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1. 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。

2. 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。

3. 发明授权

US08809380B2 Picolinamide derivatives as TTX-S blockers 有权
标题翻译：吡啶酰胺衍生物作为TTX-S阻断剂
公开(公告)号：US08809380B2
公开(公告)日：2014-08-19
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： A61K31/4439
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。

4. 发明申请

US20080255113A1 Quinolonecarboxylic Acid Compounds Having 5-Ht4 Receptor Agonistic Activity 失效
标题翻译：具有5-Ht4受体激活活性的喹诺酮羧酸化合物
公开(公告)号：US20080255113A1
公开(公告)日：2008-10-16
申请号：US10595948
申请日：2004-11-10
申请人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
发明人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
IPC分类号： A61K31/5377 , C07D405/14 , A61K31/4709 , C07D401/12 , C07D401/14 , C07D413/14
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic 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.
摘要翻译：本发明提供式（I）化合物：其中Het表示具有一个氮原子的杂环基团，B直接与该碳原子结合，并且具有4至7个碳原子，所述杂环基团未被取代或被1至4个取代基取代独立地选自取代基α1， A表示具有1至4个碳原子的亚烷基; B表示共价键或具有1至5个碳原子的亚烷基; R 1表示异丙基，正丙基或环戊基; R 2表示甲基，氟原子或氯原子; R 3独立地表示（i）氧代基，羟基，氨基，烷基氨基或羧基; （ii）具有3至8个碳原子的环烷基，所述环烷基被1至5个取代基取代，或（iii）具有3至8个原子的杂环基，所述杂环基未被取代或被1 至5个取代基，n为1,2或3，或其药学上可接受的盐。这些化合物具有5-HT 4受体激动活性，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。

5. 发明授权

US07964727B2 Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity 失效
标题翻译：具有5-HT 4受体激动活性的喹诺酮羧酸化合物
公开(公告)号：US07964727B2
公开(公告)日：2011-06-21
申请号：US10595948
申请日：2004-11-10
申请人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
发明人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
IPC分类号： C07D221/02 , C07D215/00 , C07D413/00 , A01N43/40 , A01N43/42 , A61K31/435 , A61K31/44
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic 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.
摘要翻译：本发明提供式（I）化合物：其中Het表示具有一个氮原子的杂环基团，B直接与该碳原子结合，并且具有4至7个碳原子，所述杂环基团未被取代或被1至4个取代基取代独立地选自取代基α1; A表示具有1至4个碳原子的亚烷基; B表示共价键或具有1至5个碳原子的亚烷基; R1表示异丙基，正丙基或环戊基; R2表示甲基，氟原子或氯原子; R3独立地表示（i）氧代基，羟基，氨基，烷基氨基或羧基; （ii）具有3至8个碳原子的环烷基，所述环烷基被1至5个取代基取代，或（iii）具有3至8个原子的杂环基，所述杂环基未被取代或被1 至5个取代基，n为1,2或3，或其药学上可接受的盐。这些化合物具有5-HT 4受体激动活性，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。

6. 发明授权

US06979690B2 Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators 失效
公开(公告)号：US06979690B2
公开(公告)日：2005-12-27
申请号：US10337497
申请日：2003-01-07
申请人： Geoffrey Gymer , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita , Alan Stobie , Chikara Uchida , Seiji Nukui
发明人： Geoffrey Gymer , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita , Alan Stobie , Chikara Uchida , Seiji Nukui
IPC分类号： A61K31/4545 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/10 , A61P1/14 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/22 , A61P25/28 , A61P43/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , A61K31/445
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14
摘要： This invention provides compounds of the formula (I) and (II): or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R1 is hydrogen or halo; R2 and R3 are independently hydrogen or C1-6 alkyl; R4 and R5 are independently hydrogen or C1-6 alkyl; R6 is hydrogen, C1-12 alkyl, C1-6 alkoxy (C1-6)alkyl or C1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R7 and R8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R9 is C1-6 alkyl or C3-8 cycloalkyl; R10 is C1-6 alkyl or NR11R12; L is (CR11R12)n or NR11; M is NR11 or (CR11R12)n; R11 and R12 are independently hydrogen or C1-6 alkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C1-6 alkyl; with the proviso that when R9 is C1-6 alkyl, L is not NR11. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

7. 发明授权

US4543208A Magnetic core and method of producing the same 失效
标题翻译：磁芯及其制造方法
公开(公告)号：US4543208A
公开(公告)日：1985-09-24
申请号：US564847
申请日：1983-12-23
申请人： Hiromichi Horie , Mikio Morita , Itsuo Arima
发明人： Hiromichi Horie , Mikio Morita , Itsuo Arima
IPC分类号： B22F1/00 , C22C32/00 , H01F1/26 , H01F27/255 , C04B35/04 , H01F27/24
CPC分类号： C22C32/0094 , B22F1/0059 , H01F1/26 , H01F27/255
摘要： Disclosed is an magnetic core comprising a molded product made of an iron powder and/or an iron alloy magnetic powder having a mean particle size of 10 to 100 .mu.m, and 1.5 to 40%, as a total amount in terms of volume ratio, of an insulating binder resin and an insulating inorganic compound powder. Also disclosed is a useful method of producing the magnetic core.
摘要翻译：公开了一种磁芯，其包括由铁粉和/或平均粒径为10〜100μm的铁合金磁性粉末和1.5〜40％的以体积比计的总量的成型体，的绝缘粘合剂树脂和绝缘无机化合物粉末。还公开了制造磁芯的有用方法。

8. 发明授权

US09101616B2 Aryl substituted carboxamide derivatives as calcium or sodium channel blockers 有权
标题翻译：芳基取代的甲酰胺衍生物作为钙或钠通道阻断剂
公开(公告)号：US09101616B2
公开(公告)日：2015-08-11
申请号：US13375117
申请日：2010-05-31
申请人： Tadashi Inoue , Shuzo Watanabe , Tatsuya Yamagishi , Yoshimasa Arano , Mikio Morita , Kaoru Shimada
发明人： Tadashi Inoue , Shuzo Watanabe , Tatsuya Yamagishi , Yoshimasa Arano , Mikio Morita , Kaoru Shimada
IPC分类号： A61K31/498 , C07D401/12 , C07D213/65 , C07D241/18 , A61K31/497 , A61K31/444 , A61K31/44 , A61K31/4965 , A61K31/4439 , A61K31/4709 , C07D413/12 , A61K31/4725 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4706 , A61K31/506 , C07D215/40 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
CPC分类号： A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4706 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/506 , C07D213/65 , C07D215/40 , C07D241/18 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as NaV1.3 and NaV1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or 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 T-type calcium channels or voltage gated sodium channels are involved.
摘要翻译：本发明涉及式（I）的芳基取代的甲酰胺衍生物或其药学上可接受的盐，其具有作为河豚毒素敏感型（TTX-S）阻滞剂如NaV1的T型钙通道或电压门控钠通道的阻断活性 3和NaV1.7，其可用于治疗或预防其中涉及T型钙通道或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T型钙通道或电压门控钠通道的疾病中的用途。

9. 发明授权

US08466166B2 Benzimidazole derivatives as selective acid pump inhibitors 有权
标题翻译：苯并咪唑衍生物作为选择性酸泵抑制剂
公开(公告)号：US08466166B2
公开(公告)日：2013-06-18
申请号：US12442277
申请日：2007-09-17
申请人： Hiroki Koike , Mikio Morita
发明人： Hiroki Koike , Mikio Morita
IPC分类号： A61K31/44 , A61K31/445 , A61K31/41
CPC分类号： C07D491/052 , C07D491/14
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zolliπger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中：R 1，R 2，R 3，R 4，A和E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治疗和使用方法，包括用于治疗由酸泵拮抗活性介导的病症的化合物，例如但不限于胃肠道疾病，胃食管疾病，胃食管反流病（GERD），喉咽反流病，消化性溃疡，胃溃疡，十二指肠溃疡，NSAID诱发的溃疡，胃炎，幽门螺杆菌感染，消化不良，功能性消化不良，佐里皮埃里森综合征，非侵蚀性反流病（NERD），内脏痛，癌症，胃灼热，恶心，食管炎，吞咽困难，过度激活，气道障碍或哮喘。

10. 发明授权

US5977295A Continuous process for preparing polytetrafluoroethylene wet powder 失效
标题翻译：连续制备聚四氟乙烯湿粉
公开(公告)号：US5977295A
公开(公告)日：1999-11-02
申请号：US134851
申请日：1993-10-12
申请人： Tetsuya Higuchi , Shunichi Nomura , Shigeru Ichiba , Hiroshi Yamaguchi , Masaomi Goromaru , Akira Watanabe , Kazuhiro Takeda , Mikio Morita , Kazuhisa Fujita , Yasuyuki Moriyama
发明人： Tetsuya Higuchi , Shunichi Nomura , Shigeru Ichiba , Hiroshi Yamaguchi , Masaomi Goromaru , Akira Watanabe , Kazuhiro Takeda , Mikio Morita , Kazuhisa Fujita , Yasuyuki Moriyama
IPC分类号： C08J3/16 , C08F6/14 , C08J3/05
CPC分类号： C08J3/16 , C08J2327/18
摘要： A process for continuously preparing a wet powder of PTFE, comprising the step of continuously slurrying a PTFE aqueous dispersion with a high shear machine having a rotating element, and the step of continuously granulating the slurry by using vertical agitator. The process can be carried out for a long time without trouble, and can continuously provide a dry powder having good powder properties. The powder properties can be controlled by regulating operation conditions.
摘要翻译：一种用于连续制备PTFE湿粉的方法，包括用具有旋转元件的高剪切机连续制备PTFE水分散体的步骤，以及通过使用立式搅拌器使浆料连续造粒的步骤。该方法可长时间无故障地进行，并可连续提供具有良好粉末性能的干粉。粉末特性可以通过调节操作条件来控制。

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