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

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。

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.

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。

公开(公告)号：US4680386A

公开(公告)日：1987-07-14

申请号：US789771

申请日：1985-10-21

申请人： Shigeo Morimoto ,  Takashi Adachi ,  Toshifumi Asaka ,  Yoshiaki Watanabe ,  Kaoru Sota

发明人： Shigeo Morimoto ,  Takashi Adachi ,  Toshifumi Asaka ,  Yoshiaki Watanabe ,  Kaoru Sota

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08

摘要： A novel 6-O-methylerythromycin A derivative represented by the formula ##STR1## and the salts thereof are disclosed. These compounds are useful as intermediates for preparation of 6-O-methylerythromycin A and useful as antibiotics.

摘要翻译： 公开了由式“IMAGE”表示的新型6-O-甲基红霉素A衍生物及其盐。 这些化合物可用作制备6-O-甲基红霉素A并用作抗生素的中间体。

公开(公告)号：US4672109A

公开(公告)日：1987-06-09

申请号：US720383

申请日：1985-04-05

申请人： Yoshiaki Watanabe ,  Shigeo Morimoto ,  Masami Goi ,  Morihiro Mitsukuchi ,  Takashi Adachi ,  Jozi Nakagami ,  Toshifumi Asaka ,  Tadashi Eguchi ,  Kaoru Sota

发明人： Yoshiaki Watanabe ,  Shigeo Morimoto ,  Masami Goi ,  Morihiro Mitsukuchi ,  Takashi Adachi ,  Jozi Nakagami ,  Toshifumi Asaka ,  Tadashi Eguchi ,  Kaoru Sota

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： A method for the selective methylation of a hydroxy group at the 6-position of an erythromycin A derivative which comprises converting an erythromycin A derivative into an erythromycin A 9-oxime derivative, and reacting the resulting ethythromycin A 9-oxime derivative with an methylating agent.

摘要翻译： 一种在红霉素A衍生物的6位上羟基选择性甲基化的方法，其包括将红霉素A衍生物转化为红霉素A9-肟衍生物，并使得到的乙酸霉素A9-肟衍生物与甲基化试剂 。

公开(公告)号：US4833236A

公开(公告)日：1989-05-23

申请号：US43470

申请日：1987-04-28

申请人： Shigeo Morimoto ,  Yoko Takahashi ,  Yoshiaki Watanabe ,  Takashi Adachi ,  Toshifumi Asaka ,  Kaoru Sota

发明人： Shigeo Morimoto ,  Yoko Takahashi ,  Yoshiaki Watanabe ,  Takashi Adachi ,  Toshifumi Asaka ,  Kaoru Sota

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08

摘要： Erythromycin derivatives represented by the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or a hydroxy group, R.sup.3 is a hydrogen atom, a lower alkanoyl group, an alkoxycarbonyl group or an alkylsuccinyl group, and the salts thereof are disclosed. These compounds have antibacterial activity.

公开(公告)号：US4668776A

公开(公告)日：1987-05-26

申请号：US846520

申请日：1986-03-31

申请人： Toshiro Yamada ,  Hiroshi Fujisawa ,  Kuniaki Goto ,  Shigeo Morimoto ,  Takashi Adachi ,  Yoshiaki Watanabe

发明人： Toshiro Yamada ,  Hiroshi Fujisawa ,  Kuniaki Goto ,  Shigeo Morimoto ,  Takashi Adachi ,  Yoshiaki Watanabe

IPC分类号： C07H17/08

CPC分类号： C07H17/08 ,  Y02P20/55

摘要： There is disclosed a novel protected des-N-methylerythromycin derivative, in which 2', 3' and 9-positions are protected with new substituents that can provide stabler derivative and can be eliminated in a single reaction under neutral condition.

摘要翻译： 公开了一种新的受保护的脱-N-甲基红霉素衍生物，其中2'，3'和9“位置被新的取代基保护，所述取代基可以提供更稳定的衍生物并且可以在中性条件下在单一反应中消除。

公开(公告)号：US4496717A

公开(公告)日：1985-01-29

申请号：US444170

申请日：1982-11-24

申请人： Takashi Adachi ,  Shigeo Morimoto ,  Yoko Takahashi ,  Yoshiaki Watanabe ,  Sadafumi Omura

发明人： Takashi Adachi ,  Shigeo Morimoto ,  Yoko Takahashi ,  Yoshiaki Watanabe ,  Sadafumi Omura

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08 ,  Y02P20/55

摘要： Novel erythromycin B derivatives of the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each hydrogen or methyl, and the pharmaceutically acceptable acid addition salts thereof are disclosed. They exhibit excellent in vivo antibacterial activity against Gram-positive bacteria.

摘要翻译： 其中R1和R2相同或不同并且各自为氢或甲基的新颖的红霉素B衍生物及其药学上可接受的酸加成盐。 它们对革兰氏阳性菌表现出优异的体内抗菌活性。

公开(公告)号：US06713615B2

公开(公告)日：2004-03-30

申请号：US10344529

申请日：2003-02-12

申请人： Masato Kashimura ,  Hiroaki Kamiyama ,  Takeshi Kuwada ,  Nobuyuki Suzuki ,  Takashi Adachi

发明人： Masato Kashimura ,  Hiroaki Kamiyama ,  Takeshi Kuwada ,  Nobuyuki Suzuki ,  Takashi Adachi

IPC分类号： C07H100

CPC分类号： C07H17/08

摘要： There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C—O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.

摘要翻译： 提供了一种用于有效合成6-O-取代的酮内酯衍生物的制备方法，其通过组合在6位上引入取代基的特征性步骤，通过选择性裂解环状缩醛在9位上的CO键 通过6,9-环状缩醛5-O-去氨基酰基红新环素衍生物，在9位和3位转化为羰基的步骤和11,12-环状氨基甲酰化作用以产生6-O-取代的步骤 酮内酯衍生物。