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公开(公告)号:US4504584A
公开(公告)日:1985-03-12
申请号:US379851
申请日:1982-05-19
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 , Y10S435/886 , Y10S930/19
摘要: The invention relates to a biologically pure culture of new strains of the microorganism Streptomyces which are capable upon fermentation of producing a peptide of pharmacological activity.
摘要翻译: 本发明涉及生物学纯培养的新型菌株的微生物链霉菌,其能够在发酵时产生药理活性肽。
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公开(公告)号:US4666890A
公开(公告)日:1987-05-19
申请号:US380061
申请日:1982-05-20
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 , C07K5/06052 , C07K5/06069 , C07K5/06078 , 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 alkanoyl;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.sub.b.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R1是烷酰基; R 2和R q各自为氢,羧基,被保护的羧基或下式的基团:其中R 2a是单或二羧基(或保护的羧基)低级烷基或芳(羧基或保护的羧基)低级烷基,其芳基 部分可以被羟基取代,Rb2是氢或低级烷基; RP是氢,羧基,保护的羧基,条件是当R 2和R q中的一个是氢时,另一个是羧基或被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:US4311640A
公开(公告)日:1982-01-19
申请号:US93523
申请日:1979-11-13
申请人: Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka , Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
发明人: Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka , Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
CPC分类号: C07C243/00 , C07K5/0215 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55
摘要: The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. Included is the peptide FR900156 having the structure: ##STR1## as well as the peptides of the structure ##STR2## wherein R.sup.1 is acyl;R.sub.b.sup.1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl or benzyl;R.sup.2 is hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR3## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl or ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy,R.sub.b.sup.2 is hydrogen or lower alkyl;R.sup.p and R.sup.q are each 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;R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3; and n is 1 provided that when R.sup.1 is hydrogen, t-butoxycarbonyl or N-acetylmuramyl, R.sub.b.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is hydrogen, protected carboxy or a group of the formula: ##STR4## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl having 1 and 3 to 6, carbon atoms, .alpha.-carboxyethyl, ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy and R.sub.b.sup.2 is as defined above, or its pharmaceutically acceptable salt.
摘要翻译: 本发明涉及可用于治疗由病原微生物引起的感染性疾病的新型肽。 包括具有以下结构的肽FR900156:
以及结构 的肽,其中R 1是酰基; Rb1是氢,甲基,异丙基,羟甲基,保护的羟甲基或苄基; R2是氢,羧基,受保护的羧基或下式的基团:其中R 2a是其芳基部分可以被羟基取代的一或二羧基低级烷基或芳(羧基)低级烷基,R 2b是氢或 低级烷基 Rp和Rq各自为氢,羧基,保护的羧基,条件是当R 2和R q中的一个为氢时,则另一个为羧基或被保护的羧基; Rr为氢或氨基保护基; m为整数1〜3; 并且n为1,条件是当R 1为氢时,叔丁氧基羰基或N-乙酰胞壁酰基,R 1b为甲基,m为整数2,n为整数1,则R 2为氢,被保护的羧基或下式基团: 其中Ra2是具有1和3至6个碳原子的一或二羧基低级烷基,其α-芳基部分可以被羟基取代的α-羧乙基,芳(羧基)低级烷基,如上所定义,或其 药学上可接受的盐。 -
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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公开(公告)号:USRE32992E
公开(公告)日:1989-07-18
申请号:US611733
申请日:1984-05-18
申请人: Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka , Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
发明人: Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka , Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
CPC分类号: C07C243/00 , C07K5/0215 , C07K5/06026 , C07K5/06052 , C07K5/06069 , C07K5/06078 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55
摘要: The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. Included is the peptide FR900156 having the structure: ##STR1## as well as the peptides of the structure ##STR2## wherein R.sup.1 is acyl;R.sub.b.sup.1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl or benzyl;R.sup.2 is hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR3## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl or ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy,R.sub.b.sup.2 is hydrogen or lower alkyl;R.sup.p and R.sup.q are each 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;R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3, and n is 1 .Iadd.provided that when R.sup.1 is benzyloxycarbonyl R.sub.5.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is not protected carboxy, and .Iaddend.provided that when R.sup.1 is .[.hydrogen,.]. t-butoxycarbonyl or N-acetylmuramyl, R.sub.b.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is hydrogen, protected carboxy or a group of the formula: ##STR4## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl having 1 and 3 to 6, carbon atoms, .[..alpha.-carboxyethyl,.]. .Iadd.--CH.sub.2 --CH.sub.2 --COOH, .Iaddend.ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy and R.sub.b.sup.2 is as defined above, or its pharmaceutically acceptable salt.
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公开(公告)号:US4725582A
公开(公告)日:1988-02-16
申请号:US377836
申请日:1982-05-13
申请人: Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Takeno Hidekazu , 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 , Takeno Hidekazu , 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 , C07K5/06052 , C07K5/06069 , C07K5/06078 , C07K9/005 , C12R1/465 , A61K38/00 , Y02P20/55
摘要: The invention concerns peptides, having the pharmaceutical property of enhancing the immune response, having the structure: ##STR1## wherein R.sup.1 is alkanoyl,R.sub.b.sup.1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl or benzyl,R.sup.2 is 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 is substituted by hydroxy or not substituted,R.sub.b.sup.2 is hydrogen or lower alkyl,R.sup.p is hydrogen, carboxy or protected carboxy,R.sup.q is carboxy, 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, andn is an integer 1.
摘要翻译: 本发明涉及具有以下结构的具有增强免疫应答的药学性质的肽:其中R 1是烷酰基,R 1b是氢,甲基,异丙基,羟甲基,被保护的羟甲基或苄基,R 2是氢,羧基,被保护的羧基 或下式的基团:其中R 2a是其芳基部分被羟基或未取代的单或二羧基(或保护的羧基)低级烷基或芳(羧基或被保护的羧基)低级烷基,R 2b是氢 或低级烷基,Rp是氢,羧基或受保护的羧基,Rq是羧基,被保护的羧基或下式的基团:其中Ra2和Rb2各自如上定义,Rr是氢或氨基保护基,m是整数 1〜3,n为整数1。
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公开(公告)号:US4487763A
公开(公告)日:1984-12-11
申请号:US402440
申请日:1982-07-28
申请人: Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
发明人: Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
IPC分类号: A61K38/00 , A61P31/04 , A61P37/00 , A61P37/04 , C07C237/22 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/04 , C07K7/02 , C07K9/00 , C07C103/52 , A61K37/02
CPC分类号: C07C243/00 , C07K5/0215 , C07K9/005 , C12R1/465 , A61K38/00
摘要: The invention relates to novel peptides and their pharmaceutically acceptable salts, particularly useful for pharmaceutical purposes such as in the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. The compounds have the structure ##STR1## wherein R.sup.1 is hydrogen or acyl;R.sup.2 is carboxy or protected carboxy or a group of the formula: --COHN--R.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl;R.sup.3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl or a group of the formula: ##STR2## wherein R.sub.a.sup.3 is hydrogen, amino, protected amino or acylamino, R.sub.b.sup.3 is carboxy or protected carboxy,R.sup. is carboxy, protected carboxy, carbamoyl, carboxy (lower) alkyl or protected carboxy (lower) alkyl;l is an integer 2,m is an integer 0 to 2 andn is an integer 1, provided that, whenR.sup.1 is hydrogen or acyl,R.sup.2 is carboxy, protected carboxy or a group of the formula: --CONHR.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl,R.sup.P is carboxy, or protected carboxy, m is an integer 2, thenR.sup.3 is carbamoyl, lower alkyl or hydroxyphenyl or a group of the formula: ##STR3## wherein R.sub.a.sup.3 is hydrogen or acylamino and R.sub.b.sup.3 is carboxy or protected carboxy, and whenR.sup.P is carbamoyl, thenR.sup.1 is acyl.
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