公开(公告)号：US20240299347A1

公开(公告)日：2024-09-12

申请号：US18601908

申请日：2024-03-11

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

发明人： Wei GU

IPC分类号： A61K31/381 ,  A61K31/122 ,  A61K31/19 ,  A61K31/352 ,  A61K31/405 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4245 ,  A61K31/7088 ,  A61K38/46 ,  A61P25/28 ,  C12N15/113 ,  G01N33/68

CPC分类号： A61K31/381 ,  A61K31/122 ,  A61K31/19 ,  A61K31/352 ,  A61K31/405 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4245 ,  A61K31/7088 ,  A61K38/465 ,  A61P25/28 ,  C12N15/1137 ,  C12Y113/11034 ,  G01N33/6896 ,  C12N2310/14 ,  G01N2333/90241 ,  G01N2800/2835

摘要： Disclosed herein are compositions and methods for treating or preventing Huntington's disease. In one aspect, the disclosed methods relate to targeting arachidonate 5-lipoxygenase (ALOX5) and 5-lipoxygenase-activating protein (FLAP). The compositions and methods disclosed herein can be used as disease modifying therapies to enable treatment of Huntington's disease and related disorders earlier in disease progression and improve clinical outcomes.

公开(公告)号：US20240277658A1

公开(公告)日：2024-08-22

申请号：US18030875

申请日：2021-10-15

申请人： ALBERT-LUDWIGS-UNIVERSITÄT FREIBURG

发明人： Olaf GROSS ,  Emilia NEUWIRT ,  Manfred JUNG

IPC分类号： A61K31/397 ,  A61K31/17 ,  A61K31/277 ,  A61K31/341 ,  A61K31/351 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5375 ,  A61P37/04

CPC分类号： A61K31/397 ,  A61K31/17 ,  A61K31/277 ,  A61K31/341 ,  A61K31/351 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5375 ,  A61P37/04

摘要： The present invention relates to a compound or pharmaceutically acceptable salts thereof, that modulates NLRP3 in that the NLRP3 inflammasome is activated. This invention further relates to the compounds and/or compositions for use in the prevention and treatment of a condition, disease or a disorder by activating the NLRP3 inflammasome, wherein the disease is selected from a group comprising infectious diseases, or cancer. Moreover, the invention relates to the use of the present compounds for analyzing a the activity of NLRP3 activation.

公开(公告)号：US20240262916A1

公开(公告)日：2024-08-08

申请号：US18561127

申请日：2022-05-16

申请人： METANOIA BIO INC.

发明人： Slavica TUDZAROVA-TRAJKOVSKA ,  Oppel GREEFF ,  Abraham VAN WYK

IPC分类号： C07K16/28 ,  A61K31/196 ,  A61K31/198 ,  A61K31/245 ,  A61K31/26 ,  A61K31/352 ,  A61K31/357 ,  A61K31/37 ,  A61K31/381 ,  A61K31/403 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/501 ,  A61K31/519 ,  A61K31/661 ,  A61K38/06 ,  A61K38/08 ,  C12N15/113

CPC分类号： C07K16/2857 ,  A61K31/196 ,  A61K31/198 ,  A61K31/245 ,  A61K31/26 ,  A61K31/352 ,  A61K31/357 ,  A61K31/37 ,  A61K31/381 ,  A61K31/403 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/501 ,  A61K31/519 ,  A61K31/661 ,  A61K38/06 ,  A61K38/08 ,  C12N15/1138 ,  C07K2317/569 ,  C12N2310/11

摘要： The disclosure provides methods and compositions for treating cardiovascular disease with HIF1-a Pathway Inhibitors and PFKFB3 Inhibitors. Exemplary cardiovascular diseases ns treated using the provided methods and compositions include acute coronary syndrome, coronary artery disease, myocardial infarction, coronary heart disease, carditis or cardiomyopathy, an ischemic cardiovascular disease, heart failure, stroke, peripheral vascular disease peripheral arterial disease, and ischemia/reperfusion injury.

公开(公告)号：US20240254089A1

公开(公告)日：2024-08-01

申请号：US18245700

申请日：2021-09-16

申请人： ESCIENT PHARMACEUTICALS, INC.

发明人： Brandon SELFRIDGE ,  Liming HUANG ,  Adam YEAGER ,  Marcos SAINZ ,  Marion LANIER ,  Esther MARTINBOROUGH ,  Marcus BOEHM

IPC分类号： C07D231/56 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

CPC分类号： C07D231/56 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4-dependent condition more specifically, by contacting MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein E, Q, W, Z, R1, R2, R3, and R4 are as defined herein. Pharmaceutical compositions containing such compounds, as well as compounds themselves, are also provided.

公开(公告)号：US12037324B2

公开(公告)日：2024-07-16

申请号：US17861809

申请日：2022-07-11

申请人： Université de Montréal ,  Bristol-Myers Squibb Company

发明人： Eldon Scott Priestley ,  Samuel Kaye Reznik ,  Edward H. Ruediger ,  James R. Gillard ,  Oz Scott Halpern ,  Wen Jiang ,  Jeremy Richter ,  Rejean Ruel ,  Sasmita Tripathy ,  Wu Yang ,  Xiaojun Zhang

IPC分类号： C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

CPC分类号： C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

摘要： The present invention provides compounds of Formula (I):




wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are biased agonists, or β-Arrestin agonists of the angiotensin II receptor, which may be used as medicaments.

公开(公告)号：US20240208954A1

公开(公告)日：2024-06-27

申请号：US18013696

申请日：2021-06-29

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong LIU ,  Jiang WANG ,  Cen XIE ,  Yameng LIU ,  Shulei HU ,  Cuina LI ,  Feng GAO ,  Kanglong WANG ,  Yong WANG ,  Xianchun ZHONG ,  Yuqiang SHI ,  Hualiang JIANG ,  Kaixian CHEN

IPC分类号： C07D413/10 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/675 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D271/06 ,  C07D413/14 ,  C07F9/6558

CPC分类号： C07D413/10 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/675 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D271/06 ,  C07D413/14 ,  C07F9/65583

摘要： The present invention relates to the fields of pharmaceutical chemistry and pharmacotherapeutics, and in particular to a compound as represented by general formula I, a racemate, an R-isomer, an S-isomer and a pharmaceutically acceptable salt thereof and a mixture of same, a preparation method therefor, a pharmaceutical composition containing the compound and the use thereof as an SIP receptor agonist. The oxadiazole compound involved in the present invention can be used for treating SIP receptor agonist related diseases.

公开(公告)号：US20240207234A1

公开(公告)日：2024-06-27

申请号：US18478029

申请日：2023-09-29

申请人： Ellipses Pharma Ltd

发明人： Gary Hattersley ,  Jamal Saeh ,  Ziyang Yu ,  Chris P. Miller ,  Teeru Bihani

IPC分类号： A61K31/4245 ,  A61K31/138 ,  A61K31/436 ,  A61K31/519

CPC分类号： A61K31/4245 ,  A61K31/138 ,  A61K31/436 ,  A61K31/519

摘要： A method for treating AR+ breast cancer in a subject comprising administering to the subject an AR agonist (e.g., SARMs such as RAD140), or in combination with one or more therapeutic agents selected from the group consisting of cdk4/6 inhibitors, m-TOR inhibitors, PI3k inhibitors, PARP inhibitors, BCL-2 inhibitors, and MCL-1 inhibitors.

公开(公告)号：US20240199593A1

公开(公告)日：2024-06-20

申请号：US18426461

申请日：2024-01-30

申请人： NOVARTIS AG

发明人： Andreas Kordikowski ,  Yugang Liu ,  Rainer Martin Lüönd ,  Christian Markert ,  Wolfgang Miltz ,  Till Roehn ,  Carsten Spanka ,  Gebhard Thoma ,  Tian XIE

IPC分类号： C07D413/10 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/436 ,  A61K31/4439 ,  A61K45/06 ,  C07D257/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04

CPC分类号： C07D413/10 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/436 ,  A61K31/4439 ,  A61K45/06 ,  C07D257/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04

摘要： The present invention provides a crystalline form of (S)-2-amino-3-(3-(4-((3-fluoro-5-(1H-pyrazol-5-yl)pyridin-2-yl)oxy)phenyl)-1H-pyrazol-1-yl)propan-1-ol, in its free form;

a method for manufacturing said crystalline form, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

公开(公告)号：US20240199554A1

公开(公告)日：2024-06-20

申请号：US18355792

申请日：2023-07-20

申请人： Board of Regents, The University of Texas System

发明人： Richard T. LEWIS ,  Matthew Michael HAMILTON ,  William J. RAY ,  Fernando ALVAREZ ,  Dana E. PFAFFINGER ,  Naphtali REYNA ,  Jason CROSS ,  Suyambu Kesava Vijayan RAMASWAMY

IPC分类号： C07D231/06 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/10 ,  C07D231/56 ,  C07D241/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D413/08 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D231/06 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/10 ,  C07D231/56 ,  C07D241/24 ,  C07D401/12 ,  C07D401/14 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D413/08 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.

公开(公告)号：US20240166758A1

公开(公告)日：2024-05-23

申请号：US18500706

申请日：2023-11-02

申请人： Fred Hutchinson Cancer Center

发明人： Stanley R. RIDDELL ,  Damian GREEN ,  Tyler HILL

IPC分类号： C07K16/28 ,  A61K9/00 ,  A61K31/192 ,  A61K31/216 ,  A61K31/417 ,  A61K31/4245 ,  A61K31/5513 ,  A61P35/00 ,  C07K14/475 ,  C07K14/52 ,  C07K16/40

CPC分类号： C07K16/2878 ,  A61K9/0053 ,  A61K31/192 ,  A61K31/216 ,  A61K31/417 ,  A61K31/4245 ,  A61K31/5513 ,  A61P35/00 ,  C07K14/475 ,  C07K14/52 ,  C07K16/2887 ,  C07K16/40 ,  A61K45/06

摘要： The present disclosure relates to methods for using BCMA-specific binding molecules (such as a BCMA-specific chimeric antigen receptor or antibody) in combination with γ-secretase inhibitors, which can be done concurrently or sequentially, to treat or prevent a B-cell related proliferative disease, such as a cancer or autoimmune disease, or the like. A BCMA-specific binding molecule in combination with γ-secretase inhibitor can be used in, for example, adoptive immunotherapy.