosed compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 each is hydrogen or lower alkyl or R.sup.1 and R.sup.2 together form an alkylene of the formula (CH.sub.2).sub.n wherein n is an integer from 4 to 6, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.

6,7,8,9-Tetrahydronaphtho(1,2-B)furan-8-amine derivatives and their use

Herein is disclosed compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.

6,7,8,9-Tetrahydro-3H-benz(e)indol-7-amines and a method of dopamine

6,7,8,9-Tetrahydro-3H-benz[E]indol-8-amine derivatives

13-Chloro-octahydrobanzo[6,7]cyclohepta[1,2,3-de]pyrido[2,1-a]isoquinolin-5 -ols, substituted on the piperidine ring with lower alkyl or a cycloalkyl are disclosed. The compounds are useful CNS depressants. Methods for their preparation and use also are disclosed.

13-Chloro-benzocycloheptapyridoisoquinolines and use as neuroleptics

Indole derivatives characterized by having a 1,2,3,4-tetrahydrocarbazole or 1,2,3,4-tetrahydrocyclopent[b]indole nucleus with a hydroxyalkanamine substituent are disclosed. The nucleus is optionally further substituted at various positions. The derivatives are useful diuretic agents, and methods for the preparation and use are also disclosed.

Hydroxyalkanamide tetrahydrocarbazoles

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucelus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

Tricyclic indole derivatives

Herein is disclosed ethanocarbazole derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful for treating depression in a mammal and are represented by the following formula ##STR1## in which R.sup.1 is hydrogen or lower alkyl, R.sup.2 and R.sup.3 each is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom form a 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, 4-morpholinyl or 4-thiomorpholinyl ring, and m is an integer from 0 to 3.

Ethanocarbazole derivatives and antidepressant compositions

Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano-[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucleus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.

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St. Laurent, Canada

Andre A Asselin