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1. 发明授权

US4205163A Tylosin derivatives 失效
标题翻译：泰乐菌素衍生物
公开(公告)号：US4205163A
公开(公告)日：1980-05-27
申请号：US954055
申请日：1978-10-23
申请人： Shunro Mori , Rokuro Okamoto , Taiji Inui , Tomio Takeuchi
发明人： Shunro Mori , Rokuro Okamoto , Taiji Inui , Tomio Takeuchi
IPC分类号： C07H17/08 , A61K31/71
CPC分类号： C07H17/08
摘要： A number of 4"-acyl derivatives of tylosin and acetyltylosin which are prepared by first protectively acylating at the 2'-hydroxyl group of tylosin or acetyltylosin, secondly at the 4'"-hydroxyl group thereof, thirdly at the 4"-hydroxyl group thereof and finally deacylating the 2'- and 4'"-acyl groups to produce new 4"-acyl derivatives of tylosin or acetyltylosin which effect high blood level compared to those tylosin derivatives heretofore are disclosed.
摘要翻译：通过首先在泰乐菌素或乙酰转铁蛋白的2'-羟基保护性酰化制备泰乐菌素和乙酰转铁蛋白的4个“酰基衍生物，其次是其4”'羟基，第三次在4“ - 羟基，最后使2'-和4“ - 酰基脱酰基，以产生与迄今公开的那些泰乐菌素衍生物相比，其效应高血药浓度的泰乐菌素或乙酰转铁蛋白的新4'-酰基衍生物。

2. 发明授权

US5091370A Angolamycin derivatives 失效
标题翻译：角叉菜胶衍生物
公开(公告)号：US5091370A
公开(公告)日：1992-02-25
申请号：US539743
申请日：1990-06-18
申请人： Takeo Yoshioka , Azuma Watanabe , Koichiro Kominato , Hiroshi Tone , Rokuro Okamoto , Tsutomu Sawa , Tomio Takeuchi
发明人： Takeo Yoshioka , Azuma Watanabe , Koichiro Kominato , Hiroshi Tone , Rokuro Okamoto , Tsutomu Sawa , Tomio Takeuchi
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： An angolamycin derivative represented by the following formula ##STR1## wherein X represents an acetyl, methanesulfonyl, methylthio, benzoyl or methoxy group. This compound is useful as a medicament such as antibacterial agent and an animal feed additive.

3. 发明授权

US4463171A Derivatives of macrolide antibiotics 失效
标题翻译：大环内酯类抗生素衍生物
公开(公告)号：US4463171A
公开(公告)日：1984-07-31
申请号：US502480
申请日：1983-06-09
申请人： Hamao Umezawa , Tomio Takeuchi , Kuniaki Tatsuta , Tomoyuki Ishikura , Rokuro Okamoto , Masao Yamamoto , Kohki Kiyoshima
发明人： Hamao Umezawa , Tomio Takeuchi , Kuniaki Tatsuta , Tomoyuki Ishikura , Rokuro Okamoto , Masao Yamamoto , Kohki Kiyoshima
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of the following general formula ##STR1## wherein R.sup.1 and R.sup.2 represent a hydrogen atom or a lower alkanoyl group;R.sup.3 represents a hydrogen atom or the group --COCH.sub.2 R.sup.5 in which R.sup.5 represents a lower alkyl group or an aryl or pyridyl group bonded through a sulfur atom;R.sup.4 represents a methyl group which may be substituted by aryl, pyridyl, pyridylthio, hydroxyl or arylthioamino, an aryl group, a nitrile group, a 5- or 6-membered heterocyclic group having 1 to 4 hetero atoms selected from nitrogen and sulfur atoms, or a tetrahydropyranyl group which may be substituted by methoxy;A represents the group --OCO--, --OSO.sub.2 --, --O-- or --S--, or A and R.sup.4, taken together, represent a halogen atom, a nitrile group or a group of the formula ##STR2## in which R.sup.6 represents two lower alkyl groups, the group ##STR3## or an alkylene group having 4 to 6 carbon atoms which may have in the chain an oxygen atom or a lower alkyl-substituted nitrogen atom; and said aryl group and heterocyclic group may optionally be substituted by a methyl, methoxy or nitro group, and when R.sup.1 represents a lower alkyl group,R.sup.3 does not represent a lower alkyl group,or their salts.These novel derivatives of macrolide antibiotics have excellent antibacterial activity.
摘要翻译：下列通式的化合物：其中R 1和R 2表示氢原子或低级烷酰基; R3表示氢原子或基团-COCH2R5，其中R5表示低级烷基或通过硫原子键合的芳基或吡啶基; R 4表示可以被芳基，吡啶基，吡啶硫基，羟基或芳硫基氨基，芳基，腈基，具有1-4个选自氮和硫原子的杂原子的5或6元杂环基取代的甲基，或可被甲氧基取代的四氢吡喃基; A代表基团-OCO-，-OSO 2 - ， - O-或-S-，或A和R 4一起代表卤素原子，腈基或式（IMAGE）基团，其中R6代表二低级烷基，基团或具有4-6个碳原子的亚烷基，其可以在链中具有氧原子或低级烷基取代的氮原子; 并且所述芳基和杂环基可任选被甲基，甲氧基或硝基取代，并且当R 1表示低级烷基时，R 3不表示低级烷基或其盐。这些大环内酯类抗生素的新型衍生物具有优良的抗菌活性。

4. 发明授权

US4954438A Process for preparing antibiotics D788-7 失效
标题翻译：制备抗生素D788-7的方法
公开(公告)号：US4954438A
公开(公告)日：1990-09-04
申请号：US397061
申请日：1989-08-21
申请人： Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Rokuro Okamoto , Tomio Takeuchi
发明人： Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Rokuro Okamoto , Tomio Takeuchi
IPC分类号： C12P19/56 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12R1/465
CPC分类号： C07H15/252 , Y10S435/886
摘要： This invention relates to a process for preparing an antibiotic D788-7 wherein, after culturing carborubicin-producing bacteria, the obtained culture liquid is extracted in acidic conditions while stirring to be absorbed to synthetic resin, followed by desorption from the resin and elution with acetone and the resulting acetone solution containing carborubicin is converted into an antibiotic D788-7 by photo radiation, for obtaining D788-7 in the purified form from the reaction solution. The production yield for D788-7 is extremely high and its use as an antitumor agent can be made possible.

5. 发明授权

US4612372A Tylosin derivatives 失效
标题翻译：泰乐菌素衍生物
公开(公告)号：US4612372A
公开(公告)日：1986-09-16
申请号：US754568
申请日：1985-07-12
申请人： Takeo Yoshioka , Miharu Maeda , Rokuro Okamoto , Yasutaka Shimauchi , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
发明人： Takeo Yoshioka , Miharu Maeda , Rokuro Okamoto , Yasutaka Shimauchi , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Novel tylosin derivatives are represented by formula: ##STR1## wherein R represents a hydrogen atom, an acetyl group or a propionyl group; X represents a group --CO-- or --SO.sub.2 --; Y represents a fluorine atom, an acetyl group, a methanesulfonyl group, a methylthio group, a benzoyl group or a methoxy group bound to the benzyl group at the 2-position or 4-position; and Z represents a hydrogen atom or a D-mycinose residue: ##STR2## The tylosin derivatives which are antibiotics of macrolide type provide improved antibacterial activity and improved ability of absorption and excretion in vivo.
摘要翻译：新型泰乐菌素衍生物由下式表示：其中R代表氢原子，乙酰基或丙酰基; X表示-CO-或-SO 2 - 基团; Y表示在2位或4位与苄基结合的氟原子，乙酰基，甲磺酰基，甲硫基，苯甲酰基或甲氧基; Z代表氢原子或D-霉菌素残留物：作为大环内酯类抗生素的泰乐菌素衍生物提供了改善的抗菌活性和提高体内吸收和排泄的能力。

6. 发明授权

US4201843A Process for manufacturing tylosin derivatives 失效
标题翻译：制备泰乐菌素衍生物的方法
公开(公告)号：US4201843A
公开(公告)日：1980-05-06
申请号：US881279
申请日：1978-02-27
申请人： Rokuro Okamoto , Tsumoru Fukumoto , Akira Takamatsu , Tomio Takeuchi
发明人： Rokuro Okamoto , Tsumoru Fukumoto , Akira Takamatsu , Tomio Takeuchi
IPC分类号： C07H17/08 , C12P19/62 , C12R1/55
CPC分类号： C07H17/08 , C12P19/62 , C12R1/465 , C12R1/55 , Y10S435/898
摘要： New tylosin derivatives having at least one acyl group at the 3- and 4"-positions of tylosin, and the acid addition salts thereof, which inhibit the growth of various microorganisms including drug-resistant bacterial isolants and which produce high blood levels through oral administration are produced by a biochemical reaction using the microorganisms of the genus Streptomyces which are selected for their newly-found ability to acylate at least one of the 3- and 4"-positions of macrolide antibiotics; they are recovered from the reacted mixture by conventional methods for recovering macrolide antibiotics.
摘要翻译：在泰乐菌素的3和4“位具有至少一个酰基的新泰乐菌素衍生物及其酸加成盐，其抑制各种微生物生长，包括耐药性细菌分离物，并通过口服产生高血药浓度通过使用由链霉菌属（Streptomyces）属的微生物生物化学反应来产生施用，所述微生物被选择用于其新发现的能够酰化大环内酯类抗生素的3-和4-位中的至少一个的能力; 它们通过用于回收大环内酯类抗生素的常规方法从反应混合物中回收。

7. 发明授权

US4092473A Tylosin derivatives and their manufacturing process 失效
标题翻译：泰乐菌素衍生物及其制造工艺
公开(公告)号：US4092473A
公开(公告)日：1978-05-30
申请号：US708151
申请日：1976-07-23
申请人： Rokuro Okamoto , Tsumoru Fukumoto , Akira Takamatsu , Tomio Takeuchi
发明人： Rokuro Okamoto , Tsumoru Fukumoto , Akira Takamatsu , Tomio Takeuchi
IPC分类号： C07H17/08 , C12P19/62 , A61K31/71
CPC分类号： C07H17/08 , C12P19/62 , Y10S435/886
摘要： New tylosin derivatives having at least one acyl group at the 3- and 4"-positions of tylosin, and the acid addition salts thereof, which inhibit the growth of various microorganisms including drug-resistant bacterial isolants and which produce high blood levels through oral administration are produced by a biochemical reaction using the microorganisms of the genus Streptomyces which are selected for their newly-found ability to acylate at least one of the 3- and 4"-positions of macrolide antibiotics; they are recovered from the reacted mixture by conventional methods for recovering macrolide antibiotics.
摘要翻译：在泰乐菌素的3和4“位具有至少一个酰基的新泰乐菌素衍生物及其酸加成盐，其抑制各种微生物生长，包括耐药性细菌分离物，并通过口服产生高血药浓度通过使用由链霉菌属（Streptomyces）属的微生物生物化学反应来产生施用，所述微生物被选择用于其新发现的能够酰化大环内酯类抗生素的3-和4-位中的至少一个的能力; 它们通过用于回收大环内酯类抗生素的常规方法从反应混合物中回收。

8. 发明授权

US4918172A Anthracycline antibiotics 失效
标题翻译：蒽环类抗生素
公开(公告)号：US4918172A
公开(公告)日：1990-04-17
申请号：US252636
申请日：1988-10-03
申请人： Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Rokuro Okamoto , Tomoyuki Ishikura , Hiroshi Naganawa , Tsutomu Sawa , Tomio Takeuchi
发明人： Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Rokuro Okamoto , Tomoyuki Ishikura , Hiroshi Naganawa , Tsutomu Sawa , Tomio Takeuchi
IPC分类号： C07H15/252
CPC分类号： C07H15/252
摘要： Disclosed are anthracycline antibiotics of a formula (I): ##STR1## in which R.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is 1-hydroxyethyl group, R.sup.4 is hydrogen atom and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1, R.sup.2 and R.sup.4 are hydroxyl groups, R.sup.3 is ethyl group and X represents daunosamine-rhodenose, daunosamine-deoxyfucose, rhodosamine-rhodenose, N-monomethyldaunosamine-rhodenose or N-monomethyldaunosamine-deoxyfucose; orR.sup.1 is methoxy group, R.sup.2 is hydroxyl group, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.4 are hydroxy groups, R.sup.2 is hydrogen atom, R.sup.3 is ethyl group and X represents daunosamine-deoxyfucose, as well as pharmaceutically acceptable acid addition salts thereof. The antibiotics (I) have a carcinostatic activity and are useful as a carcinostatic for murine leukemia L1210 cells in culture.

9. 发明授权

US5474923A Method for the biological preparation of hydroxyvitamin D compounds 失效
标题翻译：羟基维生素D化合物的生物制备方法
公开(公告)号：US5474923A
公开(公告)日：1995-12-12
申请号：US711988
申请日：1991-06-07
申请人： Koji Takeda , Kiyoshi Kimura , Kazuhiko Okamura , Rokuro Okamoto , Joji Sasaki , Takashi Adachi , Sadafumi Omura
发明人： Koji Takeda , Kiyoshi Kimura , Kazuhiko Okamura , Rokuro Okamoto , Joji Sasaki , Takashi Adachi , Sadafumi Omura
IPC分类号： C12P7/02 , C12R1/01 , C12R1/365
CPC分类号： C12P7/02
摘要： A method for introducing hydroxyl groups into vitamin D compound at the 1.alpha.- and/or 25-positions in the presence of a cyclodextrin compound by the use of a reaction mixture containing a microorganism being capable of hydroxylating vitamin D compound or a enzyme produced from the microorganism, is disclosed.
摘要翻译：在环糊精化合物的存在下，在1α和/或25位上将羟基引入维生素D化合物的方法是使用含有能够使维生素D化合物羟化的微生物的反应混合物或由该微生物被公开。

10. 发明授权

US5232943A Antibiotics Mer-AF1032A and Mer-AF1032B 失效
标题翻译：抗生素MER-AF1032A和MER-AF1032B
公开(公告)号：US5232943A
公开(公告)日：1993-08-03
申请号：US885771
申请日：1992-05-20
申请人： Hitosi Agematu , Yoshio Watanabe , Hiroyuki Chiba , Rei Kaneto , Norio Shibamoto , Takeo Yoshioka , Toshihiko Kumamoto , Hiroshi Nishida , Rokuro Okamoto
发明人： Hitosi Agematu , Yoshio Watanabe , Hiroyuki Chiba , Rei Kaneto , Norio Shibamoto , Takeo Yoshioka , Toshihiko Kumamoto , Hiroshi Nishida , Rokuro Okamoto
IPC分类号： C07D311/92 , C12P17/06 , C12R1/80
CPC分类号： C12P17/06 , C07D311/92
摘要： Antibiotic Mer-AF1032A represented by the following formula (I) and its isomer antibiotic Mer-AF1032B are disclosed. Also disclosed are a method for preparing the antibiotics comprising the cultivation of a strain belonging to genus Penicillium and a pharmaceutical composition comprising one of these antibiotics and useful as an antifungal agent. ##STR1##

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