Washington University

Other

Siga Pharmaceuticals, Inc.

Medimmune Limited

Quretech Bio Ab

Scott J Hultgren

Jerome Pinkner

Matti Juhani Lepisto

Charles Hal Jones

Jan Kihlberg

Zheng Xu

Meta Kuehn

Derek Ogg

Mark Harris

James Walter Janetka

Fredrik Almqvist

Zhenfu Han

Corinne Cusumano

Michael G Caparon

Jerry Pinkner

Solomon Langermann

Ana L Flores-Mireles

Nils Pemberton

Veronica Aberg

Andreas Larsson

Frederic G Sauer

Dennis E Hruby

Christopher S Liu

Gabriel Enrique Soto

Gabriel Waksman

Christine Auguste

Christine A Franke

Klaus Fuetterer

Devapriya Choudhury

Stefan D Knight

Michelle Barnhart

Frederic Almqvist

Hans Emtenas

Hal C Jones

Amy K Evans

Vasilios Kalas

Vishnu Damalanka

Amarendar Maddirala

Pardeep Singh

Aaron James Leonard Lynch

Ana Lidia Flores Mireles

Anders Lindgren

The present disclosure provides a compound of Formula I, or a pharmaceutically acceptable salt thereof.

Ring-fused thiazolino 2-pyridones, methods for preparation thereof and their use in the treatment and/or prevention of a disease involving gram-positive bacteria

The present invention is directed to various compounds, compositions, and methods for treating bacterial infections such as urinary tract infections.

Compounds and methods for treating bacterial infections

The present invention relates to compositions comprising EbpA and methods of use thereof. Specifically, methods useful in the treatment and prevention of EbpA-associated infections.

Compositions and methods for the treatment and prevention of Ebp pilus-related diseases

The present invention encompasses compounds and methods for treating urinary tract infections.

The present invention encompasses compounds and methods for treating and preventing bacterial infections specifically urinary tract infections and those caused by bacteria containing type 1 pili and FimH. The present invention also encompasses compounds and methods for treating inflammatory bowel disease specifically Crohn's Disease.

Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in this application. The present compounds may be employed to inhibit biofilm formation and thereby inhibit adherence of bacteria to a host cell.

Amino methylated 2-pyridinones

Many Gram-negative pathogens assemble adhesive pili structures on their surfaces that allow them to colonize host tissues and cause disease. The present invention relates to novel compounds that mimic a chaperone G1 beta-strand or an amino terminal motif of a pilus subunit. The present invention also relates to the complex formed from the binding of such mimic compounds to the hydrophobic groove of a pilus subunit. Competitively interacting with the binding site of pili subunits will negatively affect the chaperone/usher pathway, which is one molecular mechanism by which Gram-negative bacteria assemble adhesive pili structures, and thus prevent or inhibit pilus assembly.

Anti-bacterial compounds directed against pilus biogenesis, adhesion and activity; co-crystals of pilus subunits and methods of use thereof

Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.

Treatment or prophylaxis of diseases caused by pilus-forming bacteria

A protein construct comprising a pilus protein portion, preferably a structurally stabilized pilus-protein, and an additional, or effector, portion other than a pilus protein or chaperone and wherein said effector portion serves to stabilize the pilus protein portion and to confer a therapeutic activity, such as vaccine activity or anti-microbial or anticancer activity, on the protein construct is disclosed. Such effector portion commonly comprises a donor strand complementary segment capable of structurally stabilizing a pilus protein subunit and attaching the auxiliary portion to said subunit to form the pilus protein analog of the invention. Methods of using said protein constructs are also disclosed as well as the formation and use of analogs comprising fragments of a pilus protein linked to effector components to produce immunogenic and/or therapeutic activity.

Therapeutic compounds structurally-linked to bacterial polypeptides

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Town & Country, MO, United States of America

Scott J Hultgren