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1. 发明授权

US5616600A Griseolic acid compounds and their use as a phosphodiesterase inhibitor 失效
标题翻译：绿藻酸化合物及其作为磷酸二酯酶抑制剂的用途
公开(公告)号：US5616600A
公开(公告)日：1997-04-01
申请号：US437644
申请日：1995-05-09
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 , A61K31/415 , C07D233/02 , C07D233/04
CPC分类号： C07H19/02 , Y02P20/55
摘要： A compound of the formula (I) is provided ##STR1## wherein A represents a group of the formula: ##STR2## R.sup.1 and R.sup.2 are independently hydrogen, halogen or a group of the formula --OR.sup.9 ; R.sup.9 is hydrogen, alkyl, alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl or a hydroxy-protecting group; R.sup.3 and R.sup.4 are independently carbamoyl or carboxy; R.sup.5 and R.sup.6 both represent hydrogen or together represent an extra carbon-carbon bond between the carbon atoms to which they are attached; and Z represents hydrogen or unsubstituted or substituted hydroxy; or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as inhibitors of phosphodiesterases.
摘要翻译：提供式（I）的化合物，其中A表示下式的基团：R 1和R 2独立地是氢，卤素或式-OR 9的基团; R9是氢，烷基，烷基磺酰基，卤代烷基磺酰基，芳基磺酰基或羟基保护基团; R3和R4独立地是氨基甲酰基或羧基; R5和R6都表示氢或一起代表它们所连接的碳原子之间的额外碳 - 碳键; Z表示氢或未取代或取代的羟基; 或其药学上可接受的盐或酯。这些化合物可用作磷酸二酯酶的抑制剂。

2. 发明授权

US5556975A Griseolic acid derivatives 失效
标题翻译：灰黄酸衍生物
公开(公告)号：US5556975A
公开(公告)日：1996-09-17
申请号：US437634
申请日：1995-05-09
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： A compound of the formula (I) is provided ##STR1## wherein A represents a group of the formula: ##STR2## R.sup.1 and R.sup.2 are independently hydrogen, halogen or a group of the formula --OR.sup.9 ; R.sup.3 and R.sup.4 are independently carbamoyl or carboxy; R.sup.5 and R.sup.a both represent hydrogen or together represent an extra carbon-carbon bond between the carbon atoms to which they are attached; and R.sup.9 is hydrogen, alkyl, alkysulfonyl, haloalkylsulfonyl, arylsulfonyl or a hydroxy-protecting group; or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as inhibitors of phosphodiesterases.
摘要翻译：提供式（I）的化合物，其中A表示下式的基团：R 1和R 2独立地是氢，卤素或式-OR 9的基团; R3和R4独立地是氨基甲酰基或羧基; R5和Ra都表示氢或一起代表它们所连接的碳原子之间的额外碳 - 碳键; 且R 9为氢，烷基，烷磺酰基，卤代烷基磺酰基，芳基磺酰基或羟基保护基团; 或其药学上可接受的盐或酯。这些化合物可用作磷酸二酯酶的抑制剂。

3. 发明授权

US4634706A Griseolic acid derivatives, and their use as enzyme inhibitors 失效
标题翻译：绿藻酸衍生物及其作为酶抑制剂的用途
公开(公告)号：US4634706A
公开(公告)日：1987-01-06
申请号：US664866
申请日：1984-10-25
申请人： Masakatsu Kaneko , Misako Kimura , Yoshinobu Murofushi , Mitsuo Yamazaki , Nobuyoshi Iwata , Fumio Nakagawa
发明人： Masakatsu Kaneko , Misako Kimura , Yoshinobu Murofushi , Mitsuo Yamazaki , Nobuyoshi Iwata , Fumio Nakagawa
IPC分类号： C07H19/16 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P5/12 , A61P7/02 , A61P25/28 , A61P35/00 , A61P43/00 , C07D307/77 , C07D405/06 , C07D473/00 , C07D473/30 , C07D493/04 , C07H19/02 , A61K31/52 , C07D473/34 , C07D473/38 , C07D473/40
CPC分类号： C07H19/02
摘要： Griseolic acid derivatives of formula (I): ##STR1## wherein A represents: ##STR2## have enzyme-inhibitory activity, especially against cAMP PDE and cGMP PDE. When formulated as compositions with appropriate carriers or diluents, they may be used for the treatment of a variety of organic disorders and show toxicities less than griseolic acid itself.
摘要翻译：式（I）的格列酚酸衍生物：其中A表示：具有酶抑制活性，特别是针对cAMP PDE和cGMP PDE。当配制成具有适当载体或稀释剂的组合物时，它们可用于治疗各种有机疾病，并且显示低于griseolic acid本身的毒性。

4. 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。

5. 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。

6. 发明授权

US5760042A Griseolic acid derivatives, their preparation and their use 失效
公开(公告)号：US5760042A
公开(公告)日：1998-06-02
申请号：US319413
申请日：1994-10-06
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 , A61K31/52 , C07D473/04 , C07D473/16 , C07D473/18
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.

7. 发明授权

US5532369A Intermediates for griseolic acid derivatives 失效
标题翻译：绿藻酸衍生物的中间体
公开(公告)号：US5532369A
公开(公告)日：1996-07-02
申请号：US437632
申请日：1995-05-09
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 , C07D473/00 , A61K31/52
CPC分类号： C07H19/02 , Y02P20/55
摘要： A compound of the formula (I) is provided ##STR1## wherein A represents a group of the formula: ##STR2## R.sup.1 and R.sup.2 are independently hydrogen, halogen or a group of the formula --OR.sup.9 ; R.sup.9 is hydrogen, alkyl, alkylsulfonyl, haloalkylsulfonyl, arylsulfonyl or a hydroxy-protecting group; R.sup.3 and R.sup.4 are independently carbamoyl or carboxy; R.sup.5 and R.sup.6 both represent hydrogen or together represent an extra carbon-carbon bond between the carbon atoms to which they are attached; and W represents an alkoxy or aralkoxy; or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as inhibitors of phosphodiesterases.
摘要翻译：提供式（I）的化合物，其中A表示下式的基团：R 1和R 2独立地是氢，卤素或式-OR 9的基团; R9是氢，烷基，烷基磺酰基，卤代烷基磺酰基，芳基磺酰基或羟基保护基团; R3和R4独立地是氨基甲酰基或羧基; R5和R6都表示氢或一起代表它们所连接的碳原子之间的额外碳 - 碳键; W表示烷氧基或芳烷氧基; 或其药学上可接受的盐或酯。这些化合物可用作磷酸二酯酶的抑制剂。

8. 发明授权

US07157442B2 Antibacterial compound 有权
标题翻译：抗菌化合物
公开(公告)号：US07157442B2
公开(公告)日：2007-01-02
申请号：US10080191
申请日：2002-02-19
申请人： Hitoshi Hotoda , Masakatsu Kaneko , Masatoshi Inukai , Yasunori Muramatsu , Yukio Utsui , Satoshi Ohya
发明人： Hitoshi Hotoda , Masakatsu Kaneko , Masatoshi Inukai , Yasunori Muramatsu , Yukio Utsui , Satoshi Ohya
IPC分类号： A61K31/70 , A61K31/553 , A61K31/504 , C07D239/02 , C07D401/00
CPC分类号： C07H19/06
摘要： The present invention relates to a compound of formula (I) (wherein R1 and R2 represent an aryl group, a heterocyclic group, an alkyl group, an alkenyl group and the like which are optionally substituted, R3 represents a hydrogen atom or a hydroxyl group, and X1 and X2 represent an oxygen atom or a sulfur atom, or a nitrogen atom which may be substituted), a pharmaceutically acceptable derivative thereof or a salt thereof.The present invention also relates to a pharmaceutical composition comprising a compound described above as an active ingredient for the prevention or treatment of bacterial infections.The present invention includes the use of a compound described above in order to prepare a medicament effective in the prevention or treatment of bacterial infections.The present invention is concerned with a method for the prevention or treatment of bacterial infections in warm-blooded animals comprising administering a pharmacologically effective amount of a compound described above to them
摘要翻译：本发明涉及式（I）化合物（其中R 1和R 2表示芳基，杂环基，烷基，烯基和任选被取代的R 3表示氢原子或羟基，X 1和X 2表示氧原子或硫原子或可被取代的氮原子），其药学上可接受的衍生物或其盐。本发明还涉及包含上述化合物作为预防或治疗细菌感染的活性成分的药物组合物。本发明包括使用上述化合物以制备有效预防或治疗细菌感染的药物。本发明涉及一种预防或治疗温血动物细菌感染的方法，其包括将药理学有效量的上述化合物给予它们

9. 发明授权

US5341458A Method of and system for generating teaching data for robots 失效
标题翻译：用于生成机器人教学数据的方法和系统
公开(公告)号：US5341458A
公开(公告)日：1994-08-23
申请号：US942983
申请日：1992-09-10
申请人： Masakatsu Kaneko , Hidetaka Nosse , Katsumi Takeishi
发明人： Masakatsu Kaneko , Hidetaka Nosse , Katsumi Takeishi
IPC分类号： B25J9/18 , G05B19/425 , G06F15/46 , G05B17/00
CPC分类号： G05B19/425
摘要： In a method and system for generating teaching data for robots, a plurality of virtual target points are disposed in the vicinity of each of target points allowable on design, where a tool center point of a robot is to be positioned. The virtual target points and the original target point are combined into "target points taken in a broad sense". Each of the target points taken in the broad sense is given as a point which has been confirmed as a tool-attainable point on an off-line teaching apparatus. When a necessary correction is made on-line to teaching data generated by the off-line teaching apparatus, including as data the target points taken in the broad sense, an operator can select a suitable point from the target points taken in the broad sense and carry out a process of correcting the teaching data, regarding the suitable point as being a starting point.
摘要翻译：在用于生成机器人的教学数据的方法和系统中，将多个虚拟目标点设置在设计中允许的每个目标点附近，其中机器人的工具中心点将被定位。虚拟目标点和原始目标点被组合成“广义意义上的目标点”。给出了广义意义上的每个目标点作为在离线教学装置上被确认为可达到工具点的点。当在线地进行对由离线教学装置生成的数据进行必要的校正时，包括作为数据的广义意义上的目标点，操作者可以从广义的目标点中选择合适的点，执行校正教学数据的过程，将适合的点作为起点。

10. 发明授权

US07110859B2 Setting method and setting apparatus for operation path for articulated robot 有权
标题翻译：铰接式机器人操作路径的设置方法和设定装置
公开(公告)号：US07110859B2
公开(公告)日：2006-09-19
申请号：US10468365
申请日：2001-11-22
申请人： Kaoru Shibata , Ryo Nakajima , Masakatsu Kaneko
发明人： Kaoru Shibata , Ryo Nakajima , Masakatsu Kaneko
IPC分类号： G06F19/00
CPC分类号： B25J9/1666 , B23K11/11 , G05B2219/39094 , G05B2219/45104
摘要： A temporary operation path is set by connecting a plurality of welding points in a virtual space generated by a computer to investigate whether an end effector can be operated along the temporary operation path. If the operation cannot be operated, a path to avoid interference with a workpiece is set automatically while extracting a portion in which the workpiece exists in the internal space surrounded by the end effector in order to set a narrow-area operation path for withdrawing the end effector from a welding point. Next, in order to set a wide-area operation path for making movement between withdrawing points, a template operation is applied, in which the end effector is moved by a prescribed distance in a prescribed direction.
摘要翻译：通过将由计算机生成的虚拟空间中的多个焊接点连接起来来调查末端执行器是否可以沿着临时操作路径操作来设置临时操作路径。如果无法操作操作，则自动设置避免工件干涉的路径，同时在由端部执行器包围的内部空间中提取工件的部分提取部分，以便设置用于取出端部的窄区域操作路径效应器从焊接点。接下来，为了设定用于在抽出点之间移动的广域操作路径，应用模板操作，其中端部执行器沿规定方向移动规定距离。

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