Millennium Pharmaceuticals Limited

Eli Lilly and Company

Millenium Pharmaceuticals, Inc.

James P Kanter

Robert M Scarborough

Anjali Pandey

James Robinson

Craig Grant

Graeme Langlands

Bing-Yan Zhu

Yonghong Song

Zhaozhong Jon Jia

Wenrong Huang

John J G Mullins

Keiko Sujino

Sharique Sami Zuberi

Gerd Ruhter

Barbara S Briggs

Carroll Scarborough, Legal Representative

Uko Effiong Udodong

Derek Walker

Milton Zmijewski, Jr

Thomas Hense

Daniel Verral, Ii

The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I. 

Pharmaceutical salts and polymorphs of a factor Xa inhibitor

Novel methods of preparing a compound of Formula I which is an inhibitor of Factor Xa and its maleate salt, are described herein. 

Methods of synthesizing pharmaceutical salts of a factor Xa inhibitor

The present invention provides methods for preventing or treating a condition characterized by undesired thrombosis in a mammal using a crystalline polymorph form of a maleate salt of a compound of Formula I that has activity against mammalian factor Xa. 

Methods of using crystalline forms of a salt of a factor Xa inhibitor

The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Novel processes for producing enantiomerically enriched and enantiomerically pure compositions of 2-acyl substituted chromane compounds, and 2-acylchromane compounds that are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors are disclosed. Further disclosed are processes for producing salts such as acid addition salts for such enantiomerically enriched compositions.

Synthesis of 2-acyl substituted chromanes and intermediates thereof

Disclosed are processes for producing chromane compounds, preferably chroman-2-yl acetic acid compounds and 6-amino-chroman-2-yl acetic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors.

Methods for producing amino substituted chromanes and intermediates thereof

Disclosed are process steps and novel processes for producing chromane compositions enriched in at least one (2R or 2S) enantiomer, preferably chroman-2-yl carboxylic acid compounds and chroman-2-yl carboxylic acid esters which are intermediates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are enzymatic processes for resolving chiral intermediates or final products to provide desired enantiomers.

Methods for producing chiral chromones, chromanes, amino substituted chromanes and intermediates therefor

Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Inhibitors of factor Xa

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San Ramon, CA, United States of America

James P Kanter