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1. 发明授权

US4873225A 1-n-(4-amino-3-fluoro-2-hydroxybutyryl)-kanamycins 失效
标题翻译： 1-正（4-氨基-3-氟-2-羟基丁酰） - 卡那霉素
公开(公告)号：US4873225A
公开(公告)日：1989-10-10
申请号：US158628
申请日：1988-02-22
申请人： Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Kazuo Umezawa , Yoshiaki Takahashi , Tetsuo Shitara , Yoshihiko Kobayashi , Yasushi Takagi
发明人： Sumio Umezawa , Tsutomu Tsuchiya , Tomio Takeuchi , Kazuo Umezawa , Yoshiaki Takahashi , Tetsuo Shitara , Yoshihiko Kobayashi , Yasushi Takagi
IPC分类号： C07H15/234 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/236
CPC分类号： C07H15/234
摘要： As new compound are now provided ten compounds, namely 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}kanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-2',3'-dideoxykanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-2',3'-dideoxy-2'-fluorokanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin A; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-kanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-3'-deoxykanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-3',4'-dideoxykanamycin B; 1-N-{(2R,3R) -4-amino-3-fluoro-2-hydroxybutyryl}-5-deoxy-5-fluorokanamycin B; 1-N-{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5,3'-dideoxy-5-fluorokanamycin B; and 1-N{(2R,3R)-4-amino-3-fluoro-2-hydroxybutyryl}-5,3',4'-trideoxy-5-fluorokanamycin B, which are all useful as antibacterial agent in the therapeutic treatment of bacterial infections.

2. 发明授权

US5831072A Process for the preparation of 2'-deoxy-2'-halocoformycins or steroisomers thereof 失效
标题翻译：制备2'-脱氧-2'-卤代环霉素或其立体异构体的方法
公开(公告)号：US5831072A
公开(公告)日：1998-11-03
申请号：US808033
申请日：1997-03-04
申请人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
发明人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
IPC分类号： C07D487/04 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61P35/00 , A61P35/02 , A61P43/00 , C07H19/04 , C07H19/052 , C07H19/23
CPC分类号： C07H19/052 , C07H19/23
摘要： An object of this invention is to provide a novel process for the synthesis of a 2'-deoxy-2'-halocoformycin having an inhibitory activity against adenosine deaminase in a practically high yield. Thus, there is provided a process comprising multi-stage reactions with using as the starting intermediate a tert-butyl 1-(3,5-di-O-acyl-2-deoxy-2-halo-.beta.-D-ribofuranosyl or arabinofuranosyl)-5-aminoimidazole-4-carboxylate of formula (II) ##STR1## whereby there are produced a 2'-deoxy-2'-halocoformycin or a 2'-deoxy-2'-epi-2'-halocoformycin of formula (I-a) ##STR2## and also a 2'-deoxy-8-epi-2'-halocoformycin or a 2'-deoxy-8,2'-diepi-2'-halocoformycin of formula (I-b) ##STR3## It is expectable that a 2'-deoxy-2'-halocoformycin and epimers thereof are useful as a drug for lymphocytic leukemias and as drugs for various diseases attributable to the actions of adenosine deaminase.
摘要翻译：本发明的目的是提供一种以实际高产率合成具有抑制腺苷脱氨酶活性的2'-脱氧-2'-卤代霉素的新方法。因此，提供一种包含多级反应的方法，其用作起始中间体是1-（3,5-二-O-酰基-2-脱氧-2-卤代-β-呋喃核糖基或阿拉伯呋喃糖基））式（II）的5-氨基咪唑-4-羧酸甲酯（II），由此制备2'-脱氧-2'-卤代霉素或2'-脱氧-2'-表 - 2'-卤代霉素的式（Ia）化合物（Ia）以及式（Ib）的2'-脱氧-8-表 - 2'-卤代霉素或2'-脱氧-8,2'-二哌啶-2'-卤代霉素，（Ib）预期2'-脱氧-2'-卤代霉素及其差向异构体可用作淋巴细胞性白血病药物和作为可归因于腺苷脱氨酶作用的各种疾病的药物。

3. 发明授权

US5886167A 2'-deoxy-2'-epi-2'-fluorocoformycin 失效
标题翻译： 2'-脱氧-2'-表2-fluorocoformycin
公开(公告)号：US5886167A
公开(公告)日：1999-03-23
申请号：US990461
申请日：1997-12-15
申请人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
发明人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
IPC分类号： C07H19/04 , C07H19/052 , C07H19/16
CPC分类号： C07H19/04 , C07H19/052
摘要： 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.
摘要翻译： 2'-脱氧-2'-氟霉素和2'-脱氧-8-表2-fluorocoformycin在本发明中通过多步法通过3,5-二-O-苯甲酰基-2-脱氧-2 - 氟-α-和-β-D-呋喃核糖基溴。此外，根据本发明，通过多阶段方法从3制备2'-脱氧-2'-表2-fluorocoformycin和2'-脱氧-8,2'-二哌啶-2'-氟霉素， 5-二-O-苯甲酰基-2-脱氧-2-氟-α-D-阿拉伯呋喃糖基溴。这四种共转霉素的2'-氟衍生物是新型化合物，对腺苷脱氨酶具有较高的酶抑制活性。特别地，这些新化合物是由于上述高酶抑制活性而对急性淋巴细胞性白血病具有治疗作用的有用物质。此外，作为可用于合成上述新型共转霉素2'-氟衍生物的新型化合物，可获得多种中间体。

4. 发明授权

US5773607A Processes for preparing 2'-deoxy-2'-fluorocoformycin and stereoisomers thereof 失效
标题翻译：制备2'-脱氧-2'-氟霉素的方法及其立体异构体
公开(公告)号：US5773607A
公开(公告)日：1998-06-30
申请号：US620396
申请日：1996-03-22
申请人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
发明人： Tomio Takeuchi , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
IPC分类号： C07H19/04 , C07H19/052 , C07H1/00 , C07H19/00
CPC分类号： C07H19/04 , C07H19/052
摘要： 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.
摘要翻译： 2'-脱氧-2'-氟霉素和2'-脱氧-8-表2-fluorocoformycin在本发明中通过多步法通过3,5-二-O-苯甲酰基-2-脱氧-2 - 氟-α-和-β-D-呋喃核糖基溴。此外，根据本发明，通过多阶段方法从3制备2'-脱氧-2'-表2-fluorocoformycin和2'-脱氧-8,2'-二哌啶-2'-氟霉素， 5-二-O-苯甲酰基-2-脱氧-2-氟-α-D-阿拉伯呋喃糖基溴。这四种共转霉素的2'-氟衍生物是新型化合物，对腺苷脱氨酶具有较高的酶抑制活性。特别地，这些新化合物是由于上述高酶抑制活性而对急性淋巴细胞性白血病具有治疗作用的有用物质。此外，作为可用于合成上述新型共转霉素2'-氟衍生物的新型化合物，可获得多种中间体。

5. 发明授权

US4661474A 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof 失效
标题翻译： 2'，3'-二脱氧-2'-氟卡那霉素A及其1-N-（α-羟基-ω-氨基烷酰基）衍生物
公开(公告)号：US4661474A
公开(公告)日：1987-04-28
申请号：US807485
申请日：1985-12-10
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
IPC分类号： C07H15/236 , A61K31/71 , C07H15/234
CPC分类号： C07H15/234 , Y02P20/55
摘要： New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryl)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as antibacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-O-protected-2,3,6-trideoxy-2-fluoro-.alpha.-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-O-(2',4',6'-tri-O-protected-3'-N-protected-3'-amino-3'-deoxy-.alpha.-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the resulting condensation product to convert its azido group into an amino group, and removing the remaining amino-protecting and hydroxyl-protecting groups from the reduction product.
摘要翻译：新化合物2'，3'-二脱氧-2'-氟卡那霉素A及其1-N-（α-羟基-ω-氨基烷酰基）衍生物，特别是1-N-（DL-或L-3-氨基-2- 羟基丙酰基） - 和1-N-（L-4-氨基-2-羟基丁酰基）-2'，3'-二脱氧-2'-氟吗啉霉素A，其各自可用作抗菌剂。 2'，3'-二脱氧-2'-氟卡那霉素A通过以下方法制备，该方法包括将6-叠氮基-4-O-保护的2,3,6-三脱氧-2-氟-α-D-吡喃六氟肉豆蔻基溴化物与6-O-（2'，4'，6'-三-O-保护的3'-N-保护的-3'-氨基-3'-脱氧-α-D- D-吡喃葡萄糖基）-1,3-双-N-保护的2-脱氧链霉胺，将所得缩合产物还原，将其叠氮基转化为氨基，并从还原产物中除去剩余的氨基保护基和羟基保护基团。

6. 发明授权

US4634688A 3'-fluoro-3'-deoxykanamycin A 失效
标题翻译： 3'-氟-3'-脱氧卡那霉素A
公开(公告)号：US4634688A
公开(公告)日：1987-01-06
申请号：US758819
申请日：1985-07-25
申请人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
发明人： Hamao Umezawa , Sumio Umezawa , Tsutomu Tsuchiya , Yoshiaki Takahashi
IPC分类号： C07H15/234 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H9/04 , C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , C07H9/04 , Y02P20/55
摘要： A new compound, 3'-fluoro-3'-deoxykanamycin A is now provided, which is active against gram-negative and gram-positive bacteria, including kanamycin-resistant strains of bacteria and is useful as antibacterial agent for therapeutic treatment of bacterial infections. This new compound is produced by a process comprising reacting a 6-azido-2,4-di-O-protected-3,6-dideoxy-3-fluoro-.alpha.-D-glucopyranosyl bromide with the 4-hydroxyl group of a 6-O-(2'-O-protected-3'-N-protected-3'-amino-4',6'-di-O-protected-3'-deoxy-.alpha.-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the azido group of the resulting reaction product into an amino group, and removing the remaining protective groups from the reduction product.
摘要翻译：现在提供了一种新的化合物3'-氟-3'-脱氧卡那霉素A，其对革兰氏阴性和革兰氏阳性细菌具有活性，包括卡那霉素抗性细菌菌株，并且可用作细菌感染的治疗性治疗用抗菌剂。该新化合物通过包括使6-叠氮基-2,4-二-O-保护的3,6-二脱氧-3-氟-α-D-吡喃葡萄糖基溴与6位的4-羟基反应的方法制备 -O-（2'-O-保护的3'-N-保护的3'-氨基-4'，6'-二-O-保护的-3'-脱氧-α-D-吡喃葡萄糖基） 3-双-N-保护的2-脱氧链霉胺，将所得反应产物的叠氮基还原成氨基，并从还原产物中除去剩余的保护基团。

7. 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。

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

US07482439B2 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：US07482439B2
公开(公告)日：2009-01-27
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： A61K31/7008 , A61K31/7016 , A61K31/551 , A61K31/51 , C07H17/02 , C07D243/08
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。

10. 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。

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