公开(公告)号：US20240270699A1

公开(公告)日：2024-08-15

申请号：US18604472

申请日：2024-03-13

Applicant: Lomond Therapeutics, Inc.

Inventor： Volodymyr Kysil ,  Vladislav Zenonovich Parchinsky ,  Alexei Pushechnikov ,  Alexandre Vasilievich Ivachtchenko ,  Nikolay Savchuk

IPC: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/55 ,  A61K31/5513 ,  C07D239/50 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D411/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

CPC classification number: C07D239/48 ,  A61K31/505 ,  A61K31/506 ,  A61K31/55 ,  A61K31/5513 ,  C07D239/50 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D411/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention is generally directed to inhibitors of hematopoietic progenitor kinase 1 (HPK1), leucine rich repeat kinase 2 (LRRK2) protein, FMS-like tyrosine kinase 3 (FLT3) gene, interleukin-1 receptor-associated kinase 1 (IRAK1), interleukin-1 receptor-associated kinase 4 (IRAK4), and Janus kinases (JAKs), including Janus kinase 1 (JAK1), Janus kinase 2 (JAK2), Janus kinase 3 (JAK3), and tyrosine kinase 2 (TYK2) useful in the treatment of diseases and disorders modulated by said HPK1, LRRK2, FLT3, IRAK1, IRAK4, and JAKs, having the Formula (I):

公开(公告)号：US12060347B2

公开(公告)日：2024-08-13

申请号：US17123265

申请日：2020-12-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Xiaojun Zhang ,  Eldon Scott Priestley ,  J. Alex Bates ,  Oz Scott Halpern ,  Samuel Kaye Reznik ,  Jeremy M. Richter

IPC: C07D417/04 ,  A61P7/04 ,  A61P9/10 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D417/04 ,  A61P7/04 ,  A61P9/10 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07D519/00

Abstract: Disclosed are compounds of Formula (I) to (VIII):




or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.

公开(公告)号：US20240262815A1

公开(公告)日：2024-08-08

申请号：US18559542

申请日：2022-04-08

Applicant: VORONOI INC.

Inventor： Younho LEE ,  Seonah HWANG ,  Woomi DO ,  Inseob SHIM ,  Hwa LEE ,  Jungbeom SON ,  Namdoo KIM ,  Sunghwan KIM ,  Hongryul JUNG ,  Jihye YOO

IPC: C07D413/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61P35/00 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/08

CPC classification number: C07D413/14 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/551 ,  A61P35/00 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107 ,  C07D498/08

Abstract: The present invention relates to an isoxazolidin-2-yl-substituted heteroaryl derivative and a pharmaceutical composition for cancer prevention or treatment, comprising the compound as an active ingredient. The compound exhibits high inhibitory activity against the wild type or mutants of at least one of ErbB2 and ErbB4 and thus can be useful for treating cancers in which ErbB2 and ErbB4 are expressed.

公开(公告)号：US12053462B2

公开(公告)日：2024-08-06

申请号：US17379175

申请日：2021-07-19

Applicant: Gilead Sciences, Inc.

Inventor： Peter A. Blomgren ,  Taryn Campbell ,  Jayaraman Chandrasekhar ,  Christopher T. Clark ,  Julian A. Codelli ,  Kevin S. Currie ,  Jeffrey E. Kropf ,  Yasamin Moazami ,  Nicole Nava ,  Leena Patel ,  Stephane Perreault ,  Jason K. Perry ,  Kassandra F. Sedillo ,  Natalie Seeger ,  Kirk L. Stevens ,  Jennifer Anne Treiberg ,  Suet C. Yeung ,  Zhongdong Zhao

IPC: C07D215/02 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/541 ,  A61K45/06 ,  C07D215/14 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D215/18 ,  C07D401/04 ,  C07D413/04 ,  C07D417/14 ,  C07D475/02 ,  C07D491/04 ,  C07D491/06 ,  C07D491/08 ,  C07D498/10 ,  C07D513/04

CPC classification number: A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/541 ,  A61K45/06 ,  C07D215/14 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D215/18 ,  C07D401/04 ,  C07D413/04 ,  C07D417/14 ,  C07D475/02 ,  C07D491/04 ,  C07D491/06 ,  C07D491/08 ,  C07D498/10 ,  C07D513/04

Abstract: The present disclosure provides a compound of Formula (I):




or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

公开(公告)号：US20240254114A1

公开(公告)日：2024-08-01

申请号：US18524612

申请日：2023-11-30

Applicant: Merck Sharp & Dohme LLC

Inventor： Yeon-Hee Lim ,  Cedric L. Hugelshofer ,  James P. Roane ,  Samantha E. Shockley

IPC: C07D413/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D413/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

Abstract: Provided are compounds of Formula I, Formula Ia and Formula Ib




and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, Formula Ia and Formula Ib, pharmaceutical compositions comprising compounds of Formula I, Formula Ia and Formula Ib, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), hepatic fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I, Ia and Ib and the pharmaceutically acceptable salts, esters, and prodrugs thereof, to a patient in need thereof.

公开(公告)号：US20240253023A1

公开(公告)日：2024-08-01

申请号：US11867898

申请日：2007-10-05

Applicant: Christophe Michot ,  Michel Armand ,  Michel Gauthier ,  Yves Choquette

Inventor： Christophe Michot ,  Michel Armand ,  Michel Gauthier ,  Yves Choquette

IPC: B01J31/02 ,  B01J31/04 ,  B01J31/06 ,  B01J31/12 ,  B01J31/18 ,  B01J31/22 ,  C07B37/02 ,  C07B37/12 ,  C07C45/46 ,  C07C45/69 ,  C07C67/00 ,  C07C255/10 ,  C07C255/17 ,  C07C255/27 ,  C07C255/46 ,  C07C255/65 ,  C07C257/14 ,  C07C311/03 ,  C07C311/04 ,  C07C311/09 ,  C07C311/48 ,  C07C317/04 ,  C07C317/08 ,  C07C317/14 ,  C07C317/22 ,  C07C317/24 ,  C07C317/34 ,  C07C317/44 ,  C07D207/452 ,  C07D213/76 ,  C07D219/10 ,  C07D231/18 ,  C07D233/90 ,  C07D239/60 ,  C07D241/42 ,  C07D249/04 ,  C07D249/10 ,  C07D249/12 ,  C07D251/70 ,  C07D277/64 ,  C07D277/82 ,  C07D285/125 ,  C07D285/135 ,  C07D285/15 ,  C07D285/16 ,  C07D303/34 ,  C07D307/54 ,  C07D307/64 ,  C07D311/52 ,  C07D311/58 ,  C07D311/82 ,  C07D319/06 ,  C07D333/16 ,  C07D333/24 ,  C07D405/06 ,  C07D409/12 ,  C07D417/10 ,  C07D417/14 ,  C07F17/02 ,  C08F4/04 ,  C08G65/334 ,  C09B69/00 ,  C09B69/02 ,  C09B69/10 ,  H01B1/12 ,  H01G9/022 ,  H01G11/02 ,  H01G11/62 ,  H01M4/00 ,  H01M4/38 ,  H01M4/58 ,  H01M4/62 ,  H01M6/00 ,  H01M6/16 ,  H01M6/18 ,  H01M10/052 ,  H01M10/0525 ,  H01M10/0565 ,  H01M10/0567 ,  H01M10/0568 ,  G02F1/1516 ,  G02F1/1523 ,  H01M4/02 ,  H01M4/131 ,  H01M4/133 ,  H01M4/134 ,  H01M4/40 ,  H01M4/48 ,  H01M4/485 ,  H01M4/505 ,  H01M4/525 ,  H01M4/60 ,  H01M4/66 ,  H01M6/04

CPC classification number: B01J31/0224 ,  B01J31/0215 ,  B01J31/0222 ,  B01J31/0225 ,  B01J31/0227 ,  B01J31/0235 ,  B01J31/0239 ,  B01J31/0247 ,  B01J31/0251 ,  B01J31/0252 ,  B01J31/0267 ,  B01J31/0271 ,  B01J31/0281 ,  B01J31/0288 ,  B01J31/0289 ,  B01J31/04 ,  B01J31/06 ,  B01J31/068 ,  B01J31/124 ,  B01J31/1815 ,  B01J31/2208 ,  C07B37/02 ,  C07B37/12 ,  C07C45/46 ,  C07C45/69 ,  C07C67/00 ,  C07C255/10 ,  C07C255/17 ,  C07C255/27 ,  C07C255/46 ,  C07C255/65 ,  C07C257/14 ,  C07C311/03 ,  C07C311/04 ,  C07C311/09 ,  C07C311/48 ,  C07C317/04 ,  C07C317/08 ,  C07C317/14 ,  C07C317/22 ,  C07C317/24 ,  C07C317/34 ,  C07C317/44 ,  C07D207/452 ,  C07D213/76 ,  C07D219/10 ,  C07D231/18 ,  C07D233/90 ,  C07D239/60 ,  C07D241/42 ,  C07D249/04 ,  C07D249/10 ,  C07D249/12 ,  C07D251/70 ,  C07D277/64 ,  C07D277/82 ,  C07D285/125 ,  C07D285/135 ,  C07D285/15 ,  C07D285/16 ,  C07D303/34 ,  C07D307/54 ,  C07D307/64 ,  C07D311/52 ,  C07D311/58 ,  C07D311/82 ,  C07D319/06 ,  C07D333/16 ,  C07D333/24 ,  C07D405/06 ,  C07D409/12 ,  C07D417/10 ,  C07D417/14 ,  C07F17/02 ,  C08F4/04 ,  C08G65/3344 ,  C09B69/00 ,  C09B69/02 ,  C09B69/10 ,  H01B1/122 ,  H01B1/128 ,  H01G9/022 ,  H01G11/02 ,  H01G11/62 ,  H01M4/00 ,  H01M4/382 ,  H01M4/5815 ,  H01M4/625 ,  H01M6/00 ,  H01M6/166 ,  H01M6/181 ,  H01M6/183 ,  H01M10/052 ,  H01M10/0525 ,  H01M10/0565 ,  H01M10/0567 ,  H01M10/0568 ,  B01J2231/122 ,  B01J2231/14 ,  B01J2231/326 ,  B01J2231/341 ,  B01J2231/348 ,  B01J2231/4205 ,  B01J2231/543 ,  B01J2531/35 ,  B01J2531/824 ,  C07C2601/10 ,  C07C2602/42 ,  G02F2001/1518 ,  G02F1/1525 ,  H01M4/02 ,  H01M4/131 ,  H01M4/133 ,  H01M4/134 ,  H01M4/405 ,  H01M4/48 ,  H01M4/485 ,  H01M4/505 ,  H01M4/525 ,  H01M4/5825 ,  H01M4/60 ,  H01M4/661 ,  H01M6/04 ,  H01M6/164 ,  H01M6/168 ,  Y02E60/13 ,  Y10S430/127 ,  Y10T29/49108 ,  Y10T428/2918

Abstract: The invention concerns ionic compounds in which the anionic load has been delocalized. A compound disclosed by the invention is comprised of an amide or one of its salts, including an anionic portion combined with at least one cationic portion M+m in sufficient numbers to ensure overall electronic neutrality; the compound is further comprised of M as a hydroxonium, a nitrosonium NO+, an ammonium —NH4+, a metallic cation with the valence m, an organic cation with the valence m, or an organometallic cation with the valence m. The anionic portion matches the formula RF—SOx—N−Z, where RF is a perflourinated group, x is 1 or 3, and Z is an electroattractive substituent. The compounds can be used notably for ionic conducting materials, electronic conducting materials, colorants and the catalysis of various chemical reactions.

公开(公告)号：US20240246964A1

公开(公告)日：2024-07-25

申请号：US18551824

申请日：2022-03-25

Applicant: Arbutus Biopharma Corporation

Inventor： Vijay Ahuja ,  Andrew G. Cole ,  Bruce D. Dorsey ,  Yi Fan ,  Gavin D. Heffernan ,  Ramesh Kakarla ,  Steven G. Kultgen ,  Duyan Nguyen ,  Seyma Ozturk ,  Jorge Quintero ,  Michael J. Sofia

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61P31/14 ,  A61P35/00 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61P31/14 ,  A61P35/00 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D487/10 ,  C07D491/107 ,  C07D519/00

Abstract: The present disclosure includes substituted 1-aryl-1′-heteroaryl compounds, substituted 1,1′-biheteroaryl compounds, analogues thereof, and compositions comprising the same. Such compounds and analogues comprises compounds of formula (I). In one aspect, the compounds contemplated in the disclosure can be used to treat, ameliorate, and/or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient. In another aspect, the compounds contemplated in the disclosure can be used to treat, ameliorate, and/or prevent cancer in a patient.

公开(公告)号：US20240246962A1

公开(公告)日：2024-07-25

申请号：US18424580

申请日：2024-01-26

Applicant: Gahserbrum Bio, Inc.

Inventor： Qinghua MENG ,  Weiqiang XING ,  Haizhen ZHANG ,  Xichen LIN ,  Hui LEI ,  Andrew JENNINGS

IPC: C07D471/04 ,  A61K45/06 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D471/04 ,  A61K45/06 ,  C07D405/14 ,  C07D417/14

Abstract: This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.

公开(公告)号：US20240246957A1

公开(公告)日：2024-07-25

申请号：US18558763

申请日：2022-05-04

Applicant: 2N Pharma ApS

Inventor： Venkateswara Rao BODDU ,  Santhosh Kumar CHITTIMALLA ,  Durairaja SANKARAN ,  Ganesh Babu KARUNAKARAN ,  Thomas BRIMERT

IPC: C07D417/14 ,  A61K31/551 ,  A61P25/28 ,  C07D417/04

CPC classification number: C07D417/14 ,  A61K31/551 ,  A61P25/28 ,  C07D417/04

Abstract: Compounds of the formula (I)




wherein R1, R2, R3, L and Y have the designations described herein, or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof. Further, the invention relates to processes for the preparation of compounds of the formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof. The invention also relates to compounds of the formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof for use as a medicament. Further, the invention relates to compounds of the formula (1) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof for use in the amelioration, prevention and/or treatment of a disease caused by or related to delipidation of a neural tissue. In particular, the disease is a neurodegenerative disease.

公开(公告)号：US20240246955A1

公开(公告)日：2024-07-25

申请号：US18555139

申请日：2022-04-12

Applicant: CULLGEN (SHANGHAI), INC.

Inventor： Jing LIU ,  Jialiang WANG ,  Xiaoran HAN ,  Ting YANG

IPC: C07D417/14 ,  A61K31/506 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14

CPC classification number: C07D417/14 ,  A61K31/506 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14

Abstract: Heterobifunctional compounds (e.g., bi-functional small molecule compounds) and compositions comprising one or more of the heterobifunctional compounds are provided. The heterobifunctional compounds are used for the treatment of certain disease in a subject in need thereof. Methods for identifying such heterobifunctional compounds are also presented.