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11. 发明授权

US06472384B1 Antimicrobial compounds 有权
标题翻译：抗菌化合物
公开(公告)号：US06472384B1
公开(公告)日：2002-10-29
申请号：US09757393
申请日：2001-01-09
申请人： Masatoshi Inukai , Masakatsu Kaneko , Toshio Takatsu , Hitoshi Hotoda , Masatoshi Arai , Shunichi Miyakoshi , Masaaki Kizuka , Yasumasa Ogawa
发明人： Masatoshi Inukai , Masakatsu Kaneko , Toshio Takatsu , Hitoshi Hotoda , Masatoshi Arai , Shunichi Miyakoshi , Masaaki Kizuka , Yasumasa Ogawa
IPC分类号： A61K31553
CPC分类号： C07H19/06 , C12P17/16 , C12P17/162 , C12P17/167 , C12P19/38 , C12P19/40 , Y02P20/55
摘要： The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections. (wherein R1 is a hydrogen atom or a methyl group; R2a is a hydrogen atom, a protecting group for a hydroxy group, or a methyl group; R3 is a hydrogen atom or a protecting group for a hydroxy group; R4a is a hydrogen atom, a hydroxy group or a protected hydroxy group; R5 is a hydrogen atom or a protecting group for a hydroxy group; and X is a methylene group or a sulfur atom). The invention also includes compounds which are related to the aforeidentified compounds.
摘要翻译：本发明涉及化合物（Ia）的酯，醚和N-烷基氨基甲酰基衍生物及其药学上可接受的盐。这些化合物表现出优异的抗菌活性，可用于治疗或预防细菌感染（其中R1为氢原子或甲基; R2a为氢原子，羟基保护基或甲基; R3 是氢原子或羟基的保护基; R4a是氢原子，羟基或保护的羟基; R5是氢原子或羟基的保护基; X是亚甲基或硫原子）。本发明还包括与前述化合物有关的化合物。

12. 发明授权

US06327518B1 Off-line teaching apparatus 失效
标题翻译：离线教学仪器
公开(公告)号：US06327518B1
公开(公告)日：2001-12-04
申请号：US09659587
申请日：2000-09-11
申请人： Masakatsu Kaneko , Shinji Aoki
发明人： Masakatsu Kaneko , Shinji Aoki
IPC分类号： G06F1900
CPC分类号： G05B19/425 , G05B2219/35499 , G05B2219/36017 , G05B2219/36183 , G05B2219/39396 , G05B2219/40394
摘要： An off-line teaching apparatus includes an operation command-receiving device for receiving an operation command inputted via an input/output port from a key input device or a coordinate input device and successively storing the operation command in a buffer; an operation command-reading device for successively reading the operation command stored in the buffer; an operation command-counting device for counting a number of operation commands stored in the buffer; and a confirmation sound-generating device for generating confirmation sound upon receipt of the operation command by the operation command-receiving device when a counted value obtained by the operation command-counting device is not less than a predetermined number. Accordingly, the operator is informed, in real time, of the fact that the system responds to the input of the operation command from the operator. Thus, it is possible to improve the operability of the off-line teaching.
摘要翻译：离线示教装置包括：操作命令接收装置，用于从键输入装置或坐标输入装置接收经由输入/输出端口输入的操作命令，并将操作命令依次存储在缓冲器中; 操作命令读取装置，用于连续读取存储在缓冲器中的操作命令; 操作命令计数装置，用于对存储在缓冲器中的操作命令的数量进行计数; 以及确认声音产生装置，用于当由所述操作命令计数装置获得的计数值不小于预定数量时，在所述操作命令接收装置接收到所述操作命令时产生确认声音。因此，实时地通知操作者系统响应来自操作者的操作命令的输入。因此，可以提高离线教学的可操作性。

13. 发明授权

US5691319A Pyrimidine nucleoside derivatives having anti-tumor activity, their preparation and use 失效
标题翻译：嘧啶核苷衍生物具有抗肿瘤活性，其制备和用途
公开(公告)号：US5691319A
公开(公告)日：1997-11-25
申请号：US465127
申请日：1995-06-05
申请人： Masakatsu Kaneko , Hitoshi Hotoda , Tomoyuki Shibata , Tomowo Kobayashi , Yoshihiro Mitsuhashi , Akira Matsuda , Takuma Sasaki
发明人： Masakatsu Kaneko , Hitoshi Hotoda , Tomoyuki Shibata , Tomowo Kobayashi , Yoshihiro Mitsuhashi , Akira Matsuda , Takuma Sasaki
IPC分类号： A61K31/505 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61P35/00 , C07D405/04 , C07H19/06 , C07H19/073 , C07H19/09
CPC分类号： C07H19/06 , C07H19/073
摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen atoms, optionally substituted alkanoyl groups and alkenylcarbonyl groups, PROVIDED THAT at least one of R.sup.1, R.sup.2 and R.sup.3 represents an unsubstituted alkanoyl group having from 5 to 24 carbon atoms, said substituted alkanoyl group or said alkenylcarbonyl group; and one of R.sup.4 and R.sup.5 represents a hydrogen atom and the other represents a cyano group; have valuable anti-tumor activity.
摘要翻译：式（I）的化合物：其中：R1，R2和R3独立地选自氢原子，任选取代的烷酰基和烯基羰基，提供了R1，R2和R3中的至少一个表示具有5至24个碳原子的未取代的烷酰基，所述取代的烷酰基或所述烯基羰基; R 4和R 5中的一个表示氢原子，另一个表示氰基; 具有有价值的抗肿瘤活性。

14. 发明授权

US5498819A Griseolic acid derivatives, their preparation and their use 失效
标题翻译：绿藻酸衍生物，其制备及其用途
公开(公告)号：US5498819A
公开(公告)日：1996-03-12
申请号：US130154
申请日：1993-09-30
申请人： Masakatsu Kaneko , Yoshinobu Murofushi , Misako Kimura , Mitsuo Yamazaki , Yasuteru Iijima
发明人： Masakatsu Kaneko , Yoshinobu Murofushi , Misako Kimura , Mitsuo Yamazaki , Yasuteru Iijima
IPC分类号： C07D233/54 , C07H19/02 , C07D473/34 , A61K31/52
CPC分类号： C07H19/02 , Y02P20/55
摘要： New griseolic acid derivatives have various groups attached to the sugar part in place of the adenine group of griseolic acid itself. These groups are all purine derivatives or ring-opened purine analogs. The compounds are useful as inhibitors of phosphodiesterases.
摘要翻译：新的griseolic酸衍生物具有连接到糖部分的各种不同的基团，而不是腺嘌呤酸本身的腺嘌呤基团。这些组都是嘌呤衍生物或开环嘌呤类似物。这些化合物可用作磷酸二酯酶的抑制剂。

15. 发明授权

US4783532A Process for preparing griseolic acid derivatives 失效
标题翻译：姜黄酸衍生物的制备方法
公开(公告)号：US4783532A
公开(公告)日：1988-11-08
申请号：US856586
申请日：1986-04-25
申请人： Masakatsu Kaneko , Misako Kimura , Yoshinobu Murofushi
发明人： Masakatsu Kaneko , Misako Kimura , Yoshinobu Murofushi
IPC分类号： C07H19/02 , C07H19/052 , A61K31/52
CPC分类号： C07H19/02 , C07H19/052
摘要： Griseolic acid and dihydrodesoxygriseolic acid derivatives having an alkyl or aralkyl group as a substituent on the amino group at the 6-position are prepared by reacting the unsubstituted compound with a compound R.sup.7 -X (where R.sup.7 is alkyl or aralkyl and X is halogen or sulfonyloxy). The group first substitutes and quaternizes the 1-nitrogen atom. The compound is then subjected to an appropriate combination of temperature and pH to cause ring cleavage, rearrangement and ring closure involving the 6-amino group and this quaternized 1-nitrogen to give a 6-alkylamino or 6-aralkylamino derivative.
摘要翻译：通过使未取代的化合物与化合物R7-X（其中R7是烷基或芳烷基，X是卤素或磺酰氧基）反应制备在6-位氨基上具有烷基或芳烷基作为取代基的山梨醇酸和二氢脱氧山梨醇酸衍生物）。该组首先将1-氮原子替代并季铵化。然后将化合物进行温度和pH的适当组合以引起涉及6-氨基和该季铵化1-氮的环切割，重排和闭环，得到6-烷基氨基或6-芳烷基氨基衍生物。

16. 发明授权

US4248999A 5-Fluorouracil derivatives and process for preparing thereof 失效
标题翻译： 5-氟尿嘧啶衍生物及其制备方法
公开(公告)号：US4248999A
公开(公告)日：1981-02-03
申请号：US847452
申请日：1977-10-31
申请人： Tsuneo Baba , Masakatsu Kaneko , Bunji Shimizu , Masao Arakawa
发明人： Tsuneo Baba , Masakatsu Kaneko , Bunji Shimizu , Masao Arakawa
IPC分类号： C07H17/02 , A61K31/70
CPC分类号： C07H17/02
摘要： 5-Fluorouracil compounds having a glycoside substituent connected to the 5-fluorouracil nucleus through a bridging oxygen atom; and having anti-tumor activity.
摘要翻译：具有通过桥连氧原子与5-氟尿嘧啶核连接的糖苷取代基的5-氟尿嘧啶化合物; 并具有抗肿瘤活性。

17. 发明授权

US4126745A 7-Methoxycephalosporin derivatives 失效
标题翻译： 7-甲氧基头孢菌素衍生物
公开(公告)号：US4126745A
公开(公告)日：1978-11-21
申请号：US676488
申请日：1976-04-13
申请人： Hideo Nakao , Hiroaki Yanagisawa , Bunji Shimizu , Masakatsu Kaneko , Mitsuo Nagano , Shinichi Sugawara
发明人： Hideo Nakao , Hiroaki Yanagisawa , Bunji Shimizu , Masakatsu Kaneko , Mitsuo Nagano , Shinichi Sugawara
IPC分类号： A61K31/545 , C07D20060101 , C07D205/08 , C07D257/04 , C07D279/04 , C07D501/00 , C07D501/36 , C07D501/40 , C07D501/50 , C07D501/57 , C07D501/60
CPC分类号： C07D501/57 , Y02P20/55
摘要： A compound having the formula ##STR1## wherein Y represents a 2-carboxyethylthio group or a trifluoromethylthio group and a nontoxic pharmaceutically acceptable salt thereof are useful as antibacterial agents. They may be prepared by (a) reacting a compound having the formula ##STR2## wherein X.sub.1 represents a halogen atom with a compound having the formulaY -- Hwherein Y has the same meaning as defined above, or (b) reacting a compound having the formula ##STR3## wherein R represents a protective group for the carboxyl group with a compound having the formulaY -- CH.sub.2 COX.sub.2wherein X.sub.2 represents a halogen atom and Y has the same meaning as defined above and removing the protective group for the carboxyl group from the resulting product, or (c) reacting a compound having the formula ##STR4## wherein A represents an acetoxy group or a carbamoyloxy group and Y has the same meaning as defined above with 5-mercapto-1-methyl-1H-tetrazole or its alkali metal salt.
摘要翻译：具有式“IMAGE”的化合物，其中Y表示2-羧乙硫基或三氟甲硫基，其无毒的药学上可接受的盐可用作抗菌剂。它们可以通过以下方法来制备：（a）使具有式“IMAGE”的化合物（其中X1表示卤素原子）与具有式Y-H的化合物反应，其中Y具有与上述相同的含义，或（b）使具有其中R表示具有式Y-CH 2 COX 2的化合物的羧基保护基，其中X 2表示卤素原子，Y表示与上述相同的含义，并且从该基团除去羧基的保护基团得到的产物，或（c）使具有式“IMAGE”的化合物，其中A表示乙酰氧基或氨基甲酰氧基，Y与上述定义同上，与5-巯基-1-甲基-1H-四唑或其碱金属盐。

18. 发明申请

US20110009471A1 Oligonucleotide analogues and methods utilizing the same 有权
标题翻译：寡核苷酸类似物和利用其的方法
公开(公告)号：US20110009471A1
公开(公告)日：2011-01-13
申请号：US12804500
申请日：2010-07-22
申请人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
发明人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
IPC分类号： A61K31/7088 , A61K31/7084 , A61P29/00 , A61P17/06 , A61P31/18 , A61P31/22 , A61P31/16 , A61P35/00 , C07H21/04 , C12P19/34 , G01N33/50
CPC分类号： C07H19/10 , C07H19/06 , C07H19/16 , C07H19/20 , Y02P20/55 , Y10T436/143333
摘要： A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): wherein A is methylene; and B is an unsubstituted purin-9-yl, an unsubstituted 2-oxo-pyrimidin-1-yl or a substituted purin-9-yl; or a pharmacologically acceptable salt thereof.
摘要翻译：一种用于预防或治疗哺乳动物的疾病，其可通过所述哺乳动物体内的寡核苷酸类似物或其药理学上可接受的盐的药理学上有用的反义或反应活性可预防或治疗的疾病，所述方法包括向需要的所述哺乳动物施用这样的预防或治疗药物有效量的包含两个或多个核苷单位的寡核苷酸类似物，其中所述核苷单元中的至少一个是式（2）的结构：其中A是亚甲基; 和B是未取代的嘌呤-9-基，未取代的2-氧代 - 嘧啶-1-基或取代的嘌呤-9-基; 或其药理学上可接受的盐。

19. 发明授权

US07816333B2 Oligonucleotide analogues and methods utilizing the same 有权
标题翻译：寡核苷酸类似物和利用其的方法
公开(公告)号：US07816333B2
公开(公告)日：2010-10-19
申请号：US11881775
申请日：2007-07-27
申请人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
发明人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： C07H19/10 , C07H19/06 , C07H19/16 , C07H19/20 , Y02P20/55 , Y10T436/143333
摘要： A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): wherein A is methylene; and B is an unsubstituted purin-9-yl, an unsubstituted 2-oxo-pyrimidin-1-yl or a substituted purin-9-yl; or a pharmacologically acceptable salt thereof.
摘要翻译：一种用于预防或治疗哺乳动物的疾病，其可通过所述哺乳动物体内的寡核苷酸类似物或其药理学上可接受的盐的药理学上有用的反义或反应活性可预防或治疗的疾病，所述方法包括向需要的所述哺乳动物施用这样的预防或治疗药物有效量的包含两个或多个核苷单位的寡核苷酸类似物，其中所述核苷单元中的至少一个是式（2）的结构：其中A是亚甲基; 和B是未取代的嘌呤-9-基，未取代的2-氧代 - 嘧啶-1-基或取代的嘌呤-9-基; 或其药理学上可接受的盐。

20. 发明申请

US20090149404A1 Oligonucleotide analogues and methods utilizing the same 有权
标题翻译：寡核苷酸类似物和利用其的方法
公开(公告)号：US20090149404A1
公开(公告)日：2009-06-11
申请号：US11881775
申请日：2007-07-27
申请人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
发明人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
IPC分类号： A61K31/7084 , C12Q1/68 , C07H21/00
CPC分类号： C07H19/10 , C07H19/06 , C07H19/16 , C07H19/20 , Y02P20/55 , Y10T436/143333
摘要： A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): wherein A is methylene; and B is an unsubstituted purin-9-yl, an unsubstituted 2-oxo-pyrimidin-1-yl or a substituted purin-9-yl; or a pharmacologically acceptable salt thereof.
摘要翻译：一种用于预防或治疗哺乳动物的疾病，其可通过所述哺乳动物体内的寡核苷酸类似物或其药理学上可接受的盐的药理学上有用的反义或反应活性可预防或治疗的疾病，所述方法包括向需要的所述哺乳动物施用这样的预防或治疗药物有效量的包含两个或多个核苷单位的寡核苷酸类似物，其中所述核苷单元中的至少一个是式（2）的结构：其中A是亚甲基; 和B是未取代的嘌呤-9-基，未取代的2-氧代 - 嘧啶-1-基或取代的嘌呤-9-基; 或其药理学上可接受的盐。

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