Eli Lilly and Company

Leland O Weigel

James E Audia

David E Lawhorn

Charles David Jones

Kenneth S Hirsch

Loretta A McQuaid

Randall K Atkins

Perry C Heath

Gilbert S Staten

John M Schaus

Michael Robert Wiley

Gerald Floyd Smith

John Joseph Masters

David Kent Herron

Ying Kwong Yee

James Joseph Droste

David Mendel

Jeffry Bernard Franciskovich

Leander Merritt

Robert D Titus

Diane L Huser

Andrew Michael Ratz

Angela Lynn Marquart

Christopher William Doecke

Uko Effiong Udodong

John Brennan

Lawrence E Patterson

Jared Harris Linebarger

This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor (I). 

Antithrombotic ethers

Synthesis of benzo[f]quinolinones

This invention relates to hexa- and octaahydrobenzo�f!quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.

Benzo �F! quinolinones

A 1-pot process for preparing 10b-methyl-3-oxo-benzo[f] quinolines.

Syntheis of benzoquinolinones

This invention relates to hexa- and octahydrobenzo[f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.

Benzo(F)quinolinones

Benzo[f]quinolinones

A method for preparing a new class of protected amino intermediates is provided which utilizes reaction of an imido protected primary amine with a secondary amine. The intermediates thus provided are suitably protected for nucleophilic functionalization on the residue of the primary amine. The desired imido protected amine thus derivatized may be regenerated using acid. Further provided are methods for resolving racemic primary amines. Also provided are .beta.-lactam intermediates protected with the new amino protecting group which are useful in the preparation of .beta.-lactam antibiotics.

Bicyclic .beta.-lactams intermediates having a new amino protecting group

Bicyclic B-lactams intermediates having a new amino protecting group

This invention relates to hexa- and octahydrobenzo [f]quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.

Benzo[F]quinolinones

Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.

Process and intermediates for chiral epoxides

The invention provides compounds of the formula ##STR1## wherein R* is a group of the formula ##STR2## wherein R and R.sup.0 are individually C.sub.1 -C.sub.6 alkyl groups or together form a ring consisting of the nitrogen atom to which they are attached and two to seven carbon atoms, said ring optionally substituted by one or more C.sub.1 -C.sub.6 alkyl and/or C.sub.1 -C.sub.6 substituted alkyl groups;

Amino protecting group

The present invention provides a process for protecting an amino group in a compound exposed to nucleophilic reaction conditions in which the imido group used for protection is reacted with a secondary amine to form an acyl group which protects the amino group during exposure to the nucleophilic reaction conditions, after which the acylamino group may be reacted with an acid to reform the imido group so that the compound may then undergo non-nucleophilic manipulations. Also provided is a resolution method in which diasteriometric compounds having the acylamino group as described above are reacted with acid, and as these diasteriomers react at different rates to form the imido group, the reaction may be monitored so as to isolate the desired product at the appropriate point to maximize optical purity.

Growing community of inventors

Indianapolis, IN, United States of America

Leland O Weigel