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31. 发明公开

EP1017394A1 CYCLIN DEPENDENT KINASE INHIBITING PURINE DERIVATIVES 失效
标题翻译： CYCLIN-ABHÄNGIGE-KINASE INHIBIERENDE PURINDERIVATE
公开(公告)号：EP1017394A1
公开(公告)日：2000-07-12
申请号：EP98932413.2
申请日：1998-07-10
申请人： CANCERRESEARCHCAMPAIGN TECHNOLOGY LIMITED
发明人： GRIFFIN, Roger John , CALVERT, Alan Hilary , CURTIN, Nicola Jane , NEWELL, David Richard , GOLDING, Bernhard Thomas , ENDICOTT, Jane, Anne , NOBLE, Martin, Edward, Mantyla , BOYLE, Francis Thomas , JEWSBURY, Philip John
IPC分类号： A61K31/52 , A61K31/70 , C07D473/18 , C07D473/24 , C07D473/26 , C07D473/40 , C07H17/02
CPC分类号： C07H15/26 , C07D473/18 , C07D473/30 , C07D473/40
摘要： A range is disclosed of purine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDKs) and which thereby c an provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to be different to that of known CDK inhibitors such as olomoucine and roscovitine. In formula (I), in preferred embodiments: X is O, S or CHRx where Rx is H or C1-4 alkyl; D is H, halo or NZ1Z2 where Z1 and Z2 are each independently H or C1-4 alkyl or C1-4 hydroxyalkyl; A is selected from H, C1-4 alkyl, C1-4 alkoxy, hydroxy, CH2(CH2)nOH (n=1-4), and NRa1Ra2 where Ra1 and Ra2 are each independently H or C1-4 alkyl; B is selected from H, C1-4 alkyl, C1-4 alkoxy, CF3, an optionally substituted aryl (e.g. phenyl) or an optionally substituted aralkyl (e.g. benzyl), and an hydroxy group that provides a C=O tautomer; and Y is or includes an optionally substituted 4- to 8-membered carbocyclic or heterocyclic ring; or comprises an optionally substituted linear or branched hydrocarbon chain.

33. 发明公开

EP0690056A3 Verfahren zur Herstellung von Purinen 失效
标题翻译：一种用于嘌呤的制备方法
公开(公告)号：EP0690056A3
公开(公告)日：1996-03-27
申请号：EP95110018.9
申请日：1995-06-27
申请人： SKW Trostberg Aktiengesellschaft
发明人： Thalhammer, Franz, Dr. , Graefe, Jürgen, Dr.
IPC分类号： C07D473/18 , C07D473/34 , C07D473/26
CPC分类号： C07D473/34 , C07D473/16 , C07D473/18
摘要： Zur Herstellung eines Purins der allgemeinen Formel (I),

in der R¹ und R² gleich oder verschieden sein können und H, OH, SH, NH₂, N-(Di)-Alkyl, Halogen, O-Alkyl, S-Alkyl, Alkyl oder Aryl bedeuten und Alkyl einen aliphatischen Rest mit 1 bis 4 Kohlenstoffatomen und Aryl einen gegebenenfalls mit CH₃, OH, NH₂, Halogen-substituierten Phenylrest darstellt, aus dem entsprechenden 4-Amino-5-nitrosopyrimidin der Formel (II),

in der R¹ und R² die oben angegebene Bedeutung haben, formyliert man die Verbindung der Formel (II) in Gegenwart von Ameisensäure und einem Katalysator auf Basis eines Edelmetalls in einem Lösemittel bei einer Temperatur von 80 bis 220°C reduktiv und cyclisiert das intermediär gebildete 4-Amino-5-formylaminopyrimidin.

35. 发明公开

EP0503838A2 Heterocyclic compounds bearing acidic functional groups as angiotensin II antagonists 失效
标题翻译：异丙肾上腺素血管紧张素II拮抗剂。
公开(公告)号：EP0503838A2
公开(公告)日：1992-09-16
申请号：EP92301884.0
申请日：1992-03-05
申请人： MERCK & CO. INC.
发明人： Chakravarty, Prasun K. , Patchett, Arthur A. , Mantlo, Nathan B. , Rivero, Ralph A. , Greenlee, William J. , Kim, Dooseop
IPC分类号： C07D471/04 , C07D487/04 , C07D473/00 , C07D473/02 , C07D473/26 , C07D473/40 , A61K31/435 , A61K31/495 , A61K31/53 , A61K31/675
CPC分类号： C07D471/04 , C07D473/08 , C07D473/32 , C07F9/6561
摘要： Heterocyclic compounds of structural formula :

wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
摘要翻译：结构式的杂环化合物：其中A，B，C和D独立地为碳原子或氮原子，可用于治疗高血压和充血性心力衰竭的血管紧张素II拮抗剂。

36. 发明公开

EP0297661A1 [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1H-azepines and pyrrolidines 失效
标题翻译： [（Bizyklisch-heterozyklyl）methyl und -hetero]取代物六氢-1H-吖庚因和吡咯烷。
公开(公告)号：EP0297661A1
公开(公告)日：1989-01-04
申请号：EP88201291.7
申请日：1988-06-23
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： Janssens, Frans Eduard , Diels, Gaston Stanislas Marcella , Pille, Geert Marcel Ester
IPC分类号： C07D471/04 , C07D473/00 , C07D473/26 , C07D403/06 , C07D403/12 , C07D403/14 , A61K31/44 , A61K31/52 , A61K31/55
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D473/00
摘要： Novel [(Bicyclic heterocyclyl)methyl and -hetero] substituted hexahydro-1 H -azepines and pyrrolidines of formula
wherein
-A¹=A²-A³=A⁴- is -CH=CH-CH=CH-, -N=CH-CH=CH-, -CH=N-CH=CH-, -CH=CH-N=CH-, -CH=CH-CH=N-, -N=CH-N=CH-, or -CH=N-CH=N-,
R¹ is hydrogen, C₁₋₁₀alkyl, C₃₋₆cycloalkyl, Ar¹ or C₁₋₆alkyl substituted with one or two Ar¹ radicals;
B is NR², CH₂, O, S, SO or SO₂;
R is hydrogen or C₁₋₆alkyl;
n is 0 or 2;
L is hydrogen, C₁₋₆alkylcarbonyl, C₁₋₆alkylsulfonyl, C₁₋₆alkyloxycarbonyl, Ar²-C₁₋₆alkyloxycarbonyl, Ar²-carbonyl, Ar²-sulfonyl, C₃₋₆cycloalkyl, C₂₋₆alkenyl optionally substituted with Ar², C₁₋₁₂alkyl, a radical of formula -Alk-R³, -Alk-Y-R⁴, -Alk-Z¹-C(X)-Z²-R⁵, or -CH₂-CHOH-CH₂-O-R⁶;
the pharmaceutically acceptable acid addition salts and possible stereochemically isomeric forms thereof, which compounds are anti-allergic agents; pharmaceutical compositions containing such compounds as an active ingredient and methods of preparing said compounds and pharmaceutical compositions.
摘要翻译：新型[（双环杂环基）甲基和 - 杂]取代的六氢-1H-吖庚因和式CHEM的吡咯烷，其中-A 1 = A 2 -A 3 = A 4 - 为-CH = CH-CH = CH-，-N = CH-CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-，-CH = CH-CH = CH-N = CH-或-CH = N-CH = N-，R 1为氢，C 1-10烷基，C 3-6环烷基，Ar 1或被一个或两个Ar 1取代的C 1-6烷基自由基; B是NR 2，CH 2，O，S，SO或SO 2; R是氢或C 1-6烷基; n为0或2; L是氢，C 1-6烷基羰基，C 1-6烷基磺酰基，C 1-6烷氧基羰基，Ar 2 -C 1-6烷氧基羰基，Ar 2 - 羰基，Ar 2 - 磺酰基，C 3-6环烷基，任选被Ar取代的C 2-6链烯基 C1-C12烷基，式为-Alk-R3，-Alk-YR4，-Alk-Z-C（X）-Z2 -R5的基团，，或-CH 2 -CHOH-CH 2 -OR 6; 其药学上可接受的酸加成盐及其可能的立体化学异构形式，该化合物是抗过敏剂; 含有作为活性成分的化合物的药物组合物和制备所述化合物和药物组合物的方法。

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