Vanderbilt University

Wayne State University

The Procter Gamble Company

The United States of America As Represented by the Department of Health

Biomide Investment Limited Partnership

Radiation Oncology Center Research and Development Corporation

Carl R Johnson

Kenneth V Honn

Lawrence J Marnett

Yung-Fa Chen

Katsu-ichi Shimoji

Kenneth Alan Jacobson

John A Secrist, Iii

John M Janusz

Kamal N Tiwari

John D Taylor

Heaok Kim Jeong

Thomas D Penning

Gilles Gorins

Matthew P Braun

Suhaib M Siddiqi

Chandrawansha Bandara Senanayake

Soan Cheng

Dihydrobenzopyran and related compounds useful as anti-inflammatory

The present invention provides A.sub.3 selective agonists, particularly, adenine compounds having selected substituents at the 2, 6, and 9 positions, and related substituted compounds, particularly those containing substituents on the benzyl and/or uronamide groups, as well as pharmaceutical compositions containing such compounds. The present invention also provides a method of selectively activating an A.sub.3 adenosine receptor in a mammal, which method comprises acutely or chronically administering to a mammal in need of selective activation of its A.sub.3 adenosine receptor a therapeutically or prophylactically effective amount of a compound which binds with the A.sub.3 receptor so as to stimulate an A.sub.3 receptor-dependent response.

A.sub.3 adenosine receptor agonists

A process for the preparation of R.alpha.-cyclopentenoids and then R.alpha., R.omega.-cyclopentanoids is described. The process involves the reaction of a compound of the formula ##STR1## where X is halo, particularly Br or I and P is a protecting group with an alkylborane to produce the R.alpha.-cyclopentenone. The R.alpha.-cyclopentenone is reacted with a R.omega. cuprate to produce the R.alpha., R.omega.-cyclopentenoid. The process is used for the preparation of prostaglandins which are known pharmaceutically active compounds.

Process for the preparation of a R-alpha cyclopentenones and R-alpha and

This invention is related to a cyclic hydroxamic acid of the formula: ##STR1## wherein R.sup.1 is C.sub.1-24 alkyl and R.sup.2 is benzyl.

Cyclic hydroxamic acids

Novel aryl aliphatic acids or derivatives thereof of the general formula

Aryl aliphatic acids

Novel cyclic hydroxamic acids of the general formula: ##STR1## wherein ring A is 5- or 6-membered; R.sup.1, R.sup.2 and R.sup.3 each, ipendently, is hydrogen, C1-24 alkyl, C2-24 alkenyl or a group of the formula: ##STR2## wherein R.sup.4, R.sup.5, R.sup.7 and R.sup.8 each, independently is hydrogen,

Cyclopentanoids (I) of the formula: ##STR1## including stereoisomers are described along with a process for the preparation of I. In particular the preparation of prostanoids of the formula: ##STR2## wherein R.sub.1 is a alkyl group containing 1 to 8 carbon atoms and R.sub.2 CO.sub.2 R.sub.3 is an alkenyl ester group, R.sub.2 contains 2 to 6 carbon atoms and R.sub.3 is a lower alkyl group containing 1 to 6 carbon atoms is described. A particular prostaglandin prepared by the process is PGE.sub.2. The prostanoids have been demonstrated to have pharmacological activity in animals and humans. Novel intermediates of (I) are also described.

Process for the preparation of cyclopentanoids and novel intermediates

Novel nitrone substituted 4-aryl dihydropyridines of the formula: ##STR1## are described along with a process for their preparation. The compounds exhibit calcium channel blocker and antimetastatic acitivity.

4-(nitrone aryl) dihydropyridines

Growing community of inventors

Detroit, MI, United States of America

Carl R Johnson