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1.发明申请公开(公告)号：US20050256090A1
公开(公告)日：2005-11-17
申请号：US11187073
申请日：2005-07-21
IPC分类号： A61K31/675 , A61P7/00 , A61P31/00 , A61P43/00
CPC分类号： A61K31/675
摘要： A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): wherein n is an integer of 0 to 3, or a pharmacologically acceptable salt thereof.
摘要翻译： 一种用于预防或治疗骨髓抑制，用于治疗感染性疾病和增加白细胞数量的药物，其包含作为活性成分的由通式（I）表示的磺酰头孢菌素相关化合物：其中n为整数0 3，或其药理学上可接受的盐。
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2.发明授权公开(公告)号：US07247640B2
公开(公告)日：2007-07-24
申请号：US11187073
申请日：2005-07-22
IPC分类号： A61K31/435 , A61K31/40 , C07D221/92
CPC分类号： A61K31/675
摘要： A medicament for prophylaxis or treatment of bone marrow suppression, for treatment of infectious diseases and for increasing the number of leukocytes, which comprise as an active ingredient a sulphostin-related compound represented by general formula (I): wherein n is an integer of 0 to 3, or a pharmacologically acceptable salt thereof.
摘要翻译： 一种用于预防或治疗骨髓抑制，用于治疗感染性疾病和增加白细胞数量的药物，其包含作为活性成分的由通式（I）表示的磺酰头孢菌素相关化合物：其中n为整数0 3，或其药理学上可接受的盐。
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公开(公告)号：US6043217A
公开(公告)日：2000-03-28
申请号：US915118
申请日：1997-08-20
CPC分类号： C07K5/06139 , A61K38/00
摘要： Novel amide derivatives of amythiamicin are now provided, which are soluble in water and exhibit antibacterial activities, some of which exhibit an excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
摘要翻译： 现在提供了新型的氨基安定胺衍生物，其可溶于水并具有抗菌活性，其中一些对耐甲氧西林金黄色葡萄球菌（MRSA）具有优异的抗菌活性。
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公开(公告)号：US5756763A
公开(公告)日：1998-05-26
申请号：US581507
申请日：1996-01-11
申请人： Tomio Takeuchi , Takaaki Aoyagi , Yasuhiko Muraoka , Makoto Tsuda
发明人： Tomio Takeuchi , Takaaki Aoyagi , Yasuhiko Muraoka , Makoto Tsuda
IPC分类号： C07D207/08 , C07D207/16 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/10 , C07D409/10 , C07D521/00 , C07D207/14 , C07D217/04 , C07D233/24 , C07D265/30
CPC分类号： C07D207/08 , C07D207/16 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/10 , C07D409/10
摘要： The invention relates to novel pyrrolidine derivatives represented by formula (1): ##STR1## wherein: R1 represents (1) a lower alkyl group having 1 to 6 carbon atoms, or (2) a 3- to 15-membered mono- or fused cyclic hydrocarbon group which may contain a hetero atom on the ring, or which may be substituted with a substituent(s); each of n and m represents an integer and the sum of n and m is an integer of 0 to 2; each of X and E represents oxygen, NR' (wherein R' is hydrogen or a lower alkyl group having 1 to 6 carbon atoms), sulfur, phenylene, CH.dbd.CH or CH.sub.2 ; A represents an amino acid residue or an imino acid residue, which functional group may be optionally protected, or a glycine residue which may be substituted at the amino moiety thereof; and, Y1 represents a cycloalkyl group having 3 to 8 carbon atoms; or a salt thereof. The pyrrolidine derivatives inhibit a prolyl endopeptidase and are expected to be effective for the treatment of amnesia.
摘要翻译： PCT No.PCT / JP94 / 01208 Sec。 371日期1996年1月11日 102（e）日期1996年1月11日PCT提交1994年7月22日PCT公布。 出版物WO95 / 03277 日期：1995年2月2日本发明涉及由式（1）表示的新型吡咯烷衍生物：其中：R1表示（1）具有1-6个碳原子的低级烷基，或（2）3- 至15元单环或稠合环烃基，其可以在环上含有杂原子，或可以被取代基取代; n和m各自表示整数，n和m的和为0〜2的整数， X和E各自表示氧，NR'（其中R'是氢或具有1至6个碳原子的低级烷基），硫，亚苯基，CH = CH或CH 2; A表示可以任选保护的氨基酸残基或亚氨基酸残基，或其氨基部分可被取代的甘氨酸残基; Y1表示碳原子数3〜8的环烷基。 或其盐。 吡咯烷衍生物抑制脯氨酰内肽酶，并且预期对于治疗遗忘症是有效的。
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公开(公告)号：US5359138A
公开(公告)日：1994-10-25
申请号：US905792
申请日：1992-06-29
申请人： Tomio Takeuchi , Takaaki Aoyagi , Masa Hamada , Hiroshi Naganawa , Keiji Ogawa , Machiko Nagai , Yasuhiko Muraoka , Makoto Tsuda
发明人： Tomio Takeuchi , Takaaki Aoyagi , Masa Hamada , Hiroshi Naganawa , Keiji Ogawa , Machiko Nagai , Yasuhiko Muraoka , Makoto Tsuda
CPC分类号： C07K5/0202 , C07K7/02 , A61K38/00
摘要： A novel, biologically active substance, poststatin, has been isolated from a culture medium of microorganism belonging to Streptomyces. The novel substance is a peptide compound having a novel structure, wherein the peptide chains have ketone radicals. Thus substance has a high endopeptidase inhibition activity. It is possible to chemically synthesize poststatin related compound having ketone radicals in the peptide chains. These compounds also have an endopeptidase inhibition activity.
摘要翻译： 已经从属于链霉菌的微生物的培养基中分离出一种新的生物活性物质，后抑制素。 该新物质是具有新结构的肽化合物，其中肽链具有酮基。 因此，物质具有高内肽酶抑制活性。 可以在肽链中化学合成具有酮基的后抑制素相关化合物。 这些化合物还具有内肽酶抑制活性。
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6.发明授权公开(公告)号：US06579989B1
公开(公告)日：2003-06-17
申请号：US10009707
申请日：2001-11-13
IPC分类号： C07D20746
CPC分类号： C07F9/5532 , A61K31/675 , C07F9/568 , C07F9/572 , C07F9/59 , Y02P20/55
摘要： A sulphostin analogue represented by the general formula, wherein n is an integer of from 0 to 3, provided that a case where n is 2 and steric configurations of C* and P* are S and R, respectively, is excluded, or a pharmaceutically acceptable salt thereof.
摘要翻译： 由通式表示的磺普钠类似物，其中n为0-3的整数，条件是排除n为2的情况，C *和P *的空间构型分别为S和R，或药学上 其可接受的盐。
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7.发明授权Physiologically active substances, benastatins A and B, and production and use thereof 失效生理活性物质，B和B以及其生产和使用
公开(公告)号：US5117052A
公开(公告)日：1992-05-26
申请号：US669387
申请日：1991-03-14
申请人： Tomio Takeuchi , Takaaki Aoyagi , Hiroshi Naganawa , Masa Hamada , Yasuhiko Muraoka , Takayuki Aoyama
发明人： Tomio Takeuchi , Takaaki Aoyagi , Hiroshi Naganawa , Masa Hamada , Yasuhiko Muraoka , Takayuki Aoyama
CPC分类号： C07C65/40 , C12P15/00 , C07C2103/24
摘要： Benastatins A and B which are novel and physiologically active substances having the formula ##STR1## wherein R represents --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, exhibit a potent immunomodifier activity, a glutathione transferase inhibition activity and an anti-microorganism activity and are therefore extremely useful for various drugs.
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8.发明授权Physiologically active substance sulphostin, process for producing the same, and use thereof 有权生理活性物质磺普钠，其制备方法及其用途公开(公告)号：US06214340B1
公开(公告)日：2001-04-10
申请号：US09554362
申请日：2000-05-12
申请人： Tomio Takeuchi , Masa Hamada , Yasuhiko Muraoka , Tetsuo Akiyama , Masatoshi Abe , Hiroshi Naganawa , Yoshikazu Takahashi
发明人： Tomio Takeuchi , Masa Hamada , Yasuhiko Muraoka , Tetsuo Akiyama , Masatoshi Abe , Hiroshi Naganawa , Yoshikazu Takahashi
IPC分类号： C12N120
摘要： This invention provides a physiologically active substance having a strong dipeptidyl peptidase IV inhibitory activity. The physiologically active substance sulphostin is obtained by culturing a microorganism belonging to the genus Streptomyces and having an ability to produce the physiologically active substance sulphostin, producing and accumulating this substance in the cultures, and harvesting it from the cultures.
摘要翻译： 本发明提供具有强二肽基肽酶IV抑制活性的生理活性物质。 通过培养属于链霉菌属的微生物并且具有生产生理活性物质硫酸钙的能力，在培养物中产生和积累该物质，并从培养物中收获生物活性物质硫酸钙得到。
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公开(公告)号：US5221752A
公开(公告)日：1993-06-22
申请号：US729419
申请日：1991-07-12
申请人： Tetsuya Someno , Fumika Yamada , Hideo Sugimura , Yasuhiko Muraoka , Makoto Tsuda , Tomio Takeuchi , Takaaki Aoyagi
发明人： Tetsuya Someno , Fumika Yamada , Hideo Sugimura , Yasuhiko Muraoka , Makoto Tsuda , Tomio Takeuchi , Takaaki Aoyagi
IPC分类号： A61K31/40 , A61K31/401 , A61K38/00 , A61K38/55 , A61P43/00 , C07D207/08 , C07D207/09 , C07D211/34 , C07D211/60 , C07K5/02 , C07K5/06 , C07K7/02 , C07K14/81
CPC分类号： C07D207/08 , C07D207/09 , C07D211/34 , C07K5/0202 , C07K7/02 , A61K38/00 , Y02P20/55
摘要： The present invention discloses a new .alpha.-keto amide derivative or a salt thereof represented by the formula (1): ##STR1## wherein X represents (1) a peptide residue or amino acid residue in which the functional group may be protected, (2) a hydrogen atom or (3) an amino-protective group, Y represents a peptide residue or amino acid residue in which the functional group may be protected, E represents a substituent on the alkylene (C.sub.n H.sub.2n-1) and is a halogen, lower alkoxy or hydrogen, A represents a carbonyl group or mono- or di-substituted methylene (the substituent being a hydroxy, lower alkoxy, phenylimino or benzylimino), and n represents an integer of 2 to 6.The compound of the present invention is effective in inhibiting prolyl endopeptidase activity and useful as an active ingredient of an enzyme inhibitor.
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公开(公告)号：US5162500A
公开(公告)日：1992-11-10
申请号：US613759
申请日：1990-12-07
申请人： Tomio Takeuchi , Takaaki Aoyagi , Masa Hamada , Hiroshi Naganawa , Keiji Ogawa , Machiko Nagai , Yasuhiko Muraoka , Makoto Tsuda
发明人： Tomio Takeuchi , Takaaki Aoyagi , Masa Hamada , Hiroshi Naganawa , Keiji Ogawa , Machiko Nagai , Yasuhiko Muraoka , Makoto Tsuda
IPC分类号： A61K38/00 , C07C229/22 , C07C271/22 , C07K5/02 , C07K7/02
CPC分类号： C07C229/22 , C07C271/22 , C07K5/0202 , C07K7/02 , A61K38/00
摘要： A novel, biologically active substance, poststatin, has been isolated from a culture medium of microorganism belonging to Streptomyces. The novel substance is a peptide compound having a novel structure, wherein the peptide chains have ketone radicals. Thus substance has a high endopeptidase inhibition activity. It is possible to chemically synthesize poststatin related compound having ketone radicals in the peptide chains. These compounds also have an endopeptidase inhibition activity.
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