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1. 发明申请

US20210380623A1 PRODRUG GALACTOSIDE INHIBITOR OF GALECTINS 有权
公开(公告)号：US20210380623A1
公开(公告)日：2021-12-09
申请号：US17285225
申请日：2019-10-09
申请人： GALECTO BIOTECH AB
发明人： Fredrik ZETTERBERG , Ulf NILSSON
IPC分类号： C07H19/056
摘要： A prodrug compound of the general formula I or II. The prodrug compound of formula I or II is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Also, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

2. 发明申请

US20140171630A1 NOVEL SYNTHESIS OF GALACTOSIDE INHIBITORS 审中-公开
标题翻译：糖苷抑制剂的新合成
公开(公告)号：US20140171630A1
公开(公告)日：2014-06-19
申请号：US14185253
申请日：2014-02-20
申请人： GALECTO BIOTECH AB
发明人： Ulf NILSSON
IPC分类号： C07H5/10
CPC分类号： C07H5/10 , C07H19/056
摘要： Novel synthesis routes for preparation of thiodigalactosides and intermediates are presented. The method includes the use of a 3-azido-galactosyl thiouronium salt derivative, which is activated to the corresponding thiol in situ, which in turn is directly reacted with a 3-azido-galactosyl bromide resulting in the 3,3′-di-azido-thio-di-galactoside before the thiol has a chance to reduce the azido 10 group. Hence, in situ formation of the 3-azido-galactosyl thiol from the thiouronium salt is essential in the synthesis procedure, because any other method that generate the thiol separately results in extensive unwanted azide reduction.
摘要翻译：提出了制备硫代二糖苷和中间体的新型合成路线。该方法包括使用3-叠氮基 - 半乳糖基硫脲盐衍生物，其被原位活化到相应的硫醇上，其又与3-叠氮基 - 半乳糖基溴直接反应，得到3,3'-二 - 硫代二硫代双半乳糖苷之前硫醇有机会减少叠氮基10组。因此，在合成过程中，从β-硫脲鎓盐中原位形成3-叠氮基 - 半乳糖基硫醇是必需的，因为分别产生硫醇的任何其它方法导致广泛的不希望的叠氮化物还原。

3. 发明申请

US20140011765A1 NOVEL SYNTHESIS OF GALACTOSIDE INHIBITORS 审中-公开
标题翻译：糖苷抑制剂的新合成
公开(公告)号：US20140011765A1
公开(公告)日：2014-01-09
申请号：US14018900
申请日：2013-09-05
申请人： GALECTO BIOTECH AB
发明人： Ulf NILSSON
IPC分类号： C07H19/056
CPC分类号： C07H5/10 , C07H19/056
摘要： Novel synthesis routes for preparation of thiodigalactosides and intermediates are presented. The method includes the use of a 3-azido-galactosyl thiouronium salt derivative, which is activated to the corresponding thiol in situ, which in turn is directly reacted with a 3-azido-galactosyl bromide resulting in the 3,3′-di-azido-thio-di-galactoside before the thiol has a chance to reduce the azido 10 group. Hence, in situ formation of the 3-azido-galactosyl thiol from the thiouronium salt is essential in the synthesis procedure, because any other method that generate the thiol separately results in extensive unwanted azide reduction.
摘要翻译：提出了制备硫代二糖苷和中间体的新型合成路线。该方法包括使用3-叠氮基 - 半乳糖基硫脲盐衍生物，其被原位活化到相应的硫醇上，其又与3-叠氮基 - 半乳糖基溴直接反应，得到3,3'-二 - 硫代二硫代双半乳糖苷之前硫醇有机会减少叠氮基10组。因此，在合成过程中，从β-硫脲鎓盐中原位形成3-叠氮基 - 半乳糖基硫醇是必需的，因为分别产生硫醇的任何其它方法导致广泛的不希望的叠氮化物还原。

4. 发明申请

US20210380624A1 GALACTOSIDE INHIBITOR OF GALECTINS 有权
公开(公告)号：US20210380624A1
公开(公告)日：2021-12-09
申请号：US17285233
申请日：2019-10-09
申请人： GALECTO BIOTECH AB
发明人： Fredrik ZETTERBERG , Ulf NILSSON , Thomas BRIMERT , Kristoffer PETERSON , Karl JANSSON
IPC分类号： C07H19/056
摘要： A compound of the general formula I or II. The compound of formula I or II is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

5. 发明申请

US20200115410A1 NOVEL HYBRID GALACTOSIDE INHIBITOR OF GALECTINS 审中-公开
公开(公告)号：US20200115410A1
公开(公告)日：2020-04-16
申请号：US16200464
申请日：2018-11-26
申请人： GALECTO BIOTECH AB
发明人： Hakon LEFFLER , Ulf NILSSON , Fredrik ZETTERBERG
IPC分类号： C07H19/056
摘要： Provided is a compound of the general formula (1), which is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human, as well as a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

6. 发明申请

US20230137160A1 LARGE SCALE PROCESS FOR PREPARING 1,2,4, 6-TETRA-O-ACETYL-3-AZIDO-3-DEOXY-D-GALACTOPYRANOSIDE 有权
公开(公告)号：US20230137160A1
公开(公告)日：2023-05-04
申请号：US17915690
申请日：2021-03-29
申请人： GALECTO BIOTECH AB
发明人： Ulf NILSSON , Jonathan CUMMINS
IPC分类号： C07H13/04 , C07H1/00
摘要： A process for preparing a compound of formula (X) The process includes reacting a compound of formula (IX) with an acetylating agent in the presence of a base in a suitable solvent and at a suitable temperature for a sufficient reaction time for preparing the compound of formula X. The process is suitable for large scale synthesis.

7. 发明申请

US20190359643A1 NOVEL GALACTOSIDE INHIBITOR OF GALECTINS 审中-公开
公开(公告)号：US20190359643A1
公开(公告)日：2019-11-28
申请号：US16539078
申请日：2019-08-13
申请人： Galecto Biotech AB
发明人： Thomas BRIMERT , Richard JOHNSSON , Hakon LEFFLER , Ulf NILSSON , Fredrik ZETTERBERG
IPC分类号： C07H15/203 , C07H17/02 , C07H15/207
摘要： An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

8. 发明申请

US20190225638A1 ALPHA-D-GALACTOSIDE INHIBITORS OF GALECTINS 审中-公开
公开(公告)号：US20190225638A1
公开(公告)日：2019-07-25
申请号：US16313625
申请日：2017-07-09
申请人： GALECTO BIOTECH AB
发明人： Fredrik ZETTERBERG , Hakon LEFFLER , Ulf NILSSON
IPC分类号： C07H15/203 , C07H17/02
摘要： The present invention relates to a compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human. Furthermore, the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human.

9. 发明申请

US20170349622A1 NOVEL HYBRID GALACTOSIDE INHIBITOR OF GALECTINS 审中-公开
公开(公告)号：US20170349622A1
公开(公告)日：2017-12-07
申请号：US15323967
申请日：2015-07-06
申请人： GALECTO BIOTECH AB
发明人： Hakon LEFFLER , Ulf NILSSON , Fredrik ZETTERBERG
IPC分类号： C07H19/056
CPC分类号： C07H19/056 , A61P29/00 , C07H13/04 , C07H13/08 , C07H15/26
摘要： The present invention relates to a compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

10. 发明申请

US20190315793A1 ALPHA-D-GALACTOSIDE INHIBITORS OF GALECTINS 审中-公开
公开(公告)号：US20190315793A1
公开(公告)日：2019-10-17
申请号：US16313628
申请日：2017-07-09
申请人： GALECTO BIOTECH AB
发明人： Fredrik ZETTERBERG , Ulf NILSSON , Hakon LEFFLER
IPC分类号： C07H19/056
摘要： The present invention relates to a compound of the general formula (1). The compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore, the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

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