公开(公告)号：US20240270736A1

公开(公告)日：2024-08-15

申请号：US18521254

申请日：2023-11-28

申请人： Kumquat Biosciences Inc.

发明人： Baogen Wu ,  Liansheng Li ,  Pingda Ren ,  Zhiyong Chen ,  Siling Zhao ,  Xiuwen Zhu

IPC分类号： C07D417/12 ,  A61K45/06 ,  C07C235/88 ,  C07D207/16 ,  C07D209/18 ,  C07D241/44 ,  C07D401/04 ,  C07D403/06 ,  C07D493/06

CPC分类号： C07D417/12 ,  A61K45/06 ,  C07C235/88 ,  C07D207/16 ,  C07D209/18 ,  C07D241/44 ,  C07D401/04 ,  C07D403/06 ,  C07D493/06

摘要： The present disclosure provides compounds and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.

公开(公告)号：US20230303586A1

公开(公告)日：2023-09-28

申请号：US18178452

申请日：2023-03-03

申请人： Araxes Pharma LLC

发明人： Liansheng LI ,  Jun FENG ,  Tao WU ,  Pingda REN ,  Yi LIU ,  Yuan Liu ,  Yun Oliver Long

IPC分类号： C07D495/04 ,  C07D239/94 ,  C07D401/12 ,  C07D217/22 ,  C07D215/46 ,  C07D215/54 ,  C07D239/84 ,  C07D487/04 ,  C07D239/95 ,  C07D403/04 ,  C07D241/44 ,  C07D401/04 ,  C07D409/04

CPC分类号： C07D495/04 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04

摘要： Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):





or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：US20220380311A1

公开(公告)日：2022-12-01

申请号：US17813499

申请日：2022-07-19

申请人： AGC Inc.

发明人： Yoshitaka NOMURA ,  Eiichiro ANRAKU

IPC分类号： C07D213/24 ,  C07D215/16 ,  C07D241/44 ,  C07D237/30 ,  C07D277/64 ,  C07D205/10

摘要： A method for producing an aromatic heterocycle-substituted difluoroacetic acid derivative having a partial structure represented by the formula (III), by reacting an N-oxido aromatic heterocyclic compound having a partial structure represented by the formula (I) with tetrafluoroethylene in the presence of a compound represented by the formula (II): R—YH, in a solvent selected from an aromatic hydrocarbon solvent, an ester solvent and an ether solvent:

公开(公告)号：US11465960B2

公开(公告)日：2022-10-11

申请号：US17008880

申请日：2020-09-01

申请人： Monsanto Technology LLC

发明人： David A. Morgenstern

IPC分类号： A01N37/40 ,  A01N37/38 ,  A01N39/04 ,  A01N43/40 ,  A01N43/58 ,  A01N43/60 ,  C07D213/64 ,  C07D237/32 ,  C07C65/21 ,  C07C205/34 ,  C07C205/37 ,  C07C205/42 ,  C07C255/55 ,  C07C205/43 ,  C07C205/56 ,  C07C69/712 ,  C07C69/92 ,  A01N43/42 ,  C07D213/84 ,  C07D215/32 ,  C07D237/16 ,  C07D241/18 ,  C07D213/63 ,  C07D213/69 ,  A01N43/16 ,  C07D213/85 ,  C07D241/44 ,  C07D237/26

摘要： The present invention relates to esters of carboxylic acid agrochemicals comprising a labile protecting group and having formula (I). Certain of the esters of carboxylic acid agrochemicals do not undergo hydrolysis to a significant degree in the dark, but are cleaved to regenerate the parent carboxylic acid agrochemical when exposed to light. Others of the esters of carboxylic acid agrochemicals undergo hydrolysis under both light and dark conditions. The present invention further relates to methods for the controlled release of a carboxylic acid agrochemicals, and to methods of controlling unwanted plants comprising applying to the unwanted plants an ester of a carboxylic acid agrochemical.

公开(公告)号：US20220267281A1

公开(公告)日：2022-08-25

申请号：US17618248

申请日：2020-06-12

申请人： ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR)

发明人： Ahmed MAMAI ,  Anh My CHAU ,  David Uehling

IPC分类号： C07D239/34 ,  C07D213/64 ,  C07D215/40 ,  C07D237/14 ,  C07D241/18 ,  C07D241/44 ,  C07D249/12 ,  C07D401/12 ,  C07D403/12 ,  C07D498/18

摘要： The present application is directed to compounds of Formula (I), (II), (III) or (IV) compositions comprising these compounds, methods for their preparation and their uses, for example, as acyl hydrazone linkers, which can link two chemical entities together for further use as medicaments and/or diagnostics.

公开(公告)号：US20220119356A1

公开(公告)日：2022-04-21

申请号：US17505250

申请日：2021-10-19

申请人： The Governors of the University of Alberta

发明人： James A. Nieman ,  Jack Jhamandas ,  Bing Bai ,  Alexandr Belovodskiy ,  Wen Fu ,  Mostofa Hena ,  Michael Houghton ,  Appan Srinivas Kandadai ,  Ryoichi Kimura ,  Kamlesh Kumar Sahu ,  D. Lorne Tyrrell

IPC分类号： C07D243/12 ,  C07D243/14 ,  C07D403/12 ,  C07D241/44 ,  A61P25/28

摘要： The present disclosure provides compounds that are amylin receptor antagonist compounds, compositions that include the subject compounds, methods for preparing and using the amylin receptor antagonists, and compositions containing the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease. Aspects of the present disclosure include a method of inhibiting activity of an amylin receptor by administering to a subject in need thereof a therapeutically effective amount of an amylin receptor antagonist.

公开(公告)号：US20210253539A1

公开(公告)日：2021-08-19

申请号：US17253823

申请日：2020-01-31

申请人： Kumiai Chemical Industry Co., Ltd.

发明人： Ryuji Tamai ,  Yukio Uchida ,  Fumiaki Takabe ,  Akira Kato ,  Ryo Maruyama ,  Ryo Kobayashi

IPC分类号： C07D241/44 ,  C07C213/08

摘要： A method for producing a nitroso compound of the following formula (3), comprising reacting a compound of the following formula (1) with a compound of the following formula (2) by using a tertiary alcohol and a base. wherein R1, R2, R3, R4, R5, R6, R7, R8, and R9 are each independently a hydrogen atom, a halogen atom, a (C1-C4) alkyl, or a (C1-C4) alkoxy.

公开(公告)号：US11053175B2

公开(公告)日：2021-07-06

申请号：US15573224

申请日：2016-05-11

申请人： BASF SE

发明人： Barbara Nave ,  Joachim Dickhaut ,  Peter Nesvadba ,  Mihiret Tekeste Sisay ,  Alexander Wissemeier ,  Wolfram Zerulla ,  Gregor Pasda ,  Olof Wallquist ,  Allan F. Cunningham

IPC分类号： C05G3/90 ,  C07C337/08 ,  C05C3/00 ,  C05C9/00 ,  C05F11/00 ,  C07C317/08 ,  C07D221/04 ,  C07D233/42 ,  C05D9/00 ,  C07C317/10 ,  C07C317/18 ,  C07C321/20 ,  C07C321/28 ,  C07C323/07 ,  C07C323/47 ,  C07C323/48 ,  C07D235/28 ,  C07D239/38 ,  C07D241/18 ,  C07D241/44 ,  C07D249/12 ,  C07D277/74 ,  C07D285/125 ,  C07D285/135 ,  C07D401/04 ,  C07D405/04 ,  C07D417/04 ,  C07D495/04

摘要： Provided herein are a use of thioether compounds of formula I as nitrification inhibitors, and agricultural mixtures and compositions including the thioether compounds.

公开(公告)号：US11040976B2

公开(公告)日：2021-06-22

申请号：US15568930

申请日：2016-04-22

申请人： President and Fellows of Harvard College

发明人： Juan Pablo Maianti ,  David R. Liu

IPC分类号： C07D487/04 ,  A61K31/397 ,  C07D295/185 ,  C07D295/26 ,  C07D413/06 ,  C07D493/10 ,  C07D413/12 ,  C07D405/06 ,  C07D211/14 ,  C07D211/16 ,  C07D401/06 ,  C07D401/12 ,  C07D205/04 ,  C07D211/96 ,  C07D487/08 ,  C07D405/12 ,  A61K45/06 ,  A61P3/00 ,  C07C311/16 ,  C07D241/44

摘要： Provided herein are compounds of Formulae (RL), (I), (II), (III), (IV), and (V), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, prodrugs, and isotopically labeled derivatives thereof. Also provided are pharmaceutical compositions, kits, and methods involving the inventive compounds for the treatment of metabolic disorders (e.g., diabetes, hyperglycemia, impaired glucose tolerance, insulin resistance, obesity). The compound are useful as substrate selective inhibitors of insulin-degrading enzyme (IDE).

公开(公告)号：US20210085679A1

公开(公告)日：2021-03-25

申请号：US17115317

申请日：2020-12-08

申请人： The United States of America,as represented by the Secretary,Department of Health and Human Services

发明人： Sanjay A. Desai

IPC分类号： A61K31/501 ,  A61K31/496 ,  A61K45/06 ,  C07D413/14 ,  C07D409/04 ,  C07D409/14 ,  C07D239/84 ,  C07D417/06 ,  C07D241/44 ,  C07D263/57 ,  C07D491/048 ,  C07D498/04 ,  C07D277/54 ,  C07D513/04 ,  C07D281/16 ,  A61K31/42 ,  A61K31/433 ,  A61K31/495 ,  A61K31/498 ,  A61K31/50 ,  A61K31/519 ,  A61K31/554 ,  C07K14/445 ,  A61K31/422 ,  A61K31/4741 ,  A61K31/517 ,  A61K39/015 ,  C07K16/20 ,  A61K31/423 ,  A61K31/427 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439

摘要： The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula I: Q-Y—R1—R2  (I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula I in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.