公开(公告)号：US12083176B2

公开(公告)日：2024-09-10

申请号：US17560402

申请日：2021-12-23

Applicant: Sanofi Biotechnology

Inventor： Corinne Hanotin ,  Laurence Bessac ,  Umesh Chaudhari

IPC: C07K16/40 ,  A61K39/395 ,  A61P3/06 ,  A61J1/05 ,  A61K31/215 ,  A61K31/366 ,  A61K31/404 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K39/00 ,  A61K45/06 ,  C07K14/47

CPC classification number: A61K39/3955 ,  A61P3/06 ,  C07K16/40 ,  A61J1/05 ,  A61K31/215 ,  A61K31/366 ,  A61K31/404 ,  A61K31/435 ,  A61K31/47 ,  A61K31/505 ,  A61K39/395 ,  A61K2039/505 ,  A61K2039/545 ,  A61K45/06 ,  C07K14/4703 ,  C07K2317/21 ,  C07K2317/76

Abstract: The present invention relates to methods for treating diseases or conditions in which proprotein convertase subtilisin/kexin type 9 (PCSK9) expression or activity causes an impact by administration of PCSK9-specific antibodies or antigen-binding fragments thereof and preferably by additional administration of an inhibitor of 3-hydroxy-3-methyl-glutaryl-CoA reductase (HMG-CoA reductase). The present invention further relates to PCSK9-specific antibodies or antigen-binding fragments thereof for use in the treatment of diseases or conditions in which PCSK9 expression or activity causes an impact. The present invention also relates to articles of manufacture comprising packaging material, PCSK9-specific antibodies or antigen-binding fragments thereof, and a label or packaging insert indicating which groups of patients can be treated with said antibodies or fragments, which groups of patients must not be treated with said antibodies or fragments, and which dosage regimen should be used. The present invention further relates to methods of testing the efficacy of PCSK9-specific antibodies or antigen-binding fragments thereof for the treatment of certain diseases or conditions and for the treatment of specific sub-groups of patients.

公开(公告)号：US20240285614A1

公开(公告)日：2024-08-29

申请号：US18433734

申请日：2024-02-06

Applicant: Boundless Bio, Inc.

Inventor： Anthony B. PINKERTON ,  Jacques MAUGER ,  Yen Pham Hong TRUONG ,  Camille REMEUR ,  Jérôme TOUM ,  Olivier MIRGUET

IPC: A61K31/496 ,  A61K31/404 ,  A61K31/435 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4995 ,  A61K45/06 ,  C07D207/12 ,  C07D209/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08

CPC classification number: A61K31/496 ,  A61K31/404 ,  A61K31/435 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4995 ,  A61K45/06 ,  C07D207/12 ,  C07D209/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08

Abstract: Provided herein are compounds and methods for the treatment of cancer. The methods include administering to a subject in need a therapeutically effective amount of a cyclic sulfonamide RNR inhibitor disclosed herein.

公开(公告)号：US12048748B2

公开(公告)日：2024-07-30

申请号：US17524558

申请日：2021-11-11

Applicant: C4 Therapeutics, Inc.

Inventor： Andrew J. Phillips ,  Christopher G. Nasveschuk ,  James A. Henderson ,  Yanke Liang ,  Kiel Lazarski ,  Ryan E. Michael

IPC: A61K31/435 ,  A61K31/438 ,  A61K47/54 ,  C07D471/10 ,  C07D498/20 ,  C07D519/00

CPC classification number: A61K47/545 ,  A61K31/435 ,  A61K31/438 ,  A61K47/554 ,  C07D471/10 ,  C07D498/20 ,  C07D519/00

Abstract: This invention provides compounds that have spirocyclic E3 Ubiquitin Ligase targeting moieties (Degrons), which can be used as is or linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.

公开(公告)号：US20240246909A1

公开(公告)日：2024-07-25

申请号：US18408389

申请日：2024-01-09

Applicant: The Wistar Institute of Anatomy and Biology

Inventor： Troy E. Messick ,  Garry R. Smith ,  Allen B. Reitz ,  Paul M. Lieberman ,  Mark E. McDonnell ,  Yan Zhang ,  Marianne Carlsen ,  Shuai Chen

IPC: C07D209/08 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  A61P31/20 ,  A61P35/00 ,  C07D277/62 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107

CPC classification number: C07D209/08 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  A61P31/20 ,  A61P35/00 ,  C07D277/62 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107

Abstract: The present invention provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity, such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The present invention further provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection and/or lytic EBV infection.

公开(公告)号：US11919839B2

公开(公告)日：2024-03-05

申请号：US17238529

申请日：2021-04-23

Applicant: Valo Health, Inc.

Inventor： Kenneth W. Bair ,  Nicholas Barczak ,  Bingsong Han ,  David R. Lancia, Jr. ,  Cuixian Liu ,  Matthew W. Martin ,  Pui Yee Ng ,  Aleksandra Rudnitskaya ,  Jennifer R. Thomason ,  Mary-Margaret Zablocki ,  Xiaozhang Zheng

IPC: C07C259/06 ,  A61K31/185 ,  A61K31/277 ,  A61K31/397 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/417 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/495 ,  A61K31/5377 ,  C07D207/10 ,  C07D207/267 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D209/46 ,  C07D211/16 ,  C07D211/58 ,  C07D213/56 ,  C07D213/65 ,  C07D213/75 ,  C07D213/81 ,  C07D215/12 ,  C07D221/20 ,  C07D231/14 ,  C07D231/18 ,  C07D233/36 ,  C07D233/38 ,  C07D233/68 ,  C07D235/14 ,  C07D235/30 ,  C07D239/20 ,  C07D239/22 ,  C07D241/08 ,  C07D241/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/18 ,  C07D277/56 ,  C07D295/155 ,  C07D295/192 ,  C07D307/68 ,  C07D317/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D493/08 ,  C07D495/10 ,  C07D498/04 ,  C07D513/10

CPC classification number: C07C259/06 ,  A61K31/185 ,  A61K31/277 ,  A61K31/397 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/417 ,  A61K31/4184 ,  A61K31/435 ,  A61K31/438 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/495 ,  A61K31/5377 ,  C07D207/10 ,  C07D207/267 ,  C07D209/08 ,  C07D209/42 ,  C07D209/44 ,  C07D209/46 ,  C07D211/16 ,  C07D211/58 ,  C07D213/56 ,  C07D213/65 ,  C07D213/75 ,  C07D213/81 ,  C07D215/12 ,  C07D221/20 ,  C07D231/14 ,  C07D231/18 ,  C07D233/36 ,  C07D233/38 ,  C07D233/68 ,  C07D235/14 ,  C07D235/30 ,  C07D239/20 ,  C07D239/22 ,  C07D241/08 ,  C07D241/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/18 ,  C07D277/56 ,  C07D295/155 ,  C07D295/192 ,  C07D307/68 ,  C07D317/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D491/10 ,  C07D493/08 ,  C07D495/10 ,  C07D498/04 ,  C07D513/10 ,  Y02A50/30

Abstract: The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

公开(公告)号：US11857636B2

公开(公告)日：2024-01-02

申请号：US17169217

申请日：2021-02-05

Applicant: TAGWORKS PHARMACEUTICALS B.V.

Inventor： Marc Stefan Robillard ,  Hendricus Marie Janssen ,  Wolter Ten Hoeve ,  Ronny Mathieu Versteegen ,  Raffaella Rossin

IPC: C07D257/02 ,  C07D257/08 ,  C07D237/26 ,  C07C33/16 ,  A61K47/68 ,  A61K47/54 ,  B82Y5/00 ,  A61K31/704 ,  A61K38/05 ,  A61K39/395 ,  A61K47/22 ,  A61K31/435 ,  A61K31/444

CPC classification number: A61K47/6803 ,  A61K31/435 ,  A61K31/444 ,  A61K31/704 ,  A61K38/05 ,  A61K39/3955 ,  A61K39/39558 ,  A61K47/22 ,  A61K47/545 ,  A61K47/555 ,  A61K47/558 ,  A61K47/6897 ,  B82Y5/00 ,  C07C33/16 ,  C07D237/26 ,  C07D257/08 ,  Y02A50/30

Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.

公开(公告)号：US11766412B2

公开(公告)日：2023-09-26

申请号：US16334256

申请日：2017-09-26

Applicant: GENEHEAL BIOTECHNOLOGY CO., LTD.

Inventor： Wuguang Pan ,  Wei Zhu

IPC: A61K31/132 ,  A61K31/155 ,  A61K38/05 ,  A61K38/06 ,  A61P25/00 ,  A61P35/00 ,  A61K31/661 ,  A61K31/513 ,  A61K31/198 ,  A61K31/7076 ,  A61K31/675 ,  A61K31/415 ,  A61K31/4402 ,  A61K31/197 ,  A61K31/4188 ,  A61K31/708 ,  C07D213/66 ,  C07D213/77 ,  C07D405/04 ,  C07D401/04 ,  A61K31/43 ,  A61P3/00 ,  C07D261/04 ,  C07D207/12 ,  A61P25/14 ,  A61K31/33 ,  C07D473/34 ,  A61K38/07 ,  A61K31/397 ,  A61K31/7072 ,  A61P25/08 ,  A61K31/40 ,  A61P43/00 ,  A61K31/435

CPC classification number: A61K31/155 ,  A61K31/132 ,  A61K31/197 ,  A61K31/198 ,  A61K31/33 ,  A61K31/397 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4188 ,  A61K31/43 ,  A61K31/435 ,  A61K31/4402 ,  A61K31/513 ,  A61K31/661 ,  A61K31/675 ,  A61K31/708 ,  A61K31/7072 ,  A61K31/7076 ,  A61K38/05 ,  A61K38/06 ,  A61K38/063 ,  A61K38/07 ,  A61P3/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P35/00 ,  A61P43/00 ,  C07D207/12 ,  C07D213/66 ,  C07D213/77 ,  C07D261/04 ,  C07D401/04 ,  C07D405/04 ,  C07D473/34

Abstract: Provided are compounds reducing SAICAR accumulation, and applications. On the basis of existing protein structure data and small molecule structure data, calculations and analysis are performed using software to screen and obtain compounds capable of effectively interfering with PAICS activity, reducing SAICAR synthesis, and ultimately reducing SAICAR accumulation, in order to achieve the goal of treating or improving ADSL deficiency. A better effect in the treatment or improvement of ADSL deficiency is expected from the joint use of at least two of the described compounds.

公开(公告)号：US11717573B2

公开(公告)日：2023-08-08

申请号：US17035293

申请日：2020-09-28

Applicant: South Dakota Board of Regents

Inventor： Khosrow Rezvani ,  Grigoriy Sereda

IPC: A61K47/60 ,  A61K9/51 ,  A61P35/00 ,  A61K47/64 ,  A61K31/435

CPC classification number: A61K47/60 ,  A61K9/5115 ,  A61K9/5161 ,  A61K9/5169 ,  A61K31/435 ,  A61K47/64 ,  A61K47/645 ,  A61P35/00

Abstract: Disclosed herein are compositions for treating cancer comprising a modified veratridine. In certain aspects, the modified veratridine comprises a polyglutamic acid (PLE) or polyethylene glycol/polyglutamic acid (PEG-PLE) conjugated to the 4′ hemiketal thereof. Further disclosed is a method of treating colorectal cancer in a subject comprising administering to a subject an effective amount of the disclosed compositions.

公开(公告)号：US11673890B2

公开(公告)日：2023-06-13

申请号：US17034295

申请日：2020-09-28

Applicant: Pfizer Inc.

Inventor： Mary Theresa Didiuk ,  Robert Lee Dow ,  David Andrew Griffith

IPC: A61K31/435 ,  C07D471/10 ,  C07D491/20 ,  C07D519/00 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10

CPC classification number: C07D471/10 ,  A61K31/435 ,  A61K31/438 ,  A61K31/519 ,  A61K45/06 ,  C07D487/10 ,  C07D491/20 ,  C07D519/00

Abstract: The invention provides a compound of Formula (1)




or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

公开(公告)号：US20230158103A1

公开(公告)日：2023-05-25

申请号：US17908531

申请日：2021-03-02

Applicant: PHARMA MAR, S.A.

Inventor： Nuria IZQUIERDO-USEROS ,  Júlia VERGARA-ALERT ,  Pablo AVILÉS MARÍN ,  Alejandro LOSADA GONZÁLEZ ,  José María FERNÁNDEZ SOUSA-FARO ,  Salvador FUDIO MUÑOZ

IPC: A61K38/15 ,  A61K31/675 ,  A61K31/435 ,  A61K31/27 ,  A61K31/4706 ,  A61P31/14

CPC classification number: A61K38/15 ,  A61K31/675 ,  A61K31/435 ,  A61K31/27 ,  A61K31/4706 ,  A61P31/14

Abstract: The use of PLD with one or more further CoV antiviral agent(s) in the treatment of coronavirus (CoV) infection.