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1. 发明授权

EP0255887B1 Verfahren zur Herstellung von 2.2-Bis (3-nitrophenyl)- hexafluorpropan 失效
标题翻译：制备2,2-BIS（3-硝基苯） - 六氟丙烯的方法
公开(公告)号：EP0255887B1
公开(公告)日：1990-08-29
申请号：EP87110351.1
申请日：1987-07-17
申请人： HOECHST AKTIENGESELLSCHAFT
发明人： Schneider, Klaus-Albert, Dr. , Siegemund, Günter, Dr.
IPC分类号： C07C205/07 , C07C205/06 , C07C201/06
CPC分类号： C07C205/11 , C07C205/58

2. 发明公开

EP0240659A2 N-substituierte 3,4,5,6-Tetrahydrophthalimide und deren Vorprodukte 失效
标题翻译： N-取代的3,4,5,6-四氢邻苯二甲酰亚胺和德国Vorprodukte。
公开(公告)号：EP0240659A2
公开(公告)日：1987-10-14
申请号：EP87101378.5
申请日：1987-02-02
申请人： BASF Aktiengesellschaft
发明人： Plath, Peter, Dr. , Eicken, Karl, Dr. , Goetz, Norbert, Dr. , Wild, Jochen, Dr. , Meyer, Norbert, Dr. , Würzer, Bruno, Dr.
IPC分类号： C07D209/48 , C07C205/07 , C07C205/44 , A01N43/36 , C07C255/41 , C07C229/36 , C07C233/05
CPC分类号： C07D209/48 , A01N37/46 , C07C205/44 , C07C205/56 , C07C255/00
摘要： N-substituierte 3,4,5,6-Tetrahydrophthalimide und deren Vorprodukte der allgemeinen Formel I
in der die Substituenten folgende Bedeutung haben:
B -CH₂-, -CH₂-CHR¹-, -CH₂-CHR¹-CH₂-, -CH=, -CH=CR¹- oder -CH=CR¹-CH=, wobei der Rest R¹ für -H, -Cl, -Br oder -CH₃ steht,

D je nach der Endgruppe von B -C oder =C ,

X -H, -Cl oder -Br,

Y -H, C₁-C₇-Alkyl, -Cl, -Br, -CN, CONH₂ oder -CO₂R², worin der Rest R² für H, C₁-C₆-Alkyl, C₅-C₆-Cycloalkyl, C₁-C₄-Alkoxy-C₂-C₄-alkyl C₁-C₄-Alkylmercapto-C₂-C₄-alkyl, Propargyl, Benzyl, α-Phenylethyl, α-Phenylpropyl, durch F oder Cl bis zu dreifach substituiertes C₂-C₄-Alkyl oder durch -CH₃ oder -Cl substituiertes Allyl steht
worin die Reste R³ und R⁴ H und C₁-C₄-Alkyl bedeuten oder gemeinsam einen cycloaliphatischen 5- oder 6-Ring bilden, dessen Kohlenstoffkette durch ein Sauerstoffatom unterbrochen sein kann.
摘要翻译： N-取代的3,4,5,6-四氢邻苯二酰亚胺及其前体具有通式I ... ...其中取代基具有以下含义：A是-NO 2，-NH 2或... ...相应对于化合物Ia，Ib和Ic，... A是对应于化合物Ia，Ib和Ic的-NO 2，-NH 2或...，... B是-CH 2 - ， - CH 2 -CHR 1 - ， - CH 2 -CHR 1 -CH 2 - ， - CH =， - CH = CR 1 - 或-CH = CR 1 -CH =，其中基团R 1是-H，-Cl，-Br 或-CH 3，... D取决于B的末端基团，是-CH <2b R>或= C <2b R>，... X是-H，-Cl或-Br，... Y是-H，C1-C7- 烷基，-Cl，-Br，-CN，CONH 2或-CO 2 R 2，其中基团R 2是H，C 1 -C 6烷基，C 5 -C 6环烷基，C 1 -C 4 - 烷氧基-C 2 - C 1 -C 4烷基，C 1 -C 4烷基巯基-C 2 -C 4烷基，炔丙基，苄基，α-苯乙基，α-苯基丙基，被F或Cl三取代的C 2 -C 4烷基或被 - CH 3或-Cl，... Z是-COOR 2，-CONR 3 R 4，... ...或-COR 2，其中基团R 3和R 4 是H或C 1-C4-烷基或一起形成其碳链可被氧原子间隔的脂环族5或6元环。

3. 发明授权

EP0343048B1 Process for producing nitrobenzenes 失效
标题翻译：生产硝基苯的方法
公开(公告)号：EP0343048B1
公开(公告)日：1993-01-27
申请号：EP89401325.9
申请日：1989-05-12
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Sato, Hiroshi , Hirose, Kenichi , Nagai, Koichi , Yoshioka, Hiroshi , Nagaoka, Yoshihiko
IPC分类号： C07C201/08 , C07C205/06 , C07C205/07
CPC分类号： C07C201/08 , C07C205/06 , C07C205/12

4. 发明授权

EP0252964B1 CATALYTIC METHOD FOR PRODUCING FLUOROAROMATIC COMPOUNDS USING SUBSTITUTED PYRIDINIUM SALTS 失效
标题翻译：使用取代的吡啶鎓盐生产氟代化合物的催化方法
公开(公告)号：EP0252964B1
公开(公告)日：1991-08-21
申请号：EP87900770.6
申请日：1986-12-30
申请人： MALLINCKRODT SPECIALTY CHEMICALS COMPANY
发明人： CANTRELL, Gary, L.
IPC分类号： C07C205/07 , C07C205/12 , C07D213/74
CPC分类号： C07D213/84 , C07B39/00 , C07C17/208 , C07C45/63 , C07C51/363 , C07C51/567 , C07C51/62 , C07C201/12 , C07C253/30 , C07C317/14 , C07D213/26 , C07D307/89 , C07D401/04 , C07C25/13 , C07C205/12 , C07C255/50 , C07C63/70 , C07C63/68
摘要： A process for preparing fluoroaromatic compounds (such as fluoronitrobenzene compounds) by reaction of corresponding chloroaromatic compounds (such as chloronitrobenzene compounds) with alkali metal fluoride salts in the presence of alkyldiorganoaminopyridinium salts as phase transfer catalysts. A tertiary carbon atom is directly attached to the alkyl carbon atom which is directly attached to the ring nitrogen atom. A preferred catalyst is N-neopentyl-4-(4'-methylpiperidinyl)pyridinium chloride.

5. 发明授权

EP0240659B1 N-substituierte 3,4,5,6-Tetrahydrophthalimide und deren Vorprodukte 失效
标题翻译： N-取代的3,4,5,6-四氢脑苷脂及其前体
公开(公告)号：EP0240659B1
公开(公告)日：1991-03-20
申请号：EP87101378.5
申请日：1987-02-02
申请人： BASF Aktiengesellschaft
发明人： Plath, Peter, Dr. , Eicken, Karl, Dr. , Goetz, Norbert, Dr. , Wild, Jochen, Dr. , Meyer, Norbert, Dr. , Würzer, Bruno, Dr.
IPC分类号： C07D209/48 , C07C205/07 , C07C205/44 , A01N43/36 , C07C255/41 , C07C229/36 , C07C233/05
CPC分类号： C07D209/48 , A01N37/46 , C07C205/44 , C07C205/56 , C07C255/00

6. 发明授权

EP0763009B1 PHOTOCLEAVABLE CONJUGATES FOR THE DETECTION AND ISOLATION OF BIOMOLECULES 失效
标题翻译：可光偶联物检测和生物分子隔离
公开(公告)号：EP0763009B1
公开(公告)日：2004-09-08
申请号：EP95921230.9
申请日：1995-05-11
申请人： TRUSTEES OF BOSTON UNIVERSITY
发明人： ROTHSCHILD, Kenneth, J. , SONAR, Sanjay M. , OLEJNIK, Jerzy
IPC分类号： C07C205/00 , C07C205/06 , C07C205/07 , C07D235/02 , C07H1/06 , C07H1/08 , C07K1/13
CPC分类号： C12Q1/6876 , A61K38/00 , A61K41/0042 , C07C205/45 , C07C205/57 , C07D207/404 , C07D311/16 , C07D405/12 , C07D495/04 , C07H19/04 , C07H21/00 , C07K1/1077 , C07K1/13 , C12P21/00 , G01N33/532 , Y02A50/473
摘要： The present invention relates to a bioreactive agent comprising a detectable moiety linked to a photo-reactive moiety, wherein said photoreactive moiety comprises at least one group covalently bound to a substrate to form a conjugate that can be selectively photocleaved to release said substrate, wherein said substrate is selected from proteins, peptides, amino acids, lipids, cells, virus particles, fatty acids, nucleic acids, nucleotides, nucleosides, oligonucleotides, polysaccharides and inorganic molecules.

7. 发明授权

EP0307481B1 PROCESS FOR PREPARING 3-CHLORO-4-FLUORONITROBENZENE 无效
标题翻译： PROCESS FOR 3-氯-4-氟硝基苯的制备。
公开(公告)号：EP0307481B1
公开(公告)日：1993-11-24
申请号：EP88902565.6
申请日：1988-03-18
申请人： NIPPON KAYAKU KABUSHIKI KAISHA
发明人： ISHIKURA, Tsukasa , FUKUSHIMA, Tatuharu
IPC分类号： C07C205/00 , C07C205/07 , C07C205/01 , B01J27/06 , B01J27/12
CPC分类号： C07C201/12 , C07C205/12
摘要： A process for preparing 3-chloro-4-fluoronitrobenzene, which comprises chlorinating 4-fluoronitrobenzene in the presence of: (1) iodine or its compound and iron or its compound, or (2) iodine or its compound and antimony or its compound.

8. 发明公开

EP0396250A1 Pyrimidinone derivatives 失效
标题翻译：嘧啶酮衍生物
公开(公告)号：EP0396250A1
公开(公告)日：1990-11-07
申请号：EP90303309.0
申请日：1990-03-28
申请人： ZENECA LIMITED
发明人： Whittle, Alan John , Perrior, Trevor Robert , Sunley, Raymond Leo
IPC分类号： C07D239/36 , C07C205/07 , C07C217/84 , A01N43/54
CPC分类号： C07D239/36 , A01N43/54 , C07C17/32 , C07C205/12 , C07C205/37 , C07C213/08 , C07C217/84 , C07D239/40 , C07D239/47 , C07D239/52 , C07D239/56 , C07C25/13
摘要： A compound of formula (I) :
wherein R¹ and R² are independently selected from hydrogen, halogen, haloalkyl, alkoxy or nitro, provided that R¹ and R² are not both nitro; R³ and R⁴ are independently selected from hydrogen, halogen, alkyl or cycloalkyl; R⁵ is halogen, nitro, haloalkyl, haloalkoxy or -S(O) n R¹⁰; R⁶ is halogen, nitro, haloalkyl, haloalkoxy or -S(O) n R¹⁰; R⁷ is hydrogen, halogen, hydroxyalkyl, cyano, nitro, alkoxy, -S(O) n R¹⁰, NR¹¹R¹², haloalkyl or formyl; R⁸ is hydrogen, halogen, NR¹¹R¹², alkyl, cycloalkyl or S(O) n R¹⁰; and R⁹ is oxygen or sulphur; where n is 0, 1 or 2; and R¹⁰ is alkyl, haloalkyl or cycloalkyl; and R¹¹ and R¹² are independently selected from hydrogen, alkyl or cycloalkyl or R¹¹ and R¹² together with the nitrogen to which they are attached form a heterocylic group; provided that when R⁵ is trifluoromethyl at least one of the following applies:

(i) R¹ or R² is haloalkyl or alkoxy;
(ii) R³ or R⁴ are alkyl or cycloalkyl;
(iii) R⁶ is haloalkoxy, nitro or -S(O) n R¹⁰;
(iv) R⁷ is nitro, hydroxyalkyl, alkoxy, S(O) n R¹⁰, NR¹¹R¹², formyl or haloalkyl;
(v) R⁸ is other than hydrogen;
(vi) R⁹ is sulphur; and further provided that (a) R¹, R², R³ and R⁴ are not all fluorine and (b) when R⁵ is chlorine, R¹ and R² are both halogen.
摘要翻译：式（Ⅰ）化合物：其中R 1和R 2独立地选自氢，卤素，卤代烷基，烷氧基或硝基，条件是R 1和R 2不都是硝基; R 3和R 4独立地选自氢，卤素，烷基或环烷基; R 5是卤素，硝基，卤代烷基，卤代烷氧基或-S（O）n R 17; R 7是卤素，硝基，卤代烷基，卤代烷氧基或-S（O）n R 10; R 6是氢，卤素，羟基烷基，氰基，硝基，烷氧基，-S（O）n R 10，NR 11 R 12，卤代烷基或甲酰基; R 7是氢，卤素，NR 11 R 12，烷基，环烷基或S（O）n R 10; 和R 7是氧或硫; 其中n是0,1或2; 并且R 18是烷基，卤代烷基或环烷基; 并且R 11和R 12独立地选自氢，烷基或环烷基或R 11和R 12与它们所连接的氮一起形成杂环基; 条件是当R 5是三氟甲基时，至少适用下列之一：（ⅰ）R 1或R 2是卤代烷基或烷氧基; （ⅱ）R 3或R 4是烷基或环烷基; （ⅲ）R 8是卤代烷氧基，硝基或-S（O）n R 10; （））R 7是硝基，羟烷基，烷氧基，S（O）nR 10，NR 11 R 12，甲酰基或卤代烷基; （v）R 8不是氢; （vi）R 7是硫; （a）R 1，R 2，R 3和R 4不全是氟，和（b）当R 5是氯时，R 1和R 2都是卤素。

9. 发明公开

EP0307481A1 PROCESS FOR PREPARING 3-CHLORO-4-FLUORONITROBENZENE 无效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON 3-CHLOR-4-FLUORNITROBENZOL。
公开(公告)号：EP0307481A1
公开(公告)日：1989-03-22
申请号：EP88902565.6
申请日：1988-03-18
申请人： NIPPON KAYAKU KABUSHIKI KAISHA
发明人： ISHIKURA, Tsukasa , FUKUSHIMA, Tatuharu
IPC分类号： C07C205/00 , C07C205/07 , C07C205/01 , B01J27/06 , B01J27/12
CPC分类号： C07C201/12 , C07C205/12
摘要： A process for preparing 3-chloro-4-fluoronitrobenzene, which comprises chlorinating 4-fluoronitrobenzene in the presence of: (1) iodine or its compound and iron or its compound, or (2) iodine or its compound and antimony or its compound.
摘要翻译：这种改进的制备3-氯-4-氟苯基苯的方法包括在催化剂存在下氯化4-氟硝基苯。催化剂规定为（1）碘或碘cpd。铁或铁cpd。或（2）碘或碘cpd。锑或锑cpd。铁cpd。是pref。 FeCl 2或FeCl 3。其与4-氟硝基苯的重量比为0.1-10重量％。锑cpd 是pref。 SbCl3或SbCl5。碘或碘cpd。是pref。碘，氯化碘，碘化氢，碘化铁等。与4-氟硝基苯的比例为0.3-3.0重量％（优选0.01-1.0重量％）。反应温度优先。在20和120度之间。 C反应时间通常为0.5-50小时。氯化剂是首选。氯气。

10. 发明公开

EP1412311A1 NOVEL TREATMENT OF ADRENOCORTICAL HYPERSECRETION AND TUMOUR GROWTH 审中-公开
标题翻译：肿瘤的生长和肾上腺皮质分泌过多新的治疗
公开(公告)号：EP1412311A1
公开(公告)日：2004-04-28
申请号：EP02744060.1
申请日：2002-06-27
申请人： Brandt, Ingvar
发明人： Brandt, Ingvar
IPC分类号： C07C25/18 , C07C205/07 , C07C317/14 , A61K31/03 , A61K31/04 , A61K31/10 , A61P35/00
CPC分类号： C07C25/24 , A61K31/03 , A61K31/04 , A61K31/10 , C07C205/11
摘要： The present invention relates to novel treatment of adrenocortical hypersecretion. More specifically, the present invention relates to chemical substances having selective adrenal toxicity for use in medicine, especially for treatment of adrenocortical hypersecretion and tumour growth. For this purpose the present invention provides a compound having the following formula for use in medicine, especially human medicine wherein the first phenyl ring comprises one or more substituents R1 which is halogen (F , CI, Br or 1), preferably in position 4; R2 and R3 are halogen,A is a single or double bond between the side chain carbon atoms; the second phenyl ring comprises an electrophilic group R4 , preferably in position 3, which is SO2R5 or its metabolic precursors S R5 and SOR5, NO2 or CF3 .where R5 is H or a lower alkyl, especially CH3 ; and one or more substituents R6 which is halogen (F , Cl, Br or I), preferably in position 4.

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