公开(公告)号：US20070185015A1

公开(公告)日：2007-08-09

申请号：US11361682

申请日：2006-02-24

申请人： Daniel Chu ,  Yaohui Lei ,  Yu Bai ,  Zhi-Jie Ni ,  John Wang

发明人： Daniel Chu ,  Yaohui Lei ,  Yu Bai ,  Zhi-Jie Ni ,  John Wang

IPC分类号： A61K38/14 ,  C07K9/00

CPC分类号： C07K9/008 ,  A61K38/00

摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl-vancomycin scaffold, in particular, acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. In addition, compounds of the invention include desmethyl-vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

摘要翻译： 具有抗菌活性的半合成糖肽基于脱甲基万古霉素支架的修饰，特别是在该支架上具有某些酰基的氨基取代的糖部分上的氨基取代基的酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 此外，本发明的化合物包括去甲基 - 万古霉素支架，大环上的酸部分转化为某些取代的酰胺，氨基取代的糖部分上的氨基取代基被某些烷基烷基化。 还提供了合成化合物的方法，含有化合物的药物组合物，以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。

公开(公告)号：US20070021328A1

公开(公告)日：2007-01-25

申请号：US11361311

申请日：2006-02-24

申请人： Yaohui Lei ,  Yu Bai ,  Daniel Chu ,  Zhi-Jie Ni ,  John Wang

发明人： Yaohui Lei ,  Yu Bai ,  Daniel Chu ,  Zhi-Jie Ni ,  John Wang

IPC分类号： C07K9/00 ,  A61K38/14

CPC分类号： C07K9/008

摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

摘要翻译： 具有抗菌活性的半合成糖肽基于重排的万古霉素或去甲基 - 万古霉素支架的修饰，特别是在该支架上的具有某些酰基的氨基取代的糖部分上的氨基取代基的烷基化或酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 还提供了合成化合物的方法，含有化合物的药物组合物，以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。

公开(公告)号：US07368422B2

公开(公告)日：2008-05-06

申请号：US11361311

申请日：2006-02-24

申请人： Yaohui Lei ,  Yu Bai ,  Daniel Chu ,  Zhi-Jie Ni ,  John Jian-Xin Wang

发明人： Yaohui Lei ,  Yu Bai ,  Daniel Chu ,  Zhi-Jie Ni ,  John Jian-Xin Wang

IPC分类号： A61K38/02 ,  A61K38/12 ,  A61K31/70 ,  C07K7/64 ,  C07K9/00 ,  C07K5/12

CPC分类号： C07K9/008

摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

摘要翻译： 具有抗菌活性的半合成糖肽基于重排的万古霉素或去甲基 - 万古霉素支架的修饰，特别是在该支架上的具有某些酰基的氨基取代的糖部分上的氨基取代基的烷基化或酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 还提供了合成化合物的方法，含有化合物的药物组合物，以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。

公开(公告)号：US20090131304A1

公开(公告)日：2009-05-21

申请号：US12268364

申请日：2008-11-10

申请人： Daniel Chu ,  Yaohui Lei ,  Yu Bai ,  Zhi-Jie Ni ,  John Jian-Xin Wang

发明人： Daniel Chu ,  Yaohui Lei ,  Yu Bai ,  Zhi-Jie Ni ,  John Jian-Xin Wang

IPC分类号： A61K38/12 ,  C07K9/00

CPC分类号： C07K9/008 ,  A61K38/00

摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl-vancomycin scaffold, in particular, acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. In addition, compounds of the invention include desmethyl-vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

摘要翻译： 具有抗菌活性的半合成糖肽基于脱甲基万古霉素支架的修饰，特别是在该支架上具有某些酰基的氨基取代的糖部分上的氨基取代基的酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 此外，本发明的化合物包括去甲基 - 万古霉素支架，大环上的酸部分转化为某些取代的酰胺，氨基取代的糖部分上的氨基取代基被某些烷基烷基化。 还提供了合成化合物的方法，含有化合物的药物组合物，以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。

公开(公告)号：US20080214444A1

公开(公告)日：2008-09-04

申请号：US12043076

申请日：2008-03-05

申请人： Yaohui Lei ,  Yu Bai ,  Daniel Chu ,  Zhi-Jie Ni ,  John Jian-Xin Wang

发明人： Yaohui Lei ,  Yu Bai ,  Daniel Chu ,  Zhi-Jie Ni ,  John Jian-Xin Wang

IPC分类号： A61K38/14 ,  C07K9/00

CPC分类号： C07K9/008

摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of a rearranged vancomycin or desmethyl-vancomycin scaffold, in particular, alkylation or acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

摘要翻译： 具有抗菌活性的半合成糖肽基于重排的万古霉素或去甲基 - 万古霉素支架的修饰，特别是在该支架上的具有某些酰基的氨基取代的糖部分上的氨基取代基的烷基化或酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 还提供了合成化合物的方法，含有化合物的药物组合物，以及用于治疗和/或预防疾病，特别是细菌感染的化合物的使用方法。