EA035020B1 - Пиразолопиримидиниловые ингибиторы убиквитин-активирующего фермента - Google Patents

Info

Publication number

EA035020B1

EA035020B1 EA201400831A EA201400831A EA035020B1 EA 035020 B1 EA035020 B1 EA 035020B1 EA 201400831 A EA201400831 A EA 201400831A EA 201400831 A EA201400831 A EA 201400831A EA 035020 B1 EA035020 B1 EA 035020B1

Authority

EA

Eurasian Patent Office

Prior art keywords

pyrazolo

pyrimidin

dihydroxy

cyclopentyl

phenyl

Prior art date

2012-02-17

Links

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• -1 Pyrazolopyrimidinyl Chemical group 0.000 title claims abstract description 183
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• 239000003112 inhibitor Substances 0.000 title description 17
• 150000001875 compounds Chemical class 0.000 claims abstract description 246
• FIYXUOWXHWJDAM-UHFFFAOYSA-N methyl sulfamate Chemical compound COS(N)(=O)=O FIYXUOWXHWJDAM-UHFFFAOYSA-N 0.000 claims abstract description 58
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims abstract description 40
• 150000003839 salts Chemical class 0.000 claims abstract description 40
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• KJDAGXLMHXUAGV-DGWLBADLSA-N [(1r,2r,3s,4r)-2,3-dihydroxy-4-[[2-[3-(trifluoromethylsulfanyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl sulfamate Chemical compound O[C@@H]1[C@H](O)[C@@H](COS(=O)(=O)N)C[C@H]1NC1=CC=NC2=CC(C=3C=C(SC(F)(F)F)C=CC=3)=NN12 KJDAGXLMHXUAGV-DGWLBADLSA-N 0.000 claims abstract description 6
• HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract description 4
• VKEQBMCRQDSRET-UHFFFAOYSA-N Methylone Chemical compound CNC(C)C(=O)C1=CC=C2OCOC2=C1 VKEQBMCRQDSRET-UHFFFAOYSA-N 0.000 claims abstract description 4
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• UFDGEFUTYSMTPD-UHFFFAOYSA-N 1-chloro-4-iodonaphthalene Chemical compound C1=CC=C2C(Cl)=CC=C(I)C2=C1 UFDGEFUTYSMTPD-UHFFFAOYSA-N 0.000 description 22
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