公开(公告)号：US20120101137A1

公开(公告)日：2012-04-26

申请号：US13380664

申请日：2010-06-26

申请人： Tokuyuki Yamashita ,  Kaori Chikamatsu ,  Naoki Takahashi ,  Hisakazu Iwai ,  Masakazu Kogami ,  Masao Sakairi ,  Nobuhide Watanabe ,  Hiroki Fujieda ,  Daisuke Kataoka ,  Mitsuhiro Makino ,  Noriyasu Kato ,  Toshiyuki Miyazawa ,  Kazushige Nagai ,  Nobuyoshi Kasugai ,  Hiroyo Kataoka ,  Naoki Hiramatsu ,  Nobuaki Tsuruta ,  Yurie Yamada ,  Mika Miyoshi ,  Sei Murakami ,  Izumi Goto ,  Tohru Izuchi ,  Kimie Suzuki ,  Satoko Harada ,  Martin Lang ,  Markus Hans-Juergen Seifert ,  Kristina Kaarina Wolf

发明人： Tokuyuki Yamashita ,  Kaori Chikamatsu ,  Naoki Takahashi ,  Hisakazu Iwai ,  Masakazu Kogami ,  Masao Sakairi ,  Nobuhide Watanabe ,  Hiroki Fujieda ,  Daisuke Kataoka ,  Mitsuhiro Makino ,  Noriyasu Kato ,  Toshiyuki Miyazawa ,  Kazushige Nagai ,  Nobuyoshi Kasugai ,  Hiroyo Kataoka ,  Naoki Hiramatsu ,  Nobuaki Tsuruta ,  Yurie Yamada ,  Mika Miyoshi ,  Sei Murakami ,  Izumi Goto ,  Tohru Izuchi ,  Kimie Suzuki ,  Satoko Harada ,  Martin Lang ,  Markus Hans-Juergen Seifert ,  Kristina Kaarina Wolf

IPC分类号： A61K31/433 ,  A61P3/10 ,  C07D409/04 ,  C07D333/38 ,  A61K31/427 ,  C07D417/14

CPC分类号： A61K31/427 ,  A61K31/433 ,  C07D333/40 ,  C07D409/04 ,  C07D417/14

摘要： The object of the present invention is to provide a compound having a glucokinase-activating effect.A pharmaceutical composition comprising a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: wherein X means a nitrogen atom or CR6, wherein R6 means a hydrogen atom or a halogen atom; R1 means a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 alkylthio group; R2 means a hydrogen atom or a fluorine atom; R3 means a hydrogen atom or a C1-C6 alkyl group; and one of R4 and R5 means a hydrogen atom or a C1-C6 alkyl group, and the other means a C1-C6 alkylenecarboxylic acid, a C1-C6 alkylsulfonyl group, a C1-C6 alkylcarbonyl group, or CONH2.

摘要翻译： 本发明的目的是提供具有葡糖激酶活化作用的化合物。 一种药物组合物，其包含由通式（I）表示的化合物或其药学上可接受的盐作为活性成分：其中X表示氮原子或CR 6，其中R 6表示氢原子或卤素原子; R1表示氢原子，C1-C6烷基，C1-C6烷氧基或C1-C6烷硫基; R2表示氢原子或氟原子; R3表示氢原子或C1-C6烷基; R4和R5之一表示氢原子或C1-C6烷基，另一个表示C1-C6亚烷基羧酸，C1-C6烷基磺酰基，C1-C6烷基羰基或CONH2。

公开(公告)号：US20100016263A1

公开(公告)日：2010-01-21

申请号：US12302975

申请日：2007-06-01

申请人： Hiroki Fujieda ,  Hironori Otsu ,  Shoji Yasufuku ,  Masaaki Shirai

发明人： Hiroki Fujieda ,  Hironori Otsu ,  Shoji Yasufuku ,  Masaaki Shirai

IPC分类号： A61K31/593 ,  C07C401/00 ,  A61P17/00

CPC分类号： C07C401/00

摘要： A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.

摘要翻译： 本发明的主要目的是提供一种具有优异维生素D3活性的新型有用的维生素D3衍生物，与常规维生素D3衍生物相比，对全身钙代谢的影响相对较小。 本发明包括以下通式[1]的9,10-仲孕烷衍生物和含有它作为活性成分的药物组合物。 在通式[1]中，16位和17位之间的以下部分结构是指单键或双键：Y为单键，亚烷基，亚烯基或亚苯基; R1和R2相同或不同，各自表示氢，烷基或环烷基; 或R 1和R 2与相邻碳原子一起形成环烷基; R3是氢或甲基; Z是氢，羟基或-NR 11 R 12。

公开(公告)号：US08796246B2

公开(公告)日：2014-08-05

申请号：US12302975

申请日：2007-06-01

申请人： Hiroki Fujieda ,  Hironori Otsu ,  Shoji Yasufuku ,  Masaaki Shirai

发明人： Hiroki Fujieda ,  Hironori Otsu ,  Shoji Yasufuku ,  Masaaki Shirai

IPC分类号： A61K31/593 ,  C07C401/00

CPC分类号： C07C401/00

摘要： A main object of the invention is to provide a novel useful vitamin D3 derivative, which has an excellent vitamin D3 activity and, as compared with conventional vitamin D3 derivatives, has a relatively small amount of influence on the systemic calcium metabolism. The invention includes a 9,10-secopregnane derivative of the following general formula [1] and a pharmaceutical composition containing it as active ingredient. In the general formula [1], the following partial structure between the 16-position and the 17-position means a single bond or a double bond: Y is a single bond, an alkylene, an alkenylene or phenylene; R1 and R2 are the same or different, each represents hydrogen, an alkyl or a cycloalkyl; or R1 and R2, taken together with the adjacent carbon atom, form a cycloalkyl; R3 is hydrogen or methyl; Z is hydrogen, hydroxy or —NR11R12.

摘要翻译： 本发明的主要目的是提供一种具有优异维生素D3活性的新型有用的维生素D3衍生物，与常规维生素D3衍生物相比，对全身钙代谢的影响相对较小。 本发明包括以下通式[1]的9,10-仲孕烷衍生物和含有它作为活性成分的药物组合物。 在通式[1]中，16位和17位之间的以下部分结构是指单键或双键：Y为单键，亚烷基，亚烯基或亚苯基; R1和R2相同或不同，各自表示氢，烷基或环烷基; 或R 1和R 2与相邻碳原子一起形成环烷基; R3是氢或甲基; Z是氢，羟基或-NR 11 R 12。

公开(公告)号：US20100130454A1

公开(公告)日：2010-05-27

申请号：US11720789

申请日：2005-12-05

申请人： Hiroki Fujieda ,  Hironori Otsu ,  Shoji Yasufuku

发明人： Hiroki Fujieda ,  Hironori Otsu ,  Shoji Yasufuku

IPC分类号： A61K31/59 ,  C07C401/00 ,  A61P17/12 ,  A61P17/06

CPC分类号： C07C401/00

摘要： A novel useful vitamin D3 derivative which is reduced in influence on systemic calcium metabolism while retaining excellent vitamin D3 activity. The derivative is a 9,10-secopregnane derivative represented by the following general formula [1]. Also provided is a medicinal composition containing the derivative as an active ingredient. In the general formula [1], Y represents (1) a single bond, (2) alkylene (3) alkenylene, or (4) phenylene; R1 and R2 are the same or different and each represents (1) hydrogen, (2) alkyl, or (3) cycloalkyl, or R1 and R2 in combination represent cycloalkyl in cooperation with the adjacent carbon atom; R3 represents hydrogen or methyl; and Z represents (1) hydrogen, (2) hydroxy, or (3) —NR11R12.

摘要翻译： 一种新颖有用的维生素D3衍生物，其对全身钙代谢的影响减小，同时保持优异的维生素D3活性。 该衍生物是由以下通式[1]表示的9,10-仲孕烷衍生物。 还提供含有该衍生物作为活性成分的药物组合物。 在通式[1]中，Y表示（1）单键，（2）亚烷基（3）亚烯基或（4）亚苯基; R1和R2相同或不同，各自表示（1）氢，（2）烷基或（3）环烷基，或者R1和R2组合表示与相邻碳原子配合的环烷基; R3表示氢或甲基; Z表示（1）氢，（2）羟基或（3）-NR11R12。

公开(公告)号：US20100059020A1

公开(公告)日：2010-03-11

申请号：US12552012

申请日：2009-09-01

申请人： Tetsuro Serai ,  Noriyasu Amano ,  Hiroki Fujieda ,  Hiroshi Nakamura ,  Akikazu Uchida

发明人： Tetsuro Serai ,  Noriyasu Amano ,  Hiroki Fujieda ,  Hiroshi Nakamura ,  Akikazu Uchida

IPC分类号： F02M59/36 ,  F02M37/00 ,  F02D41/30

CPC分类号： F02D41/02 ,  F02B2275/16 ,  F02D19/061 ,  F02D19/084 ,  F02D19/087 ,  F02D41/0025 ,  F02D2200/0611 ,  F02M19/08 ,  F02M37/0064 ,  F02M37/10 ,  Y02T10/123 ,  Y02T10/36

摘要： At the time of shifting a fuel property value associated with a first imaginary passage cell as a fuel property value associated with a second imaginary passage cell located on the downstream side thereof, the fuel property value associated with the second imaginary passage cell is corrected in a controller by computing a difference between the fuel property value associated with the first imaginary passage cell and the fuel property value associated with the second imaginary passage cell and multiplying the difference by a correction coefficient. A stoichiometric air/fuel ratio is computed in the controller based on the fuel property value, which is associated with a last one of the imaginary passage cells. Fuel injection of an injector is controlled by the controller based on a computed injection quantity of fuel, which is computed based on the stoichiometric air/fuel ratio.

摘要翻译： 在将与第一虚设通道电池相关联的燃料特性值变换为与位于其下游侧的第二假想通道电池相关联的燃料特性值时，与第二假想通道电池相关联的燃料特性值被校正为 控制器，通过计算与第一虚设通道单元相关联的燃料特性值与与第二虚部通道单元相关联的燃料特性值之间的差异，并将差乘以校正系数。 基于与最后一个虚拟通道单元相关联的燃料特性值，在控制器中计算化学计量空气/燃料比。 喷射器的燃料喷射由控制器基于计算的基于化学计量空气/燃料比计算的燃料喷射量来控制。