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1. 发明授权

US4071531A Oxathiino- and dithiino-aminoacetic acids 失效
标题翻译：氧硫基和二硫氨基乙酸
公开(公告)号：US4071531A
公开(公告)日：1978-01-31
申请号：US616991
申请日：1975-09-26
申请人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
发明人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
IPC分类号： C07D327/06 , C07D339/08 , C07D501/20 , C12P17/14 , C07D501/60 , A61K31/54
CPC分类号： C07D339/08 , C07D327/06 , C12P17/14
摘要： New oxathiino- and dithiino-aminoacetic acids of the formula: ##STR1## in which A represents oxygen or sulphur, together with their racemic forms, their optically active forms and mixtures thereof, their reactive derivatives and their acid addition salts, are valuable intermediates for the preparation of therapeutically active derivatives, in particular cephalosporin derivatives of the formula: ##STR2## where R is hydrogen or acetoxy.
摘要翻译：其中A代表氧或硫，其外消旋形式，它们的光学活性形式及其混合物，它们的反应性衍生物和它们的酸加成盐的新的氧亚硫基和二硫氨基 - 氨基乙酸是其中A代表氧或硫的有价值的中间体治疗活性衍生物，特别是下式的头孢菌素衍生物的制备：其中R是氢或乙酰氧基。

2. 发明授权

US4034090A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4034090A
公开(公告)日：1977-07-05
申请号：US592096
申请日：1975-06-30
申请人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
发明人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
IPC分类号： C07D501/06 , A61K31/546 , C07D257/04 , C07D285/12 , C07D285/125 , C07D285/13 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/46 , A61K31/545
CPC分类号： C07D257/04 , C07C329/00 , C07D285/125 , C07D285/13 , C07D501/20
摘要： New cephalosporin derivatives of the formula: ##STR1## in which either (a) R.sub.1 is hydrogen, acetoxy, azido or heterocyclylthio or heterocyclylcarbonylthio which is (1,3,4-thiadiazol-2-yl)-thio which is unsubstituted or substituted by straight or branched chain C.sub.1-4 alkyl or alkoxy, straight or branched chain C.sub.1-4 alkylthio, straight or branched chain C.sub.1-4 alkylsulphonyl, amino or acetylamino; (1,2,3,4-tetrazol-5-yl)-thio which is unsubstituted or substituted in the 1-position by straight or branched chain C.sub.1-4 alkyl, hydroxy straight or branched chain C.sub.1-4 alkyl, phenyl or hydroxyphenyl, or in the 2-position by straight or branched chain C.sub.1-4 alkyl or hydroxy straight or branched chain C.sub.1-4 alkyl; (1,2,4-triazol-3-yl)-thio, (4-methyl-1,3-thiazol-2-yl)-thio, (3-methyl-1,2,4-thiadiazol-5-yl)-thio or (1,2,3-thiadiazol-4-yl)-carbonylthio, and R.sub.2 is carboxy or a radical of the formula: ##STR2## in which the radical: ##STR3## is a radical which can be easily removed enzymatically, and in which R.sub.3 is hydrogen or straight or branched chain C.sub.1-4 alkyl and R.sub.4 is straight or branched chain C.sub.1-4 alkyl or cyclohexyl; or (b) R.sub.1 is a pyridinio ion and R.sub.2 is a carboxylato ion, and pharmaceutically acceptable non-toxic metal salts thereof and addition salts thereof with nitrogen containing bases possess valuable anti-bacterial properties, showing activity against both Gram-positive and Gram-negative bacteria.
摘要翻译：下式的新型头孢菌素衍生物：其中（a）R 1是氢，乙酰氧基，叠氮基或杂环基硫基或杂环基羰基硫基，其是未取代的（1,3,4-噻二唑-2-基） - 硫基直链或支链C 1-4烷基或烷氧基，直链或支链C 1-4烷硫基，直链或支链C 1-4烷基磺酰基，氨基或乙酰氨基; （1,2,3,4-四唑-5-基） - 硫基，其未被取代或在1-位被直链或支链C 1-4烷基取代，羟基直链或支链C 1-4烷基，苯基或羟基苯基或2-位的直链或支链C 1-4烷基或羟基直链或支链C 1-4烷基; （1,2,4-三唑-3-基） - 硫代，（4-甲基-1,3-噻唑-2-基） - 硫代，（3-甲基-1,2,4-噻二唑-5-基）） - 硫代或（1,2,3-噻二唑-4-基） - 羰基硫基，并且R 2是羧基或下式的基团：其中基团：（III）是其可以容易地被酶除去，其中R 3是氢或直链或支链C 1-4烷基，R 4是直链或支链C 1-4烷基或环己基; 或（b）R 1是吡啶鎓离子，R 2是羧基离子，其药学上可接受的无毒金属盐和其与含氮碱基的加成盐具有有价值的抗菌性质，显示出对革兰氏阳性和革兰氏阴性菌的活性，阴性细菌。

3. 发明授权

US4029781A 1,4-Dithiin (and oxathiin)-yl cephalosporin derivatives, and compositions containing them 失效
标题翻译： 1,4-二硫辛（和氧硫辛酸） - 基头孢菌素衍生物和含有它们的组合物
公开(公告)号：US4029781A
公开(公告)日：1977-06-14
申请号：US617066
申请日：1975-09-26
申请人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
发明人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
IPC分类号： C07D501/22 , A61K31/546 , C03C17/28 , C07D501/06 , C07D501/20 , C07D501/34 , A61K31/54
CPC分类号： C07D501/20 , C03C17/28 , Y02P20/55
摘要： New cephalosporin compounds of the formula: ##STR1## in which A is oxygen or sulphur, R.sub.1 is hydrogen or acetoxy and R.sub.2 is carboxy or a radical of the formula: ##STR2## in which the radical ##STR3## is a radical which can be easily removed enzymatically, and in which R.sub.3 is hydrogen or straight or branched chain C.sub.1-4 alkyl and R.sub.4 is straight or branched chain C.sub.1-4, alkyl or cyclohexyl, together with its diastereoisomeric forms and mixtures thereof, its acid addition salts and, where appropriate, its pharmaceutically acceptable non-toxic metal salts and addition salts with nitrogen-containing bases other than ammonia, exhibit valuable anti-bacterial properties, in particular against Gram-positive and Gram-negative bacteria.
摘要翻译：下式的新型头孢菌素化合物：其中A是氧或硫，R1是氢或乙酰氧基，R2是羧基或下式的基团：其中基团（I）（III）是可以容易地酶促去除的基团，其中R3是氢或直链或支链C1-4烷基，R4是直链或支链C1-4，烷基或环己基，以及它们的非对映异构形式和混合物其酸加成盐，并且在适当的情况下，其药学上可接受的无毒金属盐和与氨以外的含氮碱的加成盐显示出有价值的抗菌性质，特别是抗革兰氏阳性和革兰氏阴性菌。

4. 发明授权

US4007176A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4007176A
公开(公告)日：1977-02-08
申请号：US523007
申请日：1974-11-12
申请人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
发明人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
IPC分类号： C07D501/04 , A61K31/43 , A61K31/545 , A61K31/546 , C07D20060101 , C07D501/06 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/48 , C07D501/56 , C07D501/60
CPC分类号： C07D501/20
摘要： New cephalosporin derivatives of the formula: ##STR1## wherein one of A and A.sub.1 represents oxygen or sulphur and the other represents sulphur, R.sub.1 represents hydrogen, acetoxy, (5-methyl-1,3,4-thiadiazol-2-yl)thio or (1-methyl-1,2,3,4-tetrazol-5-yl)thio and R.sub.2 represents carboxy, or R.sub.1 represents a pyridinio radical and R.sub.2 represents the carboxylate ion, are therapeutically useful compounds possessing antibacterial properties.
摘要翻译：下式的新型头孢菌素衍生物：其中A和A1之一代表氧或硫，另一个代表硫，R1代表氢，乙酰氧基，（5-甲基-1,3,4-噻二唑-2-基）硫代或（1-甲基-1,2,3,4-四唑-5-基）硫基，R 2表示羧基，或R 1表示吡啶基，R 2表示羧酸根离子，是具有抗菌性质的治疗上有用的化合物。

5. 发明授权

US4034088A Cephalosporin derivatives, and compositions containing them 失效
标题翻译：头孢菌素衍生物和含有它们的组合物
公开(公告)号：US4034088A
公开(公告)日：1977-07-05
申请号：US573110
申请日：1975-04-30
申请人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
发明人： Christian Berger , Daniel Farge , Georges Gros , Mayer Naoum Messer , Claude Moutonnier
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , A61K31/546 , C07D20060101 , C07D501/04 , C07D501/16 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/26 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/60
CPC分类号： C07D501/20
摘要： New cephalosporin derivatives of the general formula: ##STR1## in which R represents a straight or branched chain C.sub.1-4 alkyl radical, or a phenyl (straight or branched chain C.sub.1-4 alkyl) radical, n is 0, 1 or 2, and either R.sub.1 is a pyridinio ion and R.sub.2 is a carboxylato ion, or R.sub.1 represents a hydrogen atom, or an acetoxy, (5-methyl-1,3,4-thiadiazol-2-yl)-thio or (1-methyl-1,2,3,4-tetrazol-5-yl)-thio radical and R.sub.2 represents a carboxy radical or a radical of the formula; ##STR2## in which the radical: ##STR3## is a radical which can be removed easily by enzymatic means and in which R.sub.3 represents a hydrogen atom or a straight or branched chain C.sub.1-4 alkyl radical, a phenyl radical or a phenyl (C.sub.1-2 alkyl) radical and R.sub.4 represents a straight or branched chain C.sub.1-4 alkyl radical, a straight or branched chain C.sub.1-4 alkoxy radical, a cyclohexyl radical, a phenyl radical or a phenyl (C.sub.1-2 alkyl) radical;With the proviso that when R is an alkyl radical and either R.sub.1 is a hydrogen atom or an acetoxy radical and R.sub.2 is a carboxy radical or R.sub.1 is a pyridinio ion and R.sub.2 is a carboxylato ion, n is 1 or 2, and metal salts thereof and addition salts thereof with nitrogen-containing bases are new compounds; they possess valuable antibacterial properties, showing activity against both Gram-positive and Gram-negative bacteria.
摘要翻译：新的头孢菌素衍生物，其通式为：其中R表示直链或支链C 1-4烷基或苯基（直链或支链C 1-4烷基）基团，n为0,1或2，以及 R1是吡啶鎓离子，R2是羧基离子，或R1代表氢原子，或乙酰氧基，（5-甲基-1,3,4-噻二唑-2-基） - 硫代或（1-甲基-1 ，2,3,4-四唑-5-基） - 硫基，R 2表示下式的羧基或基团：，其中基团：是可以通过酶学方法容易地除去的基团，其中R 3表示氢原子或直链或支链C 1-4烷基，苯基或苯基（C 1 -2烷基）基，R 4表示直链或支链C 1-4烷基，直链或支链C 1-4烷氧基，环己基，苯基或苯基（C 1-2烷基）基; 当R为烷基且R 1为氢原子或乙酰氧基且R 2为羧基或R 1为吡啶并且R 2为羧基离子时，n为1或2，其金属盐为其与含氮碱的加成盐是新化合物; 它们具有有价值的抗菌性能，显示出对革兰氏阳性菌和革兰氏阴性菌的活性。

6. 发明授权

US4508717A Cephalosporin derivatives, their preparation and compositions containing them 失效
标题翻译：头孢菌素衍生物，它们的制备和含有它们的组合物
公开(公告)号：US4508717A
公开(公告)日：1985-04-02
申请号：US522359
申请日：1983-08-11
申请人： Christian Berger , Daniel Farge , Claude Moutonnier , Jean-Francois Peyronel , Bernard Plau
发明人： Christian Berger , Daniel Farge , Claude Moutonnier , Jean-Francois Peyronel , Bernard Plau
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/24 , C07D501/36
CPC分类号： C07D501/00
摘要： Cephalosporin derivatives of the formula: ##STR1## in which A is a single bond or a radical --CH.sub.2 --, --NH-- or --NHCO--, attached to the 3-position or 4-position of the pyridinio radical, R is a methyl, carboxymethyl, carbamoylmethyl, benzyl or allyl radical, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or alternatively R.sub.a is carboxyl and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms or alkyl radicals, or together form an alkylene radical, and n equals 0 or 1, in their syn form, and also their addition salts with acids, metal salts and addition salts with nitrogen-containing bases are antibacterial agents having a broad spectrum of activity.
摘要翻译：下式的头孢菌素衍生物：其中A是单键或者连接到吡啶基的3-位或4-位的基团-CH 2 - ， - NH-或-NHCO-，R 是甲基，羧甲基，氨基甲酰基甲基，苄基或烯丙基，Ra，Rb和Rc是氢原子，或者Ra是羧基，Rb和Rc相同或不同，是氢原子或烷基，或一起形成亚烷基自由基，n等于0或1，并且它们与酸，金属盐和与含氮碱的加成盐的加成盐也是具有广谱活性的抗菌剂。

7. 发明授权

US4291032A Thiazolo(3,2-C)benzoxazine derivatives 失效
标题翻译：噻唑（3,2-C）苯并恶嗪衍生物
公开(公告)号：US4291032A
公开(公告)日：1981-09-22
申请号：US192988
申请日：1980-10-02
申请人： Christian Berger , Daniel Farge , Claude Moutonnier , Gerard Wolff
发明人： Christian Berger , Daniel Farge , Claude Moutonnier , Gerard Wolff
IPC分类号： A61K31/4188 , A61K31/535 , A61K31/5365 , A61P25/04 , A61P29/00 , C07D513/04
CPC分类号： C07D513/04
摘要： New thiazolo[3,2-c]-1,3-benzoxazine derivatives of the general formula (I), in which X is oxygen or sulfur, R.sub.1 and R.sub.2, which are identical or different, are hydrogen or halogen atoms or alkyl, alkoxy, alkylthio or trifluoromethyl radicals, in the 7-, 8-, 9- or 10-position, and R.sub.3 is a hydrogen atom or a carboxyl radical, their salts, if appropriate, their preparation and the medicaments in which they are present.These new derivatives are particularly useful as analgesic agents. ##STR1##
摘要翻译：其中X是氧或硫的通式（I）的新的噻唑并[3,2-c] -1,3-苯并恶嗪衍生物，相同或不同的R 1和R 2是氢或卤素原子或烷基，烷氧基，烷硫基或三氟甲基，在7-，8-，9-或10-位，R3是氢原子或羧基，它们的盐，如果合适，它们的制备和它们存在的药物。这些新衍生物作为止痛剂特别有用。（一）

8. 发明授权

US4178290A Dithiinoacetic acid and its preparation 失效
标题翻译：二硫乙酸及其制备方法
公开(公告)号：US4178290A
公开(公告)日：1979-12-11
申请号：US913088
申请日：1978-06-06
申请人： Christian Berger , Dominique Deprez , Daniel Farge , Claude Moutonnier , Gerard Wolff
发明人： Christian Berger , Dominique Deprez , Daniel Farge , Claude Moutonnier , Gerard Wolff
IPC分类号： C07D339/08 , C07D498/10 , C07D501/22
CPC分类号： C07D339/08
摘要： .alpha.-Amino(1,3-dithiin-5-yl)-acetic acid in the D-, L-, or D,L-form and in which the amino radical is free or protected by tert.-butoxycarbonyl or 2,2,2-trichloroethoxycarbonyl is a useful intermediate in the preparation of cephalosporins having valuable antibacterial activity.
摘要翻译： D-，L-或D，L-型的α-氨基（1,3-二噻吩-5-基） - 乙酸，其中氨基自由或被叔丁氧羰基或2,2 ，2-三氯乙氧基羰基是制备具有有价值的抗菌活性的头孢菌素的有用中间体。

9. 发明授权

US4520193A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4520193A
公开(公告)日：1985-05-28
申请号：US322961
申请日：1981-11-19
申请人： Christian Berger , Daniel Farge , Claude Moutonnier , Gerard Wolff
发明人： Christian Berger , Daniel Farge , Claude Moutonnier , Gerard Wolff
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/24 , C07D501/38
CPC分类号： C07D501/24
摘要： The invention provides new cephalosporin derivatives of the general formula, ##STR1## which are in the form of a bicyclooct-2-ene or bicyclooct-3-ene, in which formula R.sub.1 is a radical of the general formula ##STR2## [in which R.sub.5 is hydrogen, alkyl, vinyl, cyanomethyl, protected carboxyalkyl or a protective radical and R.sub.6 is a protective radical] or an amino-protecting radical, R.sub.2 is an acid-protecting radical and R.degree. represents various organic radicals, or alternatively R.sub.1 is an amino-protecting radical or various acyl radicals, R.sub.2 is a protective radical and R.degree. represents various organic radicals, and R.sub.3 and R.sub.4 are alkyl radicals optionally substituted by alkoxy or dialkylamino, or phenyl radicals, or --NR.sub.3 R.sub.4 forms a heterocyclic ring. These products are intermediates for the synthesis of cephalosporins having antibacterial activity.
摘要翻译：本发明提供了通式为（IMA）（I）的新型头孢菌素衍生物，其为双环-2-烯或双环辛-3-烯的形式，其中式R1为通式为“IMAGE” （II）[其中R5为氢，烷基，乙烯基，氰基甲基，被保护的羧基烷基或保护基，R6为保护基]或氨基保护基，R2为酸保护基，R DEG为各种有机基团或者R 1为氨基保护基或各种酰基，R 2为保护基，R≠表示各种有机基团，R 3和R 4为任选被烷氧基或二烷基氨基取代的烷基或苯基或-NR 3 R 4形式杂环。这些产品是合成具有抗菌活性的头孢菌素的中间体。

10. 发明授权

US4088761A 3-[(1,3-Dithiin-5-yl)-acetamido]-cephalosporins and antibacterial compositions containing them 失效
标题翻译： 3- {8（1,3-二噻吩-5-基） - 乙酰胺基{9-头孢菌素和含有它们的抗菌组合物
公开(公告)号：US4088761A
公开(公告)日：1978-05-09
申请号：US759906
申请日：1977-01-17
申请人： Christian Berger , Daniel Farge , Claude Moutonnier
发明人： Christian Berger , Daniel Farge , Claude Moutonnier
IPC分类号： C07D501/34 , A61K31/545 , A61K31/546 , A61P31/04 , C07D339/08 , C07D501/24 , C07D501/36
CPC分类号： C07D339/08 , Y02P20/55
摘要： The invention provides novel cephalosporins of the formula: ##STR1## in which R.sub.1 represents acetoxy, (5-methyl-1,3,4-thiadiazol-2-yl)-thio, (1-methyl-tetrazol-5-yl)-thio or [1-(2-hydroxyethyl)-tetrazol-5-yl]-thio and R.sub.2 represents carboxyl, or R.sub.1 represents pyridinio and R.sub.2 the carboxylato ion, and, when R.sub.2 represents carboxyl, their metal salts and addition salts with nitrogen-containing bases, which have useful antibacterial properties.
摘要翻译：本发明提供下式的新型头孢菌素：其中R1代表乙酰氧基，（5-甲基-1,3,4-噻二唑-2-基） - 硫代，（1-甲基 - 四唑-5-基） - 硫代或[1-（2-羟乙基） - 四唑-5-基] - 硫代，R 2表示羧基，或R 1表示吡啶并且R 2表示羧基离子，当R 2表示羧基时，其金属盐与氮 - 含有碱，具有有用的抗菌性能。

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