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1. 发明申请

US20230093176A1 PROCESS FOR STEREOSPECIFIC SYNTHESIS OF VITAMIN K2 AND ITS NOVEL INTERMEDIATES 有权
公开(公告)号：US20230093176A1
公开(公告)日：2023-03-23
申请号：US17733687
申请日：2022-04-29
申请人： SYNERGIA LIFE SCIENCES PVT. LTD.
发明人： DILIP MEHTA , MAYANK SHASHTRI , BNS RAJU , ASHWIN SHAH , PARIN VORA , UMAKANT MAHALE
IPC分类号： C07C46/06 , C07C317/14
摘要： The present disclosure relates to a novel process for the synthesis of stereospecific compounds of Vitamin K2 group in general and Vitamin K2-7. The present disclosure further discloses novel intermediates useful in the synthesis of stereospecific Vitamin K2-7. Compounds of the Vitamin K2 group obtained are crystalline and exhibit well defined melting points.

2. 发明授权

US11530180B2 Alpha-5 beta-1 inhibitors 有权
公开(公告)号：US11530180B2
公开(公告)日：2022-12-20
申请号：US17117004
申请日：2020-12-09
申请人： The Regents of the University of California , Shanghai ChemPartner Co., Ltd.
发明人： Dean Sheppard , William F. DeGrado , Hyunil Jo , Aparna Sundaram , Richard Beresis
IPC分类号： C07C279/18 , C07C279/28 , C07C317/14 , C07D239/14 , C07D265/08 , C07D265/16 , C07D265/36 , C07D295/155 , C07D311/68 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/04 , A61K31/337 , A61K31/704 , C07D235/16 , C07D213/74 , C07D233/88 , C07D215/42 , C07D279/06
摘要： The disclosure provides, inter alia, alpha-5 beta-1 inhibitors, pharmaceutical compositions comprising alpha-5 beta-1 inhibitors, methods for treating diseases using alpha-5 beta-1 inhibitors, and processes for making alpha-5 beta-1 inhibitors.

3. 发明申请

US20220348557A1 ORGANIC ELECTROLUMINESCENT ELEMENT 有权
公开(公告)号：US20220348557A1
公开(公告)日：2022-11-03
申请号：US17641882
申请日：2020-09-16
申请人： NIPPON STEEL Chemical & Material Co., Ltd.
发明人： Junya OGAWA , Takahiro KAI , Masashi TADA , Kazunari YOSHIDA
IPC分类号： C07D401/14 , C07D409/14 , C07D405/14 , C07D209/82 , C07D487/04 , C07F15/00 , C07F7/22 , C07F1/08 , C07D219/16 , C07C317/14 , C07D413/14 , H01L51/00
摘要： To provide an organic electroluminescent device having high efficiency and high driving stability while having a low driving voltage. The organic electroluminescent device has one or more light-emitting layers between an anode and a cathode opposed to each other, wherein at least one of the light-emitting layers is a light-emitting layer composed of a vapor deposition layer containing a first host, a second host and a light-emitting dopant material; the first host is selected from oligopyridine compounds represented by the general formula (1); and the second host is selected from carbazole compounds having two or more carbazole rings, indolocarbazole compounds having an indolocarbazole ring or compounds having a carbazole ring and an indolocarbazole ring.

4. 发明申请

US20220324796A1 ANTIBIOTIC COMPOUNDS 有权
公开(公告)号：US20220324796A1
公开(公告)日：2022-10-13
申请号：US17618333
申请日：2020-06-11
申请人： The General Hospital Corporation , Rhode Island Hospital, A Lifespan- Partner , Emory Univerversity
发明人： Frederick M. Ausubel , Wooseong Kim , Eleftherios Mylonakis , William M. Wuest
IPC分类号： C07C321/30 , C07C317/14 , C07C49/786 , A61P31/04
摘要： The present application provides compounds and methods for treating bacterial infections, including bacterial infections caused by MRSA.

5. 发明申请

US20220324795A1 PROCESS FOR PRODUCING 4,4'-DICHLORODIPHENYL SULFONE 有权
公开(公告)号：US20220324795A1
公开(公告)日：2022-10-13
申请号：US17635142
申请日：2020-08-20
申请人： BASF SE
发明人： Jessica Nadine HAMANN , Stefan BLEI , Oliver BEY
IPC分类号： C07C315/02 , C07C317/14
摘要： The invention relates to a process for producing 4,4′-dichlorodiphenyl sulfone comprising reacting a solution comprising 4,4′-dichlorodiphenyl sulfoxide and at least one linear C6-C10 carboxylic acid as solvent with an oxidizing agent to obtain a crude reaction product comprising 4,4′-dichlorodiphenyl sulfone, wherein the concentration of water in the reaction mixture is kept below 5 wt %, the process comprising: (a) adding 0.9 to 1.05 mol oxidizing agent per mol 4,4′-dichlorodiphenyl sulfoxide uniformly distributed to the solution at a temperature in the range from 80 to 105° C. over a period from 1.5 to 5 h in a first step to obtain the reaction mixture; (b) agitating the reaction mixture after completion of the first step at the temperature of the first step for 5 to 30 min without adding oxidizing agent; (c) adding 0.05 to 0.2 mol oxidizing agent per mol 4,4′-dichlorodiphenyl sulfoxide to the reaction mixture at a temperature in the range from 80 to 105° C. over a period of less than 40 min in a second step; (d) agitating the reaction mixture after completion of the second step at the temperature of the second step for 10 to 30 min without adding oxidizing agent, (e) heating the reaction mixture to a temperature in the range from 95 to 110° C. and hold this temperature for 10 to 90 min to obtain a crude reaction product comprising 4,4′-dichlorodiphenyl sulfone.

6. 发明申请

US20220251048A1 TEAD INHIBITORS AND USES THEREOF 有权
公开(公告)号：US20220251048A1
公开(公告)日：2022-08-11
申请号：US17646787
申请日：2022-01-03
申请人： Ikena Oncology, Inc.
发明人： Alfredo C. CASTRO
IPC分类号： C07D233/58 , A61P35/00 , C07C317/14 , C07D231/12 , C07D249/08 , C07D257/04 , C07D271/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12 , C07F5/02
摘要： The present invention provides compounds, compositions thereof, and methods of using the same.

7. 发明授权

US11304924B2 Pharmaceutical compositions comprising nitroxyl donors 有权
公开(公告)号：US11304924B2
公开(公告)日：2022-04-19
申请号：US16779015
申请日：2020-01-31
申请人： Cardioxyl Pharmaceuticals, Inc.
发明人： Vincent Jacob Kalish , John Reardon , Frederick Arthur Brookfield , Stephen Martin Courtney , Lisa Marie Frost , John P. Toscano
IPC分类号： A61K31/341 , A61K31/18 , A61P9/04 , C07C317/14 , C07D307/64 , A61K31/255 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/42 , A61K31/433 , A61K31/4436 , A61K31/5377 , A61K31/538 , A61K47/12 , A61K47/40 , A61K31/222 , A61K31/24 , A61K9/00 , A61K9/08
摘要： The present disclosure provides nitroxyl donating pharmaceutical compositions comprising N-substituted hydroxylamine derivatives. The compositions are highly efficacious in treating cardiovascular diseases (e.g., heart failure), have a suitable toxicological profile, and are sufficiently stable for intravenous or oral administration.

8. 发明授权

US11242317B2 EBNA1 inhibitors and their method of use 有权
公开(公告)号：US11242317B2
公开(公告)日：2022-02-08
申请号：US16519590
申请日：2019-07-23
申请人： THE WISTAR INSTITUTE OF ANATOMY AND BIOLOGY
发明人： Troy E. Messick , Garry R. Smith , Allen B. Reitz , Paul M. Lieberman , Mark E. McDonnell , Yan Zhang , Venkata Velvadapu
IPC分类号： A61K31/405 , A61K31/41 , A61K31/42 , A61K31/415 , A61K31/40 , C07D515/02 , C07D209/44 , C07D295/04 , C07D261/06 , C07D233/02 , C07D233/00 , C07D207/327 , A61K31/404 , A61K31/4439 , A61K31/496 , A61K31/192 , A61K31/44 , C07C229/56 , C07C255/54 , C07C255/55 , C07C211/27 , C07C217/84 , C07C233/11 , C07C233/64 , C07C233/65 , C07C235/58 , C07C311/08 , C07C311/16 , C07C311/17 , C07C317/14 , C07D235/06 , C07D403/10 , C07D239/26 , C07D409/10 , C07D417/10 , C07D471/04 , C07D487/04 , C07D209/08 , C07D295/155 , C07D213/55 , C07C53/18 , C07C63/66 , C07C65/19 , C07C65/28 , C07C229/64 , C07C317/44 , C07D207/08 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/70 , C07D213/64 , C07D213/74 , C07D215/14 , C07D231/12 , C07D249/06 , C07D277/30 , C07D307/79 , C07D333/54 , C07D401/04 , C07D401/10
摘要： Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.

9. 发明授权

US11230517B2 Method for aromatic fluorination 有权
公开(公告)号：US11230517B2
公开(公告)日：2022-01-25
申请号：US17015775
申请日：2020-09-09
申请人： DOW GLOBAL TECHNOLOGIES LLC , THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： Melanie S. Sanford , Douglas Bland , Patrick S. Hanley , Megan A. Cismesia , Sydonie D. Schimler
IPC分类号： C07C17/02 , C07D453/02 , C07D311/16 , C07C17/093 , C07D209/08 , C07D213/79 , C07D213/61 , C07C231/12 , C07C41/22 , C07C45/63 , C07D213/57 , C07C201/12 , C07C67/307 , C07D213/75 , C07J21/00 , C07D279/16 , C07C253/30 , C07D209/88 , C07D215/18 , C07C25/13 , C07C317/14
摘要： Disclosed is a fluorination method comprising providing an aryl fluorosulfonate and a fluorinating reagent to a reaction mixture; and reacting the aryl fluorosulfonate and the fluorinating reagent to provide a fluorinated aryl species.
Also disclosed is a fluorination method comprising providing, a salt comprising a cation and an aryloxylate, and SO2F2 to a reaction mixture; reacting the SO2F2 and the ammonium salt to provide a fluorinated aryl species.
Further disclosed a fluorination method comprising providing a compound having the structure Ar—OH to a reaction mixture; where Ar is an aryl or heteroaryl; providing SO2F2 to the reaction mixture; providing a fluorinating reagent to the reaction mixture; reacting the SO2F2, the fluorinating reagent and the compound having the structure Ar—OH to provide a fluorinated aryl species having the structure Ar—F.

10. 发明申请

US20210309606A1 Novel N-aryl Oxamic Acids 有权
公开(公告)号：US20210309606A1
公开(公告)日：2021-10-07
申请号：US17163650
申请日：2021-02-01
申请人： Purdue Research Foundation
发明人： Zhong-Yin Zhang , Kasi Viswanatharaju Ruddraraju
IPC分类号： C07C235/74 , C07D215/48 , C07C317/14 , A61P31/06
摘要： The present disclosure relates to novel N-aryl oxamic acid based inhibitors for Mycobacterium tuberculosis protein tyrosine phosphatase B (mPTPB), and to the method of making and using the novel N-aryl oxamic acid based inhibitors. More specifically, compounds provided in this disclosure can be used to inhibit Mycobacterium tuberculosis protein tyrosine phosphatase B (mPTPB) and to treat a patient having a Tuberculosis disease.

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