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1. 发明申请

WO0062783A2 KETOLIDE ANTIBACTERIALS 审中-公开
标题翻译：卡介胶抗菌素
公开(公告)号：WO0062783A2
公开(公告)日：2000-10-26
申请号：PCT/US0010276
申请日：2000-04-13
申请人： ORTHO MCNEIL PHARM INC , KOSAN BIOSCIENCES INC
发明人： HLASTA DENNIS , HENNINGER TODD , GRANT EUGENE , KHOSLA CHAITIN , CHU DANIEL
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： A series of ketolide antibacterials in the macrolide family of formula (a), intermediates used in their manufacture and pharmaceutical compositions containing them. The compounds are erythromycin analogues useful in the treatment of bacterial and protozoal infections and in the treatment of other conditions involving gastric motility.
摘要翻译：式（a）的大环内酯类中的一系列酮内酯抗菌剂，其制备中使用的中间体和含有它们的药物组合物。这些化合物是可用于治疗细菌和原生动物感染的红霉素类似物，以及治疗涉及胃动力的其它病症。

2. 发明专利

CA2370743A1 KETOLIDE ANTIBACTERIALS 未知
公开(公告)号：CA2370743A1
公开(公告)日：2000-10-26
申请号：CA2370743
申请日：2000-04-13
申请人： ORTHO MCNEIL PHARM INC , KOSAN BIOSCIENCES INC
发明人： GRANT EUGENE , HLASTA DENNIS , HENNINGER TODD , KHOSLA CHAITIN , CHU DANIEL
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08 , A61K31/70
摘要： A series of ketolide antibacterials in the macrolide family of formula (a), intermediates used in their manufacture and pharmaceutical compositions containing them. The compounds are erythromycin analogues useful in the treatment of bacterial and protozoal infections and in the treatment of othe r conditions involving gastric motility.

3. 发明专利

BR0114763A 未知
公开(公告)号：BR0114763A
公开(公告)日：2004-04-20
申请号：BR0114763
申请日：2001-10-12
申请人： ORTHO MCNEIL PHARM INC , KOSAN BIOSCIENCES INC
发明人： HLASTA DENNIS , HENNINGER TODD C , GRANT EUGENE B , KHOSLA CHAITIN , CHU DANIEL T W , ASHLEY GARY
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08
摘要： The present invention includes compounds of the formulawherein:X is hydrogen or halide;R2 is hydrogen, acyl, or a hydroxy protecting group;R6 is hydrogen, hydroxyl, or -ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and,R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.

4. 发明专利

HU0303935A2 KETOLIDE ANTIBACTERIAL COMPOUNDS 未知
公开(公告)号：HU0303935A2
公开(公告)日：2004-06-28
申请号：HU0303935
申请日：2001-10-12
申请人： KOSAN BIOSCIENCES INC , ORTHO MCNEIL PHARM INC
发明人： ASHLEY GARY , CHU DANIEL T W , GRANT EUGENE B , HENNINGER TODD C , HLASTA DENNIS , KHOSLA CHAITIN
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08
摘要： The present invention includes compounds of the formulawherein:X is hydrogen or halide;R2 is hydrogen, acyl, or a hydroxy protecting group;R6 is hydrogen, hydroxyl, or -ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and,R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.

5. 发明专利

CA2426593A1 KETOLIDE ANTIBACTERIALS 未知
公开(公告)号：CA2426593A1
公开(公告)日：2002-04-25
申请号：CA2426593
申请日：2001-10-12
申请人： ORTHO MCNEIL PHARM INC , KOSAN BIOSCIENCES INC
发明人： HLASTA DENNIS , KHOSLA CHAITIN , GRANT EUGENE B , HENNINGER TODD C , ASHLEY GARY , CHU DANIEL T W
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08
摘要： The present invention includes compounds of the formula wherein: X is hydrog en or halide; R2 is hydrogen, acyl, or a hydroxy protecting group; R6 is hydrogen, hydroxyl, or -ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C 2- C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, a nd heterocyclo(C2-C10)alkynyl; R13 is hydrogen or a substituted or unsubstitute d moiety wherein the moiety is selected from the group consisting of methyl; C 3- C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1- C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alky l, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and, R is hydroge n or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2- C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are usefu l for the treatment of bacterial and protozoal infections.

6. 发明专利

AU4354900A Ketolide antibacterials 未知
公开(公告)号：AU4354900A
公开(公告)日：2000-11-02
申请号：AU4354900
申请日：2000-04-13
申请人： KOSAN BIOSCIENCES INC , ORTHO MCNEIL PHARM INC
发明人： HLASTA DENNIS , HENNINGER TODD , GRANT EUGENE , KHOSLA CHAITIN , CHU DANIEL
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08 , A61K31/70
摘要： A series of ketolide antibacterials in the macrolide family of the formula:intermediates used in their manufacture and pharmaceutical compositions containing them. The compounds are erythromycin analogues useful in the treatment of bacterial and protozoal infections and in the treatment of other conditions involving gastric motility.

7. 发明专利

PL362005A1 KETOLIDE ANTIBACTERIALS 未知
公开(公告)号：PL362005A1
公开(公告)日：2004-10-18
申请号：PL36200501
申请日：2001-10-12
申请人： ORTHO MCNEIL PHARM INC , KOSAN BIOSCIENCES INC
发明人： HLASTA DENNIS , HENNINGER TODD C , GRANT EUGENE B , KHOSLA CHAITIN , CHU DANIEL T W , ASHLEY GARY
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08
摘要： The present invention includes compounds of the formulawherein:X is hydrogen or halide;R2 is hydrogen, acyl, or a hydroxy protecting group;R6 is hydrogen, hydroxyl, or -ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and,R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.

8. 发明专利

CZ20031095A3 Ketolide antibacterial formulations 未知
公开(公告)号：CZ20031095A3
公开(公告)日：2004-06-16
申请号：CZ20031095
申请日：2001-10-12
申请人： ORTHO MCNEIL PHARM INC , KOSAN BIOSCIENCES INC
发明人： HLASTA DENIS , HENNINGER TODD C , GRANT EUGENE B , KHOSLA CHAITIN , CHU DANIEL T W , ASHLEY GARY
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08
摘要： The present invention includes compounds of the formulawherein:X is hydrogen or halide;R2 is hydrogen, acyl, or a hydroxy protecting group;R6 is hydrogen, hydroxyl, or -ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and,R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.

9. 发明专利

ZA200303795B Ketolide antibacterials. 未知
公开(公告)号：ZA200303795B
公开(公告)日：2004-05-17
申请号：ZA200303795
申请日：2003-05-15
申请人： ORTHO MCNEIL PHARM INC , KOSAN BIOSCIENCES INC
发明人： HLASTA DENNIS , GRANT EUGENE B , CHU DANIEL T W , HENNINGER TODD C , KHOSLA CHAITIN , ASHLEY GARY
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08 , C07H , A61K , A61P
摘要： The present invention includes compounds of the formulawherein:X is hydrogen or halide;R2 is hydrogen, acyl, or a hydroxy protecting group;R6 is hydrogen, hydroxyl, or -ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and,R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.

10. 发明申请

WO0232918A3 KETOLIDE ANTIBACTERIALS 审中-公开
标题翻译：卡介胶抗菌素
公开(公告)号：WO0232918A3
公开(公告)日：2003-01-03
申请号：PCT/US0132119
申请日：2001-10-12
申请人： ORTHO MCNEIL PHARM INC
发明人： HLASTA DENNIS , HENNINGER TODD C , GRANT EUGENE B , KHOSLA CHAITIN , CHU DANIEL T W , ASHLEY GARY
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08 , Y02P20/55
摘要： The present invention includes compounds of the formula wherein: X is hydrogen or halide; R is hydrogen, acyl, or a hydroxy protecting group; R is hydrogen, hydroxyl, or -OR wherein R is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl;and the pharmaceutically acceptable salts, esters and pro-drug forms thereof. These compounds possess anti-infective activity and are useful for the treatment of bacterial and protozoal infections.
摘要翻译：本发明包括下式的化合物其中：X是氢或卤化物; R 2是氢，酰基或羟基保护基; R 6是氢，羟基或-OR a，其中R a是选自C1-C10烷基，C2-C10烯基，C2-C10炔基，芳基，杂环的取代或未取代的部分，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10）烯基，芳基（C 2 -C 10）炔基，杂环（C 1 -C 10）烷基，杂环（C 2 -C 10）烯基和杂环（C 2 -C 10） R 13是氢或取代或未取代的部分，其中部分选自甲基; C 1 -C 10烷基，C 2 -C 10烯基，C 2 -C 10炔基，芳基，杂环基，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10），杂环基（C 2 -C 10）烯基和杂环基（C 2 -C 10）炔基;且R是氢或取代或未取代的部分，其中该部分选自C1-C10烷基，C2-C10链烯基，C2 -C 1 -C 10炔基，芳基，杂环基，芳基（C 1 -C 10）烷基，芳基（C 2 -C 10）烯基，芳基（C 2 -C 10）炔基，杂环（C 1 -C 10）烷基，杂环（C 2 -C 10）（C 2 -C 10）炔基;及其药学上可接受的盐，酯和前药形式。这些化合物具有抗感染活性，可用于治疗细菌和原生动物感染。

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