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1. 发明申请

US20110105460A1 TRIAZOLE DERIVATIVE OR SALT THEREOF 有权
标题翻译：三唑衍生物或其盐
公开(公告)号：US20110105460A1
公开(公告)日：2011-05-05
申请号：US13002373
申请日：2009-07-02
申请人： Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
发明人： Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
IPC分类号： A61K31/4196 , C07D401/12 , A61K31/4439 , C07D249/08 , C07D403/12 , A61K31/506 , C07D413/12 , A61K31/422 , A61K31/4245 , A61K31/5377 , C07D417/12 , A61K31/541 , C07D405/12 , A61K31/427 , C07D413/14 , C07D409/04 , C07D403/10 , C07D471/04 , A61K31/437 , A61P3/10 , A61P25/24 , A61P25/18 , A61P25/28
CPC分类号： C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
摘要： [Problem] A compound, which can be used for preventing or treating diseases, in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided.[Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11β-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.
摘要翻译： [问题]提供了一种可用于预防或治疗疾病的化合物，其中涉及11种β-羟基类固醇脱氢酶（11＆bgr-HSD1），特别是糖尿病，胰岛素抵抗，痴呆，精神分裂症和抑郁症。 [解决方案]发现三唑环的3-和5-位之一具有（二）烷基甲基或环烷基的三唑衍生物，其各自被-O-（芳基或杂环）基团，其各自可以被取代，或低级亚烷基 - 环烷基），另一个具有可以被取代的芳基，杂环基或环烷基，或其药学上可接受的盐显示出有效的11β-HSD1抑制作用。由上可知，本发明的三唑衍生物可用于预防或治疗糖尿病，胰岛素抵抗，痴呆，精神分裂症和抑郁症。

2. 发明授权

US08377923B2 Triazole derivative or salt thereof 有权
标题翻译：三唑衍生物或其盐
公开(公告)号：US08377923B2
公开(公告)日：2013-02-19
申请号：US13002373
申请日：2009-07-02
申请人： Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
发明人： Seiji Yoshimura , Noriyuki Kawano , Tomoaki Kawano , Daisuke Sasuga , Takanori Koike , Hideyuki Watanabe , Hiroki Fukudome , Nobuyuki Shiraishi , Ryosuke Munakata , Hiroaki Hoshii , Kayoko Mihara
IPC分类号： A01N43/00 , A01N43/58 , A61K31/55 , C07D241/36 , C07D249/08 , C07D249/14
CPC分类号： C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/10 , C07D417/12
摘要： [Problem] A compound, which can be used for preventing or treating diseases, in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided.[Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11β-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.
摘要翻译： [问题]提供了一种可用于预防或治疗疾病的化合物，其中涉及11种β-羟基类固醇脱氢酶（11＆bgr-HSD1），特别是糖尿病，胰岛素抵抗，痴呆，精神分裂症和抑郁症。 [解决方案]发现三唑环的3-和5-位之一具有（二）烷基甲基或环烷基的三唑衍生物，其各自被-O-（芳基或杂环）基团，其各自可以被取代，或低级亚烷基 - 环烷基），另一个具有可以被取代的芳基，杂环基或环烷基，或其药学上可接受的盐显示出有效的11β-HSD1抑制作用。由上可知，本发明的三唑衍生物可用于预防或治疗糖尿病，胰岛素抵抗，痴呆，精神分裂症和抑郁症。

3. 发明申请

US20090082367A1 TRIAZOLE DERIVATIVE OR A SALT THEREOF 审中-公开
标题翻译：三唑衍生物或其盐
公开(公告)号：US20090082367A1
公开(公告)日：2009-03-26
申请号：US12293214
申请日：2007-03-14
申请人： Seiji Yoshimura , Ryota Shiraki , Tomoaki Kawano , Daisuke Sasuga , Mitsuru Hosaka , Hiroki Fukudome , Kazuo Kurosawa , Hirofumi Ishii , Takanori Koike
发明人： Seiji Yoshimura , Ryota Shiraki , Tomoaki Kawano , Daisuke Sasuga , Mitsuru Hosaka , Hiroki Fukudome , Kazuo Kurosawa , Hirofumi Ishii , Takanori Koike
IPC分类号： A61K31/4196 , C07D401/06 , A61K31/4439 , A61K31/497 , A61P3/10 , A61K31/4709 , C07D403/06
CPC分类号： C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/08 , C07D409/06 , C07D409/08 , C07D409/12 , C07D413/06 , C07D417/06
摘要： [Problem] To provide a compound which may be used in treating diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is concerned, especially diabetes and insulin resistance.[Means for Solution] It was found that a triazole derivative or a pharmaceutically acceptable salt thereof, in which the 3-position of triazole ring is substituted with a trisubstituted methyl group and the 5-position is substituted with a lower alkyl, cycloalkyl or the like, has a strong 11β-HSD1-inhibitory activity. In addition, since the triazole derivative of the present invention shows excellent blood glucose-lowering action, it may be used in the treatment of diabetes and insulin resistance.
摘要翻译： [问题]提供可用于治疗其中涉及11β-羟类固醇脱氢酶1型（11beta-HSD1）的疾病的化合物，特别是糖尿病和胰岛素抵抗。 [解决方法]发现三唑环的3-位被三取代甲基取代的三唑衍生物或其药学上可接受的盐，并且5位被低级烷基，环烷基或具有强的11beta-HSD1抑制活性。此外，由于本发明的三唑衍生物显示出优异的降血糖作用，因此可用于治疗糖尿病和胰岛素抵抗。

4. 发明申请

US20070259854A1 Triazole Derivative or Salt Thereof 有权
标题翻译：三唑衍生物或其盐
公开(公告)号：US20070259854A1
公开(公告)日：2007-11-08
申请号：US11663089
申请日：2005-09-14
申请人： Takeshi Murakami , Tomoaki Kawano , Ryota Shiraki , Hirofumi Ishii , Seiji Yoshimura , Takehiko Ohkawa , Mitsuru Hosaka , Hiroki Fukudome , Yutaka Inoki
发明人： Takeshi Murakami , Tomoaki Kawano , Ryota Shiraki , Hirofumi Ishii , Seiji Yoshimura , Takehiko Ohkawa , Mitsuru Hosaka , Hiroki Fukudome , Yutaka Inoki
IPC分类号： A61K31/4196 , A61K31/55 , A61P7/12 , C07D223/00 , C07D249/08
CPC分类号： C07D409/14 , C07D249/08 , C07D401/04 , C07D401/08 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/06 , C07D409/08 , C07D417/12 , C07D471/04 , C07D487/04
摘要： [Problem] There is provided a compound which can be used for therapy of diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) participates, in particular diabetes, insulin resistance. [Means for Solution] It has been found that a triazole derivative wherein the triazole ring is substituted with a trisubstituted methyl group in the 2-position or a pharmaceutically acceptable salt thereof has a strong 11β-HSD1 inhibitory activity. Moreover, the triazole derivative of the invention exhibits an excellent blood-glucose level-lowering action and hence can be used for therapy of diabetes, insulin resistance.
摘要翻译： [问题]提供了可用于治疗其中参与了11β-羟类固醇脱氢酶1型（11beta-HSD1）的疾病的化合物，特别是糖尿病，胰岛素抵抗。 [解决方案]已经发现，其中三唑环被2-位上的三取代甲基或其药学上可接受的盐取代的三唑衍生物具有强的11beta-HSD1抑制活性。此外，本发明的三唑衍生物显示出优异的血糖降低作用，因此可用于治疗糖尿病，胰岛素抵抗。

5. 发明授权

US07776897B2 Triazole derivative or salt thereof 有权
标题翻译：三唑衍生物或其盐
公开(公告)号：US07776897B2
公开(公告)日：2010-08-17
申请号：US11663089
申请日：2005-09-14
申请人： Takeshi Murakami , Tomoaki Kawano , Ryota Shiraki , Hirofumi Ishii , Seiji Yoshimura , Takehiko Ohkawa , Mitsuru Hosaka , Hiroki Fukudome , Yutaka Inoki
发明人： Takeshi Murakami , Tomoaki Kawano , Ryota Shiraki , Hirofumi Ishii , Seiji Yoshimura , Takehiko Ohkawa , Mitsuru Hosaka , Hiroki Fukudome , Yutaka Inoki
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： C07D409/14 , C07D249/08 , C07D401/04 , C07D401/08 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/06 , C07D409/08 , C07D417/12 , C07D471/04 , C07D487/04
摘要： There is provided a compound which can be used for therapy of diseases in which 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) participates, in particular diabetes, insulin resistance.It has been found that a triazole derivative wherein the triazole ring is substituted with a trisubstituted methyl group in the 2-position or a pharmaceutically acceptable salt thereof has a strong 11β-HSD1 inhibitory activity. Moreover, the triazole derivative of the invention exhibits an excellent blood-glucose level-lowering action and hence can be used for therapy of diabetes, insulin resistance.
摘要翻译：提供了一种化合物，其可以用于治疗其中参与的11β-羟基类固醇脱氢酶（11＆bgr--HSD1）的疾病，特别是糖尿病，胰岛素抵抗。已经发现，其中三唑环被2-位上的三取代的甲基或其药学上可接受的盐取代的三唑衍生物具有强的11β-HSD1抑制活性。此外，本发明的三唑衍生物显示出优异的血糖降低作用，因此可用于治疗糖尿病，胰岛素抵抗。

6. 发明申请

US20120046292A1 DIACYLETHYLENEDIAMINE COMPOUND 审中-公开
标题翻译：二乙烯基胺化合物
公开(公告)号：US20120046292A1
公开(公告)日：2012-02-23
申请号：US13263258
申请日：2010-04-19
申请人： Tomoaki Kawano , Yasuhiro Yonetoku , Takeshi Hanazawa , Takahiro Nigawara , Hiroki Fukudome , Hiroshi Moritani
发明人： Tomoaki Kawano , Yasuhiro Yonetoku , Takeshi Hanazawa , Takahiro Nigawara , Hiroki Fukudome , Hiroshi Moritani
IPC分类号： A61K31/197 , C07D307/79 , A61K31/343 , A61P3/04 , A61K31/495 , C07D239/42 , A61K31/498 , A61K31/5375 , C07C229/38 , C07D295/155
CPC分类号： C07D207/06 , C07B2200/05 , C07C233/62 , C07C235/46 , C07C235/50 , C07C235/84 , C07C237/34 , C07C255/46 , C07C271/20 , C07C275/26 , C07C275/28 , C07C307/06 , C07C311/51 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/18 , C07C2602/42 , C07C2602/44 , C07D209/08 , C07D209/42 , C07D209/44 , C07D211/16 , C07D211/18 , C07D211/32 , C07D211/34 , C07D211/38 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/60 , C07D211/62 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/54 , C07D217/02 , C07D217/06 , C07D217/26 , C07D231/14 , C07D231/22 , C07D239/28 , C07D239/42 , C07D241/04 , C07D241/42 , C07D257/04 , C07D263/32 , C07D263/34 , C07D263/48 , C07D271/06 , C07D271/10 , C07D275/02 , C07D277/20 , C07D277/56 , C07D277/68 , C07D295/14 , C07D295/155 , C07D295/18 , C07D295/20 , C07D295/205 , C07D307/79 , C07D309/06 , C07D317/46 , C07D317/72 , C07D319/18 , C07D333/38 , C07D333/54 , C07D333/68 , C07D333/70 , C07D409/12 , C07D451/02 , C07D495/04
摘要： [Problem]A compound which is useful as an anti-obesity agent is provided.[Means for Solution]The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.
摘要翻译： [问题]提供了可用作抗肥胖剂的化合物。 [解决方案]本发明人研究了具有DGAT1抑制作用的化合物，其有希望作为用于治疗肥胖，II型糖尿病，脂肪肝和与这些疾病相关的疾病的药物组合物的活性成分，以及作为结果发现本发明的二酰亚乙基二胺化合物具有优异的DGAT1抑制作用，从而完成了本发明。也就是说，本发明的二酰亚胺二胺化合物具有DGAT1抑制作用，因此可以用作预防和/或治疗肥胖，II型糖尿病，脂肪肝和与这些疾病相关的疾病的药剂。

7. 发明申请

US20050003015A1 Process for producing granules containing branched amino acids 有权
标题翻译：生产含有支链氨基酸的颗粒的方法
公开(公告)号：US20050003015A1
公开(公告)日：2005-01-06
申请号：US10897000
申请日：2004-07-23
申请人： Hidetoshi Sakai , Mitsuyasu Ida , Chisato Makino , Tomoaki Kawano , Akira Yabuki
发明人： Hidetoshi Sakai , Mitsuyasu Ida , Chisato Makino , Tomoaki Kawano , Akira Yabuki
IPC分类号： A61J3/06 , A61K9/00 , A61K9/16 , A61K31/198 , A61K47/04 , A61K47/12 , A61P1/16 , A61K9/14
CPC分类号： A61K9/0095 , A61K9/1617 , A61K9/1635 , A61K31/198
摘要： The problem of the present invention is to provide pharmaceutical granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine, which has a smaller specific volume than conventional products, and a production method thereof. As a result of intensive studies, granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine and a production method thereof have been provided, which are characterized by adding an acid to a particle mixture of three kinds of branched chain amino acids of isoleucine, leucine and valine and granulating the mixture, which has solved the above-mentioned problem.
摘要翻译：本发明的问题是提供含有作为活性氨基酸成分的异氰酸，亮氨酸，缬氨酸三种支链氨基酸的药物颗粒，其具有比常规产品更小的比容量及其制备方法。作为深入研究的结果，提供了含有作为活性氨基酸成分的异亮氨酸，亮氨酸和缬氨酸的三种支链氨基酸的颗粒及其制备方法，其特征在于将酸添加到 3种异亮氨酸，亮氨酸，缬氨酸的支链氨基酸，混合造粒，解决了上述问题。

8. 发明申请

US20050032855A1 Tetrahydro-2H-thiopyran-4-carboxamide derivative 有权
公开(公告)号：US20050032855A1
公开(公告)日：2005-02-10
申请号：US10912232
申请日：2004-08-06
申请人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
发明人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
IPC分类号： A61P31/22 , C07D335/02 , C07D413/12 , A61K31/4245 , A61K31/422 , C07D413/02
CPC分类号： C07D335/02 , C07D413/12
摘要： A pharmaceutical drug, particularly a novel compound useful for the prophylaxis or therapeutic treatment of various diseases involving infections with viruses of the Herpesviridae family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. N-{2-[(4-Substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative where the phenyl group is substituted at position 4 with a specific five-membered or 6-membered heteroaryl group, has such great anti-virus activity that the oral dosing thereof at a low dose enabled the therapeutic treatment of the diseases.

9. 发明授权

US07465748B2 Amide derivative 有权
标题翻译：酰胺衍生物
公开(公告)号：US07465748B2
公开(公告)日：2008-12-16
申请号：US10567565
申请日：2004-08-05
申请人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
发明人： Toru Kontani , Junji Miyata , Wataru Hamaguchi , Tomoaki Kawano , Akio Kamikawa , Hiroshi Suzuki , Kenji Sudo
IPC分类号： A61K31/41 , C07D271/06
CPC分类号： C07D335/02 , C07D413/12
摘要： There is provided a pharmaceutical drug, particularly a novel compound useful for prophylaxis or a therapeutic treatment of various diseases involving infections with viruses of the herpesvirus family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection.An N-{2-[(4-substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative, of which phenyl group is substituted at position 4 with a specific 5- or 6-membered heteroaryl group, and a salt thereof have an effective anti-virus activity, and the oral administration thereof at a low dose enabled the therapeutic treatment of the above diseases.
摘要翻译：提供药物，特别是可用于预防或治疗涉及疱疹病毒家族病毒感染的各种疾病的新型化合物，特别是各种疱疹病毒感染如通过水痘带状疱疹病毒的水痘（水痘），水痘带状疱疹经由复发通过HSV-1和生殖器疱疹通过HSV-2感染感染潜伏性水痘带状疱疹病毒，唇疱疹和疱疹脑炎。 N-（2 - [（4-取代苯基）氨基] -2-氧代乙基}四氢-2H-噻喃-4-甲酰胺衍生物，其苯基在4位被特定的5或6元杂芳基取代基团和其盐具有有效的抗病毒活性，并且以低剂量口服给药能够治疗上述疾病。

10. 发明授权

US07138142B2 Process for producing granules containing branched amino acids 有权
标题翻译：生产含有支链氨基酸的颗粒的方法
公开(公告)号：US07138142B2
公开(公告)日：2006-11-21
申请号：US10897000
申请日：2004-07-23
申请人： Hidetoshi Sakai , Mitsuyasu Ida , Chisato Makino , Tomoaki Kawano , Akira Yabuki
发明人： Hidetoshi Sakai , Mitsuyasu Ida , Chisato Makino , Tomoaki Kawano , Akira Yabuki
IPC分类号： A61K9/14 , A61K9/50
CPC分类号： A61K9/0095 , A61K9/1617 , A61K9/1635 , A61K31/198
摘要： The problem of the present invention is to provide pharmaceutical granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine, which has a smaller specific volume than conventional products, and a production method thereof. As a result of intensive studies, granules containing, as active amino acid ingredients, three kinds of branched chain amino acids of isoleucine, leucine and valine and a production method thereof have been provided, which are characterized by adding an acid to a particle mixture of three kinds of branched chain amino acids of isoleucine, leucine and valine and granulating the mixture, which has solved the above-mentioned problem.
摘要翻译：本发明的问题是提供含有作为活性氨基酸成分的异氰酸，亮氨酸，缬氨酸三种支链氨基酸的药物颗粒，其具有比常规产品更小的比容量及其制备方法。作为深入研究的结果，提供了含有作为活性氨基酸成分的异亮氨酸，亮氨酸和缬氨酸的三种支链氨基酸的颗粒及其制备方法，其特征在于将酸添加到 3种异亮氨酸，亮氨酸，缬氨酸的支链氨基酸，混合造粒，解决了上述问题。

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