Texas Biotechnology Corporation

Signal Pharmaceuticals, Inc.

Immunopharmaceutics, Inc.

Pharmacopeia Drug Discovery, Inc.

Encysive Pharmaceuticals, Inc.

Pharmacopeia Inc.

Adam Kois

Ming Fai Chan

Vitukudi Narayanaiyengar Balaji

Chengde Wu

Bore G Raju

Rosario Silvestre Castillo

Erik Joel Verner

Venkatachalapathi Yalamoori

Yoshitaka Satoh

Moorthy S S Palanki

Shripad S Bhagwat

Timothy P Kogan

Veronique Plantevin-Krenitsky

Marianne Sloss

Robert Hilgraf

Ronald J Albers

Meg McCarrick

Kiran Sahasrabudhe

Maria Mercedes Delgado Mederos

Steven Spencer Clareen

Jonathan Wright

Lisa Nadolny

Leticia Ayala

Kevin Hughes

Elise Sudbeck

John J Sapienza

Paul E Erdman

Jason Parnes

Graziella I Shevlin

Bernd M Stein

Sayee Gajanan Hegde

Jeffrey A McKie

Moorthy S Palanki

Leah Marie Gayo-Fung

David Wesley Anderson

Kalyanaraman Ramnarayan

Mary Doubleday

Sak Khammungkhune

Ravi Kumar Jalluri

Karen J MacFarlane

Meg Mccarrick

Ian Henderson

Andrew Graham Cole

Andrew G Cole

Venkatachalapathi Yalamorri

May S Sutherland

Yalamoori Venkatachalapathi

Marianne K Sloss

Moorthy SS Palanki

Kiran c/o Wilson Sonsini Goodrich Sahasramudhe

Sayee G c/o Wilson Sonsini Goodrich  Hegde

Sayee Hedge

Marian Sloss

Ronald Albers

Kiram Sahasrabudhe

Moorthy Ss Palanki

Karen J Macfarlane

Jason S Parnes

Provided herein are Aminopurine Compounds having the following structure: 

Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith

Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein Rand Rare as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto

Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure:wherein Rand Rare as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.

Biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, bicyclic or tricyclic carbon or heterocyclic ring biphenylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin

N-(5-isoxazolyl)benzenesulfonamides and N-(3-isoxazolyl)benzenesulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. N-isoxzolyl-4-biphenylsulfonamides are particularly preferred. These compounds exhibit activity as endothelin receptor B antagonists. Methods for treating endothelin-mediated disorders, particularly inflammatory diseases, such as asthma, by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Benzenesulfonamides and the use thereof to modulate the activity of endothelin

Compounds and methods for modulation of estrogen receptors

Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin

N-alkyl, N-alkenyl, N-alkynyl, N-aryl and N-fused bicyclo or tricyclo thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, (phenyl) and (phenoxy)thienylsulfonamides, (phenyl) and (phenoxy)furylsulfonamides, and (phenyl) and (phenoxy)pyrrolylsulfonamides and methods of using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

N-Alkyl, N-Alkenyl, N-Alkynyl, N-Aryl and N-fused bicyclo or tricyclo thienyl-, furyl-,and Pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin

Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same:

Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1):

Substituted phenyl compounds and derivatives thereof that modulate the activity of endothelin

N-(5-isoxazolyl)benzenesulfonamides and N-(3-isoxazolyl) benzene-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(5-isoxazolyl)-biphenylsulfonamides and N-(3-isoxazolyl)biphenylsulfonamides and methods for inhibiting the binding of an endothelin peptide to an endothelin receptor or increasing the activity of endothelin peptides by contacting the receptor with a sulfonamide are provided. N-isoxzolyl-4-biphenylsulfonamides are particularly preferred. These compounds exhibit activity as endothelin receptor B antagonists. Methods for treating endothelin-mediated disorders, particularly inflammatory diseases, such as asthma, by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Benzenesulfonamides and the use thereof to modulate the activity of

Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (I): ##STR1## where X and Y are selected from groups that include O, S, and NH; and Ar.sup.1, Ar.sup.2 and Ar.sup.3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteraryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

Substituted phenyl compounds and derivatives thereof that modulate the

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San Diego, CA, United States of America

Adam Kois