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：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：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：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：US4812562A

公开(公告)日：1989-03-14

申请号：US887941

申请日：1986-07-22

申请人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Kaoru Sota

发明人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Kaoru Sota

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/36 ,  C07D501/59

CPC分类号： C07D501/59 ,  Y02P20/55

摘要： Cephalosporin derivatives represented by the general formula ##STR1## wherein X represents a halogen atom, a hydroxyl group, a cyano group, a trifluoromethyl group, an amino group, a lower alkylcarbonylamino group, a lower alkoxy group, a lower alkylthio group, a lower alkoxycarbonyl group, a carbamoyl group, a substituted carbamoyl group, a carbamoyloxy group, a lower alkylcarbonyl group, a lower alkenyl group, an ethynyl group, a thiocyanate group, an .alpha.-carboxyaminomethyl group, a phenyl group, a pyridinyl group or an aminothiazolyl group, and n is an integer of 1 to 3, and the non-toxic salts thereof, are disclosed. These compounds are useful as antibacterial agents.

摘要翻译： 由通式表示的头孢菌素衍生物，其中X表示卤素原子，羟基，氰基，三氟甲基，氨基，低级烷基羰基氨基，低级烷氧基，低级烷硫基，低级 烷氧基羰基，氨基甲酰基，取代氨基甲酰基，氨基甲酰氧基，低级烷基羰基，低级烯基，乙炔基，硫氰酸酯基，α-羧基氨基甲基，苯基，吡啶基或氨基噻唑基 基，n为1〜3的整数，并且其无毒盐被公开。 这些化合物可用作抗菌剂。

公开(公告)号：US4841044A

公开(公告)日：1989-06-20

申请号：US943037

申请日：1986-12-18

申请人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Minoru Taguchi ,  Kaoru Sota

发明人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Masami Goi ,  Akira Onodera ,  Mitsuo Murata ,  Hiroshi Fukushima ,  Minoru Taguchi ,  Kaoru Sota

IPC分类号： A61K31/545 ,  C07D501/36 ,  C07D501/59

CPC分类号： C07D501/59

摘要： Cephalosporin derivatives represented by the general formula ##STR1## wherein R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R' is a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, or R and R' together with the nitrogen atom to which they are attached form a tetrahydropyridinyl group, a morpholinyl group or pyrroridinyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.

摘要翻译： 其中R为氢原子或碳原子数为1〜4的低级烷基，R'为氢原子，碳原子数1〜4的低级烷基， ，具有5或6个碳原子的环烷基或苄基，或R和R'与它们所连接的氮原子一起形成四氢吡啶基，吗啉基或吡咯烷基，其无毒盐是 披露 这些化合物可用作抗菌剂。

公开(公告)号：US4357470A

公开(公告)日：1982-11-02

申请号：US256780

申请日：1981-04-23

申请人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Toshifumi Asaka ,  Akira Onodera ,  Kaoru Sota ,  Jiro Sawada

发明人： Yoshiaki Watanabe ,  Chihiro Yokoo ,  Toshifumi Asaka ,  Akira Onodera ,  Kaoru Sota ,  Jiro Sawada

IPC分类号： C07D519/06 ,  A61K31/545 ,  A61P31/04 ,  C07D471/04 ,  C07D501/26 ,  C07D501/36 ,  C07D501/56

CPC分类号： C07D471/04

摘要： Novel cephalosporin compounds having the general formula ##STR1## wherein X represents hydrogen atom or hydroxy group, and the non-toxic pharmacologically acceptable salts thereof are disclosed. These compounds are useful as antibacterial agents.

摘要翻译： 公开了具有通式 + TR 的新型头孢菌素化合物，其中X表示氢原子或羟基，并且其无毒的药理学上可接受的盐被公开。 这些化合物可用作抗菌剂。