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1. 发明授权

US3362952A alpha-methoxyfluorobenzylpenicillins 失效
标题翻译： α-甲氧基氟苄基青霉素
公开(公告)号：US3362952A
公开(公告)日：1968-01-09
申请号：US46456865
申请日：1965-06-16
申请人： BEECHAM GROUP LTD
发明人： RAYMOND STOVE EDWARD , RODNEY THOMAS GORDON
IPC分类号： C07D499/00 , C07D499/60
CPC分类号： C07D499/00

2. 发明专利

DE1545590A1 未知
公开(公告)号：DE1545590A1
公开(公告)日：1969-08-07
申请号：DE1545590
申请日：1965-05-26
申请人： BEECHAM GROUP LTD
发明人： RAYMOND STOVE EDWARD , RODNEY THOMAS GORDON
IPC分类号： C07D499/00 , C07D499/60

3. 发明专利

DE1795861B1 未知
公开(公告)号：DE1795861B1
公开(公告)日：1979-03-08
申请号：DE1795861
申请日：1967-05-12
申请人： BEECHAM GROUP LTD
发明人： JOHN NEAL DAVID PATRICK , RAYMOND STOVE EDWARD
IPC分类号： C07D499/00 , C07D499/72
摘要： (A) Penicillins (I) R = alkyl or aralkyl, possibly substd. in the ring X = -S or -O Preferred cpds. have X = - S and R = benzyl (B) Non-toxic salts of (I) including metal salts, ammonium and substd. ammonium salts. The new cpds. are valuable antibacterial agents; they may be used as feed additives in animal feeds, as agents for the treatment of mastitis in cattle and as therapeutic agents for poultry and animals, including man, in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria. They are also valuable intermediates in the prepn. of corresponding carboxy cpds. as described in Pat. 64/04384.

4. 发明专利

DE1670284A1 未知
公开(公告)号：DE1670284A1
公开(公告)日：1971-01-28
申请号：DE1670284
申请日：1967-10-31
申请人： BEECHAM GROUP LTD
发明人： DAVID HARDY KENNETH , CHARLES NAYLER JOHN HERBERT , RAYMOND STOVE EDWARD
IPC分类号： A61K31/43 , C07D499/00 , C07D499/72 , A61K21/00

5. 发明专利

DE1670084A1 未知
公开(公告)号：DE1670084A1
公开(公告)日：1970-10-29
申请号：DE1670084
申请日：1966-05-24
申请人： BEECHAM GROUP LTD
发明人： DAVID HARDY KENNETH , CHARLES NAYLER JOHN HERBERT , RAYMOND STOVE EDWARD
IPC分类号： C07D499/00 , C07D499/44 , C07D499/46 , C07D499/48 , C07D99/20
摘要： The invention relates to betaine penicillins of formula where Q+ is a quaternary ammonium group derived from a tertiary amine Q and X is a divalent organic radical. Typical betaines are a -trimethylaminobenzylpenicillin betaine, pyridinium methyl penicillin betaine and a -(pyridinoacetamido)benzyl penicillin betaine. The betaines are prepared by quaternizing, with a tertiary amine Q, a penicillin or non-toxic salt thereof, of formula where Q and X have the above meanings and R is the acid residue of a reactive ester, e.g. a halogen atom, a sulphuric acid residue, e.g. methoxy-sulphonyloxy or a sulphonic acid residue, e.g. toluene p-sulphonyloxy group. The tertiary amine is a trialkylamine, a heteroaromatic base or a reduced heteroaromatic base.

6. 发明专利

DE1545596A1 未知
公开(公告)号：DE1545596A1
公开(公告)日：1969-08-07
申请号：DE1545596
申请日：1965-06-28
申请人： BEECHAM GROUP LTD
发明人： RAYMOND STOVE EDWARD , RODNEY THOMAS GORDON
IPC分类号： C07D499/00 , C07D499/60
摘要： Penicillins, particularly effective in the presence of human serum, have the formula where X is hydrogen or chlorine. Salts are formed with alkali and alkaline earth metals, aluminium, ammonium and organic amines. The penicillins are prepared by reacting 6-aminopenicillanic acid or a salt thereof, with an acid of formula wherein X has the above meaning. A functional equivalent of the acid, e.g. acid chloride, or an intermediate formed from the a -methoxy acid and a condensing agent, e.g. dicyclohexyl-carbodiimide may be used. The penicillins are effective antibacterials when administered orally. They may be used as nutritional supplements in animal feed and for the treatment of mastitis in cattle. m-Fluoro-a -methoxyphenyl acetyl chloride is prepared by treating m - fluoro - a - methoxy - phenylacetic acid with thionyl chloride. 4-Chloro-3-fluorotoluene is prepared by treating 4-chloro-m-toluidine with sodium nitrite and fluoroboric acid and decomposing the resultant 2-chloro-5-methyl benzene diazonium fluoroborate by heat. 4 - Chloro - 3 - fluoro - a - methoxyphenylacetic acid is prepared by reacting 4-chloro-3 fluoro-toluene with bromine and conc. H2SO4 to form 4-chloro-3-fluorobenzaldehyde, which is treated with bromoform and KOH in methanol followed by acidification with HCl to form the sodium hydrogen salt, which is dissolved in aqueous KOH and the free acid liberated by the addition of HCl. Reference has been directed by the Comptroller to Specification 880,042.

7. 发明专利

DE1770225A1 未知
公开(公告)号：DE1770225A1
公开(公告)日：1971-10-07
申请号：DE1770225
申请日：1968-04-18
申请人： BEECHAM GROUP LTD
发明人： DAVID HARDY KENNETH , RAYMOND STOVE EDWARD
IPC分类号： C07D499/00 , C07D499/72 , A61K21/00

8. 发明专利

DE1670222A1 未知
公开(公告)号：DE1670222A1
公开(公告)日：1971-01-21
申请号：DEB0092496
申请日：1967-05-12
申请人： BEECHAM GROUP LTD
发明人： NEIL DILKUSHA DAVID PATRICK JO , RAYMOND STOVE EDWARD
IPC分类号： C07D499/00 , C07D499/72 , C07D99/16
摘要： (A) Penicillins (I) R = alkyl or aralkyl, possibly substd. in the ring X = -S or -O Preferred cpds. have X = - S and R = benzyl (B) Non-toxic salts of (I) including metal salts, ammonium and substd. ammonium salts. The new cpds. are valuable antibacterial agents; they may be used as feed additives in animal feeds, as agents for the treatment of mastitis in cattle and as therapeutic agents for poultry and animals, including man, in the treatment of infectious diseases caused by Gram-positive and Gram-negative bacteria. They are also valuable intermediates in the prepn. of corresponding carboxy cpds. as described in Pat. 64/04384.

9. 发明专利

DE1545642A1 未知
公开(公告)号：DE1545642A1
公开(公告)日：1969-08-07
申请号：DE1545642
申请日：1965-12-02
申请人： BEECHAM GROUP LTD
发明人： RAYMOND STOVE EDWARD
IPC分类号： C07D499/00 , C07D499/60

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