Eli Lilly and Company

Mark Alan Richardson

Brian W Grinnell

David Thompson Berg

George J Cullinan

Paul R Rosteck, Jr

Stuart A Kuhstoss

Ramachandra N Rao

Stanley Gene Burgett

The present invention provides methods of inhibiting PAI-1 using benzopyrans.

Effect of compounds that suppress induction of plasminogen activator

Novel benzothiophenes, and intermediates thereof, and the uses and formulations thereof, are provided by the present invention.

Benzothiophene compounds, and uses and formulations thereof

Novel benzothiophenes, ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 are independently --OH, --OCO(C.sub.1 -C.sub.6 alkyl), --O(CO)O(C.sub.1 -C.sub.6 alkyl), --OCO--Ar, where Ar is phenyl or substituted phenyl, or --O(CO)O--phenyl; and R.sub.4 is N-pyrrolidinyl, N-piperidinyl, or N-hexamethyleneimino, and intermediates thereof, and the uses and formulations thereof, are provided by the present invention.

Benzothiopene compounds, and uses and formulations thereof

A DNA molecule isolated from Streptomyces ambofaciens encodes the multi-functional proteins which direct the synthesis of the polyketide platenolide.

Platenolide synthase gene

Methods of inhibiting plasminogen activator inhibitor 1 comprising administering to a human in need thereof an effective amount of a compound having the formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --H, --C.sub.1 -C.sub.4 alkyl, or taken together with the nitrogen to which they are attached form a pyrrolidine, piperidine, or hexamethyleneimino ring;

Method for inhibiting plasminogen activator inhibitor 1

Benzothiophenes, and uses and formulations thereof, are provided by the present invention.

Benzothiophene compounds, and uses formulations thereof

A method of inhibiting plasminogen activator inhibitor 1 comprising administering to a human in need thereof an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine, hexamethyleneimino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.

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Bloomington, IN, United States of America

Mark Alan Richardson