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1. 发明授权

US4370327A Cephalosporins and pharmaceutical compositions 失效
标题翻译：头孢菌素和药物组合物
公开(公告)号：US4370327A
公开(公告)日：1983-01-25
申请号：US237066
申请日：1981-02-23
申请人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
发明人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/20 , C07D501/24 , C07D501/57 , C07D501/22 , C07D501/36 , C07D501/46
CPC分类号： C07D277/587 , Y02P20/55
摘要： The invention is directed to cephalosporins of the formula ##STR1## and the tautomers thereof, and, when E is a hydrogen atom, the pharmacologically acceptable salts thereof with inorganic or organic bases.
摘要翻译：本发明涉及式IMA的头孢菌素及其互变异构体，并且当E是氢原子时，其药理上可接受的盐与无机或有机碱形成。

2. 发明授权

US4364944A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4364944A
公开(公告)日：1982-12-21
申请号：US323382
申请日：1981-11-20
申请人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
发明人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
IPC分类号： C07D501/06 , A61K20060101 , A61K31/545 , A61K31/546 , C07D20060101 , C07D501/00 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/56 , C07D501/57
CPC分类号： C07D501/20 , Y02P20/55
摘要： Compounds of the formula ##STR1## wherein Y is hydrogen or methoxy;A is ##STR2## or, when Y is methoxy, also phenyl, 4-hydroxy-phenyl, 2-thienyl, 3-thienyl of 3,4-dihydroxy-phenyl;A' is hydrogen, --COCH.sub.2 Cl, --COCH.sub.2 Br, --COOCH.sub.2 CCL.sub.3, formyl or trityl;D is hydrogen, acetoxy, aminocarbonyloxy, pyridinium, 4-aminocarbonyl-pyridinium or -S-Het, where Het is 3-methyl-1,2,4-thiadiazol-5-yl, 1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 4H-5,6-dioxo-1,2,4-triazine-3-yl, 4-methyl-5,6-dioxo-1,2,4-triazin-3-yl, 1-vinyl-tetrazol-5-yl, 1-allyl-tetrazol-5-yl or ##STR3## n is 1, 2 or 3; R.sub.1 is hydroxyl, amino, dimethylamino, acetylamino, aminocarbonyl, aminocarbonylamino, aminosulfonyl, aminosulfonylamino, methylcarbonyl, methylsulfonylamino, cyano, hydroxysulfonylamino, methylsulfonyl, methylsulfinyl, a carboxylic acid group or a sulfonic acid group; or--(CH.sub.2).sub.n R.sub.1 is alkyl of 1 to 4 carbon atoms or 2,3-dihydroxy-propyl;R.sub.2 is unsubstituted or monosubstituted 3-pyridyl, 5-pyrimidinyl, 2-thienyl, 2-furyl-methyl, 2-thienyl-methyl, 2-imidazolyl-methyl, 2-thiazolyl-methyl, 3-pyridyl-methyl or 5-pyrimidinyl-methyl, where the substituent is chlorine, methyl, acetylamino, hydroxyl, methylsulfinyl, methylsulfonyl, aminocarbonyl or aminosulfonyl; andE is hydrogen or a carboxyl-protective group which is easily removable in vitro or in vivo;and, E is hydrogen, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases; the compounds as well as their salts are useful as antibiotics.
摘要翻译：其中Y是氢或甲氧基的式“IMAGE”的化合物; A是，或者当Y是甲氧基时，3,4-二羟基 - 苯基的苯基，4-羟基 - 苯基，2-噻吩基，3-噻吩基; A'是氢，-COCH 2 Cl，-COCH 2 Br，-COOCH 2 CCl 3，甲酰基或三苯甲基; D是氢，乙酰氧基，氨基羰氧基，吡啶鎓，4-氨基羰基 - 吡啶鎓或-S-Het，其中Het是3-甲基-1,2,4-噻二唑-5-基，1,2,4-噻二唑-5-基， 1,3,4-噻二唑-5-基，2-甲基-1,3,4-噻二唑-5-基，4H-5,6-二氧代-1,2,4-三嗪-3-基， 4-甲基-5,6-二氧代-1,2,4-三嗪-3-基，1-乙烯基 - 四唑-5-基，1-烯丙基 - 四唑-5-基或n为1,2 或3; R1是羟基，氨基，二甲基氨基，乙酰基氨基，氨基羰基，氨基羰基氨基，氨基磺酰基，氨基磺酰基氨基，甲基羰基，甲基磺酰基氨基，氰基，羟基磺酰基氨基，甲基磺酰基，甲基亚磺酰基，羧酸基或磺酸基团。或 - （CH 2）n R 1是1至4个碳原子的烷基或2,3-二羟基 - 丙基; R2是未取代的或单取代的3-吡啶基，5-嘧啶基，2-噻吩基，2-呋喃基 - 甲基，2-噻吩基 - 甲基，2-咪唑基 - 甲基，2-噻唑基 - 甲基，3-吡啶基 - 甲基或5-嘧啶基甲基，其中取代基是氯，甲基，乙酰氨基，羟基，甲基亚磺酰基，甲基磺酰基，氨基羰基或氨基磺酰基; E是氢或羧基保护基，其在体外或体内容易除去; 和E是氢，与无机或有机碱形成的无毒的药理学上可接受的盐; 化合物及其盐可用作抗生素。

3. 发明授权

US4379784A Pyrimidinyl ureido penicillins 失效
标题翻译：嘧啶基脲基青霉素
公开(公告)号：US4379784A
公开(公告)日：1983-04-12
申请号：US323383
申请日：1981-11-20
申请人： Roland Maier , Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Uwe Lechner , Hanns Goeth
发明人： Roland Maier , Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Uwe Lechner , Hanns Goeth
IPC分类号： C07D239/48 , C07D499/00 , C07D499/64 , A61K31/505 , A61K31/635 , C07D499/70
CPC分类号： C07D239/48 , C07D499/00
摘要： Compounds of the formula ##STR1## wherein A is phenyl, 4-hydroxy-phenyl, 2-thienyl or 3,4-dihydroxy-phenyl; andR is ##STR2## where R.sub.1 and R.sub.2, which may be identical to or different from each other, are each methylmercapto or amino;Z' is oxygen, sulfur or .dbd.NR.sub.3 ;R.sub.3 is hydrogen, alkyl of 1 to 3 carbon atoms or hydroxy-(alkyl of 1 to 3 carbon atoms);R.sub.4 is hydrogen, hydroxyl, hydroxymethyl or methyl;n is 2, 3 or 4;Y is --SO.sub.2 NH--, --SO-- or --SO.sub.2 --;Z is straight or branched alkylene of 1 to 3 carbon atoms;X is hydroxyl, aminocarbonyl, aminosulfonyl, formylamino, acetylamino, amino, methylsulfinyl, methylsulfonyl or ##STR3## or --Y--Z--X is ##STR4## and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as the salts are useful as antibiotics.
摘要翻译：其中A是苯基，4-羟基 - 苯基，2-噻吩基或3,4-二羟基 - 苯基的式IMA化合物; 其中R 1和R 2可以相同或不同，分别是甲基巯基或氨基; Z'是氧，硫或= NR3; R3是氢，1至3个碳原子的烷基或羟基 - （1至3个碳原子的烷基）; R4是氢，羟基，羟甲基或甲基; n为2,3或4; Y是-SO 2 NH-，-SO-或-SO 2 - ; Z是1〜3个碳原子的直链或支链亚烷基; X是羟基，氨基羰基，氨基磺酰基，甲酰氨基，乙酰氨基，氨基，甲基亚磺酰基，甲基磺酰基或者-YZX是无毒的，药理学上可接受的盐其形成有无机或有机碱。化合物和盐可用作抗生素。

4. 发明授权

US4256738A 9-(.omega.-Heteroarylamino-alkylamino)-erythromycins and salts thereof 失效
标题翻译： 9-（ω-异芳基氨基 - 烷基氨基） - 红霉素及其盐
公开(公告)号：US4256738A
公开(公告)日：1981-03-17
申请号：US957451
申请日：1978-11-03
申请人： Eberhard Woitun , Bernd Wetzel , Roland Maier , Wolfgang Reuter , Uwe Lechner , Rolf G. Werner , Hanns Goeth
发明人： Eberhard Woitun , Bernd Wetzel , Roland Maier , Wolfgang Reuter , Uwe Lechner , Rolf G. Werner , Hanns Goeth
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of the formulaR--NH--(CH.sub.2).sub.n --NH--EwhereinR is a pyrimidinyl, a quinazolinyl, a 5,6,7,8-tetrahydro-quinazolinyl, a thieno[3,2,-d]pyrimidinyl, a thieno[2,3-d]pyrimidyl, a pyrido[3,2-d]primidinyl, a 5,6-dihydro-4-pyrido[3,4-d]pyrimidinyl, an isothiazola [5,4-d]pyrimidinyl or a pyrimido[4,5-d]-pyrimidinyl group;n is 2 or 3; andE is the 9-erythromycyl group;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antibacterials.
摘要翻译：式R-NH-（CH2）n-NH-E的化合物，其中R是嘧啶基，喹唑啉基，5,6,7,8-四氢 - 喹唑啉基，噻吩并[3,2-d]嘧啶基，噻吩并[2,3-d]嘧啶基，吡啶并[3,2-d]嘧啶基，5,6-二氢-4-吡啶并[3,4-d]嘧啶基，异噻唑并[5,4-d] 嘧啶基或嘧啶并[4,5-d] - 嘧啶基; n为2或3; E为9-红霉素基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作抗细菌剂。

5. 再颁专利

USRE31926E Penicillins and salts thereof 失效
标题翻译：青霉素及其盐
公开(公告)号：USRE31926E
公开(公告)日：1985-06-25
申请号：US420804
申请日：1982-09-21
申请人： Bernd Wetzel , Wolfgang Reuter , Eberhard Woitun , Roland Maier , Uwe Lechner , Hanns Goeth , Rolf Werner
发明人： Bernd Wetzel , Wolfgang Reuter , Eberhard Woitun , Roland Maier , Uwe Lechner , Hanns Goeth , Rolf Werner
IPC分类号： C07D499/66 , A61K31/43 , A61P31/04 , C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D499/00 , C07D499/12 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D499/00
摘要： Compounds of the formula ##STR1## wherein A is phenyl; 4-hydroxy-phenyl; 2- or 3-thienyl; cyclohexyl; cyclohexen-1-yl; cyclohexa-1, 4-dien-1-yl; or 3,4-disubstituted phenyl, where the substituents may be identical to or different from each other and are selected from the group consisting of chlorine, hydroxyl or methoxy; andR is an aliphatic, cycloaliphatic; aromatic or heterocyclic group of diverse types;and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antibiotics.

6. 发明授权

US4362725A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4362725A
公开(公告)日：1982-12-07
申请号：US305953
申请日：1981-09-28
申请人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
发明人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
IPC分类号： A01N43/86 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/00 , C07D501/36 , C07D501/46 , C07D501/56 , C07D501/57
CPC分类号： C07D501/36 , Y02P20/55
摘要： Compounds of the formula ##STR1## wherein A is phenyl, 4-hydroxy-phenyl, 2-thienyl, 2-furyl or 3,4-dihydroxy-phenyl;Y is hydrogen or methoxy;Het is 4H-5,6-dioxo-1,2,4-triazin-3-yl,4-methyl-5,6-dioxo-1,2,4-triazin-3-yl,2-methyl-5,6-dioxo-1,2,4-triazin-3-yl,1-vinyl-tetrazol-5-yl, 1-allyl-tetrazol-5-yl or ##STR2## where n is an integer from 1 to 3, inclusiveR.sub.1 is hydroxyl, amino, dimethylamino, acetylamino, aminocarbonyl, aminocarbonylamino, aminosulfonyl, aminosulfonylamino, methylcarbonyl, methylsulfonylamino, cyano, hydroxysulfonylamino, methylsulfonyl, methylsulfinyl, a carboxylic acid group or a sulfonic acid group, and--(CH.sub.2).sub.n --R.sub.1 may also be alkyl of 2 to 4 carbon atoms or 2,3-dihydroxy-propyl;R is cyclopropyl, 4'-hydroxycyclohexyl-amino ##STR3## where R.sub.2 is straight or branched, saturated or unsaturated hydrocarbyl of 1 to 4 carbon atoms or cycloalkyl of 3 to 6 carbon atoms;G is hydroxyl, aminocarbonyl, aminosulfonyl, aminocarbonylamino, acetylamino, methylsulfonylamino, methylsulfinyl or methylsulfonyl;m is 0 or 1; andR.sub.3 and R.sub.4, which may be identical to or different from each other, are each hydrogen, chlorine, fluorine, hydroxyl, methoxy, acetylamino, aminocarbonylamino, nitro, acetyl, methylcarbonyloxy, methoxycarbonyl, aminocarbonyl, cyano, methylsulfinyl, methylsulfonyl, aminosulfonyl, methylaminosulfonyl or methyl; andE is hydrogen or a protective group which is easily removable in vitro or in vivo;and, when E is hydrogen, non-toxic, pharmacologically acceptable salts thereof; the compounds as well as their salts are useful as antibiotics.
摘要翻译：其中A是苯基，4-羟基 - 苯基，2-噻吩基，2-呋喃基或3,4-二羟基 - 苯基的式IMA化合物; Y是氢或甲氧基; Het是4H-5,6-二氧代-1,2,4-三嗪-3-基，4-甲基-5,6-二氧代-1,2,4-三嗪-3-基，2-甲基-5- 6-二氧代-1,2,4-三嗪-3-基，1-乙烯基 - 四唑-5-基，1-烯丙基 - 四唑-5-基或其中n是1至3的整数，包括1和3 R 1是羟基，氨基，二甲基氨基，乙酰氨基，氨基羰基，氨基羰基氨基，氨基磺酰基，氨基磺酰基氨基，甲基羰基，甲基磺酰基氨基，氰基，羟基磺酰基氨基，甲磺酰基，甲基亚磺酰基，羧酸基或磺酸基，和 - （CH 2）n -R 具有2至4个碳原子的烷基或2,3-二羟基丙基; 其中R 2是具有1至4个碳原子的直链或支链，饱和或不饱和的烃基或3至6个碳原子的环烷基; R 2是环丙基，4'-羟基环己基氨基， G是羟基，氨基羰基，氨基磺酰基，氨基羰基氨基，乙酰氨基，甲基磺酰基氨基，甲基亚磺酰基或甲基磺酰基; m为0或1; 可以相同或不同的R 3和R 4各自为氢，氯，氟，羟基，甲氧基，乙酰氨基，氨基羰基氨基，硝基，乙酰基，甲基羰基氧基，甲氧基羰基，氨基羰基，氰基，甲基亚磺酰基，甲基磺酰基，氨基磺酰基，甲基氨基磺酰基或甲基; E是氢或在体外或体内容易除去的保护基; 并且当E是氢时，其无毒的药学上可接受的盐; 化合物及其盐可用作抗生素。

7. 发明授权

US4016263A N-Substituted erythromcylamines and salts thereof 失效
公开(公告)号：US4016263A
公开(公告)日：1977-04-05
申请号：US671422
申请日：1976-03-29
申请人： Bernd Wetzel , Eberhard Woitun , Roland Maier , Wolfgang Reuter , Hanns Goeth , Uwe Lechner
发明人： Bernd Wetzel , Eberhard Woitun , Roland Maier , Wolfgang Reuter , Hanns Goeth , Uwe Lechner
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： Compounds of the formula ##STR1## wherein E is ##STR2## R.sub.1 is hydrogen; straight or branched alkyl of 1 to 3 carbon atoms; (alkoxy of 1 to 5 carbon atoms)-(alkyl of 1 to 3 carbon atoms); phenyl; or benzyl;R.sub.2 is hydrogen; hydroxyl; straight or branched alkyl of 1 to 3 carbon atoms; or phenyl;R.sub.3 is hydroxyl; alkanoyloxy of 1 to 5 carbon atoms; benzoyloxy; straight or branched alkoxy of 1 to 5 carbon atoms; amino; mono(alkyl of 1 to 5 carbon atoms)-amino; dialkyl-amino, where the sum of carbon atoms in the alkyls is from 2 to 8, inclusive; mono(hydroxy-alkyl of 1 to 4 carbon atoms) -amino; di(hydroxy-alkyl)-amino, where the sum of carbon atoms in the alkyls is from 2 to 8, inclusive; phenyl(alkyl of 1 to 2 carbon atoms)-amino; phenyl-amino, where the phenyl moiety may optionally have one or more halogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or hydroxyl substituents attached thereto; (alkanoyl of 1 to 5 carbon atoms)-amino; phenyl(alkanoyl of 1 to 5 carbon atoms)-amino; benzoyl-amino; methoxybenzoyl-amino; halobenzoyl-amino; carboxybenzoyl-amino; p-tolylsulfonamino; -HN-NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are alkyl of 1 to 3 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a 5- to 6-membered heterocycle optionally comprising an additional oxygen, sulfur or nitrogen heteroatom in the ring, and said additional nitrogen heteroatom optionally having an alkyl of 1 to 5 carbon atoms substituent attached thereto; ##STR3## where R.sub.6 is amino; mono(straight or branched alkyl of 1 to 8 carbon atoms)-amino; dialkylamino, where the sum of carbon atoms in the alkyls is from 2 to 6, inclusive; cyclohexyl-amino; N-(alkyl of 1 to 3 carbon atoms)-N-cyclohexyl-amino; dicyclohexyl-amino; methoxy(alkyl of 1 to 3 carbon atoms)-amino; di-methoxy(alkyl of 1 to 3 carbon atoms)-amino; benzyl-amino, where the phenyl moiety may optionally have from one to three (alkoxy of 1 to 3 carbon atoms)-substituents attached thereto; phenethyl-amino, where the phenyl moiety may optionally have from one to three(alkoxy of 1 to 3 carbon atoms)-substituents attached thereto; dibenzyl-amino; di(phenethyl)-amino; benzhydrylamino; N-methyl-N-benzyl-amino; N-phenyl-N-benzyl-amino; N-methyl-N-phenyl-amino; N-ethyl-N-phenyl-amino; piperidino; methyl-piperidino; benzyl-piperidino; pyrrolidino; methyl-pyrrolidino; benzyl-pyrrolidino; morpholino; methyl-morpholino; benzyl-morpholino; piperazino; methyl-piperazino; benzyl-piperazino; hexamethyleneimino; methyl-hexamethyleneimino; benzyl-hexamethyleneimino; thiomorpholino; methyl-thiomorpholino; benzyl-thiomorpholino; heptamethyleneimino; methyl-heptamethyleneimino; or benzyl-heptamethylimino; andR.sub.7 is amino; cyclohexylamino; di(alkyl of 1 to 3 carbon atoms)-amino; benzyl-amino; phenethyl-amino; dibenzyl-amino; phenoxy-methyl-amino; phenoxyethyl-amino; N-phenyl-N-benzyl-amino; N-methyl-N-phenyl-amino; piperidino, benzyl-piperidino; pyrrolidino; benzyl-pyrrolidino; morpholino; benzyl-morpholino; piperazino; benzyl-piperazino; thiomorpholino; benzyl-thiomorpholino; hexamethyleneimino; benzyl-hexamethyleneimino; hydrogen; alkyl of 1 to 3 carbon atoms; cyclohexyl, benzyl, methoxy-benzyl; phenethyl; methoxyphenethyl; thienyl; furyl; pyridyl; (alkyl of 1 to 3 carbon atoms)-thio; methoxy(alkyl of 1 to 3 carbon atoms)-thio; cyano(alkyl of 1 to 3 carbon atoms)-thio; benzyl-thio; methylbenzyl-thio; phenyl-thio; or tolyl-thio;R.sub.3 = is also NH-A-B, where A is alkylene of 1 to 4 carbon atoms; and B is alkoxy of 1 to 3 carbon atoms, di(alkyl of 1 to 3 carbon atoms)-amino or carbalkoxy of 2 to 4 carbon atoms;thiazolyl-amino; orpyridyl-amino; andn is 0 or 1;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antibacterials.

8. 发明授权

US4388315A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4388315A
公开(公告)日：1983-06-14
申请号：US307117
申请日：1981-09-30
申请人： Bernd Wetzel , Eberhard Woitun , Roland Maier , Wolfgang Reuter , Uwe Lechner , Hanns Goeth
发明人： Bernd Wetzel , Eberhard Woitun , Roland Maier , Wolfgang Reuter , Uwe Lechner , Hanns Goeth
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D239/46 , C07D501/20 , C07D501/36 , C07D501/57
CPC分类号： C07D239/47 , Y02P20/55
摘要： Cephalosporins of the formula ##STR1## wherein A is phenyl, 4-hydroxyphenyl, cyclohexyl, cyclohexene-1-yl, cyclohexa-1,4-diene-1-yl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl or 3,4-disubstituted phenyl, where the substituents, which may be identical to or different from each other, are each chlorine, hydroxyl or methoxy;Y is hydrogen or methoxy;D is hydrogen, hydroxyl, acetoxy, aminocarbonyloxy, pyridinium, aminocarbonyl-pyridinium or the group S-Het, where Het is 1-methyl-tetrazol-5-yl, tetrazol-5-yl, 3-methyl-1,2,4-thiadiazol-5-yl,1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 2-methylamino-1,3,4-thiadiazol-5-yl, 2-dimethylamino-1,3,4-thiadiazol-5-yl, 2-formylamino-1,3,4-thiadiazol-5-yl, 2-acetylamino-1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-oxadiazol-5-yl, 1,2,3-triazol-4-yl or 1,2,4-triazol-3-yl;R is hydrogen, methyl, cyclopropyl, hydroxyl, methoxy, ethoxy, mercapto, morpholino, thiomorpholino, thiomorpholino-S-oxide, thiomorpholino-S,S-dioxide, ##STR2## E is hydrogen or a protective group which is easily removable in vitro or in vivo;and non-toxic, pharmacologically acceptable salts thereof.
摘要翻译：其中A为苯基，4-羟基苯基，环己基，环己烯-1-基，环己-1,4-二烯-1-基，2-噻吩基，3-噻吩基，2-呋喃基，3-甲氧基苯基，呋喃基或3,4-二取代的苯基，其中可以相同或不同的取代基各自为氯，羟基或甲氧基; Y是氢或甲氧基; D是氢，羟基，乙酰氧基，氨基羰基氧基，吡啶鎓，氨基羰基 - 吡啶鎓或S-Het基团，其中Het是1-甲基 - 四唑-5-基，四唑-5-基，3-甲基-1,2,4- 噻二唑-5-基，1,2,4-噻二唑-5-基，1,3,4-噻二唑-5-基，2-甲基-1,3,4-噻二唑-5-基，2-甲基氨基 -1,3,4-噻二唑-5-基，2-二甲基氨基-1,3,4-噻二唑-5-基，2-甲酰氨基-1,3,4-噻二唑-5-基，2-乙酰基氨基-1 ，3,4-噻二唑-5-基，2-甲基-1,3,4-恶二唑-5-基，1,2,3-三唑-4-基或1,2,4-三唑-3-基 ; R是氢，甲基，环丙基，羟基，甲氧基，乙氧基，巯基，吗啉代，硫代吗啉代，硫代吗啉代S-氧化物，硫代吗啉代-S，S-二氧化物，E是氢或保护基，在体外或体内容易移除; 和无毒的药理学上可接受的盐。

9. 发明授权

US4048306A Aldehyde-erythromycylamine condensation products 失效
标题翻译：醛 - 红霉素缩合产物
公开(公告)号：US4048306A
公开(公告)日：1977-09-13
申请号：US671421
申请日：1976-03-29
申请人： Roland Maier , Eberhard Woitun , Bernd Wetzel , Wolfgang Reuter , Hanns Goeth , Uwe Lechner
发明人： Roland Maier , Eberhard Woitun , Bernd Wetzel , Wolfgang Reuter , Hanns Goeth , Uwe Lechner
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07D295/145 , C07F9/6558 , C07F9/6561 , C07H17/08
CPC分类号： C07D295/145 , C07F9/65586 , C07F9/6561 , C07H17/08
摘要： The invention relates to novel erythromycin derivatives, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as antibacterials.
摘要翻译：本发明涉及新型的红霉素衍生物及其无毒的药学上可接受的酸加成盐。化合物以及盐可用作抗细菌剂。

10. 发明授权

US4415566A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4415566A
公开(公告)日：1983-11-15
申请号：US191423
申请日：1980-09-26
申请人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
发明人： Bernd Wetzel , Eberhard Woitun , Wolfgang Reuter , Roland Maier , Uwe Lechner , Hanns Goeth
IPC分类号： C07D499/66 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D239/36 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D239/36 , C07D499/00 , Y02P20/55
摘要： Penicillins and cephalosporins of the formula ##STR1## wherein A is phenyl, 4-hydroxyphenyl, cyclohexyl, cyclohene-1-yl, cyclohexa-1,4-diene-1-yl, 2-thienyl, 3-thienyl, 2-furyl, 3-furyl or 3,4-disubstituted phenyl, where the substituents, which may be identical to or different from each other, are each chlorine, hydroxyl or methoxy;R.sub.1 is an unsubstituted or substituted 5- or 6-membered heterocycle comprising carbon atoms and 1 to 4, preferably 1 to 2, identical or different heteroatoms such as oxygen, sulfur or nitrogen;n is 0 or 1;X is ##STR2## D is hydrogen, hydroxyl, acetoxy, aminocarbonyloxy, pyridinium, aminocarbonyl-pyridinium or S-Het, where Het is 1-methyl-tetrazol-5-yl, tetrazol-5-yl, 3-methyl-1,2,4-thiadiazol-5-yl, 1,2,4-triadiazol-5-yl, 1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-thiadiazol-5-yl, 2-methylamino-1,3,4-thiadiazol-5-yl, 2-dimethylamino-1,3,4-thiadiazol-5-yl, 2-formylamino-1,2,4-thiadiazol-5-yl, 2-acetylamino-1,3,4-thiadiazol-5-yl, 2-methyl-1,3,4-oxadiazol-5-yl, 1,2,3-triazol-4-yl or 1,2,4-triazol-3-yl; andE is hydrogen or a protective group which is easily removable in nitro or in vivo, especially an ester-forming group which can be removed under mild conditions by hydrogenation or hydrolysis or other treatments, or an ester-forming group which can easily be split off in the living organism;and, when E is hydrogen, their non-toxic, pharmacologically acceptable salts thereof, such as their alkali metal or alkaline earth metal salts, especially the sodium, potassium, magnesium or calcium salts; their ammonium salts; or their organic amine salts, especially the triethylamine or dicyclohexylamine salts. The compounds are useful as antibiotics.
摘要翻译：其中A是苯基，4-羟基苯基，环己基，环烯-1-基，环己-1,4-二烯-1-基，2-噻吩基，3-噻吩基，2-呋喃基， 3-呋喃基或3,4-二取代的苯基，其中可以相同或不同的取代基各自为氯，羟基或甲氧基; R1是包含碳原子和1至4个，优选1至2个相同或不同的杂原子如氧，硫或氮的未取代或取代的5或6元杂环; n为0或1; X是H，羟基，乙酰氧基，氨基羰基氧基，吡啶鎓，氨基羰基 - 吡啶鎓或S-Het，其中Het是1-甲基 - 四唑-5-基，四唑-5-基，3-甲基-1- 2,4-噻二唑-5-基，1,2,4-三唑-5-基，1,3,4-噻二唑-5-基，2-甲基-1,3,4-噻二唑-5-基， 2-甲基氨基-1,3,4-噻二唑-5-基，2-二甲基氨基-1,3,4-噻二唑-5-基，2-甲酰氨基-1,2,4-噻二唑-5-基，2- 乙酰氨基-1,3,4-噻二唑-5-基，2-甲基-1,3,4-恶二唑-5-基，1,2,3-三唑-4-基或1,2,4-三唑-4-基，吡啶-3-基; E是氢或在硝基或体内容易除去的保护基团，特别是可在温和条件下通过氢化或水解或其它处理方法除去的酯形成基团或易于分解的酯形成基团在有机体中脱落; 并且当E是氢时，其无毒的药学上可接受的盐，例如它们的碱金属或碱土金属盐，特别是钠，钾，镁或钙盐; 其铵盐; 或它们的有机胺盐，特别是三乙胺或二环己基胺盐。该化合物可用作抗生素。

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