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1. 发明申请

US20230122651A1 C7-FLUORO SUBSTITUTED TETRACYCLINE COMPOUNDS 有权
公开(公告)号：US20230122651A1
公开(公告)日：2023-04-20
申请号：US17718915
申请日：2022-04-12
申请人： Tetraphase Pharmaceuticals, Inc.
发明人： Jingye Zhou , Xiao-Yi Xiao , Louis Plarnondon , Diana K. Hunt , Roger B. Clark , Robert Zahler
IPC分类号： C07C233/57 , C07C311/08 , C07C311/21 , C07D205/04 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/34 , C07D209/94 , C07D211/60 , C07D211/76 , C07D213/74 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/14 , C07D231/56 , C07D233/61 , C07D239/42 , C07D249/04 , C07D257/04 , C07D261/18 , C07D261/20 , C07D277/56 , C07D295/088 , C07D295/15 , C07D295/26 , C07D333/34 , C07D333/38 , C07D413/12 , A61K31/65 , A61K45/06 , C07D207/09 , C07D295/12 , C07D311/08 , C07D207/06
摘要： The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

2. 发明申请

US20230113598A1 HETEROCYCLIC COMPOUNDS USEFUL AS PDK1 INHIBITORS 有权
公开(公告)号：US20230113598A1
公开(公告)日：2023-04-13
申请号：US17814224
申请日：2022-07-21
申请人： Viracta Therapeutics, Inc. , Millennium Pharmaceuticals, Inc.
发明人： Joseph ARNDT , Timothy Chan , Kevin Guckian , Gnanasambandam Kumaravel , Wen-Cheng Lee , Edward Yin-Shiang Lin , Daniel Scott , Lihong Sun , Jermaine Thomas , Kurt Van Vloten , Deping Wang , Lei Zhang , Daniel Erlanson
IPC分类号： C07D471/04 , C07D213/82 , C07D213/85 , C07D241/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , C07D473/34 , C07D487/04 , C07D491/052 , C07D519/00 , C07D241/28 , C07D498/04 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/452 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/5383
摘要： The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.

3. 发明申请

US20230094341A1 MODULATORS OF HSD17B13 AND METHODS OF USE THEREOF 有权
公开(公告)号：US20230094341A1
公开(公告)日：2023-03-30
申请号：US17622454
申请日：2020-07-01
申请人： REGENERON PHARMACEUTICALS, INC.
发明人： Joseph VACCA
IPC分类号： A61K31/5377 , C07D213/82 , C07D405/12 , C07D295/135 , C07D409/12 , C07D239/36 , C07D401/12 , C07D405/14 , C07D409/14 , C07D239/56 , C07D498/04 , C07D513/04 , A61K31/4412 , A61K31/4433 , A61K31/443 , A61K31/444 , A61K31/4436 , A61K31/513 , A61K31/497 , A61K31/496 , A61K31/506 , A61K31/4427 , A61K31/4545 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61P1/16
摘要： The disclosure relates to compounds and pharmaceutical compositions capable of modulating the hydroxysteroid 17-beta dehydrogenase (HSD17B) family member proteins including inhibiting the HSD17B member proteins, e.g. HSD17B13. The disclosure further relates to methods of treating liver diseases, disorders, or conditions with the compounds and pharmaceutical compositions disclosed herein, in which the HSD17B family member protein plays a role.

4. 发明授权

US11603351B2 Carboxamides as modulators of sodium channels 有权
公开(公告)号：US11603351B2
公开(公告)日：2023-03-14
申请号：US16824255
申请日：2020-03-19
申请人： VERTEX PHARMACEUTICALS INCORPORATED
发明人： Nadia M. Ahmad , Corey Anderson , Vijayalaksmi Arumugam , Iuliana Luci Asgian , Joanne Louise Camp , Lev Tyler Dewey Fanning , Sara Sabina Hadida Ruah , Dennis Hurley , Yvonne Schmidt , David Shaw , Urvi Patel , Stephen Andrew Thomson , Lidio Marx Carvalho Meireles
IPC分类号： C07C235/64 , C07C237/42 , C07D307/86 , C07D239/42 , C07D213/69 , C07D213/82 , C07D213/89 , C07D239/34 , C07D307/79 , C07D317/46 , C07D405/12 , A61K31/165 , C07D213/81
摘要： 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.

5. 发明申请

US20230002353A1 HETEROARYL COMPOUNDS AND THEIR USE AS THERAPEUTIC DRUGS 有权
公开(公告)号：US20230002353A1
公开(公告)日：2023-01-05
申请号：US17138309
申请日：2020-12-30
申请人： Dong-A Socio Holdings Co., Ltd.
发明人： Myeong-Seop KIM , Sumin KIM , Jin Kwan KIM , Hadong KIM , Ki Moon RYU , Seong Jin PARK , Taesun PARK , Joon-Ho SHEEN , Taeyoung YOON , Mi Yeon JANG
IPC分类号： C07D401/14 , C07D401/10 , C07D213/82 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/14
摘要： The present invention provides heterocyclic compounds, the stereoisomer thereof, the enantiomer thereof, or the pharmaceutically acceptable salt, which are capable of modulating the activity of Mer receptor tyrosine kinase (MERTK). This invention also provides pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament.
The present invention is directed to MERTK inhibitory compounds with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to MERTK dysregulation.

6. 发明申请

US20230002324A1 NAPHTHOQUINONE DERIVATIVES FOR TREATMENT OF OXIDATIVE STRESS DISORDERS 有权
公开(公告)号：US20230002324A1
公开(公告)日：2023-01-05
申请号：US17618428
申请日：2020-06-13
申请人： PTC THERAPEUTICS, INC.
发明人： Maulen M. UTEULIYEV , Lianhe SHU , Steven J. RICHARDS , Alexander A. WARKENTIN , Dana DAVIS
IPC分类号： C07D213/82 , C07D213/50 , C07D213/61 , C07D405/10 , C07D213/84 , C07D213/79 , C07D237/14 , C07D237/24 , C07D237/08 , C07D213/65
摘要： Disclosed herein are naphthoquinone derivative compounds of the formula shown below, compositions thereof, and methods of using such compounds and compositions for treating or suppressing oxidative stress disorders and/or neurodegenerative disorders and/or for inhibiting ferroptosis.

7. 发明授权

US11542234B2 2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues 有权
公开(公告)号：US11542234B2
公开(公告)日：2023-01-03
申请号：US16981456
申请日：2019-03-15
申请人： Universität zu Köln
发明人： Bernd Neumaier , Boris Zlatopolskiy , Philipp Krapf , Raphael Richarz , Alexander Drzezga
IPC分类号： A61K51/00 , A61M36/14 , C07D213/82 , A61K51/04 , C07B59/00
摘要： 6-[18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [18F]DCFPyL, [68Ga]HBED-CC-PSMA, [18F]PSMA-1007 and [Al18F]HBED-CC-PSMA. Unexpectedly, the 6-[18F]fluoro-2-alkoxy and 6-[18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the 18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.

8. 发明申请

US20220324809A1 ATP-REGULATED POTASSIUM CHANNEL OPENERS AND USES THEREOF 有权
公开(公告)号：US20220324809A1
公开(公告)日：2022-10-13
申请号：US17753470
申请日：2020-09-02
申请人： SALZMAN GROUP LTD.
发明人： Prakash JAGTAP , Andrew Lurie SALZMAN
IPC分类号： C07D213/82 , A61P9/12
摘要： Compounds and compositions including an ATP-regulated potassium (KATP) channel opener can be including in pharmaceutical compositions. These compounds and compositions are useful for prevention, treatment, or management of pulmonary arterial or venous hypertension. The composition including the compounds may be formulated for intravenous, intraarterial, intramuscular, intranasal, rectal, anal, intravaginal, intratracheal, intraperitoneal, or subcutaneous, administration, or for inhalation.

9. 再颁专利

USRE49240E1 Inhibitors of histone deacetylase 有权
公开(公告)号：USRE49240E1
公开(公告)日：2022-10-11
申请号：US16815755
申请日：2020-03-11
申请人： THE GENERAL HOSPITAL CORPORATION , DANA-FARBER CANCER INSTITUTE, INC.
发明人： Ralph Mazitschek , Teru Hideshima , Kenneth C. Anderson , Stephen J. Haggarty , Balaram Ghosh
IPC分类号： C07C237/40 , A61K31/167 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/455 , A61K31/4965 , A61K31/505 , A61K31/69 , A61K38/05 , A61K45/06 , C07C237/42 , C07D213/81 , C07D213/82 , C07D239/42 , C07D241/24
摘要： The present invention relates to compounds which inhibit histone deacetylase activity and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to methods of treating and preventing hematological cell proliferative disorders, such as multiple myeloma, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

10. 发明授权

US11427543B2 Compounds for targeting cancer stem cells 有权
公开(公告)号：US11427543B2
公开(公告)日：2022-08-30
申请号：US16318846
申请日：2017-07-18
申请人： The General Hospital Corporation
发明人： Igor Garkavtsev , Rakesh K. Jain
IPC分类号： C07C241/00 , A61K31/343 , A61P35/00 , C07D213/82 , C07C251/80 , C07D213/53
摘要： This invention relates to antagonists of G3BP2, G3BP1, and ZEB1. Pharmaceutical compositions comprising G3BP2 inhibitors, methods of inhibiting G3BP2, G3BP1, and ZEB1, methods of treating cancer and inflammation, and methods of identifying an inhibitor of cancer stems cells are also provided.

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