Astrazeneca Ab

Lieber Institute, Inc.

Lieber Institute for Brain Development

The Johns Hopkins University

Glen E Ernst

James C Barrow

Yifang Huang

Michael Steven Poslusney

John McCauley

Daniel Weinberger

Ingrid Price Buchler

Stephen Connolly

Peter Robert Bernstein

William Frietze

Michael Balestra

David Nugiel

Cathy Dantzman

Megan Murphy King

Lihong Shen

Dominique Swinnen

Eifion D Phillips

Marc Chapdelaine

Greg A Hostetler

Richard Schmiesing

Marikki Laiho

Thomas Hudzik

Sara Sanders

Florian Montel

Khanh Bui

Sabine Defays

Dannielle Kissel

Laureen Colis

Pablo De León

Sarah Sanders

Pablo De Leon

Valerie Hoesch

Jingbo Yan

Jie Liu

Ingrid Buchler

Pyridine carboxamide compounds for inhibiting NaV1.8 and methods for treating a condition, disease, or disorder associated with an increased NaV1.8 activity or expression are disclosed.

Pyridine carboxamide compounds for inhibiting NAV1.8

Pyridazine compounds for inhibiting NaV1.8 and methods for treating a condition, disease, or disorder associated with an increased NaV1.8 activity or expression are disclosed.

Pyridazine compounds for inhibiting Nav1.8

RNA polymerase I (Pol I) is a dedicated polymerase for the transcription of the 47S ribosomal RNA precursor subsequently processed into the mature 5.8S, 18S and 28S ribosomal RNAs and assembled into ribosomes in the nucleolus. Pol I activity is commonly deregulated in human cancers. Based on the discovery of lead molecule BMH-21, a series of pyridoquinazolinecarboxamides were synthesized as inhibitors of Pol I and activators of the destruction of RPA194, the Pol I large catalytic subunit protein. The present invention identifies a set of bioactive compounds, including purified stereoisomers, that potently cause RPA194 degradation that function in a tightly constrained chemical space. Pharmaceutical compositions comprising these compounds and their uses in cancer and other Pol I related diseases is also provided.

Compounds which inhibit RNA polymerase, compositions including such compounds, and their use

Compounds that inhibit COMT enzyme and pharmaceutical compositions comprising the same are provided herein. Methods of treating various psychiatric and neurological disorders with the compounds and pharmaceutical compositions described herein are also provided.

COMT inhibiting methods and compositions

The present inventions include a method of inhibiting COMT enzyme in a subject as well as compounds of formula I, or a pharmaceutically acceptable salt thereof, that are useful in the treatment of various disorders mediated by COMT, including Parkinson's disease and/or schizophrenia. 

The present invention is directed to ethanamine compounds, pharmaceutical compositions comprising the same, and methods of treating depression by administering the ethanamine compound.

Ethanamine compounds and methods of using the same

Ethanamine compounds and methods of using the same 545

N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, pharmaceutically acceptable salts thereof, and/or mixtures thereof, as well as, pharmaceutical compositions thereof, methods of treatment therewith, and processes of making N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide and intermediates thereof.

N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl

N-(2-hydroxyethyl)-N-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide

Compounds of Formula I: and pharmaceutically-acceptable salts thereof, wherein Q, E and D are as defined in the specification, enantiomers, in vivo-hydrolysable precursors, pharmaceutical compositions and formulations containing them, methods of using them to treat diseases and conditions either alone or in combination with other therapeutically-active compounds or substances, processes and intermediates used to prepare them and uses of them for diagnostic and analytic purposes.

Non-amide nonanes

There are provided novel compounds of formula (I) wherein A, R, R, R, R, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory diseases, pain and CNS diseases.

Compounds for the inhibition of nitric oxide synthase

There are provided novel compounds of formula (I) wherein A, R, R, R, R, T, U, V, W, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory diseases, pain and CNS diseases 

Compounds useful for the treatment of pain in accord with the following structural diagram,wherein R, R, R, Rand Rare any of a number of groups as defined in the specification, A and D are as defined in the specification, and pharmaceutical compositions and methods of treatment utilising such compounds.

N-type calcium channel antagonists for the treatment of pain

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Wilmington, DE, United States of America

Glen E Ernst