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1. 发明授权

US4556735A Spergualin-related compounds having a phenylene group as well as a process for producing the same 失效
标题翻译：具有亚苯基的精氨蝶呤相关化合物及其制备方法
公开(公告)号：US4556735A
公开(公告)日：1985-12-03
申请号：US706312
申请日：1985-02-27
申请人： Hamao Umezawa , Tomio Takeuchi , Rinzo Nishizawa , Katsutoshi Takahashi , Teruya Nakamura , Yoshihisa Umeda
发明人： Hamao Umezawa , Tomio Takeuchi , Rinzo Nishizawa , Katsutoshi Takahashi , Teruya Nakamura , Yoshihisa Umeda
IPC分类号： A61K31/165 , A61P31/04 , A61P35/00 , C07C67/00 , C07C239/00 , C07C277/08 , C07C279/14 , C07C279/18 , C07D209/48 , C07C103/28
CPC分类号： C07D209/48 , C07C279/14 , C07C279/18 , Y02P20/55
摘要： The invention relates to Spergualin-related compounds of the formula: ##STR1## (wherein R.sub.1 is a lower alkylene group which may be substituted by a hydroxymethyl group; X is a hydrogen atom or a halogen atom; m and n are each 0 or an integer of 1 to 5) and salts thereof and a process for producing the same.
摘要翻译：本发明涉及下列化学式的精神百灵素相关化合物：其中R 1为可被羟甲基取代的低级亚烷基; X为氢原子或卤素原子; m和n各自为0或1〜5的整数）及其盐及其制造方法。

2. 发明授权

US4529549A Spergualin-related compounds and process for the preparation thereof 失效
标题翻译：精毒素相关化合物及其制备方法
公开(公告)号：US4529549A
公开(公告)日：1985-07-16
申请号：US524354
申请日：1983-08-18
申请人： Hamao Umezawa , Tomio Takeuchi , Rinzo Nishizawa , Katsutoshi Takahashi , Teruya Nakamura , Yoshihisa Umeda
发明人： Hamao Umezawa , Tomio Takeuchi , Rinzo Nishizawa , Katsutoshi Takahashi , Teruya Nakamura , Yoshihisa Umeda
IPC分类号： A61K31/155 , A61K31/16 , A61K31/165 , A61K31/195 , A61K31/40 , A61K31/415 , A61P35/00 , A61P35/02 , C07C67/00 , C07C239/00 , C07C279/04 , C07C279/14 , C07D207/16 , C07D209/48 , C07D233/54 , C07D233/64 , C07F5/00 , C07F7/00
CPC分类号： C07D209/48 , C07C279/14 , C07D233/64 , Y02P20/55
摘要： This invention relates to a novel spergualin-related compound and a process for the production thereof. The novel compound, which has a high antitumor activity, is represented by the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, hydroxyl group, or an aliphatic acyloxy group having 1 to 10 carbon atoms, R.sub.2 represents an amino acid residue (except for the residue of .alpha.-hydroxyglycine) formed by removing one hydrogen atom and hydroxyl group from respectively the .alpha.- or .omega.-amino group and the .alpha.-carboxyl group of an .alpha.- or .omega.-amino acid, said amino acid residue forming acid amide linkages with the adjacent carbonyl group and amino group, and m is an integer of 4 to 6.
摘要翻译：本发明涉及一种新颖的精毒素相关化合物及其生产方法。具有高抗肿瘤活性的新化合物由通式（I）表示，其中R1表示氢原子，羟基或具有1-10个碳原子的脂族酰氧基，R2表示氨基酸通过从α或ω-氨基和α-或ω-氨基酸的α-羧基分别除去一个氢原子和羟基而形成的残基（除了α-羟基甘氨酸的残基除外），所述氨基酸残基与相邻的羰基和氨基形成酰胺键，m是4至6的整数。

3. 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。

4. 发明授权

US4472304A (Amido)N-substituted bleomycins, salts thereof and process for preparation thereof 失效
标题翻译：（酰氨基）N-取代的白霉素，其盐及其制备方法
公开(公告)号：US4472304A
公开(公告)日：1984-09-18
申请号：US451437
申请日：1982-12-20
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P35/00 , C07H17/00 , C07K9/00 , C07C103/52
CPC分类号： C07K9/003 , Y10S930/19
摘要： A promising carcinostatic (amido)N-substituted bleomycin represented by the following formula, or a salt thereof and a process for the preparation thereof: ##STR1## wherein BM represents a moiety of bleomycin skeleton; X represents an alkyl of 1 to 18 carbon atoms, an aminoalkyl of 1 to 12 carbon atoms, a lower alkyl having a halogen, phenyl indolyl, 5- or 6-membered heterocyclic group, or (lower)alkylamino (the alkyl group may have a substituent group) as a substituent, naphthyl, thiazolyl, or N-phenyl(lower)alkylpiperazinyl; and R represents a terminal amino residue of the bleomycin.
摘要翻译：由下式表示的有希望的制癌（酰氨基）N-取代的博来霉素或其盐及其制备方法：其中BM表示博来霉素骨架的部分; X表示1〜18个碳原子的烷基，1〜12个碳原子的氨基烷基，具有卤素的低级烷基，苯基吲哚基，5元或6元杂环基或（低级）烷基氨基（该烷基可以具有取代基），萘基，噻唑基或N-苯基（低级）烷基哌嗪基; R代表博来霉素的末端氨基残基。

5. 发明授权

US4500452A (Amido)N-substituted bleomycins, salts thereof and process for preparation thereof 失效
标题翻译：（酰氨基）N-取代的白霉素，其盐及其制备方法
公开(公告)号：US4500452A
公开(公告)日：1985-02-19
申请号：US621795
申请日：1984-06-18
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P35/00 , C07H17/00 , C07K9/00 , C07C103/52
CPC分类号： C07K9/003 , Y10S930/19
摘要： A promising carcinostatic (amido)N-substituted bleomycin represented by the following formula, or a salt thereof and a process for the preparation thereof: ##STR1## wherein BM represents a moiety of bleomycin skeleton; X represents an alkyl of 1 to 18 carbon atoms, an aminoalkyl of 1 to 12 carbon atoms, a lower alkyl having a halogen, phenyl indolyl, 5- or 6-membered heterocyclic group, or (lower)alkylamino (the alkyl group may have a substituent group) as a substituent, naphthyl, thiazolyl, or N-phenyl(lower)alkylpiperazinyl; and R represents a terminal amino residue of the bleomycin.
摘要翻译：由下式表示的有希望的制癌（酰氨基）N-取代的博来霉素或其盐及其制备方法：其中BM表示博来霉素骨架的部分; X表示1〜18个碳原子的烷基，1〜12个碳原子的氨基烷基，具有卤素的低级烷基，苯基吲哚基，5或6元杂环基或（低级）烷基氨基（烷基可以具有取代基），萘基，噻唑基或N-苯基（低级）烷基哌嗪基; R代表博来霉素的末端氨基残基。

6. 发明授权

US4808703A Novel 3-(4'-aminobutylamino) propylaminobleomycin derivatives 失效
标题翻译：新型3-（4'-氨基丁基氨基）丙基氨基倍半霉素衍生物
公开(公告)号：US4808703A
公开(公告)日：1989-02-28
申请号：US622884
申请日：1984-06-21
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P31/04 , A61P35/00 , C07K9/00 , C07C103/52
CPC分类号： C07K9/003
摘要： Disclosed is a 3-(4'-aminobutylamino) propylaminobleomycin having low pulmonary toxicity, which expressed by the following general formula[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.4 --Bwherein [BX] represents a residue remaining after removing a hydroxyl group from the carboxyl group of bleomycinic acid, A represents a group of the formula ##STR1## in which R.sub.1 represents (i) a hydrogen atom, (ii) an alkyl group having 1 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group having 5 to 13 carbon atoms, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, and benzyloxy group; and R.sub.2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group, B represents a group of the formula ##STR2## in which R.sub.3 and R.sub.4 each represents (i) a hydrogen atom, (ii) an alkyl group having 5 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms and a benzyloxy group, with the proviso that at least one of R.sub.3 and R.sub.4 is a group other than a hydrogen atom, and salt thereof.
摘要翻译：公开了具有低肺毒性的3-（4'-氨基丁基氨基）丙基氨基巴豆霉素，其由以下通式[BX] -NH-（CH 2）3 -A-（CH 2）4 -B表示，其中[BX]表示残基在从博来霉素酸的羧基中除去羟基后残留，A代表式为“IMAGE”的基团，其中R1表示（i）氢原子，（ii）具有1-10个碳原子的烷基或（ iii）可以被苯基和具有5至13个碳原子的环烷基中的至少一个取代的甲基，所述取代基各自任选地被一个或多个选自下列的取代基中的一个或多个取代基取代：卤素原子，碳原子数1〜4的低级烷基，碳原子数1〜4的低级烷氧基和苄氧基; 并且R 2表示具有1至4个碳原子的低级烷基或苄基，B表示下式的基团：其中R 3和R 4各自表示（i）氢原子，（ii）具有5个至少10个碳原子，或（iii）可以被苯基和环烷基中的至少一个取代的甲基，所述取代基各自任选地被一个或多个取代基取代，所述取代基选自：卤素原子，碳原子数1〜4的低级烷基，碳原子数1〜4的低级烷氧基和苄氧基，条件是R3和R4中的至少一个为氢原子以外的基团，及其盐。

7. 发明授权

US4568490A Aminopropylaminobleomycin derivatives and process for preparation thereof 失效
标题翻译：氨丙基氨基甜菜碱素衍生物及其制备方法
公开(公告)号：US4568490A
公开(公告)日：1986-02-04
申请号：US743738
申请日：1985-06-12
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P35/00 , C07K9/00
CPC分类号： C07K9/003 , Y10S930/19 , Y10S930/27
摘要： An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--)CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,(b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,(c) lower alkyl substituted by cycloalkyl or anthranyl,(d) phenylethyl substituted by one or more halogen atoms, or(e) diphenylethyl; or(ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more(a) benzyloxy groups,(b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or(c) cycloalkylmethoxy groups;and a process for the preparation thereof.
摘要翻译：由下式表示的氨基丙基氨基伯合珠霉素或其盐，其在副作用如肺毒性中最小化：[BX] -NH-（CH2）3-A-）CH2）3-B其中[BX]表示酰基通过从所述酸的羧基除去羟基，其公式不同于博来霉素酸的博来霉素酸; A表示通式为其中R 1为低级烷基或苄基的基团，R 2为低级烷基或苄基，R为低级亚烷基，n为0或1; 并且B代表下式的基团：其中（i）R3是氢，R4是（a）被一个或多个卤素原子取代的苄基，条件是当R 1是低级烷基时，苄基被两个卤原子取代，（（c）由氰基，两个或多个烷氧基或两个或更多个苄氧基取代的苄基，（c）被环烷基或蒽基取代的低级烷基，（d）被一个或多个卤素原子取代的苯基乙基，或（e）二苯基乙基; 或（ii）R 3和R 4均为可被一个或多个（a）苄氧基取代的苄基，（b）环取代的苄氧基，其中环取代基可以是一个或多个卤素原子，低级烷氧基或苄氧基，或（c）环烷基甲氧基; 及其制备方法。

8. 发明授权

US4537880A Aminopropylaminobleomycin derivatives and process for preparation thereof 失效
标题翻译：氨丙基氨基甜菜碱素衍生物及其制备方法
公开(公告)号：US4537880A
公开(公告)日：1985-08-27
申请号：US635096
申请日：1984-07-27
申请人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
发明人： Hamao Umezawa , Akio Fujii , Yasuhiko Muraoka , Tokuji Nakatani , Takeyo Fukuoka , Katsutoshi Takahashi
IPC分类号： C07H15/26 , A61K31/70 , A61K31/7028 , A61P35/00 , C07K9/00 , A61K37/00 , C07C103/52
CPC分类号： C07K9/003 , Y10S930/19 , Y10S930/27
摘要： An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,(b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,(c) lower alkyl substituted by cycloalkyl or anthranyl,(d) phenylethyl substituted by one or more halogen atoms, or(e) diphenylethyl; or(ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more(a) benzyloxy groups,(b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or(c) cycloalkylmethoxy groups;and a process for the preparation thereof.
摘要翻译：由下式表示的氨丙基氨基伯基霉素或其盐，其在副作用如肺毒性方面最小化：[BX] -NH-（CH2）3-A-（CH2）3-B其中[BX]表示酰基通过从所述酸的羧基除去羟基，其公式不同于博来霉素酸的博来霉素酸; A表示通式为其中R 1为低级烷基或苄基的基团，R 2为低级烷基或苄基，R为低级亚烷基，n为0或1; 并且B代表下式的基团：其中（i）R3是氢，R4是（a）被一个或多个卤素原子取代的苄基，条件是当R 1是低级烷基时，苄基被两个卤原子取代，（（c）由氰基，两个或更多个烷氧基或两个或更多个苄氧基取代的苄基，（c）被环烷基或蒽基取代的低级烷基，（d）被一个或多个卤素原子取代的苯基乙基，或（e）二苯基乙基; 或（ii）R 3和R 4均为可被一个或多个（a）苄氧基取代的苄基，（b）环取代的苄氧基，其中环取代基可以是一个或多个卤素原子，低级烷氧基或苄氧基，或（c）环烷基甲氧基; 及其制备方法。

9. 发明申请

US20070035722A1 System for measuring the wavelength dispersion and nonlinear coefficient of an optical fiber 有权
标题翻译：用于测量光纤的波长色散和非线性系数的系统
公开(公告)号：US20070035722A1
公开(公告)日：2007-02-15
申请号：US11580473
申请日：2006-10-13
申请人： Masateru Tadakuma , Yu Mimura , Misao Sakano , Osamu Aso , Takeshi Nakajima , Katsutoshi Takahashi
发明人： Masateru Tadakuma , Yu Mimura , Misao Sakano , Osamu Aso , Takeshi Nakajima , Katsutoshi Takahashi
IPC分类号： G01N21/00
CPC分类号： G01M11/3172 , G01M11/31 , G01M11/3181 , G01M11/319 , G01M11/39
摘要： A method of simultaneously specifying the wavelength dispersion and nonlinear coefficient of an optical fiber. Pulsed probe light and pulsed pump light are first caused to enter an optical fiber to be measured. Then, the power oscillation of the back-scattered light of the probe light or idler light generated within the optical fiber is measured. Next, the instantaneous frequency of the measured power oscillation is obtained, and the dependency of the instantaneous frequency relative to the power oscillation of the pump light in a longitudinal direction of the optical fiber is obtained. Thereafter, a rate of change in the longitudinal direction between phase-mismatching conditions and nonlinear coefficient of the optical fiber is obtained from the dependency of the instantaneous frequency. And based on the rate of change, the longitudinal wavelength-dispersion distribution and longitudinal nonlinear-coefficient distribution of the optical fiber are simultaneously specified.
摘要翻译：一种同时指定光纤的波长色散和非线性系数的方法。首先引入脉冲探头光和脉冲泵浦光，进入要测量的光纤。然后，测量在光纤内产生的探测光或空载光的背散射光的功率振荡。接下来，获得测量的功率振荡的瞬时频率，并且获得瞬时频率相对于光纤在纵向方向上的功率振荡的依赖性。此后，根据瞬时频率的依赖性，获得相位不匹配条件和光纤的非线性系数之间的纵向变化率。并且基于变化率，同时规定了光纤的纵向波长色散分布和纵向非线性系数分布。

10. 发明授权

US5214048A Oxetanocins 失效
标题翻译：氧自由基
公开(公告)号：US5214048A
公开(公告)日：1993-05-25
申请号：US439270
申请日：1989-11-20
申请人： Nobuyoshi Shimada , Shigeru Hasegawa , Takayuki Tomizawa , Seiichi Saito , Kyoichi Shibuya , Akio Fujii , Hiroo Hoshino , Kenichi Matsubara , Takemitsu Nagahata , Katsutoshi Takahashi , Yukihiro Nishiyama
发明人： Nobuyoshi Shimada , Shigeru Hasegawa , Takayuki Tomizawa , Seiichi Saito , Kyoichi Shibuya , Akio Fujii , Hiroo Hoshino , Kenichi Matsubara , Takemitsu Nagahata , Katsutoshi Takahashi , Yukihiro Nishiyama
IPC分类号： C07D473/00 , C07D501/00 , C07H19/02
CPC分类号： C07D473/00 , C07D501/00 , C07H19/02
摘要： This invention relates to novel oxetanocins represented by the following general formula (I): ##STR1## wherein R represents a group represented by ##STR2## and their pharmacologically acceptable salts which have antiviral activities.
摘要翻译：本发明涉及由以下通式（I）表示的新型氧杂环丁酮：其中R表示由IMAGE＆lt; IMAGE＆gt;表示的基团及其具有抗病毒活性的药理学上可接受的盐。

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