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11. 发明授权

US5231103A Quinolin-2-yl-methoxybenzylhydroxyureas 失效
标题翻译：喹啉-2-基 - 甲氧基苯甲醛
公开(公告)号：US5231103A
公开(公告)日：1993-07-27
申请号：US917641
申请日：1992-07-21
申请人： Michael Matzke , Klaus-Helmut Mohrs , Siegfried Raddatz , Romanis Fruchtmann , Armin Hatzelmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen-Popp
发明人： Michael Matzke , Klaus-Helmut Mohrs , Siegfried Raddatz , Romanis Fruchtmann , Armin Hatzelmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen-Popp
IPC分类号： A61K31/47 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/14 , C07D215/16 , C07D215/20 , C07D215/48
CPC分类号： C07D215/14
摘要： The novel quinolin-2-yl-methoxybenzylhydroxyureas can be prepared by reaction of appropriate ketones with hydroxylamine and reduction of the ketoximes and subsequent reaction with isocyanates. The new substances can be employed as active substances in medicaments.
摘要翻译：该新型喹啉-2-基 - 甲氧基苄基羟基脲可以通过使适当的酮与羟胺反应并还原酮肟并随后与异氰酸酯反应来制备。新物质可用作药物中的活性物质。

12. 发明授权

US5399698A Quinolin-2-yl-methoxybenzylhydroxyureas 失效
标题翻译：喹啉-2-基 - 甲氧基苄基羟基脲
公开(公告)号：US5399698A
公开(公告)日：1995-03-21
申请号：US18669
申请日：1993-02-17
申请人： Michael Matzke , Klaus-Helmut Mohrs , Siegfried Raddatz , Romanis Fruchtmann , Armin Hatzelmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen-Popp
发明人： Michael Matzke , Klaus-Helmut Mohrs , Siegfried Raddatz , Romanis Fruchtmann , Armin Hatzelmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen-Popp
IPC分类号： A61K31/47 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/00 , A61P17/00 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/14 , C07D215/16 , C07D215/20 , C07D215/48 , C07D215/06 , C07D215/12
CPC分类号： C07D215/14
摘要： The novel quinolin-2-yl-methoxybenzylhydroxyureas can be prepared by reaction of appropriate ketones with hydroxylamine and reduction of the ketoximes and subsequent reaction with isocyanates. The new substances can be employed as active substances in medicaments.
摘要翻译：该新型喹啉-2-基 - 甲氧基苄基羟基脲可以通过使适当的酮与羟胺反应并还原酮肟并随后与异氰酸酯反应来制备。新物质可用作药物中的活性物质。

13. 发明授权

US5391747A Substituted (quinolin-2-yl-methoxy)phenyl-acyl-sulphon-amides and -cyanamides, processes for their preparation and their use in medicaments 失效
标题翻译：取代的（喹啉-2-基 - 甲氧基）苯基 - 酰基 - 磺酰胺和氰胺，其制备方法及其在药物中的应用
公开(公告)号：US5391747A
公开(公告)日：1995-02-21
申请号：US764435
申请日：1991-09-23
申请人： Siegfried Raddatz , Klaus-Helmut Mohrs , Romanis Fruchtmann , Christian Kohlsdorfer , Pia Theisen-Popp , Reiner Muller-Peddinghaus
发明人： Siegfried Raddatz , Klaus-Helmut Mohrs , Romanis Fruchtmann , Christian Kohlsdorfer , Pia Theisen-Popp , Reiner Muller-Peddinghaus
IPC分类号： C07D215/14 , C07D215/48 , C07D215/18 , C07D215/20 , C07D215/38
CPC分类号： C07D215/14
摘要： A (quinolin-2-yl-methoxy) phenylacyl-sulphonamide or -cyanamide of the formula ##STR1## and physiologically acceptable salts thereof. The (quinolin-2-yl-methoxy)phenylacylsulphonamide or -cyanamide is useful as an active compound in medicaments, particularly as a lipoxygenase inhibitor.
摘要翻译： A（喹啉-2-基 - 甲氧基）苯甲酰基 - 磺酰胺或 - 氰基酰胺及其生理学上可接受的盐。（喹啉-2-基 - 甲氧基）苯基酰基磺酰胺或氰基酰胺可用作药物中的活性化合物，特别是脂氧合酶抑制剂。

14. 发明授权

US5304563A 2-substituted quinolines, and their use in medicaments 失效
标题翻译： 2-取代喹啉及其在药物中的用途
公开(公告)号：US5304563A
公开(公告)日：1994-04-19
申请号：US967881
申请日：1992-10-28
申请人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen-Popp
发明人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Christian Kohlsdorfer , Reiner Muller-Peddinghaus , Pia Theisen-Popp
IPC分类号： C07D215/14 , C07D401/12 , C07D403/06 , A61K31/47 , A61K31/505 , C07D215/48
CPC分类号： C07D401/12 , C07D215/14
摘要： The title compounds are prepared either by reacting the corresponding halogenomethylquinolines with substituted phenols, optionally subsequently alkylating these or hydrolysing esters to acids, or by reacting phenyl-substituted quinolinecarboxylic acid derivatives with sulphonamides. The new phenyl-substituted quinolines are utilizable as active substances in medicaments, in particular as lipoxygenase inhibitors.
摘要翻译：标题化合物可以通过使相应的卤代甲基喹啉与取代的苯酚反应，任选地将这些或水解酯酸化为酸，或者使苯基取代的喹啉羧酸衍生物与磺酰胺反应来制备。新的苯基取代的喹啉可用作药物中的活性物质，特别是作为脂氧合酶抑制剂。

15. 发明授权

US5288733A Quinolylmethoxyphenylacetic acid acylamides and ureas 失效
标题翻译：醌基甲氧基苯乙酸酰胺和脲
公开(公告)号：US5288733A
公开(公告)日：1994-02-22
申请号：US979756
申请日：1992-11-23
申请人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Reiner Muller-Peddinghaus
发明人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Reiner Muller-Peddinghaus
IPC分类号： A61K31/47 , A61P9/00 , A61P11/00 , A61P37/08 , A61P43/00 , C07D215/14 , C07D215/16 , C07D215/48
CPC分类号： C07D215/14
摘要： Quinolylmethoxyphenylacetic acid acylamides and ureas can be prepared either by reacting corresponding carboxylic acids with amides or reacting corresponding amides with isocyanates or ureas. The quinolylmethoxyphenylacetic acid acylamides or ureas can be used as active compounds in medicaments.
摘要翻译：喹喔啉基甲氧基苯基乙酸酰胺和脲可以通过使相应的羧酸与酰胺反应或使相应的酰胺与异氰酸酯或脲反应来制备。喹喔啉基甲氧基苯乙酸酰胺或脲可用作药物中的活性化合物。

16. 发明授权

US5283252A Thiazolyl-substituted quinolylmethoxyphenylacetic acid derivatives 失效
标题翻译：噻唑基取代的喹啉基甲氧基苯基乙酸衍生物
公开(公告)号：US5283252A
公开(公告)日：1994-02-01
申请号：US979755
申请日：1992-11-23
申请人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Reiner Muller-Peddinghaus
发明人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Reiner Muller-Peddinghaus
IPC分类号： A61K31/47 , A61P43/00 , C07D215/14 , C07D417/12 , C07D521/00 , C07D417/10 , A61K31/425
CPC分类号： C07D231/12 , C07D215/14 , C07D233/56 , C07D249/08 , C07D417/12
摘要： Thiazolyl-substituted quinolylmethoxyphenylacetic acid derivatives are prepared by reaction of halogenoacetoacetic acid esters with quinolylmethoxyphenylacetic acid thioamides, which are obtainable from corresponding amides with Lawesson's reagent. The substances can be employed in medicaments as inhibitors of enzymatic reactions in the context of arachidonic acid metabolism.
摘要翻译：噻唑基取代的喹啉基甲氧基苯基乙酸衍生物通过卤代乙酰乙酸酯与喹喔啉基甲氧基苯基乙酸硫代酰胺的反应来制备，可用相应的酰胺与Lawesson's试剂得到。在花生四烯酸代谢的情况下，这些物质可以用作药物中的酶反应抑制剂。

17. 发明授权

US5310744A Quinolylmethoxyphenyl-acetamides 失效
标题翻译：醌基甲氧基苯基 - 乙酰胺
公开(公告)号：US5310744A
公开(公告)日：1994-05-10
申请号：US979745
申请日：1992-11-23
申请人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Reiner Muller-Peddinghaus
发明人： Siegfried Raddatz , Klaus-Helmut Mohrs , Michael Matzke , Romanis Fruchtmann , Armin Hatzelmann , Reiner Muller-Peddinghaus
IPC分类号： A61K31/47 , A61K31/495 , A61K31/535 , A61P9/00 , A61P11/00 , A61P37/08 , C07D215/14 , C07D215/16 , C07D215/48
CPC分类号： C07D215/14
摘要： Quinolylmethoxyphenyl-acetamides of the formula: ##STR1## in which A, B, D, E, G, L and M are hydrogen, hydroxyl, halogen, cyano, carboxyl, nitro, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy or optionally substituted aryl;R.sub.1 represents optionally substituted cycloalkyl; andR.sub.2 and R.sub.3 independently represent hydrogen, alkyl, benzyl, or optionally substituted cycloalkyl; or together represent piperidinyl, morpholino, or piperazinyl;show a high in vitro activity as leukotriene synthesis inhibitors and, therefore, are suitable for the treatment and prevention of inflammations.
摘要翻译：其中A，B，D，E，G，L和M是氢，羟基，卤素，氰基，羧基，硝基，三氟甲基，三氟甲氧基，烷基，烷氧基或任选取代的芳基的下式的醌基甲氧基苯基 - 乙酰胺： R1代表任选取代的环烷基; 并且R 2和R 3独立地表示氢，烷基，苄基或任选取代的环烷基; 或一起代表哌啶基，吗啉代或哌嗪基; 作为白细胞三烯合成抑制剂显示高体外活性，因此适用于治疗和预防炎症。

18. 发明授权

US5070096A Quinolinoxy phenylsulphonamides 失效
标题翻译：喹啉氧基苯酚
公开(公告)号：US5070096A
公开(公告)日：1991-12-03
申请号：US614329
申请日：1990-11-15
申请人： Klaus Mohrs , Elisabeth Perzborn , Friedel Seuter , Romanis Fruchtmann , Christian Kohlsdorfer
发明人： Klaus Mohrs , Elisabeth Perzborn , Friedel Seuter , Romanis Fruchtmann , Christian Kohlsdorfer
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4418 , A61K31/47 , A61K31/472 , A61P3/00 , A61P7/02 , A61P9/08 , A61P9/10 , A61P29/00 , A61P37/08 , C07D213/38 , C07D213/74 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/22 , C07D215/227 , C07D215/26 , C07D215/38 , C07D217/02 , C07D217/14 , C07D217/22
CPC分类号： C07D213/74 , C07D213/38 , C07D215/14 , C07D215/20 , C07D215/227 , C07D215/26
摘要： New phenylsulphonamide of the formula in which ##STR1## R.sup.1 represents a pyridyl, quinolyl or isoquinolyl radical which is unsubstituted or substituted by halogen, alkyl, cycloalkyl, alkoxy, cyano, nitro, halogenoalkyl, halogenoalkoxy, alkoxycarbonyl or alkylsulphonyl,R.sup.2 represents hydrogen, cyano, nitro, halogen, alkyl, alkoxy, halogenoalkyl, halogenoalkoxy or alkoxycarbonyl,R.sup.3 represents an aryl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted by halogen, halogenoalkyl, halogenoalkoxy, alkyl, alkoxy, alkylthio, alkylsulphonyl, cyano, nitro or alkoxycarbonyl, the substituents being identical or different, or represents pentafluorophenyl or represents a straight-chain, branched or cyclic alkyl which is unsubstituted or substituted by halogen, aryl, aryloxy, cyano, alkoxycarbonyl, alkoxy, alkylthio or trifluoromethyl, andX represents an --O--, --A--B-- or --B--A-- groupwhereA denotes --O--, ##STR2## and B denotes --CH.sub.2 -- or ##STR3## where R.sup.1 does not represent a pyridyl radical when x represents an --O-- group, and salts thereof are prepared by reacting appropriate amines with sulphonyl halides. The substituted phenylsulphonamides can be employed as active compounds for inhibiting enzymatic reactions and for inhibiting thrombocyte aggregations.
摘要翻译：新的具有下式的苯基磺酰胺，其中R 1表示未被取代或被卤素，烷基，环烷基，烷氧基，氰基，硝基，卤代烷基，卤代烷氧基，烷氧基羰基或烷基磺酰基取代的吡啶基，喹啉基或异喹啉基，R2表示氢，氰基，硝基，卤素，烷基，烷氧基，卤代烷基，卤代烷氧基或烷氧基羰基，R3表示未被取代或被卤素，卤代烷基，卤代烷氧基，烷基，烷氧基，烷硫基，烷基磺酰基，氰基，硝基取代或三取代的芳基或烷氧基羰基，取代基相同或不同，或表示五氟苯基，或表示未被取代或被卤素，芳基，芳氧基，氰基，烷氧基羰基，烷氧基，烷硫基或三氟甲基取代的直链，支链或环状烷基，X表示 -O-，-AB-或-BA-基团，其中A表示-O-，和B表示-CH2-或，其中R1不表示当x表示-O-基团时，是一个吡啶基，其盐可以通过使适当的胺与磺酰卤反应来制备。取代的苯基磺酰胺可用作抑制酶反应和抑制血小板聚集的活性化合物。

19. 发明授权

US4771062A Diaryl sulphide derivatives 失效
标题翻译：二芳基硫化物衍生物
公开(公告)号：US4771062A
公开(公告)日：1988-09-13
申请号：US18091
申请日：1987-02-20
申请人： Siegfried Raddatz , Hans Plumpe , Romanis Fruchtmann , Christian Kohlsdorfer , Bernhard Pelster
发明人： Siegfried Raddatz , Hans Plumpe , Romanis Fruchtmann , Christian Kohlsdorfer , Bernhard Pelster
IPC分类号： C07D277/18 , C07D277/38 , C07D277/42 , C07D279/06 , A61K31/425
CPC分类号： C07D279/06 , C07D277/18 , C07D277/42
摘要： A diaryl sulphide derivative of the formula ##STR1## in which R.sup.1 represents a thiazolamino radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, alkyl, aralkyl or acyl,R.sup.6 and R.sup.6 ' are identical or different and represent hydrogen, alkyl, aralkyl or aryl,R.sup.7 represents alkyl, cycloalkyl, aralkyl, acyl or aryl andn represents the number 1 or 2,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represent a group of the formula ##STR3## wherein R.sup.8 and R.sup.9 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, acyl, trifluoroacetyl, alkylsulphonyl, arylsulphonyl, trifluoromethylphenylsulphonyl or tolylsulphonyl andR.sup.4 has one of the abovementioned meanings or R.sup.1, or represents hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represents a group of the formula ##STR4## wherein R.sup.8 and R.sup.9 have the abovementioned meanings, and salts thereof. Such diaryl sulphide derivatives being useful as active compounds in the treatment and prevention of diseases of the respiratory tract and cardiovascular diseases.
摘要翻译：式（I）的二芳基硫化物衍生物，其中R 1表示下式的噻唑烷基：其中R 5表示氢，烷基，芳烷基或酰基，R 6和R 6'相同或不同代表氢，烷基，芳烷基或芳基，R7代表烷基，环烷基，芳烷基，酰基或芳基，n代表数字1或2，R2和R3相同或不同，代表氢，烷基，烯基，环烷基，烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，芳基，芳烷基，芳氧基，芳烷氧基，芳烷硫基，酰基，羧基，烷氧基羰基，羧基烷基，烷氧基羰基烷基，硝基，氰基或卤素，或表示下式的基团：其中R8和R9相同或代表氢，烷基，芳基，芳烷基，酰基，三氟乙酰基，烷基磺酰基，芳基磺酰基，三氟甲基苯磺酰基或甲苯磺酰基，R4具有上述含义之一或R 1，或表示氢，烷基，烯基，C 烷氧基，烷硫基，卤代烷基，卤代烷氧基，卤代烷硫基，芳基，芳烷基，芳氧基，芳烷氧基，芳烷硫基，酰基，羧基，烷氧基羰基，羧基烷基，烷氧基羰基烷基，硝基，氰基或卤素，或表示下式的基团其中R8 和R9具有上述含义及其盐。这种二芳基硫化物衍生物可用作活性化合物，用于治疗和预防呼吸道疾病和心血管疾病。

20. 发明授权

US5202336A Antiflammatory quinolin methoxy phenylsulphonamides 失效
标题翻译：抗炎喹啉甲氧基苯磺酰胺
公开(公告)号：US5202336A
公开(公告)日：1993-04-13
申请号：US729020
申请日：1991-07-12
申请人： Klaus Mohrs , Elisabeth Perzborn , Friedel Seuter , Romanis Fruchtmann , Christian Kohlsdorfer
发明人： Klaus Mohrs , Elisabeth Perzborn , Friedel Seuter , Romanis Fruchtmann , Christian Kohlsdorfer
IPC分类号： C07D213/38 , C07D213/74 , C07D215/14 , C07D215/20 , C07D215/22 , C07D215/227 , C07D215/26
CPC分类号： C07D213/74 , C07D213/38 , C07D215/14 , C07D215/20 , C07D215/227 , C07D215/26
摘要： New phenylsulphonamide of the formula in which ##STR1## R.sup.1 represents a pyridyl, quinolyl or isoquinolyl radical which is unsubstituted or substituted by halogen, alkyl, cycloalkyl, alkoxy, cyano, nitro, halogenoalkyl, halogenoalkoxy, alkoxycarbonyl or alkylsulphonyl,R.sup.2 represents hydrogen, cyano, nitro, halogen, alkyl, alkoxy, halogenoalkyl, halogenoalkoxy or alkoxycarbonyl,R.sup.3 represents an aryl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted by halogen, halogenoalkyl, halogenoalkoxy, alkyl, alkoxy, alkylthio, alkylsulphonyl, cyano, nitro or alkoxycarbonyl, the substituents being identical or different, or represents pentafluorophenyl or represents a straight-chain, branched or cyclic alkyl which is unsubstituted or substituted by halogen, aryl, aryloxy, cyano, alkoxycarbonyl, alkoxy, alkylthio or trifluoromethyl, andX represents an --O--, --A--B-- or --B--A-- group, whereA denotes ##STR2## and B denotes ##STR3## where R.sup.1 does not represent a pyridyl radical when X represents an --O-- group, and salts thereof are prepared by reacting appropriate amines with sulphonyl halides. The substituted phenylsulphonamides can be employed as active compounds for inhibiting enzymatic reactions and for inhibiting thrombocyte aggregations.
摘要翻译：新的具有下式的苯基磺酰胺，其中R1表示未被取代或被卤素，烷基，环烷基，烷氧基，氰基，硝基，卤代烷基，卤代烷氧基，烷氧基羰基或烷基磺酰基取代的吡啶基，喹啉基或异喹啉基，R2表示氢，氰基，硝基，卤素，烷基，烷氧基，卤代烷基，卤代烷氧基或烷氧基羰基，R3表示未被取代或被卤素，卤代烷基，卤代烷氧基，烷基，烷氧基，烷硫基，烷基磺酰基，氰基，硝基取代或三取代的芳基或烷氧基羰基，取代基相同或不同，或表示五氟苯基，或表示未被取代或被卤素，芳基，芳氧基，氰基，烷氧基羰基，烷氧基，烷硫基或三氟甲基取代的直链，支链或环状烷基，X表示 -O-，-AB-或-BA-基团，其中A表示，B表示，其中R1不表示吡啶基当X表示-O-基团时，其盐，其盐通过使适当的胺与磺酰卤反应制备。取代的苯基磺酰胺可用作抑制酶反应和抑制血小板聚集的活性化合物。

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