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1. 发明授权

US06710168B1 Glycopeptide antibiotics, combinatorial libraries of glycopeptide antibiotics and methods of producing same 失效
标题翻译：糖肽抗生素，糖肽抗生素组合文库及其生产方法
公开(公告)号：US06710168B1
公开(公告)日：2004-03-23
申请号：US09353368
申请日：1999-07-14
申请人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
发明人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
IPC分类号： A61K3816
CPC分类号： C07K9/008
摘要： A glycopeptide of the formula A1—A2—A3—A4—A5—A6—A7, in which each dash represents a covalent bond; wherein A1 comprises a modified or unmodified &agr;-amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, alkylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of A2 to A7 comprises a modified or unmodified &agr;-amino acid residue, whereby (i) A1 is linked to an amino group on A2, (ii) each of A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, at least one of the sugar residues bearing one or more substituents of the formula YXR, N+(R1)═CR2R3, N═PR1R2R3, N+R1R2R3 or P+R1R2R3 in which Y is a single bond, O, NR1 or S; X is O, NR1, S, SO2, C(O)O, C(O)S, C(S)O, C(S)S, C(NR1)O, C(O)NR1, or halo (in which case Y and R are absent). A chemical library comprising a plurality of the glycopeptides of the invention. A method for preparing a glycopeptide by glycosylation of an aglycone derived from a glycopeptide antibiotic. A method for preparing a glycopeptide by preparing a pseudoaglycone from a glycopeptide antibiotic and glycosylating the pseudoaglycone.
摘要翻译：式A1-A2-A3-A4-A5-A6-A7的糖肽，其中每个短划线代表共价键; 其中A1包含经修饰或未修饰的α-氨基酸残基，烷基，芳基，芳烷基，烷酰基，芳酰基，芳烷酰基，杂环，杂环羰基，杂环烷基，杂环 - 烷基 - 羰基，烷基磺酰基，芳基磺酰基，胍基，氨基甲酰基或呫吨其中A2至A7各自包含经修饰或未修饰的α-氨基酸残基，由此（i）A1与A2上的氨基连接，（ii）每个A2，A4和A6均带有芳香侧链，该芳族侧链通过两个或更多个共价键交联在一起，和（iii）A7具有末端羧基，酯，酰胺或N-取代的酰胺基;并且其中A1至A7中的一个或多个通过糖苷键连接至一个或多个糖苷基各自具有一个或多个糖残基，至少一个带有一个或多个式YXR，N +（R 1）= CR 2 R 3，N = PR 1 R 2 R 3，N + R 1 R 2 R 3或其中Y是单键，O，NR1或S的P +，R1R2R3; X是O，NR1，S，SO2，C（O）O，C（O）S，C（S）O，C（S）S，C（NR1）O，C（O）NR1或卤素一种含有本发明多糖的化学文库。一种通过糖衍生自糖肽抗生素的糖苷配基糖基化制备糖肽的方法。一种制备糖肽的方法，所述糖肽通过从糖肽抗生素和糖基化假糖苷配基。

2. 发明授权

US07331920B2 Glycopeptide antibiotics, combinational libraries of glycopeptide antibiotics and methods of producing same 失效
标题翻译：糖肽抗生素，糖肽抗生素组合文库及其生产方法
公开(公告)号：US07331920B2
公开(公告)日：2008-02-19
申请号：US10676391
申请日：2003-10-01
申请人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
发明人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
IPC分类号： C40B50/00
CPC分类号： C07K1/047 , A61K38/00 , C07K9/008 , Y10S930/19
摘要： Methods for preparing a glycopeptide are disclosed. The methods comprise the steps of selecting a protected glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, wherein the groups A1 to A7 comprise the heptapeptide structure of naturally occurring vancomycin; at least A4 is linked to a glycosidic group which has a hexose residue linked to A4; and the protected glycopeptide has no free amino or carboxyl groups and has a free primary hydroxyl group only at the 6-position of said hexose residue. The protected glycopeptide is contacted with a compound of the formula ArSO2G where Ar is an aryl group and G is a leaving group under conditions effective to allow reaction of said free primary hydroxyl group to form a glycopeptide sulfonate ester; and the glycopeptide sulfonate ester is contacted with a nucleophile under conditions effective to allow displacement of a sulfonate group to produce a substituted glycopeptide.
摘要翻译：公开了制备糖肽的方法。所述方法包括以下步骤：选择式A 1 -A 2 -A 3 -S 3 -A 4的保护的糖肽，基团A 1〜A 5 - - - - - - - - - - - - - - - - - 7包含天然存在的万古霉素的七肽结构; 至少A 4连接于具有与A 4连接的己糖残基的糖苷基; 并且保护的糖肽不具有游离氨基或羧基，并且仅在所述己糖残基的6-位具有游离的伯羟基。保护的糖肽与式ArSO 2 G的化合物接触，其中Ar是芳基，G是离去基团，条件是有效使所述游离伯羟基反应形成糖肽磺酸盐酯; 并且糖肽磺酸酯在有效使得磺酸酯基取代以产生取代的糖肽的条件下与亲核试剂接触。

3. 发明授权

US07473671B2 Glycopeptide antibiotics, combinatorial libraries of glycopeptide antibiotics and methods of producing same 失效
标题翻译：糖肽抗生素，糖肽抗生素组合文库及其生产方法
公开(公告)号：US07473671B2
公开(公告)日：2009-01-06
申请号：US10631883
申请日：2003-07-31
申请人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
发明人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
IPC分类号： C40B40/14
CPC分类号： C07K9/008
摘要： A glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, in which each dash represents a covalent bond; wherein A1 comprises a modified or unmodified α-amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, alkylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of A2 to A7 comprises a modified or unmodified α-amino acid residue, whereby (i) A1 is linked to an amino group on A2, (ii) each of A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, at least one of the sugar residues bearing one or more substituents of the formula YXR, N+(R1)=CR2R3, N=PR1R2R3, N+R1R2R3 or P+R1R2R3 in which Y is a single bond, O, NR, or S; X is O, NR1, S, SO2, C(O)O, C(O)S, C(S)O, C(S)S, C(NR1)O, C(O)NR1, or halo (in which case Y and R are absent). A chemical library comprising a plurality of the glycopeptides of the invention.A method for preparing a glycopeptide by glycosylation of an aglycone derived from a glycopeptide antibiotic.A method for preparing a glycopeptide by preparing a pseudoaglycone from a glycopeptide antibiotic and glycosylating the pseudoaglycone.
摘要翻译：式A1-A2-A3-A4-A5-A6-A7的糖肽，其中每个短划线代表共价键; 其中A1包含经修饰或未修饰的α-氨基酸残基，烷基，芳基，芳烷基，烷酰基，芳酰基，芳烷酰基，杂环，杂环羰基，杂环烷基，杂环 - 烷基 - 羰基，烷基磺酰基，芳基磺酰基，胍基，氨基甲酰基或呫吨其中A2至A7各自包含经修饰或未修饰的α-氨基酸残基，由此（i）A1与A2上的氨基连接，（ii）每个A2，A4和A6均带有芳香侧链，该芳族侧链通过两个或更多个共价键交联在一起，和（iii）A7具有末端羧基，酯，酰胺或N-取代的酰胺基; 并且其中A1至A7中的一个或多个通过糖苷键与一个或多个各自具有一个或多个糖残基的糖苷基连接，至少一个具有一个或多个式YXR，N +（R1）的取代基的糖残基， = CR2R3，N = PR1R2R3，N + R1R2R3或P + R1R2R3，其中Y为单键，O，NR或S; X是O，NR1，S，SO2，C（O）O，C（O）S，C（S）O，C（S）S，C（NR1）O，C（O）NR1或卤素哪种情况下Y和R不存在）。包含本发明多种糖肽的化学文库。通过糖衍生自糖肽抗生素的糖苷配基制备糖肽的方法。一种通过从糖肽抗生素制备假糖苷配基并糖基化假糖苷配基来制备糖肽的方法。

4. 发明申请

US20050075483A1 Glycopeptide antibiotics, combinatorial libraries of glycopeptide antibiotics and methods of producing same 失效
标题翻译：糖肽抗生素，糖肽抗生素组合文库及其生产方法
公开(公告)号：US20050075483A1
公开(公告)日：2005-04-07
申请号：US10676391
申请日：2003-10-01
申请人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
发明人： Daniel Kahne , Robert Kerns , Seketsu Fukuzawa , Min Ge , Christopher Thompson
IPC分类号： A61K38/00 , A61K38/14 , A61K38/16 , A61P31/04 , C07K1/00 , C07K1/04 , C07K7/50 , C07K9/00 , C07K14/00 , C07K17/00
CPC分类号： C07K1/047 , A61K38/00 , C07K9/008 , Y10S930/19
摘要： A glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, in which each dash represents a covalent bond; wherein A1 comprises a modified or unmodified α-amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, alkylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of A2 to A7 comprises a modified or unmodified α-amino acid residue, whereby (i) A1 is linked to an amino group on A2, (ii) each of A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, at least one of the sugar residues bearing one or more substituents of the formula YXR, N+(R1)═CR2R3, N═PR1R2R3, N+R1R2R3 or P+R1R2R3 in which Y is a single bond, O, NR1 or S; X is O, NR1, S, SO2, C(O)O, C(O)S, C(S)O, C(S)S, C(NR1)O, C(O)NR1, or halo (in which case Y and R are absent). A chemical library comprising a plurality of the glycopeptides of the invention. A method for preparing a glycopeptide by glycosylation of an aglycone derived from a glycopeptide antibiotic. A method for preparing a glycopeptide by preparing a pseudoaglycone from a glycopeptide antibiotic and glycosylating the pseudoaglycone.
摘要翻译：式A1-A2-A3-A4-A5-A6-A7的糖肽，其中每个短划线代表共价键; 其中A1包含经修饰或未修饰的α-氨基酸残基，烷基，芳基，芳烷基，烷酰基，芳酰基，芳烷酰基，杂环，杂环羰基，杂环烷基，杂环 - 烷基 - 羰基，烷基磺酰基，芳基磺酰基，胍基，氨基甲酰基或呫吨其中A2至A7各自包含经修饰或未修饰的α-氨基酸残基，由此（i）A1与A2上的氨基连接，（ii）每个A2，A4和A6均带有芳香侧链，该芳族侧链通过两个或更多个共价键交联在一起，和（iii）A7具有末端羧基，酯，酰胺或N-取代的酰胺基; 并且其中A1至A7中的一个或多个通过糖苷键连接至每个具有一个或多个糖残基的一个或多个糖苷基，至少一个含有一个或多个式YXR，N + （R1）= CR2R3，N = PR1R2R3，N + R1R2R3或P + R1R2R3，其中Y为单键，O，NR1或S; X是O，NR1，S，SO2，C（O）O，C（O）S，C（S）O，C（S）S，C（NR1）O，C（O）NR1或卤素哪种情况下Y和R不存在）。包含本发明多种糖肽的化学文库。通过糖衍生自糖肽抗生素的糖苷配基制备糖肽的方法。一种通过从糖肽抗生素制备假糖苷配基并糖基化假糖苷配基来制备糖肽的方法。

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