公开(公告)号：US20240342186A1

公开(公告)日：2024-10-17

申请号：US18734077

申请日：2024-06-05

Applicant: Boehringer Ingelheim International GmbH

Inventor： Annekatrin Charlotte HEIMANN ,  Sandra Ruth HANDSCHUH ,  Christoph HOENKE ,  Cédrickx GODBOUT ,  Christian GNAMM ,  Patrick GROSS ,  Marc Alexander GRUNDL ,  Joerg Thomas KLEY ,  Christian Andreas KUTTRUFF ,  Dirk REINART ,  Raphael STUBER ,  Theodor THEIS

IPC: A61K31/5386 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/395 ,  A61K45/06 ,  A61P37/06 ,  C07D491/048 ,  C07D519/00

CPC classification number: A61K31/5386 ,  A61K31/4412 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/3955 ,  A61K45/06 ,  A61P37/06 ,  C07D491/048 ,  C07D519/00

Abstract: The invention relates to new proline derivatives of formula (I) as cGAS inhibitors,






wherein
wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and G are defined as in claim 1,
and prodrugs or pharmaceutically acceptable salts of these compounds
for the treatment of diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), non-alcoholic steatotic hepatitis (NASH), interstitial lung disease (ILD) and idiopathic pulmonary fibrosis (IPF).

公开(公告)号：US20240335434A1

公开(公告)日：2024-10-10

申请号：US18511042

申请日：2023-11-16

Applicant: Akebia Therapeutics, Inc.

Inventor： Robert Shalwitz ,  Charlotte Hartman ,  Akshay Buch ,  Isaiah Shalwitz ,  John Janusz ,  Joseph Gardner

IPC: A61K31/44 ,  A61K9/00 ,  A61K31/4412 ,  A61K33/26 ,  A61K38/18

CPC classification number: A61K31/44 ,  A61K9/0053 ,  A61K31/4412 ,  A61K33/26 ,  A61K38/1816

Abstract: Provided herein are specific doses of, and dosing regimens for, using a HIF prolyl hydroxylase inhibitor in treating or preventing anemia, such as anemia secondary to or associated with chronic kidney disease, anemia associated with or resulting from chemotherapy, or anemia associated with AIDS.

公开(公告)号：US12083106B2

公开(公告)日：2024-09-10

申请号：US17351151

申请日：2021-06-17

Applicant: Excalibur Pharmaceuticals, Inc.

Inventor： Juan Socorro Armendáriz Borunda ,  José Agustín Rogelio Magaña Castro ,  Jorge Cervantes Guadarrama

IPC: A61K31/4418 ,  A61K9/00 ,  A61K9/20 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/717 ,  A61P25/02 ,  A61P29/00

CPC classification number: A61K31/4418 ,  A61K9/0053 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2054 ,  A61K9/2095 ,  A61K31/4412 ,  A61P25/02 ,  A61P29/00 ,  A61K31/44 ,  A61K31/717

Abstract: The instant invention relates to a process for the preparation of a pharmaceutical composition in sustained-release tablet form comprising from 600 milligrams to 2400 milligrams of Pirfenidone (PFD), in such a way that the drug is bioavailable during an extended period of time of 12 hours from its administration. In this way, the anti-fibrotic and anti-inflammatory action of the drug Pirfenidone is optimized. Moreover, the instant invention offers advantages and a higher therapeutic efficacy compared to other pharmaceutical forms of Pirfenidone for oral administration and its therapeutic application in the regression of chronic renal failure secondary to primary glomerulosclerosis; it shows a better activity with regard to the reduction and/or regression of deleterious effects in breast capsular contracture observed after the surgical implantation of breast implants in humans and has an important anti-TNF-α and anti-TGF-β1 action for the treatment of hepatic fibrosis.

公开(公告)号：US20240293419A1

公开(公告)日：2024-09-05

申请号：US18478483

申请日：2023-09-29

Applicant: Epizyme, Inc. ,  Health Research, Inc.

Inventor： Heike KEILHACK ,  Roberto Pili

IPC: A61K31/5377 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K45/06 ,  A61P35/00

CPC classification number: A61K31/5377 ,  A61K31/404 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K45/06 ,  A61P35/00

Abstract: The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents (such as tyrosine kinase inhibitors or VEGF/VEGFR inhibitors), particularly anticancer agents such as sunitinib, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

公开(公告)号：US20240293381A1

公开(公告)日：2024-09-05

申请号：US18431267

申请日：2024-02-02

Applicant: CELGENE QUANTICEL RESEARCH, INC.

Inventor： Lynnie Trzoss ,  Juan Manuel Betancort ,  Toufike Kanouni ,  Michael Brennan Wallace ,  Amogh Boloor

IPC: A61K31/4412 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

CPC classification number: A61K31/4412 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

Abstract: The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.

公开(公告)号：US20240285971A1

公开(公告)日：2024-08-29

申请号：US18569636

申请日：2022-06-19

Applicant: ALPHA TAU MEDICAL LTD.

Inventor： Yona Keisari ,  Itzhak Kelson ,  Vered Domankevich ,  Yossi Nishri ,  Tomer Cooks ,  Margalit Efrati ,  Ronen Segal ,  Robert Den ,  Ishai Luz ,  Maayan Hedva Vatarescu ,  Sara Del Mare Roumani ,  Amit Shai

IPC: A61N5/10 ,  A61K9/00 ,  A61K31/4412 ,  A61K39/00 ,  A61K51/12 ,  C07K16/22

CPC classification number: A61N5/1001 ,  A61K9/0019 ,  A61K31/4412 ,  A61K51/1282 ,  C07K16/22 ,  A61K2039/505 ,  A61K2039/545 ,  A61N2005/101 ,  A61N2005/1024

Abstract: A vascular inhibitor for use as a medicament for treatment of a tumor of a patient wherein the administration pattern of the medicament comprises administering a therapeutically effective amount of the vascular inhibitor to the patient, in one or more sessions, and implanting seeds (204) carrying radium-224 in the tumor for intra-tumoral alpha-emitter radiotherapy less than two weeks from administering the vascular inhibitor.

公开(公告)号：US20240245698A1

公开(公告)日：2024-07-25

申请号：US18606946

申请日：2024-03-15

Applicant: Epizyme, Inc.

Inventor： Kevin W. KUNTZ ,  Richard CHESWORTH ,  Kenneth W. DUNCAN ,  Heike KEILHACK ,  Natalie WARHOLIC ,  Christine KLAUS ,  Sarah K. KNUTSON ,  Timothy J.N. WIGLE ,  Masashi SEKI ,  Syuji SHIROTORI ,  Satoshi KAWANO

IPC: A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

CPC classification number: A61K31/5377 ,  A61K31/4412 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/551 ,  A61K31/553 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/08 ,  C07D491/107 ,  C07D498/08

Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：US20240217949A1

公开(公告)日：2024-07-04

申请号：US18429297

申请日：2024-01-31

Applicant: ZHUHAI UNITED LABORATORIES CO., LTD.

Inventor： Peng LI ,  Xiaolin LI ,  Zhi LUO ,  Haiying HE ,  Guoping HU ,  Jian LI ,  Shuhui CHEN

IPC: C07D401/12 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/444 ,  A61P27/04 ,  C07D213/73 ,  C07D401/04 ,  C07D401/06

CPC classification number: C07D401/12 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/444 ,  A61P27/04 ,  C07D213/73 ,  C07D401/04 ,  C07D401/06

Abstract: Provided is an aldehyde binder, specifically, disclosed is a compound as represented by formula (II) or a pharmaceutically acceptable salt.

公开(公告)号：US20240216501A1

公开(公告)日：2024-07-04

申请号：US18607027

申请日：2024-03-15

Applicant: Gritstone bio, Inc.

Inventor： Raphael Rousseau ,  Andrew Ferguson ,  Karin Jooss

IPC: A61K39/235 ,  A61K9/00 ,  A61K31/4412 ,  A61K39/00 ,  A61K45/06 ,  A61P35/00 ,  C07K16/22 ,  C07K16/28 ,  C12N7/00

CPC classification number: A61K39/235 ,  A61K9/0019 ,  A61K31/4412 ,  A61K45/06 ,  A61P35/00 ,  C07K16/22 ,  C07K16/2818 ,  C07K16/2827 ,  C12N7/00 ,  A61K2039/507 ,  A61K2039/54 ,  A61K2039/545 ,  A61K2039/55555 ,  C12N2710/10321 ,  C12N2710/10334 ,  C12N2710/10343 ,  C12N2770/36134 ,  C12N2770/36143

Abstract: Disclosed herein are compositions that include antigen-encoding nucleic acid sequences and/or antigen peptides. Also disclosed are nucleotides, cells, and methods associated with the compositions including their use as vaccines, including vectors and methods for a heterologous prime/boost vaccination strategy.

公开(公告)号：US20240189292A1

公开(公告)日：2024-06-13

申请号：US18278715

申请日：2022-02-25

Applicant: MEDSHINE DISCOVERY INC.

Inventor： Xiaobing YAN ,  Wei LAI ,  Charles Z. DING ,  Shuhui CHEN

IPC: A61K31/4412 ,  A61K31/438 ,  A61P9/04 ,  C07D213/73 ,  C07D221/20 ,  C07D471/10 ,  C07D491/107

CPC classification number: A61K31/4412 ,  A61K31/438 ,  A61P9/04 ,  C07D213/73 ,  C07D221/20 ,  C07D471/10 ,  C07D491/107

Abstract: The present invention relates to a series of substituted pyridine-2,4-dione derivatives and preparation methods therefor, and in particular, to a compound represented by formula (I) and a pharmaceutically acceptable salt thereof.