Pharmacia Corporation

G.d. Searle & Company

Pfizer Corporation

Warner-lambert Company

Pharmacia Corporation Global Patent Department

Mark A Massa

Deborah A Mischke

Margaret Lanahan Grapperhaus

James A Sikorski

Melvin L Rueppel

Richard C Durley

Lijuan Jane Wang

Yvette M Fobian

Michael B Tollefson

Monica B Norton

William F Vernier

Dale P Spangler

Brian S Hickory

Michele A Promo

Emily J Reinhard

Ashton T Hamme

Barry L Parnas

Jane L Wang

John Jeffrey Talley

John Nicholas Freskos

Bruce D Roth

Donald W Hansen, Jr

Matthew James Graneto

Ish K Khanna

Barnett S Pitzele

Daniel Paul Becker

Robert M Heintz

Timothy J Hagen

David Louis Brown

E Ann Hallinan

Joseph J McDonald

Thomas E Barta

Clara I Villamil

Joseph Gerace Rico

William Chester Patt

Susan Landis Hockerman

Alan Frank Gasiecki

Helen Tsenwhei Lee

Terri L Boehm

Arija A Bergmanis

Steven W Kramer

Ronald Keith Webber

Louis J Bedell

Jeffery N Carroll

Brent V Mischke

Darren J Kassab

Todd M Maddux

Nathan W Stehle

Stephen A Kolodziej

Grace Mary Wagner

Matthew William Mahoney

Edgardo Alvira

Patrick B Mullins

Michelle Ann Schmidt

Michelle A Schmidt

Jon Gordon Selbo

Richard Alan Vonder Embse

Kirby Ray Sample

Ronald Edward Seidel

Scott Santford Woodard

Yiyuan Chen

James A Sikorsky

Mark A Nagy

Thomas A Wynn

Kaliappan Iyanar

The invention relates to compounds of formula (I) processes for their preparation, their use as 5-lipoxygenase inhibitors and pharmaceutical compositions containing the same.

Pyrazole derivatives as 5-LO-inhibitors

The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.

(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity

This invention is directed generally to proteinase (also known as 'protease') inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as 'matrix metalloprotease' or &#x201c;MMP&#x201d;) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A, A, Y, E, E, E, and Rare as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.

Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors

The present invention relates to 2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.

2-amino-2-alkyl-5 heptenoic and heptynoic acid derivatives useful as nitric oxide synthase inhibitors

The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

Substituted aromatic policyclic tertiary-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n&plus;1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n&plus;1)-Alkanol compounds are substituted (R)-Chiral N,N-bis-phenyl aminoalcohols. A preferred specific (R)-Chiral N,N-bis phenyl aminoclcohol is the compound.

(R)-Chiral halogenated substituted n,n-bis-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols. A preferred specific N,N-disubstituted reverse aminoalcohols is the compound:

Use of substituted N, N-disubstituted reverse aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n&plus;1 )-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n&plus;1)-Alkanol compounds are substituted (R)-Chiral N-benzyl-N-phenyl aminoalcohols. A preferred specific (R)-Chiral N-benzyl-N-phenyl aminoalcohol is the compound:

(R)-chiral halogenated substituted n-benzyl-n-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols. A preferred specific N-benzyl-N-phenyl aminoalcohol is the compound:

Substituted n-benzyl-n-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols. A preferred specific N-fused-phenyl-N-benzyl aminoalcohol is the compound:

Substituted N-fused-phenyl-N-benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines. A preferred specific N,N-disubstituted non-fused heterocyclo amine is the compound:

Substituted N,N-disubstituted non-fused heterocyclo amino compounds useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted fused-heterocyclo amines. A preferred specific N,N-disubstituted fused-heterocyclo amine is the compound:

Substituted N,N-disubstituted fused-heterocyclo amino compounds useful for inhibiting cholesteryl ester transfer protein activity

The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols. A preferred specific N-phenoxy-N-phenyl aminoalcohol is the compound:

Substituted N-phenoxy-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity

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Ballwin, MO, United States of America

Mark A Massa