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1. 发明授权

US4925877A Physiologically active erbstatin analogue compounds and compositions 失效
标题翻译：生理活性的erbstatin类似物和组合物
公开(公告)号：US4925877A
公开(公告)日：1990-05-15
申请号：US17108
申请日：1987-02-20
申请人： Hamao Umezawa, deceased , Tomio Takeuchi , Kuniaki Tatsuta , Kunio Isshika , Masaya Imoto
发明人： Hamao Umezawa, deceased , Tomio Takeuchi , Kuniaki Tatsuta , Kunio Isshika , Masaya Imoto
IPC分类号： A01N37/18 , A01N47/40 , A61K31/16 , A61K31/165 , A61K31/24 , A61K31/275 , C07C233/16
CPC分类号： C07C251/00
摘要： The present invention provides new physiological active substance erbstatin analogue compounds of a general formula (I), which have excellent tyrosine-specific protein-kinase inhibitory activity, antitumor activity and antimicrobial activity. ##STR1## (in which R.sup.1 represents a hydrogen atom, a lower alkanoyl group or a lower alkyl group; n represents a positive integer of 1 to 3;X represents a hydrogen atom or a halogen atom;Y represents a group of formula --CH.dbd.CH--NC, --CH.dbd.CH--NHR.sup.2 or --CH.sub.2 --CH.sub.2 --NHR.sup.2(where R.sup.2 represents a formyl group or a lower alkanoyl group; with the exception of the cases where X is hydrogen atom, (R.sup.1 O).sub.n group is 2,5-dihydroxy group and Y is --CH.dbd.CH--NHCHO or --CH.sub.2 --CH.sub.2 --NHCHO).The present invention further provides a tyrosine-specific protein-kinase inhibitor, tumoricide or bactericide containing at least one compound of the said formula (I).
摘要翻译：本发明提供了具有优异的酪氨酸特异性蛋白激酶抑制活性，抗肿瘤活性和抗菌活性的通式（I）的新的生理活性物质抑制剂类似物化合物。（I）（其中R 1表示氢原子，低级烷酰基或低级烷基; n表示1〜3的正整数; X表示氢原子或卤素原子; Y表示式-CH = CH-NC，-CH = CH-NHR 2或-CH 2 -CH 2 -NH 2（其中R 2表示甲酰基或低级烷酰基;除了X是氢原子，（R 1 O）n 基团是2,5-二羟基，Y是-CH = CH-NHCHO或-CH 2 -CH 2 -NHCHO），本发明还提供一种酪氨酸特异性蛋白激酶抑制剂，杀伤剂或杀菌剂，其含有至少一种化合物所述式（I）。

2. 发明申请

US20060211638A1 Exon 1 ss of pdgf alpha gene and utilization thereof 审中-公开
标题翻译： pdgfα基因的外显子1 ss及其利用
公开(公告)号：US20060211638A1
公开(公告)日：2006-09-21
申请号：US10534836
申请日：2003-11-14
申请人： Masaya Imoto , Yusuke Minato , Etsu Tashiro
发明人： Masaya Imoto , Yusuke Minato , Etsu Tashiro
IPC分类号： A61K48/00 , C07H21/02 , C12N15/87
CPC分类号： C12N15/1138 , A61K31/7088
摘要： By using an antisense nucleotide, a ribozyme, a maxizyme, or an RNAi constructed based on the nucleotide sequence of exon 1 beta of the PDGF receptor alpha gene, which is expressed in specific cancer cells, or a polypeptide containing a portion thereof, translation of an mRNA transcribed from exon 1 beta of the PDGF receptor alpha gene is suppressed. An agent for suppressing expression containing as an active ingredient a substance for inhibiting expression, such as an antisense nucleotide, a ribozyme, a maxizyme, or an RNAi, is effective as a therapeutic agent for cancer.
摘要翻译：通过使用基于在特定癌细胞中表达的PDGF受体α基因的外显子1β的核苷酸序列构建的反义核苷酸，核酶，maxizyme或RNAi，或含有其部分的多肽，翻译从PDGF受体α基因的外显子1β转录的mRNA被抑制。抑制表达的物质作为活性成分的表达抑制剂如反义核苷酸，核酶，maxizyme或RNAi，作为癌症的治疗剂是有效的。

3. 发明授权

US4565861A Serirubicum 失效
标题翻译：丝。属
公开(公告)号：US4565861A
公开(公告)日：1986-01-21
申请号：US567792
申请日：1984-01-03
申请人： Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Hiroshi Naganawa , Tsutomu Sawa , Takeshi Uchida , Masaya Imoto
发明人： Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Hiroshi Naganawa , Tsutomu Sawa , Takeshi Uchida , Masaya Imoto
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P35/00 , C07H15/252 , C12P19/56 , C12R1/465 , C07H15/24
CPC分类号： C07H15/252 , C12P19/56 , C12R1/465
摘要： An anthracycline, serirubicin, of the formula: ##STR1## wherein R represents the substituent: ##STR2## is produced by a process which comprises cultivating a strain of Streptomyces in a suitable culture medium under aerobic conditions, said strain having the ability to produce the anthracycline compound, serirubicin, and then recovering the anthracycline compound, serirubicin, from the cultured medium. This serirubicin, or an acid addition salt of the serirubicin, can be contained as the active ingredient in anti-tumor agents and in pharmaceutical compositions for treatment of infections induced by gram-positive microorganisms, whereby good results are attainable.
摘要翻译：蒽环霉素，维拉霉素，其结构式如下：其中R表示取代基：IMAMA是通过包括在需氧条件下在合适的培养基中培养链霉菌属菌株的方法产生的，所述菌株具有产生蒽环霉素化合物，苏维菌素，然后从培养基中回收蒽环霉素化合物，丝衣霉素。作为抗肿瘤剂和用于治疗由革兰氏阳性微生物诱导的感染的药物组合物，可以含有这种苏维菌素或者苏维菌素的酸加成盐作为活性成分，从而获得了良好的效果。

4. 发明申请

US20080167201A1 Method For Synthesizing Derivative, Compound Library and Method For Constructing the Same, and Method For Screening 审中-公开
标题翻译：合成衍生物，化合物库及其构建方法的方法和筛选方法
公开(公告)号：US20080167201A1
公开(公告)日：2008-07-10
申请号：US11663082
申请日：2005-09-27
申请人： Masaya Imoto , Hiromichi Ohta , Kenji Miyamoto
发明人： Masaya Imoto , Hiromichi Ohta , Kenji Miyamoto
IPC分类号： C40B30/10 , C12P1/00 , C12P1/04 , C12P1/02 , C40B50/06 , C40B40/04 , C40B30/00
CPC分类号： C12P17/16 , C07D405/06 , G01N2500/00
摘要： [Object] To provide a method for synthesizing derivatives of natural compounds; a method for constructing a compound library containing derivatives of natural compounds; a compound library containing derivatives of natural compounds; and a screening method using a compound library, which are useful for a HTS random screening, a search for drugs or agricultural chemicals, or a search for a lead compound of a drug or an agricultural chemical.[Solving Means] A derivative of an organic compound can be synthesized by culturing a microorganism producing the organic compound in a predetermined culture broth, and reacting the organic compound obtained by the culturing with a reaction reagent for synthesizing the derivative of the organic compound in the culturing broth. By constructing a library containing the thus obtained organic compound derivative, a HTS (high-throughput) random screening, a search for a drug or agricultural chemical, or a search for a lead compound of a drug or agricultural chemical can be performed.
摘要翻译：提供合成天然化合物衍生物的方法; 一种构建含有天然化合物衍生物的化合物文库的方法; 含有天然化合物衍生物的化合物库; 以及使用化合物文库的筛选方法，其可用于HTS随机筛选，寻找药物或农药，或搜索药物或农药的铅化合物。 [解决方案]有机化合物的衍生物可以通过在预定的培养肉汤中培养产生有机化合物的微生物来合成，并将通过培养获得的有机化合物与用于合成有机化合物的衍生物的反应试剂反应培养肉汤通过构建含有这样得到的有机化合物衍生物的文库，可以进行HTS（高通量）随机筛选，药物或农药的检索，或者寻找药物或农药的铅化合物。

5. 发明授权

US4550159A Anthracycline compounds 失效
标题翻译：蒽环类化合物
公开(公告)号：US4550159A
公开(公告)日：1985-10-29
申请号：US545137
申请日：1983-10-25
申请人： Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Hiroshi Naganawa , Tsutomu Sawa , Takeshi Uchida , Masaya Imoto
发明人： Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Hiroshi Naganawa , Tsutomu Sawa , Takeshi Uchida , Masaya Imoto
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P19/56 , C12R1/465 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , C12P19/56 , C12R1/465
摘要： An anthracycline compound, ditrisarubicin, of the formula: ##STR1## wherein R represents one of the following substituents (A), (B), and (C): ##STR2## is produced by a process which comprises cultivating a strain of Streptomyces in a suitable culture medium under aerobic conditions, said strain having the ability to produce the anthracycline compound, ditrisarubicin, and then recovering the anthracycline compound, ditrisarubicin, from the cultured medium. This ditrisarubicin, or an acid addition salt of the ditrisarubicin, can be contained as the active ingredient in antitumor agents and in pharmaceutical compositions for treatment of infections induced by gram-positive microorganisms, whereby good results are attainable.
摘要翻译：其中R代表以下取代基之一（A），（B）和（C）的蒽环类化合物，二硝基菌素：其中R代表下列取代基之一：（A） C）是通过包括在有氧条件下在合适的培养基中培养链霉菌菌株的方法生产的，所述菌株具有生产蒽环类化合物，二硝酸菌素的能力，然后从培养基中回收蒽环类化合物二硝酸菌素。这种二硝维菌素或二硝基阿霉素的酸加成盐可以作为活性成分包含在抗肿瘤剂和用于治疗由革兰氏阳性微生物诱导的感染的药物组合物中，从而获得良好的结果。

6. 发明申请

US20060246047A1 Peptide wirh apoptosis-inhibiting activity 审中-公开
标题翻译：肽纤维细胞凋亡抑制活性
公开(公告)号：US20060246047A1
公开(公告)日：2006-11-02
申请号：US10562143
申请日：2004-06-24
申请人： Masaya Imoto , Hirokazu Tabe , Etsu Tashiro , Yusuka Ohmori
发明人： Masaya Imoto , Hirokazu Tabe , Etsu Tashiro , Yusuka Ohmori
IPC分类号： A61K38/54 , C07H21/04 , C12P21/06 , C12N9/99
CPC分类号： C07K14/4747 , A61K38/00 , C07K2319/21 , C07K2319/60
摘要： A peptide consisting of part of the amino acid sequence of SEQ ID No: 8 and having an amino acid sequence of SEQ ID No: 1 or SEQ ID No: 2, e.g., a peptide consisting of the amino acid sequence of any one of SEQ ID Nos: 1 to 5, has an excellent apoptosis-suppressive activity. Therefore, a peptide consisting of part of the amino acid sequence of SEQ ID No: 8 and having an amino acid sequence of SEQ ID No: 2, particularly SEQ ID No: 1, is useful as a pharmaceutical composition for a Bax-dependent apoptosis-induced disease, such as a neurodegenerative disease.
摘要翻译：由SEQ ID No：8的氨基酸序列的一部分组成并且具有SEQ ID No：1或SEQ ID No：2的氨基酸序列的肽，例如由SEQ ID No：8中任一项的氨基酸序列组成的肽 ID号：1〜5，具有优异的细胞凋亡抑制活性。因此，由SEQ ID No：8的氨基酸序列的一部分构成并具有SEQ ID No：2的氨基酸序列，特别是SEQ ID No：1的肽可用作Bax依赖性细胞凋亡的药物组合物引起的疾病，如神经退行性疾病。

7. 发明授权

US4686308A Novel physiologically active substance MH435 失效
标题翻译：新型生理活性物质MH435
公开(公告)号：US4686308A
公开(公告)日：1987-08-11
申请号：US879069
申请日：1986-06-26
申请人： Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Hiroshi Naganawa , Tsutomu Sawa , Masaya Imoto , Hironobu Iinuma , Takeshi Uchida , Kunio Isshiki
发明人： Hamao Umezawa , Tomio Takeuchi , Masa Hamada , Hiroshi Naganawa , Tsutomu Sawa , Masaya Imoto , Hironobu Iinuma , Takeshi Uchida , Kunio Isshiki
IPC分类号： C12P13/02 , A61K31/16 , A61P31/04 , A61P35/00 , C07C67/00 , C07C231/00 , C07C233/18 , C07C233/22 , C12P13/00 , C12R1/465 , C07C103/34
CPC分类号： C12P13/02 , C12R1/465
摘要： Disclosed is a novel physiologically active substance, MH435, represented by the formula: ##STR1## wherein R represents either of the following groups A and B A: --CH.dbd.CH--NHCHOB: --CH.sub.2 --CH.sub.2 --NHCHO.The substance MH435 has an inhibitory activity against tyrosine specific protein kinase, and the 50% inhibitory concentrations of the substances MH435-A and MH435-B are respectively 0.55 .mu.g/ml and 6.0 .mu.g/ml.
摘要翻译：公开了一种新的生理活性物质MH435，由下式表示：其中R表示以下基团A和B A之一：A = -CH = CH-NHCHO B：-CH 2 -CH 2 -NHCHO。物质MH435具有对酪氨酸特异性蛋白激酶的抑制活性，MH435-A和MH435-B物质的50％抑制浓度分别为0.55μg/ ml和6.0μg/ ml。

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