公开(公告)号：US12024525B2

公开(公告)日：2024-07-02

申请号：US17592679

申请日：2022-02-04

申请人： AGENEBIO, INC.

发明人： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang

IPC分类号： A61P25/00 ,  A61K31/13 ,  A61K31/27 ,  A61K31/445 ,  A61K31/496 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61K31/5517 ,  A61K45/06 ,  C07D487/14

CPC分类号： C07D487/14 ,  A61K31/13 ,  A61K31/27 ,  A61K31/445 ,  A61K31/496 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5517 ,  A61K45/06 ,  A61P25/00 ,  A61K31/13 ,  A61K2300/00 ,  A61K31/551 ,  A61K2300/00 ,  A61K31/27 ,  A61K2300/00 ,  A61K31/496 ,  A61K2300/00 ,  A61K31/445 ,  A61K2300/00 ,  A61K31/55 ,  A61K2300/00

摘要： This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of α5-containing GABAA receptor agonist (e.g., a α5-containing GABAA receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.

公开(公告)号：US12023343B2

公开(公告)日：2024-07-02

申请号：US17814567

申请日：2022-07-25

申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM ,  AustinPx, LLC

发明人： Chris Brough ,  James W. McGinity ,  Dave A. Miller ,  James C. Dinunzio ,  Robert O. Williams, III

IPC分类号： A61J3/00 ,  A61J3/07 ,  A61J3/10 ,  A61K9/14 ,  A61K9/16 ,  A61K9/20 ,  A61K31/343 ,  A61K31/496 ,  A61K31/573 ,  A61K47/32 ,  A61K47/38

CPC分类号： A61K31/573 ,  A61J3/00 ,  A61J3/07 ,  A61J3/10 ,  A61K9/146 ,  A61K9/1694 ,  A61K9/2077 ,  A61K31/343 ,  A61K31/496 ,  A61K47/32 ,  A61K47/38

摘要： Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.

公开(公告)号：US12023332B2

公开(公告)日：2024-07-02

申请号：US16977772

申请日：2019-03-05

申请人： Wylder Nation Foundation

发明人： Maria Dolores Ledesma ,  Adrian Bartoll ,  Edward H. Schuchman

IPC分类号： A61K31/501 ,  A61K9/00 ,  A61K31/16 ,  A61K31/164 ,  A61K31/232 ,  A61K31/325 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/573 ,  A61K35/28 ,  A61K45/06 ,  A61P1/00 ,  A61P25/28 ,  C12N9/16

CPC分类号： A61K31/501 ,  A61K9/0085 ,  A61K31/16 ,  A61K31/164 ,  A61K31/232 ,  A61K31/325 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/573 ,  A61K35/28 ,  A61K45/06 ,  A61P1/00 ,  A61P25/28 ,  C12N9/16 ,  C12Y301/04012

摘要： The present invention provides, inter alia, compositions and methods for using CB1 cannabinoid receptor agonists, or other compounds capable of increasing endocannabinoids or endocannabinoid signaling, for treating and preventing lysosomal storage disorders in which lipid storage occurs (including, e.g., disorders associated with sphingomyelin accumulation). In particular embodiments, the present invention provides compositions and methods for treating such lysosomal storage disorders with one or more fatty acid amide hydrolase inhibitor alone or in combination with one or more additional agent.

公开(公告)号：US20240208956A1

公开(公告)日：2024-06-27

申请号：US18286037

申请日：2022-04-07

申请人： CHONG KUN DANG PHARMACEUTICAL CORP.

发明人： Chang Sik Lee ,  Jung Taek Oh ,  Hyeseung Song ,  Hyunjin Michael Kim

IPC分类号： C07D413/14 ,  A61K31/4245 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  C07D413/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

CPC分类号： C07D413/14 ,  A61K31/4245 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/4995 ,  A61K31/5377 ,  C07D413/12 ,  C07D417/14 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D491/107

摘要： The present invention relates to a novel 1,3,4-oxadiazole thiocarbonyl compound having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof, pharmaceutically acceptable salts thereof, a use thereof for preparing a medicament, a pharmaceutical composition containing the same, a therapeutic method using the composition, and a preparation method thereof, wherein a novel compound having a selective HDAC6 inhibitory activity is represented by formula I.

公开(公告)号：US20240208940A1

公开(公告)日：2024-06-27

申请号：US18556241

申请日：2022-04-19

申请人： H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.

发明人： Haitao JI

IPC分类号： C07D401/14 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K47/55 ,  A61P35/00 ,  C07D405/14 ,  C07D409/14 ,  C07D471/10 ,  C07D487/04

CPC分类号： C07D401/14 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K47/55 ,  A61P35/00 ,  C07D405/14 ,  C07D409/14 ,  C07D471/10 ,  C07D487/04

摘要： Described herein are small molecule inhibitors of the β-catenin/B-cell lymphoma 9 interaction and pharmaceutical compositions including a therapeutically effective amount of the small molecule inhibitors described herein. Described are also methods of treating oncological disorders, for example cancer by administering the small molecule inhibitors of the β-catenin/B-cell lymphoma interaction described herein.

公开(公告)号：US20240207253A1

公开(公告)日：2024-06-27

申请号：US18283035

申请日：2022-05-18

申请人： UNM RAINFOREST INNOVATIONS ,  THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES ,  THE UNITED STATES GOVERNMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIRS

发明人： Larry A. Sklar ,  Stella Jubay ,  Clemencia Panilla ,  Marcello Giulianotti ,  Richard Allen Houghten ,  Samuel Lee

IPC分类号： A61K31/496 ,  A61K31/13 ,  A61K31/137 ,  A61K31/155 ,  A61K31/381 ,  A61K31/4015 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/495 ,  A61P31/10

CPC分类号： A61K31/496 ,  A61K31/13 ,  A61K31/137 ,  A61K31/155 ,  A61K31/381 ,  A61K31/4015 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/495 ,  A61P31/10

摘要： The present invention is directed to compounds which have been identified, as inhibitors of the expression of CDR1 (Cdr1p) and/or CDR2 (Cdr2p), both ABC-type plasma, membrane transporters, which are major contributor to antifungal therapy resistance. These compounds may be used in the treatment of fungal infections, especially Candida infections, either alone or in combination with azole antifungal agents such as fluconazole, itraconazole, miconazole, clotrimazole and the like. Often the inhibitor compounds described herein are useful for reversing the antifungal therapy resistance exhibited by the overexpression of CDR1 and/or CDR2 in strains of fungi, especially including Candida spp. Combination therapy and compositions for treating fungal infections, especially including azole resistant fungal infections represent important embodiments of the present invention.

公开(公告)号：US12018402B2

公开(公告)日：2024-06-25

申请号：US16325856

申请日：2017-08-17

申请人： Quest Diagnostics Investments LLC

发明人： Michael J. McPhaul ,  Heather R. Sanders

IPC分类号： C40B30/04 ,  A61K31/03 ,  A61K31/48 ,  A61K31/567 ,  A61K31/4174 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/451 ,  A61K31/496 ,  A61K31/506 ,  C12Q1/6806 ,  C12Q1/6886

CPC分类号： C40B30/04 ,  A61K31/03 ,  A61K31/48 ,  A61K31/567 ,  A61K31/4174 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/451 ,  A61K31/496 ,  A61K31/506 ,  C12Q1/6806 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156

摘要： The present technology is related to methods for detecting genetic alterations underlying intracranial neoplasms such as pituitary adenomas, meningiomas, and craniopharyngiomas. The methods disclosed herein are useful in determining whether a patient harboring an intracranial tumor will benefit from or is predicted to be responsive to treatment with an individual therapeutic agent or a specific combination of therapeutic agents. Kits for use in practicing the methods are also provided.

公开(公告)号：US12016927B2

公开(公告)日：2024-06-25

申请号：US18148860

申请日：2022-12-30

申请人： OTSUKA PHARMACEUTICAL CO., LTD.

发明人： Daiki Kaneko ,  Takakuni Matsuda ,  Yusuke Hoshika

IPC分类号： A61K47/32 ,  A61K9/00 ,  A61K9/06 ,  A61K31/496 ,  A61K47/10 ,  A61K47/38

CPC分类号： A61K47/32 ,  A61K9/0019 ,  A61K9/06 ,  A61K31/496 ,  A61K47/10 ,  A61K47/38 ,  A61K9/0024

摘要： An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 s−1 end having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1.000 s−1, as measured.

公开(公告)号：US20240199587A1

公开(公告)日：2024-06-20

申请号：US18490967

申请日：2023-10-20

申请人： Hoffmann-La Roche Inc.

发明人： Machoud AMOUSSA ,  Joerg BENZ ,  Niels Kevin BRIAN ,  Kallie FRISTON ,  Maude GIROUD ,  Uwe GRETHER ,  Katrin GROEBKE ZBINDEN ,  Benoit HORNSPERGER ,  Carsten KROLL ,  Bernd KUHN ,  Camiel John LEAKE ,  Rainer E. MARTIN ,  David Friedrich Erhard NIPPA ,  Fionn Susannah O’HARA ,  Bernd PUELLMANN ,  Hans RICHTER ,  Martin RITTER ,  Didier ROMBACH ,  Philipp Claudio SCHMID ,  Shounan ZHANG

IPC分类号： C07D403/14 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

CPC分类号： C07D403/14 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/438 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

摘要： The invention provides new heterocyclic compounds having the general formula (I)




wherein A, B, X, and R1 to R7 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20240199572A1

公开(公告)日：2024-06-20

申请号：US18280531

申请日：2022-03-15

申请人： THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS ,  ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA

发明人： Gregory R. THATCHER ,  Cutler T. LEWANDOWSKI ,  Manel BEN AISSA ,  Brian LAYDEN ,  Yeng-Jeng SHAW ,  Ganga Reddy VELMA ,  Mary Jo LADU

IPC分类号： C07D333/40 ,  A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/69 ,  A61P3/10 ,  A61P25/28 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07F5/02

CPC分类号： C07D333/40 ,  A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/69 ,  A61P3/10 ,  A61P25/28 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07F5/025

摘要： Compounds that induce expression of ATP-binding cassette transporter A1 (ABCA1) without lipogenesis are provided, as are methods of using the same to treat or prevent type 2 diabetes or dementia.