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1. 发明授权

US4288364A Fragmentation procedure for preparing 3-amino-azetidinones 失效
标题翻译：制备3-氨基 - 氮杂环丁酮的分段方法
公开(公告)号：US4288364A
公开(公告)日：1981-09-08
申请号：US39239
申请日：1979-05-15
申请人： Karl Schaffner , Hansuli Wehrli , Beat Muller , Riccardo Scartazzini
发明人： Karl Schaffner , Hansuli Wehrli , Beat Muller , Riccardo Scartazzini
IPC分类号： C07D205/085 , C07D205/08 , C07D403/06
CPC分类号： C07D205/085
摘要： When 3-(2-hydroxyiminoacetylamino)-2-oxo-azetidine compounds are treated with reactive derivatives of carbonic acid half-esters in aqueous media in the presence of bases a fragmentation takes place which, in addition to 3-amino-2-oxo-azetidines, also yields nitriles which, compared with the 2-hydroxyiminoacetyl group, have one less carbon atom. The resulting products are intermediates for the preparation of nocardicin-like antibiotics.The deacylation procedure of this specification offers advantages over the multi-stage deacylation procedure known hitherto, inasmuch as higher yields of 3-amino-2-oxoazetidine compounds are obtained and the acyl group can be obtained in the form of a nitrile which is shorter by one carbon atom.
摘要翻译：当在碱存在下，在含水介质中用3-羧酸半酯的活性衍生物处理3-（2-羟基亚氨基乙酰基氨基）-2-氧代 - 氮杂环丁烷化合物时，进行断裂，除3-氨基-2-氧代 - 氮杂环丁烷也产生与2-羟基亚氨基乙酰基相比少一个碳原子的腈。所得产物是用于制备心肌素样抗生素的中间体。本说明书的脱酰基化方法优于迄今为止已知的多级脱酰作用方法，因为得到3-氨基-2-氧代氮杂环丁烷化合物的较高产率，酰基可以以腈的形式获得，腈的形式较短一个碳原子

2. 发明授权

US4464366A Cephem compounds having a terminal aminocarboxylic acid grouping and containing an azacyclyl(thio)ureido group 失效
标题翻译：具有末端氨基羧酸基并含有氮杂环酰基（硫代）脲基的头孢烯化合物
公开(公告)号：US4464366A
公开(公告)日：1984-08-07
申请号：US214155
申请日：1980-12-08
申请人： Hansuli Wehrli , Karoly Kocsis , Riccardo Scartazzini
发明人： Hansuli Wehrli , Karoly Kocsis , Riccardo Scartazzini
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D233/38 , C07D317/28 , C07D501/20 , C07D501/57 , C07D501/59 , C07D501/36
CPC分类号： C07D233/38 , C07D317/28
摘要： Compounds of the formula ##STR1## in which the index n represents an integer of from 1 to 4,the index m represents 0 or 1,X represents oxygen, sulphur or the group --NH--,W represents a group --CO--, --CO--NHSO.sub.2 -- or --SO.sub.2 NH--CO--,or X-W together represent a group --CO-- or --CO--NHSO.sub.2 --,A represents optionally substituted phenylene, thienylene or furylene,Z represents oxygen or sulphur,Y represents lower alkylene,the index k represents the value 1 or 2,R.sub.4 represents hydrogen, an optionally substituted lower aliphatic or cycloaliphatic radical or acyl,R.sub.1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 represents a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.3 represents hydrogen or methoxy,and in which the carboxyl groups are optionally esterified in a form that can be split under physiological conditions, and salts of such compounds having salt-forming groups, are obtained by liberating the functional group(s) in a compound of the formula I in which at least one of the functional groups present is protected.The compounds are effective in vitro and in vivo against gram-positive and gram-negative bacteria and cocci.
摘要翻译：其中索引n表示1至4的整数的式（I）＆lt; IMAGE＆gt;的化合物，指数m表示0或1，X表示氧，硫或基团-NH-，W表示 -CO-，-CO-NHSO2-或-SO2NH-CO-，或XW一起表示-CO-或-CO-NHSO 2 - 基团，A表示任选取代的亚苯基，亚噻吩基或呋喃基，Z表示氧或硫，Y 代表低级亚烷基，指数k代表值1或2，R4代表氢，任选取代的低级脂族或脂环族基或酰基，R1代表氢，低级烷基，低级烷氧基，卤素或式-CH2-R2基团其中R2表示游离的，酯化的或醚化的羟基或巯基或季铵基团，并且R 3表示氢或甲氧基，并且其中羧基任选地以生理条件下分裂的形式进行酯化，这种具有成盐基团的化合物是通过以下方法获得的释放其中至少一个存在的官能团被保护的式I化合物中的官能团。这些化合物在体外和体内对革兰氏阳性和革兰氏阴性细菌和球菌有效。

3. 发明授权

US4508723A 6-Azaoligocycloalkylmethyleneaminopenam compounds 失效
标题翻译： 6-氮杂环烷基亚甲基氨基戊酸化合物
公开(公告)号：US4508723A
公开(公告)日：1985-04-02
申请号：US385139
申请日：1982-06-04
申请人： Karl Schaffner , Riccardo Scartazzini
发明人： Karl Schaffner , Riccardo Scartazzini
IPC分类号： A61K31/43 , A61P31/04 , C07D499/00 , C07D499/10 , C07D499/21 , A61K31/38 , C07D499/32
CPC分类号： C07D499/00
摘要： 6-Amino-penam compounds, having an antimicrobial action, of the formula ##STR1## in which R.sub.1 is an azaoligocycloalkyl radical which is bonded via the ring nitrogen atom and contains at least one endo-bridge atom and a total of 7 to 12 ring atoms and can contain a double bond and/or, if desired, as a further ring hetero-atom, an oxygen atom, or a nitrogen atom which can link the radical X.sub.1, where X.sub.1 is hydrogen or lower alkyl, and/or, if desired, free, esterified or etherified hydroxyl which is bonded to a ring carbon atom, and in which R.sub.2 is free carboxyl or carboxyl esterified by a physiologically detachable group, and salts of such compounds, processes for their preparation, pharmaceutical preparations which contain these compounds, including mixtures of these compounds with other antimicrobial, especially antibacterial and/or antiviral, active ingredients and/or additional substances or substance mixtures which alleviate the symptoms in the case of infections, the use of the novel compounds of the formula I and their salts, and of the novel substance mixtures, for combating micro-organisms and the preparation of corresponding medicaments by non-chemical means.
摘要翻译：具有抗微生物作用的6-氨基 - penam化合物，其具有式（I），其中R1是通过环氮原子键合并且含有至少一个内桥原子并且总共7个的氮杂稠环烷基至12个环原子，并且可以含有双键和/或如果需要，作为另外的环杂原子，氧原子或可连接基团X 1的氮原子，其中X 1是氢或低级烷基，和/ 或者如果需要，与环碳原子键合的游离的，酯化的或醚化的羟基，其中R2是通过生理上可分离的基团游离羧基或羧基酯化的化合物，以及这些化合物的盐，其制备方法，药物制剂包含这些化合物，包括这些化合物与其他抗微生物剂，特别是抗细菌和/或抗病毒活性成分和/或其他物质或物质混合物的混合物，其在感染的情况下减轻症状，使用nove 1种式I化合物及其盐，以及新型物质混合物，用于防治微生物和通过非化学方法制备相应的药物。

4. 发明授权

US4591642A Cephem and cepham derivatives 失效
标题翻译： Cephem和cepham衍生物
公开(公告)号：US4591642A
公开(公告)日：1986-05-27
申请号：US645472
申请日：1984-08-29
申请人： Riccardo Scartazzini , Hans Bickel
发明人： Riccardo Scartazzini , Hans Bickel
IPC分类号： A61K31/545 , C07D501/00 , C07D501/04 , C07D501/14 , C07D501/16 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/42 , C07D501/44 , C07D501/46 , C07D501/59 , C07D501/60 , C07F7/18
CPC分类号： C07D501/04 , Y02P20/55
摘要： The invention concerns 7.beta.-amino-cepham-3-one-4-carboxylic acid compounds, particularly esters thereof, and the N-substituted, especially N-acylated derivatives of such compounds. They can be used as intermediates, for example, for the manufacture of the corresponding enol ethers and esters, as well as the corresponding 3-unsubstituted 7.beta.-amino-3-cephem-4-carboxylic acid compounds, which show outstanding pharmacological effects.
摘要翻译：本发明涉及7种β-氨基 - 头孢-3-酮-4-羧酸化合物，特别是其酯，以及这些化合物的N-取代的，特别是N-酰化的衍生物。它们可以用作中间体，例如用于制备相应的烯醇醚和酯，以及相应的3-未取代的7-氨基-3-头孢烯-4-羧酸化合物，其显示出优异的药理作用。

5. 发明授权

US4389524A Cepham compounds 失效
标题翻译： Cepham化合物
公开(公告)号：US4389524A
公开(公告)日：1983-06-21
申请号：US655664
申请日：1976-02-05
申请人： Riccardo Scartazzini , Hans Bickel
发明人： Riccardo Scartazzini , Hans Bickel
IPC分类号： A61K31/545 , C07D501/00 , C07D501/04 , C07D501/14 , C07D501/16 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/42 , C07D501/44 , C07D501/46 , C07D501/59 , C07D501/60 , C07F7/18
CPC分类号： C07D501/04 , Y02P20/55
摘要： The invention concerns 7.beta.-amino-cepham-3-one-4-carboxylic acid compounds, particularly esters thereof, and the N-substituted, especially N-acylated derivatives of such compounds. They can be used as intermediates, for example, for the manufacture of the corresponding enol ethers and esters, as well as the corresponding 3-unsubstituted 7.beta.-amino-3-cephem-4-carboxylic acid compounds, which show outstanding pharmacological effects.
摘要翻译：本发明涉及7种β-氨基 - 头孢-3-酮-4-羧酸化合物，特别是其酯，以及这些化合物的N-取代的，特别是N-酰化的衍生物。它们可以用作中间体，例如用于制备相应的烯醇醚和酯，以及相应的3-未取代的7-氨基-3-头孢烯-4-羧酸化合物，其显示出优异的药理作用。

6. 发明授权

US4411897A Crystalline salts 失效
标题翻译：结晶盐
公开(公告)号：US4411897A
公开(公告)日：1983-10-25
申请号：US225295
申请日：1981-01-15
申请人： Riccardo Scartazzini
发明人： Riccardo Scartazzini
IPC分类号： C07D501/00 , A61K20060101 , A61K31/545 , C07D20060101 , C07D501/12 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/60
CPC分类号： C07D501/34
摘要： The invention relates to the novel crystalline hydrochloride and the crystalline hydrobromide of 7.beta.-[2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-cephem-4-carboxylic acid pivaloyloxymethyl ester, a process for the production thereof, and pharmaceutical preparations that contain these compounds.
摘要翻译：本发明涉及7β-[2-（2-氨基-4-噻唑基）-2-甲氧基亚氨基乙酰氨基] -3-头孢烯-4-羧酸新戊酰氧基甲酯的新结晶盐酸盐和结晶氢溴酸盐，一种生产方法和含有这些化合物的药物制剂。

7. 发明授权

US4405778A Process for preparing cephalosporin ethers 失效
标题翻译：制备头孢菌素醚的方法
公开(公告)号：US4405778A
公开(公告)日：1983-09-20
申请号：US657904
申请日：1976-02-13
申请人： Riccardo Scartazzini , Hans Bickel
发明人： Riccardo Scartazzini , Hans Bickel
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04 , C07D501/14 , C07D501/16 , C07D501/59 , C07D501/60 , C07F9/6561
CPC分类号： C07D501/04 , C07D501/59 , C07F9/65613 , Y02P20/55
摘要： The invention relates to O-substituted 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds of the formula ##STR1## wherein R.sub.1.sup.a represents hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represents hydrogen or an acyl group Ac, or R.sub.1.sup.a and R.sub.1.sup.b together represent a bivalent amino protective group, R.sub.2 represents hydroxyl or a radical R.sub.2.sup.A which together with the carbonyl grouping --C(.dbd.O)-- forms a protected carboxyl group and R.sub.3 represents an optionally substituted hydrocarbon radical or an acyl group, and to 1-oxides of 3-cephem compounds of the formula I, and also to the corresponding 2-cephem compounds of the formula ##STR2## wherein R.sub.1.sup.a, R.sub.1.sup.b, R.sub.2 and R.sub.3 have the abovementioned meanings, or salts of such compounds with salt-forming groups. 3-Cephem compound of the formula IA, particularly those, in which R.sub.1.sup.a represents an acyl group, R.sub.1.sup.b is hydrogen and R.sub.2 is hydroxy exhibit pronounced antimicrobial effects, the others, and particularly the 1-oxides of these 3-cephem compounds and the corresponding 2-cephem compounds are useful as intermediates.
摘要翻译：本发明涉及式（IA）的O-取代的7-氨基-3-头孢烯-3-醇-4-羧酸化合物，其中R 1a表示氢或氨基保护基R1A，并且R 1b表示氢或酰基Ac或R 1a和R 1b一起表示二价氨基保护基，R 2表示羟基或基团R 2 A，其与羰基-C（= O） - 形成被保护的羧基，R 3表示任选取代的烃基或酰基，以及式I的3-头孢烯化合物的1-氧化物，以及式（Ⅰb）的相应的2-头孢烯化合物，其中R1a，R1b，R2和R3具有上述含义，或这些化合物与成盐基团的盐。具有式IA的3-头孢烯化合物，特别是其中R 1a表示酰基，R 1b为氢且R 2为羟基的化合物表现出显着的抗微生物效果，其它化合物，特别是这些3-头孢烯化合物的1-氧化物和相应的 2-头孢烯化合物可用作中间体。

8. 发明授权

US4668781A Ceph-3-one compounds and process for their manufacture 失效
标题翻译： Ceph-3一种化合物及其制备方法
公开(公告)号：US4668781A
公开(公告)日：1987-05-26
申请号：US649636
申请日：1984-09-12
申请人： Riccardo Scartazzini , Hans Bickel
发明人： Riccardo Scartazzini , Hans Bickel
IPC分类号： A61K31/545 , C07D501/00 , C07D501/04 , C07D501/14 , C07D501/16 , C07D501/18 , C07D501/20 , C07D501/22 , C07D501/42 , C07D501/44 , C07D501/46 , C07D501/59 , C07D501/60 , C07F7/18
CPC分类号： C07D501/04 , Y02P20/55
摘要： The invention concerns 7.beta.-amino-cepham-3-one-4-carboxylic acid compounds, particularly esters thereof, and the N-substituted, especially N-acylated derivatives of such compounds. They can be used as intermediates, for example, for the manufacture of the corresponding enol ethers and esters, as well as the corresponding 3-unsubstituted 7.beta.-amino-3-cephem-4-carboxylic acid compounds, which show outstanding pharmacological effects.
摘要翻译：本发明涉及7种β-氨基 - 头孢-3-酮-4-羧酸化合物，特别是其酯，以及这些化合物的N-取代的，特别是N-酰化的衍生物。它们可以用作中间体，例如用于制备相应的烯醇醚和酯，以及相应的3-未取代的7-氨基-3-头孢烯-4-羧酸化合物，其显示出优异的药理作用。

9. 发明授权

US4467101A Compounds with terminal aminocarboxylic acid grouping 失效
标题翻译：具有末端氨基羧酸分子的化合物
公开(公告)号：US4467101A
公开(公告)日：1984-08-21
申请号：US420534
申请日：1982-09-20
申请人： Karoly Kocsis , Peter Schneider , Bruno Fechtig , Riccardo Scartazzini
发明人： Karoly Kocsis , Peter Schneider , Bruno Fechtig , Riccardo Scartazzini
IPC分类号： C07D499/06 , A61K31/545 , A61K31/546 , A61P31/04 , C07D307/34 , C07D307/52 , C07D307/54 , C07D333/04 , C07D333/24 , C07D501/00 , C07D501/20 , C07D501/32 , C07D501/34 , C07D501/57 , C07D501/59 , C07C143/52 , C07C147/13 , C07C153/00
CPC分类号： C07D333/24 , C07D307/52 , C07D307/54
摘要： Acylamido-3-cephem-4-carboxylic acid compounds of the formula ##STR1## in which the index n represents an integer of from 1 to 4,the index m represents 0 or 1,X represents oxygen, sulphur or an --NH-- group,W represents a --CO--, --CO--NHSO.sub.2 -- or --SO.sub.2 NH--CO-- group, orX-W together represent a --CO-- or --CO--NHSO.sub.2 -- group,A represents optionally substituted phenylene, thienylene or furylene,Y represents hydrogen, hydroxyl, formyloxy, amino or sulpho optionally present in salt form, andZ represents hydrogen, orY and Z together represent an oxo group or an .dbd.N--O--R.degree. group in which R.degree. represents hydrogen or optionally substituted lower alkyl,R.sub.1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 is a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.3 represents hydrogen or methoxy,wherein the carboxyl groups are optionally esterified in a form that can be split under physiological conditions, and the salts thereof, are obtained by liberating the functional group(s) in a starting compound of the formula I in which at least one of the functional groups present is protected.The compounds are effective in vitro and in vivo against gram-positive and gram-negative bacteria and cocci.
摘要翻译：酰亚胺基-3-头孢烯-4-羧酸化合物，其中指数n表示1至4的整数，指数m表示0或1，X表示氧，硫或-NH-基团，W表示-CO-，-CO-NHSO2-或-SO2NH-CO-基团，或XW一起表示-CO-或-CO-NHSO2-基团，A表示任选取代的亚苯基，亚噻吩基或呋喃基，Y表示氢，羟基，甲酰氧基，任选以盐形式存在的氨基或磺基，Z表示氢，或Y和Z一起表示氧代基或= NOROR基，其中R DEG表示氢或任选取代的低级烷基，R 1表示氢，低级烷基，低级烷氧基，卤素或式-CH 2 -R 2的基团，其中R 2是游离的，酯化的或醚化的羟基或巯基或季铵基团，R 3表示氢或甲氧基，其中羧基任选地以可在生理学上分裂的形式进行酯化定义及其盐通过释放其中存在至少一个官能团被保护的式I起始化合物中的官能团而获得。这些化合物在体外和体内对革兰氏阳性和革兰氏阴性细菌和球菌有效。

10. 发明授权

US4301279A Process for the production of 3-hydroxy compounds 失效
标题翻译： 3-羟基化合物的制备方法
公开(公告)号：US4301279A
公开(公告)日：1981-11-17
申请号：US121085
申请日：1980-02-13
申请人： Riccardo Scartazzini
发明人： Riccardo Scartazzini
IPC分类号： C07D205/095 , C07D501/04 , C07D501/59 , C07D501/20
CPC分类号： C07D205/095 , Y02P20/55
摘要： Process for the production of 7.beta.-substituted 3-hydroxycepham-4-carboxylic acid compounds of the formula ##STR1## in which R.sub.1.sup.a represents hydrogen or an amino-protecting group R.sub.1.sup.A, andR.sub.1.sup.b represents hydrogen or an acyl radical Ac,or in whichR.sub.1.sup.a and R.sub.1.sup.b together form a bivalent amino-protecting group, andR.sub.2 represents a radical that, together with the carbonyl grouping --C(.dbd.O)--, forms a protected carboxyl group,and 1-oxides thereof as well as salts of such compounds with salt-forming groups, from a 7.beta.-substituted 3-hydroxy-3-cephem-4-carboxylic acid compound of the formula ##STR2## from a 1-oxide or a salt thereof, and a complex borohydride, characterized in that the reduction is carried out in the presence of an organic acid.The reduction in the presence of an organic acid produces higher yields.
摘要翻译：制备其中R 1a表示氢或氨基保护基R 1A的式（I）的7β-取代的3-羟基头孢-4-羧酸化合物的方法，并且R 1b表示氢或酰基Ac，或其中R 1a和R 1b一起形成二价氨基保护基团，并且R 2表示与羰基-C（= O） - 一起形成被保护的羧基的基团，及其1-氧化物以及其盐的具有成盐基团的化合物，得自式I的3-取代的3-羟基-3-头孢烯-4-羧酸化合物（II）的1-氧化物或其盐和络合物硼氢化物，其特征在于还原在有机酸的存在下进行。存在有机酸的减少产生更高的产率。

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