Eli Lilly and Company

Sphinx Pharmaceuticals Corporation

Merial Limited

Mary George Johnson

Daniel Jon Sall

Gerald Floyd Smith

Ho-Shen Lin

Minsheng Zhang

Richard Waltz Harper

Kumiko Takeuchi

Jefferson Ray McCowan

Robert J Foglesong

Michael Lyle Denney

Nickolay Y Chirgadze

Michael P Lynch

Jack B Jiang

Alan David Palkowitz

Matthew Joseph Fisher

Jolie Anne Bastian

Michael Enrico Richett

Valentine Joseph Klimkowski

Jennifer Marie Tinsley

Shawn Christopher Miller

Todd Jonathan Kohn

Michael Robert Wiley

Nicholas J Bach

Charles Q Meng

Jeffrey Thomas Mullaney

Mustapha Soukri

Jeffrey B Nichols

Clare Louise Murray

Itta Bluhn-Chertudi

The subject matter disclosed herein is directed to amido-pyridyl ether compounds of formula I: wherein, R, R, R, R, R, R, R, R, R, R, R, R, a, b and d are as described herein, compositions comprising the compounds of formula I, methods for their preparation and methods for their uses against parasites.

Amido-pyridyl ether compounds and compositions and their use against parasites

The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.

Antithrombotic agents

This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.

Thrombin inhibitors

This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.

This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Antithrombotic diamines

The present invention provides compounds having the formula ##STR1## wherein R.sub.1 is alkyl, alkenyl and alkynyl having from 2 to about 20 carbon atoms; R.sub.2, R.sub.3 and R.sub.6 are independently H, phenyl or alkyl having from 1 to about 20 carbon atoms; and R.sub.4 and R.sub.5 are independently H, R.sub.6 imino, or amidino, and pharmaceutically acceptable salts thereof which are useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

1,3-dioxane derivatives having protein kinase C inhibitory activity

##STR1## The present invention provides novel substituted anthraquinones having formula (.alpha.), wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl, or R.sub.1 and R.sub.2 taken together with the adjacent nitrogen atom N form a substituted or unsubstituted cyclic ring which may contain additional heteroatoms; n and m are independently 1, 2, or 3; A is halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2)=NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom; R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl; X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; and R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryl useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

Bis-(hydroxylakylamino)-anthraquinone inhibitors of protein kinase C

The present invention provides novel furocoumarinsufonamide derivatives having the formula ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H or lower alkyl; m, n and p are independently 2, 3, 4, 5 or 6; A is NR.sub.4 (CH.sub.2).sub.P NR.sub.5, NR.sub.6, O or S; R.sub.2 is independently H, lower alkyl or a moiety of the formula ##STR2## useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

Furo-coumarinsulfonamides as protein kinase C inhibitors

The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;

Bis-(hydroxyalkylamino)-anthraquinone inhibitors of protein kinase C

The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, alkyl, aryl, or arylalkyl;

1,4-bis-(amino-hydroxyalkylamino)-anthraquinones for inhibiting protein

Growing community of inventors

Durham, NC, United States of America

Mary George Johnson