公开(公告)号：US12220401B2

公开(公告)日：2025-02-11

申请号：US18362249

申请日：2023-07-31

Applicant: Loxo Oncology, Inc.

Inventor： Nicolas Guisot

IPC: A61K31/415 ,  A61K31/4155 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  C07D231/14 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/08 ,  C07D405/14 ,  C07D413/06 ,  C07D417/04

Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.

公开(公告)号：US12215086B2

公开(公告)日：2025-02-04

申请号：US17582851

申请日：2022-01-24

Applicant: University of Tennessee Research Foundation

Inventor： Ramesh Narayanan ,  Duane D. Miller ,  Thamarai Ponnusamy ,  Dong-Jin Hwang ,  Yali He

IPC: C07D231/16 ,  A61K9/00 ,  A61K31/277 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/517 ,  A61K31/5375 ,  A61K45/06 ,  C07C255/60 ,  C07C317/46 ,  C07D207/06 ,  C07D207/34 ,  C07D209/08 ,  C07D213/84 ,  C07D233/68 ,  C07D239/74 ,  C07D249/04 ,  C07D249/08 ,  C07D295/15 ,  C07D401/12

Abstract: This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors. R-isomers, and non-hydroxylated and/or non-chiral propenamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic to or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

公开(公告)号：US20250009713A1

公开(公告)日：2025-01-09

申请号：US18712518

申请日：2022-11-24

Applicant: BIOTRON LIMITED

Inventor： Michelle MILLER ,  Gary Dinneen EWART

IPC: A61K31/415 ,  A61P31/14

Abstract: The present invention relates to the treatment or prevention of SARS-COV-2 infection or COVID-19. In particular, the present invention relates to the use of N-carbamimidoyl-5-(1-methyl-1H-pyrazol-4-yl)-2-naphthamide, or a pharmaceutically acceptable salt thereof, in the treatment or prevention of SARS-COV-2 infection or COVID-19.

公开(公告)号：US12187682B2

公开(公告)日：2025-01-07

申请号：US18337313

申请日：2023-06-19

Applicant: Vettore, LLC

Inventor： Kenneth Mark Parnell ,  John McCall

IPC: C07D231/12 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D401/06 ,  C07D405/12 ,  C07D409/04 ,  C07D417/04

Abstract: Provided herein is a method for treating a monocarboxylate transporter MCT4-mediated disorder in a subject in need thereof. The method comprises the step of administering to the subject a compound of structural Formula I and/or a salt thereof. The treatment of the monocarboxylate transporter MCT4-mediated disorder may inhibit activity of MCT4, or a mutant thereof, sometimes with at least a 100-fold selectivity for MCT4 over MCT1.

公开(公告)号：US12151999B2

公开(公告)日：2024-11-26

申请号：US18606722

申请日：2024-03-15

Applicant: Hangzhou PhecdaMed Co., Ltd.

Inventor： Hongguang Xia ,  Mengyang Fan ,  Xufeng Cen ,  Xiaoyan Xu ,  Ronghai Wu ,  Dong Liu ,  Zhen Tian

IPC: C07C311/21 ,  A61K31/18 ,  A61K31/337 ,  A61K31/381 ,  A61K31/402 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/433 ,  A61K31/44 ,  C07D207/06 ,  C07D231/18 ,  C07D249/04 ,  C07D249/12 ,  C07D257/04 ,  C07D261/10 ,  C07D285/06 ,  C07D305/08 ,  C07D333/34 ,  C07D333/62

Abstract: The present application discloses small molecule compounds having a naphthylamine structure and an application thereof. In the present application, the structure of a compound having a structure as shown in general formula (I) is as shown in the drawing. The compound and the pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof that are provided by the present application or the pharmaceutical composition provided by the present application can selectively induce autophagy in damaged mitochondria without affecting or only weakly affecting normal mitochondria, and further have superior metabolic stability and pharmacokinetic properties, lower toxicity, and better druggability.

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：US20240382455A1

公开(公告)日：2024-11-21

申请号：US18788074

申请日：2024-07-29

Applicant: TSD LIFE SCIENCES CO., LTD.

Inventor： Wook KIM ,  Sung-Hwa YOON ,  Ji Hye HAN ,  Han Ho SHIN ,  Ju-Young PARK

IPC: A61K31/415 ,  A61P1/16 ,  A61P19/04

Abstract: The present inventive concept relates to a pharmaceutical composition for prevention or treatment of fibrosis or a health functional food composition for prevention or alleviation of fibrosis, each composition containing a 1H-pyrazole-3-amide-based compound or a pharmaceutically acceptable salt thereof as an active ingredient. The compound exhibits a fibrosis mitigation effect in fibrosis-induced mouse models, and thus the compositions containing the compound as an active ingredient can be favorably utilized for prevention or treatment of fibrosis.

公开(公告)号：US20240368307A1

公开(公告)日：2024-11-07

申请号：US18642451

申请日：2024-04-22

Applicant: THE UNIVERSITY OF CHICAGO

Inventor： Nicolas CHEVRIER ,  Michihiro TAKAHAMA

IPC: C07K16/40 ,  A61K31/201 ,  A61K31/202 ,  A61K31/415 ,  A61K31/497 ,  A61K45/00 ,  G01N33/68

Abstract: Aspects of the disclosure relate to methods for treating sepsis in a patient comprising administering a PLA2G5 targeting molecule, fatty acids, LPA inhibitors, and/or other compositions to the patient.

公开(公告)号：US20240368087A1

公开(公告)日：2024-11-07

申请号：US18433099

申请日：2024-02-05

Applicant: VANDERBILT UNIVERSITY ,  The UAB Research Foundation ,  The Trustees of the University of Pennsylvania ,  The Trustees of the University of Pennsylvania

Inventor： David J. MALONEY ,  Alex Gregory WATERSON ,  Ganesh Rai BANTUKALLU ,  Kyle Ryan BRIMACOMBE ,  Plamen CHRISTOV ,  Chi V. DANG ,  Victor DARLEY-USMAR ,  Xin HU ,  Ajit JADHAV ,  Somnath JANA ,  Kwangho KIM ,  Jennifer L. KOUZNETSOVA ,  William J. MOORE ,  Bryan T. MOTT ,  Leonard M. NECKERS ,  Anton SIMEONOV ,  Gary Allen SULIKOWSKI ,  Daniel Jason URBAN ,  Shyh Ming YANG

IPC: C07D231/20 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K45/06 ,  C07D231/38 ,  C07D401/04 ,  C07D403/04 ,  C07D403/06 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D495/14

Abstract: Provided is a compound of formula (I) in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.

公开(公告)号：US20240366608A1

公开(公告)日：2024-11-07

申请号：US18262155

申请日：2022-01-19

Applicant: Lupin Limited

Inventor： Mandar Ramesh Bhonde ,  Sukanya Patra ,  Venkata P. Palle ,  Rajender Kumar Kamboj

IPC: A61K31/519 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/7068 ,  A61P35/00

Abstract: This disclosure relates to pharmaceutical combinations for treating and/or preventing cancer and methods and uses thereof. More particularly, provided is a pharmaceutical combination comprising a SOS1 Inhibitor and an additional active ingredient selected from a KRAS inhibitor such as a KRAS G12C inhibitor and a KRASG12D inhibitor, KRAS G13C inhibitor, and panKRAS inhibitor; an EGFR inhibitor; an ERK1/2 inhibitor; a BRAF inhibitor; a pan-RAF inhibitor; a MEK inhibitor; a AKT inhibitor; a SHP2 inhibitor; protein arginine methyltransferases (PRMTs) inhibitor such as a PRMT5 inhibitor and Type 1 PRMT inhibitor; a PI3K inhibitor; a cyclin-dependent kinase (CDK) inhibitor such as CDK4/6 inhibitor; a FGFR inhibitor; a c-Met inhibitor; a RTK inhibitor; a non-receptor tyrosine kinase inhibitor; a histone methyltransferases (HMTs) inhibitor; a DNA methyltransferases (DNMTs) inhibitor; a Focal Adhesion Kinase (FAK) inhibitor; a Bcr-Abl tyrosine kinase inhibitor; a mTOR inhibitor; a PD1 inhibitor; a PD-L1 inhibitor; CTLA4 inhibitor; and chemotherapeutic agents such as gemcitabine, doxorubicin, cisplatin, carboplatin, paclitaxel, docetaxel, topotecan, irinotecan and temozolomide.