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1. 发明授权

US4390702A 3-Substituted-3-fluoropyruvic acids and their esters and salts, and production thereof 失效
标题翻译： 3-取代的3-氟异丙酸及其酯和盐及其制备
公开(公告)号：US4390702A
公开(公告)日：1983-06-28
申请号：US220917
申请日：1980-12-29
申请人： Susumu Misaki , Masahiro Suefuji , Tadahiko Tsushima , Hiroshi Tanida
发明人： Susumu Misaki , Masahiro Suefuji , Tadahiko Tsushima , Hiroshi Tanida
IPC分类号： C07C69/716 , C07C51/00 , C07C51/363 , C07C59/21 , C07C59/84 , C07C59/88 , C07C67/00 , C07C67/307 , C07C69/738 , C07C201/00 , C07C205/55 , C07C205/56 , C07D213/26 , C07D213/55 , C07C53/21 , C07C69/76
CPC分类号： C07C59/21 , C07C201/12 , C07C205/56 , C07C51/09 , C07C59/88 , C07C67/307 , C07D213/26
摘要： A 3-substituted-3-fluoropyruvic acid and its ester and salt of the formula: ##STR1## wherein R is a lower alkyl group, a lower alkanoyl group, a fluorinated lower alkanoyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted pyridyl group and R' is a hydrogen atom, an ester-forming residue or a salt-forming residue, and their production.
摘要翻译： 3-取代-3-氟代丙酸及其下式的酯和盐：其中R是低级烷基，低级烷酰基，氟化低级烷酰基，取代或未取代的苯基或取代或未取代的吡啶基，R'是氢原子，成酯残基或成盐残基，以及它们的制备。

2. 发明授权

US4216231A 9,10-Dihydro-9,10-methanoanthracene N-oxide derivatives 失效
标题翻译： 9,10-二氢-9,10-亚甲基蒽N-氧化物衍生物
公开(公告)号：US4216231A
公开(公告)日：1980-08-05
申请号：US7711
申请日：1979-01-30
申请人： Hiroshi Tanida , Tadashi Irie
发明人： Hiroshi Tanida , Tadashi Irie
IPC分类号： A61K31/13 , A61K31/135 , A61K31/435 , A61K31/495 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C291/04 , C07D211/94 , C07D241/52 , C07D295/02 , C07D295/03 , C07D295/088 , C07D295/24 , A01N9/20 , A01N9/24
CPC分类号： C07D295/03 , C07D295/088 , C07D295/24
摘要： 9,10-Dihydro-9,10-methanoanthracene N-oxide derivatives represented by the formula: ##STR1## wherein A represents a straight or branched C.sub.1 -C.sub.6 alkylene; R.sup.1 and R.sup.2 each represents C.sub.1 -C.sub.4 alkyl or phenyl-C.sub.1 -C.sub.4 alkyl, or ##STR2## represents the group ##STR3## and X represents methylene, hydroxymethylene, C.sub.1 -C.sub.4 alkyl ##STR4## or hydroxy-C.sub.1 -C.sub.4 alkyl ##STR5## and their pharmaceutically acceptable acid addition salts which are useful as anti-depressants, tranquilizers, or anti-epileptics.
摘要翻译： 9,10-二氢-9,10-亚甲基蒽N-氧化物衍生物，由下式表示：其中A表示直链或支链C1-C6亚烷基; R1和R2各自表示C1-C4烷基或苯基-C1-C4烷基，或表示基团，X表示亚甲基，羟基亚甲基，C 1 -C 4烷基或羟基-C 1 -C 4烷基

3. 外观设计

USD260846S Plasma cutting-welding torch head 失效
公开(公告)号：USD260846S
公开(公告)日：1981-09-22
申请号：US9534
申请日：1979-02-05
申请人： John E. Summers , Hiroshi Tanida
设计人： John E. Summers , Hiroshi Tanida

4. 发明授权

US4160085A Cyclization to form cephem ring and intermediates therefor 失效
标题翻译：环化形成头孢烯环及其中间体
公开(公告)号：US4160085A
公开(公告)日：1979-07-03
申请号：US856806
申请日：1977-12-01
申请人： Teruji Tsuji , Yoshio Hamashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
发明人： Teruji Tsuji , Yoshio Hamashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
IPC分类号： C07D205/095 , C07D501/08 , C07D501/10 , C07D501/20 , C07D501/59 , C07D501/02
CPC分类号： C07D205/095 , Y02P20/55
摘要： Intermediates represented by the following formulas are useful for synthesizing 3-hydroxy-3-cephem compounds ##STR1## wherein A and B each is a hydrogen or amino substituent; R is a hydrogen or thiol substituent; Hal is a halogen; X is a hydroxy or carboxy protecting group; the broken line between A and R shows that when R and B are hydrogens, and A is a carboxylic acyl, the substituents can be combined to form an azetidinothiazoline bicyclic ring; and the enamine derivatives thereof. One embodiment provides for cyclizing a compound of the formula: ##STR2## wherein A, B, X and Hal are as defined above, which comprises treating the said compound with an acid, base, or solvent if required in the presence of a catalyzer to give a compound represented by following formula ##STR3## In a further embodiment a compound represented by the following formula ##STR4## wherein A, B, R and X are as defined above, is prepared by a process which comprises treating an enamine of a compound represented by following formula ##STR5## wherein A, B, R, X, Hal and broken line are as defined above, with a disubstituted amino containing from 2 to 20 carbon atoms, with the action of an aqueous acid.
摘要翻译：由下式表示的中间体可用于合成3-羟基-3-头孢烯化合物，其中A和B各自为氢或氨基取代基; R是氢或硫醇取代基; 卤素是卤素; X是羟基或羧基保护基; A和R之间的虚线表示当R和B为氢时，A为羧酰基时，可以将取代基结合形成氮杂环丁烷异噻唑啉双环; 及其烯胺衍生物。一个实施方案提供使下式化合物环化：其中A，B，X和Hal如上定义，其包括如果需要，在催化剂存在下用酸，碱或溶剂处理所述化合物，得到由下式表示的化合物。在另一个实施方案中，由以下通式表示的化合物其中A，B，R和X如上定义的化合物通过包括处理烯胺其中A，B，R，X，Hal和虚线如上所定义，与含有2-20个碳原子的二取代的氨基酸反应。

5. 发明授权

US3989685A Process for making a 2'-halopenicillin 失效
标题翻译：制备2 {40-青霉素的方法
公开(公告)号：US3989685A
公开(公告)日：1976-11-02
申请号：US372016
申请日：1973-06-21
申请人： Hiroshi Tanida , Teruji Tsuji
发明人： Hiroshi Tanida , Teruji Tsuji
IPC分类号： C07D499/00 , C07D499/04 , C07D499/21 , C07D501/04 , C07D501/10 , C07D501/14 , C07D501/16
CPC分类号： C07D499/00
摘要： A 2'-halopenicillin compound is prepared from a penicillin-1-oxide compound by the action of an acid halide in the presence of a base. The product on heating rearranges to a 3-halo-3-methylcepham compound which itself gives a 3-methyl-3-cephem compound on further heating. A 2'-halopenicillin compound gives a 3-methyl-3-cephem compound on heating. The 2'-halopenicillin compounds, 3-halo-3-methylcepham compound and 3-methyl-3-cephem compounds are antibacterials which are also useful as intermediates for the synthesis of other penicillins and cephalosporins.
摘要翻译：在碱存在下，通过酰基卤的作用由青霉素-1-氧化物化合物制备2'-卤青霉素化合物。加热产物重新排列为3-卤-3-甲基头孢烯化合物，其本身在进一步加热时得到3-甲基-3-头孢烯化合物。 2'-卤青霉素化合物在加热时得到3-甲基-3-头孢烯化合物。 2'-卤青霉素化合物，3-卤代-3-甲基头孢烯化合物和3-甲基-3-头孢烯化合物是还可用作合成其它青霉素和头孢菌素的中间体的抗菌剂。

6. 发明授权

US4153629A 9,10-Dihydro-9,10-methanoanthracene N-oxide 失效
标题翻译： 9,10-二氢-9,10-亚甲基蒽N-氧化物
公开(公告)号：US4153629A
公开(公告)日：1979-05-08
申请号：US750630
申请日：1976-12-15
申请人： Hiroshi Tanida , Tadashi Irie
发明人： Hiroshi Tanida , Tadashi Irie
IPC分类号： A61K31/13 , A61K31/135 , A61K31/435 , A61K31/495 , A61P25/08 , A61P25/20 , A61P25/24 , A61P25/26 , C07C291/04 , C07D211/94 , C07D241/52 , C07D295/02 , C07D295/03 , C07D295/088 , C07D295/24 , C07C87/28
CPC分类号： C07D295/03 , C07D295/088 , C07D295/24
摘要： 9,10-Dihydro-9,10-methanoanthracene N-oxide derivatives represented by the formula: ##STR1## wherein A represents a straight or branched C.sub.1 -C.sub.6 alkylene; R.sup.1 and R.sup.2 each represents C.sub.1 -C.sub.4 alkyl or phenyl-C.sub.1 -C.sub.4 alkyl, or ##STR2## represents the group ##STR3## and X represents methylene, hydroxymethylene, C.sub.1 -C.sub.4 ##STR4## or hydroxy-C.sub.1 -C.sub.4 ##STR5## and their pharmaceutically acceptable acid addition salts which are useful as anti-depressants, tranquilizers, or anti-epileptics.
摘要翻译： 9,10-二氢-9,10-亚甲基蒽N-氧化物衍生物，由下式表示：其中A表示直链或支链C1-C6亚烷基; R 1和R 2各自表示C 1 -C 4烷基或苯基-C 1 -C 4烷基，或者表示基团，X表示亚甲基，羟基亚甲基，C 1 -C 4或羟基-C 1 -C 4 其药学上可接受的酸加成盐，其可用作抗抑郁剂，止痛剂或抗癫痫药。

7. 发明授权

US4066641A Method for cyclization to give cephem ring 失效
标题翻译：循环给CEPHEM环的方法
公开(公告)号：US4066641A
公开(公告)日：1978-01-03
申请号：US707288
申请日：1976-07-21
申请人： Yoshio Hamashima , Mitsuru Yoshioka , Hiroshi Tanida , Teruji Tsuji , Masayuki Narisada , Taichiro Komeno , Wataru Nagata
发明人： Yoshio Hamashima , Mitsuru Yoshioka , Hiroshi Tanida , Teruji Tsuji , Masayuki Narisada , Taichiro Komeno , Wataru Nagata
IPC分类号： C07D205/095 , C07D501/08 , C07D501/10 , C07D501/59 , C07D501/60 , C07D501/02
CPC分类号： C07D501/10 , C07D205/095
摘要： A compound represented by ##STR1## is treated with a base to give an antibacterial cephem compound represented by ##STR2## (wherein A is amino or substituted amino;Cob is carboxy or protected carboxy;Rs is substituted thio;Y is an electron-attracting group selected from acyloxy, halogen, cyano, nitro, and nitroso; andThe dotted line shows .DELTA..sup.2 or .DELTA..sup.3).

8. 发明授权

US4440683A Cyclization to form cephem ring and azetidinone intermediates therefor 失效
标题翻译：环化形成头孢烯环和氮杂环丁酮的中间体
公开(公告)号：US4440683A
公开(公告)日：1984-04-03
申请号：US338651
申请日：1982-01-11
申请人： Teruji Tsuji , Yoshio Hahashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
发明人： Teruji Tsuji , Yoshio Hahashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
IPC分类号： C07D205/095 , C07D501/08 , C07D501/10 , C07D501/20 , C07D501/59 , C07D205/08 , C07D401/12 , C07D403/04 , C07D405/12
CPC分类号： C07D205/095 , Y02P20/55
摘要： An intermediate represented by following formula for synthesizing 3-hydroxy-3-cephem compounds. ##STR1## wherein A and B each is a hydrogen or amine substituent; R is a hydrogen or thiol substituent; Nal is a halogen; X is a hydroxy or carboxy protecting group; the broken line between A and R shows that when R and B are hydrogens, and A is a carboxylic acyl, the substituents can be combined to form an azetidimethiazoline bicyclic ring; and the enamine derivatives thereof.
摘要翻译：由3-羟基-3-头孢烯化合物合成的下式表示的中间体。其中A和B各自为氢或胺取代基; R是氢或硫醇取代基; 纳尔是卤素; X是羟基或羧基保护基; A和R之间的虚线表明当R和B为氢时，A为羧酰基时，可以将取代基结合形成氮杂环丁二烯环二环; 及其烯胺衍生物。

9. 发明授权

US4346218A Cyclization process to form cephem ring 失效
标题翻译：环化过程形成头孢烯环
公开(公告)号：US4346218A
公开(公告)日：1982-08-24
申请号：US125233
申请日：1980-02-27
申请人： Teruji Tsuji , Yoshio Hamashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
发明人： Teruji Tsuji , Yoshio Hamashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
IPC分类号： C07D205/095 , C07D501/08 , C07D501/10 , C07D501/20 , C07D501/59
CPC分类号： C07D205/095 , Y02P20/55
摘要： An intermediate represented by following formula for synthesizing 3-hydroxy-3-cephem compounds ##STR1## wherein A and B each is a hydrogen or amino substituent; R is a hydrogen or thiol substituent; Hal is a halogen; X is a hydroxy or carboxy protecting group; the broken line between A and R shows that when R and B are hydrogens, and A is a carboxylic acyl, the substituents can be combined to form an azetidinothiazoline bicyclic ring; and the enamine derivatives thereof.
摘要翻译：用于合成3-羟基-3-头孢烯化合物的下式表示的中间体，其中A和B各自为氢或氨基取代基; R是氢或硫醇取代基; 卤素是卤素; X是羟基或羧基保护基; A和R之间的虚线表明当R和B为氢时，A为羧酰基时，可以将取代基结合形成氮杂环丁烷异噻唑啉双环; 及其烯胺衍生物。

10. 发明授权

US4332722A Cyclization to form cephem ring and intermediates therefor 失效
标题翻译：环化形成头孢烯环及其中间体
公开(公告)号：US4332722A
公开(公告)日：1982-06-01
申请号：US125232
申请日：1980-02-27
申请人： Teruji Tsuji , Yoshio Hamashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
发明人： Teruji Tsuji , Yoshio Hamashima , Mitsuru Yoshioka , Masayuki Narisada , Hiroshi Tanida , Taichiro Komeno , Wataru Nagata
IPC分类号： C07D205/095 , C07D501/08 , C07D487/04
CPC分类号： C07D205/095 , Y02P20/55
摘要： An intermediate represented by the following formula, for synthesizing --3-hydroxy-3-cephem compounds. ##STR1## wherein A and B each is a hydrogen or amino substituent; R is a hydrogen or thiol substituent; Hal is a halogen; X is a hydroxy or carboxy protecting group; the broken line between A and R shows that when R and B are hydrogens, and A is a carboxylic acyl, the substituents can be combined to form an azetidinothiazoline bicyclic ring; and the enamine derivatives thereof.
摘要翻译：用于合成3-羟基-3-头孢烯化合物的由下式表示的中间体。其中A和B各自为氢或氨基取代基; R是氢或硫醇取代基; 卤素是卤素; X是羟基或羧基保护基; A和R之间的虚线表明当R和B为氢时，A为羧酰基时，可以将取代基结合形成氮杂环丁烷异噻唑啉双环; 及其烯胺衍生物。

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