公开(公告)号：US20220298213A1

公开(公告)日：2022-09-22

申请号：US17750833

申请日：2022-05-23

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：US20210255193A1

公开(公告)日：2021-08-19

申请号：US17139697

申请日：2020-12-31

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：US20200278355A1

公开(公告)日：2020-09-03

申请号：US16650810

申请日：2018-09-27

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Benjamin F. CRAVATT ,  Liron BAR-PELED ,  Esther KEMPER

IPC: G01N33/68 ,  C07C233/05

Abstract: Disclosed herein, in certain embodiments, are protein-probe adducts and synthetic ligands that inhibit protein-probe adduct formation, in which the proteins are regulated by NRF2. In some instances, also described herein are protein-binding domains that interact with a probe and/or a ligand described herein, in which the proteins are regulated by NRF2.

公开(公告)号：US20200270223A1

公开(公告)日：2020-08-27

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 ,  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 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：US20180344729A1

公开(公告)日：2018-12-06

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

CPC classification number: A61K31/496 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  A61P25/28 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D513/12

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：US20210221790A1

公开(公告)日：2021-07-22

申请号：US17055081

申请日：2019-05-14

Applicant: THE SCRIPPS RESEARCH INSTITUTE

Inventor： Daisuke OGASAWARA ,  Taka-Aki ICHU ,  Jonathan HULCE ,  Benjamin F. CRAVATT

IPC: C07D401/14 ,  C07D401/12 ,  C07D471/08 ,  C07D471/04 ,  C07D401/04

Abstract: Provided herein are compounds and compositions useful as modulators of ABHD12. Furthermore, the subject compounds and compositions are useful as immunotherapies in treating, for instance, cancer or infectious diseases.

公开(公告)号：US20210188793A1

公开(公告)日：2021-06-24

申请号：US17195351

申请日：2021-03-08

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 ,  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：US20200216507A1

公开(公告)日：2020-07-09

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

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：US20170073320A1

公开(公告)日：2017-03-16

申请号：US15272313

申请日：2016-09-21

Applicant: Abide Therapeutics, Inc.

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 ,  C07D307/79 ,  C07D215/46 ,  C07D295/26 ,  C07D263/32 ,  C07D231/56 ,  C07D213/38 ,  C07D413/10 ,  C07D403/10 ,  C07D401/10 ,  C07D231/12 ,  C07D207/14 ,  C07D231/16 ,  C07D491/107 ,  C07D471/10 ,  C07D205/04 ,  C07D471/04 ,  C07D487/04 ,  C07D317/58

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.

Abstract translation: 本公开提供了可以是MAGL和/或ABHD6的调节剂的化合物和组合物及其作为药物的用途，其制备方法和包含公开的化合物作为至少一种活性剂的药物组合物。 本公开还提供了治疗有需要的患者的方法，其中患者患有诸如疼痛，实体瘤癌症和/或肥胖的适应症，其包括施用所公开的化合物或组合物。