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1. 发明授权

US3819707A 4-(aminoalkylamino)-2-halobenzyl alcohols 失效
标题翻译： 4-（氨基甲酰氨基）-2-甲氧基乙醇
公开(公告)号：US3819707A
公开(公告)日：1974-06-25
申请号：US22104772
申请日：1972-01-26
申请人： STERLING DRUG INC
发明人： ARCHER S , ROSI D
IPC分类号： C07D295/073 , C07D295/08 , C07D295/096 , C07D295/112 , C07C87/48
CPC分类号： C07D295/073 , C07D295/08 , C07D295/096 , C07D295/112 , Y10S435/913
摘要： 4-(AMINO-(POLYCARBON - LOWER-ALKYL)-AMINO)-2-HALOBENZYL ALCOHOLS AND LOWER-ALKYL ETHERS THEREOF HAVE SCHISTOSMOCIDAL ACTIVITY. THE BENZYL ALCOHOLS ARE PREPARED: BY REDUCTION OF THE CORRESPONDING BENZALDEHYDES OR LOWER-ALKYL BENZOATES; BY MICROBIOLOGICAL OXIDATION OF THE CORRESPONDING 4-SUBSTITUTED-AMINO-2-HALOTOLUENES; OR, FOR THE COMPOUNDS WHERE POLYCARBON-LOWER-ALKYL IS ETHYLENE, BY REDUCING THE CORRESPONDING LOWER-ALKYL 4(AMINOACETYLAMINO)-2-HALOBENZOATES OR BY REDUCING THE CORRESPONDING 4-(AMINOACETYLAMINO) - 2 - HALOBENZYL ALCOHOLS. THE ETHERS ARE PREPARED BY HEATING THE BENZYL ALCOHOLS WITH A LOWER-ALKANOL IN THE PRESENCE OF AN ACID.

2. 发明授权

US3714167A 4-aminoalkylamino-2-halobenzyl alcohols and alkyl ethers thereof 失效
标题翻译： 4-氨基亚氨基-2-羰基乙醇及其烷基醚
公开(公告)号：US3714167A
公开(公告)日：1973-01-30
申请号：US3714167D
申请日：1970-06-02
申请人： STERLING DRUG INC
发明人： ARCHER S , ROSI D
IPC分类号： C07D295/08 , C07D51/70
CPC分类号： C07D295/08
摘要： 4-8AMINO-(POLYCARBON-LOWER-ALKKYL)-AMINO) - 2 - HALOBENZYL ALCOHOLS AND LOWER-ALKYL ETHERS THEREOF HAVE SCHISTOSOMACIDAL ACTIVITY. THE BENZYL ALCOHOLS ARE PREJPARED: BY RREDUCTION OF THE CORRESPONDING BENZALDEHYDES OR LOWER-ALKYL BENZOATES; BY MICROBOILOGICAL OXIDATION OF THE CORRESPONDING 4-SUBSTITUTED-AMINO-2-HALOTOLUENES; OR, FOR THE COMPOUNDS WHERE POLYCARON-LOWER-ALKYL IS ETHYLENE, BY REDUCING THE CORRESPONDING LOWER-ALKYL 4-(AMINOACETYLAMINO)-2-HALOBENZOATES OR BY REDUCING THE CORRESPONDING 4 - (AMINOACETYLAMINO)-2-HALOBENZYL ALCOHOLS. THE ETHERS ARE PREPARED BY THE HEATING THE BENZYL ALCOHOLS WITH A LOWER-ALKANOL IN THE PRESENCE OF AN ACID.

3. 发明授权

US3711512A Preparation of 1-(aminoalkylamino)-4-hydroxymethylthioxanthen-9-ones 失效
标题翻译： 1-（氨基亚氨基）-4-羟基甲基硫代吗啉-9-酮的制备
公开(公告)号：US3711512A
公开(公告)日：1973-01-16
申请号：US3711512D
申请日：1970-10-05
申请人： STERLING DRUG INC
发明人： ROSI D , COLLINS J , MILLER T
IPC分类号： C07D335/16 , A61K27/00 , C07D65/18
CPC分类号： C07D335/16
摘要： A PROCESS FOR THE PREPARATION OF 1-(R1R2N-Y-N (R)-4-HYDROXYMETHYLTHIOXANETHEN-9 - ONE, SCHISTOSOMACIDAL AGENT, WHICH COMPRISES REACTING 1-(R1R2N-Y-N 8R)THIOXANTHEN-9-ONE WITH EXCESS FORMALDEHYDE AT AN ACIDIC PH WHERE R IS HYDROGEN OR METHYL, R1 AND R2 ARE EACH LOWER-ALKYL, AND Y IS LOWER-ALKYLENE HAVING FROM TWO TO FOUR CARBON ATOMS AND HAVING ITS TWO CONNECTING LINKAGES ON DIFFERENT CARBON ATOMS.

4. 发明授权

US3855291A 2-halo-4-(aminoacetamido)-benzyl alcohols 失效
标题翻译： 2-氨基-4-（氨基甲酰胺） - 苯甲醇
公开(公告)号：US3855291A
公开(公告)日：1974-12-17
申请号：US36818373
申请日：1973-06-08
申请人： STERLING DRUG INC
发明人： ARCHER S , ROSI D
IPC分类号： C07D295/096 , C07D295/13 , C12P17/12 , C07C103/38
CPC分类号： C07D295/096 , C07D295/13 , C12P17/12
摘要： 4-(Amino-(polycarbon-lower-alkyl)-amino)-2-halobenzyl alcohols and lower-alkyl ethers thereof have schistosomacidal activity. The benzyl alcohols are prepared: by reduction of the corresponding benzaldehydes or lower-alkyl benzoates; by microbiological oxidation of the corresponding 4-substitutedamino-2-halotoluenes; or, for the compounds where polycarbonlower-alkyl is ethylene, by reducing the corresponding loweralkyl 4-(aminoacetylamino)-2-halobenzoates or by reducing the corresponding 4-(aminoacetylamino)-2-halobenzyl alcohols. The ethers are prepared by heating the benzyl alcohols with a loweralkanol in the presence of an acid.
摘要翻译： 4- [氨基 - （聚碳 - 低级 - 烷基） - 氨基] -2-卤代苄醇及其低级烷基醚具有血吸虫活性。制备苄醇：通过还原相应的苯甲醛或苯甲酸低级烷基酯; 通过相应的4-取代 - 氨基-2-卤代甲苯的微生物氧化; 或通过还原相应的4-（氨基乙酰基氨基）-2-卤代苯甲酸的低级烷基酯或通过还原相应的4-（氨基乙酰基氨基）-2-卤代苄醇，对于聚碳 - 低级 - 烷基是亚乙基的化合物。醚通过在酸存在下用低级链烷醇加热苄醇来制备。

5. 发明授权

US3764612A Preparation of 1-aminoalkylamino-9-orothioxanthene-4-carbox-aldehydes 失效
标题翻译： 1-氨基甲酰氨基-9-异二氢-4-羧酸 - 醛酸的制备
公开(公告)号：US3764612A
公开(公告)日：1973-10-09
申请号：US3764612D
申请日：1970-10-05
申请人： STERLING DRUG INC
发明人： COLLINS J , ROSI D
IPC分类号： C07D335/16 , A61K27/00 , C07D65/18
CPC分类号： C07D335/16
摘要： 1-(R1R2N-Y-NH)-9-oxothioxanthene-4-carboxaldehydes, intermediates for the preparation of the corresponding 4hydroxymethyl compounds, are prepared by heating 1-chlorothioxanthen-9-one with R1R2N-Y-NHCH3 to yield 1-(R1R2N-Y-NH(CH3)) thioxanthen-9-one, reacting the latter compound with phosphorus oxyhalide and dimethylformamide to yield 1-(R1R2N-Y-N(CH3))-9oxothioxanthene-4-carboxaldehyde and reacting said aldehyde with pyridine hydrochloride to produce 1-(R1R2N-Y-NH)-9oxothioxanthene-4-carboxaldehyde, where R1 and R2 are each loweralkyl and Y is lower-alkylene having from two to four carbon atoms and having its two connecting linkages on different carbon atoms. The novel intermediates, 1-(R1R2N-Y-N(CH3))thioxanthen-9ones, also have antibacterial activity.
摘要翻译：通过用R1R2N-Y-NHCH3加热1-氯 - 噻吨-9-酮，制备1-（R1R2N-Y-NH）-9-氧代噻吨-4-甲醛，制备相应的4-羟甲基化合物的中间体，得到1- [R 1 R 2 N -Y-NH（CH 3）]噻吨-9-酮，使后一化合物与磷酰卤和二甲基甲酰胺反应，得到1- [R 1 R 2 N -YN（CH 3）] - 9-氧代噻吨-4-甲醛，所述醛与吡啶盐酸盐反应，得到1-（R1R2N-Y-NH）-9-氧代噻吨-4-甲醛，其中R 1和R 2各自为低级烷基，Y为具有2至4个碳原子的低级亚烷基，两个不同碳原子上的连接键。新型中间体1- [R1R2N-Y-N（CH3）]噻吨-9-酮也具有抗菌活性。

6. 发明授权

US3745172A 1-(di-(lower-alkyl)aminoalkylamino)-9-oxothioxanthenes 失效
标题翻译： 1-（DI-（低级 - 烷基）氨基亚氨基）-9-氧代二甲基
公开(公告)号：US3745172A
公开(公告)日：1973-07-10
申请号：US3745172D
申请日：1970-10-05
申请人： STERLING DRUG INC
发明人： COLLINS J , ROSI D
IPC分类号： C07D335/16 , A61K27/00 , C07D65/18
CPC分类号： C07D335/16
摘要： A PROCESS WHICH COMPRISES REACTING 1-(DI(LOWER-ALKYL) AMINO - Y - AMINO)-9-OXOTHIOXANTHENE-4-CARBOXALDEHYDE ALDOXIME, WHERE Y IS LOWER-ALKYLENE, WITH A LOWER-ALKANOYLATING AGENT TO PRODUCE 1-(DI-(LOWER-ALKYL)-AMINO-YAMINO) - 9 - OXOTHIOXANTHENE - 4-CARBOXALDEHYDE (LOWERALKANOYL)ALDOXIME, HEATING SAID (LOWER-ALKANOYL)ALDOXIME TO PRODUCE 1 - (DI - (LOWER-ALKYL)AMINO-Y-AMINO)-9OXOTHIOXANTHENE-4-CARBONITRILE, HEATING SAID 4-CARBONITRILE IN AN AQUEOUS ACIDIC MEDIUM TO PRODUCE 1-(DI-(LOWERALKYL) - AMINO-Y-AMINO)THIOXANTHEN-9-ONE, INTERMEDIATES IN THE SYNTHESIS OF KNOW SCHISTOSOMACIDAL AGENTS.

7. 发明专利

DK116663B 未知
公开(公告)号：DK116663B
公开(公告)日：1970-02-02
申请号：DK442764
申请日：1964-09-08
申请人： STERLING DRUG INC
发明人： ROSI D , PERUZZOTTI G
IPC分类号： C07D311/82 , C07D311/86 , C12P17/06 , C12P17/18 , C07D7/42 , C07D65/16

8. 发明专利

BR6804817D0 未知
公开(公告)号：BR6804817D0
公开(公告)日：1973-03-08
申请号：BR20481768
申请日：1968-12-13
申请人： STERLING DRUG INC
发明人： ARCHER S , DENNIS E , BAILY D , ROSI D
IPC分类号： C07D215/18 , C07D215/38 , C07D215/48

9. 发明专利

ZA716590B PROCESS FOR PREPARING THIOXANTHENES AND INTERMEDIATES 未知
公开(公告)号：ZA716590B
公开(公告)日：1972-06-28
申请号：ZA716590
申请日：1971-10-01
申请人： STERLING DRUG INC
发明人： COLLINS J , ROSI D , MILLER T
IPC分类号： C07D335/16 , C07D
摘要： 1-(R1R2N-Y-NH)-9-oxothioxanthene-4-carboxaldehydes, intermediates for the preparation of the corresponding 4-hydroxymethyl compounds, are prepared by heating 1-chloro-thioxanthen-9-one with R1R2N-Y-NHCH3 to yield 1-[R1R2N-Y-NH(CH3)] thioxanthen-9-one, reacting the latter compound with phosphorus oxyhalide and dimethylformamide to yield 1-[R1R2N-Y-N(CH3)]-9-oxothioxanthene-4-carboxaldehyde and reacting said aldehyde with pyridine hydrochloride to produce 1-(R1R2N-Y-NH)-9-oxothioxanthene-4-carboxaldehyde, where R1 and R2 are each lower-alkyl and Y is lower-alkylene having from two to four carbon atoms and having its two connecting linkages on different carbon atoms. The novel intermediates, 1-[R1R2N-Y-N(CH3)]thioxanthen-9-ones, also have antibacterial activity.

10. 发明专利

PH11755A PROCESS FOR PREPARING THIOXANTHENES AND INTERMEDIATES 未知
公开(公告)号：PH11755A
公开(公告)日：1978-06-27
申请号：PH12899
申请日：1971-10-05
申请人： STERLING DRUG INC
发明人： COLLINS J , ROSI D
IPC分类号： C07D335/12

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