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公开(公告)号：US4904685A
公开(公告)日：1990-02-27
申请号：US301422
申请日：1989-02-27
IPC分类号： C07D209/34 , C07D209/38 , C07D235/26 , C07D263/58 , C07D277/68 , C07D413/12
CPC分类号： C07D263/58 , C07D209/34 , C07D209/38 , C07D235/26 , C07D277/68 , C07D413/12
摘要： Compounds of the formula ##STR1## where Y is alkyl, aryl or heterocyclic, n is 1-7, R is hydrogen, alkyl, aralkyl or carboxymethyl, R.sub.1 is acetoxy, thiophenoxy, hydrogen, halo, alkyl, alkoxy or trifluoromethyl, R.sub.2 is hydrogen, alkyl or alkanoyl and X is C.dbd.O, CH.sub.2, NH, O or S as antiallergy and antiinflammatory agents.
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公开(公告)号：US4801580A
公开(公告)日：1989-01-31
申请号：US377931
申请日：1982-05-13
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
CPC分类号： C07C243/00 , C07K5/0215 , C07K5/06026 , C07K5/06104 , C07K9/005 , C12R1/465 , A61K38/00
摘要： The invention relates to novel peptides, of pharmacological activity, of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sub.b.sup.1 is methyl,R.sup.2 is carboxy, carboxymethylcarbamoyl, 1-carboxyethylcarbamoyl or ethoxycarbonylmethylcarbamoyl,R.sup.q is carboxy or 3-t-butoxycarbonylcarbazoyl,R.sup.p is carboxy or methoxycarbonyl,R.sup.r is hydrogen, t-butoxycarbonyl or benzyloxycarbonyl,m is the integer 2, andn is the integer 1, or its pharmaceutically acceptable salt.
摘要翻译： 本发明涉及药理学活性的新肽，其结构式如下：其中R1是氢，Rb1是甲基，R2是羧基，羧甲基氨基甲酰基，1-羧基乙基氨基甲酰基或乙氧基羰基甲基氨基甲酰基，Rq是羧基或3-叔丁氧基羰基咔唑基，Rp 是羧基或甲氧基羰基，R r是氢，叔丁氧基羰基或苄氧基羰基，m是整数2，n是整数1或其药学上可接受的盐。
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公开(公告)号：US4749691A
公开(公告)日：1988-06-07
申请号：US37470
申请日：1987-04-13
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
CPC分类号： C07C243/00 , C07K5/0215 , C07K5/06017 , C07K5/06026 , C07K5/06052 , C07K5/06078 , C07K5/06104 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55
摘要： The invention relates to novel peptides of enhanced pharmacological activity of the formula: ##STR1## wherein R.sup.1 is hydroxyalkanoyl,R.sup.2 and R.sup.q are each hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR2## wherein R.sub.a.sup.2 is mono- or di-carboxy (or protected carboxy) lower alkyl or ar(carboxy or protected carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy, R.sup. 2 is hydrogen or lower alkyl; R.sup.p is hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy or a group of the formula: ##STR3## wherein R.sub.a.sup.2 and R.sub.b.sup.2 are each as defined above; R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3;or its pharmaceutically acceptable salt.
摘要翻译： 本发明涉及增强的药理活性的新肽，其具有下式：其中R 1是羟基烷酰基，R 2和R q各自是氢，羧基，被保护的羧基或下式的基团：其中Ra 2是单 - 或 二羧基（或被保护的羧基）低级烷基或芳基部分可以被羟基取代的芳（羧基或被保护的羧基）低级烷基，R 2是氢或低级烷基; Rp是氢，羧基，受保护的羧基，条件是当R 2和R q中的一个是氢时，另一个是羧基或保护的羧基或下式的基团：其中Ra2和Rb2各自如上所定义; Rr为氢或氨基保护基; m为整数1〜3; 或其药学上可接受的盐。
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公开(公告)号：US4539155A
公开(公告)日：1985-09-03
申请号：US515590
申请日：1983-07-21
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
IPC分类号： A61K38/00 , C07K5/02 , C07K7/02 , C07K9/00 , C07C103/52 , C07C69/74 , C07C101/20 , C07C101/30
CPC分类号： C07C243/00 , C07K5/0215 , C07K9/005 , C12R1/465 , A61K38/00
摘要： The invention relates to compounds and salts of compounds which are diaminopimelyl peptides, N-acetoxypropionyl or N-t-butoxycarbonyl-amino-acid - (.alpha.-OBzl) glutamic acid peptides or N-acylated derivatives of (.alpha.-OBzl) glytamic acid or of (.alpha.-OBzl) aminoadipic acid.The compounds and their salts are starting materials for the preparation of pharmacologically active peptides.
摘要翻译： 本发明涉及化合物和化合物的盐，它们是二氨基辛基肽，N-乙酰氧基丙酰基或N-叔丁氧基羰基 - 氨基酸 - （α-Boc z）谷氨酸肽或（α-Boc z）谷氨酸的N-酰化衍生物或（ α-OBzl）氨基己二酸。 化合物及其盐是制备药理活性肽的起始原料。
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公开(公告)号：US4458078A
公开(公告)日：1984-07-03
申请号：US377841
申请日：1982-05-13
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
CPC分类号： C07C243/00 , C07K5/0215 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55 , Y10S930/19
摘要： The invention relates to novel intermediates for the preparation of peptides of pharmacological activity, said intermediates being of the formulas: ##STR1## wherein R.sub.2.sup.r is amino protective group andY is hydrogen or amino protective group; and : ##STR2##
摘要翻译： 本发明涉及用于制备药理学活性肽的新型中间体，所述中间体具有下式：其中R2r为氨基保护基，Y为氢或氨基保护基; 和：
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