HUP0302411A2 - Proteinkináz inhibitorként alkalmazható pirazolvegyületek és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Proteinkináz inhibitorként alkalmazható pirazolvegyületek és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0302411A2
HUP0302411A2 HU0302411A HUP0302411A HUP0302411A2 HU P0302411 A2 HUP0302411 A2 HU P0302411A2 HU 0302411 A HU0302411 A HU 0302411A HU P0302411 A HUP0302411 A HU P0302411A HU P0302411 A2 HUP0302411 A2 HU P0302411A2
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HU
Hungary
Prior art keywords
group
con
ring
so2n
substitutable
Prior art date
Application number
HU0302411A
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English (en)
Inventor
David Bebbington
Hayley Binch
Jean-Damien Charrier
Robert Davies
Cornelia Forster
Julian M. C. Golec
David Kay
Ronald Knegtel
Pan Li
Sanjay Patel
Albert Pierce
Marion Wannamaker
Original Assignee
Vertex Pharmaceuticals Incorporated
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27398347&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0302411(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HUP0302411A2 publication Critical patent/HUP0302411A2/hu

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Abstract

A találmány a proteinkináz, különösen GSK-3 és Aurora-2 proteinkinázinhibitorokként funkcionáló általános képletű vegyületekre - amelyekképletében D gyűrű az aril-, heteroaril-, heterociklil- vagykarbociklilcsoportok köréből kiválasztott 5-7 tagú monociklusoscsoportot vagy 8-10 tagú biciklusos csoportot jelent, amelyheteroaril- vagy heterociklilcsoport 1-4 heteroatomot tartalmaz, ahola D gyűrű bármely szubsztituálható gyűrűszénatomon oxo- vagy -R5csoporttal szubsztituált és bármely szubsztituálható gyűrűnitrogén-atomon -R4 csoporttal szubsztituált; RX és RY jelentése egymástólfüggetlenül -T-R3 általános képletű csoport, vagy RX és RY a közöttüklévő atomokkal együtt egy kondenzált, telítetlen vagy részlegesentelítetlen, 1-3 heteroatomot tartalmazó 5-8 tagú gyűrűt képez,amelyben bármely szubsztituálható szénatom -T-R3 csoporttal és bármelyszubsztituálható nitrogénatom -R4 csoporttal szubsztituált; Tvegyértékkötés vagy alkilidénlánc; R2 és R2' -R vagy -T-W-R6 csoport,vagy R2 és R2' a közöttük lévő atomokkal együtt egy kondenzált,telítetlen vagy részlegesen telítetlen, adott esetben legfeljebb háromheteroatomot tartalmazó, 5-8 tagú gyűrűt képez, amelyben a kondenzáltgyűrűben bármely szubsztituálható szénatom halogénatommal, oxo-,ciano-, nitro-, -R7 vagy -V-R6 csoporttal szubsztituált; R3halogénatom, -R, -OR, -C(=O)R, -CO2R, -COCOR, -COCH2COR, nitro-,ciano-, -S(O)R, -S(O)2R, -N(R7)COR, -N(R7)COO (adott esetbenszubsztituált alifás), -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)2csoport; R hidrogénatom vagy egy adott esetben szubsztituált alifás,aril-, heteroaril- vagy heterociklilcsoport; R4 -R7, -COR7, -CO2(alifás), -CON(R7)2 vagy -SO2R7 csoport, vagy két ugyanazon anitrogénatomon lévő R4 együtt egy 5-8 tagú heterociklil- vagyheteroarilcsoportot képez; 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 szubsztituáltalifás), -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)2, -N(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)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)-CO
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