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1. 发明授权

US4983726A Process for preparing nitrosourea derivatives 失效
标题翻译：亚硝基脲衍生物的制备方法
公开(公告)号：US4983726A
公开(公告)日：1991-01-08
申请号：US440905
申请日：1989-11-24
申请人： Pierre Roger , Patrick Choay , Claude Monneret , Jean-Paul Fournier
发明人： Pierre Roger , Patrick Choay , Claude Monneret , Jean-Paul Fournier
IPC分类号： C07C271/06 , C07H13/12
CPC分类号： C07H13/12 , C07C271/06 , Y10S514/908
摘要： The invention relates to nitrosourea derivatives, a process for their preparation and pharmaceutical compositions containing them.The nitrosourea derivatives of the invention correspond to the following formula (I): ##STR1## in which: R can represent a hydrogen atom or an alkyl group from 1 to 30 carbon atoms, X represents a hydroxy group or an -NR.sub.1 R.sub.2 group, Y represents a hydrogen atom, a hydroxy group or an -NR'.sub.1 R'.sub.2 group, where R.sub.1 and/or R'.sub.1 each represent a hydrogen atom or a ##STR2## group, Hal being a halogen, and R.sub.2 and/or R'.sub.2 can each represent a hydrogen atom or an alkyl group comprising from 1 to 6 carbon atoms, R' and R" can represent hydrogen or OH, provided that at least X represents ##STR3## with R.sub.1 representing ##STR4## or Y represents ##STR5## with R'.sub.1 representing ##STR6## and provided that either R' represents hydrogen or R" represents hydrogen, and R' and R" cannot be simultaneously hydrogen atoms.These compounds present an antitumor activity.

2. 发明授权

US4585769A Benzenesulfonyl-lactams and their use as active substances of pharmaceutical compositions 失效
标题翻译：苯磺酰基内酰胺及其作为药物组合物的活性物质的用途
公开(公告)号：US4585769A
公开(公告)日：1986-04-29
申请号：US662187
申请日：1984-10-18
申请人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
发明人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
IPC分类号： A61K31/40 , A61P25/00 , C07D207/48 , C07D211/96 , C07D223/10 , A61K31/55 , C07D209/32 , C07D211/40
CPC分类号： C07D223/10 , C07D207/48 , C07D211/96
摘要： The invention relates to new benzenesulfonyl-lactams, process for their preparation and their use as active substance in pharmaceutical compositions.Compounds according to the invention correspond to the general formula (I): ##STR1## in which: X can represent hydrogen,Y can represent the CF.sub.3 group,Z can represent chlorine,W can represent hydrogen,n is 1, 2 or 3,R.sub.1 can represent hydrogen,R.sub.2 can represent the OH group, provided that when n is 2 or 3, X or Z represents an alkoxy group from 1 to 4 carbon atoms or that Y represents the CF.sub.3 or NO.sub.2 group, and when n is 1, Y or W represents the CF.sub.3 group.These new compounds may be introduced as active substances, particularly in the treatment of disorders of the memory.
摘要翻译：本发明涉及新的苯磺酰基内酰胺，其制备方法及其作为药物组合物中活性物质的用途。根据本发明的化合物对应于通式（I）：其中：X可以表示氢，Y可以表示CF 3基团，Z可以表示氯，W可以表示氢，n是1,2 或3，R 1可以表示氢，R 2可以表示OH基团，条件是当n为2或3时，X或Z表示1至4个碳原子的烷氧基或Y表示CF 3或NO 2基团，并且当n 是1，Y或W表示CF 3基团。这些新化合物可以作为活性物质引入，特别是用于治疗记忆障碍。

3. 发明授权

US4760062A Pharmaceutical compositions of N-heterocyclic benzenesulfonamides and their use 失效
标题翻译： N-杂环苯磺酰胺的药物组合物及其用途
公开(公告)号：US4760062A
公开(公告)日：1988-07-26
申请号：US662178
申请日：1984-10-18
申请人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
发明人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
IPC分类号： A61K31/395 , A61K31/443 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P25/20 , C07D243/00 , C07D243/08 , C07D295/22 , C07D295/26 , C07D307/68 , C07D405/06
CPC分类号： C07D295/26 , C07C309/00 , C07D243/08 , C07D405/06
摘要： The invention relates to new N-cyclic benzenesulfonamides, their process of preparation and their use as active substance of pharmaceutical compositions. The new benzenesulfonamides according to the invention correspond to the following general formula (I): ##STR1## in which: V represents, for example, hydrogen,W represents, for example CF.sub.3,X represents, for example, hydrogen,Y represents, for example, hydrogen,n is 2 or 3,Z represents, for example, the group NR.sub.4, in which R.sub.4 represents, for example, hydrogen.These compounds are useful in pharmaceutical compositions for the treatment of nervous disorders with anxiety.
摘要翻译：本发明涉及新的N-环苯磺酰胺，其制备方法及其作为药物组合物的活性物质的用途。根据本发明的新型苯磺酰胺对应于以下通式（I）：其中：V表示例如氢，W表示例如CF 3，X表示例如氢，Y 表示例如氢，n为2或3，Z表示例如NR4基团，其中R4表示例如氢。这些化合物可用于用焦虑治疗神经障碍的药物组合物中。

4. 发明授权

US4714700A N-substituted 2,4-dialkoxy benzenesulfonamides and pharmaceutical compositions 失效
标题翻译： N-取代的2,4-二烷氧基苯磺酰胺和药物组合物
公开(公告)号：US4714700A
公开(公告)日：1987-12-22
申请号：US700478
申请日：1985-02-12
申请人： Jean-Paul Fournier , Patrick Choay
发明人： Jean-Paul Fournier , Patrick Choay
IPC分类号： C07D295/13 , A61K31/435 , A61K31/535 , C07D295/12
CPC分类号： C07D295/13
摘要： The invention relates to new N-substituted benzenesulfonamides, the process for their preparation and their use.The compounds according to the invention correspond to the general formula (I): ##STR1## in which: n and m have values from 0 to 4;R.sub.3 and R.sub.4 represent in particular a lower alkyl radical;R.sub.1 and R.sub.2 represent in particular hydrogen atoms, linear or branched alkyl groups having from 1 to 4 carbon atoms;R.sub.5 represents particularly a hydrogen atom, a halogen, the NO.sub.2, NH.sub.2, or CF.sub.3 group;R.sub.6 and R.sub.7 represent in particular a hydrogen atom, an alkyl radical of 1 to 6 carbon atoms.The invention is useful in the preparation of tranquilizing or anxiolytic medicines.
摘要翻译：本发明涉及新的N-取代苯磺酰胺，其制备方法及其应用。根据本发明的化合物对应于通式（I）：其中：n和m具有0至4的数值; R3和R4特别表示低级烷基; R1和R2特别表示氢原子，具有1至4个碳原子的直链或支链烷基; R5特别表示氢原子，卤素，NO2，NH2或CF3基团; R6和R7特别表示氢原子，1〜6个碳原子的烷基。本发明可用于镇静或抗焦虑药物的制备。

5. 发明授权

US4225611A Novel n-substituted benzenesulfonamide, process for its preparation and medicaments containing it 失效
标题翻译：新型正取代苯磺酰胺，其制备方法和含有它的药物
公开(公告)号：US4225611A
公开(公告)日：1980-09-30
申请号：US893250
申请日：1978-04-05
申请人： Jean-Paul Fournier , Patrick Choay
发明人： Jean-Paul Fournier , Patrick Choay
IPC分类号： A61K31/40 , A61P1/00 , C07C205/26 , C07C205/37 , C07D207/08 , C07D207/09
CPC分类号： C07D207/09 , C07C205/26 , C07C205/37 , C07C309/00 , Y10S514/926
摘要： Amino-4 chloro-5 methoxy-2 N-(N-ethyl methyl-2 pyrrolidino) benzenesulfonamide is a novel compound corresponding to the formula ##STR1## and is prepared by reacting sulfonyl chloride of the formula ##STR2## with the amine of the formula ##STR3## This compound and its addition salts with physiologically acceptable mineral or organic acids, is a useful medicament for the treatment of ulcerous gastro-duodenal disorders.
摘要翻译：氨基-4-氯-5甲氧基-2N-（N-乙基甲基-2-吡咯烷子基）苯磺酰胺是对应于式“IMAGE”的新型化合物，其通过将式“IMAGE”的磺酰氯与该化合物及其与生理上可接受的矿物质或有机酸的加成盐是治疗溃疡性胃十二指肠疾病的有用药物。

6. 发明授权

US4457875A Substituted 2,4 dialkoxy benzene sulfonyl chlorides 失效
标题翻译：取代2,4-二烷氧基苯磺酰氯
公开(公告)号：US4457875A
公开(公告)日：1984-07-03
申请号：US371451
申请日：1982-04-23
申请人： Jean-Paul Fournier , Patrick Choay
发明人： Jean-Paul Fournier , Patrick Choay
IPC分类号： C07D295/12 , A61K31/10 , A61K31/445 , A61P25/20 , C07C20060101 , C07C67/00 , C07C301/00 , C07C303/02 , C07C303/08 , C07C303/10 , C07C303/32 , C07C303/38 , C07C309/86 , C07C309/87 , C07C311/29 , C07C317/14 , C07D207/04 , C07D207/06 , C07D207/30 , C07D211/14 , C07D295/00 , C07C147/06
CPC分类号： C07C317/00 , C07C309/00
摘要： The invention relates to trisubstituted sulfohalides, the process for their preparation and their use as intermediate products for the manufacture of novel compounds. The trisubstituted sulfohalides according to the invention correspond to the following general formula (I): ##STR1## in which: X is a halogen atom, particularly bromine or preferably chlorine;R.sub.3 and R.sub.4 each represent, independently of one another, a lower alkyl radical having from 1 to 4 carbon atoms, A represents hydrogen, halogen, alkoxy radicals having from 1 to 4 carbon atoms, alkylsulfonyl groups having from 1 to 4 carbon atoms, or the group NO.sub.2, or CF.sub.3. The invention is useful in the manufacture of medicaments.
摘要翻译：本发明涉及三取代磺酰卤，其制备方法及其作为制备新化合物的中间产物的用途。根据本发明的三取代磺酰卤对应于以下通式（I）：其中：X是卤素原子，特别是溴或优选氯; R 3和R 4各自独立地表示具有1至4个碳原子的低级烷基，A表示氢，卤素，具有1至4个碳原子的烷氧基，具有1至4个碳原子的烷基磺酰基，或组NO2或CF3。本发明在制备药物中是有用的。

7. 发明授权

US4902791A Nitrosourea derivatives, process for their preparation and medicaments containing them 失效
标题翻译：亚硝基脲衍生物，其制备方法和含有它们的药物
公开(公告)号：US4902791A
公开(公告)日：1990-02-20
申请号：US181760
申请日：1988-04-14
申请人： Pierre Roger , Patrick Choay , Claude Monneret , Jean-Paul Fournier , Alain Martin
发明人： Pierre Roger , Patrick Choay , Claude Monneret , Jean-Paul Fournier , Alain Martin
IPC分类号： C07C271/06 , C07H13/12
CPC分类号： C07H13/12 , C07C271/06 , Y10S514/908
摘要： The invention relates to nitrosourea derivatives, a process for their preparation and pharmaceutical compositions containing them.The nitrosourea derivatives of the invention correspond to the following formula (I): ##STR1## in which: R can represent a hydrogen atom or an alkyl group from 1 to 30 carbon atoms, X represents a hydroxy group or an --NR.sub.1 R.sub.2 group, Y represents a hydrogen atom, a hydroxy group or an --NR'.sub.1 R'.sub.2 group, where R.sub.1 and/or R'.sub.1 each represent a hydrogen atom or a ##STR2## group, Hal being a halogen, and R.sub.2 and/or R'.sub.2 can each represent a hydrogen atom or an alkyl group comprising from 1 to 6 carbon atoms, R' and R" can represent hydrogen or OH, provided that at least X represents ##STR3## with R.sub.1 representing ##STR4## or Y represents ##STR5## with R'.sub.1 representing ##STR6## and provided that either R' represents hydrogen or R" represents hydrogen, and R' and R" cannot be simultaneously hydrogen atoms.These compounds present an antitumor activity. No drawing.
摘要翻译：本发明涉及亚硝基脲衍生物，其制备方法和含有它们的药物组合物。本发明的亚硝基脲衍生物对应于下式（I）：其中：R可以表示氢原子或1〜30个碳原子的烷基，X表示羟基或-NR1R2基，Y表示表示氢原子，羟基或-NR'1R'2基团，其中R1和/或R'1各自表示氢原子或基团，Hal表示卤素，R2和/或R' 2可以各自表示氢原子或含有1至6个碳原子的烷基，R'和R“可以表示氢或OH，条件是至少X表示，其中R1表示或Y表示< IMAGE>，其中R'1表示，并且条件是R'表示氢或R“表示氢，并且R'和R”不能同时为氢原子。这些化合物具有抗肿瘤活性。没画

8. 发明授权

US4871843A Cyclic benzenesulfonamides, process for their preparation and their use as active substance of pharmaceutical compositions 失效
标题翻译：环状苯磺酰胺，其制备方法及其作为药物组合物的活性物质的用途
公开(公告)号：US4871843A
公开(公告)日：1989-10-03
申请号：US224549
申请日：1985-07-26
申请人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
发明人： Pierre Roger , Patrick Choay , Jean-Paul Fournier
IPC分类号： C07D243/08 , C07D295/22 , C07D295/26 , C07D405/06
CPC分类号： C07D295/26 , C07C309/00 , C07D243/08 , C07D405/06
摘要： The invention relates to new N-cyclic benzenesulfonamides, their process of preparation and their use as active substance of pharmaceutical compositions. The new benzenesulfonamides according to the invention correspond to the following general formula (I): ##STR1## in which: V represents, for example, hydrogen,W represents, for example CF.sub.3,X represents, for example, hydrogen,Y represents, for example, hydrogen,n is 2 or 3,Z represents, for example, the group NR.sub.4, in which R.sub.4 represents, for example, hydrogen.These compounds are useful in pharmaceutical compositions for the treatment of nervous disorders with anxiety.
摘要翻译：本发明涉及新的N-环苯磺酰胺，其制备方法及其作为药物组合物的活性物质的用途。根据本发明的新型苯磺酰胺对应于以下通式（I）：其中：V表示例如氢，W表示例如CF 3，X表示例如氢，Y 表示例如氢，n为2或3，Z表示例如NR4基团，其中R4表示例如氢。这些化合物可用于用焦虑治疗神经障碍的药物组合物中。

9. 发明授权

US4618459A Substituted 2,4-dialkoxy benzene sulfonyl chlorides 失效
标题翻译：取代的2,4-二烷氧基苯磺酰氯
公开(公告)号：US4618459A
公开(公告)日：1986-10-21
申请号：US567161
申请日：1983-12-30
申请人： Jean-Paul Fournier , Patrick Choay
发明人： Jean-Paul Fournier , Patrick Choay
IPC分类号： C07D295/12 , A61K31/10 , A61K31/445 , A61P25/20 , C07C20060101 , C07C67/00 , C07C301/00 , C07C303/02 , C07C303/08 , C07C303/10 , C07C303/32 , C07C303/38 , C07C309/86 , C07C309/87 , C07C311/29 , C07C317/14 , C07D207/04 , C07D207/06 , C07D207/30 , C07D211/14 , C07D295/00 , C07C143/70 , C07C147/06
CPC分类号： C07C317/00 , C07C309/00
摘要： The invention relates to trisubstituted sulfohalides, the process for their preparation and their use as intermediate products for the manufacture of novel compounds.The trisubstituted sulfohalides according to the invention correspond to the following general formula (I): ##STR1## in which: X is a halogen atom, particularly bromine or preferably chlorine;R.sub.3 and R.sub.4 each represent, independently of one another, a lower alkyl radical having from 1 to 4 carbon atoms, A represents hydrogen, halogen, alkoxy radicals having from 1 to 4 carbon atoms, alkylsulfonyl groups having from 1 to 4 carbon atoms, or the group NO.sub.2, or CF.sub.3.The invention is useful in the manufacture of medicaments.
摘要翻译：本发明涉及三取代磺酰卤，其制备方法及其作为制备新化合物的中间产物的用途。根据本发明的三取代磺酰卤对应于以下通式（I）：其中：X是卤素原子，特别是溴或优选氯; R 3和R 4各自独立地表示具有1至4个碳原子的低级烷基，A表示氢，卤素，具有1至4个碳原子的烷氧基，具有1至4个碳原子的烷基磺酰基，或组NO2或CF3。本发明在制备药物中是有用的。

10. 发明授权

US4211776A N-Substituted 2-methoxybenzenesulphonamides, process for preparing them and medicaments containing them 失效
标题翻译： N-取代的2-甲氧基苯磺酰胺，其制备方法和含有它们的药物
公开(公告)号：US4211776A
公开(公告)日：1980-07-08
申请号：US947623
申请日：1978-10-02
申请人： Robert C. Moreau , Jean-Paul Fournier
发明人： Robert C. Moreau , Jean-Paul Fournier
IPC分类号： C07C205/26 , C07D295/12 , C07D295/13 , A61K31/32 , A61K31/40 , C07D207/00 , C07D209/00
CPC分类号： C07D295/13 , C07C205/26 , C07C309/00
摘要： The invention relates to new N-substituted benzenesulphonamides of general formula ##STR1## in which n is 2 or 3,R.sub.1 and R.sub.2 are hydrogen atoms, methyl, ethyl groups, or jointly form with the nitrogen a nitrogenized heterocyclic ring having 5 or 6 members, in particular a piperidino, pyrrolidino or morpholino group.R.sub.3 is a hydrogen atom, an NO.sub.2 group, an NH.sub.2 group, or a halogen,R.sub.4 is a hydrogen, a halogen, NH.sub.2 group or a sulphonamide group.These compounds are useful as active substances of medicaments, in particular as antiemetic.
摘要翻译：本发明涉及通式为“IMAGE”的新的N-取代苯磺酰胺，其中n为2或3，R 1和R 2为氢原子，甲基，乙基或与氮一起形成具有5或6个成员的氮杂环，特别是哌啶子基，吡咯烷子基或吗啉代基团。 R3是氢原子，NO2基，NH2基或卤素，R4是氢，卤素，NH2基或磺酰胺基。这些化合物可用作药物的活性物质，特别是作为止吐剂。

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