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1. 发明授权

US4454128A 6.alpha.-Methoxy-penicillins 失效
标题翻译： 6α-甲氧基青霉素
公开(公告)号：US4454128A
公开(公告)日：1984-06-12
申请号：US410007
申请日：1982-08-20
申请人： Bernd Wetzel , Wolfgang Eberlein , Gunter Trummlitz , Eberhard Woitun , Roland Maier , Wolfang Reuter , Uwe Lechner , Hanns Goeth
发明人： Bernd Wetzel , Wolfgang Eberlein , Gunter Trummlitz , Eberhard Woitun , Roland Maier , Wolfang Reuter , Uwe Lechner , Hanns Goeth
IPC分类号： C07D499/68 , A61K31/43 , A61K31/431 , A61P31/04 , C07D499/00 , C07D499/21 , C07D499/64 , A61K31/635 , A61K31/505 , C07D499/54
CPC分类号： C07D499/00
摘要： Compounds of the formula ##STR1## wherein A is phenyl, p=hydroxy-phenyl, 2-thienyl or 3-thienyl; andR represents substituents of various 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.
摘要翻译：其中A是苯基，p =羟基 - 苯基，2-噻吩基或3-噻吩基的式IMA化合物; R代表各种类型的取代基; 和与无机或有机碱形成的无毒的，药学上可接受的盐。化合物及其盐可用作抗生素。

2. 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。

3. 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。

4. 发明授权

US5178857A Pharmaceutical compositions and their use in the treatment of parasitoses 失效
标题翻译：药物组合物及其在治疗寄生虫药物中的应用
公开(公告)号：US5178857A
公开(公告)日：1993-01-12
申请号：US501812
申请日：1990-03-30
申请人： Hanns Goeth , Werner Frank , Ingeborg Renner
发明人： Hanns Goeth , Werner Frank , Ingeborg Renner
IPC分类号： A61K38/21 , A61K45/06
CPC分类号： A61K38/21
摘要： The present invention relates to pharmaceutical combinations containing IFN.gamma. and at least one anthelminthic, and the use thereof for treating parasitoses in mammals or in humans.
摘要翻译：本发明涉及含有IFNγ和至少一种anthelminthic的药物组合物及其用于治疗哺乳动物或人类寄生虫的用途。

5. 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。

6. 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。

7. 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.

8. 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。

9. 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.

10. 发明授权

US3937712A (5-Nitro-2-furyl)-pyridines 失效
标题翻译：（5-硝基-2-呋喃基） - 吡啶
公开(公告)号：US3937712A
公开(公告)日：1976-02-10
申请号：US473324
申请日：1974-05-28
申请人： Ludwig Schroder , Klaus Thomas , Hanns Goeth
发明人： Ludwig Schroder , Klaus Thomas , Hanns Goeth
IPC分类号： A61K31/44 , C07D405/04 , C07D213/44
CPC分类号： C07D405/04 , A61K31/44 , Y10S514/96 , Y10S514/969
摘要： Compounds of the formula ##SPC1##WhereinA is chlorine, alkoxy of 1 to 10 carbon atoms, dimethylamino-ethoxy or diethylamino-ethoxy, andR is hydrogen, alkyl of 1 to 4 carbon atoms or pyridyl;The compounds are useful as antimicrobial agents, especially against gramnegative microorganisms, for the treatment of infections of the intestinal and urogential tract.

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