公开(公告)号：US08163746B2

公开(公告)日：2012-04-24

申请号：US12297275

申请日：2007-04-19

申请人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Matsuzawa ,  Ryushi Seo ,  Hironori Harada ,  Akira Suga ,  Tomoaki Abe ,  Hidenori Azami ,  Shunichiro Matsumoto ,  Takashi Shin ,  Masayuki Tanahashi ,  Toru Watanabe

发明人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Matsuzawa ,  Ryushi Seo ,  Hironori Harada ,  Akira Suga ,  Tomoaki Abe ,  Hidenori Azami ,  Shunichiro Matsumoto ,  Takashi Shin ,  Masayuki Tanahashi ,  Toru Watanabe

IPC分类号： A61K31/5355 ,  A61K31/496 ,  A61K31/451 ,  A61K31/4535 ,  A61K31/426 ,  C07D413/14 ,  C07D211/32 ,  C07D211/46 ,  C07D277/24

CPC分类号： C07D277/56 ,  C07D263/34 ,  C07D263/48 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/08

摘要： Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.

摘要翻译： 提供治疗或预防与膀胱过度活动相关的尿频，尿急和尿失禁的药物，诸如间质性膀胱炎的下尿路疾病和伴有下尿路疼痛的慢性前列腺炎以及伴有疼痛的各种疾病。 通过甲酰胺将唑环或吡唑环或吡啶环或吡啶环与吡唑或恶唑等唑类结合的新型偶氮甲酰胺衍生物被证实具有强的trkA受体抑制活性，被发现是用于治疗或预防较低 泌尿道疾病，伴有疼痛的各种疾病，其功效和安全性优异，从而完成了本发明。

公开(公告)号：US20090286766A1

公开(公告)日：2009-11-19

申请号：US12297275

申请日：2007-04-19

申请人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Matsuzawa ,  Ryushi Seo ,  Hironori Harada ,  Akira Suga ,  Tomoaki Abe ,  Hidenori Azami ,  Shunichiro Matsumoto ,  Takashi Shin ,  Masayuki Tanahashi ,  Toru Watanabe

发明人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Matsuzawa ,  Ryushi Seo ,  Hironori Harada ,  Akira Suga ,  Tomoaki Abe ,  Hidenori Azami ,  Shunichiro Matsumoto ,  Takashi Shin ,  Masayuki Tanahashi ,  Toru Watanabe

IPC分类号： A61K31/496 ,  C07D417/12 ,  C07D487/04 ,  C07D417/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/55 ,  A61K31/541 ,  A61P13/00

CPC分类号： C07D277/56 ,  C07D263/34 ,  C07D263/48 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/08

摘要： Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.

摘要翻译： 本发明提供一种治疗或预​​防尿频，尿急，尿失禁，与膀胱过度活动，下尿路疾病如间质性膀胱炎和伴有下尿路疼痛的慢性前列腺炎以及伴有疼痛的各种疾病相关的尿失禁。 通过甲酰胺将唑环或吡唑环或吡啶环或吡啶环与吡唑或恶唑等唑类结合的新型偶氮甲酰胺衍生物被证实具有强的trkA受体抑制活性，被发现是用于治疗或预防较低 泌尿道疾病，伴有疼痛的各种疾病，其功效和安全性优异，从而完成了本发明。

公开(公告)号：US08304547B2

公开(公告)日：2012-11-06

申请号：US12739433

申请日：2008-10-23

申请人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Nomura ,  Shunichiro Matsumoto ,  Takashi Shin ,  Hidenori Azami ,  Tomoaki Abe ,  Akira Suga ,  Ryushi Seo ,  Masayuki Tanahashi ,  Toru Watanabe

发明人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Nomura ,  Shunichiro Matsumoto ,  Takashi Shin ,  Hidenori Azami ,  Tomoaki Abe ,  Akira Suga ,  Ryushi Seo ,  Masayuki Tanahashi ,  Toru Watanabe

IPC分类号： C07D211/68 ,  C07D221/20 ,  C07D491/20 ,  C07D413/14 ,  C07D239/09 ,  A61K31/535 ,  A61K31/505 ,  A61K31/44 ,  A61K31/445

CPC分类号： C07D263/34 ,  C07D263/48 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D498/10

摘要： [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.[Means for Solution] A novel azolecarboxamide compound in which a thiazole ring or an oxazole ring is bonded to a benzene ring, a pyridine ring, a pyridazine ring, a thiophene ring, a pyrazole ring or a pyrrole ring through carboxamide, or a salt thereof is confirmed to have a potent trkA receptor inhibitory activity, and found to be capable of being used as a therapeutic and/or prophylactic agent which is excellent in efficacy and safety for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, thereby completing the present invention.

摘要翻译： 本发明提供一种用于与各种下尿路疾病（包括膀胱过度活动症，伴有下尿路疼痛，诸如间质性膀胱炎等）的各种下尿路疾病相关的尿频，尿急和尿失禁的治疗和/或预防剂， 慢性前列腺炎等，以及伴有疼痛的各种疾病，基于优异的trkA受体抑制作用。 [解决方案]通过甲酰胺或其盐将噻唑环或恶唑环与苯环，吡啶环，哒嗪环，噻吩环，吡唑环或吡咯环结合的新型偶氮甲酰胺化合物 被证实具有强的trkA受体抑制活性，发现能够用作治疗和/或预防剂，其对于尿频，尿急和与各种下尿路相关的尿失禁的功效和安全性优异 包括膀胱活动过度，伴有尿路下下尿路疼痛的下尿路疾病，如间质性膀胱炎，慢性前列腺炎等多种疾病，伴有疼痛的各种疾病，从而完成本发明。

公开(公告)号：US20100249088A1

公开(公告)日：2010-09-30

申请号：US12739433

申请日：2008-10-23

申请人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Nomura ,  Shunichiro Matsumoto ,  Takashi Shin ,  Hidenori Azami ,  Tomoaki Abe ,  Akira Suga ,  Ryushi Seo ,  Masayuki Tanahashi ,  Toru Watanabe

发明人： Keizo Sugasawa ,  Kenichi Kawaguchi ,  Takaho Nomura ,  Shunichiro Matsumoto ,  Takashi Shin ,  Hidenori Azami ,  Tomoaki Abe ,  Akira Suga ,  Ryushi Seo ,  Masayuki Tanahashi ,  Toru Watanabe

IPC分类号： A61K31/4545 ,  C07D413/14 ,  C07D417/14 ,  A61P13/02 ,  A61P13/10 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K31/397 ,  A61P13/00 ,  A61P13/08

CPC分类号： C07D263/34 ,  C07D263/48 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D498/10

摘要： [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.[Means for Solution] A novel azolecarboxamide compound in which a thiazole ring or an oxazole ring is bonded to a benzene ring, a pyridine ring, a pyridazine ring, a thiophene ring, a pyrazole ring or a pyrrole ring through carboxamide, or a salt thereof is confirmed to have a potent trkA receptor inhibitory activity, and found to be capable of being used as a therapeutic and/or prophylactic agent which is excellent in efficacy and safety for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, thereby completing the present invention.

摘要翻译： 本发明提供一种用于与各种下尿路疾病（包括膀胱过度活动症，伴有下尿路疼痛，诸如间质性膀胱炎等）的各种下尿路疾病相关的尿频，尿急和尿失禁的治疗和/或预防剂， 慢性前列腺炎等，以及伴有疼痛的各种疾病，基于优异的trkA受体抑制作用。 [解决方案]通过甲酰胺或其盐将噻唑环或恶唑环与苯环，吡啶环，哒嗪环，噻吩环，吡唑环或吡咯环结合的新型偶氮甲酰胺化合物 被证实具有强的trkA受体抑制活性，发现能够用作治疗和/或预防剂，其对于尿频，尿急和与各种下尿路相关的尿失禁的功效和安全性优异 包括膀胱活动过度，伴有尿路下下尿路疼痛的下尿路疾病，如间质性膀胱炎，慢性前列腺炎等多种疾病，伴有疼痛的各种疾病，从而完成本发明。

公开(公告)号：US07585886B2

公开(公告)日：2009-09-08

申请号：US11662539

申请日：2006-05-18

申请人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

发明人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

IPC分类号： C07D207/00 ,  A61K31/40

CPC分类号： C07D207/09 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D417/06 ,  C07D417/10

摘要： [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).

摘要翻译： [问题]提供可用于治疗其中涉及钙感觉受体（CaSR）的疾病的化合物，特别是甲状旁腺机能亢进。 [解决方法]发现以芳基烷基等取代的氨甲基为特征的新型吡咯烷衍生物或其盐具有优异的CaSR激动调节活性，并且对于CYP2D6抑制活性也具有优异的选择性，具有 引起药物相互作用的可能性。 基于上述，这些新型吡咯烷衍生物可用作治疗涉及CaSR的疾病（甲状旁腺功能亢进，肾性骨营养不良，高钙血症等）的治疗剂。

公开(公告)号：US20090062366A1

公开(公告)日：2009-03-05

申请号：US11662539

申请日：2006-05-18

申请人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

发明人： Shunichiro Hachiya ,  Makoto Oku ,  Hana Mukai ,  Takashi Shin ,  Keisuke Matsuura ,  Ryushi Seo ,  Takashi Kamikubo ,  Yoh Terada ,  Masanao Sanagi ,  Kousei Yoshihara ,  Taisuke Takahashi

IPC分类号： A61K31/40 ,  C07D207/04

CPC分类号： C07D207/09 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D417/06 ,  C07D417/10

摘要： [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism.[Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).

公开(公告)号：US07960562B2

公开(公告)日：2011-06-14

申请号：US11887384

申请日：2006-03-30

申请人： Masaaki Hirano ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Eiji Kawaminami ,  Kei Ohnuki ,  Hirofumi Yamamoto ,  Kazuhiko Osoda ,  Tatsuhisa Takahashi ,  Takashi Shin ,  Takanori Koike ,  Itsuro Shimada ,  Hiroyuki Hisamichi ,  Toshiyuki Kusayama

发明人： Masaaki Hirano ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Eiji Kawaminami ,  Kei Ohnuki ,  Hirofumi Yamamoto ,  Kazuhiko Osoda ,  Tatsuhisa Takahashi ,  Takashi Shin ,  Takanori Koike ,  Itsuro Shimada ,  Hiroyuki Hisamichi ,  Toshiyuki Kusayama

IPC分类号： A61K31/4184 ,  C07D235/12

CPC分类号： C07D235/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.

摘要翻译： 旨在提供可用作GnRH受体拮抗剂的化合物。 本发明人进一步研究了丙烷-1,3-二酮衍生物。 结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。 因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。 此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

公开(公告)号：US20090181964A1

公开(公告)日：2009-07-16

申请号：US11887384

申请日：2006-03-30

申请人： Masaaki Hirano ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Eiji Kawaminami ,  Kei Ohnuki ,  Hirofumi Yamamoto ,  Kazuhiko Osoda ,  Tatsuhisa Takahisa ,  Takashi Shin ,  Takanori Koike ,  Itsuro Shimada ,  Hiroyuki Hisamichi ,  Toshiyuki Kusayama

发明人： Masaaki Hirano ,  Isao Kinoyama ,  Shunichiro Matsumoto ,  Eiji Kawaminami ,  Kei Ohnuki ,  Hirofumi Yamamoto ,  Kazuhiko Osoda ,  Tatsuhisa Takahisa ,  Takashi Shin ,  Takanori Koike ,  Itsuro Shimada ,  Hiroyuki Hisamichi ,  Toshiyuki Kusayama

IPC分类号： A61K31/5377 ,  C07D235/04 ,  A61K31/4184 ,  C07D401/02 ,  A61K31/4439 ,  C07D403/02 ,  A61K31/496 ,  C07D413/14 ,  A61K31/506 ,  A61K31/501 ,  A61P35/00

CPC分类号： C07D235/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.

摘要翻译： 旨在提供可用作GnRH受体拮抗剂的化合物。 本发明人进一步研究了丙烷-1,3-二酮衍生物。 结果证实，在具有2-（1,3-二氢-2H-苯并咪唑）的丙烷-1,3-二酮衍生物中具有被-SO 2 -R 3表示的基团取代的苯环或噻吩环的化合物 -2-亚基）具有优异的GnRH受体拮抗作用，完成了本发明。 因为本发明的化合物具有强的GnRH受体拮抗作用，因此可用于治疗性激素依赖性疾病，特别是GnRH相关疾病。 此外，由于本发明的化合物在人体中具有优异的代谢稳定性，药物相互作用少，因此作为上述疾病的药物具有优选的特性。

公开(公告)号：US5354685A

公开(公告)日：1994-10-11

申请号：US40184

申请日：1993-03-29

申请人： Sawao Murao ,  Takashi Shin ,  Kyoichi Sugawa ,  Amachi Teruo

发明人： Sawao Murao ,  Takashi Shin ,  Kyoichi Sugawa ,  Amachi Teruo

IPC分类号： A01N63/02 ,  A01N63/00 ,  C07G99/00 ,  C12N9/99 ,  C12P1/06 ,  C12R1/465 ,  C12N1/20 ,  C12N9/98

CPC分类号： A01N63/00 ,  C12P1/06 ,  Y10S435/886

摘要： A novel trehalase inhibitor having the following physicochemical properties:(1) Activity: a specific inhibitory activity to trehalase;(2) Form: white powder, water-soluble;(3) Somogy-Nelson test: negative(4) Rydon-Smith test: positive(5) Optical rotation [.alpha.].sub.D.sup.23 : 113.8.degree. (C, 0.1 H.sub.2 O)(6) Molecular weight: 335 ([M+H].sup.+ =336)(7) Ultraviolet absorption spectrum: 258.5 nm (max.)(8) .sup.13 C-NMR(ppm): 28.9, 41.0, 56.9, 58.4, 64.3, 65.0, 71.3, 74.0, 75.2, 75.8, 76.0, 77.1, 123.0, 144.7

摘要翻译： 具有以下物理化学性质的新型海藻糖酶抑制剂：（1）活性：对海藻糖酶的特异性抑制活性; （2）形式：白色粉末，水溶性; （3）Somogy-Nelson测试：阴性（4）Rydon-Smith测试：阳性（5）旋光度D23：113.8℃（C，0.1H 2 O）（6）分子量：335（[M + H] + = 336）（7）紫外吸收光谱：258.5nm（最大）（8）13 C-NMR（ppm）：28.9,41.0,56.9,58.4,64.3,65.0,71.3,74.0,75.02,75.8,76.0,77.1， 123.0,144。

公开(公告)号：US5494812A

公开(公告)日：1996-02-27

申请号：US274896

申请日：1994-07-14

申请人： Sawao Murao ,  Takashi Shin ,  Kyoichi Sugawa ,  Amachi Teruo

发明人： Sawao Murao ,  Takashi Shin ,  Kyoichi Sugawa ,  Amachi Teruo

IPC分类号： A01N63/02 ,  A01N63/00 ,  C07G99/00 ,  C12N9/99 ,  C12P1/06 ,  C12R1/465 ,  C12N1/20 ,  C12N9/98

CPC分类号： A01N63/00 ,  C12P1/06 ,  Y10S435/886

摘要： A novel trehalase inhibitor having the following physicochemical properties:(1) Activity: a specific inhibitory activity to trehalase;(2) Form: white powder, water-soluble;(3) Somogy-Nelson test: negative(4) Rydon-Smith test: positive(5) Optical rotation [.alpha.].sub.D.sup.23 : 113.8.degree. (C, 0.1, H.sub.2 O)(6) Molecular weight: 335 ([M+H].sup.+ =336)(7) Ultraviolet absorption spectrum: 258.5 nm (max.)(8) .sup.13 C-NMR(ppm): 28.9, 41.0, 56.9, 58.4, 64.3, 65.0, 71.3, 74.0, 75.2, 75.8, 76.0, 77.1, 123.0, 144.7

摘要翻译： 具有以下物理化学性质的新型海藻糖酶抑制剂：（1）活性：对海藻糖酶的特异性抑制活性; （2）形式：白色粉末，水溶性; （3）Somogy-Nelson测试：阴性（4）Rydon-Smith测试：阳性（5）旋光度D23：113.8°（C，0.1，H 2 O）（6）分子量335（[M + H] + = 336）（7）紫外吸收光谱：258.5nm（最大）（8）13 C-NMR（ppm）：28.9,41.0,56.9,58.4,64.3,65.0,71.3,74.0,75.02,75.8,76.0,77.1 ，123.0,144。