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公开(公告)号:US4990602A
公开(公告)日:1991-02-05
申请号:US283387
申请日:1988-12-12
申请人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Toshifumi Asaka , Yoshiaki Watanabe , Kaoru Sota , Kazuto Sekiuchi
发明人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Toshifumi Asaka , Yoshiaki Watanabe , Kaoru Sota , Kazuto Sekiuchi
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: Erthromycin A derivatives represented by the general formula ##STR1## wherein R.sup.1 is a group of the formula R.sup.7 CH.sub.2 -- (wherein R.sup.7 is a hydrogen group or a lower alkyl group) or a group of the formula R.sup.8 O-- (wherein R.sup.8 is a lower alkyl group), R.sup.2 is R.sup.8, a cycloalkyl group, a phenyl group or an aralkyl group.), or R.sup.2 and R.sup.7 together form an alkylene group, R.sup.3 is a hydrogen atom, a lower alkyl group, a phenyl group or an aralkyl group, or R.sup.3 and R.sup.7 together form an alkylene group, or R.sup.2 and R.sup.3 together form an alkylene group, R.sup.4 is a lower alkyl group, R.sup.5 is a substituted silyl group, and R.sup.6 is a hydrogen atom or R.sup.5, are disclosed. These compounds are useful as intermediates for the synthesis of antibacterial agents.
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公开(公告)号:US4670549A
公开(公告)日:1987-06-02
申请号:US832322
申请日:1986-02-24
申请人: Shigeo Morimoto , Takashi Adachi , Toshifumi Asaka , Masato Kashimura , Yoshiaki Watanabe , Kaoru Sota
发明人: Shigeo Morimoto , Takashi Adachi , Toshifumi Asaka , Masato Kashimura , Yoshiaki Watanabe , Kaoru Sota
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: A method for the selective methylation of the hydroxy group at the 6-position of erythromycin A derivatives which comprises reacting a compound represented by the formula R-X (wherein R is a 2-alkenyl group, a benzyl group or a substituted benzyl group, and X is a halogen atom), reacting the resulting quaternary salt compound with a methylating agent, and then eliminating R groups of the resulting compound to give 6-O-methylerythromycin A 9-oxime, is disclosed.
摘要翻译: 一种在红霉素A衍生物的6-位选择性甲基化羟基的方法,其包括使由式RX表示的化合物(其中R为2-链烯基,苄基或取代的苄基)和X 是卤素原子),使所得季盐化合物与甲基化剂反应,然后除去所得化合物的R基团,得到6-O-甲基红霉素A9-肟。
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公开(公告)号:USRE39560E1
公开(公告)日:2007-04-10
申请号:US10766747
申请日:2004-01-28
申请人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Yoshiaki Watanabe , Kaoru Sota
发明人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Yoshiaki Watanabe , Kaoru Sota
IPC分类号: C07H1/00
CPC分类号: C07H17/08
摘要: Erythromycin A derivatives represented by the general formula wherein R1 is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 of a halogen atom, an alkoxy group 1 to 4 carbon atoms, a nitro group or an alkoxycarbonyl group having 2 to 6 carbon atoms, R2 is a substituted silyl group and R3 is a hydrogen atom or R2, are disclosed. These compounds are useful as intermediates of the anti-bacterial agents.
摘要翻译: 以一般形式表示的红霉素A衍生物
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公开(公告)号:US06342590B1
公开(公告)日:2002-01-29
申请号:US07869111
申请日:1992-04-14
申请人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Yoshiaki Watanabe , Kaoru Sota
发明人: Shigeo Morimoto , Takashi Adachi , Tohru Matsunaga , Masato Kashimura , Yoshiaki Watanabe , Kaoru Sota
IPC分类号: C07H100
CPC分类号: C07H17/08
摘要: Erythromycin A derivatives represented by the general formula wherein R1 is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 of a halogen atom, an alkoxy group 1 to 4 carbon atoms, a nitro group or an alkoxycarbonyl group having 2 to 6 carbon atoms, R2 is a substituted silyl group and R3 is a hydrogen atom or R2, are disclosed. These compounds are useful as intermediates of the anti-bacterial agents.
摘要翻译: 由通式化合物R1表示的红霉素A衍生物是具有3〜15个碳原子的2-烯基,芳基甲基或被1〜3个卤素原子取代的芳甲基,1〜4个碳原子的烷氧基, 硝基或碳原子数为2〜6的烷氧基羰基,R2为取代甲硅烷基,R3为氢原子或R2。 这些化合物可用作抗细菌剂的中间体。
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公开(公告)号:US5350839A
公开(公告)日:1994-09-27
申请号:US39121
申请日:1993-04-15
申请人: Toshifumi Asaka , Yoko Misawa , Masato Kashimura , Shigeo Morimoto , Yoshiaki Watanabe , Katsuo Hatayama
发明人: Toshifumi Asaka , Yoko Misawa , Masato Kashimura , Shigeo Morimoto , Yoshiaki Watanabe , Katsuo Hatayama
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: Erythromycins showing an extremely relieved bitterness at administration and an improved absorbability in vivo when orally administered are provided.A compound having a group represented by the following formula:--O--CO--O--[(CH.sub.2).sub.m --O].sub.n --R(wherein R represents an alkyl group having from 1 to 12 carbon atoms, m represents an integer of from 2 to 4, and n represents an integer of from 1 to 7) at the 2'-position of erythromycins or a salt thereof.
摘要翻译: PCT No.PCT / JP91 / 01368 Sec。 371日期:1992年4月15日 102(e)日期1992年4月15日PCT 1991年10月8日PCT PCT。 出版物WO92 / 06991 日期:1992年4月30日。提供了施用时极度缓和的苦味和口服给药时体内吸收性改善的类似物。 具有由下式表示的基团的化合物:-O-CO-O - [(CH 2)m O] n R(其中R表示具有1至12个碳原子的烷基,m表示2至4的整数, 并且n表示1至7的整数)在红霉素的2'-位或其盐处。
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公开(公告)号:US5302705A
公开(公告)日:1994-04-12
申请号:US590805
申请日:1990-10-01
申请人: Yoko Misawa , Toshifumi Asaka , Masato Kashimura , Shigeo Morimoto , Yoshiaki Watanabe , Katsuo Hatayama
发明人: Yoko Misawa , Toshifumi Asaka , Masato Kashimura , Shigeo Morimoto , Yoshiaki Watanabe , Katsuo Hatayama
IPC分类号: A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号: C07H17/08
摘要: A 6-O-methylerythromycin A oxime derivative represented by the formula ##STR1## wherein X is a substituted benzyl group, a substituted phenyl group, an .alpha.-methylbenzyl group, an .alpha.-methylphenethyl group, a diphenylmethyl group, a trityl group, a dibenzosuberanyl group, or a group of the formula --(CH.sub.2).sub.n --R, and Y is a hydrogen atom, a substituted phenyl group or a 2-aminothiazol-4-ylmethylcarbonyl group, and a pharmaceutically acceptable salt thereof are disclosed. These compounds have antibacterial activity against erythromycin resistant bacteria.
摘要翻译: 由式(*化学结构*)表示的6-0-甲基红霉素A肟衍生物,其中X是取代的苄基,取代的苯基,(α) - 甲基苄基,(α) - 甲基苯乙基,二苯基甲基 基团,三苯甲基,二苯并胞苷基或式 - (CH 2)n R的基团,Y是氢原子,取代的苯基或2-氨基噻唑-4-基甲基羰基及其药学上可接受的盐 被披露。 这些化合物对抗红霉素的细菌具有抗菌活性。
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公开(公告)号:US5602239A
公开(公告)日:1997-02-11
申请号:US491860
申请日:1995-07-13
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: A novel macloride antibiotic having a potent antibacterial activity, represented by the formula: ##STR1## which is obtained by introducing a specific aryloxy or alkoxy group into the 3-position of a 5-O-desosaminylerythronolide derivative; or phamaceutically acceptable acid addition salts thereof.
摘要翻译: PCT No.PCT / JP94 / 00087 Sec。 371日期1995年7月13日 102(e)日期1995年7月13日PCT 1994年1月24日PCT公布。 公开号WO94 / 17088 日期1994年8月4日一种具有强效抗菌活性的新型macloride抗生素,由下式表示:通过将特定的芳氧基或烷氧基引入到5-O-去甲氨基戊三醇内酯衍生物的3-位而获得; 或其药学上可接受的酸加成盐。
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公开(公告)号:US5523399A
公开(公告)日:1996-06-04
申请号:US244981
申请日:1994-06-20
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: Provision of novel macrolide antibiotics having a strong antibacterial activity.Construction:Compounds represented by the formula: ##STR1## which are obtained by introducing a carbamoyl group into 5-O-desosaminyl-6-O-methylerythronolide derivatives at the 3-position; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译: PCT No.PCT / JP92 / 01713 Sec。 371日期:1994年6月20日 102(e)日期1994年6月20日PCT提交1992年12月15日PCT公布。 出版物WO93 / 日期:1993年7月8日。具有强抗菌活性的新型大环内酯类抗生素的制备。 结构:通过在3-位上将氨基甲酰基引入5-O-脱氨基-6-O-甲基红霉内酯衍生物而获得的由下式表示的化合物:
及其药学上可接受的酸加成盐。 -
公开(公告)号:US5631355A
公开(公告)日:1997-05-20
申请号:US318862
申请日:1994-10-17
IPC分类号: A61K31/395 , C07D491/00 , C07H17/00 , C07H17/08
摘要: Object: To provide novel macrolide antibiotics having a strong antibacterial activity. Constitution: 5-O-desosaminylerythronolide A derivatives represented by the formula: ##STR1## [wherein -A- - is a group of --N(R.sup.3)-- (wherein R.sup.3 is a hydrogen atom or an alkyl group having 1-3 carbon atoms) or a group represented by --N.dbd., and R.sup.1 and R.sup.2 are each a hydrogen atom or an alkyl group having 1-3 carbon atoms] which is a tricyclic carbamate of 5-0-desosaminylerythronolide A derivative having a ketone at the 3-position, being substituted by a methoxy group at the 6-position, and a pharmaceutically acceptable acid addition salt thereof; and a compound represented by the formula: ##STR2## (wherein R.sup.4 is an acetyl group or a propionyl group) which is an intermediate useful for the preparation of the 3-ketone forms of 5-O-desosaminylerythronolide A derivatives.
摘要翻译: PCT No.PCT / JP93 / 00517 Sec。 371日期:1994年10月17日 102(e)日期1994年10月17日PCT提交1993年4月21日PCT公布。 公开号WO93 / 21200 PCT 日期:1993年10月28日目的:提供具有强抗菌活性的新型大环内酯类抗生素。 结构式:5-O-去甲氨基戊三醇酯由下式表示的A衍生物:其中-A + E,非 - + EE是-N(R3) - (其中R3是氢原子或烷基 具有1-3个碳原子)或由-N =表示的基团,并且R 1和R 2各自为氢原子或具有1-3个碳原子的烷基],其为具有5-0-去甲氨基戊三烯酸酯A衍生物的三环氨基甲酸酯,其具有 3-位上的酮被6位的甲氧基取代,其药学上可接受的酸加成盐; 和由下式表示的化合物:其中R 4是乙酰基或丙酰基,其是可用于制备5-O-去甲氨基戊二烯内酰脲衍生物的3-酮形式的中间体。
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公开(公告)号:US5631354A
公开(公告)日:1997-05-20
申请号:US256124
申请日:1994-06-21
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: Object:Provision of novel macrolide antibiotics having a strong antibacterial activity.Construction:Compounds represented by the formula: ##STR1## which are obtained by introducing a certain substituted carbonyloxy group into 5-O-desosaminylerythronolide derivatives at the 3-position; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译: PCT No.PCT / JP92 / 01714 Sec。 371日期:1994年6月21日 102(e)日期1994年6月21日PCT提交1992年12月25日PCT公布。 公开号WO93 / 13116 PCT 日期1993年7月8日目的:提供具有强抗菌活性的新型大环内酯类抗生素。 结构:通过在3-位上将某些取代的羰基氧基引入到5-O-脱氨基甲基红霉内酯衍生物中而获得的由下式表示的化合物:
及其药学上可接受的酸加成盐。
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