Allergan, Inc.

Allergan Sales, Inc.

Ash Stevens, Inc.

Stephen A Munk

James A Burke

Michael E Garst

Ken Chow

Daniel W Gil

Larry Allen Wheeler

Dale A Harcourt

Todd M Heidelbaugh

Dario G Gomez

Ronald K Lai

Pranab K Gupta

A process for substantially enhancing the regio and stereoselective synthesis of 9-&#x3b2;-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-&#x3b2;-D- or L-purine nucleoside analogs were obtained. This regio and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs and in particular 2'-deoxy, 3&#x2032;-deoxy, 2&#x2032;-deoxy-2&#x2032;-&#x3b2;-fluoro and 2&#x2032;,3&#x2032;-dideoxy-2&#x2032;-&#x3b2;-fluoro purine nucleoside analogs in high yield without virtually any formation of the 7-positional isomers. The compounds are drugs or intermediates to drugs.

Process for the preparation of 9-&#x3b2;-anomeric nucleoside analogs

Methods and compounds for the treatment of conditions including pain, particularly chronic pain, glaucoma or elevated intraocular pressure with reduced cardiovascular or sedative side effects. Also included are methods of making and using such compounds.

Imidiazoles having reduced side effects

Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents

Methods of treating glaucoma or elevated pressure and other diseases with reduced side effects by treating a mammal in need thereof an agonist of the alpha 2B or alpha 2B/2C adrenergic receptor(s). Also described are compounds having such selective agonist activity.

Methods of treating pain and other conditions

A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

Comformationally rigid bicyclic and adamantane derivatives useful as

Methods are disclosed for treating a mammal with a condition that responds to .alpha.2 agonist treatment without causing cardiovascular side effects using compounds of the formula ##STR1## wherein R.sub.1 is H, alkyl or 1 to 4 carbon atoms or a halogen atom, X is O or NH and A is H or an oxo group and wherein said compound does not cause a concomitant reduction in blood pressure of said mammal.

Aryl-imidazolines and aryl-imidazoles useful as .alpha.-2 adrenergic

A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

Growing community of inventors

Northville, MI, United States of America

Stephen A Munk