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1. 发明授权

US4910196A Highly soluble antibacterially active organic salts of pyridobenzothiazines 失效
标题翻译：吡啶并苯并噻嗪的高溶性抗菌活性有机盐
公开(公告)号：US4910196A
公开(公告)日：1990-03-20
申请号：US64460
申请日：1987-06-22
申请人： Patrizia Terni , Pier L. Rugarli , Stefano Maiorana , Pier G. Pagella , Raffaello Fusco
发明人： Patrizia Terni , Pier L. Rugarli , Stefano Maiorana , Pier G. Pagella , Raffaello Fusco
IPC分类号： A61K31/54 , A61P31/04 , C07D513/06
CPC分类号： C07D513/06
摘要： New highly soluble antibacterially active salts of pyridobenzothiazines with organic acids are described.In particular, organic salts of 9-fluoro-10[N-(4'-methyl)piperazinyl]-7-oxo-2,3-dihydro-7H-pyrido[1,2,3][1,4]-benzothiazine-6-carboxylic acid are prepared with an acid chosen from the group consisting of methanesulphonic acid, ethanesulphonic acid, n-dodecanesulphonic acid, p-toluenesulphonic acid, 1-actadecanesulphonic acid, 2-chloro-ethanesulphonic acid, 2-bromo-ethanesulphonic acid, 3-hydroxy-propanesulphonic acid, citric acid, malonic acid, gluconic acid, malic acid, lactic acid and L-tartaric acid.A new process is also described for preparing said salts from 2,3,4-trichloronitrobenzene, by way of a 2-fluoro-3-chloro-4-mercapto derivative of the nitrobenzene and cyclizing the corresponding amino derivative.
摘要翻译：描述了具有有机酸的吡啶并苯并噻嗪的新的高度可溶的抗菌活性盐。特别地，9-氟-10 [N-（4'-甲基）哌嗪基] -7-氧代-2,3-二氢-7H-吡啶并[1,2,3] [1,4] - 苯并噻嗪的有机盐 -6-甲酸用选自甲磺酸，乙磺酸，正十二烷磺酸，对甲苯磺酸，1-十八烷磺酸，2-氯 - 乙磺酸，2-溴 - 乙磺酸，，3-羟基 - 丙磺酸，柠檬酸，丙二酸，葡萄糖酸，苹果酸，乳酸和L-酒石酸。还描述了通过硝基苯的2-氟-3-氯-4-巯基衍生物从2,3,4-三氯硝基苯制备所述盐的新方法，并使相应的氨基衍生物环化。

2. 发明授权

US4923859A Pyrido-benzothiazine derivatives having high antibacterial activity and high bioavailability to tissues 失效
标题翻译：吡啶并苯并噻嗪衍生物对组织具有高抗菌活性和高生物利用度
公开(公告)号：US4923859A
公开(公告)日：1990-05-08
申请号：US251457
申请日：1988-09-30
申请人： Patrizia Terni , Stefano Maiorana , Antonio Papagni , Piergiuseppe Pagella
发明人： Patrizia Terni , Stefano Maiorana , Antonio Papagni , Piergiuseppe Pagella
IPC分类号： A61K31/54 , A61P31/04 , C07D513/06
CPC分类号： C07D513/06
摘要： Pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a S.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form.The invention also comprises the process for the preparation of derivatives of formula (I) starting from 2.4-difluoro-3-chloronitrobenzene.Said derivatives possess a high antibacterial acitvity as well as a high bioavailability to tissues; the invention also refers to pharmaceutical compositions containing them as active components.

3. 发明授权

US5066802A Process for preparing pyrido-benzothiazine derivatives having high antibacterial activity and high bioavailability to tissues 失效
标题翻译：制备具有高抗细菌活性和高组织生物可利用性的吡咯并苯并噻嗪衍生物的方法
公开(公告)号：US5066802A
公开(公告)日：1991-11-19
申请号：US447406
申请日：1989-12-07
申请人： Patrizia Terni , Stefano Maiorana , Antonio Papagni , Piergiuseppe Pagella
发明人： Patrizia Terni , Stefano Maiorana , Antonio Papagni , Piergiuseppe Pagella
IPC分类号： A61K31/54 , A61P31/04 , C07D513/06
CPC分类号： C07D513/06
摘要： A process for preparing pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a C.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form. The process for the preparation of derivatives of formula (I) starts with a first reaction cycle starting from 2,4-difluoro-3-chloronitrobenzene. Said derivatives possess a high antibacterial activity as well as a high bioavailability to tissues. The invention also refers to pharmaceutical compositions containing them as active components.

4. 发明授权

US5869484A Phenylcarbamate derivatives suitable to the use as anticholinesterase substances 失效
标题翻译：苯基氨基甲酸酯衍生物适合用作抗胆碱酯酶物质
公开(公告)号：US5869484A
公开(公告)日：1999-02-09
申请号：US776052
申请日：1997-01-17
申请人： Patrizia Terni , Lucia Mairani , Giacomina Mandelli , Pier Giuseppe Pagella , Donata Marchesini , Stefano Maiorana , Mario Brufani
发明人： Patrizia Terni , Lucia Mairani , Giacomina Mandelli , Pier Giuseppe Pagella , Donata Marchesini , Stefano Maiorana , Mario Brufani
IPC分类号： C07C271/44 , C07C271/56 , C07C271/58 , C07D239/95 , C07D295/13 , C07D295/185 , C07D491/113 , A61K31/535 , C07D265/30 , C07D265/32 , C07D413/00
CPC分类号： C07D295/185 , C07C271/44 , C07C271/56 , C07C271/58 , C07D239/95 , C07D295/13 , C07C2101/14
摘要： Phenylcarbamate derivatives suitable to the use as anticholinesterase substances having the general formula (I) ##STR1## wherein the meaning of R.sub.1 -R.sub.7 and X substituentes together with n will be defined in the text.
摘要翻译： PCT No.PCT / EP95 / 02752 Sec。 371日期1997年1月17日 102（e）日期1997年1月17日PCT提交1995年7月13日PCT公布。公开号WO96 / 02524 日期：1996年2月1日适用于具有通式（I）的抗胆碱酯酶物质的苯基氨基甲酸酯衍生物，其中R1和R7的取代基与n的含义将在文中定义。

5. 发明授权

US4868299A Antibacterially active pyrido-benzothiazine derivatives with long-term action 失效
标题翻译：具有长期作用的抗菌活性吡啶并苯并噻嗪衍生物
公开(公告)号：US4868299A
公开(公告)日：1989-09-19
申请号：US106665
申请日：1987-10-13
申请人： Arnaldo Fravolini , Patrizia Terni , Piergiuseppe Pagella
发明人： Arnaldo Fravolini , Patrizia Terni , Piergiuseppe Pagella
IPC分类号： C07D513/06
CPC分类号： C07D513/06
摘要： The invention relates to antibacterially active pyrido-benzothiazine derivatives with long-term action, having the following general formula: ##STR1## in which R is ##STR2## Where R.sup.1 is H, C.sub.1 -C.sub.6 alkyl, p-fluorophenyl, m-fluorophenyl, o-fluorophenyl or 2-pyridyl; or ##STR3## where R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are lower alkyls. The invention also comprises the process for preparing compounds of general formula (I). Said process consists of a synthesis cycle using 2,4-difluoro-3-chloronitrobenzene and thiolactic acid as starting substances.The inventiona also comprises pharmaceutical compositions containing at least one of the compounds of general formula (I) as active principle.

6. 发明授权

US4668784A Derivatives of pyrido-benzothiazine with high anti-microbial activity 失效
标题翻译：具有高抗微生物活性的吡啶并苯并噻嗪的衍生物
公开(公告)号：US4668784A
公开(公告)日：1987-05-26
申请号：US765154
申请日：1985-08-13
申请人： Giuseppe Mascellani , Arnaldo Fravolini , Patrizia Terni
发明人： Giuseppe Mascellani , Arnaldo Fravolini , Patrizia Terni
IPC分类号： A61K31/54 , A61P31/04 , C07D277/82 , C07D279/16 , C07D513/06 , C07D513/04
CPC分类号： C07D513/06 , C07D277/82 , C07D279/16
摘要： Pyrido-benzothiazine compounds having anti-microbial activity are prepared by (a) reacting 3-chloro-4-fluoroaniline with potassium thiocyanate and bromine to produce 2-amino-6-fluoro-7-chlorobenzothiazole, (b) reacting 2-amino-6-fluoro-7-chlorobenzothiazole with sodium hydroxide to produce the disulfide of 2-amino-5-fluoro 6-chlorothiophenol, (c) reacting the disulfide with sodium monochloroacetate to produce 7-fluoro-8-chloro-2H-1,4-benzothiazin-3(4H)-one, (d) reducing 7-fluoro-8-chloro-2H-1,4-benzothiazin-3(4H)-one to produce 7-fluoro-8-chloro-3,4-dihydro-2H-1,4-benzothiazone, (e) reacting 7-fluoro-8-chloro-3,4-dihydro-2-H-1,4-benzothiazone with ethyl ethoxymethylenemalonate and cyclyzing the intermediate formed with polyphosphoric acid to produce ethyl 9-fluoro-10-chloro-7-oxo-2,3-dihydro-7H-pyrido[1,2,3 de] [1,4]-benzothiazine-6-carboxylate and (f) hydrolyizing the ethyl carboxylate to produce the corresponding carboxylic acid.
摘要翻译：通过（a）使3-氯-4-氟苯胺与硫氰酸钾和溴反应制备2-氨基-6-氟-7-氯苯并噻唑，（b）使2-氨基-6-氟-7-氯苯并噻唑反应，制备具有抗微生物活性的吡啶并苯并噻嗪化合物， 6-氟-7-氯苯并噻唑与氢氧化钠反应，得到2-氨基-5-氟-6-氯苯硫酚的二硫化物，（c）使二硫化物与一氯乙酸钠反应，生成7-氟-8-氯-2H-1,4 - 苯并噻嗪-3（4H） - 酮，（d）还原7-氟-8-氯-2H-1,4-苯并噻嗪-3（4H） - 酮，得到7-氟-8-氯-3,4- （e）使7-氟-8-氯-3,4-二氢-2H-1,4-苯并噻唑与乙氧基亚甲基丙二酸乙酯反应，并循环形成多磷酸的中间产物乙基9-氟-10-氯-7-氧代-2,3-二氢-7H-吡啶并[1,2,3-de] [1,4] - 苯并噻嗪-6-羧酸乙酯和（f）将羧酸乙酯水解成产生相应的羧酸。

7. 发明授权

US4684647A Anti-bacterial pyrido-benzothiazine derivative and pharmaceutical composition therefor 失效
标题翻译：抗菌吡啶并苯并噻嗪衍生物及其药物组合物
公开(公告)号：US4684647A
公开(公告)日：1987-08-04
申请号：US922712
申请日：1986-10-24
申请人： Giuseppe Mascellani , Arnaldo Fravolini , Patrizia Terni
发明人： Giuseppe Mascellani , Arnaldo Fravolini , Patrizia Terni
IPC分类号： A61K31/54 , A61P31/04 , C07D277/82 , C07D279/16 , C07D513/06 , A01N43/60 , A61K31/495 , C07D513/16
CPC分类号： C07D513/06 , C07D277/82 , C07D279/16
摘要： A new class of antimicrobial pyrido-benzothiazine compounds and processes for their preparation are described. The compounds have the general formula: ##STR1##

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