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1. 发明授权

US07816405B2 Calcium bis [(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl ]-2-isopropoxypropionate] and intermediate thereof 失效
标题翻译： [（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸钙]及其中间体
公开(公告)号：US07816405B2
公开(公告)日：2010-10-19
申请号：US11405619
申请日：2006-04-18
申请人： Masanobu Shinoda , Fumiyoshi Matsuura , Kaoru Murata , Masaharu Gotoda , Kenji Hayashi , Manabu Sasho , Naoki Ozeki , Susumu Inoue , Katsutoshi Nishiura , Yoshihiko Hisatake , Teiji Takigawa , Mamoru Miyazawa , Shigeto Negi , Keisuke Matsuyama
发明人： Masanobu Shinoda , Fumiyoshi Matsuura , Kaoru Murata , Masaharu Gotoda , Kenji Hayashi , Manabu Sasho , Naoki Ozeki , Susumu Inoue , Katsutoshi Nishiura , Yoshihiko Hisatake , Teiji Takigawa , Mamoru Miyazawa , Shigeto Negi , Keisuke Matsuyama
IPC分类号： A61K31/277 , C07C255/55
CPC分类号： C07C255/54
摘要： The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy) -2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof.There is need for (2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same.Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S) -3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.
摘要翻译：本发明涉及由式（I）表示的双[（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸钙] ），其水合物，式（I）化合物的结晶和可用作药物的式（I）化合物的水合物的结晶及其制备方法和中间体，以及其生产方法。需要药物形式的（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸，纯化以使残留溶剂含量最小化并且具有均匀的规格和高度有利的可加工性，以及其制备方法。结晶的[（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸钠]，（2S） - 3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸解决了上述问题。

2. 发明申请

US20090069591A1 Calcium Bis [ (2S) -3- [3-[ (2S) -3- (4-Chloro-2-Cyanophenoxy) -2- Fluoropropoxy]Phenyl] -2- Isopropoxypropionate] and Intermediate Thereof 审中-公开
标题翻译： [（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸酯]及其中间体
公开(公告)号：US20090069591A1
公开(公告)日：2009-03-12
申请号：US11886664
申请日：2006-04-18
申请人： Masanobu Shinoda , Fumiyoshi Matsuura , Kaoru Murata , Masaharu Gotoda , Kenji Hayashi , Manabu Sasho , Naoki Ozeki , Susumu Inoue , Katsutoshi Nishiura , Yoshihiko Hisatake , Teiji Takigawa , Mamoru Miyazawa , Shigeto Negi , Keisuke Matsuyama
发明人： Masanobu Shinoda , Fumiyoshi Matsuura , Kaoru Murata , Masaharu Gotoda , Kenji Hayashi , Manabu Sasho , Naoki Ozeki , Susumu Inoue , Katsutoshi Nishiura , Yoshihiko Hisatake , Teiji Takigawa , Mamoru Miyazawa , Shigeto Negi , Keisuke Matsuyama
IPC分类号： C07C69/734 , C07C59/68
CPC分类号： C07C255/54
摘要： The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof.[Problem] There is need for (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. [Solution] Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem. [Selected Drawing] None
摘要翻译：本发明涉及由式（I）表示的双[（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸钙] ），其水合物，式（I）化合物的结晶和可用作药物的式（I）化合物的水合物的结晶及其制备方法和中间体，以及其生产方法。 [问题]需要（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸，其形式为纯化，以使残留溶剂含量最小化并具有均匀的规格和高度有利的可加工性，及其制备方法。 [溶液]结晶的双[（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸]钙， 2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸解决了上述问题。 [已选图]无

3. 发明申请

US20070117866A1 Calcium bis [ (2S) - 3- [3-[ (2S) -3- (4-chloro-2-cyanophenoxy) -2- fluoropropoxy]phenyl ]-2-isopropoxypropionate] and intermediate thereof 失效
标题翻译： [（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸钙]及其中间体
公开(公告)号：US20070117866A1
公开(公告)日：2007-05-24
申请号：US11405619
申请日：2006-04-18
申请人： Masanobu Shinoda , Fumiyoshi Matsuura , Kaoru Murata , Masaharu Gotoda , Kenji Hayashi , Manabu Sasho , Naoki Ozeki , Susumu Inoue , Katsutoshi Nishiura , Yoshihiko Hisatake , Teiji Takigawa , Mamoru Miyazawa , Shigeto Negi , Keisuke Matsuyama
发明人： Masanobu Shinoda , Fumiyoshi Matsuura , Kaoru Murata , Masaharu Gotoda , Kenji Hayashi , Manabu Sasho , Naoki Ozeki , Susumu Inoue , Katsutoshi Nishiura , Yoshihiko Hisatake , Teiji Takigawa , Mamoru Miyazawa , Shigeto Negi , Keisuke Matsuyama
IPC分类号： A61K31/277 , C07C255/55
CPC分类号： C07C255/54
摘要： The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. [Problem]There is need for (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. [Solution]Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem. [Selected Drawing] None
摘要翻译：本发明涉及由式（I）表示的双[（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸钙] ），其水合物，式（I）化合物的结晶和可用作药物的式（I）化合物的水合物的结晶及其制备方法和中间体，以及其生产方法。 [问题]需要（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸，其形式为纯化，以使残留溶剂含量最小化并具有均匀的规格和高度有利的可加工性，及其制备方法。 [溶液]结晶的双[（2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸]钙， 2S）-3- [3 - [（2S）-3-（4-氯-2-氰基苯氧基）-2-氟丙氧基]苯基] -2-异丙氧基丙酸解决了上述问题。 [已选图]无

4. 发明授权

US07538117B2 Crystalline and amorphous pyrimidine compounds and processes for preparing pyrimidine compounds 失效
标题翻译：结晶和无定形嘧啶化合物及制备嘧啶化合物的方法
公开(公告)号：US07538117B2
公开(公告)日：2009-05-26
申请号：US11378307
申请日：2006-03-20
申请人： Hitoshi Harada , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
发明人： Hitoshi Harada , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D405/14 , C07D405/06
摘要： Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2θ±0.2°) of 9.7° and/or 21.9° in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation. Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate and amorphous 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate are also suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.
摘要翻译：在衍射角（2θ±0.2°）为9.7°的衍射峰的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮的晶体和/或21.9°在粉末X射线衍射中适用于诸如便秘的疾病的预防和治疗剂的活性成分。 5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物和无定形的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物也适用于诸如便秘等疾病的预防和治疗剂的活性成分。

5. 发明申请

US20070078151A1 Crystalline and amorphous pyrimidine compounds and processes for preparing pyrimidine compounds 失效
标题翻译：结晶和无定形嘧啶化合物及制备嘧啶化合物的方法
公开(公告)号：US20070078151A1
公开(公告)日：2007-04-05
申请号：US11378307
申请日：2006-03-20
申请人： Hitoshi Harada , Hiroshi Ishihara , Yoshiaki Sato , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
发明人： Hitoshi Harada , Hiroshi Ishihara , Yoshiaki Sato , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
IPC分类号： A61K31/506 , C07D405/14
CPC分类号： C07D405/14 , C07D405/06
摘要： Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2θ±0.2°) of 9.7° and/or 21.9° in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation. Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate and amorphous 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate are also suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.
摘要翻译：在衍射角（2θ±0.2°）为9.7°的衍射峰的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮的晶体和/或21.9°在粉末X射线衍射中适用于诸如便秘的疾病的预防和治疗剂的活性成分。 5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物和无定形的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物也适用于诸如便秘等疾病的预防和治疗剂的活性成分。

6. 发明授权

US07767812B2 Crystals of pyrimidine compound and process for producing the same 失效
标题翻译：嘧啶化合物的晶体及其制备方法
公开(公告)号：US07767812B2
公开(公告)日：2010-08-03
申请号：US12346544
申请日：2008-12-30
申请人： Hitoshi Harada , Hiroshi Ishihara , Yoshiaki Sato , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
发明人： Hitoshi Harada , Hiroshi Ishihara , Yoshiaki Sato , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
IPC分类号： C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D405/14 , C07D405/06
摘要： Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2θ±0.2°) of 9.7° and/or 21.9° in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation. Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate and amorphous 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate are also suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.
摘要翻译：在衍射角（2θ;±0.2°）为9.7°的衍射峰的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮的晶体 °和/或21.9°在粉末X射线衍射中适用于诸如便秘的疾病的预防和治疗剂的活性成分。 5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物和无定形的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物也适用于诸如便秘等疾病的预防和治疗剂的活性成分。

7. 发明授权

US06573384B1 Process for production of indole derivatives and intermediates therefor 失效
标题翻译：吲哚衍生物及其中间体的制备方法
公开(公告)号：US06573384B1
公开(公告)日：2003-06-03
申请号：US09937929
申请日：2001-11-13
申请人： Manabu Shasho , Yuki Komatsu , Mamoru Miyazawa , Kimihiro Matsuo , Susumu Inoue , Kohshi Ueno
发明人： Manabu Shasho , Yuki Komatsu , Mamoru Miyazawa , Kimihiro Matsuo , Susumu Inoue , Kohshi Ueno
IPC分类号： C07D40104
CPC分类号： C07D401/04
摘要： To provide a novel, industrially superior process for producing a 1,4-substituted cyclic amine compound which is useful as a pharmaceutical, and an intermediate for the process. That is, a process for producing an indole compound (I), which comprises reducing a 1,4-subsutituted 2-nitrophenyl compound (VII) to give a 1,4-substituted 2-aminophenyl compound (V); reacting the compound (V) with an N-substituted 4-piperidone compound (VI) to give a 1,4-substituted 2-piperidylaminophenyl compound (IV); cyclizing the compound (IV) to give a 2-oxoindoline compound (III); halogenating the compound (III) to give a 2-halogenated indole compound (II); reducing the compound (II); and if necessary subjecting the resulting compound to alcoholysis or aminolysis. wherein each of R1 and R2 represents a substituent; X represents a halogen atom; and n is a numerical subscript.
摘要翻译：提供一种工业上优异的制备用作药物的1,4-取代的环胺化合物的方法，以及该方法的中间体。也就是说，制备吲哚化合物（I）的方法，其包括还原1,4-取代的2-硝基苯基化合物（VII）以得到1,4-取代的2-氨基苯基化合物（V）; 使化合物（V）与N-取代的4-哌啶酮化合物（Ⅵ）反应，得到1,4-取代的2-哌啶基氨基苯基化合物（Ⅳ）。使化合物（IV）环化，得到2-氧代二氢吲哚化合物（III）; 卤化化合物（Ⅲ）得到2-卤代吲哚化合物（Ⅱ）; 还原化合物（II）; 并且如果需要，将所得化合物进行醇解或氨解。其中R 1和R 2各自表示取代基; X表示卤原子; n是数字下标。

8. 发明申请

US20090111986A1 NOVEL CRYSTALS OF PYRIMIDINE COMPOUND AND PROCESS FOR PRODUCING THE SAME 失效
标题翻译：吡啶化合物的新型结晶及其制造方法
公开(公告)号：US20090111986A1
公开(公告)日：2009-04-30
申请号：US12346544
申请日：2008-12-30
申请人： Hitoshi HARADA , Hiroshi Ishihara , Yoshiaki Sato , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
发明人： Hitoshi HARADA , Hiroshi Ishihara , Yoshiaki Sato , Hiroyuki Chiba , Yuki Komatsu , Susumu Inoue , Naoki Ozeki
IPC分类号： C07D405/14 , C07D405/02
CPC分类号： C07D405/14 , C07D405/06
摘要： Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one having a diffraction peak at a diffraction angle (2θ±0.2°) of 9.7° and/or 21.9° in a powder X-ray diffraction are suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation. Crystals of 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate and amorphous 5-[2-amino-4-(2-furyl)pyrimidin-5-yl]-1-methylpyridin-2(1H)-one hydrate are also suitable for an active ingredient of a preventing and therapeutic agent for diseases such as constipation.
摘要翻译：在衍射角（2θ±0.2°）为9.7°的衍射峰的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮的晶体和/或21.9°在粉末X射线衍射中适用于诸如便秘的疾病的预防和治疗剂的活性成分。 5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物和无定形的5- [2-氨基-4-（2-呋喃基）嘧啶-5-基] -1-甲基吡啶-2（1H） - 酮水合物也适用于诸如便秘等疾病的预防和治疗剂的活性成分。

9. 发明申请

US20100110271A1 SOLID-STATE IMAGING DEVICE, METHOD FOR MANUFACTURING THE SAME, AND ELECTRONIC APPARATUS 有权
标题翻译：固态成像装置，其制造方法和电子装置
公开(公告)号：US20100110271A1
公开(公告)日：2010-05-06
申请号：US12604523
申请日：2009-10-23
申请人： Takeshi Yanagita , Keiji Mabuchi , Susumu Inoue
发明人： Takeshi Yanagita , Keiji Mabuchi , Susumu Inoue
IPC分类号： H04N5/225 , H01L31/0232 , H01L21/00
CPC分类号： H01L27/14623 , H01L27/14621 , H01L27/14627 , H01L27/1464 , H01L27/14643
摘要： A solid-state imaging device includes an effective pixel portion in which a plurality of pixels including photoelectric conversion elements are arrayed; and a nonconductive interpixel light-shielding film that is placed in the effective pixel portion and that shields areas between the pixels.
摘要翻译：一种固态成像装置，包括排列具有光电转换元件的多个像素的有效像素部，以及放置在有效像素部分中并遮蔽像素之间的区域的非导电像素间屏蔽膜。

10. 发明申请

US20080283728A1 Solid-state image pickup device and a method of manufacturing the same, and image pickup apparatus 审中-公开
标题翻译：固体摄像装置及其制造方法以及摄像装置
公开(公告)号：US20080283728A1
公开(公告)日：2008-11-20
申请号：US12081531
申请日：2008-04-17
申请人： Susumu Inoue
发明人： Susumu Inoue
IPC分类号： H01L27/00 , H01L21/00
CPC分类号： H01L27/14627 , H01L27/14625 , H01L27/14629 , H01L27/1463 , H01L27/14636 , H04N9/045
摘要： Disclosed herein is a solid-state image pickup device, including: a first pixel for receiving a visible light of an incident light to subject the visible light to photoelectric conversion; a second pixel for receiving the visible light and a near-infrared light of the incident light to subject each of the visible light and the near-infrared light to the photoelectric conversion; a color filter layer; and an infrared light filter layer for absorbing or reflecting an infrared light, and transmitting the visible light.
摘要翻译：本文公开了一种固态图像拾取装置，包括：第一像素，用于接收入射光的可见光以对可见光进行光电转换; 用于接收可见光的第二像素和入射光的近红外光，以使每个可见光和近红外光进行光电转换; 滤色器层; 以及用于吸收或反射红外光的红外光滤光层，并透射可见光。

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