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1. 发明授权

US4551273A Analgesic peptide and process for the preparation thereof 失效
标题翻译：止痛肽及其制备方法
公开(公告)号：US4551273A
公开(公告)日：1985-11-05
申请号：US575804
申请日：1984-01-31
申请人： Shinro Tachibana , Shizuko Ohya , Yoshihiro Arakawa , Takahiro Nakazawa , Takeru Kaneko , Masuhiro Ikeda , Kiyomi Yamatsu
发明人： Shinro Tachibana , Shizuko Ohya , Yoshihiro Arakawa , Takahiro Nakazawa , Takeru Kaneko , Masuhiro Ikeda , Kiyomi Yamatsu
IPC分类号： C07K14/655 , A61K38/00 , A61P25/04 , C07C231/02 , C07K7/08 , C07K14/575 , C07K14/665 , C07C103/52
CPC分类号： C07K14/665 , A61K38/00 , Y02P20/55
摘要： A novel peptide having the primary structure: N-Me-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-D.Ile-Arg-Pro-Lys-D.Leu-Lys-Trp-NH.sub.2 (in which D.Ile and D.Leu represent a D-Ile and a D-Leu residue respectively, other abbreviations of amino acids represent each an L-amino acid residue and Me represents a methyl group), which exhibits a remarkable analgesic effect when administered peripherally. A process for the preparation thereof by a solid phase method is also disclosed.
摘要翻译：具有一级结构的新型肽：N-Me-Tyr-Gly-Gly-Phe-Leu-Arg-Arg-D.Ile-Arg-Pro-Lys-D.Leu-Lys-Trp-NH2（其中D. Ile和D.Leu分别表示D-Ile和D-Leu残基，氨基酸的其它缩写代表每个L-氨基酸残基，Me表示甲基），其在外周施用时显示出显着的镇痛作用。还公开了通过固相法制备其方法。

2. 发明授权

US4707468A Polypeptide 失效
公开(公告)号：US4707468A
公开(公告)日：1987-11-17
申请号：US796390
申请日：1985-11-08
申请人： Hiroshi Yoshino , Yutaka Tsuchiya , Takeru Kaneko , Takahiro Nakazawa , Masuhiro Ikeda , Shin Araki , Kiyomi Yamatsu , Shinro Tachibana , Yoshihiro Arakawa
发明人： Hiroshi Yoshino , Yutaka Tsuchiya , Takeru Kaneko , Takahiro Nakazawa , Masuhiro Ikeda , Shin Araki , Kiyomi Yamatsu , Shinro Tachibana , Yoshihiro Arakawa
IPC分类号： C07K1/14 , A61K38/00 , A61K38/08 , A61P25/04 , C07K7/06 , C07K14/665 , C07K14/675 , C07K7/12
CPC分类号： C07K14/665 , A61K38/00 , Y02P20/55 , Y10S514/809 , Y10S930/26
摘要： A novel polypeptide is defined by the below shown formula and is useful as an analgesic. ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each represents a hydrogen atom or a lower alkyl or lower alkenyl group, A represents a D-amino acid, Gly or Sar provided that when the D-amino acid is D-Cys, it is bonded with L-Cys or D-Cys in position 5 through a S--S bond to effect intramolecular ring closure, B represents L-Phe or D-Phe in which the benzene ring may be substituted or an .alpha.-N-alkyl derivative thereof, C represents an L-amino acid, D-Cys or an .alpha.-N-alkyl derivative thereof, D and E each represent an L- or D-basic amino acid or an .alpha.-N-alkyl derivative thereof, F represents a group of the formula --OR.sup.3 (in which R.sup.3 is H or a lower alkyl group), a group of the formula: ##STR2## (in which R.sup.4 and R.sup.5 are the same or different and each represents H or a lower alkyl group), a group of the formula: --G--OR.sup.6 (in which G is an L- or D-amino acid or Gly or an .alpha.-N-alkyl derivative thereof and R.sup.6 represents H or a lower alkyl group), a group of the formula: ##STR3## (in which G is as defined above and R.sup.7 and R.sup.8 may be the same or different and each represents H or a lower alkyl group), a group of the formula: --G--L--Arg--OR.sup.9 or --G--D--Arg--OR.sup.9 (in which G is as defined above and R.sup.9 represents H or a lower alkyl group or a group of the formula: ##STR4## (in which G is as defined above and R.sup.10 and R.sup.11 may be the same or different and each represents H or a lower alkyl group), a group of the formula: --G--J--OR.sup.12 in which G is defined as above, J is a neutral amono acid group or an acidic amino acid group and R.sup.12 is hydrogen or a lower alkyl group; or a group of the formula: --G--Arg--M--OR.sup.13 in which M is D-amino acid group and R.sup.13 is hydrogen or a lower alkyl group, provided that all of the amino acids constituting the polypeptide of the above formula do not represent at the same time an L-amino acid of the general formula: ##STR5## (in which R represents a group corresponding to a structural formula of an amino acid deprived of a group of the formula: ##STR6## or pharmacologically acceptable salts of them.

3. 发明授权

US5523307A Cyclic amine and pharmacological composition 失效
标题翻译：环胺和药理组成
公开(公告)号：US5523307A
公开(公告)日：1996-06-04
申请号：US258798
申请日：1994-06-07
申请人： Hachiro Sugimoto , Takaharu Nakamura , Norio Karibe , Isao Saito , Kunizo Higurashi , Masahiro Yonaga , Takeru Kaneko , Takahiro Nakazawa , Masataka Ueno , Kiyomi Yamatsu , Kohshi Ueno , Masuhiro Ikeda
发明人： Hachiro Sugimoto , Takaharu Nakamura , Norio Karibe , Isao Saito , Kunizo Higurashi , Masahiro Yonaga , Takeru Kaneko , Takahiro Nakazawa , Masataka Ueno , Kiyomi Yamatsu , Kohshi Ueno , Masuhiro Ikeda
IPC分类号： C07D211/14 , C07D211/18 , C07D211/32 , C07D211/46 , C07D211/58 , C07D223/04 , C07D401/12 , A61K31/44 , A61K31/445 , A61K31/47
CPC分类号： C07D401/12 , C07D211/14 , C07D211/18 , C07D211/32 , C07D211/46 , C07D211/58 , C07D223/04
摘要： A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --0--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat a mental symptoms associated with a cerebrovascular disease.
摘要翻译：环胺由下式定义：其中A为萘基，苯基，喹啉基或烷基，X为含羰基的基团，n为2或3，B为烷基，卤素，苯基或-YZ Y是-O - ， - CO-或-NH-，Z是苯基，萘基，吡啶基，烷基或环烷基。治疗与脑血管疾病相关的精神症状是有用的。

4. 发明授权

US5196439A Piperidine compounds useful to treat cerebrovascular diseases 失效
标题翻译：可用于治疗脑血管疾病的哌啶化合物
公开(公告)号：US5196439A
公开(公告)日：1993-03-23
申请号：US825423
申请日：1992-01-24
申请人： Hachiro Sugimoto , Takaharu Nakamura , Norio Karibe , Isao Saito , Kunizo Higurashi , Masahiro Yonaga , Takeru Kaneko , Takahiro Nakazawa , Masataka Ueno , Kiyomi Yamatsu , Kohshi Ueno , Masuhiro Ikeda
发明人： Hachiro Sugimoto , Takaharu Nakamura , Norio Karibe , Isao Saito , Kunizo Higurashi , Masahiro Yonaga , Takeru Kaneko , Takahiro Nakazawa , Masataka Ueno , Kiyomi Yamatsu , Kohshi Ueno , Masuhiro Ikeda
IPC分类号： C07D211/14 , C07D211/18 , C07D211/32 , C07D211/46 , C07D211/58 , C07D223/04 , C07D401/12
CPC分类号： C07D401/12 , C07D211/14 , C07D211/18 , C07D211/32 , C07D211/46 , C07D211/58 , C07D223/04
摘要： A cyclic amine is defined by the formula: ##STR1## in which A is naphthyl, phenyl, quinolyl or alkyl, X is a group containing carbonyl, n is 2 or 3 and B is alkyl, halogen, phenyl or --YZ, Y being --O--, --CO-- or --NH--, Z being phenyl, naphthyl, pyridyl, alkyl or cycloalkyl. It is useful to treat mental symptoms associated with a cerebrovascular disease.
摘要翻译：环胺由下式定义：其中A为萘基，苯基，喹啉基或烷基，X为含羰基的基团，n为2或3，B为烷基，卤素，苯基或-YZ ，Y为-O-，-CO-或-NH-，Z为苯基，萘基，吡啶基，烷基或环烷基。治疗与脑血管病相关的精神症状是有用的。

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