HUP0400639A2 - Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0400639A2
HUP0400639A2 HU0400639A HUP0400639A HUP0400639A2 HU P0400639 A2 HUP0400639 A2 HU P0400639A2 HU 0400639 A HU0400639 A HU 0400639A HU P0400639 A HUP0400639 A HU P0400639A HU P0400639 A2 HUP0400639 A2 HU P0400639A2
Authority
HU
Hungary
Prior art keywords
group
so2n
con
ring
condensed
Prior art date
Application number
HU0400639A
Other languages
English (en)
Inventor
David Bebbington
Jean-Damien Charrier
Robert Davies
Simon Everitt
David Kay
Ronald Knegtel
Sanjay Patel
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 HUP0400639A2 publication Critical patent/HUP0400639A2/hu
Publication of HUP0400639A3 publication Critical patent/HUP0400639A3/hu

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    • C07D513/00—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
    • 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 az általános képletű vegyületekre, illetvegyógyszerészetileg elfogadható származékaikra vagy prodrugjaikravonatkozik, amelyek képletében Rx és Ry a közöttük lévő atomokkalegyütt egy kondenzált, telítetlen vagy részlegesen telítetlen; adottesetben legfeljebb három heteroatomot tartalmazó, 5-7 tagú gyűrűtképez, amelyben az Rx és Ry által képezett kondenzált gyűrűben lévőbármely szubsztituálható szénatom oxocsoporttal, -T-R3 vagy L-Z-R3csoporttal, és az Rx és Ry által képezett kondenzált gyűrűben lévőbármely szubsztituálható nitrogénatom -R4 csoporttal szubsztituált; Rl-T- (D gyűrű) csoport; D gyűrű egy, az aril-, heteroaril-,heterociklil- vagy karbociklilcsoportok köréből kiválasztott 5-7 tagúmonociklusos csoportot vagy 8-10 tagú biciklusos csoportot jelent,amely heteroaril- vagy heterociklilcsoport a gyűrűben 1-4 heteroatomottartalmaz; T vegyértékkötés vagy alkilidéncsoport; Z alkilidéncsoport;L oxi-, tio-, szulfinil-, szulfonil-, -N(R6)-SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, karboni1-, -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)2N(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 és R2'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; 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; V oxi-, tio-, szulfinil-,szulfonil-, karbonil-, -CO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -N(R6)CO-, -N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2-N(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)2-N(R6)SO2N(R6)- vagy -C(R6)2N(R6)CON(R6)-csoport; W -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2-SO2N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-, -C(R6)OC(O)-,
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