公开(公告)号：US20240383852A1

公开(公告)日：2024-11-21

申请号：US18281038

申请日：2022-03-11

Applicant: INFEX Therapeutics Limited

Inventor： James Kirkham ,  Ian Cooper ,  Adam Bunt ,  Kevin Blades ,  David Orr ,  Andrew Wilkinson ,  Paul Schofield

IPC: C07D211/14 ,  A61K31/36 ,  A61K31/397 ,  A61K31/407 ,  A61K31/415 ,  A61K31/4375 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/451 ,  A61K31/495 ,  A61K31/4995 ,  A61K31/505 ,  A61K31/506 ,  A61K31/551 ,  C07D211/12 ,  C07D213/02 ,  C07D213/38 ,  C07D213/56 ,  C07D231/12 ,  C07D239/42 ,  C07D243/08 ,  C07D285/08 ,  C07D295/033 ,  C07D317/50 ,  C07D333/20 ,  C07D403/04 ,  C07D471/18 ,  C07D487/04 ,  C07D487/10

Abstract: This invention relates to compounds that can be used to treat viral infections. The compounds are papain-like protease (PLpro) inhibitors.

公开(公告)号：US20240374582A1

公开(公告)日：2024-11-14

申请号：US18764257

申请日：2024-07-04

Applicant: GENOSCO Inc.

Inventor： Wongil LEE ,  William G. DEVINE ,  R. Bruce DIEBOLD ,  So Young HWANG ,  Yunggeun CHOI ,  Yan LIU ,  Sang-Ae SEUNG ,  Miyong YONG ,  Sewon KIM ,  Jaekyoo LEE ,  Jong Sung KOH

IPC: A61K31/4725 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/675 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D498/08 ,  C07D513/04 ,  C07F9/6558

Abstract: The present invention relates to novel substituted bicyclic derivatives that can inhibit Rho-kinases and/or Rho-kinase mediated phosphorylation of myosin light chain phosphates, compositions comprising the derivatives, methods for preparing the derivatives, and methods for using the derivatives and/or compositions.

公开(公告)号：US20240366632A1

公开(公告)日：2024-11-07

申请号：US18684010

申请日：2022-08-31

Applicant: INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE ,  ASSISTANCE PUBLIQUE-HÔPITAUX DE PARIS (APHP) ,  SORBONNE UNIVERSITÉ ,  UNIVERSITÉ PARIS CITÉ

Inventor： Francine BEHAR-COHEN ,  Min ZHAO

IPC: A61K31/585 ,  A61K31/4375 ,  A61K31/573 ,  A61K31/575 ,  A61P27/02 ,  C12N15/113

Abstract: Ocular Rosacea (OR) is a chronic inflammatory and neurovascular diseases of the ocular surface and eyelids. associated with abnormal tear film lipids that can lead to corneal neovascularization, loss of transparency and ulceration. Here, the inventors show that the combination of mineralocorticoid receptor blockade in association with local ocular glucocorticoids that have high GR binding affinity, have superior effects as compared to MR blockade alone, without the side effects of glucocorticoids on corneal wound healing. The combination of MR antagonist and low dose of a GR activator further reduces corneal edema, corneal neovascularization and improves corneal wound healing. The combination of MR antagonist and triamcinolone that has a strong GR binding affinity reinforces the beneficial effects of MR antagonists. Finally, the inventors show that MR is overexpressed in ocular surface tissues and Meibomian glands of patients with ocular rosacea, and that transgenic rats that over express the human MR have molecular markers in their meibomian glands, similar to those of patients with OR. Thus, MR antagonists and GR agonist with strong GR affinity is a suitable combination for the treatment of OR.

公开(公告)号：US12129259B1

公开(公告)日：2024-10-29

申请号：US18635375

申请日：2024-04-15

Applicant: KING FAISAL UNIVERSITY

Inventor： Michelyne Haroun ,  Christophe Tratrat

IPC: C07D487/22 ,  A61K31/4375 ,  A61P35/00

CPC classification number: C07D487/22 ,  A61K31/4375 ,  A61P35/00

Abstract: Novel pyrazino[1′,2′:1,5]pyrazolo[4,3-b][1,6]naphthyridine, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrazino[1′,2′:1,5]pyrazolo[4,3-b][1,6]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

公开(公告)号：US20240352040A1

公开(公告)日：2024-10-24

申请号：US18293374

申请日：2022-08-02

Applicant: GENFLEET THERAPEUTICS (SHANGHAI) INC. ,  ZHEJIANG GENFLEET THERAPEUTICS CO., LTD.

Inventor： Fusheng ZHOU ,  Yuanzhi TAO ,  Jinzhu ZHAO ,  Jiong LAN

IPC: C07D519/00 ,  A61K31/185 ,  A61K31/194 ,  A61K31/4375 ,  C07C55/22 ,  C07C57/145 ,  C07C57/15 ,  C07C309/04 ,  C07C309/23 ,  C07C309/24

CPC classification number: C07D519/00 ,  A61K31/185 ,  A61K31/194 ,  A61K31/4375 ,  C07C55/22 ,  C07C57/145 ,  C07C57/15 ,  C07C309/04 ,  C07C309/23 ,  C07C309/24 ,  C07B2200/13 ,  C07C2601/14 ,  C07C2601/16

Abstract: Disclosed are a crystal form of a RIPK1 inhibitor, an acid salt thereof, and a crystal form of an acid salt thereof. The crystal form of the RIPK1 inhibitor, the acid salt thereof, and the crystal form of the acid salt thereof have advantages of good stability and low hygroscopicity, and same have good pharmaceutical prospects.

公开(公告)号：US12116363B2

公开(公告)日：2024-10-15

申请号：US16657477

申请日：2019-10-18

Applicant: SENHWA BIOSCIENCES, INC.

Inventor： John Soong

IPC: C07D471/04 ,  A61K31/4375 ,  A61K31/7068 ,  A61K33/243 ,  A61K45/06 ,  A61P35/00 ,  A61P35/04 ,  C07K16/28

CPC classification number: C07D471/04 ,  A61P35/00 ,  A61K45/06

Abstract: The present disclosure provides a method for treating a cancer or refractory cancer and/or inhibiting cancer metastasis, recurrence or progression in a subject or increasing the likelihood of survival over a relevant period in a subject diagnosed with a cancer, comprising administering to a subject a combination of an anti-cancer agent, a CK2 inhibitor and optionally an immune checkpoint inhibitor. The method of the present disclosure increases the number of T cells and activated T cells in the tumor microenvironment and thus can modulate immune in cancer therapy.

公开(公告)号：US20240335433A1

公开(公告)日：2024-10-10

申请号：US18627617

申请日：2024-04-05

Applicant: Dennis W. Stacey

Inventor： Dennis W. Stacey

IPC: A61K31/4375 ,  A61K9/00 ,  A61P35/00

CPC classification number: A61K31/4375 ,  A61K9/0019 ,  A61P35/00

Abstract: A normal cell cycle synchronization process includes repeated administration of a drug specifically toxic for a single cell cycle phase to selectively synchronize normal cells. The selective synchronization of normal cells allows for the selective targeting of abnormal cells with cell cycle phase specific toxins. Such selective targeting may be useful in the treatment of a number of medical conditions.

公开(公告)号：US20240317708A1

公开(公告)日：2024-09-26

申请号：US18573802

申请日：2022-06-30

Applicant: ZEDIRA GMBH

Inventor： Ralf PASTERNACK ,  Christian BÜCHOLD ,  Martin HILS ,  Martin STIELER ,  Uwe GERLACH

IPC: C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

CPC classification number: C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

Abstract: The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases, in particular transglutaminase 2.

公开(公告)号：US12091397B2

公开(公告)日：2024-09-17

申请号：US17878753

申请日：2022-08-01

Applicant: C4 Therapeutics, Inc.

Inventor： Roger Norcross ,  Adrian Britschgi ,  Fabian Dey ,  Annick Goergler ,  Eric Andre Kusznir ,  Moreno Attilio Wichert

IPC: C07D401/04 ,  A61K31/4375 ,  A61K31/4704 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/14 ,  C07D519/00

CPC classification number: C07D401/04 ,  A61K31/4375 ,  A61K31/4704 ,  A61K47/55 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/14 ,  C07D519/00

Abstract: The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

公开(公告)号：US20240299369A1

公开(公告)日：2024-09-12

申请号：US18663025

申请日：2024-05-13

Applicant: Allergan Pharmaceuticals International Limited ,  Merck Sharp & Dohme Corp.

Inventor： Joel M. Trugman ,  Ramesh Boinpally ,  Abhijeet Jakate ,  Michelle Finnegan ,  Mary Ann Johnson ,  Leonardo Resende Allain ,  W. Mark Eickhoff ,  Craig B. Ikeda ,  Chad D. Brown ,  Francis J. Flanagan, JR. ,  Rebecca Nofsinger ,  Melanie Marota ,  Lisa Lupton ,  Paresh B. Patel ,  Hanmi Xi ,  Wei Xu

IPC: A61K31/4375 ,  A61K31/4545 ,  A61P25/06

CPC classification number: A61K31/4375 ,  A61K31/4545 ,  A61P25/06

Abstract: The present disclosure provides methods for the acute treatment of migraine with or without aura, comprising the administration of ubrogepant. In particular, the present disclosure provides methods for the acute treatment of migraine in patients having hepatic impairment; in patients with renal impairment; and in patients concurrently taking CYP3A4 modulators or BCRP and/or P-gp only inhibitors.