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1. 发明授权

US4240975A Bestatin 失效
公开(公告)号：US4240975A
公开(公告)日：1980-12-23
申请号：US79777
申请日：1979-09-26
申请人： Hamao Umezawa , Takaaki Aoyagi , Tomohisa Takita , Rinzo Nishizawa , Tetsushi Saino
发明人： Hamao Umezawa , Takaaki Aoyagi , Tomohisa Takita , Rinzo Nishizawa , Tetsushi Saino
IPC分类号： C07K5/02 , C07C69/96 , C07C101/72
CPC分类号： C07K5/02
摘要： Bestatin, which is [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, and related compounds which inhibit aminopeptidase B, leucino aminopeptidase and Bleomycin hydrolase, enhance the anti-tumor effect of Bleomycin and exhibit an antifertility effect were synthesized and tested.

2. 发明授权

US4189604A Bestatin 失效
标题翻译：百乐达
公开(公告)号：US4189604A
公开(公告)日：1980-02-19
申请号：US809835
申请日：1977-06-24
申请人： Hamao Umezawa , Takaaki Aoyagi , Tomohisa Takita , Rinzo Nishizawa , Tetsushi Saino
发明人： Hamao Umezawa , Takaaki Aoyagi , Tomohisa Takita , Rinzo Nishizawa , Tetsushi Saino
IPC分类号： C07K5/02 , C07C79/46 , A01N9/20
CPC分类号： C07K5/02
摘要： Bestatin, which is [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, and related compounds which inhibit aminopeptidase B, leucino aminopeptidase and Bleomycin hydrolase, enhance the anti-tumor effect of Bleomycin and exhibit an antifertility effect were synthesized and tested.
摘要翻译：本品为[（2S，3R）-3-氨基-2-羟基-4-苯基丁酰] -L-亮氨酸，抑制氨肽酶B，亮氨酸氨基肽酶和博来霉素水解酶的相关化合物，可增强博来霉素的抗肿瘤效果并展示出抗菌效果。

3. 发明授权

US4281180A Process for producing threo-3-amino-2-hydroxybutanoyl-aminoacetic acids, as well as novel intermediated therefor and process for producing them 失效
公开(公告)号：US4281180A
公开(公告)日：1981-07-28
申请号：US96693
申请日：1979-11-23
申请人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
发明人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
IPC分类号： A47L13/40 , A61K20060101 , A61K31/16 , A61K31/195 , C07C20060101 , C07C51/347 , C07C233/31 , C07C233/47 , C07C233/76 , C07C233/87 , C07C271/22 , C07C271/34 , C07C271/54 , C07D209/48 , C07K1/06 , C07K5/02 , C07K5/06
CPC分类号： C07C237/20 , A61K38/00 , Y02P20/55
摘要： A process for producing threo-3-amino-2-hydroxybutanoylaminoacetic acids comprises the steps of allowing to react a starting compound represented by the general formula: ##STR1## wherein R.sub.1 represents a naphthyl or a group of the formula: ##STR2## in which R.sub.6 and R.sub.7 represent individually hydrogen, halogen, amino or a protected amino, hydroxy or a protected hydroxy, a lower alkoxy or a lower alkyl and R.sub.2 represents a protected amino, with a starting compound represented by the general formula: ##STR3## wherein R.sub.3 represents hydrogen or an ester residue, to obtain threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its ester represented by the general formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and then reducing the same into threo-3-protected amino-2-hydroxybutanoic acid or its ester represented by the general formula: ##STR5## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and further converting the above compound into 3-amino-2-hydroxybutanoic acid represented by the general formula: ##STR6## wherein R.sub.2 ' represents amino or a protected amino, thereafter condensing the same, in a conventional manner for forming a peptide coupling, with a compound represented by the general formula: ##STR7## wherein R.sub.4 represents an alkyl having 3-4 carbon atom or 3-guanidinopropyl, while previously protecting as required those groups not relevant to the reaction, and removing the protecting groups for the functional groups to produce threo-3-amino-2-hydroxybutanoylaminoacetic acids represented by the general formula: ##STR8## wherein R.sub.1 and R.sub.4 have the same meanings as above. This invention also provides the compounds represented by the general formula (III) as novel intermediates for the above aimed compounds and a process for producing the intermediates.

4. 发明授权

US4453003A Process for producing threo-3-amino-2-hydroxy-butanoyl-aminoacetic acids as well as novel intermediates therefor and process for producing them 失效
公开(公告)号：US4453003A
公开(公告)日：1984-06-05
申请号：US336492
申请日：1981-12-31
申请人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
发明人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
IPC分类号： A47L13/40 , A61K20060101 , A61K31/16 , A61K31/195 , C07C20060101 , C07C51/347 , C07C233/31 , C07C233/47 , C07C233/76 , C07C233/87 , C07C271/22 , C07C271/34 , C07C271/54 , C07D209/48 , C07K1/06 , C07K5/02 , C07K5/06 , C07C101/30
CPC分类号： C07C237/20 , A61K38/00 , Y02P20/55
摘要： A process for producing threo-3-amino-2-hydroxybutanoylaminoacetic acids comprises the steps of allowing to react a starting compound represented by the general formula: ##STR1## wherein R.sub.1 represents a naphthyl or a group of the formula: ##STR2## in which R.sub.6 and R.sub.7 represent individually hydrogen, halogen, amino or a protected amino, hydroxy or a protected hydroxy, a lower alkoxy or a lower alkyl and R.sub.2 represents a protected amino, with a starting compound represented by the general formula: ##STR3## wherein R.sub.3 represents hydrogen or an ester residue, to obtain threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its ester represented by the general formula: ##STR4## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and then reducing the same into threo-3-protected amino-2-hydroxybutanoic acid or its ester represented by the general formula: ##STR5## wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as above, and further converting the above compound into 3-amino-2-hydroxybutanoic acid represented by the general formula: ##STR6## wherein R.sub.2 ' represents amino or a protected amino, thereafter condensing the same, in a conventional manner for forming a peptide coupling, with a compound represented by the general formula: ##STR7## wherein R.sub.4 represents an alkyl having 3-4 carbon atom or 3-guanidinopropyl, while previously protecting as required those groups not relevant to the reaction, and removing the protecting groups for the functional groups to produce threo-3-amino-2-hydroxybutanoylaminoacetic acids represented by the general formula: ##STR8## wherein R.sub.1 and R.sub.4 have the same meanings as above. This invention also provides the compounds represented by the general formula (III) as novel intermediates for the above aimed compounds and a process for producing the intermediates.

5. 发明授权

US4391986A Process for producing threo-3-amino-2-hydroxybutanoyl-aminoacetic acids, as well as novel intermediates therefor and process for producing them 失效
标题翻译：产生苏氨酸-3-氨基-2-羟基丁酰氨基乙酸的方法以及其新型中间体及其制备方法
公开(公告)号：US4391986A
公开(公告)日：1983-07-05
申请号：US211035
申请日：1980-11-28
申请人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
发明人： Hamao Umezawa , Takaaki Aoyagi , Tadashi Shirai , Rinzo Nishizawa , Masao Suzuki , Tetsushi Saino
IPC分类号： A47L13/40 , A61K20060101 , A61K31/16 , A61K31/195 , C07C20060101 , C07C51/347 , C07C233/31 , C07C233/47 , C07C233/76 , C07C233/87 , C07C271/22 , C07C271/34 , C07C271/54 , C07D209/48 , C07K1/06 , C07K5/02 , C07K5/06 , C07C101/34
CPC分类号： C07C237/20 , A61K38/00 , Y02P20/55
摘要： Threo-3-protected amino-2-hydroxy-4-oxobutanoic acid or its esters represented by the formula: ##STR1## wherein R.sub.1 represents naphthyl or a group of the formula ##STR2## in which R.sub.6 and R.sub.7 represent individually hydrogen, halogen, amino, an amino protected with acyl, lower alkyloxycarbonyl or carbamoyl, hydroxy or protected with acyl, lower alkyloxycarbonyl or carbamoyl, lower alkoxy, lower alkyl or phenyl group; R.sub.2 represents an amine protected with acyl, lower alkyloxycarbonyl or carbamoyl; and R.sub.3 represents hydrogen, lower alkyl having 1 to 6 carbon atoms or benzyl.
摘要翻译： Threo-3保护的氨基-2-羟基-4-氧代丁酸或其由下式表示的酯：其中R 1表示萘基或式（VI）的基团，其中R 6和R 7分别表示氢，卤素，氨基，被酰基保护的氨基，低级烷氧基羰基或氨基甲酰基，羟基或用酰基保护，低级烷氧基羰基或氨基甲酰基，低级烷氧基，低级烷基或苯基; R2代表被酰基，低级烷氧基羰基或氨基甲酰基保护的胺; 并且R 3表示氢，具有1至6个碳原子的低级烷基或苄基。

6. 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。

7. 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。

8. 发明授权

US4224239A Process for preparing optically active amino acid or mandelic acid 失效
标题翻译：光学活性氨基酸或扁桃酸的制备方法
公开(公告)号：US4224239A
公开(公告)日：1980-09-23
申请号：US33021
申请日：1979-04-24
申请人： Yasuhisa Tashiro , Takashi Nagashima , Shigeru Aoki , Rinzo Nishizawa
发明人： Yasuhisa Tashiro , Takashi Nagashima , Shigeru Aoki , Rinzo Nishizawa
IPC分类号： C07B57/00 , C07B31/00 , C07C59/50 , C07C67/00 , C07C227/00 , C07C227/18 , C07C227/34 , C07C229/08 , C07C313/00 , C07C323/58 , C07C101/04 , C07B19/00 , C07C101/08
CPC分类号： C07C59/50
摘要： Two optically active amino acid-mandelic acid complexes are obtained by interacting in a solvent under pH conditions of 1.0-4.0 an amino acid expressed by a general formula ##STR1## (in which R represents a methyl group, an ethyl group or a methylthioethyl group) and mandelic acid, one of the acids being an optically active substance and the other being a racemic modification, and optically resolving the resulting complexes into two diastereoisomers by using solubility difference therebetween. The optically active complexes are each decomposed by means of an acid, a strongly acidic ion-exchange resin, or a weakly basis ion-exchange resin to obtain optically active amino acids or optically active mandelic acid.
摘要翻译：通过在1.0-4.0的pH条件下在溶剂中相互作用获得两个光学活性的氨基酸 - 扁桃酸复合物，所述氨基酸由通式“IMAGE”（其中R表示甲基，乙基或甲硫基乙基））和扁桃酸，其中一种酸是光学活性物质，另一种是外消旋体改性，并通过使用它们之间的溶解度差异将所得的络合物光学拆分成两个非对映异构体。光学活性复合物各自通过酸，强酸性离子交换树脂或弱碱离子交换树脂分解，得到光学活性氨基酸或光学活性扁桃酸。

9. 发明授权

US4464532A Intermediates of 7-alkoxycarbonyl-6,8-dimethyl-4-hydroxymethyl-1-phthalazone 失效
标题翻译： 7-烷氧基羰基-6,8-二甲基-4-羟甲基-1-酞嗪酮的中间体
公开(公告)号：US4464532A
公开(公告)日：1984-08-07
申请号：US386001
申请日：1982-06-07
申请人： Yukio Takei , Masao Yoshida , Rinzo Nishizawa
发明人： Yukio Takei , Masao Yoshida , Rinzo Nishizawa
IPC分类号： C07D237/32 , C07D307/88
CPC分类号： C07D307/88 , C07D237/32
摘要： A novel process for producing 7-alkoxycarbonyl-6,8-dimethyl-4-hydroxymethyl-1-phthalazone, and its intermediates. 7-Alkoxycarbonyl-6,8-dimethyl-4-hydroxymethyl-1-phthalazone can be obtained by reacting substituted methylenetriphenylphosphorane with 3,5-dimethyl-4-alkoxycarbonylphthalic anhydride to obtain 6-alkoxycarbonyl-5,7-dimethyl-.DELTA..sup.3,.alpha. -substituted methylenephthalide, reacting the latter with hydrazine to obtain a phthalazone derivative, hydrolyzing the latter, halogenating the hydrolyzate to obtain 7-alkoxycarbonyl-6,8-dimethyl-4-(.alpha.-halogeno-.alpha.-substituted methyl)-1-phthalazone and then directly hydrolyzing and decarboxylating the latter or, when said 7-alkoxycarbonyl-6,8-dimethyl-4-(.alpha.-halogeno-.alpha.-substituted methyl)-1-phthalazone is 7-alkoxycarbonyl-6,8-dimethyl-1-phthalazone-4-.alpha.-halogenoacetic acid, reacting it with a carboxylic acid salt such as sodium acetate and simultaneously decarboxylating the acyloxylated compound and then hydrolyzing the decarboxylated product or firstly decarboxylating the 1-phthalazone-4-.alpha.-halogenoacetic acid derivative, reacting the decarboxylated product with said carboxylic acid salt and then hydrolyzing the reaction product or when said 7-alkoxycarbonyl-6,8-dimethyl-4-(.alpha.-halogeno-.alpha.-substituted methyl)-1-phthalazone is 7-alkoxycarbonyl-4-(.alpha.-carbamoyl-.alpha.-halogenomethyl-6,8-dimethyl-1-phthalazone, reacting it with said carboxylic acid salt and then hydrolyzing and decarboxylating the acyloxylated compound simultaneously.
摘要翻译： 7-烷氧基羰基-6,8-二甲基-4-羟甲基-1-酞嗪酮及其中间体的新方法。 7-烷氧基羰基-6,8-二甲基-4-羟甲基-1-酞嗪酮可以通过使取代的亚甲基三苯基正膦与3,5-二甲基-4-烷氧基羰基邻苯二甲酸酐反应得到6-烷氧基羰基-5,7-二甲基-D-三唑， α-取代的亚甲基对苯二甲酸盐，使后者与肼反应得到酞嗪衍生物，水解后者，卤化水解产物得到7-烷氧基羰基-6,8-二甲基-4-（α-卤素-α-取代的甲基）-1- 然后直接水解和脱羧后者，或当所述7-烷氧基羰基-6,8-二甲基-4-（α-卤素-α-取代的甲基）-1-酞嗪酮为7-烷氧基羰基-6,8-二甲基 - 1-酞嗪-4-α-卤代乙酸，使其与羧酸盐如乙酸钠反应，同时使酰氧基化化合物脱羧，然后水解脱羧产物，或首先使1-酞嗪-4--α-卤代乙酸衍生物脱羧使脱羧产物与所述羧酸盐反应，然后水解反应产物，或当所述7-烷氧基羰基-6,8-二甲基-4-（α-卤代-α-取代的甲基）-1-酞嗪酮为7-烷氧羰基 - 4-（α-氨基甲酰基-α-卤代甲基-6,8-二甲基-1-酞嗪酮）与所述羧酸盐反应，然后同时水解和脱羧酰氧基化化合物。

10. 发明授权

US4198524A Optically active amino acid-mandelic acid complexes 失效
标题翻译：光活性氨基酸 - 扁桃酸复合物
公开(公告)号：US4198524A
公开(公告)日：1980-04-15
申请号：US886745
申请日：1978-03-15
申请人： Yasuhisa Tashiro , Takashi Nagashima , Shigeru Aoki , Rinzo Nishizawa
发明人： Yasuhisa Tashiro , Takashi Nagashima , Shigeru Aoki , Rinzo Nishizawa
IPC分类号： C07B57/00 , C07B31/00 , C07C59/50 , C07C67/00 , C07C227/00 , C07C227/18 , C07C227/34 , C07C229/08 , C07C313/00 , C07C323/58 , C07C65/135
CPC分类号： C07C59/50
摘要： Two optically active amino acid-mandelic acid complexes are obtained by reacting in a solvent under pH conditions of 1.0-4.0, an amino acid expressed by a general formula ##STR1## (in which R represents a methyl group, an ethyl group or a methylthioethyl group) and mandelic acid, one of the acids being an optically active substance and the other being a racemic modification, and optically resolving the resulting complexes into two diastereomers by using a solubility difference therebetween. The optically active complexes are each decomposed by means of an acid, a strongly acidic ion-exchange resin, or a weakly basic ion-exchange resin to obtain optically active amino acids or optically active mandelic acid.
摘要翻译：两种光学活性的氨基酸 - 扁桃酸配合物通过在溶剂中在1.0-4.0的pH条件下反应得到，该通式为通式（IMAGE）表示的氨基酸（其中R表示甲基，乙基或甲基硫代乙基基团）和扁桃酸，其中一种酸是光学活性物质，另一种是外消旋体改性，并通过使用它们之间的溶解度差异将所得复合物光学拆分成两种非对映异构体。光学活性复合物各自通过酸，强酸性离子交换树脂或弱碱性离子交换树脂分解，得到光学活性氨基酸或光学活性扁桃酸。

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