公开(公告)号：US20240350451A1

公开(公告)日：2024-10-24

申请号：US18754070

申请日：2024-06-25

Applicant: Vanda Pharmaceuticals Inc.

Inventor： Marlene Michelle Dressman ,  John Joseph Feeney ,  Louis William Licamele ,  Mihael H. Polymeropoulos

IPC: A61K31/343 ,  A61K31/15 ,  A61K31/277 ,  A61K31/31 ,  A61K31/496 ,  A61K45/06 ,  G16H10/60 ,  G16H20/10

CPC classification number: A61K31/343 ,  A61K31/15 ,  A61K31/277 ,  A61K31/31 ,  A61K31/496 ,  A61K45/06 ,  G16H10/60 ,  G16H20/10 ,  Y02A90/10

Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g. blind patients, and to methods of measuring circadian rhythm.

公开(公告)号：US12076312B2

公开(公告)日：2024-09-03

申请号：US17692376

申请日：2022-03-11

Applicant: Wisconsin Alumni Research Foundation

Inventor： Gopal Iyer ,  Albert Wang

IPC: A61K31/4166 ,  A61K31/167 ,  A61K31/277 ,  A61K31/4155 ,  A61K31/4439 ,  A61P37/06

CPC classification number: A61K31/4166 ,  A61K31/167 ,  A61K31/277 ,  A61K31/4155 ,  A61K31/4439 ,  A61P37/06

Abstract: Use of an AR antagonist, e.g., enzalutamide and other known AR antagonists, for reducing inflammatory genes of COVID-19 subjects is provided by the present invention. In other aspects, the present invention is directed to the use of an AR antagonist, e.g., the drug enzalutamide and other known AR antagonists, to treat lung cancer in a subject. In yet other aspects, the present invention is directed to an AR antagonist, e.g., the drug enzalutamide and other known AR antagonists, as an immunotherapy.

公开(公告)号：US12065485B2

公开(公告)日：2024-08-20

申请号：US17508692

申请日：2021-10-22

Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN

Inventor： Gabriel Nunez ,  Jon Oscherwitz ,  Kemp Cease ,  Yumi Nakamura ,  Tyler Nygaard

IPC: C07K16/12 ,  A61K31/05 ,  A61K31/18 ,  A61K31/192 ,  A61K31/196 ,  A61K31/235 ,  A61K31/277 ,  A61K31/366 ,  A61K31/37 ,  A61K31/47 ,  A61K31/713 ,  A61K39/00 ,  A61K39/085 ,  A61K39/40 ,  A61K45/06 ,  C12N15/113

CPC classification number: C07K16/1271 ,  A61K31/05 ,  A61K31/18 ,  A61K31/192 ,  A61K31/196 ,  A61K31/235 ,  A61K31/277 ,  A61K31/366 ,  A61K31/37 ,  A61K31/47 ,  A61K31/713 ,  A61K39/085 ,  A61K39/40 ,  A61K45/06 ,  C12N15/113 ,  A61K2039/505 ,  A61K2039/575 ,  C07K2317/34 ,  C07K2317/76 ,  C12N2310/11 ,  C12N2310/14 ,  C12N2320/31

Abstract: Materials and methods are provided for treatment and/or prevention of Staphylococcal diseases and disorders such as infection and dermal inflammation.

公开(公告)号：US12054493B2

公开(公告)日：2024-08-06

申请号：US17143326

申请日：2021-01-07

Applicant: ENANTA PHARMACEUTICALS, INC.

Inventor： Yao-Ling Qiu ,  Xuri Gao ,  Wei Li ,  Hui Cao ,  Meizhong Jin ,  Jorden Kass ,  Xiaowen Peng ,  Yat Sun Or

IPC: C07D493/08 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/365 ,  A61K31/39 ,  A61K31/401 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/00 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07D207/16 ,  C07D211/54 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D261/08 ,  C07D261/20 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D303/34 ,  C07D307/32 ,  C07D307/33 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04

CPC classification number: C07D493/08 ,  A61K31/167 ,  A61K31/18 ,  A61K31/196 ,  A61K31/215 ,  A61K31/223 ,  A61K31/277 ,  A61K31/325 ,  A61K31/335 ,  A61K31/336 ,  A61K31/341 ,  A61K31/351 ,  A61K31/357 ,  A61K31/365 ,  A61K31/39 ,  A61K31/401 ,  A61K31/41 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/439 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4425 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/655 ,  C07B59/001 ,  C07C235/56 ,  C07C311/53 ,  C07C317/32 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07D207/16 ,  C07D211/54 ,  C07D213/52 ,  C07D213/81 ,  C07D213/89 ,  C07D231/12 ,  C07D233/64 ,  C07D257/04 ,  C07D261/02 ,  C07D261/08 ,  C07D261/20 ,  C07D263/52 ,  C07D277/26 ,  C07D295/088 ,  C07D303/26 ,  C07D303/34 ,  C07D307/32 ,  C07D307/33 ,  C07D309/08 ,  C07D313/04 ,  C07D317/72 ,  C07D327/10 ,  C07D401/04 ,  C07D451/04 ,  C07D493/04 ,  C07B2200/05 ,  C07B2200/07 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/44 ,  C07C2602/46 ,  C07C2603/74

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:

X-A-Y-L-R  (I)

which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

公开(公告)号：US20240252501A1

公开(公告)日：2024-08-01

申请号：US18241389

申请日：2023-09-01

Applicant: MORGANDANE SCIENTIFIC, LLC

Inventor： Sundar SRINIVASAN ,  Maulik PATEL ,  Christina CHOW WALLEN

IPC: A61K31/5377 ,  A61K31/277

CPC classification number: A61K31/5377 ,  A61K31/277

Abstract: The present disclosure in various embodiments teaches methods of treating patients in need of treatment with a Factor Xa inhibitor, and who are also concomitantly administered verapamil.

公开(公告)号：US20240246901A1

公开(公告)日：2024-07-25

申请号：US17929597

申请日：2021-03-10

Applicant: Sheldon Cao ,  Xiaolei Wang ,  Eubulus Biotherapeutics Inc.

Inventor： Sheldon Cao ,  Xiaolei Wang

IPC: C07C237/22 ,  A61K31/167 ,  A61K31/18 ,  A61K31/245 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/36 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/5377 ,  A61P35/00 ,  C07C255/60 ,  C07C311/08 ,  C07C311/16 ,  C07C317/40 ,  C07D213/56 ,  C07D213/64 ,  C07D213/89 ,  C07D231/56 ,  C07D249/18 ,  C07D271/12 ,  C07D277/64 ,  C07D285/14 ,  C07D303/04 ,  C07D305/06 ,  C07D309/06 ,  C07D309/14 ,  C07D317/66 ,  C07D333/24 ,  C07D405/12 ,  C07D407/12

CPC classification number: C07C237/22 ,  A61K31/167 ,  A61K31/18 ,  A61K31/245 ,  A61K31/277 ,  A61K31/337 ,  A61K31/351 ,  A61K31/36 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/5377 ,  A61P35/00 ,  C07C255/60 ,  C07C311/08 ,  C07C311/16 ,  C07C317/40 ,  C07D213/56 ,  C07D213/64 ,  C07D213/89 ,  C07D231/56 ,  C07D249/18 ,  C07D271/12 ,  C07D277/64 ,  C07D285/14 ,  C07D303/04 ,  C07D305/06 ,  C07D309/06 ,  C07D309/14 ,  C07D317/66 ,  C07D333/24 ,  C07D405/12 ,  C07D407/12 ,  C07C2601/02 ,  C07C2601/14

Abstract: Provided herein are GPX4 inhibitors, e.g., a compound of Formula (I), and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a GPX4-mediated disorder, disease, or condition.

公开(公告)号：US12042507B2

公开(公告)日：2024-07-23

申请号：US17181921

申请日：2021-02-22

Applicant: University of Georgia Research Foundation, Inc.

Inventor： Hang Yin ,  Liwei Xie ,  Amelia Yao-Ye Yin

IPC: A61K31/7105 ,  A61K9/00 ,  A61K31/015 ,  A61K31/277 ,  A61P21/04 ,  A61P25/14 ,  C12Q1/6876

CPC classification number: A61K31/7105 ,  A61K9/0019 ,  A61K31/015 ,  A61K31/277 ,  A61P21/04 ,  A61P25/14 ,  C12Q1/6876

Abstract: Compositions and methods for modulating HIF-2α to meditate of hypoxia signaling in satellite cells and applications thereof for improving skeletal muscle generation and repair are provided. For example, methods of enhancing, increasing, accelerating or/and otherwise improving skeletal muscle generation or regeneration in a subject in need thereof are disclosed. In some embodiments, the methods include administering the subject an effective amount of HIF-2α inhibitor. The HIF-2α inhibitor can be effective to, for example, increase muscle satellite cell proliferation, differentiation, or a combination thereof in a subject. Composition and methods for improving respiration, and reducing or preventing the development or progression of fibrosis are also provided. The disclosed compositions and methods are particularly useful for treating muscular dystrophies, myopathies, and other muscle-related diseases and disorders.

公开(公告)号：US20240238274A1

公开(公告)日：2024-07-18

申请号：US18556534

申请日：2022-04-25

Applicant: Northwestern University

Inventor： Deyu Fang ,  Elena Montauti ,  Ming Yan ,  Beixue Gao ,  Amy Tang ,  Huiping Liu

IPC: A61K31/4745 ,  A61K31/255 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/366 ,  A61K31/37 ,  A61K31/381 ,  A61K31/435 ,  A61K31/4418 ,  A61K31/4436 ,  A61K31/4965 ,  A61K31/517 ,  A61K31/519 ,  A61P35/00

CPC classification number: A61K31/4745 ,  A61K31/255 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/366 ,  A61K31/37 ,  A61K31/381 ,  A61K31/435 ,  A61K31/4418 ,  A61K31/4436 ,  A61K31/4965 ,  A61K31/517 ,  A61K31/519 ,  A61P35/00

Abstract: Disclosed are methods of treating diseases or disorders associated with the expression of Ubiquitin Specific Peptidase 22 (USP22). The disclosed methods may be utilized to treat diseases or disorders associated with cell proliferation, including cancer. Also disclosed are inhibitors of USP22 that specifically inhibit the EC:3.4.19.12 activity, or the thiol-dependent hydrolysis of ester, thioester, amide, peptide and isopeptide bonds formed by the C-terminal glycine of ubiquitin. The disclosed compounds may also be used in pharmaceutical compositions and methods for treatment of cell proliferative diseases or disorders associated with USP22 activity.

公开(公告)号：US12036190B2

公开(公告)日：2024-07-16

申请号：US17408397

申请日：2021-08-21

Applicant: Duke University

Inventor： Priya Kishnani ,  Baodong Sun ,  Dwight D. Koeberl

IPC: A61K38/47 ,  A61K31/05 ,  A61K31/12 ,  A61K31/137 ,  A61K31/155 ,  A61K31/167 ,  A61K31/192 ,  A61K31/198 ,  A61K31/216 ,  A61K31/277 ,  A61K31/352 ,  A61K31/355 ,  A61K31/385 ,  A61K31/436 ,  A61K31/519 ,  A61K31/522 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/575 ,  A61K31/7016 ,  A61K33/00 ,  A61K38/46 ,  A61P3/00

CPC classification number: A61K31/137 ,  A61K31/05 ,  A61K31/12 ,  A61K31/155 ,  A61K31/167 ,  A61K31/192 ,  A61K31/198 ,  A61K31/216 ,  A61K31/277 ,  A61K31/352 ,  A61K31/355 ,  A61K31/385 ,  A61K31/436 ,  A61K31/519 ,  A61K31/522 ,  A61K31/5415 ,  A61K31/55 ,  A61K31/575 ,  A61K31/7016 ,  A61K33/00 ,  A61K38/465 ,  A61K38/47 ,  A61P3/00 ,  C12Y301/04012 ,  C12Y302/0102 ,  C12Y302/01022 ,  C12Y302/01045 ,  C12Y302/01049 ,  C12Y302/01076 ,  A61K38/465 ,  A61K2300/00 ,  A61K38/47 ,  A61K2300/00

Abstract: The present disclosure is directed to methods of treating a steatosis-associated disorder and methods of treating a cytoplasmic glycogen storage disorder, including glycogen storage disease I, glycogen storage disease III, glycogen storage disease IV, and/or conditions associated with a PRKAG2 mutation, by administering a therapeutic agent selected from a lysosomal enzyme, an autophagy-inducing agent, or a combination thereof. Steatosis-associated disorders discussed herein include GSD Ia, GSD Ib, GSD Ic, NAFLD, and NASH. Other embodiments are directed to methods of reversing steatosis, modulating autophagy, inducing autophagy, and reversing glycogen storage. Methods of treating a cytoplasmic glycogen storage disorder by administering a lysosomal enzyme and a second therapeutic agent are also described. Other embodiments are directed to methods of treating a cytoplasmic glycogen storage disorder by administering a therapeutic agent as an adjunctive therapy to lysosomal enzyme replacement therapy.

公开(公告)号：US12023333B2

公开(公告)日：2024-07-02

申请号：US17609177

申请日：2020-05-07

Applicant: GREY WOLF THERAPEUTICS LIMITED

Inventor： Martin Quibell ,  Jason John Shiers ,  Michael Sparenberg

IPC: A61K31/505 ,  A61K31/192 ,  A61K31/277 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/50 ,  A61K45/06 ,  A61P37/02 ,  C07C311/29 ,  C07D207/325 ,  C07D207/327 ,  C07D207/335 ,  C07D213/42 ,  C07D213/56 ,  C07D213/57 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/08 ,  C07D257/04 ,  C07D263/32 ,  C07D275/02 ,  C07D277/28 ,  C07D277/30 ,  C07D307/52 ,  C07D333/20 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

CPC classification number: A61K31/505 ,  A61K31/192 ,  A61K31/277 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/402 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/50 ,  A61K45/06 ,  A61P37/02 ,  C07C311/29 ,  C07D207/325 ,  C07D207/327 ,  C07D207/335 ,  C07D213/42 ,  C07D213/56 ,  C07D213/57 ,  C07D231/12 ,  C07D233/64 ,  C07D237/08 ,  C07D239/26 ,  C07D249/08 ,  C07D257/04 ,  C07D263/32 ,  C07D275/02 ,  C07D277/28 ,  C07D277/30 ,  C07D307/52 ,  C07D333/20 ,  C07D333/22 ,  C07D333/24 ,  C07D333/38 ,  C07D401/10 ,  C07D403/10 ,  C07D409/10 ,  C07D413/10 ,  C07D417/10

Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X—Y is —NHSO2— or —SO2NH—; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, C land alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; and R9 is H, alkyl or halo; R10 and R11 are each independently H or alkyl; and R12 and R13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (1a) and (1b).