公开(公告)号：US12060335B1

公开(公告)日：2024-08-13

申请号：US18625130

申请日：2024-04-02

申请人： KING FAISAL UNIVERSITY

发明人： Hany Mohamed Abd El-Lateef Ahmed ,  Mai Mostafa Khalaf Ali ,  Antar Ahmed Abdelhamid Ahmed ,  Amer A. Amer

IPC分类号： C07D263/57 ,  A61P31/04 ,  A61P31/10

CPC分类号： C07D263/57 ,  A61P31/04 ,  A61P31/10 ,  C07B2200/13

摘要： A 2-(benzo[d]oxazol-2-yl)-N′-(3,5-dichlorobenzoyloxy)acetimidamide compound, its synthesis, and its use as an antimicrobial agent.

公开(公告)号：US20240059661A1

公开(公告)日：2024-02-22

申请号：US18548691

申请日：2022-02-25

申请人： CIPLA LIMITED

发明人： Arijit DAS ,  Srinivas Laxminarayan PATHI ,  Ramanaiah CHENNURA ,  Anjaneya INDUKARI ,  Prathap RENGARAJ

IPC分类号： C07D263/57

CPC分类号： C07D263/57

摘要： The present disclosure relates to novel solid state forms of Tafamidis of Formula (I), and process for preparation thereof. The invention is also directed to pharmaceutical compositions containing at least one solid form and to the therapeutic or prophylactic use of such solid forms and compositions. Such compositions may be used for the treatment of transthyretin-related hereditary amyloidosis, neurodegenerative diseases, amyloidosis, neuropathic pain, amyloid fibril formation and cardiomyopathy related diseases.

公开(公告)号：US20230287021A1

公开(公告)日：2023-09-14

申请号：US17759265

申请日：2021-01-27

申请人： Protego Biopharma, Inc.

发明人： Bradley Dean Tait ,  Richard F. Labaudiniere ,  Joseph Salvino

IPC分类号： C07F9/653 ,  C07D263/57 ,  C07D413/12 ,  C07H17/00 ,  C07D417/12 ,  C07D487/04 ,  C07D471/04 ,  C07D413/14

CPC分类号： C07F9/65324 ,  C07D263/57 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07H17/00 ,  C07B2200/05

摘要： Provided herein are compounds having activity against TTR related conditions, and pharmaceutically accepted salts and solvates thereof. Also provided are methods of using the compounds for inhibiting and preventing TTR aggregation and/or amyloid formation in the peripheral nerves, kidney, cardiac tissue, eye and CNS, and of treating a subject with peripheral TTR amyloidosis.

公开(公告)号：US20230278993A1

公开(公告)日：2023-09-07

申请号：US17926863

申请日：2021-05-24

申请人： SHANGHAI LONGWOOD BIOPHARMACEUTICALS CO., LTD.

发明人： Zhe WANG ,  Haiyun BAI ,  Anran QIAN ,  Deliang LI

IPC分类号： C07D413/04 ,  C07D405/04 ,  C07D307/78 ,  C07D405/14 ,  C07D407/10 ,  C07D413/14 ,  C07D263/57 ,  C07D413/10

CPC分类号： C07D413/04 ,  C07D405/04 ,  C07D307/78 ,  C07D405/14 ,  C07D407/10 ,  C07D413/14 ,  C07D263/57 ,  C07D413/10

摘要： Provided in the present invention are a novel tricyclic aromatic heterocyclic compound and a preparation method therefor, a pharmaceutical composition and a use thereof. Specifically, provided in the present invention is a compound as shown in formula I below, or an optical isomer, a hydrate, a solvate thereof, or a pharmaceutically acceptable salt thereof. The definitions of each group are as specified in the description. The compound of formula I can be used for treating diseases related to a PD-1/PD-L1 signaling pathway.

公开(公告)号：US11739040B2

公开(公告)日：2023-08-29

申请号：US17194617

申请日：2021-03-08

申请人： Unigen, Inc.

发明人： Sandip K. Nandy ,  Jiyun Liu ,  Alexandre Mikhailovitch Nesterov ,  Carmen Hertel ,  Abeysinghe Arrachchigae Papmapiya

IPC分类号： C07C43/295 ,  A23B7/154 ,  A23L3/3481 ,  A61K8/49 ,  A61Q19/02 ,  C07C39/11 ,  C07C39/15 ,  C07C43/23 ,  C07C45/67 ,  C07C45/74 ,  C07C49/83 ,  C07D213/30 ,  C07D307/12 ,  C07D307/42 ,  C07D317/54 ,  A61K8/34 ,  A61K31/09 ,  A61K31/341 ,  A61K31/357 ,  A61K31/4406 ,  A61Q19/08 ,  C07D213/64 ,  C07D263/57

CPC分类号： C07C43/295 ,  A23B7/154 ,  A23L3/3481 ,  A61K8/345 ,  A61K8/347 ,  A61K8/4926 ,  A61K8/4973 ,  A61K31/09 ,  A61K31/341 ,  A61K31/357 ,  A61K31/4406 ,  A61Q19/02 ,  A61Q19/08 ,  C07C39/11 ,  C07C39/15 ,  C07C43/23 ,  C07C45/673 ,  C07C45/74 ,  C07C49/83 ,  C07D213/30 ,  C07D213/64 ,  C07D263/57 ,  C07D307/12 ,  C07D307/42 ,  C07D317/54 ,  A61K2800/782 ,  C07C45/673 ,  C07C49/83 ,  C07C45/74 ,  C07C49/84

摘要： The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

公开(公告)号：US11724982B2

公开(公告)日：2023-08-15

申请号：US16868343

申请日：2020-05-06

申请人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

发明人： Ming-Yu Ngai ,  Katarzyna N. Hojczyk

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

CPC分类号： C07C233/25 ,  C07C231/12 ,  C07C231/14 ,  C07C233/33 ,  C07C233/54 ,  C07C233/80 ,  C07C233/81 ,  C07C253/30 ,  C07C255/58 ,  C07C255/60 ,  C07C259/06 ,  C07C259/10 ,  C07C269/06 ,  C07C271/38 ,  C07C273/1809 ,  C07C273/1854 ,  C07C275/34 ,  C07D209/08 ,  C07D213/75 ,  C07D213/76 ,  C07D215/40 ,  C07D239/47 ,  C07D239/91 ,  C07D263/57 ,  C07D347/00 ,  C07D401/04 ,  C07D405/04 ,  C07D417/04 ,  C07D471/04 ,  C07D473/40 ,  C07J43/003 ,  C07C273/1854 ,  C07C275/64 ,  C07C269/06 ,  C07C271/38 ,  C07C231/14 ,  C07C233/25 ,  C07C253/30 ,  C07C255/60 ,  C07C253/30 ,  C07C255/58 ,  C07C273/1809 ,  C07C275/34

摘要： 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：US11572366B2

公开(公告)日：2023-02-07

申请号：US17001129

申请日：2020-08-24

申请人： Incyte Corporation

发明人： Jingwei Li ,  Liangxing Wu ,  Wenqing Yao

IPC分类号： C07D491/048 ,  C07D413/10 ,  C07D263/57 ,  C07D413/14 ,  C07D417/10 ,  C07D277/66 ,  C07D413/12 ,  C07D491/04 ,  C07D498/04

摘要： Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.

公开(公告)号：US20230021476A1

公开(公告)日：2023-01-26

申请号：US17835559

申请日：2022-06-08

申请人： ARCUS BIOSCIENCES, INC.

发明人： Joel Worley BEATTY ,  Samuel Lawrie DREW ,  Matthew EPPLIN ,  Jeremy Thomas Andre FOURNIER ,  Balint GAL ,  Tezcan GUNEY ,  Karl T. HAELSIG ,  Clayton HARDMAN ,  Steven Donald JACOB ,  Jenna Leigh JEFFREY ,  Jaroslaw KALISIAK ,  Kenneth Victor LAWSON ,  Manmohan Reddy LELETI ,  Erick Allen LINDSEY ,  Artur Karenovich MAILYAN ,  Debashis MANDAL ,  Guillaume MATA ,  Hyunyoung MOON ,  Jay Patrick POWERS ,  Brandon Reid ROSEN ,  Yongli SU ,  Anh Thu TRAN ,  Zhang WANG ,  Xuelei YAN ,  Kai YU

IPC分类号： C07C317/32 ,  A61K31/10 ,  A61K31/277 ,  A61K31/343 ,  A61K31/353 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4174 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/5025 ,  A61K31/505 ,  A61K31/519 ,  A61K31/538 ,  A61K39/395 ,  A61K45/06 ,  C07C255/53 ,  C07C317/22 ,  C07C317/36 ,  C07D209/34 ,  C07D211/86 ,  C07D213/57 ,  C07D213/71 ,  C07D213/73 ,  C07D213/74 ,  C07D213/84 ,  C07D215/48 ,  C07D217/04 ,  C07D231/12 ,  C07D231/56 ,  C07D233/64 ,  C07D237/20 ,  C07D239/42 ,  C07D241/12 ,  C07D249/06 ,  C07D249/08 ,  C07D263/32 ,  C07D263/57 ,  C07D265/36 ,  C07D277/30 ,  C07D277/56 ,  C07D277/64 ,  C07D307/83 ,  C07D311/22 ,  C07D333/64 ,  C07D401/04 ,  C07D401/10 ,  C07D409/10 ,  C07D413/10 ,  C07D471/04 ,  C07D487/04

摘要： Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.

公开(公告)号：US20220289695A1

公开(公告)日：2022-09-15

申请号：US17690131

申请日：2022-03-09

申请人： Alliance for Sustainable Energy, LLC

发明人： Caroline Bradshaw HOYT ,  Gregg Tyler BECKHAM

IPC分类号： C07D263/58 ,  C07D263/57 ,  C07D413/10

摘要： The present disclosure relates to a composition having a structure that includes where R1 includes at least one of hydrogen, carbon, and/or fluorine, and includes a covalent bond. In some embodiments of the present disclosure, R1 may include at least one of hydrogen, fluorine, a carboxyl group, a hydroxyl group, an alkoxy group, and/or a hydrocarbon chain. In some embodiments of the present disclosure, the composition may be derived from at least one of In some embodiments of the present disclosure, at least a portion of the composition may be bioderived.

公开(公告)号：US20220252593A1

公开(公告)日：2022-08-11

申请号：US17475098

申请日：2021-09-14

申请人： Alnylam Pharmaceuticals, Inc.

发明人： Brian Bettencourt

IPC分类号： G01N33/566 ,  C12N15/113 ,  C07D263/57 ,  G01N33/50 ,  G01N33/53 ,  G01N33/567 ,  G01N33/68

摘要： Disclosed herein are methods for reducing or arresting an increase in a Neuropathy Impairment Score (NIS) or a modified NIS (mNIS+7) in a human subject by administering an effective amount of a transthyretin (TTR)-inhibiting composition.