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1. 发明授权

US5417862A Process for inactivating the biological activity of DNA 失效
标题翻译：灭活DNA生物活性的方法
公开(公告)号：US5417862A
公开(公告)日：1995-05-23
申请号：US942057
申请日：1992-09-08
申请人： Klaus Bergemann , Georg Bader , Wolfgang Berthold , Rolf-Gunter Werner
发明人： Klaus Bergemann , Georg Bader , Wolfgang Berthold , Rolf-Gunter Werner
IPC分类号： C02F1/02 , A61L2/00 , A61L2/04 , C02F1/50 , C12N1/08
CPC分类号： A61L2/0088 , C12N1/08
摘要： A process for inactivating the biological activity of DNA, especially recombinant DNA, is disclosed. The process includes the step of heating the DNA at 60.degree. to 100.degree. C. in the presence of an acid other than percarboxylic acid at a concentration of at least 0.2 mM and a pH value of maximum 4, preferably 3.
摘要翻译：公开了一种灭活DNA，特别是重组DNA的生物活性的方法。该方法包括在至少0.2mM的浓度和最大值4，优选3的pH下，在不同于过羧酸的酸存在下，在60℃至100℃下加热DNA的步骤。

2. 发明授权

US4409220A Fused-ring amino-pyrazines as bradycardiac agents 失效
标题翻译：稠环氨基吡嗪作为心动过缓剂
公开(公告)号：US4409220A
公开(公告)日：1983-10-11
申请号：US297024
申请日：1981-08-27
申请人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
发明人： Rudolf Hurnaus , Gerhart Griss , Robert Sauter , Wolfgang Grell , Walter Kobinger , Ludwig Pichler
IPC分类号： A61K31/495 , A61K31/55 , A61P9/02 , A61P9/06 , A61P9/12 , A61P25/02 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要翻译：其中A和B可以相同或不同，各自表示亚甲基，（1至3个碳原子的烷基） - 亚甲基，亚乙基或（1至3个碳原子的烷基） - 亚乙基; R 1是氢，1至6个碳原子的烷基，3至7个碳原子的环烷基，3至6个碳原子的烯基，苯基 - （1至3个碳原子的烷基），卤代苯基 - （1至3个碳原子的烷基），1〜3个碳原子的烷酰基，1〜3个碳原子的苯基 - （烷酰基），1〜3个碳原子的卤代苯基 - （烷酰基），2〜4个碳原子的烷氧基羰基，8〜10个碳原子的芳烷氧羰基，苯基; R2和R3中的一个是氨基，另一个是氢，氯，溴，1至3个碳原子的烷基，1至3个碳原子的烷氧基，2至4个碳原子的烷氧基羰基，苯基或卤代苯基; 和无毒的，药学上可接受的酸加成盐。化合物及其盐可用作心动过缓。

3. 发明授权

US4379788A 2-Phenyl-pyrimidones 失效
标题翻译： 2-苯基 - 嘧啶酮
公开(公告)号：US4379788A
公开(公告)日：1983-04-12
申请号：US327348
申请日：1981-12-04
申请人： Joachim Heider , Volkhard Austel , Wolfgang Eberlein , Rudolf Kadatz , Christian Lillie
发明人： Joachim Heider , Volkhard Austel , Wolfgang Eberlein , Rudolf Kadatz , Christian Lillie
IPC分类号： C07D239/88 , A61K31/513 , A61P9/00 , C07D213/82 , C07D239/91 , C07D265/22 , C07D471/04 , C07D498/04 , A61K31/505
CPC分类号： C07D213/82 , C07D239/91 , C07D265/22 , C07D471/04
摘要： Compounds of the formula ##STR1## wherein A and B, together with each other and the respective carbon atoms to which they are attached, form a phenyl or pyridine ring;R.sub.1 is hydrogen, halogen, amino, nitro, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;R.sub.2 is hydrogen or alkoxy of 1 to 3 carbon atoms;D is alkylene of 3 to 4 carbon atoms or hydroxy(alkylene of 3 to 4 carbon atoms);R.sub.3 and R.sub.5, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.4 is hydrogen or alkoxy of 1 to 3 carbon atoms; andR.sub.6 is straight or branched alkyl of 1 to 6 carbon atoms or --E--R.sub.7 ;where E is straight alkylene of 2 to 4 carbon atoms or hydroxy-substituted straight alkylene of 2 to 4 carbon atoms, andR.sub.7 is ##STR2## where R.sub.8 and R.sub.9 are each hydrogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof formed with inorganic or organic acids; the compounds as well as their salts are useful as hypotensives, antiarrhythmics and .beta.-receptor-blockers.
摘要翻译：其中A和B与它们相连的相互连接的碳原子一起形成苯基或吡啶环; R 1是氢，卤素，氨基，硝基，1至3个碳原子的烷基或1至3个碳原子的烷氧基; R2是氢或1〜3个碳原子的烷氧基; D是3至4个碳原子的亚烷基或羟基（3至4个碳原子的亚烷基）; R 3和R 5可以相同或不同，分别为氢或1-3个碳原子的烷基; R4是氢或1〜3个碳原子的烷氧基; R6是1-6个碳原子的直链或支链烷基或-E-R7; 其中E是2至4个碳原子的直链亚烷基或2至4个碳原子的羟基取代的直链亚烷基，并且R 7是R 8和R 9各自为氢，1至3个碳原子的烷基或1至 3个碳原子; 和与无机或有机酸形成的无毒的，药学上可接受的酸加成盐; 化合物及其盐可用作低血糖，抗心律失常药和β-受体阻滞剂。

4. 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。

5. 发明授权

US4361563A Pyridazinone-substituted benzimidazoles and salts 失效
标题翻译：哒嗪酮取代的苯并咪唑和盐
公开(公告)号：US4361563A
公开(公告)日：1982-11-30
申请号：US259537
申请日：1981-05-01
申请人： Volkhard Austel , Joachim Heider , Wolfgang Eberlein , Willi Diederen , Walter Haarmann
发明人： Volkhard Austel , Joachim Heider , Wolfgang Eberlein , Willi Diederen , Walter Haarmann
IPC分类号： A61K31/50 , C07D235/18 , C07D237/04 , C07D403/04
CPC分类号： C07D237/04 , A61K31/50 , C07D235/18 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; trifluoromethyl; alkyl of 1 to 11 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; hydroxyl; alkoxy of 1 to 6 carbon atoms; mercapto; (alkyl of 1 to 6 carbon atoms)-mercapto; phenyl-(alkyl of 1 to 3 carbon atoms); phenyl; or mono-, di- or tri-substituted phenyl, where the substituents, which may be identical to or different from each other, are each halogen, alkyl of 1 to 4 carbon atoms, (alkyl of 1 to 6 carbon atoms)-sulfinyl, hydroxyl, alkoxy of 1 to 6 carbon atoms, mercapto or (alkyl of 1 to 6 carbon atoms)-mercapto;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms or phenyl-(alkyl of 1 to 3 carbon atoms); andR.sub.3 is alkyl of 1 to 6 carbon atoms; optically active antipodes thereof; and non-toxic, pharmaceutically acceptable acid addition salts of said compounds or of said optically active antiposed. The compounds are useful as cardiotonics and antithrombotics.
摘要翻译：其中R 1是氢的式IMAMA的化合物; 三氟甲基 1至11个碳原子的烷基; 3至7个碳原子的环烷基; 羟; 1至6个碳原子的烷氧基; 巯基（1-6个碳原子的烷基） - 巯基; 苯基 - （1至3个碳原子的烷基）; 苯基; 或单取代，二取代或三取代的苯基，其中可以相同或不同的取代基各自为卤素，具有1至4个碳原子的烷基，（1至6个碳原子的烷基） - 亚磺酰基，羟基，1至6个碳原子的烷氧基，巯基或（1至6个碳原子的烷基） - 巯基; R2是氢，1至6个碳原子的烷基，3至6个碳原子的环烷基或苯基 - （1至3个碳原子的烷基）; 且R 3为1至6个碳原子的烷基; 光学活性对映体; 和所述化合物或所述光学活性药物的无毒的药学上可接受的酸加成盐。这些化合物可用作强心剂和抗血栓药物。

6. 发明授权

US4353909A 6-Hydroxy-2-phenyl-imidazo[4,5-b]pyridines and salts thereof 失效
标题翻译： 6-羟基-2-苯基 - 咪唑并[4,5-b]吡啶及其盐
公开(公告)号：US4353909A
公开(公告)日：1982-10-12
申请号：US305159
申请日：1981-09-24
申请人： Willi Diederen , Axel Prox , Albert Reuter , Willy Roth , Jochen Schmid
发明人： Willi Diederen , Axel Prox , Albert Reuter , Willy Roth , Jochen Schmid
IPC分类号： A61K31/435 , A61P9/04 , C07D471/04 , A61K31/44 , C07D487/04
CPC分类号： C07D471/04
摘要： Compounds of the formula ##STR1## wherein R is methylsulfinyl or methylsulfonyl, their 3H-tautomers, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.
摘要翻译：其中R是甲基亚磺酰基或甲基磺酰基，其3H-互变异构体和无毒的药理学上可接受的酸加成盐的式IMA化合物。这些化合物可用作强心剂。

7. 发明授权

US4442111A Antithrombotic sulfimino and sulfoximino indolinones-2 失效
标题翻译：抗血栓形成亚硫酰亚氨基和磺酰肟基吲哚啉酮-2
公开(公告)号：US4442111A
公开(公告)日：1984-04-10
申请号：US395631
申请日：1982-07-06
申请人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
发明人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
IPC分类号： A61K31/40 , A61K31/455 , A61K31/47 , C07D209/34 , C07D215/22 , C07D215/227 , C07D401/02 , C07D401/12 , C07D409/02 , C07D409/12
CPC分类号： C07D215/227 , C07D209/34 , C07D401/12 , C07D409/12
摘要： Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.
摘要翻译：其中n为0或1的式（I）的化合物; A是任选被低级烷基取代的亚甲基，亚乙烯基或乙烯基; B是亚烷基; R1是任选取代的烷基，苯基或萘基，或环烷基或吡啶基; 并且R 2是氢或酰基; 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血栓形成剂。

8. 发明授权

US4421755A Method of treating coronary heart disease with imidazo(4,5-B)pyridines 失效
标题翻译：用咪唑并（4,5-B）吡啶治疗冠心病的方法
公开(公告)号：US4421755A
公开(公告)日：1983-12-20
申请号：US349838
申请日：1982-02-18
申请人： Lothar Benedikter , Eberhard Kutter
发明人： Lothar Benedikter , Eberhard Kutter
IPC分类号： C07D471/04 , A61K31/435 , A61K31/44 , A61P9/08 , A61P9/10
CPC分类号： A61K31/44
摘要： Pharmaceutical compositions containing, as an active ingredient, a compound of the formula ##STR1## wherein R.sub.1 is alkoxy of 1 to 4 carbon atoms, and R.sub.2 is (alkyl of 1 to 4 carbon atoms) sulfinyl, or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same for the treatment of coronary heart diseases or coronary spasms.
摘要翻译：含有下式的化合物作为活性成分的药物组合物，其中R1是1-4个碳原子的烷氧基，R2是（1至4个碳原子的烷基）亚磺酰基，或无毒的药学上可接受的其酸加成盐; 以及使用该方法治疗冠心病或冠状动脉痉挛的方法。

9. 发明授权

US4560685A 2-Piperazino-pteridines useful as antithrombotics and antimetastatics 失效
标题翻译： 2-Piperazino-pteridines可用作抗血栓形成和抗转移
公开(公告)号：US4560685A
公开(公告)日：1985-12-24
申请号：US621438
申请日：1984-06-18
申请人： Josef Roch , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Rainer Zimmermann , Walter Haarmann
发明人： Josef Roch , Josef Nickl , Erich Muller , Berthold Narr , Johannes Weisenberger , Rainer Zimmermann , Walter Haarmann
IPC分类号： C07D475/06 , C07D475/08 , A61K31/505
CPC分类号： C07D475/06 , C07D475/08
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is phenylalkylamino, alkylamino, dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino;R.sub.2 is dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; andR.sub.3 is halogen, alkoxy, alkylthio, phenylalkoxy or phenylalkylthio;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics and antimetastatics.
摘要翻译：其中R 1是苯基烷基氨基，烷基氨基，二烷基氨基，哌啶子基，吗啉代，硫代吗啉代或1-氧代硫代吗啉代; R2是二烷基氨基，哌啶子基，吗啉代，硫代吗啉代或1-氧代硫代吗啉代; R3是卤素，烷氧基，烷硫基，苯基烷氧基或苯基烷硫基; 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血栓形成和抗转移酶。

10. 发明授权

US4551464A Antithrombotic sulfoximino carbostyrils 失效
标题翻译：抗血栓形式的磺酰亚胺喹诺酮类
公开(公告)号：US4551464A
公开(公告)日：1985-11-05
申请号：US573964
申请日：1984-01-26
申请人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
发明人： Erich Muller , Josef Nickl , Berthold Narr , Josef Roch , Walter Haarmann , Johannes M. Weisenberger
IPC分类号： A61K31/40 , A61K31/455 , A61K31/47 , C07D209/34 , C07D215/22 , C07D215/227 , C07D401/02 , C07D401/12 , C07D409/02 , C07D409/12
CPC分类号： C07D215/227 , C07D209/34 , C07D401/12 , C07D409/12
摘要： Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.
摘要翻译：其中n为0或1的式（I）的化合物; A是任选被低级烷基取代的亚甲基，亚乙烯基或乙烯基; B是亚烷基; R1是任选取代的烷基，苯基或萘基，或环烷基或吡啶基; 并且R 2是氢或酰基; 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血栓形成剂。

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