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21. 发明申请

US20110003807A1 Thiazole derivatives 有权
标题翻译：噻唑衍生物
公开(公告)号：US20110003807A1
公开(公告)日：2011-01-06
申请号：US12657854
申请日：2010-01-28
申请人： Hiroshi Banno , Masaaki Hirose , Osamu Kurasawa
发明人： Hiroshi Banno , Masaaki Hirose , Osamu Kurasawa
IPC分类号： A61K31/5377 , C07D417/04 , A61K31/4439 , C07D413/14 , C07D471/02 , A61K31/437 , C07D513/04 , A61K31/429 , C07D487/02 , A61K31/5025 , C07D409/14 , A61K31/444 , A61K31/496 , A61P35/00 , A61P29/00 , A61P9/00
CPC分类号： C07D417/14 , A61K9/2059 , C07D417/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to a compound represented by the formula (I) or (I′): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.
摘要翻译：本发明涉及由式（I）或（I'）表示的化合物：其中每个符号如说明书中所定义，或其盐，和含有该化合物或前药的PI3K和（或）mTOR抑制剂其中。

22. 发明申请

US20090137597A1 Novel quinoxalinone derivatives 审中-公开
标题翻译：新型喹喔啉酮衍生物
公开(公告)号：US20090137597A1
公开(公告)日：2009-05-28
申请号：US12081773
申请日：2008-04-21
申请人： Hiroshi Hirai , Nobuhiko Kawanishi , Masaaki Hirose , Tetsuya Sugimoto , Kaori Kamijyo , Jun Shibata , Kouta Masutani
发明人： Hiroshi Hirai , Nobuhiko Kawanishi , Masaaki Hirose , Tetsuya Sugimoto , Kaori Kamijyo , Jun Shibata , Kouta Masutani
IPC分类号： A61K31/4985 , C07D513/22 , A61P35/00
CPC分类号： C07D487/18 , A61K31/4995 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/55 , C07D498/18 , C07D498/22 , C07D515/18 , C07D515/22
摘要： A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, . . . , Bn−1 and Bn, (in which n is 4, 5 or 6) are each independently CH, N or the like; B′1, B′2, . . . , B′n−1 and B′n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like.
摘要翻译：式（I）的喹喔啉酮衍生物或其药学上可接受的盐或酯，其中： X是NH，S等; Y为O等; 部分结构是例如公式：B1，B2，...。。。，Bn-1和Bn（其中n为4,5或6）各自独立地为CH，N等; B'1，B'2，。。。，B'n-1和B'n（其中n为4,5或6）各自独立地为氢等; 和R是氢，低级烷基等。

23. 发明申请

US20070202569A1 Process for producing protein with reduction of acidic sugar chain and glycoprotein produced thereby 有权
标题翻译：生产蛋白质的方法是由此产生的酸性糖链和糖蛋白的还原
公开(公告)号：US20070202569A1
公开(公告)日：2007-08-30
申请号：US11707737
申请日：2007-02-16
申请人： Masami Miura , Masaaki Hirose , Taeko Miwa , Hiroyuki Irie , Shinobu Kuwae , Kenmi Miyano , Wataru Otani , Hideyuki Ohi
发明人： Masami Miura , Masaaki Hirose , Taeko Miwa , Hiroyuki Irie , Shinobu Kuwae , Kenmi Miyano , Wataru Otani , Hideyuki Ohi
IPC分类号： C12P21/06 , C12P19/04 , C12N15/74 , C12N1/21 , C12N1/18
CPC分类号： C12N9/1205 , C12P21/005
摘要： The present invention intends to find out a gene participating in addition of mannose phosphate to a sugar chain of a glycoprotein originating in a yeast belonging to the genus Pichia and provide a means of controlling the same. The present invention also intends to provide a process for producing a protein with reduction of an acidic sugar chain by using the thus controlled yeast strain belonging to the genus Pichia. Namely, the present invention includes a protein participating in the addition of mannose phosphate to a sugar chain of a glycoprotein; a gene coding this protein; a mutant of this gene; a vector carrying the mutant gene; a yeast strain belonging to the genus Pichia having been transformed by this vector; a process for producing a protein with reduction of an acidic sugar chain by using the transformed yeast strain; and a glycoprotein thus produced.
摘要翻译：本发明意图将参与加入甘露糖磷酸酯的基因找到源自属于毕赤酵母属的酵母的糖蛋白的糖链，并提供对其进行控制的方法。本发明还提供通过使用由此控制的属于毕赤酵母属的酵母菌株来制备具有酸性糖链还原性蛋白质的方法。即，本发明包括参与向糖蛋白的糖链添加甘露糖磷酸的蛋白质; 编码该蛋白的基因; 该基因的突变体; 携带突变基因的载体; 已经通过该载体转化了属于毕赤酵母属的酵母菌株; 通过使用转化的酵母菌株来生产具有降低酸性糖链的蛋白质的方法; 和由此产生的糖蛋白。

24. 发明申请

US20120142732A1 HETEROARYLS AND USES THEREOF 有权
标题翻译： HETEROARYLS及其用途
公开(公告)号：US20120142732A1
公开(公告)日：2012-06-07
申请号：US13206671
申请日：2011-08-10
申请人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
发明人： Courtney A. Cullis , Krista E. Granger , Jianping Guo , Masaaki Hirose , Gang Li , Miho Mizutani , Tricia J. Vos
IPC分类号： A61K31/443 , C07D413/14 , A61K31/4439 , C07D413/04 , A61K31/422 , A61K31/444 , C07D405/14 , A61K31/4545 , C07D409/14 , A61P35/00 , A61P29/00 , A61P9/00 , A61P37/08 , A61P7/02 , A61P9/12 , A61P9/04 , C07D405/04
CPC分类号： A61K31/422 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
摘要翻译：本发明提供式IA或IB的化合物：其中HY，R1，R2和G1如说明书中所述。这些化合物是VPS34和/或PI3K的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。

25. 发明申请

US20090004725A1 Process For Producing Protein With Reduction of Acidic Sugar Chain and Glycoprotein Produced Thereby 有权
标题翻译：通过减少酸性糖链和糖蛋白产生蛋白质的方法
公开(公告)号：US20090004725A1
公开(公告)日：2009-01-01
申请号：US12184334
申请日：2008-08-01
申请人： Masami Miura , Masaaki Hirose , Taeko Miwa , Hiroyuki Irie , Shinobu Kuwae , Kenmi Miyano , Wataru Otani , Hideyuki Ohi
发明人： Masami Miura , Masaaki Hirose , Taeko Miwa , Hiroyuki Irie , Shinobu Kuwae , Kenmi Miyano , Wataru Otani , Hideyuki Ohi
IPC分类号： C12N1/19 , C07H21/04 , C12N15/64
CPC分类号： C12N9/1205 , C12P21/005
摘要： The present invention intends to find out a gene participating in addition of mannose phosphate to a sugar chain of a glycoprotein originating in a yeast belonging to the genus Pichia and provide a means of controlling the same. The present invention also intends to provide a process for producing a protein with reduction of an acidic sugar chain by using the thus controlled yeast strain belonging to the genus Pichia. Namely, the present invention includes a protein participating in the addition of mannose phosphate to a sugar chain of a glycoprotein; a gene coding this protein; a mutant of this gene; a vector carrying the mutant gene; a yeast strain belonging to the genus Pichia having been transformed by this vector; a process for producing a protein with reduction of an acidic sugar chain by using the transformed yeast strain; and a glycoprotein thus produced.
摘要翻译：本发明意图将参与加入甘露糖磷酸酯的基因找到源自属于毕赤酵母属的酵母的糖蛋白的糖链，并提供对其进行控制的方法。本发明还提供通过使用由此控制的属于毕赤酵母属的酵母菌株来制备具有酸性糖链还原性蛋白质的方法。即，本发明包括参与向糖蛋白的糖链添加甘露糖磷酸的蛋白质; 编码该蛋白的基因; 该基因的突变体; 携带突变基因的载体; 已经通过该载体转化了属于毕赤酵母属的酵母菌株; 通过使用转化的酵母菌株来生产具有降低酸性糖链的蛋白质的方法; 和由此产生的糖蛋白。

26. 发明授权

US07198921B2 Process for producing protein with reduction of acidic sugar chain and glycoprotein produced thereby 有权
标题翻译：生产蛋白质的方法是由此产生的酸性糖链和糖蛋白的还原
公开(公告)号：US07198921B2
公开(公告)日：2007-04-03
申请号：US10276075
申请日：2001-05-16
申请人： Masami Miura , Masaaki Hirose , Taeko Miwa , Hiroyuki Irie , Shinobu Kuwae , Kenmi Miyano , Wataru Otani , Hideyuki Ohi
发明人： Masami Miura , Masaaki Hirose , Taeko Miwa , Hiroyuki Irie , Shinobu Kuwae , Kenmi Miyano , Wataru Otani , Hideyuki Ohi
IPC分类号： C12P19/04 , C12P21/02 , C12N1/18 , C07H21/04 , C12N14/39
CPC分类号： C12N9/1205 , C12P21/005
摘要： The present invention intends to find out a gene participating in addition of mannose phosphate to a sugar chain of a glycoprotein originating in a yeast belonging to the genus Pichia and provide a means of controlling the same. The present invention also intends to provide a process for producing a protein with reduction of an acidic sugar chain by using the thus controlled yeast strain belonging to the genus Pichia. Namely, the present invention includes a protein participating in the addition of mannose phosphate to a sugar chain of a glycoprotein; a gene encoding this protein; a mutant of this gene; a vector carrying the mutant gene; a yeast strain belonging to the genus Pichia having been transformed by this vector; a process for producing a protein with reduction of an acidic sugar chain by using the transformed yeast strain; and a glycoprotein thus produced.
摘要翻译：本发明意图将参与加入甘露糖磷酸酯的基因找到源自属于毕赤酵母属的酵母的糖蛋白的糖链，并提供对其进行控制的方法。本发明还提供通过使用由此控制的属于毕赤酵母属的酵母菌株来制备具有酸性糖链还原性蛋白质的方法。即，本发明包括参与向糖蛋白的糖链添加甘露糖磷酸的蛋白质; 编码该蛋白的基因; 该基因的突变体; 携带突变基因的载体; 已经通过该载体转化了属于毕赤酵母属的酵母菌株; 通过使用转化的酵母菌株来生产具有降低酸性糖链的蛋白质的方法; 和由此产生的糖蛋白。

27. 发明授权

US06838465B2 N-acyltetrahydroisoquinoline derivatives 失效
标题翻译： N-酰基四氢异喹啉衍生物
公开(公告)号：US06838465B2
公开(公告)日：2005-01-04
申请号：US10275712
申请日：2001-04-27
申请人： Koji Yamada , Masaaki Hirose , Hisashi Iwaasa
发明人： Koji Yamada , Masaaki Hirose , Hisashi Iwaasa
IPC分类号： A61K31/472 , A61K31/4725 , A61K31/506 , A61P3/04 , A61P25/20 , A61P43/00 , C07D217/06 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： C07D401/12 , A61K31/472 , A61K31/4725 , A61K31/506 , C07D217/06 , C07D405/12 , C07D409/12 , C07D417/12
摘要： This invention relates to novel compounds represented by the general formula [I]: (wherein, R1 and R4 are the same or different, and represent hydrogen atoms, lower alkyl groups or the like; R2 and R3 are the same or different, and represent lower alkoxy groups or lower alkyl groups; R5 represents a lower alkyl group or aralkyl group optionally having substituent(s); R6 represents a hydrogen atom or a lower alkyl group; X represents O, S or NH; m represents an integer of 0 to 3; n represents an integer of 0 or 1; and Ar represents a phenyl group or heteroaryl group optionally having substituent(s)). The compounds of the invention have an antagonistic action on orexin receptors, and are useful for treatment of appetite abnormality, obesity, sleeping disorder or the like.
摘要翻译：本发明涉及由通式[I]表示的新化合物:(其中R 1和R 4相同或不同，表示氢原子，低级烷基等; R 2和 R 3相同或不同，表示低级烷氧基或低级烷基; R 5表示任选具有取代基的低级烷基或芳烷基; R 6表示氢原子或低级烷基烷基; X表示O，S或NH; m表示0至3的整数; n表示0或1的整数; Ar表示任选具有取代基的苯基或杂芳基）本发明对食欲肽受体具有拮抗作用，可用于治疗食欲异常，肥胖，睡眠障碍等。

28. 发明授权

US06717386B1 Electric power supply system 有权
标题翻译：电力供应系统
公开(公告)号：US06717386B1
公开(公告)日：2004-04-06
申请号：US09577010
申请日：2000-05-24
申请人： Katsumi Kanasugi , Atsushi Kurauchi , Masaaki Hirose
发明人： Katsumi Kanasugi , Atsushi Kurauchi , Masaaki Hirose
IPC分类号： H02H706
CPC分类号： H02M7/217 , B60R16/03 , G05F1/66 , H02J7/1492 , Y02T10/92
摘要： A rectifying section 2, and a DCDC converter 3 which lowers an input DC voltage and then outputs the voltage are disposed between an AC generator 1 and a load 4. When the output voltage Vt of the AC generator 1 is gradually lowered with starting from E0, the output power P is increased, and is maximum at Vt=V12. When the output voltage Vt is further lowered, the output power P is reduced. As an operating point at which the same output power P is obtained, there are a point of Vt=V11, and that of Vt=V13. The operation of the DCDC converter 3 is controlled so as to operate at the point of Vt=V13 where the output current I is lower.
摘要翻译：整流部分2和降低输入直流电压然后输出电压的DCDC转换器3设置在AC发电机1和负载4之间。当AC发电机1的输出电压Vt从E0开始逐渐降低时，输出功率P增加，并且在Vt = V12时最大。当输出电压Vt进一步降低时，输出功率P减小。作为获得相同输出功率P的工作点，存在Vt = V11，Vt = V13的点。控制DCDC转换器3的操作，以便在输出电流I较低的Vt = V13的点处工作。

29. 发明授权

US5416798A Device for measuring the average value of pulse signals 失效
标题翻译：用于测量脉冲信号平均值的装置
公开(公告)号：US5416798A
公开(公告)日：1995-05-16
申请号：US965272
申请日：1993-08-20
申请人： Masaaki Hirose , Kazuo Katoh , Yutaka Ueki , Yohei Hirakoso , Mitsunori Satoh , Takashi Kosuge
发明人： Masaaki Hirose , Kazuo Katoh , Yutaka Ueki , Yohei Hirakoso , Mitsunori Satoh , Takashi Kosuge
IPC分类号： G01R19/00 , G01R29/08 , G01R29/26 , H04B3/46 , H04B17/00
CPC分类号： G01R19/003 , G01R29/0892 , G01R29/26
摘要： The device of the present invention is used to measure the intensity of a disturbing wave and measures an average value of impulsive noise. The invention permits accurate and short-time measurements. Impulsive noise, which is input via a variable attenuator, a frequency converter, an intermediate-frequency amplifier and a band-pass filter of a 9 or 120 kHz pass frequency, is provided to a linear detector. The detected output is applied to a low-pass filter which is composed of CR elements and whose cut-off frequency is tens of kilohertz. By the low-pass filter, the peak value of the detected output is lowered and its width is increased. The filter output is converted by an A-D converter to a digital signal. Digital values at respective sample points in the digital signal of one frame are added by an arithmetic circuit, and the added value is divided by the number of samples to obtain an average value, which is displayed.
摘要翻译： PCT No.PCT / JP92 / 00677 Sec。 371日期：1993年8月20日 102（e）日期1993年8月20日PCT提交1992年5月26日PCT公布。第WO92 / 21984号公报日本1992年12月10日。本发明的装置用于测量干扰波的强度并测量脉冲噪声的平均值。本发明允许精确和短时间的测量。通过可变衰减器，频率转换器，中频放大器和9或120kHz通过频率的带通滤波器输入的脉冲噪声被提供给线性检测器。检测到的输出被施加到由CR元件组成并且截止频率为几十赫兹的低通滤波器。通过低通滤波器，检测输出的峰值降低，其宽度增加。滤波器输出由A-D转换器转换为数字信号。通过算术电路将一帧的数字信号中的各采样点的数字值相加，并将该相加值除以采样数，得到显示的平均值。

30. 发明授权

US5098840A Human prourokinase mutants 失效
标题翻译：人类prourokinase突变体
公开(公告)号：US5098840A
公开(公告)日：1992-03-24
申请号：US525011
申请日：1990-05-18
申请人： Shunji Kasai , Ryuji Hiramatsu , Shusei Uno , Masanori Nagai , Hirofumi Arimura , Toshizumi Tanabe , Yasuo Amatsuji , Masaaki Hirose , Masanori Morita , Haruhide Kawabe
发明人： Shunji Kasai , Ryuji Hiramatsu , Shusei Uno , Masanori Nagai , Hirofumi Arimura , Toshizumi Tanabe , Yasuo Amatsuji , Masaaki Hirose , Masanori Morita , Haruhide Kawabe
IPC分类号： A61K38/00 , C12N9/72 , C12N15/58
CPC分类号： C12N9/6462 , C12Y304/21073 , A61K38/00
摘要： A human prourokinase mutant in which the entire or a partial epidermal growth factor domain of human prourokinase is deleted or a partial epidermal growth factor domain of human prourokinase is replaced by one or more different amino acid residues, said mutant having a longer blood half-life than naturally occurring human prourokinase while retaining prourokinase enzymatic activity. In this human prourokinase mutant the region selected from the group consisting of: (a) from asparagine (10) to cysteine (42); (b) from asparagine (10) to aspartic acid (45); and (c) from asparagine (10) to threonine (49) is missing.
摘要翻译：其中缺少人原尿激酶的全部或部分表皮生长因子结构域的人prourokinase突变体或人原尿激酶的部分表皮生长因子结构域被一个或多个不同的氨基酸残基替代，所述突变体具有较长的血液半衰期而不是天然存在的人类prourokinase，同时保留prourokinase酶活性。在该人类prourokinase突变体中，选自：（a）天冬酰胺（10）至半胱氨酸（42）的区域; （b）从天冬酰胺（10）到天冬氨酸（45）; 和（c）从天冬酰胺（10）到苏氨酸（49）缺失。

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