公开(公告)号：US20240358688A1

公开(公告)日：2024-10-31

申请号：US18756533

申请日：2024-06-27

申请人： Boehringer Ingelheim International GmbH

发明人： Harald ENGELHARDT ,  Mark PETRONCZKI ,  Juergen RAMHARTER ,  Ulrich REISER ,  Heinz STADTMUELLER ,  Dirk SCHARN ,  Tobias WUNBERG

IPC分类号： A61K31/437 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00

CPC分类号： A61K31/437 ,  A61K31/4545 ,  A61K31/4995 ,  A61K31/553 ,  A61P35/00 ,  C07D211/04 ,  C07D519/00 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541

摘要： The present invention encompasses compounds of formula (I)




wherein the groups R1 to R4 and X1 to X5 have the meanings given in the claims and specification, their use as inhibitors of mutant EGFR, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US12128026B2

公开(公告)日：2024-10-29

申请号：US17694183

申请日：2022-03-14

申请人： University of Tennessee Research Foundation ,  Oncternal Therapeutics, Inc.

发明人： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He ,  Jayaprakash Pagadala ,  Christopher C. Coss ,  James T. Dalton ,  Charles B. Duke

IPC分类号： A61K31/404 ,  A61K31/403 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/47 ,  A61K31/472 ,  A61P35/00

CPC分类号： A61K31/404 ,  A61K31/403 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/47 ,  A61K31/472 ,  A61P35/00

摘要： This invention provides novel indole, indazole, benzimidazole, benzotriazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, other AR-expressing cancers, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels (through degradation) and/or activity (through inhibition) of any androgen receptor including androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

公开(公告)号：US20240343728A1

公开(公告)日：2024-10-17

申请号：US18293823

申请日：2022-08-08

申请人： Scorpion Therapeutics, Inc.

发明人： David St. Jean, JR.

IPC分类号： C07D473/32 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/52 ,  C07D405/12 ,  C07D471/04

CPC分类号： C07D473/32 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/52 ,  C07D405/12 ,  C07D471/04

摘要： This disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, that inhibit phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3Kα). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) PI3Kα activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.

公开(公告)号：US20240343692A1

公开(公告)日：2024-10-17

申请号：US18682031

申请日：2022-06-21

申请人： University of Pittsburgh - Of the Commonwealth System of Higher Education

发明人： Peter Wipf ,  Nikhil R. Tasker ,  Ethan J. Pazur

IPC分类号： C07D221/22 ,  A61K31/4045 ,  A61K31/437 ,  A61K31/439 ,  C07D221/18

CPC分类号： C07D221/22 ,  A61K31/4045 ,  A61K31/437 ,  A61K31/439 ,  C07D221/18

摘要： A compound, or a pharmaceutically acceptable salt thereof, of formula I:






wherein R1, R8, R9, R31, R32, R33, and R34 are each independently H, C1-C6 alkyl, or substituted C1-C6 alkyl; and
R2, R4, R5, R6, and R7 are each independently H, F, Cl, Br, —OR1—NR8R9, C1-C6 alkyl, or substituted C1-C6 alkyl.

公开(公告)号：US20240342142A1

公开(公告)日：2024-10-17

申请号：US18628366

申请日：2024-04-05

申请人： Salix Pharmaceuticals, Inc.

发明人： William FORBES ,  Enoch BORTEY

IPC分类号： A61K31/437

CPC分类号： A61K31/437

摘要： The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects.

公开(公告)号：US20240336594A1

公开(公告)日：2024-10-10

申请号：US18576708

申请日：2022-06-24

申请人： BETTA PHARMACEUTICALS CO., LTD

发明人： Bang FU ,  Yinlong LI ,  Wei REN ,  Qichao SHEN ,  Guolong DU ,  Xiaojun ZHOU ,  Yun SUN ,  Yuzhen ZHOU ,  Xiao SUN ,  Weidong CAI ,  Xiangyong LIU ,  Lieming DING ,  Jiabing WANG

IPC分类号： C07D401/14 ,  A61K31/167 ,  A61K31/18 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61K31/538 ,  C07C237/40 ,  C07C311/32 ,  C07C317/32 ,  C07C323/33 ,  C07D205/12 ,  C07D213/56 ,  C07D263/56 ,  C07D265/36 ,  C07D401/04 ,  C07D401/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107

CPC分类号： C07D401/14 ,  A61K31/167 ,  A61K31/18 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61K31/538 ,  C07C237/40 ,  C07C311/32 ,  C07C317/32 ,  C07C323/33 ,  C07D205/12 ,  C07D213/56 ,  C07D263/56 ,  C07D265/36 ,  C07D401/04 ,  C07D401/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D491/048 ,  C07D491/107

摘要： A compound of formula I and a use thereof as an MALT1 inhibitor, and a pharmaceutical composition containing the compound. The compound can be used to treat diseases or disorders such as cancer.

公开(公告)号：US12109270B2

公开(公告)日：2024-10-08

申请号：US17862491

申请日：2022-07-12

申请人： CIPLA LIMITED

发明人： Maruti Ganpati Ghagare ,  Sunilkumar Parasnath Saroj ,  Dharmaraj Ramachandra Rao ,  Rajendra Narayanrao Kankan

IPC分类号： A61K47/40 ,  A61K9/20 ,  A61K31/4184 ,  A61K31/437 ,  A61K47/32 ,  A61K47/58 ,  A61K47/69 ,  B82Y5/00

CPC分类号： A61K47/40 ,  A61K9/2095 ,  A61K31/4184 ,  A61K31/437 ,  A61K47/32 ,  A61K47/58 ,  A61K47/6951 ,  B82Y5/00 ,  Y02A50/30

摘要： There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex.

公开(公告)号：US20240327418A1

公开(公告)日：2024-10-03

申请号：US18293840

申请日：2022-08-01

申请人： OCEAN UNIVERSITY OF CHINA ,  QINGDAO HIGENE BIOPHARMACEUTICAL CO., LTD ,  MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD

发明人： Xiaoyang LI ,  Zhongren ZHOU ,  Yuqi JIANG ,  Kairui YUE ,  Wenfang XU

IPC分类号： C07D491/048 ,  A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/655 ,  A61P35/00 ,  A61P35/02 ,  C07C247/12 ,  C07D209/42 ,  C07D213/40 ,  C07D213/56 ,  C07D307/85 ,  C07D333/70 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04

CPC分类号： C07D491/048 ,  A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/655 ,  A61P35/00 ,  A61P35/02 ,  C07C247/12 ,  C07D209/42 ,  C07D213/40 ,  C07D213/56 ,  C07D307/85 ,  C07D333/70 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04

摘要： A compound targeting HDAC and NAD synthesis and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof, as well as preparation and application thereof. Specifically, a compound shown in structural general formula (I) and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof are provided. The compound of the structural general formula (I) is a multi-target inhibitor, targeting HDAC and NAD targets, and exhibiting significant HDAC inhibitory activity, while representative compounds exhibit certain NAD inhibitory activity.


Ring E-B-L-C (O)—(NH)r-R   (General formula I)

公开(公告)号：US20240308999A1

公开(公告)日：2024-09-19

申请号：US18653750

申请日：2024-05-02

申请人： TACTOGEN INC

发明人： Matthew J. Baggott

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P25/22

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61P25/22

摘要： The present invention discloses a compound, composition, method for modulating central nervous system activity, or method for treating central nervous system disorders, such as post-traumatic stress and adjustment disorders, comprising an indolizine-containing compound having a structure disclosed herein.

公开(公告)号：US20240307400A1

公开(公告)日：2024-09-19

申请号：US18676439

申请日：2024-05-28

申请人： TING THERAPEUTICS LLC

发明人： Jian ZUO ,  Tal TEITZ

IPC分类号： A61K31/519 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/506 ,  A61P27/16

CPC分类号： A61K31/519 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/506 ,  A61P27/16

摘要： This disclosure provides for methods, kits and pharmaceutical compositions comprising an inhibitor of EGFR signaling for the treatment of hearing loss. In particular, one such EGFR inhibitor, Dabrafenib, is a therapeutic candidate for treating cisplatin-induced and/or noise-induced hearing loss.