Abbott Laboratories Corporation

David L Arendsen

John F DeBernardis

Martin Winn

Robert E Zelle

Jyoti R Patel

David M Stout

Philip R Kym

John K Pratt

Steven Armen Boyd

Andrew O Stewart

Meena V Patel

Gui-Dong Zhu

Pramila A Bhatia

Irini Akritopoulou-Zanze

Nicholas A Mort

Indrani W Gunawardana

Catherine M McCarty

Michael A Staeger

Jennifer C Freeman

Tom Von Geldern

Carl W Nordeen

Benjamin C Lane

Jehrod Brenneman

Kraig Lartey

Kevin R Condroski

David S Garvey

Wang Shen

Gerard M Sullivan

David John Augeri

Bryan K Sorensen

Todd Warren Rockway

William J McClellan

Saul H Rosenberg

Anthony K Fung

Stephen J O'Connor

James T Link

William R Baker

Herman H Stein

Harold Elmer Zaugg

Kresna Hartandi

Stephen A Fakhoury

Gaoquan Li

Rajnandan N Prasad

Kimba L Ashworth

Glucocorticoid receptor antagonists for treatment of diabetes

Glucocorticoid receptor modulators

Cell adhesion-inhibiting antiinflammatory compounds

The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful for inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.

Inhibitors of squalene synthase and protein farnesyltransferase

The present invention includes compounds represented by the formula: ##STR1## wherein X is O or S;

Aminomethyl-chroman and -thiochroman compounds

The present invention includes compounds represented by the formula: ##STR1## wherein X is O or S; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, hydroxy, halo, loweralkoxy, thioalkoxy and loweralkyl; or R.sub.1 and R.sub.2 taken together can form a methylenedioxy or ethylenedioxy bridge;

Aminomethyl-thiochroman compounds

Aminomethyl-chroman compounds

A method of producing .alpha..sub.2 -adrenergic receptor agonist activity by contacting an .alpha..sub.2 -adrenergic receptor with an effective amount of a compound of the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently selected from hydrogen or loweralkyl of 1 or 2 carbon atoms, or a pharmaceutically acceptable salt thereof.

Method of producing .alpha..sub.2 -adrenergic receptor agonist activity

Disclosed herein are 1-aminomethyl-phthalans represented by the formula ##STR1## wherein R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.10 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R.sub.9 and R.sub.10 can be taken together to form a methylenedioxy or ethylenedioxy bridge; or 1,4-benzodioxan of the formula ##STR5## wherein q is 1, 2 or 3, and R.sub.11 is hydrogen, methoxy, or halo; or R.sub.3 and R.sub.4 can be taken together to form a piperazino, piperidino or morpholino moiety; and the pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and a pharmaceutically acceptable carrier or diluent.

Substituted 1-aminomethyl-phthalans

Disclosed herein are 1-aminoalkyl-3,4-dihydronaphthalenes represented by the formula ##STR1## wherein n is 1 or 2; R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.10 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R.sub.9 and R.sub.10 can be taken together to form a methylenedioxy or ethylenedioxy bridge; or 1,4-benzodioxan of the formula ##STR5## wherein q is 1, 2 or 3, and R.sub.11 is hydrogen, methoxy, or halo; or R.sub.3 and R.sub.4 can be taken together to form a piperazino, piperidino or morpholino moiety; and the pharmaceutically acceptable salts thereof. Also disclosed are novel intermediates useful in the preparation of these compounds.

Aminoalkyl dihydronaphthalenes

Described is a method of treating hypertensive by administering to mammalian patients compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, loweralkyl, lowercycloalkyl, aralkyl, aryl, pyridyl, isoquinolyl, phthalazinyl, or aryl substituted by one or more hydrogen, halo, loweralkyl, lowercycloalkyl, haloloweralkyl, haloloweralkyl, aminosulfonyl, nitro, hydroxy, alkoxy, carboxy, alkoxycarbonyl, cycloalkoxy carbonyl, aminocarbonyl, diloweralkylaminocarbonyl or ##STR2## wherein n is 4 or 5.

Pyrazolyl amino imidazolines as antihypertensive agents

Disclosed are pyrazoles of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, or phenyl, R.sub.2 is hydrogen or lower alkyl, R.sub.3 is alkoxy or hydroxy, R.sub.4 is lower alkyl, and the pharmaceutically acceptable acid addition salts thereof. The compounds are useful primarily as antipsychotic agents. As an example, they exhibit central nervous system activity as antischizophrenic agents.

Pyrazoles active in the central nervous system

A compound of the formula ##STR1## wherein n = 2 or 3; R.sub.1 is a C.sub.3 -C.sub.20 alkyl or arylalkyl; R.sub.2 is loweralkyl or phenyl; and R.sub.3 is H or replaces the hydrogens in (CH.sub.2).sub.n with CH.sub.3 ; and m is 1, 2 or 4. These compounds exhibit central nervous system activity and are useful as antidepressants.

6A-Azacannabinoids

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Libertyville, IL, United States of America

David L Arendsen