Sharps Associates

Sisa Incorporated

Beth Israel Deaconess Medical Center, Inc.

Arthur D. Little, Inc.

The Beth Israel Hospital Association

Miles Laboratories, Inc.

Sisa Pharmaceutical Laboratories, Inc.

The John C. Sheehan Institute for Research, Inc.

Sheehan Institute for Research, Inc.

Raj Kumar Razdan

Harry George Pars

Haldean Cloyce Dalzell

John C Sheehan

Louis Selig Harris

Anil C Ghosh

Peter C Meltzer

Howard Paul Sard

Richard J Sharpe

Kenneth A Arndt

Martin Winn

Stephen J Galli

Joyce Ruth Krei

James E Quick

Patricia Herlihy

Barbara Zitko Terris

Stephen L Galli

Barbara Z Terris

A method for the treatment of a cutaneous, ocular, or mucosal pathological condition which is associated with immune response in a human or other mammal, that includes topical application of an effective amount of spiperone or a spiperone derivative or its pharmaceutically acceptable salt, in a pharmaceutically-acceptable diluent or carrier for topical application.

Topical application of spiperone or derivatives thereof for treatment of

Use of spiperone or spiperone derivatives as immunosuppressant agents

A method for suppressing an immune response in a mammal by treating the mammal with an effective amount of spiperone derivative that is without significant neuroleptic effect due to decreased binding to serotonin and/or dopamine receptors as compared with unmodified or uncomplexed spiperone, or due to topical application which maximizes local immunosuppression while limiting systemic absorption and neuroleptic effects. The spiperone derivatives are capable of inhibiting classic contact hypersensitivity reactions.

Use of spiperone derivatives as immunosuppressant agents

A method for suppressing an immune response in a mammal by systemically treating the mammal with an effective amount of buspirone that is capable of inhibiting classic contact hypersensitivity reactions.

Buspirone as a systemic immunosuppressant

The present invention involves 7-carboethoxymorphinan-6-one compounds of the formula: ##STR1## These compounds are useful as analgesic and/or narcotic antagonists.

7-Carboethoxy-morphinan-6-one compounds

Disclosed is the novel analgesic/narcotic antagonist 17-cyclopropylmethyl-3-hydroxy-14-methoxy-7.alpha.-methyl-morphinan-6-one.

17-Cyclopropylmethyl-3-hydroxy-14-methoxy

Disclosed are certain 14-ethoxymorphinan-6-one compounds exhibiting analgesic and, in some cases, mixed analgesic/narcotic antagonist activity.

N-Cyclopropylmethyl-14-ethoxymorphinan-6-one compounds exhibiting mixed

Disclosed are 4,5.alpha.-epoxy-3-hydroxy or methoxy-7-(1-hydroxyalkyl or 1-oxoalkyl)morphinan-6-one compounds characterized by the structural formulae: ##STR1## In the foregoing formulae R is methyl, cyclopropylmethyl, cyclobutylmethyl, propargyl, allyl, dimethylallyl, cis-chloroallyl or furfuryl; R.sub.1 is H or methyl; R.sub.2 is straight or branched chain alkyl of from 1 to 10 carbon atoms, aryl, substituted aryl or arylalkyl, in which the alkyl group contains from 1 to 6 carbon atoms, and R.sub.3 is a straight chain alkyl of 1 to 4 carbon atoms.

4,5.alpha.-Epoxy-3-hydroxy or methoxy-7-(1-hydroxy-alkyl or

Disclosed are 14-methoxy substituted 3-hydroxy or 3-methoxy -6-one morphinans characterized by the structural formula: ##STR1## wherein R is H or methyl; R.sub.1 is H, .alpha. methyl or .beta. methyl; and R.sub.2 is cyclobutylmethyl, cyclopropylmethyl, tetrahydrofurfuryl or dimethylallyl. The compounds of the present invention are variously useful as analgesics, narcotic antagonists and mixed analgesics/narcotic antagonists.

14-Methoxymorphinan-6-one compounds and therapeutic methods of treating

Disclosed is 17-cyclopropylmethyl-14-hydroxy-3-methoxymorphinan-6-one. This compound is a mixed agonist (analgesic)/narcotic antagonist and therefore useful for the treatment of moderate to severe pain without the liability of inducing physical dependence.

17-Cyclopropylmethyl-14-hydroxy-3-methoxymorphinan-6-one and method of

Disclosed is 17-cyclobutylmethyl-4,5.alpha.-epoxy-3-hydroxy-14-methoxy-8.alpha.-methylm orphinan-6-one characterized by the formula: ##STR1## This compound is useful as a mixed analgesic/narcotic antagonist.

17-Cyclobutylmethyl-4,5.alpha.-e

Tetrahydrodibenzopyrans having the structure ##STR1## in which R.sub.1 is hydrogen or acetyl and R.sub.2 is alkyl having from 1 to 4 carbon atoms are effective anti-glaucoma agents, free from all but a very small amount of CNS activity, when applied topically.

Anti-glaucoma composition and method

Tetrahydrodibenzopyrans having the structure ##STR1## in which R, R.sub.1, and R.sub.2 are alkyl having from 1 to 4 carbon atoms and ophthalmologically acceptable acid addition salts thereof are effective anti-glaucoma agents, free from all but a very small amount of CNS activity, when applied topically.

Composition and method for treating glaucoma

(-)-6A,10A-Trans-1-hydroxy-3-n-pentyl-6,6,9-trimethyl-6a,7,8,10a-tetrahydro dibenzo[b,d]pyran and related pyrans are prepared by a one-step process from (+)-p-mentha-2,8-dien-1-ol and substituted resorcinols. The pyrans produced by the process of this invention have useful pharmacological properties.

Process for the preparation of

Benzopyrano[3,4-d]pyridine-2-cyano, carboxamidoximes and carboximidates of the formula ##STR1## wherein R represents -C.ident.N, ##STR2## R.sub.1 is a lower alkyl, R.sub.2 is hydrogen or a lower alkyl and R.sub.3 is a straight or branched alkyl having 1 to 20 carbons, a cycloalkyl-lower alkyl group in which the cycloalkyl group has 3 to 8 carbons or it is an arylalkyl group, and R.sub.4 is a lower alkyl group. The compounds are useful for lowering blood pressure.

Growing community of inventors

Belmont, MA, United States of America

Raj Kumar Razdan