公开(公告)号：US11535597B2

公开(公告)日：2022-12-27

申请号：US16478444

申请日：2018-01-17

Applicant: The Scripps Research Institute

Inventor： Benjamin F. Cravatt ,  Christopher G. Parker ,  Bruno Correia

IPC: C07D229/02 ,  C07D223/06 ,  C07C233/06 ,  C07D295/10 ,  C07D317/46 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  G01N1/28 ,  G01N1/44 ,  G01N33/68

Abstract: Disclosed herein are methods for identifying proteins as targets for interaction with a small molecule ligand. Also disclosed herein are small molecule ligands and compositions for use in profiling druggable proteins.

公开(公告)号：US10583137B2

公开(公告)日：2020-03-10

申请号：US15778207

申请日：2016-12-02

Applicant: THE SCRIPPS RESEARCH INSTITUTE ,  LEIDEN UNIVERSITY

Inventor： Benjamin F. Cravatt ,  Daisuke Ogasawara ,  Andreu Viader ,  Hui Deng ,  Tom Van Der Wel ,  Marcelis Van Der Stelt

IPC: A61K31/496 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/4192 ,  A61K31/506 ,  A61P25/28

Abstract: Provided herein are triazole compounds and pharmaceutical compositions comprising said compounds useful as modulators of DAGL(α) and DAGL(β). In some embodiments, the compounds described herein are selective DAGL(α) inhibitors. Furthermore, the subject compounds and compositions are useful for the treatment of neurodegenerative or neuroinflammatory disease.

公开(公告)号：US20190216893A1

公开(公告)日：2019-07-18

申请号：US16306362

申请日：2017-06-02

Applicant: The Scripps Research Institute

Inventor： Benjamin F. Cravatt

IPC: A61K38/17

CPC classification number: A61K38/1709 ,  G01N33/566

Abstract: Disclosed herein are methods, pharmaceutical compositions, and vaccines for modulating an immune response. Also disclosed, herein are methods, pharmaceutical compositions, and vaccines for inducing an immune response.

公开(公告)号：US10781239B2

公开(公告)日：2020-09-22

申请号：US16536227

申请日：2019-08-08

Applicant: Vividion Therapeutics, Inc. ,  The Scripps Research Institute

Inventor： David Weinstein ,  Benjamin F. Cravatt ,  Matthew Patricelli ,  Dean Stamos ,  Gabe Simon ,  Benjamin Horning ,  Ekaterina Vinogradova ,  Brian Nordin ,  Kristen Baltgalvis ,  Todd Kinsella

IPC: C07K14/47 ,  C07D211/94

Abstract: Disclosed herein are in vivo engineered cereblon protein and methods of making the same. The in vivo engineered cereblon protein can include a site-specific non-naturally occurring modification at cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO:2 or 3, the modification comprising a moiety resulting from an in vivo Michael addition reaction between an exogenous Michael acceptor and the cysteine 287 as set forth in SEQ ID NO:1, or cysteine 286 as set forth in SEQ ID NO:2 or 3.

公开(公告)号：US20190293666A1

公开(公告)日：2019-09-26

申请号：US16235096

申请日：2018-12-28

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Benjamin F. Cravatt ,  Micah J. Niphakis ,  Kenneth Lum ,  Bruno Correia ,  Armand Cognetta ,  Jonathan Hulce

IPC: G01N33/92 ,  G01N33/68

Abstract: Disclosed herein are methods, compositions, probes, assays and kits for identifying a lipid binding protein as a drug binding target. Also disclosed herein are methods, compositions, and probes for mapping a ligand binding site on a lipid binding protein, identification of lipid binding proteins, generating drug-lipid binding protein profiles, high throughput drug screening, and identification of drugs as potential lipid binding protein ligands.

公开(公告)号：US10168342B2

公开(公告)日：2019-01-01

申请号：US15080767

申请日：2016-03-25

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Benjamin F. Cravatt ,  Micah J. Niphakis ,  Kenneth Lum ,  Bruno Correia ,  Armand Cognetta ,  Jonathan Hulce

IPC: G01N33/92 ,  G01N33/68

Abstract: Disclosed herein are methods, compositions, probes, assays and kits for identifying a lipid binding protein as a drug binding target. Also disclosed herein are methods, compositions, and probes for mapping a ligand binding site on a lipid binding protein, identification of lipid binding proteins, generating drug-lipid binding protein profiles, high throughput drug screening, and identification of drugs as potential lipid binding protein ligands.

公开(公告)号：US12018004B2

公开(公告)日：2024-06-25

申请号：US18053582

申请日：2022-11-08

Applicant: H. Lundbeck A/S ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Justin S. Cisar ,  Cheryl A. Grice ,  Todd K. Jones ,  Micah J. Niphakis ,  Jae Won Chang ,  Kenneth M. Lum ,  Benjamin F. Cravatt

IPC: C07D295/205 ,  A61P25/22 ,  C07C271/10 ,  C07C271/12 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D213/38 ,  C07D213/40 ,  C07D213/55 ,  C07D215/42 ,  C07D215/46 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D295/26 ,  C07D307/79 ,  C07D317/46 ,  C07D317/58 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/14 ,  C07D407/06 ,  C07D413/06 ,  C07D413/10 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107

CPC classification number: C07D295/205 ,  A61P25/22 ,  C07C271/10 ,  C07C271/12 ,  C07D205/04 ,  C07D207/09 ,  C07D207/14 ,  C07D213/38 ,  C07D213/40 ,  C07D213/55 ,  C07D215/42 ,  C07D215/46 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D295/26 ,  C07D307/79 ,  C07D317/46 ,  C07D317/58 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10 ,  C07D405/14 ,  C07D407/06 ,  C07D413/06 ,  C07D413/10 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107

Abstract: 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.

公开(公告)号：US11530189B2

公开(公告)日：2022-12-20

申请号：US17195351

申请日：2021-03-08

Applicant: H. Lundbeck A/S ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Justin S. Cisar ,  Cheryl A. Grice ,  Todd K. Jones ,  Micah J. Niphakis ,  Jae Won Chang ,  Kenneth M. Lum ,  Benjamin F. Cravatt

IPC: C07D295/205 ,  C07C271/12 ,  C07D317/46 ,  C07D317/58 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D471/04 ,  C07D471/10 ,  C07D261/08 ,  C07D487/04 ,  C07D263/32 ,  C07D205/04 ,  C07D491/107 ,  C07D207/14 ,  C07D271/06 ,  C07D307/79 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  A61P25/22 ,  C07D295/26 ,  C07D213/55 ,  C07D401/04 ,  C07D407/06 ,  C07D413/06 ,  C07C271/10 ,  C07D207/09 ,  C07D213/38 ,  C07D215/46 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

Abstract: 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.

公开(公告)号：US11021453B2

公开(公告)日：2021-06-01

申请号：US16717813

申请日：2019-12-17

Applicant: Lundbeck La Jolla Research Center, Inc. ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Justin S. Cisar ,  Cheryl A. Grice ,  Todd K. Jones ,  Micah J. Niphakis ,  Jae Won Chang ,  Kenneth M. Lum ,  Benjamin F. Cravatt

IPC: C07D295/205 ,  A61P25/22 ,  C07C271/12 ,  C07D317/46 ,  C07D317/58 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D471/04 ,  C07D471/10 ,  C07D261/08 ,  C07D487/04 ,  C07D263/32 ,  C07D205/04 ,  C07D491/107 ,  C07D207/14 ,  C07D271/06 ,  C07D307/79 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  C07D295/26 ,  C07D213/55 ,  C07D401/04 ,  C07D407/06 ,  C07D413/06 ,  C07C271/10 ,  C07D207/09 ,  C07D213/38 ,  C07D215/46 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

Abstract: 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.

公开(公告)号：US11771689B2

公开(公告)日：2023-10-03

申请号：US16950697

申请日：2020-11-17

Applicant: Vividion Therapeutics, Inc. ,  The Scripps Research Institute

Inventor： Benjamin F. Cravatt ,  Matthew Patricelli ,  Dean Stamos ,  Gabe Simon ,  Benjamin Horning ,  David Weinstein ,  Ekaterina Vinogradova

IPC: A61K31/44 ,  A61K31/50 ,  A61K31/445 ,  A61K31/501 ,  A61K31/439 ,  A61K31/397 ,  A61K31/4545

CPC classification number: A61K31/445 ,  A61K31/397 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/501

Abstract: Disclosed herein are compositions and methods for modulating cereblon neosubstrates. A small molecule modulator of Formula (I*), or a pharmaceutically acceptable salt or solvate thereof can be used to modulate cereblon neosubstrates.