公开(公告)号：WO2022226425A1

公开(公告)日：2022-10-27

申请号：PCT/US2022/026225

申请日：2022-04-25

Applicant: WANG, Lai-Xi ,  ZHANG, Xiao

Inventor： WANG, Lai-Xi ,  ZHANG, Xiao

IPC: C07H17/00

Abstract: The present disclosure provides compounds useful for enzymatic glycan remodeling of a glycoprotein. Also provided is a method for remodeling a glycoprotein using M6P-glycan oxazolines in a one-pot deglycosylation/transglycosylation process, which may enable siteselective M6P-glycan remodeling of glycoproteins to obtain homogeneous products. The remodeled glycoprotein (such as a recombinant human acid α-glucosidase) may have enhanced affinity for the CI-MPR, increased uptake by a cell, and improved therapeutic efficacy compared to the original glycoprotein. A method of treating Pompe disease using a glycanremodeled lysosomal enzyme is also provided.

公开(公告)号：WO2022084738A2

公开(公告)日：2022-04-28

申请号：PCT/IB2021/000707

申请日：2021-10-20

Applicant: AZURA OPHTHALMICS LTD.

Inventor： HOLMES, Ian ,  ALSTER, Yair ,  BARASH, Hila ,  BOSWORTH, Charles ,  RAFAELI, Omer ,  BURK, Robert, M. ,  GLEESON, Marc ,  STEWART, Mark, Richard ,  DUNN, Jonathan ,  NICHOLLS, Alexander, James

IPC: A61P17/00 ,  A61P27/02 ,  C07D413/14 ,  C07H17/00

Abstract: Described herein are compositions and methods for the treatment or prevention of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory and/or infectious diseases of the anterior surface of the eye(s). Said compositions and methods comprise keratolytic conjugates which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.

公开(公告)号：WO2021160670A1

公开(公告)日：2021-08-19

申请号：PCT/EP2021/053207

申请日：2021-02-10

Applicant: GLYCOSCIENCE, S.L.

Inventor： SUTTON, Peter William

IPC: C07H15/18 ,  C07H15/04 ,  C07H15/20 ,  C07H17/00 ,  C07H1/00 ,  A01N43/16 ,  A61K8/60 ,  A01P17/00

Abstract: The present invention relates to a 3'-ketoglycoside compound defined by formula (I) and its use for controlled release of alcohols, in particular alcohols showing an insect repellent effect. It relates also to a process for preparing the 3'-ketoglycoside compound of formula (I). It further relates to a composition comprising a 3'- ketoglycoside compound of formula (I). It relates also to the use of a 3'-ketoglycoside compound of formula (I) for the controlled release of alcohols. It related also to a method of use of such composition.

公开(公告)号：WO2021026450A1

公开(公告)日：2021-02-11

申请号：PCT/US2020/045399

申请日：2020-08-07

Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS

Inventor： BURKE, Martin D. ,  MAJI, Arun ,  ZHANG, Jiabao

IPC: A61K31/7042 ,  A61K31/7048 ,  A61P31/10 ,  C07H17/00 ,  C07H17/04 ,  C07H17/08

Abstract: Disclosed are C16 ester derivatives of C2'epi-amphotericin B (C2'epiAmB) characterized by improved clinical efficacy with reduced toxicity compared to AmB. Also disclosed are pharmaceutical compositions comprising the C 16 ester derivatives of C2'epiAmB, therapeutic methods of using the C16 ester derivatives of C2'epiAmB, and methods of making the C16 ester derivatives of C2'epiAmB.

公开(公告)号：WO2020251862A1

公开(公告)日：2020-12-17

申请号：PCT/US2020/036515

申请日：2020-06-06

Applicant: AGILENT TECHNOLOGIES, INC.

Inventor： HAXO, Francis

IPC: G01N21/64 ,  C07H17/00

Abstract: The present invention provides methods and kits to improve the signal from sialic acids labeled with the dye 1, 2-diamino-4, 5-methylenedioxybenzene ("DMB"). The methods include labeling the sialic acids with DMB in an aqueous solution comprising the amino acid glycine, with pH adjusted to 1.5-3.2 by an acid, such as phosphoric acid or hydrochloric acid, and a reductant.

公开(公告)号：WO2020040233A1

公开(公告)日：2020-02-27

申请号：PCT/JP2019/032722

申请日：2019-08-21

Applicant: 東和薬品株式会社 ,  国立大学法人 東京大学

Inventor： 助川　潤平 ,  荒木　大悟 ,  鈴木　俊平 ,  巳浪　真輝 ,  尾内　拓馬 ,  脇田　文博 ,  劉　超 ,  中村　栄一 ,  原野　幸治

IPC: C30B29/54 ,  C07D333/20 ,  C07D401/12 ,  C07D409/04 ,  C07D495/04 ,  C07H1/06 ,  C07H17/00 ,  C07H17/08 ,  C30B7/08 ,  C30B29/60 ,  A61K31/198 ,  A61K31/381 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/4535 ,  A61K31/7048 ,  A61K31/7052 ,  A61K33/24

Abstract: 化合物の特定形状の結晶（特に球晶）を再現性良く得るための方法の提供。化合物の特定形状の結晶（特に球晶）の製造方法であって、（１）臨界過飽和度以上の過飽和度を有する化合物の過飽和溶液を調製する工程；及び（２）前記過飽和溶液から化合物の特定形状の結晶（特に球晶）を析出させる工程を含む、方法。

公开(公告)号：WO2018193111A1

公开(公告)日：2018-10-25

申请号：PCT/EP2018/060226

申请日：2018-04-20

Applicant: NOVINTUM BIOTECHNOLOGY GMBH

Inventor： SPAREY, Tim ,  RATCLIFFE, Andrew ,  STEVENSON, Brett ,  LAGASSE, Franz ,  COCHRANE, Edward ,  LASSALLE, Gilbert

IPC: C07H17/00 ,  A61K31/7052 ,  A61P35/00

CPC classification number: C07H17/00 ,  A61P35/00

Abstract: This invention relates to compounds that are useful as cancer therapies. The compounds comprise azithromycin derivatives having a phosphonium cation tethered to the azithromycin macrocycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds. The compounds comprise an ion of formula (I) wherein either Z 1 is formula (A) and Z 2 is OR 3c ; or Z 2 is formula (B) and Z 1 is R 2c ;

公开(公告)号：WO2018161039A1

公开(公告)日：2018-09-07

申请号：PCT/US2018/020769

申请日：2018-03-02

Applicant: SYNOVO GMBH ,  PIETRZIK, Nikolas ,  BURNET, Michael, W. ,  BAEUERLEIN, Christiane ,  EGGERS, Mary ,  GUSE, Jan-hinrich ,  HAHN, Ulrike ,  STRASS, Simon

Inventor： PIETRZIK, Nikolas ,  BURNET, Michael, W. ,  BAEUERLEIN, Christiane ,  EGGERS, Mary ,  GUSE, Jan-hinrich ,  HAHN, Ulrike ,  STRASS, Simon

IPC: A61K47/50 ,  A61K47/54 ,  C07H17/00 ,  C07H17/02 ,  C07H17/08

Abstract: Lysosomally accumulated substances that release a nitroxy group, or a short chain fatty acid or a product of anaerobic metabolism or a thiol or a sulfide often from an ester or similar labile linkage have anti-inflammatory, anti-cancer and anti-bacterial activity. They are useful in treating infectious, inflammatory and malignant disease.

公开(公告)号：WO2017151575A1

公开(公告)日：2017-09-08

申请号：PCT/US2017/019873

申请日：2017-02-28

Applicant: DOW AGROSCIENCES LLC

Inventor： FOSKEY, Takiya J.

IPC: C07H17/00 ,  B01J23/46

Abstract: This invention is based on the discovery that homogeneous catalysts, [Rh(C 2 H 4 ) 2 Cl] 2 and/or [Rh(COD) 2 ][BF 4 ], can be used to produce spinetoram in higher yields at lower catalyst loadings as compared to previous methodologies. In addition, one or more phosphorus ligand donors can also be added to further increase yields/efficiency. The methods and/or systems provided herein enable cost-effective ways to produce spinetoram in large quantity with relatively simple procedures.

Abstract translation: 本发明基于以下发现：均相催化剂[Rh（C≡2）4）2 Cl ] 2和/或[Rh（COD）2] [BF 4]]可用于在较低催化剂下以较高产率生产spinetoram 与以前的方法相比的负载。 另外，还可以加入一个或多个磷配体供体以进一步提高产率/效率。 本文提供的方法和/或系统能够以相对简单的程序大量生产spinetoram的成本有效的方式。

公开(公告)号：WO2017069561A1

公开(公告)日：2017-04-27

申请号：PCT/KR2016/011900

申请日：2016-10-21

Applicant: 주식회사 아모레퍼시픽

Inventor： 남기백 ,  김동현 ,  홍용덕 ,  박준성 ,  변경희

IPC: C12P19/44 ,  C12P33/16 ,  C12N9/24 ,  C07H17/00 ,  C07J17/00

CPC classification number: C07H17/00 ,  C07J17/00 ,  C12N9/24 ,  C12P19/44 ,  C12P33/16

Abstract: 본 발명은 인삼의 사포닌으로부터, 원래 인삼 내에 미량으로 존재하는 진세노사이드 F2, 컴파운드 Mc 및 컴파운드 O를 선택적으로 제조하는 방법에 관한 것으로서, 보다 상세하게는 인삼으로부터 얻은 사포닌에 특정 효소를 처리하여, 상기 사포닌을 구조 전환시킴으로써 원하는 목표 화합물, 즉 진세노사이드 F2, 컴파운드 Mc 및 컴파운드 O를 고수율로 수득할 수 있는 방법에 관한 것이다.

Abstract translation:

本发明是从人参从人参皂苷作为获得，涉及一种方法，用于选择性地产生人参皂苷F2，化合物MC和化合物O为以痕量存在于原人参，更具体地 通过转换皂苷结构来处理皂苷特定酶，以期望的目标化合物，即人参皂甙F2，以及如何化合物和MC 2 O 3化合物可以高收率得到。