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1. 发明授权

US4857645A Process for introducing a thiocarboxylic ester group at the orthoposition of phenols or phenylamines 失效
标题翻译：在酚或苯胺的定位处引入硫代羧酸酯基团的方法
公开(公告)号：US4857645A
公开(公告)日：1989-08-15
申请号：US116792
申请日：1987-11-05
申请人： Adachi Makoto , Hiromu Matsumura , Tsutomu Sugasawa
发明人： Adachi Makoto , Hiromu Matsumura , Tsutomu Sugasawa
IPC分类号： C07C327/26 , B01J27/08 , C07B45/00 , C07B45/06 , C07B61/00 , C07C67/00 , C07C325/00 , C07C327/20 , C07D207/14 , C07D209/08 , C07D211/58 , C07D215/06 , C07D241/42 , C07D279/16 , C07D279/18
CPC分类号： C07D279/16 , C07B45/00 , C07C327/00 , C07D207/14 , C07D209/08 , C07D211/58 , C07D215/06 , C07D241/42
摘要： A process for introducing thiocarboxylic ester at ortho-position of phenols or phenylamines which comprises reacting a phenyl compound having group or optionally substituted amino or cyclic amino group, of which at least one ortho-position is vacant, with C.sub.1 -C.sub.5 alkyl thiocyanate, C.sub.7 -C.sub.13 aralkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and hydrolyzing the resultant product under acidic conditions is provided, and said process is useful in the synthesis of medicinals, pesticides and dyes.

2. 发明授权

US4774331A Process for ortho-cyanation of phenols or phenylamines 失效
标题翻译：苯酚或苯胺的邻氰氰化处理
公开(公告)号：US4774331A
公开(公告)日：1988-09-27
申请号：US87885
申请日：1987-08-21
申请人： Makoto Adachi , Hiromu Matsumura , Tsutomu Sugasawa
发明人： Makoto Adachi , Hiromu Matsumura , Tsutomu Sugasawa
IPC分类号： C07B31/00 , C07B43/08 , C07C67/00 , C07C253/00 , C07C255/53 , C07C255/54 , C07C255/58 , C07C313/00 , C07C319/20 , C07C323/45 , C07C323/62 , C07D207/09 , C07D207/14 , C07D209/08 , C07D211/56 , C07D211/58 , C07D215/48 , C07D241/38 , C07D241/42 , C07D265/36 , C07D265/38 , C07D279/16 , C07D279/20 , C07D401/04 , C07D403/04 , C07D403/06 , C07C43/08
CPC分类号： C07C255/00 , C07C323/00 , C07D207/09 , C07D207/14 , C07D209/08 , C07D211/56 , C07D211/58 , C07D215/48 , C07D241/42 , C07D279/16 , C07D279/20
摘要： A process for ortho-cyanation of phenols or phenylamines which comprises reacting a phenyl compound having hydroxy or optionally substituted amino or cyclic amino, of which ortho position is vacant, with trichloroacetonitrile, C.sub.1 -C.sub.5 alkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and treating the resultant product with an alkali is provided, and said process is useful in the synthesis of intermediates for medicinals or pesticides.

3. 发明授权

US4529722A Oxacephalosporin derivatives 失效
标题翻译：牛蒡子衍生物
公开(公告)号：US4529722A
公开(公告)日：1985-07-16
申请号：US559293
申请日：1983-12-05
申请人： Hiromu Matsumura , Toshisada Yano , Masayuki Narisada
发明人： Hiromu Matsumura , Toshisada Yano , Masayuki Narisada
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00 , Y02P20/55
摘要： A 7.beta.-ureidoacetamido-7.alpha.-methoxy-3-[1-(2-hydroxyethyl)-1H-tetrazol-5-yl]thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid derivative represented by the following formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 is hydrogen or alkyl optionally substituted by halogen or pyridinium; R.sup.2 is hydrogen or a hydroxy-protecting group; and R.sup.3 is hydrogen, a light metal, or a carboxy-protecting group.
摘要翻译：将7β-脲基乙酰氨基-7α-甲氧基-3- [1-（2-羟乙基）-1H-四唑-5-基]硫甲基-1-脱硫-1-氧杂-3-头孢烯-4-羧酸衍生物（I）其中R是芳基或杂芳基; R1是氢或任选被卤素或吡啶鎓取代的烷基; R2是氢或羟基保护基; 并且R 3是氢，轻金属或羧基保护基。

4. 发明授权

US5243051A Tetrahydropyridine derivatives 失效
标题翻译：四氢吡啶衍生物
公开(公告)号：US5243051A
公开(公告)日：1993-09-07
申请号：US903924
申请日：1992-06-26
申请人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Akira Matsushita , Masami Eigyo
发明人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Akira Matsushita , Masami Eigyo
IPC分类号： C07D211/70 , C07D211/76 , C07D401/12 , C07D409/14
CPC分类号： C07D401/12 , C07D211/70 , C07D211/76 , C07D409/14
摘要： The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.
摘要翻译：本发明涉及对σ受体具有高亲和力和特异性的四氢吡啶衍生物，由此认为这些化合物对治疗某些精神病有效。

5. 发明授权

US5202345A Carbamoylpyrrolidone derivatives and drugs for senile dementia 失效
标题翻译：氨基甲酰吡咯烷酮衍生物和老年痴呆药物
公开(公告)号：US5202345A
公开(公告)日：1993-04-13
申请号：US832407
申请日：1992-02-07
申请人： Hiromu Matsumura , Toshisada Yano , Akira Matsushita , Masami Eigyo
发明人： Hiromu Matsumura , Toshisada Yano , Akira Matsushita , Masami Eigyo
IPC分类号： C07D207/26 , C07D207/263 , C07D401/12 , C07D403/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/10
CPC分类号： C07D207/27 , C07D401/12 , C07D403/12 , C07D409/14 , C07D413/10 , C07D417/12 , C07D471/10
摘要： A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 14 C.sub.6 alkyl; n is an integer of from 2 to 3; Z.sup.1 is phenyl, benzyl, or isoxazolyl and each is optionally substituted by a halogen, a methoxy, or a methyl group; Z.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, allyl, unsubstituted phenyl, or phenyl substituted by halogen, methyl, or methoxy; orZ.sub.1 and Z.sub.2 are taken together with the adjacent nitrogen atom to form triazolyl, imidazolyl or pyrazolyl; or a pharmaceutically acceptable acid addition salt thereof.
摘要翻译：下式的化合物：其中R 1是氢或C 11-14烷基; n为2〜3的整数， Z 1是苯基，苄基或异恶唑基，并且各自任选被卤素，甲氧基或甲基取代; Z2为氢，C1-C5烷基，烯丙基，未取代的苯基或被卤素，甲基或甲氧基取代的苯基; 或Z 1和Z 2与相邻的氮原子一起形成三唑基，咪唑基或吡唑基; 或其药学上可接受的酸加成盐。

6. 发明授权

US5410058A Tetrahydropyridine derivatives 失效
标题翻译：四氢吡啶衍生物
公开(公告)号：US5410058A
公开(公告)日：1995-04-25
申请号：US202554
申请日：1994-02-28
申请人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Akira Matsushita , Masami Eigyo
发明人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Akira Matsushita , Masami Eigyo
IPC分类号： C07D211/70 , C07D211/76 , C07D401/12 , C07D409/14 , C07D401/06
CPC分类号： C07D401/12 , C07D211/70 , C07D211/76 , C07D409/14
摘要： The compounds of the present invention relates to tetrahydropyridine derivatives and have high affinity and specificity to .sigma. receptors, whereby these are thought to be effective for some psychoses.
摘要翻译：本发明的化合物涉及四氢吡啶衍生物，并且对σ受体具有高亲和力和特异性，因此认为这些对某些精神病有效。

7. 发明授权

US4652652A Thiazolylpropenedicarboxylic acid half esters and process for making 失效
标题翻译：噻唑基丙二酸半酯及其制备方法
公开(公告)号：US4652652A
公开(公告)日：1987-03-24
申请号：US746564
申请日：1985-06-19
申请人： Hiromu Matsumura , Toshisada Yano
发明人： Hiromu Matsumura , Toshisada Yano
IPC分类号： C07D277/20 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/44 , C07D277/46 , C07D277/48
CPC分类号： C07D277/20 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , Y02P20/55
摘要： A useful intermediate for synthesizing penicillins or cephalosporins {i.e., 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid half ester (VI)} is prepared by a process comprising (1) treating haloacetylmalonic acid ester (I) with thiourea to give 2-(2-amino-4-thiazolyl)malonic acid ester (II), (2) protecting the amino group of the latter to give 2-(2-protected amino-4-thiazolyl)malonic acid ester (III), (3) treating the product with haloalkenoic acid ester to give 1-(2-protected amino-4-thiazolyl)-2-propene-(1,1,3-tri or 1,1,3,3-tetra)carboxylic acid ester (IV), (4) hydrolyzing and decarboxylating the latter to give 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid (V), and (5) treating the product with alcohol and a hemi-esterifying reagent to give the objective 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid half ester (VI).
摘要翻译：用于合成青霉素或头孢菌素（即，1-（2-保护的氨基-4-噻唑基）丙烯-1,3-二羧酸半酯（VI）}的有用中间体是通过以下方法制备的：（1）将卤代乙酰基丙二酸酯（I）与硫脲反应，得到2-（2-氨基-4-噻唑基）丙二酸酯（II），（2）保护后者的氨基，得到2-（2-保护的氨基-4-噻唑基）丙二酸酸酯（III），（3）用卤代链烯酸酯处理产物得到1-（2-保护的氨基-4-噻唑基）-2-丙烯 - （1,1,3-三或1,1,3，（IV），（4）使其后水解和脱羧，得到1-（2-保护的氨基-4-噻唑基）丙烯-1,3-二羧酸（V），和（5）处理产物与醇和半酯化试剂反应得到目的1-（2-保护的氨基-4-噻唑基）丙烯-1,3-二羧酸半酯（VI）。

8. 发明授权

US4211779A 7.alpha.-Methoxy substituted cephalosporins 失效
标题翻译： 7α-甲氧基取代头孢菌素
公开(公告)号：US4211779A
公开(公告)日：1980-07-08
申请号：US821314
申请日：1977-08-02
申请人： Masayuki Narisada , Teruji Tsuji , Hiromu Matsumura , Wataru Nagata
发明人： Masayuki Narisada , Teruji Tsuji , Hiromu Matsumura , Wataru Nagata
IPC分类号： A61K31/545 , C07D501/36
CPC分类号： C07D501/36
摘要： Antibacterial 7.alpha.-methoxy-3-cephem derivatives of the formula: ##STR1## [wherein R.sup.1 is hydrogen, or organic or inorganic acyl;R.sup.2 is alkyl; andCOR.sup.3 is carboxy or protected carboxy],methods of production, and pharmaceutical preparations thereof.
摘要翻译：下式的抗菌7α-甲氧基-3-头孢烯衍生物：其中R 1是氢或有机或无机酰基; R2是烷基; 和COR 3是羧基或受保护的羧基]，生产方法及其药物制剂。

9. 发明授权

US5321035A Piperidine derivatives and process for preparation thereof 失效
标题翻译：哌啶衍生物及其制备方法
公开(公告)号：US5321035A
公开(公告)日：1994-06-14
申请号：US93950
申请日：1993-07-21
申请人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Nobuhiro Ibii , Teruo Shiomi
发明人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Nobuhiro Ibii , Teruo Shiomi
IPC分类号： C07D401/12 , A61K31/545
CPC分类号： C07D401/12
摘要： A compound of the formula (I): ##STR1## wherein X.sup.1 nd X.sup.2 each independently represents lower alkyl, lower alkoxy or halogen or a pharmaceutically acceptable salt thereof, which is useful as an active ingredient for a pharmaceutical composition for treating antidepressant or aftereffects of cerebrovascular impairments.
摘要翻译：式（I）的化合物：其中X1和X2各自独立地表示低级烷基，低级烷氧基或卤素或其药学上可接受的盐，其可用作用于治疗抗抑郁药的药物组合物的活性成分或脑血管障碍的后遗症。

10. 发明授权

US5149817A Teirahydropyridine derivatives 失效
标题翻译：噻吩衍生物
公开(公告)号：US5149817A
公开(公告)日：1992-09-22
申请号：US655585
申请日：1991-02-15
申请人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Akira Matsushita , Masami Eigyo
发明人： Hiromu Matsumura , Toshisada Yano , Hiroshi Hashizume , Akira Matsushita , Masami Eigyo
IPC分类号： C07D211/70 , C07D211/76 , C07D401/12 , C07D409/14
CPC分类号： C07D401/12 , C07D211/70 , C07D211/76 , C07D409/14
摘要： The present invention relates to tetrahydropyridine derivatives which have high affinity and specificity to .sigma. receptors, whereby these compounds are thought to be effective for treatment of some psychoses.

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