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1. 发明申请

US20090018056A1 Heteroarylcarbamoylbenzene derivatives 有权
标题翻译：杂芳基氨基甲酰基苯衍生物
公开(公告)号：US20090018056A1
公开(公告)日：2009-01-15
申请号：US12231856
申请日：2008-09-05
申请人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K38/28 , C07D277/28 , C07D241/10 , C07D239/28 , C07D261/14 , A61K31/426 , A61K31/495 , A61K31/433 , A61K31/4439 , A61P3/10 , A61K31/501 , A61K31/4365 , A61K31/42 , A61K31/4965 , C07D285/08 , C07D471/04 , C07D401/10 , C07D403/10
CPC分类号： C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C═N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.
摘要翻译：具有葡糖激酶活化作用的化合物，可用作由下式（I）表示的糖尿病治疗：[其中X1表示氧等，X2表示氧等，R1表示环A上的基团，例如烷基磺酰基等等，R 2表示任选被卤素取代的C 3-7环烷基等，R 3表示环B上的取代基，例如低级烷基等，式（II）：[化学式1]表示6-至10 （III）表示：[式1]表示在环B上任选具有由上述R 3表示的取代基的单环或双环杂芳基，其中键合到氮原子上的环B的碳原子式（I）的酰胺基与环的氮原子形成CN键，以及它们的药学上可接受的盐。

2. 发明授权

US07432287B2 Heteroarylcarbamoylbenzene derivative 有权
标题翻译：杂芳基氨基甲酰基苯衍生物
公开(公告)号：US07432287B2
公开(公告)日：2008-10-07
申请号：US10546962
申请日：2004-02-26
申请人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/4439 , A61K31/4155 , C07D401/10 , C07D231/40
CPC分类号： C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.
摘要翻译：公开了由式（I）表示的化合物及其药学上可接受的盐。该化合物可用作糖尿病治疗和相关病症的葡糖激酶活化剂。还包括组合物和治疗方法。

3. 发明授权

US07754743B2 Heteroarylcarbamoylbenzene derivatives 有权
标题翻译：杂芳基氨基甲酰基苯衍生物
公开(公告)号：US07754743B2
公开(公告)日：2010-07-13
申请号：US12231856
申请日：2008-09-05
申请人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Tomoharu Iino , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/44 , A61K31/425 , C07D417/12
CPC分类号： C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I): [wherein X1 represents oxygen, etc., X2 represents oxygen, etc., R1 represents a group on Ring A such as alkylsulfonyl, etc., R2 represents C3-7 cyclic alkyl optionally substituted with a halogen, etc., R3 represents a substituent on Ring B such as lower alkyl, etc., formula (II): [Chemical Formula 1] represents 6- to 10-membered aryl, etc., and formula (III): [Formula 1] represents monocyclic or bicyclic heteroaryl optionally having on Ring B a substituent represented by R3 above, wherein the carbon atom of Ring B which is bonded to the nitrogen atom of the amide group of formula (I) forms a C═N bond with the nitrogen atom of the ring], as well as their pharmaceutically acceptable salts.
摘要翻译：具有葡糖激酶活化作用的化合物，可用作由下式（I）表示的糖尿病治疗：[其中X1表示氧等，X2表示氧等，R1表示环A上的基团，例如烷基磺酰基等等，R 2表示任选被卤素取代的C 3-7环烷基等，R 3表示环B上的取代基，例如低级烷基等，式（II）：[化学式1]表示6-至10 （III）表示：[式1]表示在环B上任选具有由上述R 3表示的取代基的单环或双环杂芳基，其中键合到氮原子上的环B的碳原子式（I）的酰胺基与环的氮原子形成C = N键，以及它们的药学上可接受的盐。

4. 发明申请

US20060167053A1 Heteroarylcarbamoylbenzene derivative 有权
标题翻译：杂芳基氨基甲酰基苯衍生物
公开(公告)号：US20060167053A1
公开(公告)日：2006-07-27
申请号：US10546962
申请日：2004-02-26
申请人： Tomoharu IIno , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Junichi Eiki
发明人： Tomoharu IIno , Noriaki Hashimoto , Hiroshi Nakashima , Keiji Takahashi , Teruyuki Nishimura , Junichi Eiki
IPC分类号： A61K31/454 , A61K31/433 , A61K31/426 , A61K31/42 , A61K31/41
CPC分类号： C07D213/75 , C07D231/40 , C07D237/20 , C07D239/42 , C07D241/20 , C07D249/04 , C07D261/14 , C07D271/07 , C07D275/03 , C07D277/18 , C07D277/46 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/10 , C07D285/135 , C07D401/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D513/04
摘要： Compounds represented by formula (I): as well as their pharmaceutically acceptable salts are disclosed. The compounds are useful as glucokinase activating agents for the treatment of diabetes and related conditions. Compositions and methods of treatment are also included.
摘要翻译：公开了由式（I）表示的化合物及其药学上可接受的盐。该化合物可用作糖尿病治疗和相关病症的葡糖激酶活化剂。还包括组合物和治疗方法。

5. 发明申请

US20080125429A1 Aryloxy-Substituted Benzimidazole Derivatives 有权
标题翻译：芳氧基取代的苯并咪唑衍生物
公开(公告)号：US20080125429A1
公开(公告)日：2008-05-29
申请号：US11666555
申请日：2005-11-01
申请人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/5377 , C07D213/02 , C07D221/00 , C07D239/06 , C07D241/10 , C07D295/00 , A61P3/10 , A61K31/4439 , A61K31/4545 , A61K31/444 , A61K31/506 , A61K31/497
CPC分类号： A61K38/31 , A61K31/155 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K38/28 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/06 , C07D413/14 , A61K2300/00
摘要： A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
摘要翻译：提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防，或治疗和/或预防糖尿病如视网膜病，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的治疗和/或预防肥胖症。本发明涉及式（I）的化合物：其中R 1和R 2代表氢等; R 3表示氢原子，卤素原子等; R 4各自独立地表示氢原子，低级烷基等; Q表示碳原子，氮原子或硫原子（硫原子可以被氧代基单取代或二取代）。 R 5和R 6各自表示氢原子，低级烷基等; X 1，X 2，X 3和X 4各自独立地表示碳原子或氮原子; Z表示氧原子，硫原子或氮原子; Ar表示任选被选自取代基组β的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数， n表示0〜3的整数， p表示0〜2的整数（条件是X 1〜X 4中的至少2个为碳原子）; q表示0或1]或其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用作糖尿病的治疗。

6. 发明授权

US07932394B2 Aryloxy-substituted benzimidazole derivatives 有权
标题翻译：芳氧基取代的苯并咪唑衍生物
公开(公告)号：US07932394B2
公开(公告)日：2011-04-26
申请号：US11666555
申请日：2005-11-01
申请人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： C07D401/00 , A61K31/445
CPC分类号： A61K38/31 , A61K31/155 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K38/28 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/06 , C07D413/14 , A61K2300/00
摘要： A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
摘要翻译：提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防，或治疗和/或预防糖尿病如视网膜病，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的治疗和/或预防肥胖症。本发明涉及式（I）化合物：其中R 1和R 2表示氢等; R3表示氢原子，卤原子等; R4各自独立地表示氢原子，低级烷基等; Q表示碳原子，氮原子或硫原子（硫原子可以被氧代基单取代或二取代）。 R5和R6各自表示氢原子，低级烷基等; X1，X2，X3和X4各自独立地表示碳原子或氮原子; Z表示氧原子，硫原子或氮原子; Ar表示任选被选自取代基组中的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数， n表示0〜3的整数， p表示0〜2的整数（X1〜X4中的至少2个为碳原子）。 q表示0或1]或其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用作糖尿病的治疗。

7. 发明授权

US08338460B2 2-pyridinecarboxamide derivative having GK-activating effect 有权
标题翻译：具有GK活化作用的2-吡啶甲酰胺衍生物
公开(公告)号：US08338460B2
公开(公告)日：2012-12-25
申请号：US11973240
申请日：2007-10-05
申请人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
发明人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
IPC分类号： A61K31/433 , A61K31/4439 , C07D417/14 , C07D417/10
CPC分类号： C07D417/14
摘要： Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity. R1 and R2 each independently represent a lower alkyl group; X1 represent a group of a formula (II-1): wherein: R11 and R12 each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH2)m, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐。该化合物具有葡糖激酶活化作用，因此可用于治疗糖尿病和肥胖症。 R1和R2各自独立地表示低级烷基; X 1表示式（II-1）的基团：其中：R 11和R 12各自独立地表示氢原子或低级烷基，或与它们所键合的氮原子一起，R 11和R 12可以形成4- 至7元含氮脂肪族环（构成4〜7元含氮脂肪族环的一个碳原子可以被氧原子取代），或与（CH 2）m，R 11和 R12可以形成4-至7-元含氮脂族环; m表示1〜3的整数。

8. 发明申请

US20100261699A1 N-PYRAZOLE-2-PYRIDINE CARBOXAMIDE DERIVATIVE 审中-公开
标题翻译： N-吡咯-2-吡啶酰胺衍生物
公开(公告)号：US20100261699A1
公开(公告)日：2010-10-14
申请号：US12746567
申请日：2008-12-15
申请人： Noriaki Hashimoto , Teruyuki Nishimura , Yufu Sagara
发明人： Noriaki Hashimoto , Teruyuki Nishimura , Yufu Sagara
IPC分类号： A61K31/4439 , C07D401/14 , A61P3/10
CPC分类号： A61K31/155 , A61K31/427 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K38/28 , A61K38/31 , C07D401/14 , A61K2300/00
摘要： The present invention relates to a compound represented by the formula: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently a lower alkyl group, X is CH or the like, and X1 is an aminoalkoxy group or the like, which has a glucokinase-activating effect and thus is useful in the treatment of diabetes, obesity, and the like.
摘要翻译：本发明涉及由下式表示的化合物或其药学上可接受的盐，其中R1和R2各自独立地为低级烷基，X为CH等，X1为氨基烷氧基等，其具有葡糖激酶活化作用，因此可用于治疗糖尿病，肥胖症等。

9. 发明申请

US20080090799A1 2-PYRIDINECARBOXAMIDE DERIVATIVE HAVING GK-ACTIVATING EFFECT 有权
标题翻译：具有GK活化作用的2-吡啶甲酰胺衍生物
公开(公告)号：US20080090799A1
公开(公告)日：2008-04-17
申请号：US11973240
申请日：2007-10-05
申请人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
发明人： Noriaki Hashimoto , Yufu Sagara , Masanori Asai , Teruyuki Nishimura
IPC分类号： A61K31/4439 , A61K31/433 , A61K31/4545 , A61K31/5377 , A61P3/10 , C07D417/14
CPC分类号： C07D417/14
摘要： Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity. R1 and R2 each independently represent a lower alkyl group; X1 represent a group of a formula (II-1): wherein: R11 and R12 each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH2)m, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐。该化合物具有葡糖激酶活化作用，因此可用于治疗糖尿病和肥胖症。 R 1和R 2各自独立地表示低级烷基; X 1表示式（II-1）的基团：其中：R 11和R 12各自独立地表示氢原子或低级烷基或与它们键合的氮原子一起，R 11和R 12可以形成4-至7-元含氮脂族环（构成4〜7元含氮脂肪族环的一个碳原子可以被氧原子取代），或者与（CH 2 2）m < R 11，R 11和R 12可以形成4-至7-元含氮脂族环; m表示1〜3的整数。

10. 发明授权

US4580214A Memory control system 失效
标题翻译：内存控制系统
公开(公告)号：US4580214A
公开(公告)日：1986-04-01
申请号：US460807
申请日：1983-01-25
申请人： Kanji Kubo , Noriaki Hashimoto
发明人： Kanji Kubo , Noriaki Hashimoto
IPC分类号： G06F9/34 , G06F12/04 , G06F12/06 , G06F12/08 , G06F9/36
CPC分类号： G06F9/3816 , G06F12/04 , G06F12/08
摘要： The present memory control system fetches data blocks from memories, fetches data corresponding to the unit of processing in the execution unit from the data blocks, and transfers the data to the execution unit. Data blocks fetched from the memories are held in first hold device. The data blocks held in the first hold device are transferred to second hold device via gate. The gate selectively transfers all or a part of data in data blocks held by the first hold device to the second hold device. When a part of data held in the first hold device is transferred, the second hold device forms data blocks by using the data previously held and the data newly transferred from the first hold device. A data fetch device fetches the data corresponding to the unit length of data processing in the execution unit from the data blocks held in said second hold device and transfers the data to said execution unit.
摘要翻译：本存储器控制系统从存储器中取出数据块，从数据块中取出与执行单元中的处理单元对应的数据，并将数据传送到执行单元。从存储器取出的数据块被保持在第一保持装置中。保持在第一保持装置中的数据块经由门被传送到第二保持装置。门选择性地将由第一保持装置保持的数据块中的数据的全部或一部分传送到第二保持装置。当保持在第一保持装置中的数据的一部分被传送时，第二保持装置通过使用先前保存的数据和从第一保持装置新传送的数据来形成数据块。数据提取装置从保持在所述第二保持装置中的数据块中取出与执行单元中的数据处理的单位长度相对应的数据，并将数据传送到所述执行单元。

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