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公开(公告)号：JP2010195796A
公开(公告)日：2010-09-09
申请号：JP2010069022
申请日：2010-03-25
发明人： NELSON MARK L , OHEMENG KWASI , FRECHETTE ROGER , ISMAIL MOHAMED Y , HONEYMAN LAURA , BOWSER TODD , ABATO PAUL , AMOO VICTOR , ASSEFA HAREGEWEIN , BERNIAC JOEL , BHATIA BEENA , CHEN JACKSON , KIM OAK , MECHICHE RACHID , REDDY N LAXMA , VERMA ATUL K , VISKI PETER , WARCHOL TADEUSZ , YANACHKOV IVAN
IPC分类号： C07C237/26 , C07D295/14 , A61K31/65 , A61P1/02 , A61P1/04 , A61P1/12 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/00 , A61P13/02 , A61P13/10 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P17/16 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P29/02 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07C275/34 , C07C323/60 , C07D207/06 , C07D207/16 , C07D207/20 , C07D207/327 , C07D207/335 , C07D207/40 , C07D207/404 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/56 , C07D213/74 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/36 , C07D261/10 , C07D261/14 , C07D261/18 , C07D263/22 , C07D277/14 , C07D277/20 , C07D277/42 , C07D277/56 , C07D295/18 , C07D295/20 , C07D307/54 , C07D317/66
CPC分类号： C07D207/404 , C07C237/26 , C07C239/20 , C07C255/58 , C07C271/22 , C07C275/34 , C07C323/60 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/46 , C07D207/16 , C07D207/20 , C07D207/335 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/64 , C07D213/82 , C07D213/89 , C07D231/12 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/42 , C07D277/56 , C07D295/116 , C07D295/155 , C07D295/215 , C07D307/52 , C07D307/54 , C07D317/66 , C07D335/02
摘要： PROBLEM TO BE SOLVED: To provide amino-methyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof. SOLUTION: The tetracycline compounds expressed by formula (I), or pharmacologically permitted salts, prodrugs, and esters thereof are provided. In the formula, R 1 and R 2 unitedly form a ring. R 1 and R 2 unitedly form a five-membered ring or a six-membered ring. In another one, R 1 and R 2 unitedly form a six-membered ring. R 1 and R 2 may be bonded with a chain of atoms for example, -(CH 2 ) 5-6 -, -(CH 2 ) 1-5 -CH=CH-(CH 2 ) 1-5 -, -(CH 2 ) 1-5 -O-(CH 2 ) 1-5 -, -(CH 2 ) 1-5 -NR-(CH 2 ) 1-5 -, or other. Rings formed may be saturated, or unsaturated. For example, R 1 and R 2 may unitedly form a piperidine ring, a morpholine ring, a pyridine ring, or a pyrazinyl ring. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译： 待解决的问题：提供氨基甲基取代的四环素化合物，药物组合物及其使用方法。 解决方案：提供由式（I）表示的四环素化合物或其药理学允许的盐，前药和酯。 在该式中，R
1 和R 2 统一形成环。 R 1 和R 2 统一形成五元环或六元环。 在另一个中，R 1 和R 2 统一形成六元环。 R 1 和R 2 可以与一个原子链键合，例如 - （CH 2 SB 2） SB> - ， - （CH 2 ） 1-5 -CH = CH-（CH 2 SB> - ， - （CH 2 ）＆lt; SB＆gt; -O-（CH 2 SB 2） - ， - （CH 2 ）＆lt; SB＆gt; 1-5 - / - （CH 2 SB 2） 或其他。 形成的环可以是饱和的或不饱和的。 例如，R 1 和R 2可以一起形成哌啶环，吗啉环，吡啶环或吡嗪基。 版权所有（C）2010，JPO＆INPIT -
公开(公告)号：JP2011063592A
公开(公告)日：2011-03-31
申请号：JP2010229234
申请日：2010-10-12
发明人： NELSON MARK L , OHEMENG KWASI , AMOO VICTOR , KIM OAK K , ABATO PAUL , ASSEFA HAREGEWEIN , BERNIAC JOEL , BHATIA BEENA , BOWSER TODD , CHEN JACKSON , GRIER MARK , HONEYMAN LAURA , ISMAIL MOHAMED Y , MECHICHE RACHID , MATHEWS JUDE
IPC分类号： C07C237/48 , A61K31/165 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/44 , A61K31/445 , A61K31/505 , A61P31/04 , C07C237/26 , C07C243/18 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07D211/38 , C07D211/58 , C07D211/70 , C07D213/61 , C07D231/12 , C07D233/61 , C07D233/64 , C07D235/18 , C07D239/26
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46
摘要： PROBLEM TO BE SOLVED: To provide new substituted tetracycline compounds, to be used in at least part of relevant cases.
SOLUTION: These new tetracycline compounds are to be used for treating numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as for other known applications to tetracycline compounds such as blocking tetracycline efflux and modulating gene expression.
COPYRIGHT: (C)2011,JPO&INPIT摘要翻译： 待解决的问题：提供新的取代四环素化合物，用于至少部分相关病例。 解决方案：这些新的四环素化合物用于治疗许多四环素化合物反应状态，如细菌感染和肿瘤，以及其他已知的应用于四环素化合物，如阻断四环素外排和调节基因表达。 版权所有（C）2011，JPO＆INPIT
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公开(公告)号：JP2012111770A
公开(公告)日：2012-06-14
申请号：JP2012014078
申请日：2012-01-26
发明人： ABATO PAUL , ASSEFA HAREGEWEIN , BERNIAC JOEL , BHATIA BEENA , BOWSER TODD , CHEN JACKSON , GRIER MARK , HONEYMAN LAURA , ISMAIL MOHAMED Y , NELSON MARK , KWASI OHEMENG , PAN JINGWEN
IPC分类号： C07C237/26 , A61K31/65 , A61P31/04 , A61P35/00 , A61P43/00 , C07D295/18
CPC分类号： C07D471/04 , C07C237/26 , C07C251/48 , C07C255/59 , C07C259/10 , C07C271/18 , C07C271/22 , C07C271/24 , C07C2601/02 , C07C2603/46 , C07D207/335 , C07D207/337 , C07D211/70 , C07D213/30 , C07D213/38 , C07D213/61 , C07D213/73 , C07D213/74 , C07D213/84 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D261/08 , C07D263/32 , C07D277/28 , C07D277/30 , C07D295/096 , C07D295/155 , C07D295/192 , C07D307/46 , C07D307/52 , C07D307/54 , C07D309/14 , C07D333/20 , C07D333/24 , C07D333/38 , C07D403/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide, at least in part, novel substituted tetracycline compounds.SOLUTION: This invention relates to substituted tetracycline compounds expressed by the following formula, wherein R9 is substituted or unsubstituted aminocarbonylalkyl, aminoalkylcarbonylaminoalkyl, carboxylate, arylalkylaminoalkyl, alkylcarbonylaminoalkyl, dialkylaminoalkyl, N-piperazinyl alkyl substituted phenyl, alkoxy-substituted phenyl, substituted furanyl, alkylaminocarbony. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.
摘要翻译： 待解决的问题：至少部分提供新型取代的四环素化合物。 解决方案：本发明涉及由下式表示的取代四环素化合物，其中R9为取代或未取代的氨基羰基烷基，氨基烷基羰基氨基烷基，羧酸酯，芳基烷基氨基烷基，烷基羰基氨基烷基，二烷基氨基烷基，N-哌嗪基烷基取代的苯基，烷氧基取代的苯基，取代的呋喃基 ，烷基氨基羰基。 这些四环素化合物可用于治疗许多四环素化合物反应状态，如细菌感染和肿瘤。 版权所有（C）2012，JPO＆INPIT
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公开(公告)号：JP2011102296A
公开(公告)日：2011-05-26
申请号：JP2010242947
申请日：2010-10-29
发明人： NELSON MARK L , OHEMENG KWASI , FRECHETTE ROGER , ISMAIL MOHAMED Y , HONEYMAN LAURA , BOWSER TODD , ABATO PAUL , AMOO VICTOR , ASSEFA HAREGEWEIN , BERNIAC JOEL , BHATIA BEENA , CHEN JACKSON , KIM OAK , MECHICHE RACHID , REDDY N LAXMA , VERMA ATUL K , VISKI PETER , WARCHOL TADEUSZ , YANACHKOV IVAN
IPC分类号： C07C237/26 , C07D295/14 , A61K31/65 , A61P1/02 , A61P1/04 , A61P1/12 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/00 , A61P13/02 , A61P13/10 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P17/16 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P29/02 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07C275/34 , C07C323/60 , C07D207/06 , C07D207/16 , C07D207/20 , C07D207/325 , C07D207/327 , C07D207/335 , C07D207/40 , C07D207/404 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/56 , C07D213/74 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/36 , C07D261/10 , C07D261/14 , C07D261/18 , C07D263/22 , C07D277/14 , C07D277/20 , C07D277/42 , C07D277/56 , C07D295/18 , C07D295/20 , C07D307/54 , C07D317/66
CPC分类号： C07D207/404 , C07C237/26 , C07C239/20 , C07C255/58 , C07C271/22 , C07C275/34 , C07C323/60 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/46 , C07D207/16 , C07D207/20 , C07D207/335 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/64 , C07D213/82 , C07D213/89 , C07D231/12 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/42 , C07D277/56 , C07D295/116 , C07D295/155 , C07D295/215 , C07D307/52 , C07D307/54 , C07D317/66 , C07D335/02
摘要： PROBLEM TO BE SOLVED: To provide an aminomethyl-substituted tetracycline compound, a pharmaceutical composition, and methods of use thereof. SOLUTION: A tetracycline compound represented by formula (I) (wherein R 1 and R 2 are combined to form a ring), a salt, a prodrug and an ester thereof, all being pharmaceutically acceptable, are provided. A tetracycline compound represented by formula (α), a salt, an ester and a prodrug thereof, all being pharmaceutically permitted, are also provided. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译： 待解决的问题：提供氨基甲基取代的四环素化合物，药物组合物及其使用方法。 解决方案：将由式（I）表示的四环素化合物（其中R 1和R 2彼此组合形成环），盐，前药和 酯，均为药学上可接受的。 还提供了全部为药学上允许的由式（α）表示的四环素化合物，其盐，酯和前药。 版权所有（C）2011，JPO＆INPIT
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公开(公告)号：JP2010090138A
公开(公告)日：2010-04-22
申请号：JP2009275040
申请日：2009-12-03
发明人： NELSON MARK L , OHEMENG KWASI , FRECHETTE ROGER , ABATO PAUL , ASSEFA HAREGEWEIN , BANDARAGE UPUL , BERNIAC JOEL , BHATIA BEENA , CHEN JACKSON , ISMAIL MOHAMED Y , KIM OAK A , MATHEWS JUDE , HONEYMAN LAURA , NIHLAWI MOHAMMED , PEARSON ANDRE , REDDY LAXMA , SHEAHAN PAUL , SIZENSKY EMMANUELLE , TOURIGNY JUSTIN , VERMA ATUL K , VISKI PETER , WARCHOL TADEUSZ , AMOO VICTOR , MECHICHE RACHID
IPC分类号： C07C237/26 , C07D295/20 , A61K31/65 , A61P1/02 , A61P1/04 , A61P1/10 , A61P1/14 , A61P3/04 , A61P3/10 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/08 , A61P13/10 , A61P15/08 , A61P17/02 , A61P19/02 , A61P19/10 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/06 , A61P35/00 , A61P35/04 , A61P43/00 , C07C239/18 , C07C245/20 , C07C251/08 , C07C251/38 , C07C251/48 , C07C255/25 , C07C255/30 , C07C255/43 , C07C255/57 , C07C255/58 , C07C255/59 , C07C257/12 , C07C271/28 , C07C271/44 , C07C275/34 , C07C279/18 , C07C281/14 , C07C309/61 , C07C311/06 , C07C311/08 , C07C311/19 , C07C311/21 , C07C317/48 , C07C323/32 , C07C323/60 , C07D207/16 , C07D211/58 , C07D213/30 , C07D213/61 , C07D213/65 , C07D213/75 , C07D239/26 , C07D239/30 , C07D239/42 , C07D261/10 , C07D261/18 , C07D295/108 , C07D295/14 , C07D295/155 , C07D295/215 , C07D307/28 , C07D307/52 , C07D307/54 , C07D307/68 , C07D317/54 , C07D317/60 , C07D401/04 , C07F7/10
CPC分类号： C07D307/52 , C07C237/26 , C07C239/18 , C07C251/08 , C07C251/48 , C07C255/25 , C07C255/43 , C07C255/58 , C07C255/59 , C07C271/28 , C07C271/44 , C07C275/34 , C07C279/18 , C07C281/14 , C07C309/61 , C07C311/19 , C07C311/21 , C07C317/48 , C07C323/32 , C07C323/60 , C07C2603/46 , C07D207/16 , C07D211/58 , C07D213/30 , C07D213/61 , C07D213/65 , C07D213/75 , C07D239/26 , C07D239/30 , C07D239/42 , C07D261/10 , C07D261/18 , C07D295/108 , C07D295/155 , C07D295/215 , C07D307/28 , C07D307/68 , C07D317/54 , C07D401/04
摘要： PROBLEM TO BE SOLVED: To provide a novel substituted tetracycline compound useful to treat numerous tetracycline compound-responsive states such as bacterial infections and neoplasms. SOLUTION: The compound is represented by formula (I), wherein X is CH 2 , CH-alkyl or the like; R 2 , R 2' , R 3 , R 10 , R 11 and R 12 are hydrogen or the like; R 4 is dimethylamino or the like; R 5 is hydrogen or the like; R 7 is hydrogen, carboxyl, amino, cyano, phenyl that may be substituted, a heterocycle or the like; R 8 is hydrogen or the like; and R 9 is hydrogen, alkyl, amino or the like. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译： 要解决的问题：提供用于治疗许多四环素化合物反应状态的新型取代的四环素化合物，例如细菌感染和赘生物。 解决方案：该化合物由式（I）表示，其中X是CH 2，CH-烷基等; R
2 ，R 2'，R 3 ，R SP SP 10， 并且R 12为氢等; R 4是二甲基氨基等; R 5是氢等; R 7是氢，羧基，氨基，氰基，可被取代的苯基，杂环等; R 8是氢等; 并且R 9是氢，烷基，氨基等。 版权所有（C）2010，JPO＆INPIT -
公开(公告)号：JP2008266330A
公开(公告)日：2008-11-06
申请号：JP2008104216
申请日：2008-04-14
发明人： NELSON MARK L , OHEMENG KWASI , FRECHETTE ROGER , ISMAIL MOHAMED Y , HONEYMAN LAURA , BOWSER TODD , ABATO PAUL , AMOO VICTOR , ASSEFA HAREGEWEIN , BERNIAC JOEL , BHATIA BEENA , CHEN JACKSON , KIM OAK , MECHICHE RACHID , REDDY N LAXMA , VERMA ATUL K , VISKI PETER , WARCHOL TADEUSZ , YANACHKOV IVAN
IPC分类号： C07C237/26 , C07D295/14 , A61K31/65 , A61P1/02 , A61P1/04 , A61P1/12 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/00 , A61P13/02 , A61P13/10 , A61P15/00 , A61P15/14 , A61P17/00 , A61P17/02 , A61P17/16 , A61P19/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/16 , A61P29/00 , A61P29/02 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/06 , A61P37/08 , A61P43/00 , C07C275/34 , C07C323/60 , C07D207/06 , C07D207/16 , C07D207/20 , C07D207/327 , C07D207/335 , C07D207/40 , C07D207/404 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/56 , C07D213/74 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/36 , C07D261/10 , C07D261/14 , C07D261/18 , C07D263/22 , C07D277/14 , C07D277/20 , C07D277/42 , C07D277/56 , C07D295/18 , C07D295/20 , C07D307/54 , C07D317/66
CPC分类号： C07D207/404 , C07C237/26 , C07C239/20 , C07C255/58 , C07C271/22 , C07C275/34 , C07C323/60 , C07C335/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2603/46 , C07D207/16 , C07D207/20 , C07D207/335 , C07D209/44 , C07D211/58 , C07D211/70 , C07D213/20 , C07D213/64 , C07D213/82 , C07D213/89 , C07D231/12 , C07D261/10 , C07D261/14 , C07D261/18 , C07D277/42 , C07D277/56 , C07D295/116 , C07D295/155 , C07D295/215 , C07D307/52 , C07D307/54 , C07D317/66 , C07D335/02
摘要： PROBLEM TO BE SOLVED: To provide an aminomethyl-substituted tetracycline compound, a pharmaceutical composition, and methods of use thereof. SOLUTION: The tetracycline compound is represented by formula (I) (wherein R 1 and R 2 are combined to form a ring). COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译： 待解决的问题：提供氨基甲基取代的四环素化合物，药物组合物及其使用方法。 解决方案：四环素化合物由式（I）表示（其中R
1 和R 2 组合形成环）。 版权所有（C）2009，JPO＆INPIT
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