公开(公告)号：US12180182B2

公开(公告)日：2024-12-31

申请号：US18060922

申请日：2022-12-01

Applicant: Purdue Research Foundation

Inventor： Mingji Dai

IPC: C07D401/06 ,  C07C229/34 ,  C07D209/50 ,  C07D211/14 ,  C07D211/62 ,  C07D263/56 ,  C07D295/145 ,  C07D311/16 ,  C07D333/34 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D491/107 ,  C07J43/00

Abstract: One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.

公开(公告)号：US12180171B1

公开(公告)日：2024-12-31

申请号：US18414737

申请日：2024-01-17

Applicant: KING FAISAL UNIVERSITY

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

IPC: C07D263/56 ,  A61P31/04

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

公开(公告)号：US11851443B2

公开(公告)日：2023-12-26

申请号：US17579457

申请日：2022-01-19

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D249/18 ,  C07D257/04 ,  C07D261/20 ,  C07D263/34 ,  C07D271/06 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D261/18 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D249/08 ,  C07D249/12 ,  C07D261/12 ,  C07D263/56 ,  C07D277/46 ,  C07D333/40

CPC classification number: C07D498/08 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D207/34 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/04 ,  C07D237/24 ,  C07D239/34 ,  C07D239/36 ,  C07D241/24 ,  C07D249/04 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D257/04 ,  C07D261/12 ,  C07D261/18 ,  C07D261/20 ,  C07D263/34 ,  C07D263/56 ,  C07D271/06 ,  C07D277/46 ,  C07D277/56 ,  C07D307/68 ,  C07D333/40 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D471/04 ,  C07D498/04

Abstract: In one aspect, the invention relates to compounds having the formula:




where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

公开(公告)号：US20230295140A1

公开(公告)日：2023-09-21

申请号：US18201715

申请日：2023-05-24

Applicant: Acucela Inc.

Inventor： Mark W. ORME ,  Edison S. ZUNIGA ,  Vladimir A. KUKSA ,  Russell Stuart CRAFT ,  Eduardo Moreno SAVEEDRA ,  Johannes Wilhelm Georg MEISSNER ,  Jacobus Antonius Joseph den HARTOG ,  Albert Cornelis DROS

IPC: C07D413/12 ,  C07D235/08 ,  C07D249/18 ,  C07D261/20 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/82 ,  C07D413/04 ,  C07D491/107

CPC classification number: C07D413/12 ,  C07D235/08 ,  C07D249/18 ,  C07D261/20 ,  C07D263/56 ,  C07D263/58 ,  C07D277/64 ,  C07D277/82 ,  C07D413/04 ,  C07D491/107

Abstract: Provided herein are compounds and methods of use thereof for the modulation of VAP-1 activity.

公开(公告)号：US20230286968A1

公开(公告)日：2023-09-14

申请号：US18319828

申请日：2023-05-18

Applicant: Hoffmann-La Roche Inc.

Inventor： Xianfeng LIN ,  Hongying YUN ,  Bo ZHANG ,  Xiufang ZHENG

IPC: C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D263/56 ,  C07D491/107 ,  C07D417/12

CPC classification number: C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D263/56 ,  C07D491/107 ,  C07D417/12

Abstract: The present invention provides novel compounds having the general formula:






wherein A1 to A4, L1, L2, R1 and R2 are as described herein, compositions including the compounds and methods of using the compounds.

公开(公告)号：US20230257368A1

公开(公告)日：2023-08-17

申请号：US18012090

申请日：2021-07-07

Applicant: DAIICHI SANKYO COMPANY, LIMITED

Inventor： Tsuyoshi UEDA ,  Yuji KAIYA ,  Takahisa UCHIDA ,  Makoto IMAI

IPC: C07D405/12 ,  C07C67/307 ,  C07D263/56

CPC classification number: C07D405/12 ,  C07C67/307 ,  C07D263/56

Abstract: An object of the present invention is to provide an industrially useful and novel process for producing a 1,3-benzodioxole derivative, with high yield and few impurities, including a novel chlorination reaction of a benzene ring. In the novel process for producing a 1,3-benzodioxole derivative, it has been found that an industrially useful and novel chlorination reaction of a benzene ring is conducted by using sulfuryl chloride with high yield and few impurities. Based on the finding, the invention has been accomplished.

公开(公告)号：US20230002769A1

公开(公告)日：2023-01-05

申请号：US17607102

申请日：2020-04-28

Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY

Inventor： Yi YANG ,  Linyong ZHU ,  Xianjun CHEN ,  Dasheng ZHANG ,  Ni SU ,  Qiuning LIN

IPC: C12N15/115 ,  C07C255/58 ,  C12Q1/6876 ,  C12N15/10 ,  C07C255/53 ,  C07D241/20 ,  C07D213/74 ,  C07D239/42 ,  C07D213/85 ,  C07D241/24 ,  C07D263/56 ,  C07D277/64 ,  C07D333/60 ,  C07D495/04 ,  C09K11/06

Abstract: The present application relates to an aptamer nucleic acid molecule, a complex containing the aptamer nucleic acid molecules, a method of detecting intracellular or extracellular RNA, DNA or other target molecules, and a kit containing the aptamer. The aptamer of the present application is capable of specifically binding a kind of fluorophore micromolecules, and can significantly enhance fluorescence intensity under excitation light of appropriate wavelength.

公开(公告)号：US20230002366A1

公开(公告)日：2023-01-05

申请号：US17881222

申请日：2022-08-04

Applicant: TARO PHARMACEUTICALS INC.

Inventor： Curtis HARWIG ,  Jeremy D. PETTIGREW ,  Jennifer CROSS ,  Jeyaprakashnarayanan SEENISAMY ,  Mahesh Narayan KEREGADDE ,  Samir Satish KHER

IPC: C07D413/06 ,  A61P29/00 ,  C07D209/08 ,  C07D231/54 ,  C07D239/74 ,  C07D239/84 ,  C07D241/42 ,  C07D261/20 ,  C07D263/56 ,  C07D401/08 ,  C07D403/04 ,  C07D403/08 ,  C07D405/12

Abstract: Compounds of formula (I) wherein, R1, R2, R3, R4a, R4b and R5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

公开(公告)号：US20220411433A1

公开(公告)日：2022-12-29

申请号：US17531039

申请日：2021-11-19

Applicant: Denali Therapeutics Inc.

Inventor： Robert A. Craig, II ,  Javier de Vicente Fidalgo ,  Anthony A. Estrada ,  Jianwen A. Feng ,  Brian M. Fox ,  Christopher R.H. Hale ,  Katrina W. Lexa ,  Maksim Osipov ,  Travis Remarchuk ,  Zachary K. Sweeney

IPC: C07D491/048 ,  C07C235/22 ,  C07D207/27 ,  C07D233/36 ,  C07D233/42 ,  C07D233/61 ,  C07D233/64 ,  C07D249/04 ,  C07D249/08 ,  C07D257/04 ,  C07D261/04 ,  C07D261/08 ,  C07D263/32 ,  C07D263/38 ,  C07D263/56 ,  C07D271/06 ,  C07D271/10 ,  C07D291/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

Abstract: The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers or prodrug thereof, and methods of making and using thereof.

公开(公告)号：US20220073444A1

公开(公告)日：2022-03-10

申请号：US17528112

申请日：2021-11-16

Applicant: BIOPHAGY Inc.

Inventor： Ian Henderson

IPC: C07C49/255 ,  C07C235/64 ,  C07D213/30 ,  C07D263/56 ,  C07D498/04 ,  A61K45/06 ,  A61K31/44 ,  A61K31/167 ,  A61K31/536 ,  A61K31/5365 ,  A61K31/12

Abstract: The invention provides compounds and methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits.