公开(公告)号：US20090054508A1

公开(公告)日：2009-02-26

申请号：US11814753

申请日：2006-01-27

申请人： Yutaka Kanda ,  Hiromi Ando ,  Keiko Kawashima ,  Takamasa Sugita ,  Masayo Suzuki ,  Hisashi Tagaya ,  Tomoyuki Nakazato ,  Yoshinori Yamashita ,  Takeshi Takahashi ,  Shinji Nara ,  Hiroaki Nakamura

发明人： Yutaka Kanda ,  Hiromi Ando ,  Keiko Kawashima ,  Takamasa Sugita ,  Masayo Suzuki ,  Hisashi Tagaya ,  Tomoyuki Nakazato ,  Yoshinori Yamashita ,  Takeshi Takahashi ,  Shinji Nara ,  Hiroaki Nakamura

IPC分类号： A61K31/416 ,  A61P3/10

CPC分类号： C07D231/56 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/10 ,  C07D495/04

摘要： The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I): {wherein R1 represents —NR4R5 [wherein R4 represents a hydrogen atom or the like, R5 represents substituted or unsubstituted lower alkyl, —C(═O)R6 (wherein R6 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or the like], or the like, and R2 and R3 may be the same or different and each represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, or the like} or a pharmaceutically acceptable salt thereof, and the like.

摘要翻译： 本发明提供一种I型胰岛素样生长因子受体（IGF-1R）抑制剂，其包含作为活性成分的由式（I）表示的吲唑衍生物：其中R 1表示-NR 4 R 5 [其中R 4表示氢原子或 R 5表示取代或未取代的低级烷基，-C（-O）R 6（其中R 6表示取代或未取代的低级烷基，取代或未取代的芳基等）等，等等，R2和R3 可以相同或不同，各自表示氢原子，羟基，取代或未取代的低级烷氧基等}或其药学上可接受的盐等。

公开(公告)号：US20050070591A1

公开(公告)日：2005-03-31

申请号：US10498874

申请日：2002-12-17

申请人： Fumihiko Kanai ,  Chikara Murakata ,  Tetsuya Tsujita ,  Yoshinori Yamashita ,  Shiro Akinaga ,  Tamio Mizukami

发明人： Fumihiko Kanai ,  Chikara Murakata ,  Tetsuya Tsujita ,  Yoshinori Yamashita ,  Shiro Akinaga ,  Tamio Mizukami

IPC分类号： A61K31/407 ,  A61K31/409 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  A61P25/00 ,  A61P35/00 ,  A61P43/00 ,  C07D403/04 ,  C07D487/04 ,  C07D487/22 ,  C07D487/02

CPC分类号： C07D403/04 ,  A61K31/407 ,  A61K31/409 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/541 ,  C07D487/04

摘要： There is provided an indole derivative represented by the above formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of malignant tumor or a brain neurodegenerative disease: (wherein C ring represents a benzene ring or a cyclohexene ring; X and Y are the same or different and each represent —CH2—, —CH(OH)—, —CH(ORx)—, —CH(SRY)— or carbonyl; R1 and R2 are the same or different and each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or substituted or unsubstituted lower alkanoyl or R1 and R2 form a benzene ring together two carbon atoms each being adjacent thereto; and R3, R4 and R5 are the same or different and each represent a hydrogen atom, substituted or unsubstituted lower alkyl, etc.)

摘要翻译： 提供上述式（I）表示的吲哚衍生物或其药学上可接受的盐，其可用于治疗恶性肿瘤或脑神经变性疾病：（其中C环表示苯环或环己烯环; X和 Y相同或不同，各自表示-CH 2 - ， - CH（OH） - ， - CH（OR x） - ， - CH（R 3 Y） - 或羰基; R 1和R 2 各自表示氢原子，取代或未取代的低级烷基，取代或未取代的低级链烯基或取代或未取代的低级烷酰基或R 1和R 2共同形成两个碳原子的苯环， R 3，R 4和R 5相同或不同，各自表示氢原子，取代或未取代的低级烷基等）

公开(公告)号：US06869971B1

公开(公告)日：2005-03-22

申请号：US10110964

申请日：2000-10-19

申请人： Tsutomu Akama ,  Akira Asai ,  Tsutomu Agatsuma ,  Shinji Nara ,  Yoshinori Yamashita ,  Tamio Mizukami ,  Shun-ichi Ikeda ,  Yutaka Saitoh ,  Yutaka Kanda

发明人： Tsutomu Akama ,  Akira Asai ,  Tsutomu Agatsuma ,  Shinji Nara ,  Yoshinori Yamashita ,  Tamio Mizukami ,  Shun-ichi Ikeda ,  Yutaka Saitoh ,  Yutaka Kanda

IPC分类号： A61P31/04 ,  A61P35/00 ,  C07D487/04 ,  C07D487/14 ,  C07D487/16 ,  C07D491/14 ,  C07D491/147 ,  C07D491/16 ,  C07D498/08 ,  A61K31/403 ,  A61K31/4453 ,  C07D209/52 ,  C07D401/06

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14

摘要： UCS 1025 derivatives having antitumor activity or antibacterial activity which are represented by formula (I): wherein R1 represents hydrogen, lower alkyl, etc.; R2 represents hydrogen, or is combined with R3 to represent a bond, etc., or is combined with R4 to represent —O(C═O)—, etc.; R3 represents hydrogen, etc., or is combined with R2 to represent a bond, etc.; R4 represents hydrogen, etc., or is combined with R2 to represent —(C═O)O—, etc.; R5 represents hydrogen or is combined with R6 to represent a bond; R6 represents hydrogen, etc., or is combined with R5 to represent a bond; R7 represents hydrogen or is combined with R8 to represent ═O; R8 represents hydroxy or is combined with R7 to represent ═O; ---- represents a single bond or a double bond, and a represents a single bond (two carbon atoms to which a is bound are combined to form a single bond) or an oxygen atom, or pharmaceutically acceptable salts thereof.

摘要翻译： 由式（I）表示的具有抗肿瘤活性或抗菌活性的UCS 1025衍生物：其中R 1表示氢，低级烷基等; R 2表示氢，或与R 3结合以表示键等，或与R 4结合以表示-O（C = O） - 等; R 3表示氢等，或与R 2结合以表示键等; R 4表示氢等，或与R 2结合代表 - （C = O）O-等; R 5表示氢或与R 6结合以表示键; R 6表示氢等，或与R 5结合以表示键; R 7表示氢或与R 8结合以代表= O; R 8表示羟基或与R 7结合代表= O; ----表示单键或双键，a表示单键（被结合形成单键的两个碳原子）或氧原子，或其药学上可接受的盐。

公开(公告)号：US5965604A

公开(公告)日：1999-10-12

申请号：US215468

申请日：1998-12-17

申请人： Yoshinori Yamashita ,  Ryuichiro Nakai ,  Tamio Mizukami ,  Shingo Kakita ,  Shigeru Chiba ,  Shiro Akinaga

发明人： Yoshinori Yamashita ,  Ryuichiro Nakai ,  Tamio Mizukami ,  Shingo Kakita ,  Shigeru Chiba ,  Shiro Akinaga

IPC分类号： A61K31/365 ,  A61P31/04 ,  A61P35/00 ,  C07D493/18 ,  C07D493/20 ,  C12P17/18 ,  C12R1/465 ,  A01N43/08 ,  A01N43/02 ,  C07D307/77 ,  C12P17/08

CPC分类号： C07D493/20 ,  C12P17/181 ,  C12R1/465 ,  Y10S435/886

摘要： The present invention relates to chrolactomycin compound represented by the following formula (I): ##STR1## or pharmaceutically acceptable salts thereof having antibacterial and antitumor activities.

摘要翻译： 本发明涉及由下式（I）表示的己内酰霉素化合物或其药学上可接受的盐，其具有抗细菌和抗肿瘤活性。

公开(公告)号：US5663298A

公开(公告)日：1997-09-02

申请号：US730348

申请日：1996-10-15

申请人： Tamio Mizukami ,  Akira Asai ,  Yoshinori Yamashita ,  Ritsuko Katahira ,  Atsuhiro Hasegawa ,  Keiko Ochiai ,  Shiro Akinaga

发明人： Tamio Mizukami ,  Akira Asai ,  Yoshinori Yamashita ,  Ritsuko Katahira ,  Atsuhiro Hasegawa ,  Keiko Ochiai ,  Shiro Akinaga

IPC分类号： A61K38/00 ,  C07K5/06 ,  A01N43/02 ,  C07K5/00 ,  C12N1/00

CPC分类号： C07K5/06026 ,  A61K38/00

摘要： The present invention relates to UCK14 compounds having antitumor activity which are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or --COOC(CH.sub.3).sub.3 ; and R.sup.2 and R.sup.3 are taken together to form --CH.sub.2 --, or each R.sup.2 and R.sup.3 independently are hydrogen,and pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及具有抗肿瘤活性的UCK14化合物，其由下式表示：其中R 1为氢或-COOC（CH 3）3; 并且R 2和R 3一起形成-CH 2 - ，或每个R 2和R 3独立地是氢，及其药学上可接受的盐。

公开(公告)号：US5259272A

公开(公告)日：1993-11-09

申请号：US951115

申请日：1992-09-25

申请人： Hiroaki Yamamoto ,  Yoshinori Yamashita ,  Katsuhiko Taniguchi

发明人： Hiroaki Yamamoto ,  Yoshinori Yamashita ,  Katsuhiko Taniguchi

IPC分类号： B60W10/06 ,  B60W30/18 ,  F16H59/06 ,  F16H61/00 ,  F16H61/12 ,  F16H61/66 ,  F16H61/662 ,  F16H61/02

CPC分类号： B60W10/06 ,  B60W10/04 ,  B60W10/101 ,  B60W30/18 ,  B60W30/1819 ,  F16H61/66 ,  F16H61/66259 ,  F16H2061/6618 ,  F16H61/12 ,  Y10T477/624

摘要： In a continuously variable transmission of the type in which a speed change ratio is changed in a manner that the radius of rotation of a belt wound around a drive pulley and a driven pulley is varied by changing the width of a groove between the pulley parts of each pulley with an oil pressure. A control means for controlling an oil pressure in various control modes shifts the control mode from a hold mode to a start mode, when a driver manipulates a vehicle carrying the continuously variable transmission with his intention to start the vehicle, and an amount of discharge flow of an oil pump for generating an oil pressure exceeds a preset value. The safety factor in a stationary state is calculated using the effective tension of the CVT belt, secondary side oil pressure, and the speed change ratio. Using the calculated stationary state safety factor, a manipulated variable previously gained, and a changing rate of the primary oil pressure, a safety factor in a speed change state (transient state) is calculated. A manipulated variable of the speed change control means is limited so that the safety factor in a speed changing state exceeds a predetermined value. When the speed change performance may be damaged with the limitation of manipulated variable, a necessary quantity of the line pressure or the CVT input torque is corrected so as to increase the limit value.

摘要翻译： 在变速比变化的无级变速器中，通过改变带轮部分之间的槽的宽度来改变缠绕在驱动带轮和从动带轮上的带的旋转半径， 每个滑轮都有油压。 用于控制各种控制模式中的油压的控制装置将控制模式从保持模式转移到起动模式，当驾驶员操纵携带无级变速器的车辆时，意图启动车辆，并且排出流量 用于产生油压的油泵超过预设值。 使用CVT带的有效张力，二次侧油压和变速比来计算静止状态下的安全系数。 使用计算出的静止状态安全系数，先前获得的操纵变量和初级油压的变化率，速度变化状态（过渡状态）的安全系数。 变速控制装置的操作变量被限制，使得变速状态下的安全系数超过预定值。 当变速性能受到可控变量的限制而可能损坏时，校正线路压力或CVT输入转矩的必要量，以便增加极限值。

公开(公告)号：US5131297A

公开(公告)日：1992-07-21

申请号：US662287

申请日：1991-02-28

申请人： Yoshinori Yamashita ,  Hiroaki Yamamoto

发明人： Yoshinori Yamashita ,  Hiroaki Yamamoto

IPC分类号： F16H61/662

CPC分类号： F16H61/66259 ,  Y10T477/62429

摘要： A shift control method is provided for controlling shifting in a continuously variable transmission. The transmission changes a gear ratio by increasing or decreasing the turning radius of a belt installed on a pair of pulleys. Each pulley includes a fixed pulley member and a movable pulley member, and the belt turning radius is varied by varying the width of a groove defined between the respective pulley members. The transmission has a shift control range associated therewith which is determined on the basis of the component structural elements thereof, and this shift control range is bounded by a ratio line. The shift control method includes providing a control means for setting a target engine speed according to input throttle opening and vehicle speed information, and setting a limit value of said target engine speed in the vicinity of the ratio line but outside of the shift control range.

摘要翻译： 提供了一种用于控制无级变速器中的换档的换档控制方法。 传动通过增加或减少安装在一对滑轮上的皮带的转弯半径来改变传动比。 每个滑轮包括固定滑轮构件和可动滑轮构件，并且通过改变限定在各个滑轮构件之间的凹槽的宽度来改变皮带转动半径。 变速器具有与其相关联的变速控制范围，其基于其部件结构要素而确定，并且该变速控制范围由比例线限制。 变速控制方法包括提供一种控制装置，用于根据输入的节气门开度和车速信息来设定目标发动机转速，并将所述目标发动机转速的极限值设定在所述比例线附近，但是在变速控制范围之外。

公开(公告)号：US5079376A

公开(公告)日：1992-01-07

申请号：US468915

申请日：1990-01-23

申请人： Hirofumi Nakano ,  Yoshinori Yamashita ,  Katsuhiko Ando ,  Yutaka Saito ,  Keiichi Takahashi ,  Hiroe Ohno

发明人： Hirofumi Nakano ,  Yoshinori Yamashita ,  Katsuhiko Ando ,  Yutaka Saito ,  Keiichi Takahashi ,  Hiroe Ohno

IPC分类号： C07C50/36 ,  C12P29/00 ,  C12R1/645

CPC分类号： C12R1/645 ,  C07C50/36 ,  C12P29/00 ,  C07C2103/44

摘要： Disclosed is novel compound UCT-1003 represented by the following formula: ##STR1## and having anti-tumor activity. UCT-1003 is produced by culturing a microorganism belonging to the genus Paecilomyces.

公开(公告)号：US5069083A

公开(公告)日：1991-12-03

申请号：US588762

申请日：1990-09-26

申请人： Sadayuki Hirano ,  Yoshinori Yamashita ,  Takumi Tatsumi ,  Hiroaki Yamamoto

发明人： Sadayuki Hirano ,  Yoshinori Yamashita ,  Takumi Tatsumi ,  Hiroaki Yamamoto

IPC分类号： B60W10/02 ,  B60W10/10 ,  B60W10/18 ,  F16D48/02 ,  F16D48/06 ,  F16H9/00 ,  F16H59/06 ,  F16H59/62 ,  F16H61/00 ,  F16H61/02 ,  F16H61/04 ,  F16H61/662 ,  F16H63/46

CPC分类号： F16H61/66259 ,  B60W10/02 ,  B60W10/10 ,  B60W10/107 ,  B60W30/18 ,  B60W30/1819 ,  F16D48/066 ,  B60W2550/13 ,  F16D2500/1026 ,  F16D2500/1088 ,  F16D2500/3021 ,  F16D2500/3026 ,  F16D2500/3065 ,  F16D2500/3067 ,  F16D2500/30806 ,  F16D2500/3101 ,  F16D2500/3108 ,  F16D2500/3121 ,  F16D2500/3144 ,  F16D2500/31466 ,  F16D2500/50858 ,  F16D2500/70258 ,  F16D2500/70406 ,  F16D2500/70668 ,  F16H59/62 ,  F16H63/46 ,  Y10T477/6203 ,  Y10T477/624 ,  Y10T477/653

摘要： A method and apparatus for controlling a continuous speed variable transmission includes a pressure sensor for detecting atmospheric pressure, and a control unit which receives a detection signal from the pressure sensor. The control unit responds to the detected atmospheric pressure, the shift position of the transmission, and other predetermined conditions to correct clutch pressure and line pressure.

摘要翻译： 用于控制连续变速变速器的方法和装置包括用于检测大气压的压力传感器，以及从压力传感器接收检测信号的控制单元。 控制单元响应检测到的大气压力，变速器的换档位置和其他预定条件来校正离合器压力和管路压力。

公开(公告)号：US5050455A

公开(公告)日：1991-09-24

申请号：US588614

申请日：1990-09-26

申请人： Yoshinori Yamashita ,  Sadayuki Hirano ,  Takumi Tatsumi ,  Hiroaki Yamamoto

发明人： Yoshinori Yamashita ,  Sadayuki Hirano ,  Takumi Tatsumi ,  Hiroaki Yamamoto

IPC分类号： B60W10/06 ,  B60W30/18 ,  F16H59/06 ,  F16H61/66 ,  F16H61/662

CPC分类号： B60W10/06 ,  B60W10/04 ,  B60W10/101 ,  B60W30/18 ,  B60W30/1819 ,  F16H61/66 ,  F16H61/66259 ,  Y10T477/623 ,  Y10T477/6242

摘要： A method of controlling a continuously variable transmission which includes a fixed pulley member and a movable pulley member supported relative to the fixed pulley member so as to be movable both toward and away from the fixed pulley member, including the steps of decreasing and increasing the width of a groove defined between the pulley members to thereby respectively increase and decrease a rotational radius of a belt which is received between the pulley members in the groove. When a target engine rotational speed based on throttle opening degree and vehicle velocity changes during vehicle running, a transient speed change control is performed so as to change a belt ratio of the transmission based on a predetermined rate limit value. A control unit is provided for receiving the throttle opening degree and vehicle velocity and executing the transient speed change control. During execution of the transient speed change control, the rate limit value is changed in accordance with the throttle opening degree and vehicle velocity, the throttle opening is changed on the basis of vehicle velocity, and the final target engine rotational speed is changed on the basis of the rate limit value. A time limit for execution of transient control is set on the basis of the throttle opening degree and the vehicle velocity.