The Scripps Research Institute

Dana-Farber-Cancer Institute Inc.

Abide Therapeutics, Inc.

H. Lundbeck A/s

Whitehead Institute for Biomedical Research

Lundbeck La Jolla Research Center, Inc.

Jae Won Chang

Nathanael Schiander Gray

Benjamin F Cravatt

Jianming Zhang

Todd Kevin Jones

Cheryl A Grice

Justin S Cisar

Micah J Niphakis

Kenneth M Lum

Xianming Deng

Barun Okram

Amy Wojciechowski

Hwan Geun Choi

David Sabatini

Taebo Sim

Qingsong Liu

Ellen Weisberg

Carson C Thoreen

Olivia Delene Weber

Nathanael S Gray

Wenjun Zhou

Seong Woo Anthony Kang

Armand Cognetta

Dong-Hui Wang

Daniel K Nomura

David M Sabatini

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

Carbamate compounds and methods of making and using same

The present disclosure provides novel heteroaryl compounds of formula (VII). Such compounds are useful for the treatment of cancers.

Small molecule myristate inhibitors of Bcr-abl and methods of use

The present disclosure provides novel heteroaryl compounds of formula (IV). Such compounds are useful for the treatment of cancers. 

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for a method of treating a patient in need thereof, where the patient is suffering from post-traumatic stress disorder comprising administering a disclosed compound or composition.

The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers. 

Small molecule myristate inhibitors of BCR-ABL and methods of use

This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.

Carbamate compounds and of making and using same

The present application relates to therapeutic organic compounds, compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.

Fused 2-aminothiazole compounds

This disclosure provides compounds having the structure: wherein L, R, Rand p are defined herein, which are modulators of MAGL and/or ABHD6. Further provided is the use of these compounds as medicinal agents, processes for their preparation, and pharmaceutical compositions that include the disclosed compounds. The disclosure also provides a method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar ICvalues. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.

Anti-cancer serine hydrolase inhibitory carbamates

This disclosure provides piperazine carbamates and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed piperazine carbamates as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.

Soluble mTOR complexes and modulators thereof

The present application relates to therapeutic organic compounds of formula (I), wherein Q, R1, R2, R3, and R4 are defined herein. The invention also relates to pharmaceutical compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease such as cancer comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.

Growing community of inventors

San Diego, CA, United States of America

Jae Won Chang