Smithkline Beecham Corporation

Duke University

Glaxo Wellcome Inc.

Glaxo Inc.

Other

Glaxosmithkline LLC

University of Minnesota

Gilead Sciences, Inc.

Robert Anthony Mook

Mui Cheung

Wei Chen

Jiangbo Wang

James Marvin Veal

John Joseph Partridge

Amogh Boloor

Philip Anthony Harris

Herbert K Lyerly

Grady Evan Boswell

James Michael Salovich

Jeffery Alan Stafford

Xiu-rong Ren

Kevin Hinkle

John W Lackey

Roy A Swaringen, Jr

Eric C Bigham

Stephen V Frye

Lawrence S Barak

John J Savarese

Eric Eugene Boros

Kenneth William Batchelor

Kevin Kuntz

Sanjay Shashikant Patel

Brian Wilson

Vincente Samano

Ronda Davis

Hongtao Guo

Amy Hobeika

Mark L Peterson

George F Dorsey, Jr

Mark D Matteucci

Kuei-Ying Lin

Alex Gregory Waterson

Mark Andrew Pobanz

Timothy Mark Willson

Istvan Kaldor

David Needham

David Norman Deaton

Nigel Paul King

Matthew J Sharp

Randolph B DePrince

Jon Loren Collins

Michael J Neeb

David Edward Uehling

Kyle Allen Emmitte

Marcus Brackeen

Kirk Stevens

Brad Richard Henke

John Brad Shotwell

Kristen Elizabeth Nailor

Richard W Wagner

John Mark O'Callaghan

Jason G Lewis

Stephon Cornell Smith

Kevin L Facchine

George S Lewis

Christopher P Lauderman

Greg Alan Erickson

Jeffrey Edmond Cobb

Ronda Davis-Ward

Ronda Gayle Davis-Ward

Ganesh Moorthy

Erich W Baum

Anthony Angelo Ribeiro

H Kim Lyerly

Minyong Chen

Described are methods of treating a disease associated with dysregulation of the Wnt/Frizzled signaling pathway. The methods include identifying subjects in need of therapy, administering inhibitors of the Wnt/Frizzled signaling pathway, pharmaceutical compositions including the inhibitors, and methods of using the compounds and compositions for treating cancer, bacterial and viral infection, lupus, type II diabetes, nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD) in a subject.

Chemical modulators of signaling pathways and therapeutic use

Compounds and pharmaceutical compositions that down-regulate immune checkpoints such as PD-1, PD-L1 and CTLA-4 are provided. Also provided are methods of treating a disease by down-regulating immune checkpoints such as PD-1, PD-L1 and CTLA-4. The methods are useful for treating cancer and viral infection in a subject.

Chemical modulators of immune checkpoints and therapeutic use

Compounds of general Formulas (I), (IA), (IB) are described, along with compositions containing the same and methods of use thereof, inhibiting the hedgehog pathway in a cell or inhibiting unwanted proliferation of a cell.

Smoothened modulators and methods of use thereof

The present invention provides imidazopyridine compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.

Imidazopyridine kinase inhibitors

Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

Pyrimidineamines as angiogenesis modulators

The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

Pyrimidine compounds

Imidazotriazine compounds

Pyrimidine derivatives, which are useful as VEGFR2 inhibitors are described herein. The described invention also Includes methods of making such pyrimidine derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.

A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C,alkyl, C,alkoxy, C,fluoroalkoxy, nitrile, or &mdash;NR,R,where R,and R,are independently hydrogen or C,alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C,alkylene; (v) &mdash;MC,alkylene or C,alkyleneMC,alkylene, wherein M is O, S, or &mdash;NR,wherein R,represents hydrogen or C,alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C,alkyl; and (vii) Het-C,alkylene, wherein Het represents a heterocyclic group as defined in point (vi) above; Alk represents C,alkylene; R,represents hydrogen or C,alkyl; Z is selected from the group consisting of: (viii) &mdash;(C,alkylene) phenyl, which phenyl is optionally substituted by one or more halogen atoms; and (ix) &mdash;NR,R,, wherein R,represents hydrogen or C,alkyl, and R,represents &mdash;Y&mdash;(C&boxH;O)&mdash;T&mdash;R,, or &mdash;Y&mdash;(CH(OH))&mdash;T&mdash;R,.

Substituted 4-hydroxy-phenylalcanoic acid derivatives with agonist activity to PPAR-gamma

Ultrashort acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein: X is a halogen; h is from 1 to 2; Y is hydrogen or methoxy; Z,and Z,are methyl; W,and W,are carbon; and A is a pharmaceutically acceptable anion.

Substituted isoquinolines as ultra short acting neuromuscular blockers

Ultra short acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein q and t are independently from 0 to 4; X,and X,are independently halogen; h,and h,are independenity from 0 to 2; Z,and Z,are indepentdently hydrogen, C,alkyl, C,alkenyl or C,alkynyl with the proviso that Z,and Z,are not both hydrogen; Y,, Y,, and Y,and Y,are independently hydrogen, halogen or C,alkoxy; m and p are independently 1 to 6; n and r are independently 0 to 4; with the proviso the if h,and h,are both 0, then r is 0 and n is 0 to 2; R,to R,are independently hydrogen, halogen, C,alkoxy, or R,and R,together with the carbon atoms to which they are bonded, R,and R,together with the carbon atoms to which they are bonded, R,and R,together with the carbon atoms to which they are bonded, R,and R,together with the carbon atoms to which they are bonded, may independently form a methylenedioxy or ethylenedioxy moiety contained in five- or six-membered ring; W,and W,are carbon; and A is a pharmaceutically acceptable anion.

The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.

Androstenone derivative

The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted arginine, lysine or ornithine residues, or derivatives thereof, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.

Cationic lipids

Growing community of inventors

Durham, NC, United States of America

Robert Anthony Mook