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1. 发明授权

US06423725B1 4-(2-keto-1-benzimidazolinyl)piperidine compounds as ORL1-receptor agonists 失效
标题翻译： 4-（2-酮-1-苯并咪唑啉基）哌啶化合物作为ORL1-受体激动剂
公开(公告)号：US06423725B1
公开(公告)日：2002-07-23
申请号：US09403408
申请日：2000-03-06
申请人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hiroshi Kondo , Tatsuya Yamagishi
发明人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hiroshi Kondo , Tatsuya Yamagishi
IPC分类号： A61K31454
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14
摘要： A compound of the formula: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined above are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.
摘要翻译：下式化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如上定义，可用作ORL1-受体激动剂，并且可用作哺乳动物受试者中的止痛剂等。

2. 发明授权

US06861425B2 Benzimidazole compounds as ORL1-receptor agonists 失效
标题翻译：苯并咪唑化合物作为ORL1受体激动剂
公开(公告)号：US06861425B2
公开(公告)日：2005-03-01
申请号：US09753954
申请日：2001-01-03
申请人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hirohisa Shimokawa
发明人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hirohisa Shimokawa
IPC分类号： A61K31/4427 , A61K31/454 , A61K31/46 , A61K31/4985 , A61K31/499 , A61K31/4995 , A61P1/00 , A61P3/12 , A61P9/00 , A61P23/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/36 , A61P27/16 , A61P29/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D451/06 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08 , A61K31/496 , C07D403/14
CPC分类号： C07D401/04 , C07D401/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
摘要： A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R1 is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5)alkenyl, hydroxy-(C1-C4)alkyl, (C1-C4)alkoxy-(C═O), or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, M is a covalent bond O, S, NH or the like, Y is 4- to 12-membered bicyclic-carbocyclic rings or 4- to 12-membered bicyclic-heterocyclic rings, or 5- to 17 membered spirocarbocyclic rings or 5- to 17-membered spiroheterocyclic rings or the like, Z1, Z2, Z3 and Z4 are hydrogen or the like, is disclosed. These compounds have ORL1-receptor agonist activity, and are thus useful as analgesics or the like in mammalian subjects.
摘要翻译：下式的化合物或其药学上可接受的盐，其中R 1是未被取代的，单 - ，二 - 或三 - 取代的（C 3 -C 11）环烷基或（C 3 -C 11）环烯基等，A是未取代的（C 1 -C 7）烷基或（C 2 -C 5）烯基，羟基 - （C 1 -C 4）烷基，（C 1 -C 4）烷氧基 - （C = O）或未取代的单，或芳族 - 杂环等，M是共价键O，S，NH等，Y是4至12元双环 - 碳环或4至12元双环杂环，或5-至 17元螺环环或5〜17元螺杂环等Z，Z 2，Z 3和Z 4均为氢等。这些化合物具有ORL1-受体激动剂活性，因此在哺乳动物受试者中可用作止痛剂等。

3. 发明授权

US06172067B2 2-substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists 失效
标题翻译： 2-取代-1-哌啶基苯并咪唑化合物作为ORL1-受体激动剂
公开(公告)号：US06172067B2
公开(公告)日：2001-01-09
申请号：US09369208
申请日：1999-08-05
申请人： Fumitaka Ito , Hirohide Noguchi , Hiroshi Kondo
发明人： Fumitaka Ito , Hirohide Noguchi , Hiroshi Kondo
IPC分类号： A61K31454
CPC分类号： C07D401/04 , C07D211/58 , C07D401/14
摘要： A compound of the formula: or a pharmaceutically acceptable salt thereof, wherein R is unsubstituted, mono-, di- or tri-substituted (C3-C11)cycloalkyl or (C3-C11)cycloalkenyl or the like, A is unsubstituted (C1-C7)alkyl or (C2-C5 )alkenyl, or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, Y is hydrogen, halo, amino or mercapto, or unsubstituted, mono-, di- or tri- substituted (C1-C10)alkyl-M—, (C3-C7)cycloalkyl-M—, (C2-C6)alkenyl-M—, (C1-C4)alkyl-NH-((C1-C4)alkyl)-M—, di(C1-C4)alkyl-N-((C1-C4)alkyl)-M—, aryl-M—, aromatic or non-aromatic heterocyclic-M—, aryl-(C1-C5)alkyl-M— or aromatic non-aromatic heterocyclic-(C1-C5)alkyl-M—, wherein M is a covalent bond O, S, NH or the like, or the like; Z1, Z2, Z3 and Z4 are hydrogen or the like, has ORL1-receptor agonist activity, and are useful as analgesics or the like in mammalian subjects.
摘要翻译：一种下式的化合物或其药学上可接受的盐，其中R是未取代的一价，二或三取代的（C 3 -C 11）环烷基或（C 3 -C 11）环烯基等，A是未取代的（C1- C7）烷基或（C2-C5）烯基或未取代的单，二或三取代的芳基或芳族杂环等，Y是氢，卤素，氨基或巯基，或未取代的单，二 - （C 1 -C 6）烷基-M-，（C 3 -C 7）环烷基M - ，（C 2 -C 6）烯基-M-，（C 1 -C 4）烷基-NH-（（C 1 -C 4）烷基）-M-，二（C 1 -C 4）烷基-N - （（C 1 -C 4）烷基）-M-，芳基M-，芳族或非芳族杂环M-，芳基 - （C 1 -C 5）烷基-M-或芳族非芳族杂环 - （C1-C5）烷基-M-，其中M是共价键O，S，NH等; Z1，Z2，Z3和Z4为氢等具有ORL1-受体激动剂活性，并且可用作哺乳动物受试者中的止痛剂等。

4. 发明授权

US08697877B2 Oxyindole derivatives with motilin receptor agonistic activity 有权
标题翻译：具有胃动素受体激动活性的氧吲哚衍生物
公开(公告)号：US08697877B2
公开(公告)日：2014-04-15
申请号：US13203301
申请日：2010-03-01
申请人： Masaki Sudo , Yasuhiro Iwata , Yoshimasa Arano , Madoka Jinno , Masashi Ohmi , Hirohide Noguchi
发明人： Masaki Sudo , Yasuhiro Iwata , Yoshimasa Arano , Madoka Jinno , Masashi Ohmi , Hirohide Noguchi
IPC分类号： C07D401/04 , A61K31/454
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38).
摘要翻译：本发明涉及式（I）的新型氧吲哚衍生物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用于治疗通过胃动素受体（GPR38）介导的各种病症的用途。

5. 发明申请

US20120142691A1 PICOLINAMIDE DERIVATIVES AS TTX-S BLOCKERS 有权
标题翻译： PICOLINAMIDE衍生物作为TTX-S阻断剂
公开(公告)号：US20120142691A1
公开(公告)日：2012-06-07
申请号：US13388740
申请日：2010-08-04
申请人： Hirohide Noguchi , Tadashi Inoue , Mikio Morita , Yoshimasa Arano
发明人： Hirohide Noguchi , Tadashi Inoue , Mikio Morita , Yoshimasa Arano
IPC分类号： A61K31/5377 , C07D401/14 , C07D413/14 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61P1/00 , A61P25/00 , A61P19/08 , A61P19/02 , A61P1/18 , A61P25/08 , A61P9/06 , A61P25/22 , A61P25/24 , A61P5/00 , A61P29/00 , C07D401/12
CPC分类号： C07D401/12 , A61K31/4433 , A61K31/4439 , A61K31/497 , A61K31/5377 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
摘要翻译：本发明涉及具有电压门控钠通道作为TTX-S通道的阻断活性的吡啶酰胺衍生物，其可用于治疗或预防涉及电压门控钠通道的疾病和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病中的用途。

6. 发明申请

US20140187583A1 Polymorph Form of 4-methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid 有权
标题翻译： 4-甲基）哌啶-1-基]甲基} - 四氢-2H-吡喃-4-羧酸的多晶型
公开(公告)号：US20140187583A1
公开(公告)日：2014-07-03
申请号：US14118377
申请日：2012-05-18
申请人： Toyoharu Numata , Hirohide Noguchi , Nobuaki Waizumi , Takashi Kojima
发明人： Toyoharu Numata , Hirohide Noguchi , Nobuaki Waizumi , Takashi Kojima
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.
摘要翻译：本发明涉及4 - {[4 - （{[4-（2,2,2-三氟乙氧基）-1,2-苯并异恶唑-3-基]氧基}甲基）哌啶-1-基] 甲基} - 四氢-2H-吡喃-4-羧酸。更具体地说，本发明涉及多晶型形式（多晶型I或多晶型II），以及制备含这种多晶型形式的组合物和使用方法。

7. 发明授权

US06951867B2 N-substituted piperidinyl-imidazopyridine compounds as 5-HT4 receptor modulators 失效
标题翻译： N-取代的哌啶基 - 咪唑并吡啶化合物作为5-HT 4受体调节剂
公开(公告)号：US06951867B2
公开(公告)日：2005-10-04
申请号：US10667182
申请日：2003-09-17
申请人： Yasuhiro Katsu , Kana Kon-I , Mikio Morita , Hirohide Noguchi , Chikara Uchida
发明人： Yasuhiro Katsu , Kana Kon-I , Mikio Morita , Hirohide Noguchi , Chikara Uchida
IPC分类号： C07D471/04 , A61K31/437 , A61P1/04
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，酰胺或酯，其中R 1表示氢原子或卤素原子; R 2表示氢原子等; R 3表示具有1至10个碳原子的烷基; 所述R 3的烷基被至少一个选自取代基α的取代基取代; 所述取代基α是芳基，羟基，氧代等; 所述芳基具有6至10个碳原子; 所述芳基是未取代的或被至少一个具有1至6个碳原子的烷基取代; 所述杂环基和所述杂环羰基的杂环部分，两个取代基α为含有1至4个选自氮原子，氧原子和硫原子的杂原子的5至10元环基这些化合物具有5-HT 受体结合活性，因此可用于治疗哺乳动物，特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。本发明还提供了包含上述化合物的药物组合物。

8. 发明授权

US08816090B2 Benzisoxazole derivatives 有权
标题翻译：苯并异恶唑衍生物
公开(公告)号：US08816090B2
公开(公告)日：2014-08-26
申请号：US11814588
申请日：2006-02-15
申请人： Hirohide Noguchi , Isao Sakurada , Chikara Uchida , Nobuaki Waizumi
发明人： Hirohide Noguchi , Isao Sakurada , Chikara Uchida , Nobuaki Waizumi
IPC分类号： C07D261/20 , A61K31/4439
CPC分类号： C07D413/12 , C07D413/14
摘要： This invention relates to compounds of the formula (I): wherein A, B, R1, R4, m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
摘要翻译：本发明涉及式（I）的化合物：其中A，B，R 1，R 4，m和n各自如本文所述或其药学上可接受的盐，以及含有这些化合物的组合物和这些化合物在治疗由5-HT4受体活性介导的病症，例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃肠疾病，恶心，中枢10神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心力衰竭和心律失常等心血管疾病，糖尿病和呼吸暂停综合征。

9. 发明授权

US06624162B2 Imidazopyridine compounds as 5-HT4 receptor modulators 失效
标题翻译：咪唑并吡啶化合物作为5-HT4受体调节剂
公开(公告)号：US06624162B2
公开(公告)日：2003-09-23
申请号：US10251109
申请日：2002-09-20
申请人： Chikara Uchida , Hirohide Noguchi , Alan Stobie , Geoffrey Gymer , David Fenwick
发明人： Chikara Uchida , Hirohide Noguchi , Alan Stobie , Geoffrey Gymer , David Fenwick
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R2 and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R2 and R3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8)n wherein n is an integer from 0 to 5. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R 1是氢，卤素或烷基; R 2和R 3独立地是氢，烷基，烯基，炔基，氨基烷基或羟烷基; 或R 2和R 3与它们所连接的氮原子一起可以形成环状的; R 4是氢，卤素，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 5是氢，卤素，烷基烯基，炔基，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 6是氢，烷基或烷氧基烷基; X是NR 9，其中R 9是氢或烷基; 并且Y是（CR 7 R 8）n，其中n是0至5的整数。这些化合物具有5-HT 4受体结合活性，因此可用于治疗胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。本发明还提供了包含上述化合物的药物组合物。

10. 发明授权

US09187463B2 Polymorph form of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid 有权
标题翻译： 4 - {[4 - （{[4-（2,2,2-三氟乙氧基）-1,2-苯并异恶唑-3-基]氧基}甲基）哌啶-1-基]甲基} - 四氢-2H- - 吡喃-4-羧酸
公开(公告)号：US09187463B2
公开(公告)日：2015-11-17
申请号：US14118377
申请日：2012-05-18
申请人： Toyoharu Numata , Hirohide Noguchi , Nobuaki Waizumi , Takashi Kojima
发明人： Toyoharu Numata , Hirohide Noguchi , Nobuaki Waizumi , Takashi Kojima
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.
摘要翻译：本发明涉及4 - {[4 - （{[4-（2,2,2-三氟乙氧基）-1,2-苯并异恶唑-3-基]氧基}甲基）哌啶-1-基] 甲基} - 四氢-2H-吡喃-4-羧酸。更具体地说，本发明涉及多晶型形式（多晶型I或多晶型II），以及制备含这种多晶型形式的组合物和使用方法。

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