公开(公告)号：US12227489B2

公开(公告)日：2025-02-18

申请号：US18479578

申请日：2023-10-02

Applicant: INIPHARM, INC.

Inventor： Sampath Kumar Anandan ,  Joshua Odingo ,  Heather Kay Webb Hsu ,  Vincent Florio ,  Subramanyam Janardhan Tantry ,  Athisayamani Jeyaraj Duraiswamy

IPC: C07D401/06 ,  C07D239/91 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D413/06 ,  C07D417/06

Abstract: Described herein are HSD17B13 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of liver disease, metabolic disease, or cardiovascular disease, such as NAFLD or NASH, or drug induced liver injury (DILI).

公开(公告)号：US20240109847A1

公开(公告)日：2024-04-04

申请号：US18259052

申请日：2021-12-23

Applicant: THE UNIVERSITY OF QUEENSLAND

Inventor： David FAIRLIE ,  Ligong LIU ,  Robert REID ,  Jeffrey MAK

IPC: C07D239/91 ,  C07D231/56

CPC classification number: C07D239/91 ,  C07D231/56

Abstract: The present application is directed towards compounds, pharmaceutically acceptable salts or prodrugs thereof, which are inhibitors of Histone Deacetylase (HDAC) binding or function. The compounds especially may have some selectivity for inhibiting Class IIa versus Class I HDACs. The present application also relates to methods of using the compounds and to uses of the compounds, especially in relation to the prevention of a disease, disorder or condition associated with Class IIa HDAC activity. In one form, the compounds are (ortho-phenyl) phenyl hydroxamates. In another form, the compounds are as provided in Formula (I), wherein R1 is a phenyl or cycloalkenyl which may be optionally substituted. Formula (I)

公开(公告)号：US11827619B2

公开(公告)日：2023-11-28

申请号：US18315138

申请日：2023-05-10

Applicant: INIPHARM, INC.

Inventor： Sampath Kumar Anandan ,  Joshua Odingo ,  Heather Kay Webb Hsu ,  Vincent Florio ,  Subramanyam Janardhan Tantry ,  Athisayamani Jeyaraj Duraiswamy

IPC: C07D401/06 ,  C07D239/91 ,  C07D417/06 ,  C07D413/06 ,  C07D403/06 ,  C07D401/10 ,  C07D403/10 ,  C07D401/14

CPC classification number: C07D401/06 ,  C07D239/91 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D413/06 ,  C07D417/06 ,  C07B2200/05

Abstract: Described herein are HSD17B13 inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of liver disease, metabolic disease, or cardiovascular disease, such as NAFLD or NASH, or drug induced liver injury (DILI).

公开(公告)号：US20230373925A1

公开(公告)日：2023-11-23

申请号：US18137939

申请日：2023-04-21

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： Mark Thomas Miller ,  Dennis James Hurley ,  Timothy Donald Neubert ,  Vijayalaksmi Arumugam ,  Sara Sabina Hadida Ruah ,  Jason McCartney ,  Jinglan ZHOU ,  Jaclyn Chau ,  Robert Martin Demoret ,  Senait G. Ghirmai ,  Roman Askatovich Valiulin ,  Alexander Frederik Kintzer ,  David Robert Slochower ,  Kathleen Aertgeerts ,  Elizabeth Mary Beck ,  James Jun Bon Mui ,  Miranda Adele Wright ,  Ronald Marcellus Alphonsus Knegtel ,  Ewa Iwona Chudyk ,  Joanne Louise Pinder ,  James Dodd

IPC: C07D215/233 ,  C07D471/04 ,  C07D239/91 ,  C07D401/14 ,  C07D401/04 ,  C07D519/00

CPC classification number: C07D215/233 ,  C07D471/04 ,  C07D239/91 ,  C07D401/14 ,  C07D401/04 ,  C07D519/00 ,  C07B2200/05

Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

公开(公告)号：US20220289721A1

公开(公告)日：2022-09-15

申请号：US17745346

申请日：2022-05-16

Applicant: Array BioPharma Inc.

Inventor： Patrick Michael BARBOUR ,  Katie Keaton BROWN ,  Adam Wade COOK ,  Erik James HICKEN ,  Dean Russell KAHN ,  Ellen Ruth LAIRD ,  Andrew Terrance METCALF ,  David Austin MORENO ,  Bradley Jon NEWHOUSE ,  Spencer Phillip PAJK ,  Brett Joseph PRIGARO ,  Li REN ,  Eugene TARLTON

IPC: C07D403/12 ,  C07D239/90 ,  C07D239/91

Abstract: Provided herein are compounds of the Formula I: and pharmaceutically acceptable salts, solvates and polymorphs thereof, wherein L, X1, R1, R2, R3, R4, R5 and R6 are as defined herein, for the treatment of BRAF-associated diseases and disorders, including BRAF-associated tumors, including malignant and benign BRAF-associated tumors of the CNS and malignant extracranial BRAF-associated tumors.

公开(公告)号：US11292789B1

公开(公告)日：2022-04-05

申请号：US17106799

申请日：2020-11-30

Applicant: Medicare Pharmaceuticals Inc. ,  MEDICARE LC.

Inventor： Do Hyun Na ,  Kyung Pyo Kang ,  Jin Hwan Jun ,  Geon Go ,  Hyeon Jun Na ,  Sang Jin Kang ,  Young Hyun Na ,  Se Jin Yoon ,  Su Ji Na

IPC: A61P31/14 ,  A61K31/517 ,  C07D239/91 ,  C07D455/02 ,  A61K35/66

Abstract: Disclosed is a composition for inhibiting the growth of virus. More particularly, the composition for inhibiting the growth of virus includes MDPX-V2021 represented by Formula 1, wherein MDPX-V2021 serves to inhibit a post-translational modification (PTM) stage in cells after SARS-CoV-2 penetrates into the body.

公开(公告)号：US10954199B2

公开(公告)日：2021-03-23

申请号：US16533506

申请日：2019-08-06

Applicant: Gilead Calistoga LLC

Inventor： Stacy Bremner ,  Jerry Evarts ,  Keiko Sujino ,  Duong Tran ,  Dragos Vizitiu

IPC: C07D265/22 ,  C07D487/04 ,  C07D265/10 ,  C07C265/10 ,  C07C233/90 ,  C07D239/91 ,  C07D263/58 ,  C07D473/34

Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.

公开(公告)号：US20200262784A1

公开(公告)日：2020-08-20

申请号：US16868343

申请日：2020-05-06

Applicant: Ming-Yu Ngai ,  Katarzyna N. Hojczyk

Inventor： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

IPC: C07C233/25 ,  C07C275/34 ,  C07C271/38 ,  C07C255/58 ,  C07C255/60 ,  C07C233/81 ,  C07C233/80 ,  C07C233/54 ,  C07C233/33 ,  C07C231/12 ,  C07J43/00 ,  C07D471/04 ,  C07D401/04 ,  C07D215/40 ,  C07D209/08 ,  C07D263/57 ,  C07D473/40 ,  C07D239/91 ,  C07D239/47 ,  C07D347/00 ,  C07D213/76 ,  C07D213/75 ,  C07C253/30 ,  C07C231/14 ,  C07C273/18 ,  C07C269/06 ,  C07C259/10 ,  C07C259/06 ,  C07D405/04 ,  C07D417/04

Abstract: The present invention provides a process of producing a trifluoromcthoxylated aryl or trifluoromothoxylated heteroaryl having the structure: wherein A is an aryl or heteroaryl, each with or without substitution; and R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)2, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure: with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:

公开(公告)号：US10577369B2

公开(公告)日：2020-03-03

申请号：US16244368

申请日：2019-01-10

Applicant: BIOWAY., INC

Inventor： Jongwoo Kim ,  Chiwoo Lee ,  Suji Hong

IPC: A61K31/517 ,  C07D239/91 ,  C07D473/34 ,  A61P1/16 ,  A61P35/02 ,  A61P35/00 ,  A61P37/00

Abstract: The present invention relates to novel quinazolinone derivatives inhibiting PI3K; a method for preparing the derivatives; and a pharmaceutical composition for treating hematologic neoplasms or liver diseases, containing the quinazolinone derivatives, wherein the novel quinazolinone derivatives according to the present invention have a beneficial effect in the treatment of hematologic neoplasms or liver diseases. Particularly, the quinazolinone derivatives inhibit PI3Kδ with high selectivity compared to that of a conventional anticancer drug of PI3Kδ inhibitors, thereby significantly reducing immunotoxicity, or simultaneously inhibit PI3Kδ and PI3Kγ, thereby enabling the treatment of autoimmune diseases, and anticancer therapy for blood cancer and the like. These targeted drugs have reduced side effects. The present invention provides a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof, wherein X is —H, halogen, —CH3, or —NH2; and Y is C1-2 linear alkyl or C3-4 cycloalkyl.

公开(公告)号：US10538492B2

公开(公告)日：2020-01-21

申请号：US15745632

申请日：2016-08-01

Applicant: University College Cork—National University of Ireland

Inventor： Fergal O'Gara ,  Jerry F. Reen ,  Gerard McGlacken

IPC: C07D215/233 ,  C07C215/38 ,  C07D239/91 ,  A61P31/00

Abstract: An antibiofilm composition comprising a compound of formula (A1), (A2) or (A3): wherein each of R1, R2, R3, R4, R5, R6 and R7 is independently selected from hydrogen, alkyl, alkenyl, aryl, halo, alkoxy, hydroxyl, amino, nitro, sulfoxy, thiol, carboxy, alkyl carboxy and amido; and X may be O or S, wherein the composition does not comprise a compound of formula (B1) or (B2):