Theravance, Inc.

Achaogen, Inc.

Theravance Biopharma R&d Ip, LLC

Cipla Usa, Inc.

Adam Aaron Goldblum

Paul Ross Fatheree

Daniel D Long

Seok-Ki Choi

Daniel Marquess

S Derek Turner

James Bradley Aggen

Martin Sheringham Linsell

Paola Dozzo

Roland Gendron

Micah James Gliedt

Darin James Hildebrandt

Daniel G Genov

Heinz Ernst Moser

Lan Jiang

Timothy Robert Kane

Robert S Chao

Jyanwei Liu

Raissa Trend

Michael Dappen

Christopher E Henry

Ricardo Filipe De Jesus Gonçalves Mendonça

João Carlos Falcão Sardinha

Stephen Hanessian

Alexandre Giguère

Justyna Grzyb

Juan Pablo Maianti

Darin Hildebrandt

Derek S Turner

The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds, as well as to related intermediates, and crystal forms thereof, useful in such methods.

Synthesis of antibacterial aminoglycoside analogs

Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q, Q, Q, Rand Rare as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Antibacterial aminoglycoside analogs

The invention provides novel quinolinone-carboxamide 5-HTreceptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HTreceptor activity, and processes and intermediates useful for preparing such compounds.

Quinolinone-carboxamide compounds as 5-HT4 receptor agonists

The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HTreceptor activity, and processes useful for preparing such crystalline salt forms.

Crystalline form of a quinolinone-carboxamide compound

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Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q, Q, Q, R, Ror Rare as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

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Berkeley, CA, United States of America

Adam Aaron Goldblum