公开(公告)号：US09133148B2

公开(公告)日：2015-09-15

申请号：US14599105

申请日：2015-01-16

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: A61K31/495 ,  A61K31/496 ,  C07D207/09 ,  C07D207/14 ,  C07D213/56 ,  C07D205/04 ,  C07D295/26 ,  C07D295/205 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  C07C271/12 ,  C07D317/46 ,  C07D317/58 ,  C07D231/12 ,  C07D231/16 ,  C07D231/56 ,  C07D241/04 ,  C07D471/04 ,  C07D471/10 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D307/79 ,  C07D213/55 ,  C07D401/04 ,  C07D407/06 ,  C07D413/06 ,  C07C271/10

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 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.

Abstract translation: 本公开提供哌嗪类氨基甲酸酯和可以是MAGL和/或ABHD6的调节剂的组合物及其作为药物的用途，其制备方法和包括公开的哌嗪氨基甲酸酯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。

公开(公告)号：US20150018335A1

公开(公告)日：2015-01-15

申请号：US14369982

申请日：2013-01-07

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 ,  C07D407/06 ,  C07D317/58 ,  C07D205/04 ,  C07D401/04 ,  C07D271/06 ,  C07D295/26 ,  C07D413/06 ,  C07D405/14 ,  C07D213/55

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：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：US09981972B2

公开(公告)日：2018-05-29

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: C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D487/04 ,  C07D471/04 ,  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：US09567302B2

公开(公告)日：2017-02-14

申请号：US14383076

申请日：2013-03-15

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

Inventor： Justin S. Cisar ,  Cheryl A. Grice ,  Todd K. Jones ,  Dong-Hui Wang ,  Olivia Weber ,  Benjamin F. Cravatt ,  Micah J. Niphakis ,  Armand Cognetta ,  Jae Won Chang

IPC: C07D207/46 ,  C07D401/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/496 ,  A61K31/454 ,  C07D403/12 ,  C07D401/14 ,  C07D491/08 ,  C07D233/80 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D498/08 ,  C07D209/48

CPC classification number: C07D207/46 ,  C07D209/48 ,  C07D233/80 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

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

Abstract translation: 本文提供了可用于治疗例如疼痛，实体瘤和/或肥胖症的氨基甲酸酯化合物。

公开(公告)号：US09487495B2

公开(公告)日：2016-11-08

申请号：US14369982

申请日：2013-01-07

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 ,  C07D317/46 ,  C07D317/58 ,  C07D401/06 ,  C07D403/06 ,  C07D407/06 ,  C07D413/06 ,  A61K31/495 ,  A61K31/496 ,  C07D295/26 ,  C07D405/14 ,  C07D215/42 ,  C07D213/40 ,  C07C271/12 ,  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 ,  C07D213/55 ,  C07D401/04 ,  C07C271/10 ,  C07D207/09

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 having the structure: wherein L3, R7, Rd and 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.

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。

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.

公开(公告)号：US10670605B2

公开(公告)日：2020-06-02

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 ,  C40B60/00 ,  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.