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1. 发明授权

US4529721A Vinylthioacetamido oxacephalosporin derivatives 失效
标题翻译：乙烯基硫代乙酰氨基氧杂环孢菌素衍生物
公开(公告)号：US4529721A
公开(公告)日：1985-07-16
申请号：US534147
申请日：1983-09-21
申请人： Wataru Nagata , Mitsuru Yoshioka , Yasuhiro Nishitani , Tsutomu Aoki , Toshiro Konoike , Tadatoshi Kubota
发明人： Wataru Nagata , Mitsuru Yoshioka , Yasuhiro Nishitani , Tsutomu Aoki , Toshiro Konoike , Tadatoshi Kubota
IPC分类号： A01N43/90 , C07D241/08 , C07D339/00 , C07D505/00 , C07D519/00 , C07F9/535 , A01N59/06 , C07D498/04
CPC分类号： C07F9/5352 , C07C309/00 , C07C323/00 , C07D241/08 , C07D339/00 , C07D505/00 , Y02P20/55
摘要： A compound of the formula: ##STR1## wherein u represents hydrogen, carboxamido, N-hydroxycarboxamido, carboxy, azido, an aryl, an acylamino, a protected carboxy or an N-alkoxycarboxamido, or, together with v, can represent --S-- or --CH.sub.2 S--; v represents hydrogen, halogen, cyano or an alkylthio, or, together with u, can represent --S-- or --CH.sub.2 S--, or, together with w, can represent --(CH.sub.2).sub.3 CO--; w represents hydrogen, carboamoyl, cyano, carboxy, an N-alkylcarbamoyl, an alkyl, an aryl, a protected carboxy or a heterocycle, or, together with v, can represents --(CH.sub.2).sub.3 CO--; x represents halogen, trifluoromethyl, an alkylthio or an arylthio; y represents hydrogen, a light metal or a carboxylic acid protecting group; and z represents an acyloxy or a heterocycle-thio, each of the above radicals represented by the symbols u, v, w, x, y and z being optionally substituted by halogen or a carbon-, nitrogen-, oxygen- or sulfur-containing functional group, a process for preparing the compound, a pharmaceutical composition containing the compound, and a therapeutical use of the compound.A compound of the formula: ##STR2## wherein u, v, w and x are as defined above, useful as a starting compound for preparing the compound (I) is also provided.
摘要翻译：下式的化合物：其中u表示氢，甲酰氨基，N-羟基羧甲酰氨基，羧基，叠氮基，芳基，酰氨基，被保护的羧基或N-烷氧基羧酰胺基，或与v一起可代表 -S-或-CH2S-; v表示氢，卤素，氰基或烷硫基，或与u一起可以表示-S-或-CH 2 S-，或者与w一起可以表示 - （CH 2）3 CO-; w表示氢，氨甲酰基，氰基，羧基，N-烷基氨基甲酰基，烷基，芳基，保护的羧基或杂环，或与v一起可以表示 - （CH 2）3 CO-; x表示卤素，三氟甲基，烷硫基或芳硫基; y表示氢，轻金属或羧酸保护基; 和z表示酰氧基或杂环硫基，由符号u，v，w，x，y和z表示的上述基团中的每一个任选被卤素或含碳，氮，氧或硫的官能团，制备该化合物的方法，含该化合物的药物组合物和该化合物的治疗用途。还提供了下式化合物：其中u，v，w和x如上定义，可用作制备化合物（I）的起始化合物。

2. 发明授权

US4159984A Reductive cleavage of oxazolidine compounds 失效
标题翻译：还原性裂解恶唑烷化合物
公开(公告)号：US4159984A
公开(公告)日：1979-07-03
申请号：US790618
申请日：1977-04-25
申请人： Mitsuru Yoshioka , Teruji Tsuji , Yasuhiro Nishitani , Wataru Nagata
发明人： Mitsuru Yoshioka , Teruji Tsuji , Yasuhiro Nishitani , Wataru Nagata
IPC分类号： C07D205/08 , C07D205/085 , C07D205/095 , C07D499/00 , C07D499/44 , C07D499/48 , C07D499/72 , C07D503/00 , C07D505/00
CPC分类号： C07D205/085 , C07D499/00 , C07D505/00
摘要： Compounds represented by the following formula prepared from 6-aminopenicillanic acid are key intermediates in a stereo-specific synthesis of 1-oxadethiacephalosporins, highly active antibiotics: ##STR1## [wherein COA and COB each is carboxy or protected carboxy;Cox is carboxy, protected carboxy, or a group of the formula --COCQ.dbd.N.sub.2 or --COCHQ--Z (in which Q is hydrogen, lower alkyl or aryl; and Z is hydrogen or a nucleophilic group);Hal is halogen;R is lower alkyl or aralkyl; andY is hydrogen or acyl].
摘要翻译：由6-氨基青霉烷酸制备的下列化合物所代表的化合物是立体特异性合成1-羟基乙硫菌素，高活性抗生素的关键中间体：其中COA和COB各自为羧基或被保护的羧基; COX是羧基，受保护的羧基或式-COCQ = N2或-COCHQ-Z（其中Q是氢，低级烷基或芳基; Z是氢或亲核基团）的基团; 卤素是卤素; R是低级烷基或芳烷基; 和Y是氢或酰基]。

3. 发明授权

US4592865A Azetidinone intermediates for cephalosporin analogs 失效
标题翻译：氮杂环丁酮中间体用于头孢菌素类似物
公开(公告)号：US4592865A
公开(公告)日：1986-06-03
申请号：US589670
申请日：1984-03-13
申请人： Masayuki Narisada , Hiroshi Onoue , Teruji Tsuji , Yasuhiro Nishitani , Mitsuru Yoshioka , Yoshio Hamashima , Wataru Nagata
发明人： Masayuki Narisada , Hiroshi Onoue , Teruji Tsuji , Yasuhiro Nishitani , Mitsuru Yoshioka , Yoshio Hamashima , Wataru Nagata
IPC分类号： C07D205/08 , C07D205/085 , C07D403/12 , C07D405/12 , C07D417/12 , C07D505/00 , C07F9/568 , C07D498/04
CPC分类号： C07F9/5683 , C07D205/085 , C07D505/00
摘要： Intermediates of the following formula are useful for the synthesis of 1-oxacephalosporins. Their preparation from penicillins and the transformation process to make 1-oxacephalosporins are disclosed. The compounds are of the formula: ##STR1## wherein A is amino or a selected acylamino;COB is carboxy or a selected protected-carboxy;X is halogen or the group ORin which R is a group represented by following formulas: ##STR2## wherein Nu is a selected nucleophilic group; R.sup.1 is a group of the following formula: ##STR3## in which Hal is halogen or alkylsulfonyloxy and R.sup.2 is alkyl or aryl; andY is hydrogen or methoxy; with the proviso that when R is propargyl or 2-oxopropyl andR.sup.1 is ##STR4## A is in the 3.alpha.-configuration and Y is 3.beta.-hydrogen or A is in the 3.beta.-configuration and Y is 3.alpha.-methoxy.
摘要翻译：下列配方的中间体可用于合成1-氧杂七环素。公开了它们从青霉素的制备和制备1-氧杂七环素的转化过程。化合物具有下式：其中A是氨基或选择的酰氨基; COB是羧基或选择的保护羧基; X是卤素或基团OR，其中R是由下式表示的基团：CH2CCH，CH2CCNu，CH2CHCH2，＆lt; IMAGE＆gt;＆gt;其中Nu是选择的亲核基团; R1是下式的基团：其中Hal是卤素或烷基磺酰氧基，R2是烷基或芳基的 Y为氢或甲氧基; 条件是当R为炔丙基或2-氧代丙基且R 1为A 3构型时，Y为3个β-氢，或A为3个β-构型，Y为3个α-甲氧基。

4. 发明授权

US4143038A Cephalosporin analogues 失效
标题翻译： CEPHALOSPORIN ANALOGUES
公开(公告)号：US4143038A
公开(公告)日：1979-03-06
申请号：US846503
申请日：1977-10-26
申请人： Masayuki Narisada , Hiroshi Onoue , Teruji Tsuji , Yasuhiro Nishitani , Mitsuru Yoshioka , Yoshio Hamashima , Wataru Nagata
发明人： Masayuki Narisada , Hiroshi Onoue , Teruji Tsuji , Yasuhiro Nishitani , Mitsuru Yoshioka , Yoshio Hamashima , Wataru Nagata
IPC分类号： C07D205/085 , C07D505/00 , C07D205/00
CPC分类号： C07D205/085 , C07D505/00
摘要： Potent antibacterial cephalosporin analogues of the following formula in forms of free acids, pharmaceutically acceptable salts, or esters preparable from penicillins through azetidinone derivatives by way of a new process, and utilizable as active ingredients in bactericidal compositions for pharmaceutical and veterinary use: ##STR1## (wherein Acyl is selected from phenylacetyl, D-mandeloyl, .alpha.-phenylmalonyl, D-.alpha.-(3-methanesulfonyl-2-oxoimidazolidin-l-yl)carbonamido-.alpha.-phenylacetyl, and 2-thienylacetyl).

5. 发明授权

US4223132A Selective conversion of benzyl alcohol carboxylates to the free acid form 失效
标题翻译：将苄醇羧酸盐选择性转化为游离酸形式
公开(公告)号：US4223132A
公开(公告)日：1980-09-16
申请号：US818597
申请日：1977-07-25
申请人： Teruji Tsuji , Mitsuru Yoshioka , Takahiro Kataoka , Yuji Sendo , Shoichi Hirai , Takashi Maeda , Wataru Nagata
发明人： Teruji Tsuji , Mitsuru Yoshioka , Takahiro Kataoka , Yuji Sendo , Shoichi Hirai , Takashi Maeda , Wataru Nagata
IPC分类号： C07D487/04 , C07D499/04 , C07D501/04
CPC分类号： C07D501/04 , C07D487/04 , Y02P20/55
摘要： A process for preparing free carboxylic acids which comprises treating an optionally substituted benzyl ester with a Lewis acid, preferably in the presence of a cation acceptor, followed by hydrolysis, if required.
摘要翻译：制备游离羧酸的方法，其包括用路易斯酸处理任选取代的苄基酯，优选在阳离子受体存在下，然后如果需要水解。

6. 发明授权

US4220766A Oxazolines 失效
标题翻译：恶唑啉
公开(公告)号：US4220766A
公开(公告)日：1980-09-02
申请号：US868422
申请日：1978-01-10
申请人： Teruji Tsuji , Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
发明人： Teruji Tsuji , Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
IPC分类号： C07D498/04 , C07D499/00 , C07D505/00 , C07D285/16 , C07D491/04
CPC分类号： C07D505/00 , C07D499/00 , Y02P20/582
摘要： Useful intermediates for preparing a 1-dethia-1-oxacephalosporin and represented by the following formula: ##STR1## (wherein R is a monovalent group resulting from the elimination of the carbonyl function of an acyl group derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy; andX is hydrogen or a nucleophilic group)are prepared from the corresponding penicillin 1-oxides of the following formula: ##STR2## (wherein R, COB, and X are as defined above) by heating, if required in the presence of the desulfurizing reagent, or by exchanging the X group with another one under the condition of an appropriate nucleophilic substitution.
摘要翻译：用于制备1-脱硫-1-氧杂环孢菌素并由下式表示的有用的中间体：其中R是由消除衍生自羧酸或碳酸的酰基的羰基官能团产生的一价基团; COB 是羧基或被保护的羧基; X是氢或亲核基团）由相应的下式的青霉素1-氧化物制备：如果需要，通过加热，其中R，COB和X如上所定义在脱硫试剂的存在下，或者通过在适当的亲核取代条件下与另一种X基团交换X基团。

7. 发明授权

US4366316A 1-Oxadethiacepham compounds and process for producing said compounds 失效
标题翻译： 1-氧杂十八胺化合物及其制备方法
公开(公告)号：US4366316A
公开(公告)日：1982-12-28
申请号：US322662
申请日：1981-11-18
申请人： Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Teruji Tsuji , Wataru Nagata
发明人： Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Teruji Tsuji , Wataru Nagata
IPC分类号： C07D498/04 , C07D505/00
CPC分类号： C07D505/00
摘要： Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl group derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving group are prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid. The new compounds of this invention shown by the following formula: ##STR4## wherein A is amino or substituted amino;E is hydrogen or methoxy; andY is a divalent group of the following formula: ##STR5## in which COB, X, and Z are as defined above are convertible into other compounds of the same formula by applying conventional methods in .beta.-lactam chemistry.
摘要翻译：用于制备由下式表示的抗细菌1-脱氧-1-氧杂头孢菌素的中间体：其中R是衍生自羧酸或碳酸的酰基的一价基团（减去羰基）; Y1是下式的二价基团：其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z是离去基团由下式的化合物制备：其中R和Y1如上所定义，通过酸的作用。本发明的新化合物由下式表示：其中A是氨基或取代的氨基; E是氢或甲氧基; 并且Y是下式的二价基团：其中COB，X和Z如上定义的可通过在β-内酰胺化学中应用常规方法转化为相同式的其它化合物。

8. 发明授权

US4443598A 1-Oxadethiacepham compounds 失效
标题翻译： 1-氧杂十八胺化合物
公开(公告)号：US4443598A
公开(公告)日：1984-04-17
申请号：US374862
申请日：1982-05-04
申请人： Mitsuru Yoshioka , Uyeo Shoichiro , Yoshio Hamashima , Ikuo Kikkawa , Teruji Tsuji , Wataru Nagata
发明人： Mitsuru Yoshioka , Uyeo Shoichiro , Yoshio Hamashima , Ikuo Kikkawa , Teruji Tsuji , Wataru Nagata
IPC分类号： C07D498/04 , C07D505/00
CPC分类号： C07D505/00
摘要： Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving groupare prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid. The new compounds of this invention shown by the following formula: ##STR4## wherein A is amino or substituted amino;E is hydrogen or methoxy; andY is a divalent group of the following formula: ##STR5## in which COB, X, and Z are as defined above are convertible into other compounds of the same formula by applying conventional methods in .beta.-lactam chemistry.
摘要翻译：用于制备由下式表示的抗菌1-脱氧-1-氧杂头孢菌素的中间体：其中R是衍生自羧酸或碳酸的酰基的一价基团（减去羰基）; Y1是下式的二价基团：其中COB是羧基或被保护的羧基; X是氢或亲核基团; 并且Z是离去基团由下式的化合物制备：其中R和Y1如上所定义，通过酸的作用。本发明的新化合物由下式表示：其中A是氨基或取代的氨基; E是氢或甲氧基; 并且Y是下式的二价基团：其中COB，X和Z如上定义的 + TR 可通过在β-内酰胺化学中应用常规方法转化为相同式的其它化合物。

9. 发明授权

US4271296A Oxazolines 失效
公开(公告)号：US4271296A
公开(公告)日：1981-06-02
申请号：US112145
申请日：1980-01-14
申请人： Teruji Tsuji , Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
发明人： Teruji Tsuji , Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
IPC分类号： C07D498/04 , C07D499/00 , C07D505/00 , C07D401/14 , C07D413/14
CPC分类号： C07D505/00 , C07D499/00 , Y02P20/582
摘要： Useful intermediates for preparing a 1-dethia-1-oxacephalosporin and represented by the following formula: ##STR1## (wherein R is a monovalent group resulting from the elimination of the carbonyl function of an acyl group derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy; andX is hydrogen or a nucleophilic group)are prepared from the corresponding penicillin 1-oxides of the following formula: ##STR2## (wherein R, COB, and X are as defined above) by heating, if required in the presence of a desulfurizing reagent, or by exchanging the X group with another one under the condition of an appropriate nucleophilic substitution.

10. 发明授权

US4271295A Oxazolines 失效
标题翻译：恶唑啉
公开(公告)号：US4271295A
公开(公告)日：1981-06-02
申请号：US112144
申请日：1980-01-14
申请人： Teruji Tsuji , Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
发明人： Teruji Tsuji , Mitsuru Yoshioka , Shoichiro Uyeo , Yoshio Hamashima , Ikuo Kikkawa , Wataru Nagata
IPC分类号： C07D498/04 , C07D499/00 , C07D505/00 , C07D401/14 , C07D413/14
CPC分类号： C07D505/00 , C07D499/00 , Y02P20/582
摘要： Useful intermediates for preparing a 1-dethia-1-oxacephalosporin and represented by the following formula: ##STR1## (wherein R is a monovalent group resulting from the elimination of the carbonyl function of an acyl group derived from a carboxylic or carbonic acid;COB is carboxy or protected carboxy; andX is hydrogen or a nucleophilic group)are prepared from the corresponding penicillin 1-oxides of the following formula: ##STR2## (wherein R, COB, and X are as defined above) by heating, if required in the presence of a desulfurizing reagent, or by exchanging the X group with another one under the condition of an appropriate nucleophilic substitution.
摘要翻译：用于制备1-脱硫-1-氧杂环孢菌素并由下式表示的有用的中间体：其中R是由消除衍生自羧酸或碳酸的酰基的羰基官能团产生的一价基团; COB 是羧基或被保护的羧基; X是氢或亲核基团）由相应的下式的青霉素1-氧化物制备：如果需要，通过加热，其中R，COB和X如上所定义在脱硫试剂的存在下，或者通过在适当的亲核取代条件下将X基团与另一种基团交换。

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