公开(公告)号：USRE49948E1

公开(公告)日：2024-04-30

申请号：US17592108

申请日：2022-02-03

申请人： Peloton Therapeutics, Inc.

发明人： Darryl David Dixon ,  Jonas Grina ,  John A. Josey ,  James P. Rizzi ,  Stephen T. Schlachter ,  Eli M. Wallace ,  Bin Wang ,  Paul Wehn ,  Rui Xu ,  Hanbiao Yang

IPC分类号： C07D213/85 ,  A61K31/09 ,  A61K31/10 ,  C07B39/00 ,  C07C43/205 ,  C07C43/225 ,  C07C43/23 ,  C07C43/263 ,  C07C43/285 ,  C07C205/22 ,  C07C255/54 ,  C07C255/56 ,  C07C311/29 ,  C07C313/06 ,  C07C317/22 ,  C07C317/24 ,  C07C317/32 ,  C07C317/34 ,  C07C317/36 ,  C07C317/40 ,  C07C317/42 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C323/22 ,  C07C381/10 ,  C07D213/65 ,  C07D213/89 ,  C07D231/56 ,  A61K41/00 ,  A61P35/00 ,  C07C43/275 ,  C07C43/29

CPC分类号： C07D213/85 ,  A61K31/09 ,  A61K31/10 ,  C07B39/00 ,  C07C43/205 ,  C07C43/225 ,  C07C43/23 ,  C07C43/263 ,  C07C43/285 ,  C07C205/22 ,  C07C255/54 ,  C07C255/56 ,  C07C311/29 ,  C07C313/06 ,  C07C317/22 ,  C07C317/24 ,  C07C317/32 ,  C07C317/34 ,  C07C317/36 ,  C07C317/40 ,  C07C317/42 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C323/22 ,  C07C381/10 ,  C07D213/65 ,  C07D213/89 ,  C07D231/56 ,  A61K41/0038 ,  A61P35/00 ,  C07C43/275 ,  C07C43/29 ,  C07C2602/04 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/94

摘要： The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

公开(公告)号：US11845724B2

公开(公告)日：2023-12-19

申请号：US17019097

申请日：2020-09-11

申请人： Vincere Biosciences, Inc.

发明人： Donna L. Romero ,  Michael Garrett Johnson ,  Andrew David Lee ,  Bahareh Behrouz ,  Edward Lawrence Fritzen, Jr.

IPC分类号： C07D205/04 ,  C07D209/20 ,  C07C317/36 ,  C07D309/14 ,  C07D309/12 ,  C07D217/26 ,  C07D471/04 ,  C07D213/72 ,  C07D333/36 ,  C07D305/08 ,  C07D405/12 ,  C07D211/58 ,  C07D307/22

CPC分类号： C07D205/04 ,  C07C317/36 ,  C07D209/20 ,  C07D211/58 ,  C07D213/72 ,  C07D217/26 ,  C07D305/08 ,  C07D307/22 ,  C07D309/12 ,  C07D309/14 ,  C07D333/36 ,  C07D405/12 ,  C07D471/04

摘要： The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of USP30, and the treatment of USP30-mediated disorders.

公开(公告)号：US11787762B2

公开(公告)日：2023-10-17

申请号：US17835559

申请日：2022-06-08

申请人： ARCUS BIOSCIENCES, INC.

发明人： Joel Worley Beatty ,  Samuel Lawrie Drew ,  Matthew Epplin ,  Jeremy Thomas Andre Fournier ,  Balint Gal ,  Tezcan Guney ,  Karl T. Haelsig ,  Clayton Hardman ,  Steven Donald Jacob ,  Jenna Leigh Jeffrey ,  Jaroslaw Kalisiak ,  Kenneth Victor Lawson ,  Manmohan Reddy Leleti ,  Erick Allen Lindsey ,  Artur Karenovich Mailyan ,  Debashis Mandal ,  Guillaume Mata ,  Hyunyoung Moon ,  Jay Patrick Powers ,  Brandon Reid Rosen ,  Yongli Su ,  Anh Thu Tran ,  Zhang Wang ,  Xuelei Yan ,  Kai Yu

IPC分类号： C07C317/32 ,  A61K31/10 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/5025 ,  A61K31/505 ,  A61K31/519 ,  A61K31/538 ,  A61K39/395 ,  A61K45/06 ,  C07C255/53 ,  C07C317/22 ,  C07C317/36 ,  C07D209/34 ,  C07D211/86 ,  C07D213/57 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/48 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/57 ,  C07D265/36 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D307/83 ,  C07D311/22 ,  C07D333/64 ,  C07D401/04 ,  C07D401/10 ,  C07D409/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07C317/32 ,  A61K31/10 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/472 ,  A61K31/4709 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/538 ,  A61K39/3955 ,  A61K45/06 ,  C07C255/53 ,  C07C317/22 ,  C07C317/36 ,  C07D209/34 ,  C07D211/86 ,  C07D213/57 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/48 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/57 ,  C07D265/36 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D307/83 ,  C07D311/22 ,  C07D333/64 ,  C07D401/04 ,  C07D401/10 ,  C07D409/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04 ,  C07C2602/08 ,  C07C2602/10

摘要： Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.

公开(公告)号：US11713295B2

公开(公告)日：2023-08-01

申请号：US17304409

申请日：2021-06-21

申请人： LB PHARMACEUTICALS INC.

发明人： Andrew R. Vaino ,  Vincent T. Grattan ,  Zachary Prensky

IPC分类号： C07C207/00 ,  A61K31/40 ,  C07D207/09 ,  C07C317/36 ,  A61P25/18 ,  A61K31/166 ,  A61K45/06

CPC分类号： C07D207/09 ,  A61K31/166 ,  A61K31/40 ,  A61K45/06 ,  A61P25/18 ,  C07C317/36

摘要： Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain, either individually or in combination with other CNS active agents.

公开(公告)号：US20230174470A1

公开(公告)日：2023-06-08

申请号：US17921687

申请日：2021-04-27

申请人： AUTOTAC INC.

发明人： Yong Tae KWON ,  Hyun Tae KIM ,  Jeong Eun NA ,  Yu Jin SEO ,  Chang Hoon JI ,  Ha Rim CHOI ,  Ji Eun LEE ,  Ah Jung HEO

IPC分类号： C07C311/49 ,  C07D295/135 ,  C07D209/34 ,  C07D209/08 ,  C07D209/42 ,  C07D231/18 ,  C07D209/44 ,  C07D209/30 ,  C07D231/56 ,  C07D211/54 ,  C07D277/36 ,  C07D307/68 ,  C07D207/12 ,  C07D471/04 ,  C07C243/38 ,  C07C243/36 ,  C07C311/39 ,  C07C317/28 ,  C07C317/36

CPC分类号： C07C311/49 ,  C07D295/135 ,  C07D209/34 ,  C07D209/08 ,  C07D209/42 ,  C07D231/18 ,  C07D209/44 ,  C07D209/30 ,  C07D231/56 ,  C07D211/54 ,  C07D277/36 ,  C07D307/68 ,  C07D207/12 ,  C07D471/04 ,  C07C243/38 ,  C07C243/36 ,  C07C311/39 ,  C07C317/28 ,  C07C317/36 ,  C07C2602/08

摘要： The present specification relates to a compound as a UBR box domain ligand. The present specification provides a small molecule compound that binds to the UBR box domain. Further, the present specification provides a composition for inhibiting UBR box domain substrate binding, including a ligand compound that binds to a UBR box domain, a pharmaceutical composition for treating UBR-related disease, and a use thereof.

公开(公告)号：US11040943B2

公开(公告)日：2021-06-22

申请号：US16561767

申请日：2019-09-05

申请人： LB PHARMACEUTICALS INC.

发明人： Andrew R. Vaino ,  Vincent T. Grattan ,  Zachary Prensky

IPC分类号： C07D207/09 ,  C07C317/36 ,  A61P25/18 ,  A61K45/06 ,  A61K31/166 ,  A61K31/40

摘要： Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain, either individually or in combination with other CNS active agents.

公开(公告)号：US20200079734A1

公开(公告)日：2020-03-12

申请号：US16383933

申请日：2019-04-15

申请人： LB PHARMACEUTICALS INC.

发明人： Andrew R. Vaino ,  Vincent T. Grattan ,  Zachary Prensky

IPC分类号： C07D207/09 ,  A61K31/40 ,  A61K45/06 ,  A61K31/166 ,  A61P25/18 ,  C07C317/36

摘要： Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or a2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain, either individually or in combination with other CNS active agents.

公开(公告)号：US20200055818A1

公开(公告)日：2020-02-20

申请号：US16561829

申请日：2019-09-05

申请人： LB PHARMACEUTICALS INC.

发明人： Andrew R. VAINO ,  Vincent T. GRATTAN ,  Zachary PRENSKY

IPC分类号： C07D207/09 ,  A61K31/40 ,  A61K45/06 ,  A61K31/166 ,  A61P25/18 ,  C07C317/36

摘要： Novel amisulpride derivatives and pharmaceutical compositions thereof are disclosed. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may have better membrane permeability compared to amisulpride. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for antagonizing dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more conditions responsive to modulation of dopamine and/or serotonin (e.g., 5-HT2a) and/or α2 receptor in a subject, either individually or in combination with other CNS active agents. The amisulpride derivative disclosed herein or a pharmaceutical composition thereof may be used for treating one or more disorders associated with an abnormality in levels of dopamine and/or serotonin in the brain, either individually or in combination with other CNS active agents.

公开(公告)号：US20190389814A1

公开(公告)日：2019-12-26

申请号：US16093751

申请日：2017-04-13

申请人： UNIVERSITY OF OTTAWA ,  UNIVERSITY OF MARYLAND, BALTIMORE ,  UNIVERSITY OF ROCHESTER

发明人： Jeffrey W. KEILLOR ,  Abdullah AKBAR ,  Richard L. ECKERT ,  Matthew FISHER ,  Gail V. W. JOHNSON

IPC分类号： C07D241/04 ,  C07D405/06 ,  C07C317/36

摘要： There are provided Tissue Transglutaminase (TG2) inhibitor compounds, and compositions and methods of use thereof for the prevention or treatment of a cancer. Compounds of Formula I, and pharmaceutically acceptable salts thereof, are provided:

公开(公告)号：US10208049B2

公开(公告)日：2019-02-19

申请号：US15634159

申请日：2017-06-27

申请人： Case Western Reserve University

发明人： Krzysztof Palczewski ,  Akiko Maeda ,  Marcin Golczak

IPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/56 ,  C07C211/01 ,  C07C229/12 ,  C07C229/60 ,  C07C229/64 ,  C07C237/48 ,  C07C251/58 ,  C07C317/36 ,  C07D261/04 ,  A61K9/00

摘要： A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.