HUP0400638A2 - Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0400638A2
HUP0400638A2 HU0400638A HUP0400638A HUP0400638A2 HU P0400638 A2 HUP0400638 A2 HU P0400638A2 HU 0400638 A HU0400638 A HU 0400638A HU P0400638 A HUP0400638 A HU P0400638A HU P0400638 A2 HUP0400638 A2 HU P0400638A2
Authority
HU
Hungary
Prior art keywords
group
con
so2n
optionally substituted
heteroaryl
Prior art date
Application number
HU0400638A
Other languages
English (en)
Inventor
David Bebbington
Jean-Damien Charrier
Julian M. C. Golec
Ronald Knegtel
Andrew Miller
Original Assignee
Vertex Pharmaceuticals Incorporated
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HUP0400638A2 publication Critical patent/HUP0400638A2/hu

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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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Abstract

A találmány a általános képletű vegyületekre, illetvegyógyszerészetileg elfogadható származékaikra vagy prodrugjaikravonatkozik, amelyek képletében RX és RY jelentése -T-R3 vagy -L-Z-R3csoport; R1 jelentése -T-(D gyűrű) csoport; D gyűrű egy, az aril-,heteroaril-, heterociklil- vagy karbociklilcsoportok körébőlkiválasztott 5-7 tagú monociklusos csoportot vagy 8-10 tagú biciklusoscsoportot jelent, amely heteroaril- vagy heterociklilcsoport agyűrűben 1-4 heteroatomot tartalmaz; L oxi-, tio-, szulfinil-,szulfonil-, -N(R6)-SO2-, -SO2N(R6) -, -N(R6)-, karbonil-, -C(O)O-, -N(R6)CO-, -N(R6)-C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)-C(O)-, -C(R6)2-N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)-N(R6)-, -C(R6)2N(R6)SO2N(R6)- vagy -C(R6)2N(R6)-CON(R6) csoport; R2 ésR2' jelentése -R vagy -T-W-R6 csoport, vagy R2 és R2' a közöttük lévőatomokkal együtt egy kondenzált, telítetlen vagy részlegesentelítetlen, adott esetben legfeljebb három heteroatomot tartalmazó, 5-8 tagú gyűrűt képez; R3 halogénatom, -R, -OR, -C(=O)R, -CO2R, -COCOR,-COCH2COR, nitro-, ciano-, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R7)2, -SO2N(R7)2, -OC(=O)R, -N(R7)COR, -N(R7)COO(adott esetben szubsztituáltalifás), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7)2, -N(R7)SO2N(R7)2, -N(R4)SO2R vagy -OC(=O)-N(R7)2 csoport; R hidrogénatomvagy adott esetben szubsztituált alifás, aril-, heteroaril- vagyheterociklilcsoport; R4 -R7, -COR7, -CO2(alifás), -CON(R7)2 vagy -SO2R7 csoport; R5 halogénatom, -R, -OR, -C(=O)R, -CO2R, -COCOR,nitro-, ciano-, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R4)2, -SO2N(R4)2,-OC(=O)R, -N(R4)COR, -N(R4)CO2(adott esetben szubsztituált alifás), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R4)CON(R4)2, -N(R4)SO2N(R4)2, -N(R4)SO2R vagy -OC(=O)N(R4)2 csoport; W -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2, -N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-, -C(R6)OC(O)-, -C(R6)O-C(O)-N(R6)-, -C(R6)2N(R6)CO-, -C(R6)2N(R6)C(O)O-, -C(R6)-N-N(R6)-, -C(R6)-N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2-N(R6)-, -C(R6)2N(R6)-CON(R6)- vagy -CON(R6)- csoport;R6 hidrogénatom vagy adott esetben szubsztituált alifás csoport, vagykét ugyanazon a nitrogénatomon lévő R6 csoport a nitrogénatommalegyütt egy 5-6 tagú heterociklil- vagy heteroarilcsoportot képez; ésR7 mindegyikének jelentése egymástól függetlenül hidrogénatom vagyadott esetben szubsztituált alifás csoport, vagy két ugyanazon anitrogénatomon lévő R7 csoport a nitrogénatommal együtt egy 5-8 tagúheterociklil- vagy heteroarilcsoportot képez. A találmány kiterjed avegyületeket tartalmazó gyógyszerkészítményekre, valamint a vegyületekalkalmazási eljárásaira is. Ó
HU0400638A 2000-12-21 2001-12-19 Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények HUP0400638A2 (hu)

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