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91. 发明公开

EP0625510A3 Novel N-alkylacridan carboxyl derivatives useful for chemiluminescent detection 失效
标题翻译：的N- Alkylacridancarboxylderivate，适合于检测化学发光的。
公开(公告)号：EP0625510A3
公开(公告)日：1997-03-05
申请号：EP94107632.5
申请日：1994-05-17
申请人： LUMIGEN, INC.
发明人： Akhavan-Tafti, Hashem , Desilva, Renuka , Sugioka, Katsuaki
IPC分类号： C07D219/04 , G01N33/58
CPC分类号： C12Q1/28 , C07D219/02 , C07D219/04 , C07D219/06 , Y10S435/81 , Y10S435/968
摘要： N-alkylacridan carboxylic acid derivative compounds (I) are used to generate chemiluminescence by the action of a peroxidase enzyme and an oxidant. The compounds I are useful in assays of all types.

92. 发明公开

EP0647628A1 Acridiniumderivate und ihre Verwendung in Lumineszenzimmunoassays 失效
标题翻译： Acridiniumderivate und ihre Verwendung in Lumineszenzimmunoassays。
公开(公告)号：EP0647628A1
公开(公告)日：1995-04-12
申请号：EP94119395.5
申请日：1987-08-19
申请人： HOECHST AKTIENGESELLSCHAFT
发明人： Molz, Peter, Dr. , Skrzipczyk, Heinz-Jürgen, Dr. , Lübbers, Henning, Dr. , Strecker, Helmut, Dr. , Schnorr, Gerd, Dr. , Kinkel, Tonio, Dr.
IPC分类号： C07D219/04 , G01N33/533 , C07D401/12 , G01N33/68
CPC分类号： C07D401/12 , C07D219/04 , G01N33/533 , G01N33/582
摘要： Gegenstand der Erfindung sind neuartige Acridiniumderivate der Formel I:

in der R¹ Wasserstoff, ein Alkyl-, Alkenyl- oder Alkinylrest mit 1 bis 10 Kohlenstoffatomen, eine Benzyl-, oder Arylgruppe ist, R² und R³ Wasserstoff, eine Alkylgruppe mit 1 bis 4 Kohlenstoffatomen, eine substituierte oder unsubstituierte Aminogruppe eine Carboxy-, C₁-C₄ Alkoxy-, Cyano-, Nitrogruppe oder Halogen sind, R⁴ einen Rest darstellt, in dem eine Sulfonamidgruppe über den Stickstoff direkt an die Carbonylgruppe gebunden ist und A ⊖ ein die Chemolumineszenz nicht beeinträchtigendes Anion ist; sowie ihre Verwendung in Lumineszenzimmunoassays.
Diese Verbindungen können vorteilhafterweise in Form von biologisch aktiven Konjugaten, z. B. in Immunolumineszenzassays als sogenannte "Label" eingesetzt werden.
摘要翻译：本发明涉及式I的新颖的吖啶鎓衍生物：其中R 1是氢，具有1至10个碳原子的烷基，烯基或炔基，苄基或芳基，R 2和R 3是氢，具有1至4个碳原子的烷基，取代或未取代的氨基，羧基，C 1 -C 4 - 烷氧基，氰基或硝基或卤素，R 4是其中磺酰胺基团通过氮直接键合到羰基上，A <（ - ）>是不影响化学发光的阴离子; 以及它们在发光免疫测定中的应用。

93. 发明授权

EP0369344B1 N-arylation of isatins 失效
标题翻译： isatines的N-芳基化。
公开(公告)号：EP0369344B1
公开(公告)日：1994-04-06
申请号：EP89120863.9
申请日：1989-11-10
申请人： ABBOTT LABORATORIES
发明人： Dombrowski, James E. , Mattingly, Phillip Gregory
IPC分类号： C07D209/38 , C07D219/04
CPC分类号： C07F9/94 , C07D209/38 , C07D209/60 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/18

94. 发明公开

EP0353971A3 Acridinium esters and method for detection of an analyte using acridinium esters and liposomes 失效
标题翻译：阿司匹林和使用阿司匹林和脂质体检测分析物的方法
公开(公告)号：EP0353971A3
公开(公告)日：1990-10-10
申请号：EP89307752.9
申请日：1989-07-31
申请人： Ciba Corning Diagnostics Corp.
发明人： Law, Say-Jong , Piran, Uri
IPC分类号： C07D219/04 , C07F9/64 , G01N33/53 , C12Q1/68
CPC分类号： G01N33/586 , C07D219/04 , C07F9/64 , C12Q1/6816 , C12Q2563/161
摘要： A lumisome characterised in that it comprises a liposome having encapsulated therein an acridinium ester is disclosed, as are certain acridinium esters and assay methods using same.

95. 发明公开

EP0282959A3 Substituted 9-amino-tetrahydro-acridines and related compounds, a process for their preparation and their use as medicaments 失效
标题翻译：取代的9-氨基四氢吡啶及其相关化合物，其制备方法及其作为药物的用途
公开(公告)号：EP0282959A3
公开(公告)日：1989-05-31
申请号：EP88104042.2
申请日：1988-03-15
申请人： HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED
发明人： Shutske, Gregory Michael , Helsley, Grover Cleveland
IPC分类号： C07D219/10 , C07D219/12 , C07D221/16 , A61K31/47 , C07C119/12 , C07D219/04 , C07D219/06
CPC分类号： C07D219/10 , C07D219/04 , C07D219/06
摘要： There are disclosed compounds having the formula
wherein n is 1-4; X is alkyl of 3-18 carbon atoms, cycloalkyl of 3-7 carbon atoms or cycloalkylloweralkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; R₁ is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
摘要翻译：公开了具有式CHEM的化合物，其中n为1-4; X是3-18个碳原子的烷基，3-7个碳原子的环烷基或环烷基低级烷基; R是氢，低级烷基或低级烷基羰基; R 1是氢，低级烷基，低级烷基羰基，芳基，二低级烷基氨基低级烷基，芳基低级烷基，二芳基低级烷基，氧桥连的芳基低级烷基或氧桥连的二芳基低级烷基。其立体异构体和其药学上可接受的酸加成盐，其可用于增强记忆，合成它们的方法和包含有效记忆增加量的这种化合物的药物组合物。

96. 发明公开

EP0154528A3 Alkene, alkyne or cycloalkylene derivatives 失效
标题翻译：烯烃，炔烃或环亚烷基衍生物
公开(公告)号：EP0154528A3
公开(公告)日：1989-01-04
申请号：EP85301414.0
申请日：1985-03-01
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Hughes, Leslie Richard , Oldfield, John , Tucker, Howard
IPC分类号： C07C49/248 , C07C33/48 , C07C255/49 , C07C255/37 , C07C317/00 , C07D521/00 , A61K31/33 , A61K31/10 , A61K31/12 , A61K31/275
CPC分类号： C07C17/23 , C07C17/278 , C07C33/483 , C07C33/50 , C07C45/26 , C07C45/54 , C07C45/72 , C07C45/74 , C07C47/273 , C07C49/235 , C07C49/245 , C07C49/248 , C07C59/56 , C07C205/26 , C07C205/45 , C07C255/00 , C07C317/00 , C07C323/00 , C07D213/34 , C07D213/57 , C07D213/61 , C07D213/70 , C07D213/71 , C07D215/14 , C07D215/36 , C07D219/04 , C07D233/84 , C07D239/38 , C07D239/47 , C07D239/56 , C07D249/12 , C07D251/38 , C07D277/24 , C07D277/36 , C07D303/08 , C07D333/28 , C07D333/38 , C07D333/44 , C07D339/06 , C07D473/24 , C07D473/38 , C07D487/04 , C07F7/0818 , C07C25/18
摘要： A compound of the formula
wherein X has the formula
wherein ring A is phenyl, naphthyl or heterocyclic; wherein R' is hydrogen, alkyl, alkanoyl or aroyl; wherein R 2 , R 3 and R 4 , which may be the same or different, each is an electron withdrawing substituent selected from halogeno, nitro, cyano, trifluoromethyl, alkylthio, alkylsulphinyl and alkylsulphonyl or each is hydrogen, alkyl, alkoxy or dialkylamino provided that when ring A is phenyl or naphthyl at least one of R 2 , R 3 and R 4 is an electron-withdrawing substituent; wherein R 5 and R 6 , which may be the same or different, each is hydrogen, halogeno or alkyl; wherein R 7 is alkyl or halogenoalkyl; and wherein R S is carbamoyl, alkyl, cycloalkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, halogenoalkynyl, alkanoyl, alkylcarbamoyl, dialkylcarbamoyl or aroyl; or wherein R 8 is alkyl or alkenyl which bears one or more substituents selected from cyano, carbamoyl, amino, hydroxy, alkanoyl, alkoxy, alkylthio, alkenylthio, alkylsulphinyl, alkenylsulphinyl, alkylsulphonyl, alkenylsulphonyl, alkanoylamino, alkoxycarbonylamino, alkylsulphonamido, alkylamino, dialkylamino dialkylsulphamoyl, aroyl, aryl, arylthio, arylsulphinyl, arylsulphonyl, heterocyclylthio, heterocyclylsulphinyl and heterocyclylsulphonyl; or wherein R 8 has the formula
wherein ring B is phenyl, naphthyl or heterocyclyl and wherein R 2 , R 3 and R 4 have any of the meanings stated above, provided that when R 7 is methyl R 8 is not also methyl.
摘要翻译：下式化合物其中X具有下式其中环A是苯基，萘基或杂环; 其中R'是氢，烷基，烷酰基或芳酰基; 其中R 2，R 3和R 4可以相同或不同，各自是选自卤素，硝基，氰基，三氟甲基，烷硫基，烷基亚磺酰基和烷基磺酰基的吸电子取代基或各自是氢，烷基，烷氧基或二烷基氨基，条件是当环 A是苯基或萘基，R2，R3和R4中的至少一个是吸电子取代基; 其中R5和R6可以相同或不同，各自是氢，卤素或烷基; 其中R 7是烷基或卤代烷基; 其中RS是氨基甲酰基，烷基，环烷基，烯基，炔基，卤代烷基，卤代烯基，卤代炔基，烷酰基，烷基氨基甲酰基，二烷基氨基甲酰基或芳酰基; 或者其中R8是带有一个或多个选自氰基，氨基甲酰基，氨基，羟基，烷酰基，烷氧基，烷硫基，烯硫基，烷基亚磺酰基，烯基亚磺酰基，烷基磺酰基，烯基磺酰基，烷酰基氨基，烷氧基羰基氨基，烷基磺酰氨基，烷基氨基，二烷基氨基二烷基氨磺酰基，芳基，芳硫基，芳基亚磺酰基，芳基磺酰基，杂环基硫基，杂环基亚磺酰基和杂环基磺酰基; 或其中R8具有下式其中环B为苯基，萘基或杂环基，且其中R2，R3和R4具有上述任意含义，条件是当R7为甲基时，R8也不是甲基。

97. 发明公开

EP0282959A2 Substituted 9-amino-tetrahydro-acridines and related compounds, a process for their preparation and their use as medicaments 失效
标题翻译：取代的9-氨基tetrahydroacridines和相关化合物，它们的制备方法和它们作为药物的用途。
公开(公告)号：EP0282959A2
公开(公告)日：1988-09-21
申请号：EP88104042.2
申请日：1988-03-15
申请人： HOECHST-ROUSSEL PHARMACEUTICALS INCORPORATED
发明人： Shutske, Gregory Michael , Helsley, Grover Cleveland
IPC分类号： C07D219/10 , C07D219/12 , C07D221/16 , A61K31/47 , C07C119/12 , C07D219/04 , C07D219/06
CPC分类号： C07D219/10 , C07D219/04 , C07D219/06
摘要： There are disclosed compounds having the formula
wherein n is 1-4; X is alkyl of 3-18 carbon atoms, cycloalkyl of 3-7 carbon atoms or cycloalkylloweralkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; R₁ is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
摘要翻译：有具有下式的游离缺失盘化合物 worin n为1-4; X是3-18碳原子，3-7个碳原子或cycloalkylloweralkyl的环烷基的烷基; R是氢，低级烷基或loweralkylcarbonyl; R 1是氢，低级烷基，loweralkylcarbonyl，芳基，diloweralkylaminoloweralkyl，芳基低级烷基，diarylloweralkyl，氧桥连芳基低级烷基或氧桥连的diarylloweralkyl; 它们的立体异构体和药学上可接受的酸加成盐，它们是用于增强记忆，用于合成它们的方法是有用的，和药物组合物，其包括有效的记忆增强复合搜索量。

98. 发明公开

EP0276842A2 Silver halide photographic material 失效
标题翻译：摄影术Silberhalogenidmaterial。
公开(公告)号：EP0276842A2
公开(公告)日：1988-08-03
申请号：EP88101198.5
申请日：1988-01-27
申请人： FUJI PHOTO FILM CO., LTD.
发明人： Hirano, Shigeo , Kojima, Tetsuro , Yamamoto, Kitsuru , Inoue, Noriyuki , Heki, Tatsuo
IPC分类号： G03C1/485 , G03C1/10
CPC分类号： C07D401/04 , C07D219/02 , C07D219/04 , C07D219/06 , C07D219/08 , C07D221/12 , C07D221/16 , C07D221/18 , C07D401/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07D513/04 , G03C1/067 , G03C1/48546 , Y10S430/141
摘要： A silver halide photographic material comprising a support having thereon at least one light-sensitive silver halide photographic emulsion layer, wherein at least one layer selected from the emulsion layer and other hydrophilic colloid layers contains at least one alkynyl substituted heterocyclic quaternary ammonium salt represented by the following general formula (I):
wherein Z represents a non-metallic atomic group necessary to form a substituted or unsubstituted 5- membered or 6-membered heterocyclic ring to which a aromatic ring or a heterocyclic ring may further be condensed; R I represents a substituted or unsubstituted aliphatic group; X represents = C -or - N -; Q represents a non-metallic atomic group necessary to form a substituted or unsubstituted 4-membered to 12- membered non-aromatic hydrocarbon ring or substituted or unsubstituted non-aromatic heterocyclic ring; at least one of R 1 , a substituent for Z and a substituent for Q includes an alkynyl group; Y represents a counter ion necessary for charge balance; and n represents a number necessary to balance the charge.
摘要翻译：一种卤化银照相材料，包括其上具有至少一种感光卤化银照相乳剂层的载体，其中至少一层选自乳液层和其它亲水胶体层含有至少一种炔基取代的杂环季铵盐，以下通式（I）：其中Z表示形成可以进一步稠合芳族环或杂环的取代或未取代的5元或6元杂环所必需的非金属原子团; R 1表示取代或未取代的脂族基团; X表示= @或 - @ - ; Q表示形成取代或未取代的4元至12元非芳族烃环或取代或未取代的非芳族杂环所必需的非金属原子团; R 1中的至少一个，Z的取代基和Q的取代基包括炔基; Y表示电荷平衡所需的抗衡离子; n表示平衡电荷所需的数字。

99. 发明授权

EP0025705B1 Compounds having antitumour properties, process for their preparation, these compounds for use as antitumour agents and pharmaceutical compositions containing them 失效
标题翻译：具有抗菌性质的化合物，其制备方法，用作抗菌剂的这些化合物和含有它们的药物组合物
公开(公告)号：EP0025705B1
公开(公告)日：1983-06-22
申请号：EP80303216.8
申请日：1980-09-12
申请人： DEVELOPMENT FINANCE CORPORATION OF NEW ZEALAND
发明人： Cain, Bruce Frank , Atwell, Graham John , Baguley, Bruce Charles , Denny, William Alexander
IPC分类号： C07D219/10 , A61K31/435
CPC分类号： C07D219/06 , C07D219/04 , C07D219/10 , Y10S514/908

100. 发明公开

EP0054384A1 Process for preparing pyridine derivatives 失效
标题翻译： Verfahren zur Herstellung von Pyridinderivaten。
公开(公告)号：EP0054384A1
公开(公告)日：1982-06-23
申请号：EP81305724.7
申请日：1981-12-04
申请人： JOHN WYETH & BROTHER LIMITED
发明人： Shepherd, Robin Gerald
IPC分类号： C07D215/48 , C07D219/04 , C07D221/04 , C07D221/12 , C07D221/16
CPC分类号： C07D221/04 , C07D215/48 , C07D219/04 , C07D221/12 , C07D221/16
摘要： Fused carbocyclic ring derivatives of pyridine which contain a nitrile or thioamide group on the carbocyclic ring e.g. 8-cyano or thiocarboxamido-5,6,7,8-tetrahydro- quinolines are prepared by a process in which a sodium, potassium, lithium or magnesium halide derivative of the pyridine compound is treated with a compound RaRbNCN wherein Ra and Rb are the same or different and represent alkyl, cycloalkyl, or aralkyl, or Ra and Rb are joined to form a heterocyclic ring with the nitrogen, and the product is treated with a proton source to obtain the nitrile which is optionally treated with a sulphurising agent to form the thioamide. The nitriles or thioamides may be isolated as their acid addition salts.
摘要翻译：在碳环上含有腈或硫代酰胺基团的吡啶的稠合碳环衍生物，例如 8-氰基或硫代甲酰胺基-5,6,7,8-四氢喹啉通过其中吡啶化合物的钠，钾，锂或卤化镁衍生物用化合物RaRbNCN处理的方法制备，其中Ra和Rb是相同或不同，表示烷基，环烷基或芳烷基，或者R a和R b与氮形成杂环，产物用质子源处理，得到任选用硫化剂处理的腈，形成硫代酰胺。腈或硫代酰胺可以作为其酸加成盐分离。

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