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1. 发明授权

US5541303A 3,4'-dideoxymycaminosltylonolide derivative and process for producing the same 失效
标题翻译： 3,4'-二脱氧米霉素三奈乐莱衍生物及其制备方法
公开(公告)号：US5541303A
公开(公告)日：1996-07-30
申请号：US256537
申请日：1994-07-13
申请人： Tomio Takeuchi , Sumio Umezawa , Osamu Tsuchiya , Shunji Kageyama , Toshiaki Miyake , Naoki Matsumoto , Kaichiro Kominato , Hiroshi Tanaka , Takeo Yoshioka
发明人： Tomio Takeuchi , Sumio Umezawa , Osamu Tsuchiya , Shunji Kageyama , Toshiaki Miyake , Naoki Matsumoto , Kaichiro Kominato , Hiroshi Tanaka , Takeo Yoshioka
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： A compound of the following formula is provided: ##STR1## wherein A represents a carbonyl group which may be protected; B represents an aldehyde group which may be protected; R.sup.1 represents a hydroxyl group which may be protected; R.sup.2 represents a hydrogen atom or acyl group; W represents a hydrogen atom, hydroxyl group, lower alkanoyloxy group or substituted sulfonyloxy group; Y represents a hydrogen atom, halogen atom, hydroxyl group or substituted sulfonyloxy group; and broken line "-------" represents a double bond or single bond. This compound is useful for producing 3,4'-dideoxymycaminosyltylonolide useful as an antimicrobial agent.
摘要翻译： PCT No.PCT / JP93 / 00031 Sec。 371日期：1994年7月13日 102（e）日期1994年7月13日PCT提交1993年1月12日PCT公布。公开号WO93 / 14101 日期：1993年7月22日提供下式的化合物：其中A表示可被保护的羰基; B表示可以被保护的醛基; R1表示可被保护的羟基; R2表示氢原子或酰基; W表示氢原子，羟基，低级烷酰氧基或取代磺酰氧基; Y表示氢原子，卤素原子，羟基或取代磺酰氧基; 虚线“-------”表示双键或单键。该化合物可用于生产可用作抗微生物剂的3,4'-二脱氧米霉素三奈兰内酯。

2. 发明授权

US06514946B1 Macrolide antibiotics and treatment and prophylaxis of pasteurellosis using the same 有权
标题翻译：大环内酯类抗生素，并使用其治疗和预防巴斯德氏菌病
公开(公告)号：US06514946B1
公开(公告)日：2003-02-04
申请号：US09649038
申请日：2000-08-29
申请人： Toshiaki Miyake , Tomohisa Takita , Masa Hamada , Tomio Takeuchi , Sumio Umezawa
发明人： Toshiaki Miyake , Tomohisa Takita , Masa Hamada , Tomio Takeuchi , Sumio Umezawa
IPC分类号： A61K3170
CPC分类号： C07H17/08
摘要： 20,23-disubstituted mycaminosyltylonolide derivatives and use of the same in the field of the prophylaxis and treatment of pasteurellosis are disclosed. The di-substituents are peperidino optionally substituted with one or two methyl groups. The derivatives have selective antibacterial activity against Pasteurella.
摘要翻译：公开了20,23-二取代的碳霉糖基太里洛烯衍生物及其在巴斯德氏菌病的预防和治疗领域中的应用。二取代基是任选被一个或两个甲基取代的哌啶子基。衍生物对巴氏杆菌有选择性的抗菌活性。

3. 发明授权

US4298727A 3',4'-Dideoxykanamycin A and 1-N-(S)-.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof 失效
标题翻译： 3'，4'-双脱氧卡那霉素A和1-N-（S）-α-羟基-ω-氨基烷酰基）衍生物
公开(公告)号：US4298727A
公开(公告)日：1981-11-03
申请号：US114779
申请日：1980-01-23
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomo Jikahara , Toshiaki Miyake
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Tomo Jikahara , Toshiaki Miyake
IPC分类号： C07H15/234 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/236 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： 3',4'-Dideoxy derivative and 1-N-((S)-.alpha.-hydroxy-.omega.-aminoalkanoyl)-3',4'-dideoxy derivative of kanamycin A are now synthetized from kanamycin A and show a wider and/or higher antibacterial activity than the parent kanamycin A so that they are useful in therapeutic treatment of infections by gram-negative and gram-positive bacteria, including drug-resistant strains thereof. The production of these new derivatives may be made by preparing a protected kanamycin A derivative having its 3'- and 4'-hydroxyl groups unprotected and having its all or substantially all other functional groups protected from the initial material, kanamycin A, sulfonylating the 3'- and 4'-hydroxyl groups, removing the 3'- and 4'-sulfonyloxy groups from the resulting 3',4'-di-sulfonic acid ester product to give a 3'-eno-kanamycin A derivative, hydrogenating the 3'-eno-kanamycin A derivative to saturate the 3',4'-unsaturated bond and to yield a protected 3',4'-dideoxykanamycin A product, followed by removal of the remainiing protective groups, and optionally further followed by 1-N-acylation of the 1-amino group of the resulting 3',4'-dideoxykanamycin A with an (S)-.alpha.-hydroxy-.omega.-aminoalkanoic acid or its reactive equivalent.
摘要翻译：卡那霉素A的3'，4'-二脱氧衍生物和1-N - （（S）-α-羟基-ω-氨基烷酰基）-3'，4'-二脱氧衍生物现在从卡那霉素A合成并显示出更宽和/ 或更高的抗菌活性，使得它们可用于革兰氏阴性和革兰氏阳性细菌（包括其耐药菌株）的感染的治疗性治疗。这些新衍生物的生产可以通过制备其未被保护的3'和4'-羟基的保护的卡那霉素A衍生物和其全部或基本上所有其它保护起始材料的卡那霉素A的其他官能团来制备，磺酰化3 '和4'-羟基，从所得的3'，4'-二磺酸酯产物中除去3'-和4'-磺酰氧基，得到3'-烯 - 卡那霉素A衍生物，将3 ' - 卡那霉素A衍生物使3'，4'-不饱和键饱和并产生受保护的3'，4'-二脱氧卡那霉素A产物，然后除去剩余的保护基，并且任选地进一步加入1-N 所得的3'，4'-二脱氧卡那霉素A的1-氨基酸与（S）-α-羟基-ω-氨基链烷酸或其反应性等同物的酰基化。

4. 发明授权

US4349666A Process for the production of kanomycin B derivatives and products obtained therefrom 失效
标题翻译：生产卡那霉素B衍生物的方法及由此获得的产品
公开(公告)号：US4349666A
公开(公告)日：1982-09-14
申请号：US196586
申请日：1980-10-14
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Toshiaki Miyake
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Toshiaki Miyake
IPC分类号： C07H15/234 , C07H15/236 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： 3'-Deoxykanamycin B, namely tobramycin is produced in an improved yield with a reduced reaction time under moderate reaction conditions, starting from a penta-N-protected 3'-mono-O-alkyl-, aralkyl- or arylsulfonylated derivative of kanamycin B in which all the 1, 3, 2' and 3"-amino groups and possibly the 6'-amino group have been protected by an arylsulfonyl group, especially tosyl group; the 3'-hydroxyl group of kanamycin B has been alkyl-, aralkyl- or arylsulfonylated; the 4"- and 6"-hydroxyl groups have been blocked with a di-valent hydroxyl-protecting group; and possibly the 4'-hydroxyl group and 6'-amino group have been blocked by being converted into the form of a 4', 6'-cyclic carbamate formed between the 4'-hydroxyl group and the 6'-amino group, by subjecting to a process essentially comprising reaction of said protected kanamycin B derivative with a metal halide for a reaction time of 30 min. to 2 hours at a reaction temperature of 0.degree. C..about.150.degree. C. to produce the corresponding 3'-halo compound, reductive replacement of the 3'-halo group by hydrogen and deprotection.
摘要翻译： 3-脱氧卡那霉素B，即在中等反应条件下，以5-N保护的3'-单-O-烷基 - 芳烷基 - 或芳基磺酰化衍生物开始，在中等反应条件下，产率提高，产量提高，反应时间缩短。其中所有1,3,2'和3“ - 氨基和可能的6'-氨基都被芳基磺酰基，尤其是甲苯磺酰基保护; 卡那霉素B的3'-羟基已经是烷基 - ，芳烷基 - 或芳基磺酰化; 4“和6” - 羟基已被二价羟基保护基封闭; 并且可能的4'-羟基和6'-氨基已经通过在4'-羟基和6'-氨基之间形成的4'，6'-环状氨基甲酸酯的形式被阻断，通过进行基本上包含所述受保护的卡那霉素B衍生物与金属卤化物的反应的方法，反应时间为30分钟。在0℃的反应温度下反应2小时。在150℃降解产生相应的3'-卤代化合物，通过氢还原取代3'-卤代基团并脱保护。

5. 发明授权

US4907247A Satellite delay simulation system 失效
标题翻译：卫星延时仿真系统
公开(公告)号：US4907247A
公开(公告)日：1990-03-06
申请号：US314100
申请日：1989-02-22
申请人： Toshiaki Miyake , Mikio Ujiie
发明人： Toshiaki Miyake , Mikio Ujiie
IPC分类号： H04J3/14 , H04B7/15 , H04B17/00
CPC分类号： H04B17/0085
摘要： Equipment for testing a digital satellite communication system in which multiple digital satellite communication terminals are interconnectable over multiple channels. The equipment includes a single satellite delay simulator intervening between transmit communication terminals and receive communication terminals. The delay simulator is implemented by a satellite delay circuit accommodating multiple channels, and clock matching circuits each being connected to the output or the input of the delay circuit, whereby the communication terminals are individually connectable to the delay circuit via the clock matching circuits. With this configuration, the equipment tests the system by applying a satellite delay simulation to all of the communication terminals, which are operating on independent clocks, at the same time and by using a single satellite delay simulator.
摘要翻译：用于测试数字卫星通信系统的设备，其中多个数字卫星通信终端可在多个信道上互连。该设备包括在发射通信终端和接收通信终端之间插入的单个卫星延迟模拟器。延迟模拟器由容纳多个通道的卫星延迟电路和每个连接到延迟电路的输出或输入的时钟匹配电路实现，由此通信终端经由时钟匹配电路可分别连接到延迟电路。通过这种配置，设备通过对同时在独立时钟上运行的所有通信终端应用卫星延迟仿真并通过使用单个卫星延迟模拟器来对系统进行测试。

6. 发明授权

US08710198B2 Caprazene as a novel compound and derivatives thereof, and caprazol as a novel compound and derivatives thereof 有权
标题翻译： Caprazene作为新化合物及其衍生物，以及作为新化合物及其衍生物的螯合物
公开(公告)号：US08710198B2
公开(公告)日：2014-04-29
申请号：US12345190
申请日：2008-12-29
申请人： Toshiaki Miyake , Masayuki Igarashi , Tetsuo Shitara , Yoshiaki Takahashi , Masa Hamada
发明人： Toshiaki Miyake , Masayuki Igarashi , Tetsuo Shitara , Yoshiaki Takahashi , Masa Hamada
IPC分类号： C07H19/067 , C07D403/08 , C07D403/14 , C07D243/08 , C07D405/14
CPC分类号： C07H19/067 , A61K31/7072 , C07D403/08 , C07D403/14 , C07D405/14 , C07H15/26 , C07H19/06 , Y02P20/55
摘要： Caprazene is provided which is the compound represented by the following formula (I) wherein Me stands for methyl group, and a 5″-N-alkoxycarbonyl or 5″-N-aralkyloxycarbonyl derivative thereof, and wherein said compound has the 1H-NMR and 13C-NMR data as set forth in Table 15.
摘要翻译：提供了作为Me表示甲基的下式（I）表示的化合物和5“-N-烷氧基羰基或5”-N-芳烷氧基羰基衍生物的化合物，其中所述化合物具有1H-NMR和 13C-NMR数据如表15所示。

7. 发明授权

US08507453B2 Anti-penicillin resistant pneumococci agent and novel 16-membered macrolide derivative 失效
标题翻译：抗青霉素抗性肺炎球菌剂和新型16-元大环内酯衍生物
公开(公告)号：US08507453B2
公开(公告)日：2013-08-13
申请号：US13241967
申请日：2011-09-23
申请人： Toshiaki Miyake , Yoshiaki Takahashi
发明人： Toshiaki Miyake , Yoshiaki Takahashi
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： A61K31/7048 , C07H17/08
摘要： A novel compound that has antimicrobial activity against penicillin-resistant Streptococcus pneumoniae, and an anti-penicillin resistant pneumococci agent that includes the compound as an active ingredient are provided. Thus, an anti-penicillin resistant pneumococci agent is provided that includes as an active ingredient a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof, or hydrates thereof: wherein, in the formula (I), R represents any one of a halogen atom, an azido group, Ra-Wa-, Rb-Wb-, Rc-Wc-, and RdRd′N—.
摘要翻译：提供了对青霉素耐药性肺炎链球菌具有抗微生物活性的新型化合物和包含该化合物作为活性成分的抗青霉素抗性肺炎球菌剂。因此，提供了抗青霉素抗性肺炎球菌剂，其包含作为活性成分的下式（I）表示的化合物或其药理学可接受的盐或其水合物：其中，在式（I）中，R表示任何卤素原子，叠氮基，Ra-Wa-，Rb-Wb-，Rc-Wc-和RdRd'N-之一。

8. 发明申请

US20060178319A1 Caprazene as novel compound and derivatives thereof, and caprazol as novel compound and derivatives thereof 有权
标题翻译：作为新化合物及其衍生物，并且作为新化合物及其衍生物的螯合物，
公开(公告)号：US20060178319A1
公开(公告)日：2006-08-10
申请号：US10543887
申请日：2004-01-30
申请人： Toshiaki Miyake , Masayuki Igarashi , Tetsuo Shitara , Yoshiaki Takahashi , Masa Hamada
发明人： Toshiaki Miyake , Masayuki Igarashi , Tetsuo Shitara , Yoshiaki Takahashi , Masa Hamada
IPC分类号： A61K31/7072 , C07H19/048
CPC分类号： C07H19/067 , A61K31/7072 , C07D403/08 , C07D403/14 , C07D405/14 , C07H15/26 , C07H19/06 , Y02P20/55
摘要： Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1′″- amide derivative of the formula (II) and a caprazene-1′″-ester derivative of the formula (III) from caprazene. Further, there could be synthesized a caprazol-1′″-amide derivative of the formula (V) and a caprazol-1′″-amide-3′″-ester derivative and a caprazol-3′″-ester derivative, etc. from caprazol. Furthermore, an imidazolidinone derivative could be synthesized from the ring-opened product of the 1,4-diazepinone ring of caprazol. The novel caprazene derivative, novel caprazol derivative and novel imidazolidinone derivative now synthesized exhibit excellent antibacterial activities against a variety of bacteria, including acid-fast bacteria.
摘要翻译： Caprazene和caprazol可以通过caprazamycin的水解合成。可以从癸腈合成式（II）的癸酰肼衍生物和式（III）的癸酰基-1“ - 酯衍生物。此外，可以合成式（V）的十六唑-1“ - 酰胺衍生物和十六唑-1” - 酰胺-3“ - 酯衍生物和癸酰唑-3' - 酯衍生物衍生物等。此外，咪唑啉酮衍生物可以由四唑的1,4-二氮杂环酮环的开环产物合成。现在合成的新型caprazene衍生物，新型吡唑衍生物和新型咪唑啉酮衍生物对各种细菌，包括耐酸细菌表现出优异的抗菌活性。

9. 发明授权

US08541394B2 Aminoglycoside antibiotics 有权
标题翻译：氨基糖苷类抗生素
公开(公告)号：US08541394B2
公开(公告)日：2013-09-24
申请号：US13413979
申请日：2012-03-07
申请人： Yoshihiko Kobayashi , Yoshihisa Akiyama , Takeshi Murakami , Nobuto Minowa , Masaki Tsushima , Yukiko Hiraiwa , Shoichi Murakami , Mitsuhiro Abe , Kazushige Sasaki , Shigeru Hoshiko , Toshiaki Miyake , Yoshiaki Takahashi , Daishiro Ikeda
发明人： Yoshihiko Kobayashi , Yoshihisa Akiyama , Takeshi Murakami , Nobuto Minowa , Masaki Tsushima , Yukiko Hiraiwa , Shoichi Murakami , Mitsuhiro Abe , Kazushige Sasaki , Shigeru Hoshiko , Toshiaki Miyake , Yoshiaki Takahashi , Daishiro Ikeda
IPC分类号： A61K31/702 , A61P31/04
CPC分类号： C07H15/234 , C07H15/224
摘要： This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.
摘要翻译：本发明涉及对细菌具有强力抗微生物活性的新型氨基糖苷类抗生素，其诱导感染性疾病，特别是MRSA，并且没有明显的肾毒性，以及生产它们的方法。更具体地，本发明涉及由式（Ia）表示的化合物或其药理学上可接受的盐或溶剂合物或其非对映体混合物，包含它们的抗微生物剂及其制备方法。

10. 发明申请

US20120015896A1 Anti-Penicillin Resistant Pneumococci Agent and Novel 16-Membered Macrolide Derivative 失效
标题翻译：抗青霉素抗性肺炎球菌剂和新型16-大环内酯衍生物
公开(公告)号：US20120015896A1
公开(公告)日：2012-01-19
申请号：US13241967
申请日：2011-09-23
申请人： Toshiaki Miyake , Yoshiaki Takahashi
发明人： Toshiaki Miyake , Yoshiaki Takahashi
IPC分类号： A61K31/7048 , A61P31/04
CPC分类号： A61K31/7048 , C07H17/08
摘要： A novel compound that has antimicrobial activity against penicillin-resistant Streptococcus pneumoniae, and an anti-penicillin resistant pneumococci agent that includes the compound as an active ingredient are provided. Thus, an anti-penicillin resistant pneumococci agent is provided that includes as an active ingredient a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof, or hydrates thereof: wherein, in the formula (I), R represents any one of a halogen atom, an azido group, Ra-Wa-, Rb-Wb-, Rc-Wc-, and RdRd′N—.
摘要翻译：提供了对青霉素耐药性肺炎链球菌具有抗微生物活性的新型化合物和包含该化合物作为活性成分的抗青霉素抗性肺炎球菌剂。因此，提供了抗青霉素抗性肺炎球菌剂，其包含作为活性成分的下式（I）表示的化合物或其药理学可接受的盐或其水合物：其中，在式（I）中，R表示任何卤素原子，叠氮基，Ra-Wa-，Rb-Wb-，Rc-Wc-和RdRd'N-之一。

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