公开(公告)号：US20240342185A1

公开(公告)日：2024-10-17

申请号：US18578875

申请日：2022-07-13

申请人： THE SCRIPPS RESEARCH INSTITUTE ,  SHANGPHARMA INNOVATION INC.

发明人： Luke L. LAIRSON ,  Emily CHIN ,  Brett BOOKSER ,  David LAPOINTE

IPC分类号： A61K31/5377 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

CPC分类号： A61K31/5377 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

摘要： Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions: (I) wherein R1, R2, R3, L, X, and Ar are defined in the present disclosure. The compounds are inhibitors of cyclic gmp-amp synthase (cGAS) or CGAS-related cGAMP production, and they are useful in treating or preventing inflammatory diseases or conditions in a subject.

公开(公告)号：US20240336604A1

公开(公告)日：2024-10-10

申请号：US18294663

申请日：2022-08-03

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICES ,  THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

发明人： Disha GANDHI ,  Kevin FRANKOWSKI ,  Marc FERRER ,  R. Benjamin FREE ,  David R. SIBLEY ,  Amy E. MORITZ ,  Noel Terrence SOUTHALL ,  Xin HU ,  Amber KELLEY

IPC分类号： C07D413/06 ,  A61K31/4025 ,  A61K31/424 ,  A61K31/426 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/416 ,  C07D277/14 ,  C07D401/06 ,  C07D403/06 ,  C07D498/10

CPC分类号： C07D413/06 ,  A61K31/4025 ,  A61K31/424 ,  A61K31/426 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/416 ,  C07D277/14 ,  C07D401/06 ,  C07D403/06 ,  C07D498/10

摘要： Compounds of Formula I, Formula II, and Formula III and the pharmaceutically acceptable salts thereof are disclosed. The variables R1-10 are disclosed herein. The compounds are useful for treating central nervous system disorders, especially those involving substance use disorder and/or withdrawal syndrome. Pharmaceutical compositions containing compounds of Formula I or Formula II or Formula III and methods of treatment comprising administering compounds of Formula I or Formula II or Formula III are also disclosed.

公开(公告)号：US20240317729A1

公开(公告)日：2024-09-26

申请号：US18667078

申请日：2024-05-17

申请人： YALE UNIVERSITY ,  GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  CAMBRIDGE ENTERPRISE LIMITED

发明人： CRAIG M. CREWS ,  DENNIS BUCKLEY ,  ALESSIO CIULLI ,  WILLIAM L. JORGENSEN ,  PETER C. GAREISS ,  INGE VAN MOLLE ,  JEFFREY GUSTAFSON ,  HYUN-SEOP TAE ,  JULIEN MICHEL ,  DENTON WADE HOYER ,  ANKE G. ROTH ,  JOHN DAVID HARLING ,  IAN EDWARD DAVID SMITH ,  AFJAL HUSSAIN MIAH ,  SEBASTIEN ANDRE CAMPOS ,  JOELLE LE

IPC分类号： C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/00 ,  C12N9/00

CPC分类号： C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/545 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/003 ,  C12N9/93

摘要： The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

公开(公告)号：US12091386B2

公开(公告)日：2024-09-17

申请号：US17500680

申请日：2021-10-13

申请人： Zevra Therapeutics, Inc.

发明人： Sven Guenther ,  Guochen Chi ,  Travis Mickle

IPC分类号： C07D213/56 ,  A61K9/00 ,  A61K31/44 ,  A61K31/4458 ,  A61K31/4545 ,  A61K47/55 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D401/06 ,  C07D413/06 ,  A61K9/02

CPC分类号： C07D213/79 ,  A61K9/0019 ,  A61K9/0043 ,  A61K31/4458 ,  A61K31/4545 ,  A61K47/55 ,  C07D213/80 ,  C07D213/81 ,  C07D401/06 ,  C07D413/06 ,  A61K9/0053 ,  A61K9/02

摘要： Disclosed are d-amphetamine compounds and compositions comprising at least one organic acid covalently bound to d-amphetamine, having the structure of




a salt thereof, a derivative thereof, or a combination thereof. Methods of making and using the same are also disclosed.

公开(公告)号：US12075785B2

公开(公告)日：2024-09-03

申请号：US17834252

申请日：2022-06-07

申请人： Pro Farm Group, Inc.

发明人： Ratnakar N. Asolkar ,  Marja Koivunen ,  Pamela G. Marrone ,  Ana Lucia Cordova-Kreylos ,  Huazhang Huang

IPC分类号： A01N43/16 ,  A01N43/76 ,  A01N43/86 ,  A01N43/90 ,  A01N57/20 ,  A01N63/20 ,  C07D263/32 ,  C07D263/34 ,  C07D309/14 ,  C07D407/06 ,  C07D413/04 ,  C07D413/06 ,  C07D493/10 ,  C07D498/14 ,  C07D513/04 ,  C12N1/20 ,  C12P17/04 ,  C12P17/06 ,  C12P17/14 ,  C12P17/16 ,  C12P17/18 ,  A01N43/00 ,  C12N1/00 ,  C12R1/00 ,  C12R1/01

CPC分类号： A01N63/20 ,  A01N43/16 ,  A01N43/76 ,  A01N43/86 ,  A01N43/90 ,  A01N57/20 ,  C07D263/32 ,  C07D263/34 ,  C07D309/14 ,  C07D407/06 ,  C07D413/04 ,  C07D413/06 ,  C07D493/10 ,  C07D498/14 ,  C07D513/04 ,  C12N1/20 ,  C12N1/205 ,  C12P17/04 ,  C12P17/06 ,  C12P17/14 ,  C12P17/16 ,  C12P17/18 ,  A01N43/00 ,  C12N1/00 ,  C12R2001/00 ,  C12R2001/01 ,  A01N63/20 ,  A01N43/16 ,  A01N43/74 ,  A01N43/76 ,  A01N43/90

摘要： A species of Burkholderia sp with no known pathogenicity to vertebrates but with pesticidal activity (e.g., plants, insects, fungi, weeds and nematodes) is provided. Also provided are natural products derived from a culture of said species and methods of controlling pests using said natural products.

公开(公告)号：US20240279183A1

公开(公告)日：2024-08-22

申请号：US18564839

申请日：2022-06-02

申请人： Universiteit Hasselt

发明人： Tim Vanmierlo ,  Melissa Schepers ,  Elisabeth Piccart ,  Jos Prickaerts

IPC分类号： C07D231/12 ,  A61K31/5377 ,  A61P25/08 ,  C07C45/64 ,  C07D261/08 ,  C07D405/06 ,  C07D413/06

CPC分类号： C07D231/12 ,  A61K31/5377 ,  A61P25/08 ,  C07C45/64 ,  C07D261/08 ,  C07D405/06 ,  C07D413/06

摘要： The present invention relates to compounds, pharmaceutical compositions and medicaments suitable for use in the prevention and/or treatment of neurodegenerative disorders, such as for example demyelinating diseases. These compounds have been found to improve cognition and/or neuroplasticity as well as to induce and/or stimulate remyelination of the myelin sheet. Furthermore, the present invention relates to methods for synthesis of said compounds.

公开(公告)号：US20240239776A1

公开(公告)日：2024-07-18

申请号：US18530758

申请日：2023-12-06

申请人： Janssen Pharmaceutica NV

发明人： Jesus Alcazar ,  Michael K. Ameriks ,  Cynthia B. Berry ,  Pablo Garcia-Reynaga ,  Andrew V. Samant ,  J. A. Vega-Ramiro

IPC分类号： C07D413/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/14

CPC分类号： C07D413/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/14

摘要： Azaspirocycle compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions:






wherein X, R1, R2, R2b, R3, m, n, o, and p are defined herein.

公开(公告)号：US20240208923A1

公开(公告)日：2024-06-27

申请号：US18281138

申请日：2022-03-09

申请人： Jnana Therapeutics Inc.

发明人： Dean G. Brown ,  Jaclyn L. Henderson ,  Giovanni Muncipinto ,  Joshua E. Zweig ,  Long V. Nguyen ,  Nicholas Pullen ,  Mitchell T. Antalek ,  Ryan A. Hollibaugh

IPC分类号： C07D401/04 ,  A61K31/44 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D211/58 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D401/04 ,  A61K31/44 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  C07D211/58 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Disclosed are compounds, compositions, and methods useful for treating or preventing a disease or disorder associated with abnormal levels of amino acids by modulation of SLC6A19 transport.

公开(公告)号：US12018004B2

公开(公告)日：2024-06-25

申请号：US18053582

申请日：2022-11-08

申请人： H. Lundbeck A/S ,  THE SCRIPPS RESEARCH INSTITUTE

发明人： Justin S. Cisar ,  Cheryl A. Grice ,  Todd K. Jones ,  Micah J. Niphakis ,  Jae Won Chang ,  Kenneth M. Lum ,  Benjamin F. Cravatt

IPC分类号： 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分类号： 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

摘要： 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：US20240199592A1

公开(公告)日：2024-06-20

申请号：US18471594

申请日：2023-09-21

申请人： Artax Biopharma Inc.

发明人： Julio Castro ,  Andres Gagete Mateos ,  Peter J. Machin ,  Christopher Loren Vandeusen

IPC分类号： C07D413/06 ,  A61P3/10 ,  A61P11/06 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  C07D311/22 ,  C07D311/58 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D413/06 ,  A61P3/10 ,  A61P11/06 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  C07D311/22 ,  C07D311/58 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14

摘要： The present invention provides compounds that modulate the interaction of TCR with Nck, compositions thereof, and methods of treatment using the same.