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.

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：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：US20170190669A1

公开(公告)日：2017-07-06

申请号：US15312998

申请日：2015-05-20

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

Inventor： Dale L. BOGER ,  Katerina OTRUBOVA ,  Justin S. CISAR ,  Cheryl A. GRICE ,  Todd K. JONES

IPC: C07D231/14 ,  C07D491/107 ,  C07D403/12 ,  C07D417/12 ,  C07D405/12 ,  C07D401/12

CPC classification number: C07D231/14 ,  C07D231/12 ,  C07D231/16 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D491/10 ,  C07D491/107

Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of one or more of MAGL, ABHD6, and FAAH. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain, solid tumors and/or obesity.

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：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：US20230265095A1

公开(公告)日：2023-08-24

申请号：US18051654

申请日：2022-11-01

Applicant: H. Lundbeck A/S

Inventor： Thomas VETTER ,  Martin JUHL ,  HEIDI LOPEZ DE DIEGO ,  Cheryl A. GRICE ,  John J.M. WIENER ,  Daniel J. BUZARD ,  Amy ALLAN ,  Susana DEL RIO GANCEDO ,  Samuel George ANDREW ,  Antonio CINCOTTI ,  Adam Ross PATTERSON ,  Richard James EDWARDS

IPC: C07D471/10

CPC classification number: C07D471/10 ,  C07B2200/13

Abstract: Described herein are new crystalline forms of the MAGL inhibitor 1-(1-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)b enzyl)-1,8-diazaspiro[4.5]decane-8-carbonyl)-1H-pyrazole-3-carboxylic acid, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20220213074A1

公开(公告)日：2022-07-07

申请号：US17610662

申请日：2020-05-13

Applicant: H. Lundbeck A/S

Inventor： Cheryl A. GRICE ,  Jeanne V. MOODY ,  Daniel J. BUZARD ,  Justin S. CISAR

IPC: C07D405/14 ,  C07D213/75

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：US20210323938A1

公开(公告)日：2021-10-21

申请号：US17234660

申请日：2021-04-19

Applicant: H. LUNDBECK A/S

Inventor： Cheryl A. GRICE ,  Kurt G. GRIMM ,  Todd K. JONES ,  Giuseppe GUERCIO

IPC: C07D295/02

Abstract: Described herein is the manufacture of MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate including salts thereof.

公开(公告)号：US20240018120A1

公开(公告)日：2024-01-18

申请号：US18252611

申请日：2021-11-12

Applicant: H. LUNDBECK A/S

Inventor： John J.M. WIENER ,  Cheryl A. GRICE ,  Daniel J. BUZARD ,  Justin S. CISAR ,  Olivia Delene WEBER ,  Amy ALLAN ,  Nicholas RAFFAELE ,  Jeanne V. MOODY ,  Michael B. SHAGHAFI

IPC: C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D401/14 ,  C07D487/04 ,  C07D471/04 ,  C07D221/20 ,  C07D417/12 ,  A61P29/00 ,  A61P25/08

CPC classification number: C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D401/14 ,  C07D487/04 ,  C07D471/04 ,  C07D221/20 ,  C07D417/12 ,  A61P29/00 ,  A61P25/08

Abstract: Provided herein are substituted 1,1,1,3,3,3-hexafluoropropan-2-yl 6-azaspiro[2.5]octane-6-carboxylate compounds and pharmaceutical compositions comprising said compounds. The compounds and compositions provided herein are useful as inhibitors of MAGL. Furthermore, the compounds and compositions as provided herein are useful for the treatment of diseases and disorders benefiting from the inhibition of MAGL.