公开(公告)号：US07579507B2

公开(公告)日：2009-08-25

申请号：US11871710

申请日：2007-10-12

申请人： Kiyoshi Kasai ,  Takehiro Ishikawa ,  Tetsuji Ozawa ,  Koji Kamata ,  Ritsu Suzuki ,  Hideki Takeuchi

发明人： Kiyoshi Kasai ,  Takehiro Ishikawa ,  Tetsuji Ozawa ,  Koji Kamata ,  Ritsu Suzuki ,  Hideki Takeuchi

IPC分类号： C07C217/14

CPC分类号： C07C217/22 ,  C07B2200/07 ,  C07B2200/13

摘要： Crystals of a salt of 4′-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3′,5′-dimethylbiphenyl-4-carboxylic acid. The α type, β type and γ type crystals produced by treating hydrochloride of 4′-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3′,5′-dimethylbiphenyl-4-carboxylic acid with specified solvents, which can be discriminated by the characteristic diffraction peaks of powder X-ray diffractometry and the like.

摘要翻译： 4' - {2 - [（1S，2R）-2-羟基-2-（4-羟基苯基）-1-甲基乙基氨基]乙氧基} -3-异丙基-3'，5'-二甲基联苯-4 -羧酸。 通过处理4' - {2 - [（1S，2R）-2-羟基-2-（4-羟基苯基）-1-甲基乙基氨基]乙氧基} -3-异丙基氢氧化物的盐酸盐制备的α型，β型和γ型晶体 -3'，5'-二甲基联苯-4-羧酸，其特征在于可以通过粉末X射线衍射等的特征衍射峰区分。

公开(公告)号：US20090030218A1

公开(公告)日：2009-01-29

申请号：US11914915

申请日：2006-05-17

申请人： Kiyoshi Kasai ,  Minoru Kubota ,  Ritsu Suzuki ,  Tetsuji Ozawa ,  Takehiro Ishikawa ,  Makoto Kobayashi ,  Junichi Sonehara ,  Masahiro Kobayashi

发明人： Kiyoshi Kasai ,  Minoru Kubota ,  Ritsu Suzuki ,  Tetsuji Ozawa ,  Takehiro Ishikawa ,  Makoto Kobayashi ,  Junichi Sonehara ,  Masahiro Kobayashi

IPC分类号： C07D303/40 ,  C07C69/76 ,  C07C229/38 ,  C07C255/00

CPC分类号： C07D303/22 ,  C07B53/00 ,  C07C67/08 ,  C07C67/31 ,  C07C69/94 ,  C07C213/06 ,  C07C253/30 ,  C07C255/54 ,  C07C217/22

摘要： The present invention provides an industrial method for preparing aminoalcohol derivatives (I) having a biphenyl group, biphenyloxyacetaldehyde derivatives which are used therefore, preparing methods thereof, and intermediates used for the preparing method.The present invention also provides a preparing method including processes for preparing a 3-substituted biphenylcarboxylic acid derivative represented by the following general formula: by allowing a 3-fluorobiphenylcarboxylic acid derivative prepared from a 3-fluorobiphenylcarbonitrile derivative which can be prepared by allowing a 4-halophenol derivative to react with a 2-fluorobenzonitrile derivative which is substituted by a leaving group at 4-position to react with an organometallic reagent.

摘要翻译： 本发明提供了制备具有联苯基的氨基醇衍生物（I）的工业方法，因此使用的联苯氧基乙醛衍生物及其制备方法以及用于制备方法的中间体。 本发明还提供了一种制备方法，其包括由以下通式表示的3-取代的联苯基羧酸衍生物的制备方法：通过使由3-氟联苯基腈衍生物制备的3-氟联苯基羧酸衍生物，其可以通过使4- 卤代酚衍生物与在4-位上被离去基团取代的2-氟苄腈衍生物反应，与有机金属试剂反应。

公开(公告)号：US20080249177A1

公开(公告)日：2008-10-09

申请号：US11936680

申请日：2007-11-07

申请人： Junichi KOBAYASHI ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

发明人： Junichi KOBAYASHI ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

IPC分类号： A61K31/192 ,  C07C229/00 ,  A61P3/00

CPC分类号： C07D307/79 ,  A61K31/195 ,  C07C217/18 ,  C07C217/20 ,  C07C323/62 ,  C07C2601/04

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢或低级烷基; R 3，R 4，R 5和R 6各自为氢，卤素，低级烷基或低级烷氧基 ; R 7和R 8各自为氢，卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基 ，羧基等; R 9是-C（O）-R 10，-A 1 -C（O）-R 10 O > - O 2 -C（O）-R 10或四唑-5-基，其显示出有效和选择性的β3肾上腺素受体刺激活性。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US07674938B2

公开(公告)日：2010-03-09

申请号：US11936680

申请日：2007-11-07

申请人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

发明人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

IPC分类号： C07C217/14 ,  C07C217/20 ,  C07D307/79 ,  A61K31/195 ,  A61P1/16 ,  A61P3/04

CPC分类号： C07D307/79 ,  A61K31/195 ,  C07C217/18 ,  C07C217/20 ,  C07C323/62 ,  C07C2601/04

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢或低级烷基; R3，R4，R5和R6各自为氢，卤素，低级烷基或低级烷氧基; R 7和R 8各自为氢，卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基，羧基等; R9是-C（O）-R10，-A1-C（O）-R10，-O-A2-C（O）-R10或四唑-5-基，其表现出有效和选择性的3-肾上腺素受体 刺激活动。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US07423185B2

公开(公告)日：2008-09-09

申请号：US10545380

申请日：2004-01-30

申请人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

发明人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

IPC分类号： C07C217/14 ,  C07C217/20 ,  C07D307/79 ,  A61K31/195 ,  A61P1/00 ,  A61P1/16 ,  A61P3/04

CPC分类号： C07D307/79 ,  A61K31/195 ,  C07C217/18 ,  C07C217/20 ,  C07C323/62 ,  C07C2601/04

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢或低级烷基; R 3，R 4，R 5和R 6各自为氢，卤素，低级烷基或低级烷氧基 ; R 7和R 8各自为氢，卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基 ，羧基等; R 9是-C（O）-R 10，-A 1 -C（O）-R 10 O > - O 2 -C（O）-R 10或四唑-5-基，其显示出有效和选择性的β3肾上腺素受体刺激活性。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US20060128807A1

公开(公告)日：2006-06-15

申请号：US10545380

申请日：2004-01-30

申请人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

发明人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Ritsu Suzuki ,  Hideyuki Muranaka ,  Tomonaga Ozawa ,  Yuichiro Kai ,  Takehiro Ishikawa ,  Tatsuhiro Kondo ,  Tetsuro Tamai ,  Satoshi Akahane

IPC分类号： A61K31/195 ,  C07C229/22

CPC分类号： C07D307/79 ,  A61K31/195 ,  C07C217/18 ,  C07C217/20 ,  C07C323/62 ,  C07C2601/04

摘要： The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物或其药学上可接受的盐，其中R 1和R 2各自为氢或低级烷基; R 3，R 4，R 5和R 6各自为氢，卤素，低级烷基或低级烷氧基 ; R 7和R 8各自为氢，卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基 ，羧基等; R 9是-C（O）-R 10，-A 1 -C（O）-R 10 O > - O 2 -C（O）-R 10或四唑-5-基，其显示出有效和选择性的β3肾上腺素受体刺激活性。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US20080045741A1

公开(公告)日：2008-02-21

申请号：US11923149

申请日：2007-10-24

申请人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

发明人： Nobuyuki Tanaka ,  Tetsuro Tamai ,  Harunobu Mukaiyama ,  Takehiro Ishikawa ,  Junichi Kobayashi ,  Satoshi Akahane ,  Hiromu Harada

IPC分类号： C07C69/708

CPC分类号： C07C217/60 ,  C07C43/315 ,  C07C69/712 ,  C07C213/02

摘要： The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has β3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus. The present invention also provides a process for preparing said intermediates and a method of using said intermediates.

公开(公告)号：US20070078184A1

公开(公告)日：2007-04-05

申请号：US10576753

申请日：2004-10-05

申请人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Hideyuki Muranaka ,  Takehiro Ishikawa ,  Tetsuro Tamai ,  Satoshi Akahane

发明人： Junichi Kobayashi ,  Tetsuya Nakamura ,  Hideyuki Muranaka ,  Takehiro Ishikawa ,  Tetsuro Tamai ,  Satoshi Akahane

IPC分类号： A61K31/195 ,  C07C309/50

CPC分类号： C07D235/24 ,  C07C233/43 ,  C07C311/21

摘要： The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R4, R5 and R6 is independently hydrogen, halogen, lower alkyl or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogen, lower alkyl, lower alkoxy, etc; R9 is —COR10, -A1-COR10, —O-A2-COR10, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, —OCH2—, etc, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

摘要翻译： 本发明提供由通式（I）表示的化合物：其前药或其药学上可接受的盐，其中R 1是氢或低级烷基; R2和R3各自独立地为氢或低级烷基; R 4，R 5和R 6各自独立地是氢，卤素，低级烷基或低级烷氧基; R 7是氢或低级烷基; R 8是氢，卤素，低级烷基，低级烷氧基等; R 9是-COR 10，-A 1 -OR 10，-OA 2， SUP> -COR 10等; Ar是任选取代的苯基或杂芳基; 并且A是表现出有效和选择性的β3肾上腺素受体刺激活性的键-OCH 2 - 2等。 本发明还提供含有所述化合物的药物组合物及其用途。

公开(公告)号：US06057819A

公开(公告)日：2000-05-02

申请号：US911517

申请日：1997-08-14

申请人： Takehiko Sone ,  Takehiro Ishikawa

发明人： Takehiko Sone ,  Takehiro Ishikawa

IPC分类号： G02F1/133 ,  G09G3/36

CPC分类号： G09G3/3622 ,  G09G2320/0209

摘要： A liquid crystal display apparatus is provided in which crosstalk (after-image extending from a line displayed on the screen) is eliminated. Drive circuitry used in the above type of apparatus is also provided. A delay circuit divides an alternating-current (AC) signal generated by an alternating-current (AC) signal circuit into two signals, i.e., a common AC signal (DF COM) and a segment AC signal (DF SEG). One signal is delayed later than the other. When the common AC signal is delayed later than the segment AC signal, white crosstalk (which is a white bar having a brightness level higher than a white background, appearing on the line extending from a narrow black bar displayed on the screen) is eliminated from the screen. On the other hand, when the segment AC signal is delayed later than the common AC signal, black crosstalk (which is a black bar having a brightness level slightly lower than a white background, emerging on the line extending from a thick black bar displayed on the screen) is removed from the screen. An integrating circuit or a delay line is employed as a delay function of the delay circuit.

摘要翻译： 提供一种液晶显示装置，其中消除了串扰（从屏幕上显示的行延伸的后图像）。 还提供了用于上述类型设备中的驱动电路。 延迟电路将由交流（AC）信号电路产生的交流（AC）信号分成两个信号，即公共AC信号（DF COM）和段AC信号（DF SEG）。 一个信号比另一个信号延迟。 当公共AC信号延迟到段AC信号时，白色串扰（其中出现在从屏幕上显示的窄黑条延伸的线上出现的亮度级高于白色背景的白色条纹）被从 屏幕。 另一方面，当分段AC信号比公共AC信号晚的时间延迟时，黑色串扰（其亮度级略低于白色背景的黑色条纹，出现在从显示在 屏幕）从屏幕上移除。 采用积分电路或延迟线作为延迟电路的延迟功能。

公开(公告)号：US4104864A

公开(公告)日：1978-08-08

申请号：US739855

申请日：1976-11-09

申请人： Takehiro Ishikawa ,  Kazumasa Yasuda ,  Kazuhiro Asano ,  Takashi Ishijima

发明人： Takehiro Ishikawa ,  Kazumasa Yasuda ,  Kazuhiro Asano ,  Takashi Ishijima

IPC分类号： G04F10/00 ,  G04G9/00 ,  G04G9/08 ,  G04G99/00 ,  G04F10/04 ,  G04B19/22 ,  G04F7/04

CPC分类号： G04G9/087 ,  G04G9/0076

摘要： An electronic timepiece comprising in combination: the first and secondary time counters, each having the function of 2, 4 hour measuring, which measures the signal of frequency which will be the basis for time measurement; the chronograph, having the function of 24 hour measuring to make the time measurement by measuring the signal of frequency which will be the basis for the above mentioned time measurement; and the display selecting circuit for displaying each enumerated data of the above mentioned first and secondary time counters and the chronograph selectively by the display device.

摘要翻译： 一种电子钟表，包括：第一和第二时间计数器，每个具有2,4小时测量功能，测量作为时间测量基础的频率信号; 具有24小时测量功能的计时码表，通过测量作为上述时间测量基础的频率信号进行时间测量; 以及显示选择电路，用于通过显示装置选择性地显示上述第一和第二时间计数器的每个枚举数据和计时器。