公开(公告)号：US12103904B2

公开(公告)日：2024-10-01

申请号：US17207344

申请日：2021-03-19

Applicant: Duke University ,  The University of North Carolina at Chapel Hill

Inventor： Pei Zhou ,  Eric J. Toone ,  Robert A. Nicholas ,  Ramesh Gopalaswamy ,  Xiaofei Liang ,  Frank Navas, III

IPC: C07C259/06 ,  A61P31/04 ,  C07C237/34 ,  C07C259/18 ,  C07C311/06 ,  C07C317/18 ,  C07C317/44 ,  C07D203/08 ,  C07D203/18 ,  C07D207/327 ,  C07D213/64 ,  C07D263/16 ,  C07D265/30 ,  C07D277/40 ,  C07D295/10 ,  C07D295/155 ,  C07D309/04 ,  C07D309/10 ,  C07D335/02 ,  C07H15/203

CPC classification number: C07C259/06 ,  A61P31/04 ,  C07C237/34 ,  C07C259/18 ,  C07C311/06 ,  C07C317/18 ,  C07C317/44 ,  C07D203/08 ,  C07D203/18 ,  C07D207/327 ,  C07D213/64 ,  C07D263/16 ,  C07D265/30 ,  C07D277/40 ,  C07D295/10 ,  C07D295/155 ,  C07D309/04 ,  C07D309/10 ,  C07D335/02 ,  C07H15/203 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14

Abstract: Disclosed are compounds of formulae:




and pharmaceutically acceptable salts thereof, wherein the variables, R1, R2, R3, R4, R5, R6, R7, R11, R12, R13, R14, R15, R16, R17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.

公开(公告)号：US11535597B2

公开(公告)日：2022-12-27

申请号：US16478444

申请日：2018-01-17

Applicant: The Scripps Research Institute

Inventor： Benjamin F. Cravatt ,  Christopher G. Parker ,  Bruno Correia

IPC: C07D229/02 ,  C07D223/06 ,  C07C233/06 ,  C07D295/10 ,  C07D317/46 ,  C07D401/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  G01N1/28 ,  G01N1/44 ,  G01N33/68

Abstract: Disclosed herein are methods for identifying proteins as targets for interaction with a small molecule ligand. Also disclosed herein are small molecule ligands and compositions for use in profiling druggable proteins.

公开(公告)号：US11344600B2

公开(公告)日：2022-05-31

申请号：US16335349

申请日：2017-10-05

Applicant: Baylor College of Medicine

Inventor： B. Venkataram Prasad ,  Mary K. Estes ,  Yongcheng Song

IPC: A61K38/06 ,  A61K31/27 ,  A61K31/40 ,  A61K31/407 ,  A61K38/00 ,  A61K45/06 ,  A61P31/14 ,  G16C20/50 ,  G16B15/30 ,  A01N47/12 ,  C07K5/068 ,  C07K5/062 ,  C07D295/10 ,  A01N47/28 ,  A01N47/34 ,  C07C201/00 ,  C07C271/18 ,  C07D498/08 ,  A61K9/00 ,  A01N43/90 ,  C07C271/22 ,  A61K31/395 ,  A01N43/64 ,  A01N37/46

Abstract: The present disclosure concerns inhibitors of Norovirus protease that are suitable for use against any genotype of Norovirus, including at least GII.4 Norovirus proteases. In particular embodiments, specific compositions are encompassed, including their use for prevention or treatment of Norovirus infection in an individual.

公开(公告)号：US20210206715A1

公开(公告)日：2021-07-08

申请号：US17207344

申请日：2021-03-19

Applicant: Duke University ,  The University of North Carolina at Chapel Hill

Inventor： Pei Zhou ,  Eric J. Toone ,  Robert A. Nicholas ,  Ramesh Gopalaswamy ,  Xiaofei Liang ,  Frank Navas, III

IPC: C07C259/06 ,  C07C259/18 ,  C07C311/06 ,  C07C317/18 ,  C07C317/44 ,  C07C237/34 ,  C07D207/327 ,  C07D263/16 ,  C07D295/155 ,  C07D203/08 ,  C07D213/64 ,  C07D277/40 ,  C07D335/02 ,  C07D203/18 ,  C07D309/10 ,  C07D309/04 ,  C07D265/30 ,  C07D295/10 ,  C07H15/203 ,  A61P31/04

Abstract: Disclosed are compounds of formulae: and pharmaceutically acceptable salts thereof, wherein the variables, R1, R2, R3, R4, R5, R6, R7, R11, R12, R13, R14, R15, R16, R17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.

公开(公告)号：US11034649B2

公开(公告)日：2021-06-15

申请号：US16096611

申请日：2017-04-25

Applicant: Duke University ,  The University of North Carolina at Chapel Hill

Inventor： Pei Zhou ,  Eric J. Toone ,  Robert A. Nicholas ,  Ramesh Gopalaswamy ,  Xiaofei Liang ,  Frank Navas, III

IPC: C07C259/06 ,  C07D265/30 ,  C07D295/10 ,  C07D213/64 ,  C07D277/40 ,  C07D335/02 ,  C07D203/18 ,  C07C259/18 ,  C07C311/06 ,  C07C317/44 ,  C07C317/18 ,  C07C237/34 ,  C07D207/327 ,  C07D263/16 ,  C07D295/155 ,  C07D203/08 ,  C07D309/10 ,  C07D309/04 ,  C07H15/203 ,  A61P31/04

Abstract: Disclosed are compounds of formulae: and pharmaceutically acceptable salts thereof, wherein the variables, R1, R2, R3, R4, R5, R6, R7, R11, R12, R13, R14, R15, R16, R17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.

公开(公告)号：US10351522B2

公开(公告)日：2019-07-16

申请号：US15735835

申请日：2016-06-10

Applicant: UNIVERSITY OF TSUKUBA ,  BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

Inventor： Hiroshi Nagase ,  Masashi Yanagisawa ,  Tsuyoshi Saitoh ,  Noriki Kutsumura ,  Yoko Irukayama

IPC: C07D213/81 ,  C07C311/29 ,  A61K31/18 ,  A61K31/341 ,  A61K31/36 ,  A61K31/381 ,  A61K31/4164 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4439 ,  C07D213/75 ,  C07D317/68 ,  C07D333/36 ,  C07C311/21 ,  C07D417/04 ,  C07D295/10 ,  C07D213/36 ,  C07D307/54 ,  A61P25/00 ,  C07D233/36 ,  C07D239/10 ,  C07C317/44 ,  C07D243/04 ,  C07C335/20 ,  A61P43/00

Abstract: The present invention aims to provide a novel low-molecular-weight compound exhibiting an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

公开(公告)号：US10130642B2

公开(公告)日：2018-11-20

申请号：US15638821

申请日：2017-06-30

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

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

IPC: A61K31/675 ,  A61K31/439 ,  A61K31/505 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/36 ,  C07D249/08 ,  C07D309/32 ,  C07D401/06 ,  C07D403/12 ,  A61K31/351 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/437 ,  C07F9/6518 ,  A61K31/454 ,  C07D405/14 ,  C07D231/20 ,  C07D233/90 ,  C07D403/06 ,  C07D319/06 ,  C07D471/04 ,  C07D405/12 ,  C07D401/04 ,  C07D309/40 ,  C07D263/18 ,  C07D261/12 ,  C07D249/18 ,  C07D249/12 ,  C07D249/10 ,  C07D249/04 ,  C07D239/34 ,  C07D237/14 ,  C07D235/08 ,  C07D233/70 ,  C07D231/18 ,  C07D231/14 ,  C07C271/22 ,  C07C229/34 ,  A61K31/50 ,  A61K31/4439 ,  C07D295/10

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, 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：US20180050052A1

公开(公告)日：2018-02-22

申请号：US15638821

申请日：2017-06-30

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

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

IPC: A61K31/675 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/36 ,  C07D249/08 ,  C07D309/32 ,  C07D401/06 ,  C07D403/12 ,  A61K31/351 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/437 ,  C07F9/6518 ,  A61K31/454 ,  C07D295/10 ,  C07D405/14 ,  C07D231/20 ,  C07D233/90 ,  C07D403/06 ,  C07D319/06 ,  C07D471/04 ,  C07D405/12 ,  C07D401/04 ,  C07D309/40 ,  C07D263/18 ,  C07D261/12 ,  C07D249/18 ,  C07D249/12 ,  C07D249/10 ,  C07D249/04 ,  C07D239/34 ,  C07D237/14 ,  C07D235/08 ,  C07D233/70 ,  C07D231/18 ,  C07D231/14 ,  C07C271/22 ,  C07C229/34 ,  A61K31/50

CPC classification number: A61K31/675 ,  A61K31/351 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5377 ,  A61K45/06 ,  C07B2200/07 ,  C07C229/34 ,  C07C271/22 ,  C07D231/14 ,  C07D231/18 ,  C07D231/20 ,  C07D233/70 ,  C07D233/90 ,  C07D235/08 ,  C07D237/14 ,  C07D239/34 ,  C07D239/36 ,  C07D249/04 ,  C07D249/08 ,  C07D249/10 ,  C07D249/12 ,  C07D249/18 ,  C07D261/12 ,  C07D263/18 ,  C07D295/10 ,  C07D309/32 ,  C07D309/40 ,  C07D319/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07F9/6518

Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, 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：US07910078B2

公开(公告)日：2011-03-22

申请号：US11843958

申请日：2007-08-23

Applicant: Paitoon Tontiwachwuthikul ,  Andrew G. H. Wee ,  Raphael Idem ,  Kreangkrai Maneeintr ,  Gao-jun Fan ,  Amornvadee Veawab ,  Amr Henni ,  Adisorn Aroonwilas ,  Amit Chakma

Inventor： Paitoon Tontiwachwuthikul ,  Andrew G. H. Wee ,  Raphael Idem ,  Kreangkrai Maneeintr ,  Gao-jun Fan ,  Amornvadee Veawab ,  Amr Henni ,  Adisorn Aroonwilas ,  Amit Chakma

IPC: B01D53/14 ,  B01D53/56 ,  B01D53/04 ,  B01D53/58 ,  C01B17/16 ,  C01B31/20 ,  C01C3/00 ,  C07C215/00 ,  C07D265/32 ,  C07D295/08 ,  C07D295/10 ,  C07D211/02 ,  C07D211/00 ,  C07D295/00

CPC classification number: B01D53/1493 ,  B01D2257/504 ,  Y02C10/04 ,  Y02C10/06 ,  Y02C10/08

Abstract: The present invention relates to a method for removing carbon dioxide (CO2) from a gas stream. Particularly, the present invention relates to a method for removing CO2 from a gas stream by a liquid absorbent having an amino alcohol derived from 4-amino-2-butanol. In comparison to conventional amines, the amino alcohols of the present invention have been found to provide a higher CO2 absorption capacity and a higher cyclic capacity for CO2 removal.

Abstract translation: 本发明涉及从气流中除去二氧化碳（CO 2）的方法。 特别地，本发明涉及通过具有衍生自4-氨基-2-丁醇的氨基醇的液体吸收剂从气流中除去CO 2的方法。 与常规胺相比，已经发现本发明的氨基醇提供较高的CO 2吸收能力和较高的CO 2去除能力。

公开(公告)号：US20100137588A1

公开(公告)日：2010-06-03

申请号：US12624916

申请日：2009-11-24

Applicant: Costa Metallinos

Inventor： Costa Metallinos

IPC: C07D295/10 ,  C07F17/02 ,  C07F5/02 ,  C07F9/02 ,  C07F7/22

CPC classification number: C07F17/02 ,  C07D295/112

Abstract: The present disclosure relates to a method for preparing an ortho-substituted aminoferrocene comprising reacting an aminoferrocene with a Lewis acid and a lithiating reagent in the presence of an electrophile to form the ortho-substituted aminoferrocene.

Abstract translation: 本公开涉及一种制备邻位取代的氨基二茂铁的方法，包括在亲电子试剂存在下使氨基二茂铁与路易斯酸和锂化试剂反应以形成邻位取代的氨基二茂铁。