公开(公告)号：US12122754B2

公开(公告)日：2024-10-22

申请号：US17433618

申请日：2021-06-09

Applicant: WISDOM PHARMACEUTICAL CO., LTD

Inventor： Xiaolong Qiu ,  Hu Wang ,  Tao Xu ,  Lin Hu ,  Ping Zou ,  Zhiwei Zuo ,  Wenbo Liu ,  Lingling Chu

IPC: C07D239/74

CPC classification number: C07D239/74

Abstract: A related substance of linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline, 4,4′-(2-methylpropane-1,3-diyl)bis(2-(chloromethyl)quinazoline) and a method for synthesizing the related substance (impurity) by reacting 2-(chloromethyl)-4-methylquinazoline with acetaldehyde under an alkaline condition and a purification method are provided. The preparation method is simple and convenient to operate, short in reaction time, high in product purity, and high in yield. The synthesized related substance can be used for qualitative and quantitative analysis of the linagliptin intermediate 2-(chloromethyl)-4-methylquinazoline and API impurities of linagliptin, so that the medication safety of the linagliptin is improved.

公开(公告)号：US12005127B2

公开(公告)日：2024-06-11

申请号：US16962442

申请日：2019-01-16

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： John Patrick Maxwell ,  Katrina Lee Jackson ,  Qing Tang ,  Mark A. Morris ,  Steven M. Ronkin ,  Jinwang Xu ,  Kevin M. Cottrell ,  Paul S. Charifson

IPC: C07D239/74 ,  A61K48/00 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D491/048

CPC classification number: A61K48/0066 ,  A61K48/0075 ,  C07D239/74 ,  C07D239/88 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D491/048

Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions, or disorders.

公开(公告)号：US11891363B1

公开(公告)日：2024-02-06

申请号：US18217084

申请日：2023-06-30

Applicant: KING FAISAL UNIVERSITY

Inventor： Saad Shaaban ,  Hany Mohamed Abd El-Lateef Ahmed ,  Bander Alshemary

IPC: C07D239/72 ,  A61K31/517 ,  C07D239/74 ,  C07D471/14 ,  C07D471/04

CPC classification number: C07D239/74 ,  C07D471/04 ,  C07D471/14

Abstract: Multitarget-directed compounds combining the features of reactive oxygen species (ROS) modulators, poly (ADP-ribose) polymerase 1 (PARP1), and/or heat shock protein 90 (Hsp90) inhibitors in a single molecule. These single agents constitute a systemic regimen for treating the triple-negative breast cancer phenotype that overcomes drug resistance and tumor recurrence, and may be used for other indications as well, such as the treatment of various neurodegenerative disorders.

公开(公告)号：US20230242496A1

公开(公告)日：2023-08-03

申请号：US18001516

申请日：2021-06-15

Applicant: Icahn School of Medicine At Mount Sinai

Inventor： Jian JIN ,  Marta FILIZOLA ,  Aneel AGGARWAL ,  Samir PAREKH ,  Abhijeet KAPOOR ,  Shashidhar S. JATIANI ,  H. Umit KANISKAN ,  Jianping HU ,  Yudao SHEN ,  Fanye MENG ,  Lihuai QIN ,  Yulin HAN ,  Xufen YU ,  Chengwei ZHANG ,  Prashasti KUMAR ,  Rinku JAIN ,  Clement LEE

IPC: C07D279/16 ,  C07D265/36 ,  C07C321/28 ,  C07D249/18 ,  C07D215/48 ,  C07D239/74 ,  C07D231/56 ,  C07D277/64 ,  C07D235/06 ,  C07D335/06 ,  C07D209/34 ,  C07D263/58 ,  C07D285/14 ,  C07D217/02 ,  C07D417/12 ,  C07D239/42 ,  C07D233/64 ,  C07D403/04 ,  C07D215/38 ,  C07D239/72 ,  C07C311/46 ,  C07D295/135 ,  C07D239/48 ,  C07D235/16 ,  C07D215/227 ,  C07D295/26 ,  C07D239/54 ,  C07D405/12

CPC classification number: C07D279/16 ,  C07D265/36 ,  C07C321/28 ,  C07D249/18 ,  C07D215/48 ,  C07D239/74 ,  C07D231/56 ,  C07D277/64 ,  C07D235/06 ,  C07D335/06 ,  C07D209/34 ,  C07D263/58 ,  C07D285/14 ,  C07D217/02 ,  C07D417/12 ,  C07D239/42 ,  C07D233/64 ,  C07D403/04 ,  C07D215/38 ,  C07D239/72 ,  C07C311/46 ,  C07D295/135 ,  C07D239/48 ,  C07D235/16 ,  C07D215/227 ,  C07D295/26 ,  C07D239/54 ,  C07D405/12

Abstract: Disclosed are compounds that are chemical inhibitors of SOX11. The compounds disclosed are useful in treatment of various cancers.

公开(公告)号：US20230183212A1

公开(公告)日：2023-06-15

申请号：US18109705

申请日：2023-02-14

Applicant: Stingray Therapeutics, Inc.

Inventor： Srinivas Rao Kasibhatla ,  Raman Kumar Kalakuntla ,  Alexis Weston ,  Trason Thode ,  Sunil Sharma ,  Mohan R. Kaadige

IPC: C07D403/04 ,  A61P35/00 ,  C07D239/88 ,  C07D239/94 ,  C07D239/74 ,  C07D403/14 ,  C07D487/08 ,  C07D401/14 ,  C07D401/04 ,  C07D215/54

CPC classification number: C07D403/04 ,  A61P35/00 ,  C07D239/88 ,  C07D239/94 ,  C07D239/74 ,  C07D403/14 ,  C07D487/08 ,  C07D401/14 ,  C07D401/04 ,  C07D215/54

Abstract: Compounds and methods for their preparation and use as therapeutic or prophylactic agents, for example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1).

公开(公告)号：US20190142833A1

公开(公告)日：2019-05-16

申请号：US16189113

申请日：2018-11-13

Applicant: Merck Patent GmbH

Inventor： Thomas Fuchss ,  Ulrich Emde ,  Hans-Peter Buchstaller ,  Werner Mederski

IPC: A61K31/519 ,  C07D285/01 ,  C07D405/14 ,  C07D239/72 ,  C07D237/14 ,  C07C25/02 ,  C07D513/04 ,  C07D473/00 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07D239/74 ,  C07D403/14 ,  C07D498/08 ,  C07D495/04 ,  C07D491/048 ,  C07D487/04 ,  C07D471/04 ,  C07D417/14 ,  C07D417/10 ,  C07D405/04 ,  C07D403/10 ,  C07D401/10 ,  C07D265/30

CPC classification number: A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  A61K45/06 ,  C07C25/02 ,  C07D237/14 ,  C07D239/72 ,  C07D239/74 ,  C07D265/30 ,  C07D285/01 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D487/04 ,  C07D491/048 ,  C07D495/04 ,  C07D498/08 ,  C07D513/04

Abstract: The invention relates to novel compounds of the formula (I) which can be used for the inhibition of serine-threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation.

公开(公告)号：US20180215745A1

公开(公告)日：2018-08-02

申请号：US15851434

申请日：2017-12-21

Applicant: CHDI Foundation, Inc.

Inventor： Leticia M. Toledo-Sherman ,  Celia Dominguez ,  Michael Prime ,  William Mitchell ,  Naomi Went

IPC: C07D413/12 ,  C07D231/56 ,  C07D215/18 ,  C07D333/06 ,  C07D241/42 ,  C07D277/24 ,  C07D277/64 ,  C07D213/46 ,  C07D307/79 ,  C07D263/56 ,  C07D261/20 ,  C07D239/74 ,  C07D237/28 ,  C07D235/08 ,  C07D217/02 ,  C07D209/08 ,  C07D407/12 ,  C07D333/28 ,  C07D333/10 ,  C07D319/18

CPC classification number: C07D413/12 ,  A61K31/343 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/47 ,  A61K31/502 ,  A61K31/517 ,  C07D209/08 ,  C07D213/46 ,  C07D215/18 ,  C07D217/02 ,  C07D231/56 ,  C07D235/08 ,  C07D237/28 ,  C07D239/74 ,  C07D241/42 ,  C07D261/20 ,  C07D263/56 ,  C07D277/24 ,  C07D277/64 ,  C07D307/79 ,  C07D319/18 ,  C07D333/06 ,  C07D333/10 ,  C07D333/28 ,  C07D407/12

Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

公开(公告)号：US10034886B2

公开(公告)日：2018-07-31

申请号：US15711858

申请日：2017-09-21

Applicant: Celgene International II SÀRL

Inventor： Marcus F. Boehm ,  Esther Martinborough ,  Manisha Moorjani ,  Junko Tamiya ,  Liming Huang ,  Adam R. Yeager ,  Enugurthi Brahmachary ,  Thomas Fowler ,  Andrew Novak ,  Premji Meghani ,  Michael Knaggs ,  Daniel Glynn ,  Mark Mills

IPC: A61K31/506 ,  C07D403/10 ,  A61K31/551 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/4468 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/44 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/421 ,  A61K31/4178 ,  C07D495/04 ,  C07D471/04 ,  A61K31/402 ,  C07D417/12 ,  C07D413/12 ,  C07D413/04 ,  C07D409/14 ,  C07D409/12 ,  C07D407/12 ,  C07D405/12 ,  C07D403/12 ,  C07D403/04 ,  C07D401/12 ,  C07D401/06 ,  C07D401/04 ,  C07D295/135 ,  C07D295/084 ,  C07D285/12 ,  C07D285/08 ,  C07D277/30 ,  C07D271/107 ,  C07D271/06 ,  C07D263/32 ,  C07D253/065 ,  C07D253/06 ,  C07D243/08 ,  C07D241/12 ,  C07D241/08 ,  C07D239/74 ,  C07D239/34 ,  C07D239/26 ,  C07D237/08 ,  C07D231/12 ,  C07D215/14 ,  C07D213/55 ,  C07D211/98 ,  C07D211/22 ,  C07D207/08 ,  A61K38/26 ,  A61K31/53 ,  A61K31/505 ,  A61K31/501 ,  A61K31/50 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/4709

CPC classification number: A61K31/551 ,  A61K31/402 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/433 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/4965 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61K38/26 ,  C07D207/08 ,  C07D211/22 ,  C07D211/98 ,  C07D213/55 ,  C07D215/14 ,  C07D231/12 ,  C07D237/08 ,  C07D239/26 ,  C07D239/34 ,  C07D239/74 ,  C07D241/08 ,  C07D241/12 ,  C07D243/08 ,  C07D253/06 ,  C07D253/065 ,  C07D263/32 ,  C07D271/06 ,  C07D271/107 ,  C07D277/30 ,  C07D285/08 ,  C07D285/12 ,  C07D295/084 ,  C07D295/135 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.

公开(公告)号：US09972785B2

公开(公告)日：2018-05-15

申请号：US15543312

申请日：2016-10-12

Applicant: LG Chem, Ltd.

Inventor： Yongbum Cha ,  Jin Joo Kim ,  Sang Duk Suh ,  Jungbum Kim

IPC: H01L51/50 ,  H01L51/00 ,  C09K11/02 ,  C07D239/26 ,  C07D213/16 ,  C07D239/74 ,  C07D209/86 ,  C07F9/53 ,  C07D235/18 ,  C07D307/91 ,  C07D333/76 ,  C07D215/06 ,  C07D209/08 ,  C07D263/57 ,  C07D277/66 ,  C07D307/36 ,  C07D333/08 ,  C07D271/107 ,  C07D285/12 ,  C07D279/22 ,  C07D265/38 ,  C09K11/06 ,  C07D251/24 ,  H01L51/52

CPC classification number: H01L51/0056 ,  C07C13/72 ,  C07D209/08 ,  C07D209/86 ,  C07D213/16 ,  C07D215/06 ,  C07D235/18 ,  C07D239/26 ,  C07D239/74 ,  C07D251/12 ,  C07D251/24 ,  C07D263/57 ,  C07D265/38 ,  C07D271/107 ,  C07D277/66 ,  C07D279/22 ,  C07D285/12 ,  C07D307/36 ,  C07D307/91 ,  C07D333/08 ,  C07D333/76 ,  C07F9/5325 ,  C09K11/025 ,  C09K11/06 ,  C09K2211/1007 ,  C09K2211/1022 ,  C09K2211/1029 ,  C09K2211/181 ,  C09K2211/185 ,  H01L51/00 ,  H01L51/001 ,  H01L51/005 ,  H01L51/0052 ,  H01L51/0054 ,  H01L51/0058 ,  H01L51/006 ,  H01L51/0061 ,  H01L51/0065 ,  H01L51/0067 ,  H01L51/0068 ,  H01L51/0069 ,  H01L51/007 ,  H01L51/0071 ,  H01L51/0072 ,  H01L51/0073 ,  H01L51/0074 ,  H01L51/0077 ,  H01L51/0085 ,  H01L51/50 ,  H01L51/5016 ,  H01L51/5056 ,  H01L51/5076 ,  H01L51/5088 ,  H01L51/5092 ,  H01L51/5096 ,  H01L51/5206 ,  H01L51/5221

Abstract: The present specification provides a compound having a spiro structure, and an organic light emitting device including the same.

公开(公告)号：US20180057479A1

公开(公告)日：2018-03-01

申请号：US15685707

申请日：2017-08-24

Applicant: The Regents of the University of Michigan

Inventor： Matthew B. Soellner ,  Sameer Phadke

IPC: C07D401/14 ,  C07D213/81 ,  C07D213/68 ,  C07D239/74 ,  C07D215/38 ,  C07D215/20 ,  C07D295/135

CPC classification number: C07D401/14 ,  C07D213/68 ,  C07D213/81 ,  C07D215/20 ,  C07D215/38 ,  C07D239/74 ,  C07D295/135

Abstract: Inhibitor compounds of Bcr-Abl and Bcr-Abl mutants including Bcr-Abl T315I mutant protein are disclosed. Compositions comprising the inhibitor compounds and methods of using the compounds in the treatment of leukemia such as chronic myelogenous leukemia are also disclosed.