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1. 发明申请

WO2012054510A1 OXADIAZOLE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF 审中-公开
标题翻译：抑制β-分泌酶活性的OXADIAZOLE化合物及其使用方法
公开(公告)号：WO2012054510A1
公开(公告)日：2012-04-26
申请号：PCT/US2011/056747
申请日：2011-10-18
申请人： COMENTIS, INC. , ASTELLAS PHARMA INC. , BILCER, Geoffrey, M. , DEVASAMUDRAM, Thippeswamy , LILLY, John, C. , ANKALA, Sudha, V. , MOSKALEV, Nikolai, V. , LIU, Chunfeng , INOUE, Makoto , KAWAKAMI, Shimpei , MUNAKATA, Ryosuke , HAMAJIMA, Toshihiro
发明人： BILCER, Geoffrey, M. , DEVASAMUDRAM, Thippeswamy , LILLY, John, C. , ANKALA, Sudha, V. , MOSKALEV, Nikolai, V. , LIU, Chunfeng , INOUE, Makoto , KAWAKAMI, Shimpei , MUNAKATA, Ryosuke , HAMAJIMA, Toshihiro
IPC分类号： C07D417/14 , A61K31/427 , C07D413/12 , A61K31/422 , A61K31/4439 , C07D413/14 , A61K31/4245 , A61P25/28
CPC分类号： C07D413/12 , C07D413/14 , C07D417/14
摘要： The invention provides novel beta-secretase inhibitors and methods for their including methods of treating Alzheimer's disease.
摘要翻译：本发明提供新颖的β-分泌酶抑制剂及其包括治疗阿尔茨海默氏病的方法。

2. 发明申请

WO2004051192A3 ROTATION ANGLE DETECTION DEVICE 审中-公开
标题翻译：旋转角度检测装置
公开(公告)号：WO2004051192A3
公开(公告)日：2004-10-21
申请号：PCT/JP0315367
申请日：2003-12-02
申请人： MATSUSHITA ELECTRIC IND CO LTD , INOUE MAKOTO
发明人： INOUE MAKOTO
IPC分类号： G01D5/245 , B62D15/02 , G01D5/04 , G01D5/244 , G01D5/14 , G01D5/16
CPC分类号： G01D5/24461 , B62D15/02 , G01D5/04
摘要： The rotation angle detection device of the present invention contains i) a rotation detecting body; ii) a first rotator engaging with the rotation detecting body; iii) a second rotator engaging with the first rotator; iv) a first detector that detects the rotation angle of the first rotator; v) a second detector that detects the rotation angle of the second rotator; and vi) a self-evaluating section. Referencing to the output range of the first and the second signals detected by the first and the second detectors under the normal condition of the rotation detecting body, the self-evaluating section determines, through calculation of the output range of the signals, the normal condition and the abnormal condition ranges. When at least one of the values of the signals is in the abnormal condition range, the self-evaluating section judges that the rotation detecting body is in an abnormal operation.
摘要翻译：本发明的旋转角度检测装置包括：i）旋转检测体; ii）与旋转检测体接合的第一旋转体; iii）与第一旋转器接合的第二旋转器; iv）检测第一旋转器的旋转角度的第一检测器; v）检测第二旋转器的旋转角度的第二检测器; 和vi）自我评估部分。在旋转检测体的正常状态下，参考由第一和第二检测器检测到的第一和第二信号的输出范围，自我评估部分通过计算信号的输出范围来确定正常状态和异常情况的范围。当至少一个信号值处于异常条件范围内时，自我评估部分判断旋转检测体处于异常操作中。

3. 发明申请

WO1995035298A1 PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE 审中-公开
标题翻译：吡咯并[1,5-a]吡啶衍生物
公开(公告)号：WO1995035298A1
公开(公告)日：1995-12-28
申请号：PCT/JP1995001104
申请日：1995-06-05
申请人： OTSUKA PHARMACEUTICAL FACTORY, INC. , SHOJI, Yasuo , INOUE, Makoto , OKAMURA, Takashi , HASHIMOTO, Kinji , OHARA, Masayuki , YASUDA, Tsuneo
发明人： OTSUKA PHARMACEUTICAL FACTORY, INC.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A pyrazolo[1,5-a]pyrimidine derivative represented by general formula (1) and having such a potent analgesic effect that it is useful as an analgesic, wherein R represents hydrogen, lower alkyl, cycloalkyl, thienyl, furyl, lower alkenyl or phenyl; R represents naphthyl, cycloalkyl, furyl, thienyl, pyridyl, phenoxy or phenyl; R represents hydrogen, phenyl or lower alkyl; R represents hydrogen, lower alkyl, lower alkoxy-carbonyl, phenyl-substituted lower alkyl, phenyl or halogen; R represents hydrogen or lower alkyl; R represents hydrogen, lower alkyl, phenyl-substituted lower alkyl or benzoyl; Q represents carbonyl or sulfonyl; A represents a single bond, lower alkylene or lower alkenylene; and n represents 0 or 1.
摘要翻译：具有通式（1）表示的吡唑并[1,5-a]嘧啶衍生物，具有如此有效的止痛效果，可用作止痛剂，其中R 1表示氢，低级烷基，环烷基，噻吩基，呋喃基，低级烯基或苯基; R 2表示萘基，环烷基，呋喃基，噻吩基，吡啶基，苯氧基或苯基; R 3表示氢，苯基或低级烷基; R 4表示氢，低级烷基，低级烷氧基 - 羰基，苯基取代的低级烷基，苯基或卤素; R 5表示氢或低级烷基; R 6表示氢，低级烷基，苯基取代的低级烷基或苯甲酰基; Q表示羰基或磺酰基; A表示单键，低级亚烷基或低级亚烯基; n表示0或1。

4. 发明申请

WO2006112553A3 HIGHLY SAFE INTRANASALLY ADMINISTRABLE GENE VACCINES FOR TREATING ALZHEIMER'S DISEASE 审中-公开
标题翻译：高度安全的管理基因疫苗治疗阿尔茨海默病
公开(公告)号：WO2006112553A3
公开(公告)日：2007-02-22
申请号：PCT/JP2006308913
申请日：2006-04-20
申请人： DNAVEC CORP , JAPAN GOVERNMENT , HARA HIDEO , TABIRA TAKESHI , YONEMITSU YOSHIKAZU , INOUE MAKOTO , TOKUSUMI YUMIKO , HASEGAWA MAMORU
发明人： HARA HIDEO , TABIRA TAKESHI , YONEMITSU YOSHIKAZU , INOUE MAKOTO , TOKUSUMI YUMIKO , HASEGAWA MAMORU
IPC分类号： C12N15/09
CPC分类号： C12N15/86 , A61K2039/5256 , A61K2039/543 , A61K2039/57 , C07K14/4711 , C12N2760/18843 , C12N2800/30
摘要： An objective of the present invention is to provide a safe and effective vaccine therapy for Alzheimer's disease. A minus strand RNA viral vector carrying amyloid gene was constructed, and administered intranasally to 24- to 25-months-old APP transgenic mice. The level of serum anti-A 42 antibody was determined and showed to be markedly higher than the control. The results of histological investigation showed that the administration of a vector of the present invention markedly reduced senile plaques in all of the frontal lobe, parietal lobe, and hippocampus. The brain A level was also markedly reduced. Furthermore, the administration of a vector of the present invention did not result in lymphocyte infiltration in the central nervous system.
摘要翻译：本发明的目的是为阿尔茨海默病提供安全有效的疫苗疗法。构建携带淀粉样蛋白基因的负链RNA病毒载体，鼻内给予24至25个月大的APP转基因小鼠。测定血清抗-A42抗体水平，显示明显高于对照组。组织学研究结果表明，施用本发明的载体显着降低了所有额叶，顶叶和海马中的老年斑。脑A水平也明显降低。此外，本发明的载体的施用不会导致中枢神经系统中的淋巴细胞浸润。

5. 发明申请

WO2006004191A1 PYRROLOPYRIDAZINE DERIVATIVES WHICH INHIBIT PDE IV AND TNF ALFA 审中-公开
标题翻译：抑制PDE IV和TNF ALFA的吡咯并吡啶衍生物
公开(公告)号：WO2006004191A1
公开(公告)日：2006-01-12
申请号：PCT/JP2005/012622
申请日：2005-07-01
申请人： ASTELLAS PHARMA INC. , ABE, Yoshito , INOUE, Makoto , OKUMURA, Mitsuaki , OHNE, Kazuhiko , SATO, Kentaro
发明人： ABE, Yoshito , INOUE, Makoto , OKUMURA, Mitsuaki , OHNE, Kazuhiko , SATO, Kentaro
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to compound of the formula (I) or its salt, in which R 1 , R 2 , R 3 and R 4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.
摘要翻译：本发明涉及式（I）化合物或其盐，其中R

6. 发明申请

WO2004048899A2 DEVICE AND METHOD OF DETECTING ROTATION ANGLE 审中-公开
标题翻译：检测旋转角度的装置和方法
公开(公告)号：WO2004048899A2
公开(公告)日：2004-06-10
申请号：PCT/JP2003/014872
申请日：2003-11-21
申请人： MATSUSHITA ELECTRIC INDUSTRIAL CO., LTD. , INOUE, Makoto
发明人： INOUE, Makoto
IPC分类号： G01D5/00
CPC分类号： G01D5/24461 , G01D5/04 , G01D5/145
摘要： The rotation-angle detecting device of the present invention contains two rotators having the same number of teeth, which engage with a gear fixed to a rotation-detecting axle as a detected object. The detecting device further includes a controller. Receiving a rotation-angle signal from the rotators, the controller amplifies the signal, performs calculations, and stores the results. The controller converts each rotation-angle signal from each rotator into each periodic waveform output having the same crest value, and stores an initial phase difference value at initial setting. In driving operations, monitoring an evaluation value calculated with reference to the initial phase difference value, the controller determines that abnormalities occurred, if the evaluation value exceeds a predetermined abnormality-evaluation threshold.
摘要翻译：本发明的旋转角度检测装置包括具有相同齿数的两个旋转器，所述两个旋转器与固定到作为检测对象的旋转检测轴的齿轮啮合。该检测装置还包括控制器。从旋转器接收旋转角度信号，控制器放大信号，执行计算并存储结果。控制器将来自每个旋转器的每个旋转角度信号转换为具有相同峰值的每个周期性波形输出，并且在初始设置时存储初始相位差值。在驾驶操作中，监视参考初始相位差值计算的评估值，如果评估值超过预定的异常评估阈值，则控制器确定发生了异常。

7. 发明申请

WO1995018150A1 NOVEL HUMAN CILIARY NEUROTROPHIC FACTOR 审中-公开
标题翻译：新人类神经营养因子
公开(公告)号：WO1995018150A1
公开(公告)日：1995-07-06
申请号：PCT/JP1994002269
申请日：1994-12-27
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED , INOUE, Makoto , KIKUCHI, Kaoru , ISHIGE, Yoko , ITO, Akira , KIMURA, Toru , NAKAYAMA, Chikao , NOGUCHI, Hiroshi
发明人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
IPC分类号： C07K14/475
CPC分类号： C07K14/475
摘要： A modification of a human ciliary neurotrophic factor (human CNTF) wherein the amino acid residue of the amino acid sequence corresponding to at least the 153rd amino acid residue of the amino acid sequence of a natural human CNTF has been replaced by another amino acid residue has an activity equal or superior to that of a natural human CNTF. Hence it is expected as a useful therapeuticc agent reduced in the side effects such as the occurrence of autoantibodies caused by ample administration thereof, body weight decrease, anorexia, dry cough, and boredom. The invention also provides a D1 cap region modification of alpha -helix-rich cytokines analogous to human CNTF, such as GH, PRL, EPC, G-CSF, LIF, IL-6, IL-2, IL-4, and GM-CSF.
摘要翻译：人类睫状神经营养因子（人CNTF）的修饰，其中对应于天然人CNTF的氨基酸序列的至少153个氨基酸残基的氨基酸序列的氨基酸残基已经被另一个氨基酸残基替代，与天然人类CNTF相当或优于其他活性的活性。因此，预期作为减少副作用的有用的治疗剂，例如由其充分施用，体重减轻，厌食，干咳和无聊引起的自身抗体的发生。本发明还提供类似于人CNTF的例如GH，PRL，EPC，G-CSF，LIF，IL-6，IL-2，IL-4和GM-1的富含α-螺旋的细胞因子的D1帽区修饰， CSF。

8. 发明申请

WO1992021764A1 PROCESS FOR PRODUCING ASTAXANTHIN BY FERMENTATION 审中-公开
标题翻译：通过发酵生产阿司匹林的方法
公开(公告)号：WO1992021764A1
公开(公告)日：1992-12-10
申请号：PCT/JP1992000722
申请日：1992-06-04
申请人： KYOWA HAKKO KOGYO CO., LTD. , KUGA, Tetsuro , INOUE, Makoto , IMURA, Toshiaki , AOYAMA, Yoshihide , KURATSU, Yoshiyuki
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C12P07/24
CPC分类号： C12R1/645 , C12P23/00
摘要： A process for producing astaxanthin industrially efficiently at a low cost by culturing a microorganism which belongs to the genus Pfaffia, is resistant to at least one of citronellol, primaquine and hydroxydiphenyl and can produce astaxanthin in a medium.

9. 发明申请

WO1992006096A1 PYRIMIDINE DERIVATIVE, PRODUCTION THEREOF, AND ANDROGEN INHIBITOR 审中-公开
标题翻译：吡嗪衍生物，其生产方法和安定剂抑制剂
公开(公告)号：WO1992006096A1
公开(公告)日：1992-04-16
申请号：PCT/JP1991001367
申请日：1991-10-07
申请人： OTSUKA PHARMACEUTICAL CO., LTD. , KIYOKAWA, Hiroshi , YAMADA, Satoshi , MIYAJIMA, Keisuke , HASHIMOTO, Kinji , INAI, Masatoshi , INOUE, Makoto , TATSUMI, Kunihiko , YAMAUCHI, Takeshi , KURISU, Kazunobu , CHONE, Yoshifumi
发明人： OTSUKA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A pyrimidine derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, and an androgen inhibitor comprising the same having an excellent effect of treating prostatic hyperplasia, female hypertrichosis, and male baldness or pimple: wherein R1 represents hydrogen or hydroxyl; R2 represents hydrogen, lower alkoxycarbonyl, lower alkoxy, halogen, lower alkyl, C¿3? to C8 cycloalkyl, lower alkoxycarbonyl lower alkyl, carboxyl, carboxylated lower alkyl, CONHR, cyano, phenyl, phenylated lower alkyl, lower alkanoyloxy lower alkyl, benzoyl, lower alkanoyl or hydroxylated lower alkyl; R?3¿ represents hydrogen, hydroxy, lower alkyl, C¿3? to C8 cycloalkyl, halogenated lower alkyl or phenyl; R?4¿ represents hydrogen, lower alkyl or lower alkoxy, R5 represents hydrogen, lower alkyl, lower alkoxy lower alkyl or halogenated lower alkyl.

10. 发明申请

WO2010110817A1 PYRROLIDINE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF 审中-公开
标题翻译：抑制β-分泌酶活性的吡咯烷酮化合物及其使用方法
公开(公告)号：WO2010110817A1
公开(公告)日：2010-09-30
申请号：PCT/US2009/060269
申请日：2009-10-09
申请人： COMENTIS, INC. , PURDUE RESEARCH FOUNDATION , ASTELLAS PHARMA INC. , BILCER, Geoffrey, M. , DEVASAMUDRAM, Thippeswamy , ANKALA, Sudha, V. , LILLY, John, C. , LIU, Chunfeng , LEI, Hui , GHOSH, Arun, K. , INOUE, Makoto
发明人： BILCER, Geoffrey, M. , DEVASAMUDRAM, Thippeswamy , ANKALA, Sudha, V. , LILLY, John, C. , LIU, Chunfeng , LEI, Hui , GHOSH, Arun, K. , INOUE, Makoto
IPC分类号： A61K31/16 , A61K31/40 , A61K31/195
CPC分类号： A61K31/16 , A61K31/195 , A61K31/40 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
摘要翻译：本文描述的是新型β-分泌酶抑制剂及其使用方法，包括治疗阿尔茨海默氏病的方法。

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