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1. 发明授权

US5658888A Erythromycin derivatives 失效
标题翻译：红霉素衍生物
公开(公告)号：US5658888A
公开(公告)日：1997-08-19
申请号：US318814
申请日：1994-10-19
申请人： Hiroshi Koga , Tsutomu Sato , Hisanori Takanashi
发明人： Hiroshi Koga , Tsutomu Sato , Hisanori Takanashi
IPC分类号： C07D407/00 , C07H17/08 , A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P1/00 , A61P1/12 , A61P43/00 , C07M17/08
CPC分类号： C07H17/08
摘要： Compounds represented by the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an acyl group; R.sub.2 and R.sub.3 may be the same or different, and each represents a hydrogen atom, hydroxyl group, acyloxy group or amino group, or, in combination, they represent .dbd.O or .dbd.NOR.sub.10, where R.sub.10 represents a hydrogen atom or lower alkyl group;R.sub.4 represents a hydrogen atom or lower alkyl group; andY represents --NR.sub.5 R.sub.6 or --N.sup.+ R.sub.7 R.sub.8 R.sub.9 X.sup.-, where R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 may be the same or different, and each represents a hydrogen atom or an unsubstituted or substituted lower alkyl group, lower alkenyl group, lower alkinyl group, cycloalkyl group or 3-7-membered heterocyclic group comprising an oxygen atom, nitrogen atom or sulphur atom as an heteroatom, and X represents an anion, where R.sub.5 and R.sub.6, or R.sub.7 and R.sub.8 may form an azacycloalkyl group together with the neighboring nitrogen atom, respectively, and salts thereof.These compounds and their salts are subject to a remarkably lower degree of decomposition by gastric acid than are the publicly known erythromycin derivatives of the prior art, and have an excellent enterolinesis stimulating action.
摘要翻译： PCT No.PCT / JP93 / 00702 Sec。 371日期：1994年10月19日 102（e）日期1994年10月19日PCT提交1993年5月26日PCT公布。出版物WO93 / 24509 日期1993年12月9日化合物由通式表示的化合物：酰基; R2和R3可以相同或不同，各自表示氢原子，羟基，酰氧基或氨基，或者组合表示= O或= NOR10，其中R10表示氢原子或低级烷基; R4代表氢原子或低级烷基; 并且Y表示-NR5R6或-N + R7R8R9X-，其中R5，R6，R7，R8和R9可以相同或不同，并且各自表示氢原子或未取代或取代的低级烷基，低级烯基，低级炔基基团，环烷基或包含氧原子，氮原子或硫原子作为杂原子的3-7元杂环基，X表示阴离子，其中R 5和R 6或R 7和R 8可以与相邻的基团一起形成氮杂环烷基氮原子及其盐。与现有技术中公知的红霉素衍生物相比，这些化合物及其盐受胃酸分解程度明显降低，具有优异的肠溶激素作用。

2. 发明申请

US20090062219A1 DRUGS FOR THE TREATMENT AND/OR PROPHYLAXIS OF GASTROPARESIS SYMPTOM 失效
标题翻译：治疗和/或预防胃肠道症状的药物
公开(公告)号：US20090062219A1
公开(公告)日：2009-03-05
申请号：US11813026
申请日：2005-12-28
申请人： Osamu Cynshi , Hisanori Takanashi , Tatsuhiko Iwase
发明人： Osamu Cynshi , Hisanori Takanashi , Tatsuhiko Iwase
IPC分类号： A61K31/7048 , A61P1/14
CPC分类号： A61K31/7048
摘要： The present invention provides a therapeutic and/or preventive agent against gastroparesis symptom which is appropriate for continuous medication and which comprises a compound represented by formula (1): (wherein R1 represents a C1-C6 alkyl group and R2 represents a C1-C6 alkyl group) or a pharmaceutically acceptable salt thereof as an active ingredient. The erythromycin derivative of the formula (1) has an efficacy of improving gastroparesis and this action of the derivative in improving gastroparesis symptom is not found in ABT-229, a different motilin agonist erythromycin derivative. Further, the compound of the formula (1) is also appropriate for long-term clinical use because of its much weaker antibacterial action than that of erythromycin. Accordingly, the present invention provides a pharmaceutical agent that is safe and exhibits potent therapeutic and/or preventive effect in an effort to improve symptomatic gastroparesis.
摘要翻译：本发明提供了适用于连续用药的胃轻瘫症状的治疗和/或预防剂，其包含由式（1）表示的化合物：其中R1表示C1-C6烷基，R2表示C1-C6烷基基团）或其药学上可接受的盐作为活性成分。式（1）的红霉素衍生物具有改善胃轻瘫的功效，并且在不同的胃动素激动剂红霉素衍生物的ABT-229中未发现该衍生物在改善胃轻瘫症状中的作用。此外，式（1）的化合物也适用于长期临床应用，因为其抗菌作用比红霉素弱得多。因此，本发明提供了一种安全的药物，并且在改善症状性胃轻瘫方面具有有效的治疗和/或预防效果。

3. 发明授权

US06255285B1 Phenethylamine derivatives 失效
标题翻译：苯乙胺衍生物
公开(公告)号：US06255285B1
公开(公告)日：2001-07-03
申请号：US09485620
申请日：2000-02-15
申请人： Ken-ichiro Kotake , Toshiro Kozono , Tsutomu Sato , Hisanori Takanashi
发明人： Ken-ichiro Kotake , Toshiro Kozono , Tsutomu Sato , Hisanori Takanashi
IPC分类号： A61K3805
CPC分类号： C07K5/0815 , A61K38/00 , C07K5/0202 , C07K5/06034 , C07K5/06078 , C07K5/0802 , C07K5/0812 , C07K5/0819 , C07K5/0821
摘要： The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).
摘要翻译：本发明的目的是提供通常用作胃动素受体拮抗剂并且可用作药物的苯乙胺衍生物。本发明提供由通式（1）表示的化合物:(其中A通常为氨基酸残基，R 1通常为R 6 -CO-，R 2通常为氢原子，R 3通常为-CO-R 7，R 4通常为烷基，R 5通常是羟基，R 6通常是烷基，R 7通常是氨基）。

4. 发明授权

US06248777B1 Remedies for peripheral circulation disturbances 失效
标题翻译：外周循环障碍的补救措施
公开(公告)号：US06248777B1
公开(公告)日：2001-06-19
申请号：US09380376
申请日：1999-09-01
申请人： Hiroshi Koga , Hisanori Takanashi , Eiji Kumagai
发明人： Hiroshi Koga , Hisanori Takanashi , Eiji Kumagai
IPC分类号： A61K3135
CPC分类号： C07D311/58
摘要： It is an object of the present invention to provide novel therapeutic agents for peripheral vascular disease. The present invention provides pharmaceutical compositions comprising a benzopyran or benzoxazine derivative of the general formula (1): wherein; R1 represents a hydrogen atom, a lower alkyl group or an aryl group, or R1 directly couples with Q or R11 to form a single bond; R2represents a substituted or unsubstituted amino group, a saturated or unsaturated heterocyclic group, A—O—or —C(═X)Y; Q represents ═N—, N+—O−or C(R11)R12; R3 and R4 each represent a hydrogen atom, a lower alkyl group or a substituted lower alkyl group having a halogen atom or a lower alkoxy group as a substituent or the like; and R5 and R6 each represent a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group or the like; and a pharmaceutically acceptable carrier.
摘要翻译：本发明的目的是提供用于外周血管疾病的新治疗剂。本发明提供了包含通式（1）的苯并吡喃或苯并恶嗪衍生物的药物组合物：其中：R 1表示氢原子，低级烷基或芳基，或R 1与Q或R 11直接键合形成单键; R 2表示取代或未取代的氨基，饱和或不饱和杂环基，AO或-C（= X）Y; Q表示= N- ，N + -O-或C（R 11）R 12; R 3和R 4各自表示氢原子，低级烷基或具有卤素原子或低级烷氧基作为取代基的取代的低级烷基等; R 5和R 6各自表示氢原子，卤素原子，低级烷基，低级卤代烷基等; 和药学上可接受的载体。

5. 发明授权

US07803779B2 Drugs for the treatment and/or prophylaxis of gastroparesis symptom 失效
标题翻译：用于治疗和/或预防胃轻瘫症状的药物
公开(公告)号：US07803779B2
公开(公告)日：2010-09-28
申请号：US11813026
申请日：2005-12-28
申请人： Osamu Cynshi , Hisanori Takanashi , Tatsuhiko Iwase
发明人： Osamu Cynshi , Hisanori Takanashi , Tatsuhiko Iwase
IPC分类号： A61K31/70
CPC分类号： A61K31/7048
摘要： The present invention provides a therapeutic and/or preventive agent against gastroparesis symptom which is appropriate for continuous medication and which comprises a compound represented by formula (1): (wherein R1 represents a C1-C6 alkyl group and R2 represents a C1-C6 alkyl group) or a pharmaceutically acceptable salt thereof as an active ingredient. The erythromycin derivative of the formula (1) has an efficacy of improving gastroparesis and this action of the derivative in improving gastroparesis symptom is not found in ABT-229, a different motilin agonist erythromycin derivative. Further, the compound of the formula (1) is also appropriate for long-term clinical use because of its much weaker antibacterial action than that of erythromycin. Accordingly, the present invention provides a pharmaceutical agent that is safe and exhibits potent therapeutic and/or preventive effect in an effort to improve symptomatic gastroparesis.
摘要翻译：本发明提供了适用于连续用药的胃轻瘫症状的治疗和/或预防剂，其包含由式（1）表示的化合物：其中R1表示C1-C6烷基，R2表示C1-C6烷基基团）或其药学上可接受的盐作为活性成分。式（1）的红霉素衍生物具有改善胃轻瘫的功效，并且在不同的胃动素激动剂红霉素衍生物的ABT-229中未发现该衍生物在改善胃轻瘫症状中的作用。此外，式（1）的化合物也适用于长期临床应用，因为其抗菌作用比红霉素弱得多。因此，本发明提供了一种安全的药物，并且在改善症状性胃轻瘫方面具有有效的治疗和/或预防效果。

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