EA018708B1 - ПРОИЗВОДНЫЕ МОРФОЛИНОПИРИМИДИНА, ИСПОЛЬЗУЕМЫЕ ПРИ ЗАБОЛЕВАНИЯХ, СВЯЗАННЫХ С mTOR КИНАЗОЙ И/ИЛИ PI3K - Google Patents

Info

Publication number

EA018708B1

EA018708B1 EA201000091A EA201000091A EA018708B1 EA 018708 B1 EA018708 B1 EA 018708B1 EA 201000091 A EA201000091 A EA 201000091A EA 201000091 A EA201000091 A EA 201000091A EA 018708 B1 EA018708 B1 EA 018708B1

Authority

EA

Eurasian Patent Office

Prior art keywords

alkyl

amino

6alkyl

alkoxy

bis

Prior art date

2007-07-09

Links

• Espacenet
• Global Dossier
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• 201000010099 disease Diseases 0.000 title claims abstract description 36
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 36
• 108091007960 PI3Ks Proteins 0.000 title abstract description 3
• 102000038030 PI3Ks Human genes 0.000 title abstract 2
• 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 title abstract 2
• 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 title abstract 2
• DUIMWXDLDBNUFD-UHFFFAOYSA-N 4-pyrimidin-2-ylmorpholine Chemical class C1COCCN1C1=NC=CC=N1 DUIMWXDLDBNUFD-UHFFFAOYSA-N 0.000 title description 5
• 150000001875 compounds Chemical class 0.000 claims abstract description 295
• 150000003839 salts Chemical class 0.000 claims abstract description 79
• 238000011282 treatment Methods 0.000 claims abstract description 60
• 230000002062 proliferating effect Effects 0.000 claims abstract description 17
• 238000002360 preparation method Methods 0.000 claims abstract description 9
• 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 6
• -1 furanylmethyl Chemical group 0.000 claims description 535
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 508
• 125000000217 alkyl group Chemical group 0.000 claims description 392
• 229910052736 halogen Inorganic materials 0.000 claims description 200
• 150000002367 halogens Chemical class 0.000 claims description 200
• 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims description 189
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 167
• 125000003545 alkoxy group Chemical group 0.000 claims description 166
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 160
• 125000001424 substituent group Chemical group 0.000 claims description 151
• 239000001257 hydrogen Substances 0.000 claims description 138
• 229910052739 hydrogen Inorganic materials 0.000 claims description 138
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 109
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 105
• 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims description 94
• UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims description 79
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 77
• 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 73
• 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 70
• 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims description 60
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• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 33
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• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 22
• 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 21
• 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 20
• 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 20
• 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 18
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• 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 14
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