公开(公告)号：US20180208568A1

公开(公告)日：2018-07-26

申请号：US15925517

申请日：2018-03-19

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

CPC classification number: C07D295/205 ,  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 indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.

公开(公告)号：US20170183353A1

公开(公告)日：2017-06-29

申请号：US15313012

申请日：2015-05-20

Applicant: ABIDE THERAPEUTICS, INC. ,  THE SCRIPPS RESEARCH INSTITUTE

Inventor： Benjamin F. CRAVATT ,  Armand B. COGNETTA ,  Jonathan J. HULCE ,  Micah J. NIPHAKIS ,  Todd K. JONES ,  Cheryl A. GRICE

IPC: C07D487/04 ,  C12Q1/34

CPC classification number: C07D487/04 ,  C12Q1/34

Abstract: Provided herein are N-hydroxy bicyclic hydantoin carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of serine hydrolases. Furthermore, the subject compounds and compositions are useful for the treatment of one or more of cancer, pain, diabetes, obesity/metabolic syndrome, epilepsy, traumatic brain injury, and inflammation.

公开(公告)号：US20220062248A1

公开(公告)日：2022-03-03

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: A61K31/445 ,  A61K31/501 ,  A61K31/439 ,  A61K31/397 ,  A61K31/4545

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.

公开(公告)号：US20210002337A1

公开(公告)日：2021-01-07

申请号：US16903258

申请日：2020-06-16

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：US20170313669A1

公开(公告)日：2017-11-02

申请号：US15520389

申请日：2015-10-27

Applicant: THE SCRIPPS RESEARCH INSTITUTE ,  THE UNIVERSITY OF CONNECTICUT

Inventor： Benjamin F. CRAVATT ,  Siddhesh S. KAMAT ,  William H. PARSONS ,  Amy R. HOWELL ,  Kaddy CAMARA ,  Amy ANDERSON

IPC: C07D305/12 ,  A61K31/337 ,  A61K31/365

CPC classification number: C07D305/12 ,  A61K31/337 ,  A61K31/365 ,  A61K2121/00 ,  C07D305/10 ,  C07D407/12

Abstract: Provided herein are lactone compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as inhibitors of serine hydrolases, such as ABHD16A. Furthermore, the subject compounds and compositions may be useful for the treatment of, for example, PHARC and other neuroinflammatory diseases.

公开(公告)号：US20170115303A1

公开(公告)日：2017-04-27

申请号：US15331745

申请日：2016-10-21

Applicant: The Scripps Research Institute

Inventor： Benjamin F. CRAVATT ,  Keriann M. BACKUS ,  Bruno E. CORREIA ,  Megan M. BLEWETT ,  John R. TEIJARO

IPC: G01N33/68 ,  G01N33/50 ,  C12N9/10 ,  C12N9/64 ,  C12N9/04

CPC classification number: G01N33/6845 ,  C12N9/0006 ,  C12N9/1007 ,  C12N9/6472 ,  C12Y101/01042 ,  C12Y201/01023 ,  C12Y304/22061 ,  C12Y304/22063 ,  G01N33/5005 ,  G01N33/5008 ,  G01N33/6842

Abstract: Disclosed herein are methods, compositions, probes, polypeptides, assays, and kits for identifying a cysteine containing protein as a binding target for a small molecule fragment. Also disclosed herein are methods, compositions, and probes for mapping a biologically active cysteine site on a protein and screening a small molecule fragment for interaction with a cysteine containing protein.

公开(公告)号：US20200292555A1

公开(公告)日：2020-09-17

申请号：US16890966

申请日：2020-06-02

Applicant: The Scripps Research Institute

Inventor： Benjamin F. CRAVATT ,  Keriann M. BACKUS ,  Bruno E. CORREIA ,  Megan M. BLEWETT ,  John R. TEIJARO

IPC: G01N33/68 ,  C12N9/04 ,  C12N9/10 ,  C12N9/64 ,  G01N33/50

Abstract: Disclosed herein are methods, compositions, probes, polypeptides, assays, and kits for identifying a cysteine containing protein as a binding target for a small molecule fragment. Also disclosed herein are methods, compositions, and probes for mapping a biologically active cysteine site on a protein and screening a small molecule fragment for interaction with a cysteine containing protein.

公开(公告)号：US20200206201A1

公开(公告)日：2020-07-02

申请号：US16503415

申请日：2019-07-03

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

Inventor： Benjamin F. CRAVATT ,  Matthew PATRICELLI ,  Dean STAMOS ,  Gabe SIMON ,  Benjamin HORNING ,  David WEINSTEIN

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

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.

公开(公告)号：US20180372751A1

公开(公告)日：2018-12-27

申请号：US16016392

申请日：2018-06-22

Applicant: The Scripps Research Institute

Inventor： Benjamin F. CRAVATT ,  Stephan M. HACKER ,  Keriann M. BACKUS

IPC: G01N33/68 ,  C12N9/10 ,  G01N33/58 ,  G01N33/50 ,  C12N9/64

Abstract: Disclosed herein are methods and compounds for profiling a lysine reactive protein. Also described herein are methods, compounds, and compositions for identifying a small molecule fragment ligand that interacts with a reactive lysine residue.

公开(公告)号：US20230312499A1

公开(公告)日：2023-10-05

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 ,  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

CPC classification number: 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.