公开(公告)号：US20240358844A1

公开(公告)日：2024-10-31

申请号：US18733200

申请日：2024-06-04

申请人： ORPRO THERAPEUTICS, INC.

发明人： Peter B. HEIFETZ ,  Haim MOSKOWITZ

IPC分类号： A61K47/64 ,  A61K31/337 ,  A61K31/407 ,  A61K31/427 ,  A61K31/431 ,  A61K31/475 ,  A61K31/496 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/665 ,  A61K31/675 ,  A61K31/7036 ,  A61K31/704 ,  A61K31/7048 ,  A61K31/7068 ,  A61K33/243 ,  A61K38/07 ,  A61K38/12 ,  A61K38/13 ,  A61K38/14

CPC分类号： A61K47/64 ,  A61K31/337 ,  A61K31/407 ,  A61K31/427 ,  A61K31/431 ,  A61K31/475 ,  A61K31/496 ,  A61K31/5383 ,  A61K31/546 ,  A61K31/665 ,  A61K31/675 ,  A61K31/7036 ,  A61K31/704 ,  A61K31/7048 ,  A61K31/7068 ,  A61K33/243 ,  A61K38/07 ,  A61K38/12 ,  A61K38/13 ,  A61K38/14

摘要： The present invention is related to a drug delivery composition that includes a thioredoxin homologue protein having an N-terminal monocysteinic active site, with the cysteine residue of the active site in a reduced state and an active agent conjugated to the thioredoxin homologue protein and methods of making and using the composition.

公开(公告)号：US20240342178A1

公开(公告)日：2024-10-17

申请号：US18414690

申请日：2024-01-17

申请人： Istituto Europeo di Oncologia S.r.l. ,  Università degli Studi Di Milano

发明人： Saverio MINUCCI ,  Pier Giuseppe PELICCI ,  Seyed Amir HOSSEINI

IPC分类号： A61K31/519 ,  A61K31/135 ,  A61K31/165 ,  A61K31/167 ,  A61K31/18 ,  A61K31/325 ,  A61K31/343 ,  A61K31/366 ,  A61K31/4025 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/47 ,  A61K31/473 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5375 ,  A61K38/15 ,  A61P35/00 ,  A61P35/02

CPC分类号： A61K31/519 ,  A61K31/135 ,  A61K31/165 ,  A61K31/167 ,  A61K31/18 ,  A61K31/325 ,  A61K31/343 ,  A61K31/366 ,  A61K31/4025 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/47 ,  A61K31/473 ,  A61K31/495 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5375 ,  A61K38/15 ,  A61P35/00 ,  A61P35/02

摘要： The present disclosure relates to methods of treating cancer and pharmaceutical compositions for use in the treatment of cancer, including LSD1-inhibitor-resistant cancers, comprising administering to a subject an effective amount of a cell cycle inhibitor, such as a CDK4/6 inhibitor or a p21 enhancer, and an effective amount of a LSD1 inhibitor.

公开(公告)号：US20240335453A1

公开(公告)日：2024-10-10

申请号：US18292703

申请日：2022-07-21

申请人： University of KwaZulu-Natal ,  University of Zululand

发明人： Thavendran Govender ,  Tricia Naicker ,  Per I Arvidsson ,  Hendrik G Kruger ,  Byron Peters

IPC分类号： A61K31/546 ,  A61K31/407 ,  A61K31/431 ,  A61P31/04

CPC分类号： A61K31/546 ,  A61K31/407 ,  A61K31/431 ,  A61P31/04

摘要： A metallo-β-lactamase (MBL) inhibitor of general formula (I) C-A-L (I) in which: C is a functionalised aza-cycloalkane zinc chelating moiety, L is a β-lactam moiety which may be functionalised, and A is a C1-C10 linear or cyclic linker, which may be functionalised, is provided.

公开(公告)号：US12083098B2

公开(公告)日：2024-09-10

申请号：US17056238

申请日：2019-05-16

申请人： Actuate Therapeutics Inc.

发明人： Torry A. Tucker ,  Steven Idell

IPC分类号： A61K31/407 ,  A61K9/00 ,  A61P11/00

CPC分类号： A61K31/407 ,  A61K9/0073 ,  A61P11/00

摘要： Pharmaceutical compositions and methods are described which rely upon glycogen synthase kinase 3 (form β; GSK 3 β) inhibitors, most preferably 9-ING-41, to inhibit fibrotic pulmonary remodeling in vivo including proliferation and differentiation of myofibroblasts to fibrotic fibroblasts in several mouse models. Therapeutic targeting of GSK-3β with the clinically useful specific inhibitor, 9-ING-41, mitigates fibrotic pulmonary remodeling in vivo and provides a mode of therapy of human IPF by specific GSK-3β inhibition with 9-ING-41.

公开(公告)号：US12070468B2

公开(公告)日：2024-08-27

申请号：US17984734

申请日：2022-11-10

申请人： The Trustees of Columbia University in the City of New York

发明人： Carrie J. Shawber ,  June K. Wu ,  Ajit Muley

IPC分类号： A61K31/145 ,  A61K31/407 ,  A61K31/501 ,  A61K31/69 ,  A61K38/06 ,  A61K38/07 ,  A61P9/14

CPC分类号： A61K31/69 ,  A61K31/145 ,  A61K31/407 ,  A61K31/501 ,  A61K38/06 ,  A61K38/07 ,  A61P9/14

摘要： Provided herein are methods and compositions for treating and preventing vascular malformations including lymphatic, venous, capillary, arteriovenous, and combinations thereof. Methods of treatment and prevention include the administration of proteasome inhibitors, omipalisib, disulfiram, and agents which target genes in the PI3K/AKT/mTOR or RAS/RAF/MAPK pathways, including but not limited to Pik3ca, Pik3r3, Tsc2, Rasa1, Map2k2, and Glmn.

公开(公告)号：US12059427B2

公开(公告)日：2024-08-13

申请号：US16961198

申请日：2018-01-15

申请人： YINUOKE MEDICINE SCIENCE AND TECHNOLOGY COMPANY LTD.

发明人： Lingbing Zhang ,  Dongxu Zhang

IPC分类号： A61K31/7068 ,  A61K31/12 ,  A61K31/192 ,  A61K31/196 ,  A61K31/216 ,  A61K31/40 ,  A61K31/405 ,  A61K31/407 ,  A61P21/06 ,  A61P35/00 ,  A61P37/06

CPC分类号： A61K31/7068 ,  A61K31/12 ,  A61K31/192 ,  A61K31/196 ,  A61K31/216 ,  A61K31/40 ,  A61K31/405 ,  A61K31/407 ,  A61P21/06 ,  A61P35/00 ,  A61P37/06

摘要： Provided are methods and compositions for treating cachexia in order to reduce the morbidity and mortality of chronic illnesses and to improve the effectiveness of treating chronic illness overall. More specifically, provided herein are methods and compositions for treating cachexia by agents that modulate the immune system and/or inflammation.

公开(公告)号：US12053527B2

公开(公告)日：2024-08-06

申请号：US17383494

申请日：2021-07-23

申请人： Children's Medical Center Corporation ,  Massachusetts Institute of Technology

发明人： Daniel S. Kohane ,  Rong Yang ,  Lily Yun Lin

IPC分类号： A61K47/34 ,  A61K9/00 ,  A61K9/06 ,  A61K9/46 ,  A61K31/407 ,  A61K31/424 ,  A61K31/431 ,  A61K31/445 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5383 ,  A61K31/573 ,  A61K38/12 ,  A61K45/06 ,  A61K47/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61P27/16 ,  A61P31/04 ,  C08G65/335 ,  C08G79/04

CPC分类号： A61K47/34 ,  A61K9/0046 ,  A61K9/06 ,  A61K31/407 ,  A61K31/424 ,  A61K31/431 ,  A61K31/445 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5383 ,  A61K31/573 ,  A61K38/12 ,  A61K45/06 ,  A61K47/06 ,  A61K47/10 ,  A61K47/12 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61P27/16 ,  A61P31/04 ,  C08G65/3355 ,  C08G79/04 ,  A61K31/445 ,  A61K2300/00 ,  A61K31/573 ,  A61K2300/00 ,  A61K31/407 ,  A61K2300/00 ,  A61K31/424 ,  A61K2300/00 ,  A61K31/431 ,  A61K2300/00 ,  A61K31/4709 ,  A61K2300/00 ,  A61K31/496 ,  A61K2300/00 ,  A61K31/5383 ,  A61K2300/00

摘要： The present invention provides compositions and methods for delivery of therapeutic agents across an barrier. The compositions include a therapeutic agent (e.g., antimicrobial agent, antibiotic, or anesthetic agent), a permeation enhancer which increases the flux of the therapeutic agent across the barrier, and a matrix forming agent. The matrix forming agent forms a gel at a suitable gelation temperature and rheological properties for use in drug delivery, and in some cases, the gelation temperature and rheological properties are not significantly changed from those of the composition without the permeation enhancer. The invention also provides a matrix forming agent and compositions thereof. Such compositions are particularly useful in the treatment of otitis media. Methods of treatment, methods of delivery, and kits for the compositions described herein are also provided.

公开(公告)号：US12048688B2

公开(公告)日：2024-07-30

申请号：US18086958

申请日：2022-12-22

申请人： Purdue Pharmaceutical Products L.P.

发明人： Thomas Jorg Mehrling ,  Enrique Maria Ocio

IPC分类号： A61K31/4184 ,  A61K31/407 ,  A61K31/427 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/573 ,  A61K31/58 ,  A61K31/69 ,  A61K38/05 ,  A61K38/06 ,  A61K39/395 ,  A61K45/06

CPC分类号： A61K31/4184 ,  A61K31/407 ,  A61K31/427 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/573 ,  A61K31/58 ,  A61K31/69 ,  A61K38/05 ,  A61K38/06 ,  A61K39/3955 ,  A61K45/06 ,  A61K31/69 ,  A61K2300/00 ,  A61K31/5377 ,  A61K2300/00 ,  A61K31/407 ,  A61K2300/00 ,  A61K31/427 ,  A61K2300/00 ,  A61K31/573 ,  A61K2300/00 ,  A61K31/58 ,  A61K2300/00 ,  A61K31/4184 ,  A61K2300/00

摘要： The present invention is directed to a combination comprising a proteasome inhibitor and a compound of formula I or a pharmaceutically acceptable salt thereof:




to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.

公开(公告)号：US12016859B2

公开(公告)日：2024-06-25

申请号：US18129260

申请日：2023-03-31

申请人： BOW RIVER LLC

发明人： Sundar Srinivasan ,  Christina Chow Wallen

IPC分类号： A61K31/498 ,  A61K9/00 ,  A61K9/08 ,  A61K9/10 ,  A61K9/20 ,  A61K9/48 ,  A61K31/00 ,  A61K31/397 ,  A61K31/407 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/502 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/5395 ,  A61P25/16 ,  A61P25/18 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04

CPC分类号： A61K31/496 ,  A61K9/0019 ,  A61K9/0053 ,  A61K9/0056 ,  A61K9/0078 ,  A61K9/0095 ,  A61K9/08 ,  A61K9/10 ,  A61K9/2004 ,  A61K9/4841 ,  A61K31/00 ,  A61K31/397 ,  A61K31/407 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/498 ,  A61K31/4995 ,  A61K31/502 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5383 ,  A61K31/5395 ,  A61P25/16 ,  A61P25/18 ,  A61P35/02 ,  A61P35/04

摘要： The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 3 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 3-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 3-42 days.

公开(公告)号：US20240199571A1

公开(公告)日：2024-06-20

申请号：US18549188

申请日：2022-03-04

申请人： MEDSHINE DISCOVERY INC.

发明人： Lingyun WU ,  Zhen ZHAN ,  Lele ZHAO ,  Jianjun SUN ,  Yi QIAN ,  Shuhui CHEN

IPC分类号： C07D333/22 ,  A61K31/381 ,  A61K31/407 ,  A61K31/438 ,  A61K31/439 ,  A61K31/495 ,  A61K31/551 ,  C07D403/04 ,  C07D413/04

CPC分类号： C07D333/22 ,  A61K31/381 ,  A61K31/407 ,  A61K31/438 ,  A61K31/439 ,  A61K31/495 ,  A61K31/551 ,  C07D403/04 ,  C07D413/04

摘要： The present invention relates to a thiophene compound and an application thereof. The present invention specifically relates to a compound represented by formula (II) and a pharmaceutically acceptable salt thereof, wherein L1 is —C(═O)— or —C(═O)—NH—; R1 is R1a or aa; ring A is bb or cc; R1a is C1-3 alkyl substituted with 1, 2 or 3 Ra; and R3 is independently H, halogen or C1-3 alkoxy. The compound represented by formula (II) and the pharmaceutically acceptable salt thereof can better inhibit the activity of LSD1, further shows significant inhibitory activity against NCI-H1417 cell proliferation, and has good pharmacokinetic properties (including good oral bioavailability, oral exposure, half-life, and clearance rate, etc.).