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公开(公告)号:JPS58152850A
公开(公告)日:1983-09-10
申请号:JP3403182
申请日:1982-03-05
申请人: EISAI CO LTD
发明人: UCHIYAMA MIKIO , SATOU TAKASHI , YOSHINO HIROSHI , TSUCHIYA YUTAKA , KONISHI YUUSUKE , TSUJII MASAHIKO , HISATAKE YOSHIHIKO , KOIWA ATSUSHI
IPC分类号: C07K7/06
摘要: NEW MATERIAL:The decapeptide of formulaI(X is H or benzyloxycarbonyl) and its salt. USE:Synthetic intermediate of secretin. The fragment of formulaI is condensed with the novel fragment of formula II, and the resultant novel fragment of formula III is condensed with the novel fragment of formula IV to obtain protected secretin, from which all protecting groups are removed in one step to obtain secretin easily. PROCESS:The protected amino acid of formula Z-Arg(Tos)-OH is dissolved in DMF, added with N-methylmorpholine, and reacted with isobutyl chlorophosphate under cooling to obtain an active-type anhydride mixture. Separately, the peptide of formula V is dissolved in DMF and mixed with N-methylmorpholine. The mixture is mixed with the above anhydride mixture and condensed to obtain the decapeptide of formulaI. The peptide of formula V can be prepared by reducing the Z-compound in HCl and trifluoroethanol in the presence of a catalyst.
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公开(公告)号:JPS58152848A
公开(公告)日:1983-09-10
申请号:JP3402982
申请日:1982-03-05
申请人: EISAI CO LTD
发明人: UCHIYAMA MIKIO , SATOU TAKASHI , YOSHINO HIROSHI , TSUCHIYA YUTAKA , KONISHI YUUSUKE , TSUJII MASAHIKO , HISATAKE YOSHIHIKO , KOIWA ATSUSHI
IPC分类号: C07K7/06
摘要: NEW MATERIAL:The heptapeptide of formulaI(X is H or benzyloxycarbonyl). USE:Synthetic intermediate of secretin. The fragment of formulaI is condensed with the novel fragment of formula II, and the resultant novel fragment of formula III is condensed with the novel fragment of formula IV to obtain a protected secretin, from which all protecting groups are removed in one step to obtain secretin easily. PROCESS:The Z-removed compound of the peptide of formula V is condensed with the peptide of formula VI to obtain the heptapeptide of formulaI. The reaction is carried out by dissolving the peptide of formula VI and N-hydroxysuccinimide in DMF, adding DCC as a condensation agent to the solution, and condensing the product with the Z-removed compound of the peptide of formula V obtained by removing the protecting group by reduction. The peptide of formula V can be prepared by reacting the protected arginine of formula Z- Arg(Tos)-OH with the peptide of formula VII.
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公开(公告)号:JPS58144355A
公开(公告)日:1983-08-27
申请号:JP2608882
申请日:1982-02-22
申请人: EISAI CO LTD
发明人: UCHIYAMA MIKIO , SATOU TAKASHI , YOSHINO HIROSHI , TSUCHIYA YUTAKA , KONISHI YUUSUKE , TSUJII MASAHIKO , HISATAKE YOSHIHIKO , KOIWA ATSUSHI
IPC分类号: C07K14/575 , A61K38/22 , C07K1/06 , C07K14/645
摘要: PURPOSE:To obtain the titled compound useful as an agent for testing pancreatic function, etc., at low temperature, in a short time, in high activity and purity, with simple purification process, without side reactions, by removing the protecting group of a novel heptacosapeptide having a specific structural formula. CONSTITUTION:Secretin is prepared by removing the protecting group from a heptacosapeptide having a novel structural formula (Boc, His, etc. are abbreviations of tert-butyloxycarbonyl, histidine, etc. which are widely used in the field of peptide chemistry). The removel of the protecting group is preferably carried out in a short time, in one step by treating the compound with a strong acid (e.g. trifluoromethanesulfonic acid, hydrogen fluoride, etc.). The characteristic feature of the compound is the protection of the amino group of the N-terminal and the side chain functional groups of all constituent amino acids of secretin.
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公开(公告)号:JPS5363339A
公开(公告)日:1978-06-06
申请号:JP13640476
申请日:1976-11-15
申请人: EISAI CO LTD
IPC分类号: C07C237/04 , C07C237/20 , C07C237/22
摘要: PURPOSE:To prepare petides of highly optical purity, useful as a diagnotic agent for pancreas function, by reaction of N-aminoacyl-p-aminobenzoic acid with an aliphatic or aromatic carboxylic acid or their reactive derivatives.
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公开(公告)号:JP2553506B2
公开(公告)日:1996-11-13
申请号:JP25231585
申请日:1985-11-11
申请人: EISAI CO LTD
发明人: YOSHINO HIROSHI , TSUCHA YUTAKA , KANEKO TAKETOSHI , NAKAZAWA TAKAHIRO , ARAKI SHIN , YAMATSU KYOMI , TACHIBANA SHINRO , ARAKAWA YOSHIHIRO
IPC分类号: C07K14/655 , A61K38/00 , A61P25/04 , C07K1/06 , C07K7/06 , C07K14/575
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公开(公告)号:JPH08231505A
公开(公告)日:1996-09-10
申请号:JP3745695
申请日:1995-02-27
申请人: EISAI CO LTD
发明人: YOSHINO HIROSHI , YAMATO TAKASHI , OKAUCHI TATSUO , OKABE TADASHI , YOSHIMATSU KENTARO , SUGI NAOKO , NAGASU TAKESHI , OZAWA YOICHI , KOYANAGI NOZOMI , KITO KYOSUKE
IPC分类号: C07D401/12 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4178 , A61K31/425 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/4439 , A61P35/00 , C07D209/30 , C07D209/42 , C07D403/12 , C07D409/14 , C07D417/12
摘要: PURPOSE: To obtain a new compound useful as an antineoplastic agent. CONSTITUTION: This compound is expressed by formula I [A ring is a monocyclic aromatic ring; Q is a (substituted) monocyclic nitrogen-contg. aromatic heterocycle, a (substituted) amidino or guanidino; T is a single bond or a lower alkylene; U is a single bond, O, S, N-(R ), CON(R ), N(R )SO2 (R , R and R are each H or a lower alkyl), etc.; V is a single bond or a lower alkylene; W is H or a halogen; X is a halogen or cyano; where, when Q is amidino, etc., and T is a single bond, U is a single bond], e.g. N-(3-chloro-1H- indol-7-yl)-4-[3-(1-imidazolyl)propyl]benzenesulfonamide. The compound of formula I is obtained by reaction of a sulfonic acid of formula II [Qa is a (protected) (substituted) monocyclic nitrogen-contg. aromatic heterocycle] with a compound of formula III.
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公开(公告)号:JPS5750947A
公开(公告)日:1982-03-25
申请号:JP12526280
申请日:1980-09-11
申请人: Eisai Co Ltd
发明人: UCHIYAMA MIKIO , SATOU TAKASHI , YOSHINO HIROSHI , TSUCHIYA YUTAKA , KONISHI YUUSUKE , TSUJII MASAHIKO , HISATAKE YOSHIHIKO , KOIWA ATSUSHI
IPC分类号: C07K14/575 , C07K1/113 , C07K5/103 , C07K14/645
CPC分类号: C07K5/101 , C07K14/645 , Y02P20/55
摘要: NEW MATERIAL:A heptacosapeptide of formula I (Boc is tert-butyloxycarbonyl; Bu
t is tert-butyl; OBu
t is tert-butyl ester; Tos is tosyl).
USE: A synthetic intermediate for secretin, characterized by the combination of a specific protecting group, and capable of releasing the whole protecting groups readily easily at a low temperature in a short time by using HF and giving secretin of high activity and high purity by a simple purifying method. The secretin is a kind of digestive tract hormone and useful as a pancreatic function testing agent, remedy for the duodenal ulcer, etc.
PROCESS: A decapeptide of formula II is condensed with a heptadecapeptide of formula III to give the heptacosapeptide of formula I.
COPYRIGHT: (C)1982,JPO&Japio摘要翻译: 新物质:式I的七肽(Boc是叔丁氧羰基; Bu t是叔丁基; OBu是叔丁酯; Tos是甲苯磺酰基)。 用途:用于促胰液素的合成中间体,其特征在于特异性保护基团的组合,并能够通过使用HF在短时间内容易地在低温下释放整个保护基团,并通过使用HF并且通过使用HF来提供高活性和高纯度的促胰液素 简单净化方法。 胰泌素是一种消化道激素,可用作胰腺功能测试剂,十二指肠溃疡等的治疗方法。方法:将式II的十肽与式III的十七肽缩合,得到式I的十七肽。
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公开(公告)号:JPH07165708A
公开(公告)日:1995-06-27
申请号:JP20756894
申请日:1994-08-31
申请人: EISAI CO LTD
发明人: YOSHINO HIROSHI , YAMATO TAKASHI , OKAUCHI TATSUO , YOSHIMATSU KENTARO , SUGI NAOKO , NAGASU TAKESHI , OZAWA YOICHI , KOYANAGI NOZOMI , KITO KYOSUKE
IPC分类号: A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4178 , A61K31/435 , A61K31/4355 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/635 , A61P35/00 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04
摘要: PURPOSE:To obtain a new sulfoneamide derivative having excellent antineoplastic activity and having a low-toxicity bicyclic hetero ring, and a new sulfonic acid ester derivative. CONSTITUTION:A compound of formula I [A ring is a monocyclic aromatic ring or a bicyclic aromatic ring; B ring is a 6-membered ring type unsaturated hydrocarbon or an unsaturated 6-membered heterocyclic ring containing one N as a hetero atom; C ring is a 5-membered heterocyclic ring containing 1 or 2 nitrogen atoms, wherein A to C rings may have substituent groups; W is a single bond or CH=CH; X is NR or 0; Y is C or N; Z is NR or N; R and R are each H or a lower alkyl, except (1) combination of A ring = m- ethylbenzene, W = a single bond, X=NH, B ring = methoxybenzene and C ring: an unsaturated pyrazole and (2) combination of A ring=4-(acetamide) benzene or 4-aminobenzene, W: a single bond, X=NH, B ring= an unsaturated benzene and C ring= an unsaturated pyrazole], e.g. 4-amino-N-(3-chloro-1H- indol-7-yl)benzenesulfonamide of formula II.
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公开(公告)号:JPH0741461A
公开(公告)日:1995-02-10
申请号:JP13393994
申请日:1994-05-25
申请人: EISAI CO LTD
IPC分类号: A61K31/21 , A61K31/44 , A61K31/505 , A61P35/00 , C07C303/28 , C07C309/73 , C07C309/75 , C07C309/76 , C07C309/77 , C07D213/74 , C07D213/80 , C07D213/803 , C07D213/84 , C07D239/47
摘要: PURPOSE:To obtain a new sulfonic acid derivative having excellent antitumor actions and useful as an anticancer agent. CONSTITUTION:This sulfonic acid ester derivative is expressed by formula I {R1 and R2 are each H, a halogen, lower alkyl, etc.; R3 and R4 are each H, a halogen, lower alkyl, etc.; R5 is H or a lower alkyl; A and B are each N atom or (lower alkyl-substituted)methine; Y is a (substituted)aryl, (CO)-R6 [R6 is a lower alkyl, (substituted)amino, etc.], etc.}, e.g. (2-phenylamino)-3-pyridyl 4-methoxybenzenesulfonate. The compound expressed by formula 1 is obtained by reacting, e.g. a sulfonic acid expressed by formula II or its reactive derivative with a compound expressed by formula III.
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公开(公告)号:JPH047731B2
公开(公告)日:1992-02-12
申请号:JP12227986
申请日:1986-05-29
申请人: EISAI CO LTD
发明人: YOSHINO HIROSHI , SAITO ISAO , TSUJII MASAHIKO
IPC分类号: C07K1/06 , C07B31/00 , C07B51/00 , C07C67/00 , C07C227/18 , C07C227/20 , C07C229/22 , C07C229/26 , C07C229/36 , C07K5/06
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