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1. 发明授权

US5438052A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5438052A
公开(公告)日：1995-08-01
申请号：US979519
申请日：1992-11-20
申请人： Peter Angehrn , Andre Furlenmeier , Paul Hebeisen , Werner Hofheinz , Helmut Link
发明人： Peter Angehrn , Andre Furlenmeier , Paul Hebeisen , Werner Hofheinz , Helmut Link
IPC分类号： A61K31/545 , A61K20060101 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/18 , C07D501/20 , C07D501/34 , C07D501/36 , C07D519/06
CPC分类号： C07D501/00
摘要： Cephalosporin derivatives have the formula ##STR1## wherein Z.sup.1, Z.sup.2, X, Y, P, Q, m, n and p are as defined in the following text. Also described are the readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, and hydrates of compounds of formula I, their esters and salts. Processes are provided for manufacture and pharmaceutical preparations which contain these compounds. Intermediates from the manufacture of these compounds are described, as is the use of the compounds in the control of illnesses and for the manufacture of the aforementioned preparations.
摘要翻译：头孢菌素衍生物具有下式的定义：其中Z1，Z2，X，Y，P，Q，m，n和p如下文所定义。还描述了这些化合物的易水解的酯和药学上相容的盐，以及式I化合物及其酯和盐的水合物。提供了含有这些化合物的制造方法和药物制剂。描述了这些化合物的制造中的中间体，以及化合物在控制疾病和制备上述制剂中的用途。

2. 发明授权

US5055572A Cephalosporin derivatives 失效
标题翻译： CEPHALOSPORIN衍生物
公开(公告)号：US5055572A
公开(公告)日：1991-10-08
申请号：US179199
申请日：1988-04-08
申请人： Andre Furlenmeier , Erwin Gotschi , Paul Hebeisen , Werner Hofheinz , Helmut Link
发明人： Andre Furlenmeier , Erwin Gotschi , Paul Hebeisen , Werner Hofheinz , Helmut Link
IPC分类号： C07D519/06 , A61K31/545 , A61P31/04 , C07D501/36 , C07D501/46 , C07D519/00
CPC分类号： C07D501/36 , C07D519/00 , Y02P20/55
摘要： Acyl derivatives of the formula ##STR1## in which R is an acyl group, excluding those acyl groups of the formula ##STR2## in which A is a group of the formulae --NHCO--, --NHCONHCO--, --NHCOCH.dbd.CH--, ##STR3## wherein R.sup.6 is hydrogen or lower alkyl; R.sup.1 and R.sup.2 are hydrogen or a protecting group, X is hydrogen, halogen, lower alkoxy, nitro or --OR.sup.2, n is 1 or 2, R.sup.4 and R.sup.5 are hydrogen or together represent an additional bond and Z is a direct bond or carbonyl (where R.sup.4 and R.sup.5 both represent hydrogen) or a group of the formula --O--B-- (where R.sup.4 and R.sup.5 together represent an additional bond) in which B is a straight-chain, branched or cyclic lower alkylene;and wherein R.sup.3 is a substituted bicyclic group of the formulae ##STR4## wherein R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl or trifluoromethyl or, in formulae (a), (b), (e) and (f) together represent alkylene with 3 or 4 carbon atoms, and R', R" and R"' are independently hydrogen, lower alkyl or lower cycloalkyl; wherein compounds of formula I in which R.sup.4 and R.sup.5 together represent an additional bond are present in the syn-isomeric form or as a mixture with the anti-isomeric form in which the syn-isomeric form predominates,as well as readily hydrolyzable esters and salts of these compounds and hydrates of the compounds of formula I or of their esters and salts.These compounds are useful as antibiotics.
摘要翻译：除了那些其中A是式-NHCO-，-NHCONHCO-，-NHCOCH = CH-的基团的式“IMAGE”的酰基之外，其中R是酰基的式Ⅰ的酰基衍生物，其中R6是氢或低级烷基; R1和R2是氢或保护基，X是氢，卤素，低级烷氧基，硝基或-OR2，n是1或2，R4和R5是氢或一起代表另外的键，Z是直接键或羰基（其中R4和R5都表示氢）或式-BB-（其中R4和R5一起代表附加键）的基团，其中B是直链，支链或环状低级亚烷基; 并且其中R 3是下式的取代的双环基团：其中R 7和R 8独立地是氢，低级烷基或三氟甲基，或者在式（a），（b）中，），（e）和（f）共同表示具有3或4个碳原子的亚烷基，R'，R“和R”'独立地是氢，低级烷基或低级环烷基; 其中R 4和R 5一起代表另外的键的式Ⅰ化合物以顺式异构形式存在，或作为其中顺式异构体形式占优势的抗异构体形式的混合物以及容易水解的酯和盐的这些化合物和式I化合物的水合物或它们的酯和盐。这些化合物可用作抗生素。

3. 发明授权

US4652651A Process for the manufacture of 1-sulpho-2-oxoazetidine carboxylic acid intermediates via catalytic ester cleavage 失效
公开(公告)号：US4652651A
公开(公告)日：1987-03-24
申请号：US852046
申请日：1986-04-14
申请人： Andre Furlenmeier , Werner Hofheinz , Christian N. Hubschwerlen , Hans P. Isenring
发明人： Andre Furlenmeier , Werner Hofheinz , Christian N. Hubschwerlen , Hans P. Isenring
IPC分类号： C07D205/085 , C07D263/48 , C07D277/20 , C07D277/74 , C07D403/12 , C07D413/12 , C07D417/12 , C07D277/40 , C07D213/73 , C07D231/38 , C07D233/44 , C07D285/08
CPC分类号： C07D277/587 , C07D205/085 , C07D263/48 , C07D277/74 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.1 being present at least partially in the syn-form,in racemic form or in the form of the 3S-enantiomer, and of readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, by acylating a compound of the formula ##STR2## in which R.sup.20 equals R.sup.2 or can also represent a 2,2-dimethyl-1,3-dioxolan-4-yl group and R.sup.3 is hydrogen or sulpho,or a salt thereof with a thioester of the formula ##STR3## in which Het is as above and R.sup.10 has any of the values of R.sup.1 except carboxy-lower alkyl, and can also represent a tri-lower alkyl-silyl-lower-alkoxycarbonyl-lower alkyl group or a carboxy-lower alkyl group converted into a readily hydrolyzable ester group, and the group .dbd.NOR.sup.10 is present at least partially in the syn-form, and carrying out subsequent steps (N-sulphonation, conversion of R.sup.20 into R.sup.2, R.sup.10 into R.sup.1), some of which are optional.The invention also provides certain novel products of formula I and benzthiazolyl thioesters of formula III per se and the preparation of the benzthiazolyl thioesters by esterifying corresponding carboxylic acids. Finally, the invention provides a process for the preparation of carboxylic acids in which R.sup.1 is t-alkoxycarbonylmethyl.The compounds of formula I have antimicrobial activity.

4. 发明授权

US4816582A Antimicrobial 2-oxo-1-azetidinesulphonic acids 失效
标题翻译：抗菌2-氧代-1-氮杂二磺酸
公开(公告)号：US4816582A
公开(公告)日：1989-03-28
申请号：US111480
申请日：1987-10-22
申请人： Andre Furlenmeier , Werner Hofheinz , Christian N. Hubschwerlen , Hans P. Isenring
发明人： Andre Furlenmeier , Werner Hofheinz , Christian N. Hubschwerlen , Hans P. Isenring
IPC分类号： A61K31/397 , A61K31/425 , A61K31/426 , A61K31/428 , A61P31/04 , C07D205/08 , C07D205/085 , C07D263/48 , C07D277/20 , C07D277/40 , C07D277/70 , C07D403/12 , C07D405/04 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07F7/08 , C07D401/14 , C07D403/14
CPC分类号： C07D277/20 , C07D205/085 , C07D263/48 , C07D403/12 , C07D405/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07F7/0812
摘要： Antimicrobial 2-oxo-1-azetidinesulphonic acids of the formula ##STR1## in which H.sub.2 N ##STR2## represents an amino-substituted thiazolyl group, R.sup.1 is lower alkyl which is substituted by carbamoyl, lower alkylsuphonyl, azido, piperidine-carbonyl, (hexahydro-1H-azepin-1-yl)carbonyl or lower alkynyl, and R.sup.2 is hydrogen or a lower organic group, typically, carbamoyloxymethyl.
摘要翻译：其中H 2 N“表示氨基取代的噻唑基的式”IMAGE“的抗微生物2-氧代-1-氮杂环丁磺酸，R1是被氨基甲酰基，低级烷基加酰卤，叠氮基，哌啶羰基，（六氢）代替的低级烷基 -1H-吖庚因-1-基）羰基或低级炔基，R 2是氢或低级有机基团，通常为氨基甲酰氧基甲基。

5. 发明授权

US4948898A Process for the manufacture of 1-sulpho-2-oxoazetidine derivatives 失效
公开(公告)号：US4948898A
公开(公告)日：1990-08-14
申请号：US317081
申请日：1989-02-28
申请人： Andre Furlenmeier , Werner Hofheinz , Christian N. Hubschwerlen , Hans P. Isenring
发明人： Andre Furlenmeier , Werner Hofheinz , Christian N. Hubschwerlen , Hans P. Isenring
IPC分类号： C07D205/085 , C07D231/12 , C07D263/48 , C07D277/20 , C07D277/40 , C07D277/74 , C07D403/12 , C07D405/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07F7/08
CPC分类号： C07D277/20 , C07D205/085 , C07D263/48 , C07D277/587 , C07D277/74 , C07D403/12 , C07D405/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07F7/0812
摘要： The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.1 being present at least partially in the syn-form,in racemic form or in the form of the 3S-enantiomer, and of readily hydrolyzable esters and pharmaceutically compatible salts of these compounds, by acylating a compound of the formula ##STR2## in which R.sup.20 equals R.sup.2 or can also represent a 2,2-dimethyl-1,3-dioxolan-4-yl group and R.sup.3 is hydrogen or sulpho,or a salt thereof with a thioester of the formula ##STR3## in which Het is as above and R.sup.10 has any of the values of R.sup.1 except carboxy-lower alkyl, and can also represent a tri-lower alkyl-silyl-lower-alkoxycarbonyl-lower alkyl group or a carboxy-lower alkyl group converted into a readily hydrolyzable ester group, and the group .dbd.NOR.sup.10 is present at least partially in the syn-form,and carrying out subsequent steps (N-sulphonation, conversion of R.sup.20 into R.sup.2, R.sup.10 into R.sup.1), some of which are optional.The invention also provides certain novel products of formula I and benzthiazolyl thioesters of formula III per se and the preparation of the benzthiazolyl thioesters by esterifying corresponding carboxylic acids. Finally, the invention provides a process for the preparation of carboxylic acids in which R.sup.1 is t-alkoxycarbonylmethyl.The compounds of formula I have antimicrobial activity.

6. 发明授权

US5359057A Acylation of amines 失效
标题翻译：胺的酰化
公开(公告)号：US5359057A
公开(公告)日：1994-10-25
申请号：US822173
申请日：1992-01-16
申请人： Andre Furlenmeier , Urs Weiss
发明人： Andre Furlenmeier , Urs Weiss
IPC分类号： C07D277/74 , C07D499/00 , C07D501/06 , C07D499/12
CPC分类号： C07D499/00 , C07D277/74
摘要： There is described a process for the manufacture of carboxylic acid amides by acylating amines with 2-benzothiazolyl thioesters of carboxylic acids, which process comprises reacting the amine in the form of an acid addition salt. This process is especially of great advantage when the amine is not particularly stable in the form of the free base, which is frequently the case especially with 7-aminocephalosporin derivatives. 7-Acylamino-cephalosporin derivatives can be manufactured in good yield and in high purity with the novel process.
摘要翻译：描述了通过用羧酸的2-苯并噻唑基硫酯将胺酰化而制备羧酸酰胺的方法，该方法包括以酸加成盐的形式使胺反应。当胺不是游离碱的形式不是特别稳定时，这个过程尤为重要，特别是7-氨基头孢菌素衍生物。 7-酰氨基 - 头孢菌素衍生物可通过新方法以良好的产率和高纯度制备。

7. 发明授权

US4482551A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4482551A
公开(公告)日：1984-11-13
申请号：US403951
申请日：1982-07-30
申请人： Andre Furlenmeier , Paul Lanz
发明人： Andre Furlenmeier , Paul Lanz
IPC分类号： A61K31/545 , C07D501/36 , C07D501/56
CPC分类号： C07D501/36
摘要： There is presented compounds of the formula ##STR1## in which R.sup.1 represents hydrogen or methyl, as well as readily hydrolyzable esters and salts of these compounds and the hydrates thereof.Also presented are various intermediates and a process to produce the novel derivatives.The acyl derivatives have pharmacological activity as antibacterial agents.
摘要翻译：呈现式“IMAGE”的化合物，其中R 1表示氢或甲基，以及这些化合物及其水合物的易水解的酯和盐。还提出了各种中间体和生产新型衍生物的方法。酰基衍生物具有作为抗菌剂的药理活性。

8. 发明授权

US3957758A 6-Acyl derivatives of aminopenicillanic acid 失效
标题翻译：氨基苯甲酸的6-ACY衍生物
公开(公告)号：US3957758A
公开(公告)日：1976-05-18
申请号：US492947
申请日：1974-07-30
申请人： Andre Furlenmeier , Peter Quitt , Karl Vogler , Paul Lanz
发明人： Andre Furlenmeier , Peter Quitt , Karl Vogler , Paul Lanz
IPC分类号： C07D307/24 , C07D307/68 , C07D307/84 , C07D499/60 , C07D499/44
CPC分类号： C07D307/84 , C07D307/24 , C07D307/68
摘要： Compounds represented by the following formula ##EQU1## wherein A is a substituted or unsubstituted heterocyclic radical and T is a C.sub.2 -C.sub.5 alkyl, alkenyl, cyclopropylmethyl, cyclobutylmethyl or cyclopentyl groupA process for their preparation and novel intermediates therefor are disclosed. These compounds are useful antibiotics.

9. 再颁专利

USRE29003E (R)-1-(2-furoyloxy)-3-methylbutyl-penicillin 失效
标题翻译：（R）-1-（2-呋喃氧基）-3-甲基丁基 - 青霉素
公开(公告)号：USRE29003E
公开(公告)日：1976-10-12
申请号：US619128
申请日：1975-10-02
申请人： Andre Furlenmeier , Paul Lanz , Peter Quitt , Karl Vogler, deceased , by Heinrich Vogler, heir at Law , by Niklaus Eduard Vogler, heir at Law , by Franziska Elisabeth Vogler, heir at Law
发明人： Andre Furlenmeier , Paul Lanz , Peter Quitt , Karl Vogler, deceased , by Heinrich Vogler, heir at Law , by Niklaus Eduard Vogler, heir at Law , by Franziska Elisabeth Vogler, heir at Law
IPC分类号： C07D307/24 , C07D307/68 , C07D307/84 , C07D499/00
CPC分类号： C07D499/00 , C07D307/24 , C07D307/68 , C07D307/84
摘要： Compounds represented by the following formula ##EQU1## wherein A is a substituted or unsubstituted heterocyclic radical and T is a C.sub.2 -C.sub.5 alkyl, alkenyl, cyclopropylmethyl, cyclobutylmethyl or cyclopentyl groupA process for their preparation and novel intermediates therefor are disclosed. These compounds are useful antibiotics.

10. 发明授权

US3956323A Furan, benzofuran and tetrahydrofuran carboxylic acid esters 失效
标题翻译：呋喃，苯并呋喃和四氢呋喃羧酸酯
公开(公告)号：US3956323A
公开(公告)日：1976-05-11
申请号：US494144
申请日：1974-08-02
申请人： Andre Furlenmeier , Peter Quitt , Karl Vogler , Paul Lanz
发明人： Andre Furlenmeier , Peter Quitt , Karl Vogler , Paul Lanz
IPC分类号： C07D213/79 , C07D213/89 , C07D307/24 , C07D307/68 , C07D307/84 , C07D499/60 , C07D307/56 , C07D307/85
CPC分类号： C07D213/79 , C07D213/89 , C07D307/24 , C07D307/68 , C07D307/84
摘要： Compounds represented by the following formula ##EQU1## wherein A is a substituted or unsubstituted heterocyclic radical and T is a C.sub.2 -C.sub.5 alkyl, alkenyl, cyclopropylmethyl, cyclobutylmethyl or cyclopentyl groupA process for their preparation and novel intermediates therefor are disclosed. These compounds are useful antibiotics.
摘要翻译：由下式表示的化合物S ANGLE CH 3 A-COO-CH-CO-NH-CH-CHC ANGLE |||| CH 3 TC-N-CH并行性| OCOOH其中A是取代或未取代的杂环基，T是 C 2 -C 5烷基，烯基，环丙基甲基，环丁基甲基或环戊基。其制备和新颖中间体的方法被公开。这些化合物是有用的抗生素。

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