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公开(公告)号:KR820001611B1
公开(公告)日:1982-09-08
申请号:KR820002707
申请日:1982-06-17
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KURODA YOSHIO , IKUCHI EIGO , IMANAKA HIROSHI , OKUHARA MASAKURI , AOKI HASTUO , KAMIYA TAKASHI
IPC: C07F9/40
Abstract: The title compds.(If; R1α = lower alkenoyl; A = lower alkyene), useful as antibiotics and bactericides, were prepd. by the reaction of Ie≮HN(OH)AP(O)(OH)2≉ and R1α-OH. phosphonylation of R1N(0R2)AX1≮R1 = olwer alkoxycarbonyl, a enesulfonyl; R2 = ar(lower)alkyl; X1 = acid residue≉wich POR3(0R3)2 [R3 = H, ester residue; R3 α=ester residue, followed by hy2 drolysis to give If.
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公开(公告)号:KR820001610B1
公开(公告)日:1982-09-08
申请号:KR770001737
申请日:1977-07-27
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KURODA YOSHIO , IKUCHI EIGO , IMANAKA HIROSHI , OKUHAMA MASAKUNI , AOKI HASTUO , KAMIYA TAKASHI
IPC: C07F9/40
Abstract: The title compds.(If; R1α = olwer alkanoyl; A = lower alkylene or lower alkenyiene),useful as antibiotics and bactericides, were prepd. by the reaction of HN(OH)AP(O)(0H)2≮Ie≉and R1α-OH. Ie was prepd. by the hydrolysis of R1N(OR2)A-P(O)(OR3α)2 ≮Ib; R1 = H, lower alkoxycarbonyl, arene suifonyl ; R2 = H, ar(olwer)alkyl, lower alkoxycarbonyl; R3α = ester residue obtained from the reaction of X2AP(O)(OR3α)2 2≮ X2 = acid residue≉and R1NH(OR2).
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公开(公告)号:US4349466A
公开(公告)日:1982-09-14
申请号:US22907281
申请日:1981-01-28
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KITAURA YOSHIHIKO , NAKAGUCHI OSAMU , HEMMI KEIJI , ARATANI MATSUHIKO , TAKENO HIDEKAZU , OKADA SATOSHI , TANAKA HIROKAZU , HASHIMOTO MASASHI , KURODA YOSHIO , IGUCHI EIKO , KOHSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI
CPC classification number: C07C243/00 , A61K38/00 , C07K5/0215 , C07K9/005 , C12R1/465 , Y10S435/886 , Y10S930/142
Abstract: 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: wherein R1 is hydrogen or acyl; R2 and Rq are each hydrogen, carboxy, protected carboxy, or a group of the formula wherein Ra2 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, Rb2 is hydrogen or lower alkyl; Rp is hydrogen, carboxy, protected carboxy, with proviso that when one of R2 and Rq is hydrogen, then the other is carboxy, or protected carboxy, or a group of the formula wherein Ra2 and Rb2 are each as defined above; Rr is hydrogen or aminoprotective group, m is an integer 1 to 3, and their pharmaceutically acceptable salts.
Abstract translation: 本发明涉及特别可用于药物目的的新型肽及其药学上可接受的盐,例如由病原微生物引起的感染性疾病的治疗性治疗。 该化合物具有以下结构:其中R 1是氢或酰基; 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是单或二羧基或被保护的羧基低级烷基或其芳基部分可以是芳(羧基或保护的羧基)低级烷基 被羟基取代,Rb2是氢或低级烷基; Rp是氢,羧基,被保护的羧基,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1〜3的整数,及其药学上可接受的盐。
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公开(公告)号:US4322341A
公开(公告)日:1982-03-30
申请号:US20124180
申请日:1980-10-27
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KITAURA YOSHIHIKO , NAKAGUCHI OSAMU , HEMMI KEIJI , ARATANI MATSUHIKO , TAKENO HIDEKAZU , OKADA SATOSHI , TANAKA HIROKAZU , HASHIMOTO MASASHI , KURODA YOSHIO , IGUCHI EIKO , KOHSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI
CPC classification number: C07C243/00 , A61K38/00 , C07K5/0215 , C07K9/005 , C12R1/465 , Y02P20/55
Abstract: 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: wherein R1 is hydrogen or acyl; Rb1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl, or benzyl; R2 and Rq are each hydrogen, carboxy, protected carboxy, or a group of the formula: wherein Ra2 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, Rb2 is hydrogen or lower alkyl; Rp is hydrogen, carboxy, protected carboxy, with proviso that when one of R2 and Rq is hydrogen, then the other is carboxy or protected carboxy or a group of the formula: wherein Ra2 and Rb2 are each as defined above: Rr is hydrogen or amino protective group; m is an integer 1 to 3; and n is an integer, 2, or its pharmaceutically acceptable salt.
Abstract translation: 本发明涉及特别可用于药物目的的新型肽及其药学上可接受的盐,例如由病原微生物引起的感染性疾病的治疗性治疗。 该化合物具有以下结构:其中R 1是氢或酰基; Rb1是氢,甲基,异丙基,羟甲基,保护的羟甲基或苄基; 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各自如上定义:Rr 是氢或氨基保护基; m为整数1〜3; 且n为整数2或其药学上可接受的盐。
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公开(公告)号:JPS5817198B2
公开(公告)日:1983-04-05
申请号:JP1068976
申请日:1976-02-02
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: OKUHARA MASAKUNI , KURODA YOSHIO , UMEHARA KAZUYOSHI , KOSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI
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公开(公告)号:JPS5681593A
公开(公告)日:1981-07-03
申请号:JP15857879
申请日:1979-12-05
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KURODA YOSHIO , GOTOU TOSHIO , IGUCHI HIDEKO , TANAKA HIROKAZU , KOUSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI
Abstract: NEW MATERIAL:An amino acid phosphorohydrazidate derivative expessed by formula I [R is lower alkyl or aryl; R is H or lower alkyl; Ra and Rb are H, lower alkyl or ar(lower)alkyl; Z is H or a protecting group of amino group]. EXAMPLE:Dibenzyl N -(N-benzyloxycarbonyl-D-leucyl)phosphorohydrazidate of formula II. USE:An antimicrobial agent for men and animals. PROCESS:A strain of Streptomyces unzenensis No. 2050, e.g. FERM-P No. 3936, is preferably irradiated with ultraviolet light, X rays, etc. and cultivated in a liquid culture medium at about 30 deg.C for 50-100hr by the submerged culture method. The microbial cell is then removed, and the titled substance is separated and purified by means of vacuum concentration, etc.
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公开(公告)号:JPS5585552A
公开(公告)日:1980-06-27
申请号:JP14727579
申请日:1979-11-14
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KURODA YOSHIO , IGUCHI HIDEKO , KOUSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI , KITAURA YOSHIHIKO , NAKAGUCHI OSAMU , HENMI KEIJI , ARAYA MATSUHIKO , TAKENO SHIYUUICHI , OKADA TATSU , TANAKA HIROKAZU , HASHIMOTO SHINJI
IPC: C12P21/02 , A61K38/00 , A61P35/00 , A61P37/04 , A61P43/00 , C07K1/06 , C07K5/02 , C07K14/195 , C07K14/41 , C12R1/465
Abstract: NEW MATERIAL:Lactyl-alanyl-glutamyl-mesodiaminopimelyl-glycine I and its pharmaceutically permissible acid-addition salt. USE:An immune response accelerator, a reticulo-endothelial system exasperator, an interferon producer, a juvenescent substance, a phylaxis substance, a carcinostatic substance, etc. PROCESS:A compound II (R is protected OH; R is OH-protecting goup) is reacted with a compound III [R is (protected) OH or (protected) hydrazino; R is NH2- protecting group; R is (protected) OH] to give the compound I-1. The reaction is carried out in a solvent in the presence of a condensing agent. The protecting group of the product is removed by e.g. reduction, hydrolysis, etc., to give the compound I. The compound I can be also obtained by culturing streptomyces in the fermentation method. Some of the compounds II and III are new compounds.
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公开(公告)号:JPS52118402A
公开(公告)日:1977-10-04
申请号:JP3654876
申请日:1976-03-31
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KURODA YOSHIO , OKUHARA MASAKUNI , AOKI HATSUO , IMANAKA HIROSHI
Abstract: PURPOSE:Antibiotic substance FR-900012 having the following properties. Values of elementary analysis; C 45.47%, H 5.14%, N 17.48%: specific rotation, [alpha] 5D=-28.0 deg.: melting point, 198-202 deg.C?UV absorption spectrum, =215.272nm.=215nm: IR absorption spectrum; =3880, 3080, 2940, 2750, 2650cm 1, etc; solubility: easily soluble water, slightly soluble to methanol, ninhydrin, etc., positive; Dragendorff, negative: amphoteric: colorless acicular crystal
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公开(公告)号:JPS5154988A
公开(公告)日:1976-05-14
申请号:JP11110674
申请日:1974-09-26
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: OKUHARA MASAKUNI , KURODA YOSHIO , UMEHARA KATSUYOSHI , KOSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI
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公开(公告)号:JPS63258488A
公开(公告)日:1988-10-25
申请号:JP5443588
申请日:1988-03-08
Applicant: FUJISAWA PHARMACEUTICAL CO
Inventor: KURODA YOSHIO , IGUCHI HIDEKO , KOSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI , KITAURA YOSHIHIKO , NAKAGUCHI OSAMU , HENMI KEIJI , ARAYA MATSUHIKO , TAKENO SHUICHI , OKADA TATSU , TANAKA HIROKAZU , HASHIMOTO SHINJI
IPC: A61K38/00 , A61K31/195 , A61K31/22 , A61K31/27 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/455 , A61K39/00 , A61K39/39 , A61P5/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/04 , C07C67/00 , C07C237/12 , C07C237/22 , C07C239/00 , C07C271/22 , C07D207/28 , C07D213/82 , C07D333/24 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K9/00
Abstract: NEW MATERIAL:A compound (salt) expressed by formula I (R represents H or acyl; Rb represents H, methyl, isopropyl, benzyl, etc.; R and R represent H, carboxyl, etc.; RD represents H, carboxyl, etc.; R represents H or amino- protecting group; (m) is 1-3; (n) is 1-2; R represents H, protected carboxyl, etc.) when R represents H, tert-butoxycarbonyl, etc.; (m) is 2 and (n) is 1; R represents H, protected carboxyl, etc.; when R represents lactoyl, Rb represents methyl, (m) is 2, (n) is 1, R and R represent carboxyl and R represents H, R represents H, carboxyl, etc.). USE:Useful as midicines having immunoresponse promoting action, reticuloendothelial system enhancing action, interferon-production activity, juvenilization activity, phylaxis effect, antitumor action, etc. PREPARATION:A compound expressed by formula II is reacted with a compound expressed by formula III to afford a compound expressed by formula IV (Rc represents acyl; R1 represents H or protected carboxyl; R1 represents amino- protecting group).
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