公开(公告)号：US20240299350A1

公开(公告)日：2024-09-12

申请号：US18612430

申请日：2024-03-21

申请人： AMGEN INC.

发明人： William Brett Caldwell ,  Nathan Bennette ,  Christi Hostetler ,  Kazden Ingram ,  Dory King ,  Kyle Kyburz ,  Alison Viles

IPC分类号： A61K31/4035 ,  A61K9/00 ,  A61K9/20 ,  A61K9/28

CPC分类号： A61K31/4035 ,  A61K9/0065 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/2086 ,  A61K9/2853 ,  A61K9/2866

摘要： Provided herein are oral dosage forms comprising a) a core tablet comprising (i) a drug layer comprising apremilast and hypromellose acetate succinate (HPMCAS) in an amorphous solid dispersion; and (ii) a swellable layer comprising one or more swellable polymers; and b) a coating layer disposed on the core tablet, wherein the oral dosage form surface comprises at least one drug release orifice. The disclosed oral dosage forms provide once-a-day dosing of apremilast and are suitable for treating diseases or disorders ameliorated by inhibiting phosphodiesterase subtype IV (PDE4).

公开(公告)号：US12076405B2

公开(公告)日：2024-09-03

申请号：US17164446

申请日：2021-02-01

申请人： C4 Therapeutics, Inc.

发明人： Andrew J. Phillips ,  Christopher G. Nasveschuk ,  James A. Henderson ,  Yanke Liang ,  Mark E. Fitzgerald ,  Minsheng He ,  Ryan E. Michael

IPC分类号： A61K47/54 ,  A61K31/4035 ,  A61K31/438 ,  A61K31/439 ,  A61K31/454 ,  A61K31/547 ,  A61K31/55 ,  C07D401/04 ,  C07D403/04

CPC分类号： A61K47/545 ,  A61K31/4035 ,  A61K31/438 ,  A61K31/439 ,  A61K31/454 ,  A61K31/547 ,  A61K31/55 ,  A61K47/554 ,  C07D403/04

摘要： This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.

公开(公告)号：US12071429B2

公开(公告)日：2024-08-27

申请号：US17164045

申请日：2021-02-01

申请人： ASTEX THERAPEUTICS LIMITED ,  CANCER RESEARCH TECHNOLOGY LIMITED

发明人： Gianni Chessari ,  Steven Howard ,  Ildiko Maria Buck ,  Benjamin David Cons ,  Christopher Norbert Johnson ,  Rhian Sara Holvey ,  David Charles Rees ,  Jeffrey David St. Denis ,  Emiliano Tamanini ,  Bernard Thomas Golding ,  Ian Robert Hardcastle ,  Celine Florence Cano ,  Duncan Charles Miller ,  Martin Edward Mäntylä Noble ,  Roger John Griffin ,  James Daniel Osborne ,  Joanne Peach ,  Arwel Lewis ,  Kim Louise Hirst ,  Benjamin Paul Whittaker ,  David Wyn Watson ,  Dale Robert Mitchell

IPC分类号： C07D405/14 ,  A61K31/4035 ,  A61P35/00 ,  C07D209/48 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07F9/572

CPC分类号： C07D405/14 ,  A61K31/4035 ,  A61P35/00 ,  C07D209/48 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07F9/5728 ,  C07B2200/05

摘要： The invention provides a compound of formula (I):




or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims.

Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.

公开(公告)号：US20240277659A1

公开(公告)日：2024-08-22

申请号：US18405593

申请日：2024-01-05

申请人： Trustees of Tufts College

发明人： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC分类号： A61K31/402 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/69 ,  A61K35/13 ,  A61K39/00 ,  A61K39/39 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04

CPC分类号： A61K31/402 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/4439 ,  A61K31/69 ,  A61K35/13 ,  A61K39/39 ,  A61K45/06 ,  A61P35/00 ,  A61P37/04 ,  A61K2039/505

摘要： Disclosed are combination therapies including administration of I-DASH inhibitors and PGE2 antagonists, and the use of such therapies in the treatment of cell proliferative diseases.

公开(公告)号：US20240238248A1

公开(公告)日：2024-07-18

申请号：US18289399

申请日：2022-05-10

申请人： Ji Xing Pharmaceuticals Hong Kong Limited

发明人： Naoko NISHIMURA ,  Keiji HASUMI ,  Kazuo HONDA

IPC分类号： A61K31/4035 ,  A61P9/10

CPC分类号： A61K31/4035 ,  A61P9/10

摘要： To provide a safe and effective therapy and pharmaceutical composition using SMTP-7 (Compound I) or a salt thereof in cerebral infarction patients. A pharmaceutical composition for treating cerebral infarction, comprising SMTP-7 (Compound I) or a pharmacological acceptable salt thereof, which is administered at a dose of 1 to 6 mg/kg as SMTP-7 (Compound I) or a salt thereof.

公开(公告)号：US20240199548A1

公开(公告)日：2024-06-20

申请号：US18283834

申请日：2022-03-25

申请人： Jacobio Pharmaceuticals Co., Ltd.

发明人： Yang YE ,  Xiuwei LI ,  Guiqun YANG ,  Fashun YAN ,  Yanping WANG ,  Wei LONG

IPC分类号： C07D209/44 ,  A61K31/4035 ,  A61K31/437 ,  A61K45/06 ,  C07D471/04

CPC分类号： C07D209/44 ,  A61K31/4035 ,  A61K31/437 ,  A61K45/06 ,  C07D471/04

摘要： Compounds of general Formula S-1, S-2, S-3 and their pharmaceutically acceptable salts, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are synthesis, compositions, and uses of such compounds.

公开(公告)号：US11969409B2

公开(公告)日：2024-04-30

申请号：US18196718

申请日：2023-05-12

申请人： AMGEN INC.

发明人： Nathan Bennette ,  William Brett Caldwell ,  Christi Hostetler ,  Kazden Ingram ,  Dory King ,  Kyle Kyburz ,  Alison Viles

IPC分类号： A61K9/20 ,  A61K9/00 ,  A61K9/28 ,  A61K31/4035

CPC分类号： A61K31/4035 ,  A61K9/0065 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/2086 ,  A61K9/2853 ,  A61K9/2866

摘要： Provided herein are oral dosage forms comprising a) a core tablet comprising (i) a drug layer comprising apremilast and hypromellose acetate succinate (HPMCAS) in an amorphous solid dispersion; and (ii) a swellable layer comprising one or more swellable polymers; and b) a coating layer disposed on the core tablet, wherein the oral dosage form surface comprises at least one drug release orifice. The disclosed oral dosage forms provide once-a-day dosing of apremilast and are suitable for treating diseases or disorders ameliorated by inhibiting phosphodiesterase subtype IV (PDE4).

公开(公告)号：US11945805B2

公开(公告)日：2024-04-02

申请号：US17243872

申请日：2021-04-29

申请人： CHEMOCENTRYX, INC.

发明人： Xi Chen ,  Dean R. Dragoli ,  Junfa Fan ,  Jaroslaw Kalisiak ,  Manmohan Reddy Leleti ,  Viengkham Malathong ,  Jeffrey McMahon ,  Hiroko Tanaka ,  Ju Yang ,  Chao Yu ,  Penglie Zhang ,  Venkat Mali

IPC分类号： C07D405/12 ,  A61K31/4035 ,  A61K31/422 ,  A61K31/4439 ,  A61K45/06 ,  A61P11/00 ,  A61P17/06 ,  A61P35/00 ,  A61P37/00 ,  C07B59/00 ,  C07D405/14 ,  C07D413/12

CPC分类号： C07D405/12 ,  A61K31/4035 ,  A61K31/422 ,  A61K31/4439 ,  A61K45/06 ,  A61P11/00 ,  A61P17/06 ,  A61P35/00 ,  A61P37/00 ,  C07B59/002 ,  C07D405/14 ,  C07D413/12 ,  C07B2200/05 ,  A61K31/4035 ,  A61K2300/00 ,  A61K31/422 ,  A61K2300/00 ,  A61K31/4439 ,  A61K2300/00

摘要： Compounds are provided as inhibitors of CXCR2, having the structure:

公开(公告)号：US20230381161A1

公开(公告)日：2023-11-30

申请号：US18446268

申请日：2023-08-08

申请人： THE GEORGE INSTITUTE FOR GLOBAL HEALTH

发明人： Anthony RODGERS ,  Stephen MACMAHON

IPC分类号： A61K31/4422 ,  A61P9/12 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/41 ,  A61K31/382 ,  A61K31/40 ,  A61K31/277 ,  A61K31/4178 ,  A61K31/517 ,  A61K31/4035 ,  A61K31/495 ,  A61K31/554 ,  A61K31/4418 ,  A61K31/549

CPC分类号： A61K31/4422 ,  A61P9/12 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/41 ,  A61K31/382 ,  A61K31/40 ,  A61K31/277 ,  A61K31/4178 ,  A61K31/517 ,  A61K31/4035 ,  A61K31/495 ,  A61K31/554 ,  A61K31/4418 ,  A61K31/549

摘要： Provided herein are pharmaceutical compositions that are useful for the treatment of hypertension comprising an angiotensin II receptor blocker, a diuretic, and a calcium channel blocker.

公开(公告)号：US11787782B2

公开(公告)日：2023-10-17

申请号：US17472349

申请日：2021-09-10

申请人： IDORSIA PHARMACEUTICALS LTD

发明人： Marc Bellet ,  Martin Bolli ,  Martine Clozel ,  Marc Iglarz

IPC分类号： C07D403/12 ,  A61P9/12 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/4418 ,  A61K31/506 ,  A61K31/549 ,  A61P13/12

CPC分类号： C07D403/12 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/4418 ,  A61K31/506 ,  A61K31/549 ,  A61P9/12 ,  A61P13/12 ,  C07B2200/13

摘要： The present invention concerns the compound aprocitentan, {5-(4-bromo-phenyl)-6-[2-(5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, and its use as endothelin receptor antagonist, in combination with other active ingredients or therapeutic agents including an angiotenin receptor blocker, and/or a calcium channel blocker, and preferably a diuretic which is a thiazide-like diuretic, in the prophylaxis or treatment of certain endothelin related diseases. The invention further relates to pharmaceutical compositions comprising aprocitentan in combination with said other active ingredients or therapeutic agents. The invention further relates to such pharmaceutical compositions comprising novel crystalline forms of aprocitentan.