Eli Lilly and Company

Scott Martin Sheehan

Brian Morgan Watson

Michael Robert Wiley

John Walter Liebeschuetz

Christopher William Murray

John Joseph Masters

Stephen Clinton Young

Stuart Donald Jones

Nicholas Paul Camp

William Alexander Wylie

David Birenbaum Engel

Peter Guzzo

Larry C Blaszczak

Qing Shi

Michael Alan Robertson

Shon Roland Pulley

Michael John Mayer

James E Audia

Brian Michael Mathes

Dustin James Mergott

Larry Chris Blaszczak

James Edmund Audia

The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C-Calkyl, C-Cfluoroalkyl, and &#x2014;OR12; R9 is selected from H &#x2014;NR13C(O)R14 and &#x2014;C(O)NR10R11; R12 is selected from H, C-Calkyl and C-Ccycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes. 

Pyridine derivatives as dipeptedyl peptidase inhibitors

The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C-Calkyl, aryl, heteroaryl, C-Calkylaryl, C-Calkylheteroaryl, C-Calkyl-O&#x2014;C-Calkyl, C-Chaloalkyl, hydroxy C-Calkyl, &#x2014;C(O)R9 and &#x2014;SOR9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, &#x2014;C(O)NR13R14, C-Calkyl, aryl, heteroaryl, C-Calkylaryl, C-Calkylheteroaryl, C-Calkyl-O&#x2014;C-Calkyl and hydroxy C-Calkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH, CF, aryl, heteroaryl, C-Calkylaryl or C-Calkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes. 

1-amino linked compounds

The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C-Calkyl, C-Cfluoroalkyl, and &#x2014;OR12, R9 is selected from H and &#x2014;C(O)NR1OR1 1, R12 is selected from H, C-Calkyl and C-Ccycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes. 

Phenyl compounds and their use in the treatment of Type II diabetes

The present invention provides BACE inhibitors of Formula I: methods for their use, and intermediates and methods for their preparation.

BACE inhibitors

Compounds of formula (I) in which R, n, Z, Rand Rhave any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of thrombotic disorders.

Factor Xa inhibitors

Compounds of formula (I) in which R, X, Y, Cy, L and Lp(D)have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.

Serine protease inhibitors

Compounds of formula (I)in which R, X, Y, Cy, L and Lp(D)have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.

The compound 1-(indole-6-carbonyl-D-phenylglycinyl)-4-(1-methylpiperidin-4-yl)piperazine and physiologically-tolerable salts thereof are factor Xa inhibitors useful for the treatment of thrombotic disorders.

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Carmel, IN, United States of America

Scott Martin Sheehan