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1. 发明授权

US4877870A Process for producing 10-hydroxyanthracyclines 失效
标题翻译：生产10-羟基蒽环的方法
公开(公告)号：US4877870A
公开(公告)日：1989-10-31
申请号：US68630
申请日：1987-06-30
申请人： Hamao Umezawa, deceased , Kuniaki Tatsuta , Hiroyuki Kawai , Shohachi Nakajima
发明人： Hamao Umezawa, deceased , Kuniaki Tatsuta , Hiroyuki Kawai , Shohachi Nakajima
IPC分类号： C07C50/36 , A61K31/65 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07C45/00 , C07C46/00 , C07C50/38 , C07C67/00 , C07H15/252 , C12P19/56 , C12R1/03
CPC分类号： C07H15/252
摘要： Disclosed is a process for producing a 10-hydroxyanthracycline of the following formula (II) which comprises reacting a compound of the following formula (I) or an acid addition salt thereof with an N-oxide of a tertiary amine ##STR1## wherein: R.sup.1 through R.sup.6 each designate any of H, OH and OCH.sub.3 ; R.sup.7 designates any of H, OH and a sugar residue; and R.sup.8 designates any of C.sub.2 H.sub.5, COCH.sub.3, CH(OH)CH.sub.3, CH(OH)CH.sub.2 (OH) and COCH.sub.2 OH. In accordance with this process, it is possible to efficiently introduce a hydroxyl group into the 10-position of an anthracycline having no substitutent at the same position thereof.
摘要翻译：公开了一种制备下式（II）的10-羟基蒽环的方法，其包括使下式（I）的化合物或其酸加成盐与叔胺的N-氧化物反应（I）（II）其中：R 1至R 6各自表示H，OH和OCH 3中的任一个; R7表示H，OH和糖残基中的任一个; 并且R 8表示任何C 2 H 5，COCH 3，CH（OH）CH 3，CH（OH）CH 2（OH）和COCH 2 OH。根据该方法，可以在相同位置的无结构的蒽环类的10位上有效地引入羟基。

2. 发明授权

US4818818A Method for the preparation of 4'-0-tetrahydropyranyladriamycin b 失效
标题翻译：制备4'-O-四氢吡喃阿霉素的方法b
公开(公告)号：US4818818A
公开(公告)日：1989-04-04
申请号：US925774
申请日：1986-10-30
申请人： Hamao Umezawa, deceased , Tomio Takeuchi , Kuniaki Tatsuta , Yoshikazu Takahashi
发明人： Hamao Umezawa, deceased , Tomio Takeuchi , Kuniaki Tatsuta , Yoshikazu Takahashi
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： For the preparation of 4'-0-tetrahydropyranyladriamycin b, the 9,14-position of the starting adriamycin is previously protected with phenylboronic acid and then the 4'-position of the thus protected adriamycin is selectively tetrahydropyranylated. After the tetrahydropyranylation, the by-product of 4'-0-tetrahydropyranyladriamycin a is converted to the aimed product of 4'-0-tetrahydropyranyladriamycin b. The yield of the product of 4'-0-tetrahydropyranyladriamycin b is high.The present invention provides a method for the preparation of 4'-0-tetrahydropyranyladriamycin b, where 3,4-dihydro-2H-pyran is added to a reaction solution containing a 9,14-protected adriamycin as obtained by (a) reacting adriamycin and phenyl-boronic acid or (b) reacting 4'-0-tetrahydropyranyladriamycin b and phenylboronic acid in the presence of an acid catalyst, for 4'-tetrahydropyranylation of the said 9,14-protected adriamycin, and then, the 9,14-protected position of the resulting product is deprotected and 4'-0-tetrahydropyranyladriamycin b is isolated by chromatography with silica-gel.
摘要翻译：为了制备4'-O-四氢吡喃阿霉素b，起始阿霉素的9,14位预先用苯基硼酸保护，然后由此保护的阿霉素的4'-位选择性地被四氢吡喃基化。四氢吡喃基化后，4'-O-四氢吡喃阿霉素a的副产物转化为4'-O-四氢吡喃基阿霉素b的目标产物。 4'-O-四氢吡喃阿霉素b的产物的产率高。本发明提供了制备4'-O-四氢吡喃阿霉素b的方法，其中将3,4-二氢-2H-吡喃加入到含有9,14-保护的阿霉素的反应溶液中，其通过以下步骤获得：（a）使阿霉素和苯基硼酸或（b）在酸催化剂存在下使4'-O-四氢吡喃阿霉素b和苯基硼酸反应，进行所述9,14受保护的阿霉素的4'-四氢吡喃基化，然后，9,14 将所得产物的保护位置脱保护，并用硅胶色谱分离4'-O-四氢吡喃基阿霉素b。

3. 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）。

4. 发明授权

US4870207A Synthesis of arphamenine A 失效
标题翻译：阿芬太尼A的合成
公开(公告)号：US4870207A
公开(公告)日：1989-09-26
申请号：US79319
申请日：1987-07-30
申请人： Hamao Umezawa, deceased , Takaaki Aoyagi , Kuniaki Tatsuta , Takeshi Nakamura , Shunzo Fukatsu
发明人： Hamao Umezawa, deceased , Takaaki Aoyagi , Kuniaki Tatsuta , Takeshi Nakamura , Shunzo Fukatsu
IPC分类号： A61K31/195 , A61K31/40 , A61P25/04 , A61P37/04 , C07C67/00 , C07C229/22 , C07C229/34 , C07C239/00 , C07C277/00 , C07C279/14 , C07C313/00 , C07C323/62 , C07D207/08 , C07D233/64 , C07D309/12
CPC分类号： C07D207/08 , C07C279/14 , Y02P20/55
摘要： Known compound, optically active arphamenine A can now be synthesized in an optically active pure form and in a favorable yield by a new process comprising consecutive steps with starting from L-arginine, wherein racemization of intermediate reaction products can be minimized.
摘要翻译：已知的化合物，光学活性的阿仑非因A现在可以通过包含从L-精氨酸开始的连续步骤的新方法以光学活性的纯形式合成并以有利的产率合成，其中中间反应产物的外消旋化可以最小化。

5. 发明授权

US4851446A Immunosuppressing method 失效
标题翻译：免疫抑制法
公开(公告)号：US4851446A
公开(公告)日：1989-07-25
申请号：US022409
申请日：1987-03-06
申请人： Hamao Umezawa, deceased , Tomio Takeuchi , Masaaki Ishizuka , Fuminori Abe , Akio Fujii , Teruya Nakamura
发明人： Hamao Umezawa, deceased , Tomio Takeuchi , Masaaki Ishizuka , Fuminori Abe , Akio Fujii , Teruya Nakamura
IPC分类号： A61K31/16 , A61K31/165 , C07C279/18
CPC分类号： A61K31/165 , A61K31/16 , C07C279/18 , Y10S514/885
摘要： The present invention relates to an immunosuppressing method which comprises administering a spergualin-related compound represented by the following formula ##STR1## (wherein R.sub.1 is --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.6 --, ##STR2## R.sub.2 is --(CH.sub.2).sub.2 -- or --CH.dbd.CH--; and R.sub.3 is ##STR3## or pharmacologically acceptable salts thereof in an effective amount to a warm-blood animal.
摘要翻译：本发明涉及一种免疫抑制方法，其包括给予由下式表示的精神药蛋白相关化合物+ TR NH（CH 2）3 NH（其中R 1为 - （CH 2）4 - ， - （CH 2）对于温血动物，R 2是有效量的 - （CH 2）2 - 或-CH = CH-;且R 3是或其药学上可接受的盐。

6. 发明授权

US4795743A 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives of low toxicity 失效
标题翻译： 2'-脱氨基-2'-羟基马斯汀Bo衍生物低毒
公开(公告)号：US4795743A
公开(公告)日：1989-01-03
申请号：US21781
申请日：1987-03-04
申请人： Yoshiro Okami , Shinichi Kondo , Daishiro Ikeda , Hamao Umezawa, deceased
发明人： Yoshiro Okami , Shinichi Kondo , Daishiro Ikeda , Hamao Umezawa, deceased
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61P31/04 , C07H15/222 , C07H15/224 , C07H15/22
CPC分类号： C07H15/224
摘要： As new 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives are provided four compounds, namely 2'-deamino-2'-hydroxyistamycin B; 2'-deamino-2'-hydroxy-3-O-demethylistamycin B; 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxyistamycin B.sub.o ; and 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxy-3-O-demethylistamycin B.sub.o which all exhibit high antibacterial activity and low acute toxicity in combination. These new compounds are useful as antibacterial agent.
摘要翻译：作为新的2'-脱氨基-2'-羟基毛霉素Bo衍生物，提供四种化合物，即2'-脱氨基-2'-羟基毛霉素B; 2'-脱氨基-2'-羟基-3-O-脱甲基霉素B; 4-N-（β-丙氨酰基）-2'-脱氨基-2'-羟基毛霉素Bo; 和4-N-（β-丙氨酰基）-2'-脱氨基-2'-羟基-3-O-脱甲基丝杆霉素B B，其组合表现出高的抗菌活性和低的急性毒性。这些新化合物可用作抗菌剂。

7. 发明授权

US4897470A Anthracycline antibiotics DCP-1 and 2 失效
标题翻译：蒽环类抗生素DCP-1和2
公开(公告)号：US4897470A
公开(公告)日：1990-01-30
申请号：US34879
申请日：1987-04-06
申请人： Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa, deceased
发明人： Akihiro Yoshimoto , Osamu Jodo , Yoshio Watanabe , Tomoyuki Ishikura , Tsutomu Sawa , Tomio Takeuchi , Hamao Umezawa, deceased
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C12P29/00 , C12R1/465
CPC分类号： C07H15/252
摘要： New anthracycline antibiotics of a formula (I) are provided, which are usable as an anticancer agent ##STR1## (where R represents a hydrogen atom or a hydroxyl group). The antibiotics (I) can be produced by incubation of a dye-nonproductive or hardly dye-productive mutant strain which has an ability of converting .alpha.-citromycinone or .beta.-isorhodomycinone into the antibiotics (I), in the presence of .alpha.-citromycinone or .beta.-isorhodomycinone in a pertinent nutrient medium.

8. 发明授权

US5202427A DNA segment containing streptomycin resistance gene and being capable of controlling expression of said gene 失效
标题翻译：含有链霉素抗性基因并能够控制所述基因表达的DNA片段
公开(公告)号：US5202427A
公开(公告)日：1993-04-13
申请号：US659469
申请日：1991-02-25
申请人： Hamao Umezawa, deceased , Yoji Umezawa, heir , Yoji Umezawa, heir , Yoshiro Okamo, heir
发明人： Hamao Umezawa, deceased , Yoji Umezawa, heir , Yoji Umezawa, heir , Yoshiro Okamo, heir
IPC分类号： C12N9/12 , C12N15/76
CPC分类号： C12N15/76 , C12N9/12
摘要： A DNA segment of this invention is a DNA fragment of a length of about 3.8 kb which is obtained by excising with a restriction endonuclease Bgl II a hybrid plasmid pST 141 having a length of about 12.6 kb of Streptomyces griseus 4-1 strain (FERM P-7984, namely, FERM BP-1198) to give a Bgl II-Bgl II DNA fragment, and then excising with a restriction endonuclease Sph I the resultant Bgl II-Bgl II DNA fragment having a length of about 7.0 kb and having the restriction endonuclease sites as shown in the restriction endonuclease map of FIG. 1 . This DNA fragment is a DNA which contains a streptomycin resistance gene and contains, in the vicinity of this gene, such a DNA region possessing a function to control the expression of the streptomycin resistance gene. An insertion of this DNA fragment having a length of about 3.8 kb into a suitable actinomycetes plasmid vector can produce such a hybrid plasmid which acts reliably as a selected marker of the streptomycin resistance.
摘要翻译：本发明的DNA片段是长约3.8kb的DNA片段，其通过用限制性内切核酸酶Bgl II切割具有长度为约12.6kb的灰色链霉菌4-1菌株（FERM P）的杂交质粒pST141获得 -7984，即FERM BP-1198），得到Bgl II-Bgl II DNA片段，然后用限制性内切核酸酶SphI切割得到长度为约7.0kb并具有约束条件的所得Bgl II-Bgl II DNA片段如图1的限制性内切核酸酶图所示的内切核酸酶位点。 1。该DNA片段是含有链霉素抗性基因的DNA，该基因附近含有具有控制链霉素抗性基因表达功能的DNA区域。将具有约3.8kb长度的该DNA片段插入合适的放线菌质粒载体中可以产生这样的杂交质粒，其可靠地作为链霉素抗性的选择标记物起作用。

9. 发明授权

US4956504A Novel spergualin-related compounds and process for producing the same 失效
标题翻译：新型精毒素相关化合物及其制备方法
公开(公告)号：US4956504A
公开(公告)日：1990-09-11
申请号：US32811
申请日：1987-04-01
申请人： Tomio Takeuchi , Tetsushi Saino , Masao Yoshida , Katsutoshi Takahashi , Teruya Nakamura , Hamao Umezawa, deceased
发明人： Tomio Takeuchi , Tetsushi Saino , Masao Yoshida , Katsutoshi Takahashi , Teruya Nakamura , Hamao Umezawa, deceased
IPC分类号： A61K31/40 , A61K31/16 , A61K38/00 , A61P35/02 , A61P37/00 , A61P37/06 , C07C67/00 , C07C239/00 , C07C279/14 , C07C279/18 , C07D207/16 , C07K5/06
CPC分类号： C07C279/14 , C07C279/18 , Y02P20/55
摘要： The present invention relates to novel Spergualin-related compounds represented by the general formula [I] ##STR1## (wherein X is ##STR2## R is --H or --CH.sub.2 OH; R.sub.1 is --H, ##STR3## R.sub.2 is a residue obtained by removing, from an amino acid or peptide, the hydroxyl group of the carboxyl group and, when R.sub.1 is a group other than --H, R.sub.2 is same as R.sub.1), or a pharmacologically acceptable salt thereof. Said compounds or salts thereof have an immuno-modulating action.
摘要翻译：本发明涉及由通式[I]＆lt; IMAGE＆gt;（其中X为R为-H或-CH 2 OH; R 1为-H，R 2为囟素或者其药理学上可接受的盐，通过从氨基酸或肽除去羧基的羟基而得到的残基，当R 1为除-H以外的基团时，R 2与R 1相同。所述化合物或其盐具有免疫调节作用。

10. 发明授权

US4870172A Bisucaberin 失效
公开(公告)号：US4870172A
公开(公告)日：1989-09-26
申请号：US74369
申请日：1987-07-16
申请人： Yoshiro Okami , Shogo Kurasawa , Toshiyuki Kamayama , Atsushi Takahashi , Masaaki Ishizuka , Hamao Umezawa, deceased
发明人： Yoshiro Okami , Shogo Kurasawa , Toshiyuki Kamayama , Atsushi Takahashi , Masaaki Ishizuka , Hamao Umezawa, deceased
IPC分类号： A61K31/395 , A61P35/00 , C07D257/02 , C12P17/10 , C12R1/01
CPC分类号： C12R1/01 , C07D257/02 , C12P17/10
摘要： A novel compound having anti-tumor activity is disclosed which is 1,12-dihydroxy-1,6,12,17-tetraazacyclodocosan-2,5,13,16-tetrone produced microbiologically by culturing a microorganism belonging to the genus of Alteromonas or, in particular, Alteromonas haloplanktis SB-1123. The characterization data of the compound and the microbiological properties of the microorganism are described. The results of in vitro assays are given for the anti-tumor activity of the compound against L-1210 and IMC carcinoma cells.

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