Innate Tumor Immunity, Inc.

Novartis Ag

The Scripps Research Institute

University of Florida Research Foundation, Incorporated

Ifm Due, Inc.

Novartis Inflammasome Research, Inc.

William R Roush

Shomir Ghosh

Gary D Glick

Shankar Venkatraman

Hans Martin Seidel

Dong-Ming Shen

Edward James Olhava

Jason David Katz

David Guenther Winkler

Daniel O'Malley

Luigi Franchi

Anthony William Opipari, Jr

Roger A Jones

John L Cleveland

Ashvinikumar V Gavai

Thomas D Bannister

Andy Tsai

Jun Yong Choi

Reji Nair

Jitendra K Mishra

Scott Hunter Watterson

David K Williams

Christine M Tarby

Patrice Gill

Hua Gong

Derek R Duckett

Daiqing Liao

Ryan L Stowe

Steven P Seitz

Prasanna Sivaprakasam

Yong Zhang

Christoph Rader

Jay A Markwalder

Andrew Forrest Donnell

Mathieu Bibian

Alex Nanna

Andrii Monastyrskyi

Laura H Rosenberg

Ronald Rahaim

Alex R Nanna

Roger Jones

Anthony William Opipari Jr

Anthony William Opipari

Andy S Tsai

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

Compounds and compositions for treating conditions associated with NLRP activity

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that modulate (e.g., agonizes or partially agonizes) NLRP3 that are useful, e.g., for treating a condition, disease or disorder in which an increase in NLRP3 signaling may correct a deficiency in innate immune activity (e.g., a condition, disease or disorder associated with an insufficient immune response) that contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.

NLRP3 modulators

The present invention provides compounds of Formula (I): wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human).

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) having formula (I) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

Compounds and compositions for treating conditions associated with STING activity

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured:

In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured; Formula (I), Formula (II) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein.

The instant invention describes hydrazide-containing compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.

HDAC inhibitor compounds and methods of treatment

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: wherein the variables shown in Formula AA can be as defined anywhere herein. Compounds AA are modulators of NLRP1 and/or NLRP3

Sulphonamides and compositions thereof for treating conditions associated with NLRP activity

The invention provides compounds and methods of inhibiting a cyclin-dependent kinase, comprising contacting the cyclin-dependent kinase and an effective amount or concentration of a compound of formula (I) wherein variables are as defined herein. Compounds of formula (I) can be highly selective inhibitors of cyclin-dependent kinases such as CDK12/13, relative to other kinases such as casein kinases, such as CK1&#x3b4;/&#x3b5;. Compounds can be used in treatment of cancers, such as breast cancer, brain cancer and ovarian cancer. 

Small molecule inhibitors of CDK12/CDK13

This disclosure features chemical entities of formula I (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same. 

In one aspect, compounds of Formulae (I) and (II), or pharmaceutically acceptable salts thereof, are featured: Formulae (I) and (II), wherein the variables shown in Formulae (I) and (II) can be as defined anywhere herein. 

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Tequesta, FL, United States of America

William R Roush