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公开(公告)号:US20120238751A1
公开(公告)日:2012-09-20
申请号:US13496188
申请日:2012-03-14
申请人: Daniel Bensen , Zhiyong Chen , John Finn , Thanh To Lam , Suk Joong Lee , Xiaoming Li , Douglas W. Phillipson , Leslie William Tari , Michael Trzoss , Junhu Zhang , Felice C. Lightstone , Toan B. Nguyen , Sergio E. Wong , Paul Aristoff , Michael Jung
发明人: Daniel Bensen , Zhiyong Chen , John Finn , Thanh To Lam , Suk Joong Lee , Xiaoming Li , Douglas W. Phillipson , Leslie William Tari , Michael Trzoss , Junhu Zhang , Felice C. Lightstone , Toan B. Nguyen , Sergio E. Wong , Paul Aristoff , Michael Jung
IPC分类号: C07D487/04 , C07D471/10 , C07D487/08 , C07D471/08 , C07D487/10 , C07D491/048 , C07D491/056 , C07D487/14 , C07D471/14 , C07D471/04 , C07D498/04
CPC分类号: C07D487/04 , C07D487/14
摘要: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors.Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
摘要翻译: 本文公开了具有式I结构的化合物及其药学上合适的盐,酯和前药,其可用作抗菌三环类回旋酶抑制剂。 还考虑了相关的药物组合物,用途和制备化合物的方法。
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公开(公告)号:US09732083B2
公开(公告)日:2017-08-15
申请号:US13496188
申请日:2012-03-14
申请人: Daniel Bensen , Zhiyong Chen , John Finn , Thanh To Lam , Suk Joong Lee , Xiaoming Li , Douglas W. Phillipson , Leslie William Tari , Michael Trzoss , Junhu Zhang , Felice C. Lightstone , Toan B. Nguyen , Sergio E. Wong , Paul Aristoff , Michael Jung
发明人: Daniel Bensen , Zhiyong Chen , John Finn , Thanh To Lam , Suk Joong Lee , Xiaoming Li , Douglas W. Phillipson , Leslie William Tari , Michael Trzoss , Junhu Zhang , Felice C. Lightstone , Toan B. Nguyen , Sergio E. Wong , Paul Aristoff , Michael Jung
IPC分类号: C07D487/04 , C07D487/14
CPC分类号: C07D487/04 , C07D487/14
摘要: Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors.Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.
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公开(公告)号:US20130079323A1
公开(公告)日:2013-03-28
申请号:US13394985
申请日:2010-09-10
申请人: Christopher J. Creighton , Leslie William Tari , Zhiyong Chen , Mark Hilgers , Thanh To Lam , Xiaoming Li , Michael Trzoss , Junhu Zhang , John Finn , Daniel Bensen
发明人: Christopher J. Creighton , Leslie William Tari , Zhiyong Chen , Mark Hilgers , Thanh To Lam , Xiaoming Li , Michael Trzoss , Junhu Zhang , John Finn , Daniel Bensen
IPC分类号: C07D487/04 , C07D471/04 , C07D491/048 , C07D487/16 , C07D513/04
CPC分类号: C07D519/00 , C07D471/04 , C07D471/16 , C07D487/04 , C07D487/16 , C07D491/048 , C07D513/04
摘要: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula (I), are disclosed: Formula (I), wherein Y is N or CH; Z is N or CR5; R5 is H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR7, or CR8R9; R7 is H or C1-3 alkyl; R8 and R9 are each independently H or C1-3 alkyl; R2 is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R4 is H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0-12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein R5 and R4 together may join to form a fused ring; and R6 is selected from the group consisting of H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halo C1-5 alkyl, halo C2-5 alkenyl, halo C2-5 alkynyl, C1-5 hydroxyalkyl, C1-5 alkyl chloride, C2-5 alkenyl chloride, and C2-5 alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.
摘要翻译: 新型促旋酶抑制剂和相关组合物和方法可用于阻止细菌生长。 公开了式(I)的化合物:式(I),其中Y是N或CH; Z为N或CR5; R5是H,含有0-2个选自O,S和N的杂原子的取代或未取代的烃基残基(1-3C),或是无机残基; L是O,S,NR7或CR8R9; R7是H或C1-3烷基; R 8和R 9各自独立地为H或C 1-3烷基; R2是H,含有0-10个选自O,S和N的杂原子的烃基残基(1-40℃),任选被无机残基取代; R4是H,无机残基或含有0-12个选自O,S和N的杂原子并含有0-10个无机残基的烃基残基(1-30C),其中R 5和R 4可以连接形成稠环; 并且R 6选自H,C 1-5烷基,C 2-5烯基,C 2-5炔基,卤代C 1-5烷基,卤素C 2-5烯基,卤代C 2-5炔基,C 1-5羟基烷基,C 1 -5烷基氯,C2-5烯基氯和C2-5炔基氯; 或其药学上可接受的盐,酯或前药。
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公开(公告)号:US09481675B2
公开(公告)日:2016-11-01
申请号:US13394985
申请日:2010-09-10
申请人: Christopher J Creighton , Leslie William Tari , Zhiyong Chen , Mark Hilgers , Thanh To Lam , Xiaoming Li , Michael Trzoss , Junhu Zhang , John Finn , Daniel Bensen
发明人: Christopher J Creighton , Leslie William Tari , Zhiyong Chen , Mark Hilgers , Thanh To Lam , Xiaoming Li , Michael Trzoss , Junhu Zhang , John Finn , Daniel Bensen
IPC分类号: C07D487/04 , C07D519/00 , C07D471/04 , C07D487/16 , C07D491/048 , C07D513/04
CPC分类号: C07D519/00 , C07D471/04 , C07D471/16 , C07D487/04 , C07D487/16 , C07D491/048 , C07D513/04
摘要: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth. Compounds of Formula I are disclosed: wherein Y is N or CH; Z is N or CR5; R5 is H, a substituted or unsubstituted hydrocarbyl residue (1-3C) containing 0-2 heteroatoms selected from O, S and N, or is an inorganic residue; L is O, S, NR7, or CR8R9; R7 is H or C1-3 alkyl; R8 and R9 are each independently H or C1-3 alkyl; R2 is H, a hydrocarbyl residue (1-40C) containing 0-10 heteroatoms selected from O, S and N optionally substituted with an inorganic residue; R4 is H, an inorganic residue, or a hydrocarbyl residue (1-30C) containing 0-12 heteroatoms selected from O, S and N and containing 0-10 inorganic residues, wherein R5 and R4 together may join to form a fused ring; and R6 is selected from the group consisting of H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, halo C1-5 alkyl, halo C2-5 alkenyl, halo C2-5 alkynyl, C1-5 hydroxyalkyl, C1-5 alkyl chloride, C2-5 alkenyl chloride, and C2-5 alkynyl chloride; or a pharmaceutically-acceptable salt, ester, or prodrug thereof.
摘要翻译: 新型促旋酶抑制剂和相关组合物和方法可用于阻止细菌生长。 公开了式(I)的化合物:式(I),其中Y是N或CH; Z为N或CR5; R5是H,含有0-2个选自O,S和N的杂原子的取代或未取代的烃基残基(1-3C),或是无机残基; L是O,S,NR7或CR8R9; R7是H或C1-3烷基; R 8和R 9各自独立地为H或C 1-3烷基; R2是H,含有0-10个选自O,S和N的杂原子的烃基残基(1-40℃),任选被无机残基取代; R4是H,无机残基或含有0-12个选自O,S和N的杂原子并含有0-10个无机残基的烃基残基(1-30C),其中R 5和R 4可以连接形成稠环; 并且R 6选自H,C 1-5烷基,C 2-5烯基,C 2-5炔基,卤代C 1-5烷基,卤素C 2-5烯基,卤代C 2-5炔基,C 1-5羟基烷基,C 1 -5烷基氯,C2-5烯基氯和C2-5炔基氯; 或其药学上可接受的盐,酯或前药。
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公开(公告)号:US08835445B2
公开(公告)日:2014-09-16
申请号:US13151683
申请日:2011-06-02
申请人: Zhiyong Chen , Christopher J. Creighton , Mark Cunningham , John Finn , Mark Hilgers , Michael Jung , Lucy Aguirre Kohnen , Thanh Lam , Xiaoming Li , Mark Stidham , Les Tari , Michael Trzoss , Junhu Zhang
发明人: Zhiyong Chen , Christopher J. Creighton , Mark Cunningham , John Finn , Mark Hilgers , Michael Jung , Lucy Aguirre Kohnen , Thanh Lam , Xiaoming Li , Mark Stidham , Les Tari , Michael Trzoss , Junhu Zhang
IPC分类号: A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号: C07D401/14 , C07D239/95 , C07D417/14
摘要: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.
摘要翻译: 本公开提供式I化合物或其药学上可接受的盐,其中R 5,R 6和Z如本文所述。 本公开还提供其药物组合物; 和抑制DHFR活性的方法; 以及通过给予式I化合物治疗细胞增殖性疾病,自身免疫疾病,炎性疾病或细菌,真菌或寄生虫感染的方法。
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公开(公告)号:US20120136014A1
公开(公告)日:2012-05-31
申请号:US13151683
申请日:2011-06-02
申请人: Zhiyong Chen , Christopher J. Creghton , Mark Cunningham , John Finn , Mark Hilgers , Michael Jung , Lucy Aguirre Kohnen , Thanh Lam , Xiaoming Li , Mark Stidham , Les Tari , Michael Trzoss , Junhu Zhang
发明人: Zhiyong Chen , Christopher J. Creghton , Mark Cunningham , John Finn , Mark Hilgers , Michael Jung , Lucy Aguirre Kohnen , Thanh Lam , Xiaoming Li , Mark Stidham , Les Tari , Michael Trzoss , Junhu Zhang
IPC分类号: A61K31/517 , C07D401/14 , C07D239/72 , A61P31/10 , A61P33/00 , A61P31/04 , A61P29/00 , C12N9/99 , C07D417/14
CPC分类号: C07D401/14 , C07D239/95 , C07D417/14
摘要: The present disclosure provides compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R5, R6 and Z are as described herein. The disclosure also provides pharmaceutical compositions thereof; and methods for inhibiting DHFR activity; and methods for treating cell proliferative diseases, autoimmune disease, inflammatory disease or bacterial, fungal or parasitic infection by administering a compound of Formula I.
摘要翻译: 本公开提供式I化合物或其药学上可接受的盐,其中R 5,R 6和Z如本文所述。 本公开还提供其药物组合物; 和抑制DHFR活性的方法; 以及通过给予式I化合物治疗细胞增殖性疾病,自身免疫疾病,炎性疾病或细菌,真菌或寄生虫感染的方法。
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