公开(公告)号：US12152029B2

公开(公告)日：2024-11-26

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

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

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：US11332453B2

公开(公告)日：2022-05-17

申请号：US17055079

申请日：2019-05-14

Applicant: H. Lundbeck A/S

Inventor： Cheryl A. Grice ,  Daniel J. Buzard ,  Michael B. Shaghafi

IPC: C07D295/185 ,  C07D305/06 ,  C07D263/32 ,  C07D241/12 ,  C07D213/55 ,  C07D305/08

Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

公开(公告)号：US11161856B2

公开(公告)日：2021-11-02

申请号：US16642713

申请日：2018-08-28

Applicant: H. Lundbeck A/S

Inventor： Cheryl A. Grice ,  Olivia D. Weber ,  Daniel J. Buzard ,  Michael B. Shaghafi

IPC: C07D519/00 ,  C07D401/12 ,  C07D211/58 ,  C07D471/10

Abstract: Provided herein are compounds of the formula: and compositions comprising the same, which are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

公开(公告)号：US12258340B2

公开(公告)日：2025-03-25

申请号：US18185227

申请日：2023-03-16

Applicant: H. Lundbeck A/S

Inventor： Cheryl A. Grice ,  John J. M. Wiener ,  Olivia D. Weber ,  Katharine K. Duncan

IPC: A61K31/499 ,  A61K31/496 ,  A61K31/5377 ,  A61P25/06 ,  A61P29/00 ,  C07D231/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/048 ,  C07D491/08 ,  C07D519/00

Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising the same. The compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the compounds and compositions are useful for the treatment of pain.

公开(公告)号：US11149037B2

公开(公告)日：2021-10-19

申请号：US16615746

申请日：2018-05-22

Applicant: H. Lundbeck A/S

Inventor： Cheryl A. Grice ,  Olivia D. Weber ,  Daniel J. Buzard ,  Michael B. Shaghafi ,  John J. M. Wiener ,  Justin S. Cisar ,  Katharine K. Duncan

IPC: A61K31/4155 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61P25/00 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D491/048 ,  C07D491/08 ,  C07D519/00 ,  C07D498/08

Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

公开(公告)号：US11142517B2

公开(公告)日：2021-10-12

申请号：US16349142

申请日：2017-11-15

Applicant: H. Lundbeck A/S

Inventor： Cheryl A. Grice ,  Todd K. Jones ,  Kurt G. Grimm ,  Jacqueline Lorayne Blankman ,  Channing Rodney Beals

IPC: C07D403/10

Abstract: Described herein is the MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate, including crystalline forms and pharmaceutically acceptable salts and solvates thereof.

公开(公告)号：US11059822B2

公开(公告)日：2021-07-13

申请号：US16349047

申请日：2017-11-15

Applicant: H. LUNDBECK A/S

Inventor： Cheryl A. Grice ,  Daniel J. Buzard ,  Michael B. Shaghafi

IPC: C07D471/10 ,  A61K31/438

Abstract: Provided herein are spirocyclic and fused bicyclic carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.

公开(公告)号：US11034674B2

公开(公告)日：2021-06-15

申请号：US16563733

申请日：2019-09-06

Applicant: H. Lundbeck A/S

Inventor： Jacqueline Lorayne Blankman ,  Jason Robert Clapper ,  R. Alan B. Ezekowitz ,  Iain Peter Fraser ,  Cheryl A. Grice ,  Todd K. Jones ,  Gary Paul O'Neill ,  Archie Wayne Thurston, Jr. ,  Channing Rodney Beals

IPC: A61K31/497 ,  C07D403/10 ,  A61K31/495 ,  C07D295/205 ,  A61P29/00

Abstract: Provided herein are methods of treating inflammation or neuropathic pain using an effective dose of a monoacylglycerol lipase inhibitor or a composition thereof.