JP2009501765A5 - - Google Patents

Info

Publication number

JP2009501765A5

JP2009501765A5 JP2008521971A JP2008521971A JP2009501765A5 JP 2009501765 A5 JP2009501765 A5 JP 2009501765A5 JP 2008521971 A JP2008521971 A JP 2008521971A JP 2008521971 A JP2008521971 A JP 2008521971A JP 2009501765 A5 JP2009501765 A5 JP 2009501765A5

Authority

JP

Japan

Prior art keywords

lower alkyl

mono

phenyl

amino

pharmaceutical combination

Prior art date

2006-07-19

Legal status (The legal status 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 status listed.)

Pending

Links

• Espacenet
• Global Dossier
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• 125000000217 alkyl group Chemical group 0.000 claims 15
• -1 benzcycloalkyl Chemical group 0.000 claims 6
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
• 125000004432 carbon atom Chemical group C* 0.000 claims 4
• 125000000753 cycloalkyl group Chemical group 0.000 claims 4
• 229910052757 nitrogen Inorganic materials 0.000 claims 4
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
• 229940079593 drug Drugs 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 3
• 125000000623 heterocyclic group Chemical group 0.000 claims 3
• 229910052739 hydrogen Inorganic materials 0.000 claims 3
• 239000001257 hydrogen Substances 0.000 claims 3
• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
• 229940124302 mTOR inhibitor Drugs 0.000 claims 3
• 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 3
• KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
• HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 2
• KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 2
• 125000003545 alkoxy group Chemical group 0.000 claims 2
• 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 125000002619 bicyclic group Chemical group 0.000 claims 2
• 201000010099 disease Diseases 0.000 claims 2
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
• 229960005167 everolimus Drugs 0.000 claims 2
• 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 2
• 125000001072 heteroaryl group Chemical group 0.000 claims 2
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
• 208000032839 leukemia Diseases 0.000 claims 2
• 125000002950 monocyclic group Chemical group 0.000 claims 2
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
• 125000004430 oxygen atom Chemical group O* 0.000 claims 2
• 230000002265 prevention Effects 0.000 claims 2
• 230000002062 proliferating effect Effects 0.000 claims 2
• 125000003373 pyrazinyl group Chemical group 0.000 claims 2
• 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
• 229910052717 sulfur Inorganic materials 0.000 claims 2
• 125000004434 sulfur atom Chemical group 0.000 claims 2
• CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims 1
• 125000004423 acyloxy group Chemical group 0.000 claims 1
• 125000002947 alkylene group Chemical group 0.000 claims 1
• ZDQSOHOQTUFQEM-PKUCKEGBSA-N ascomycin Chemical compound C/C([C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@]2(O)O[C@@H]([C@H](C[C@H]2C)OC)[C@@H](OC)C[C@@H](C)C\C(C)=C/[C@H](C(C[C@H](O)[C@H]1C)=O)CC)=C\[C@@H]1CC[C@@H](O)[C@H](OC)C1 ZDQSOHOQTUFQEM-PKUCKEGBSA-N 0.000 claims 1
• ZDQSOHOQTUFQEM-XCXYXIJFSA-N ascomycin Natural products CC[C@H]1C=C(C)C[C@@H](C)C[C@@H](OC)[C@H]2O[C@@](O)([C@@H](C)C[C@H]2OC)C(=O)C(=O)N3CCCC[C@@H]3C(=O)O[C@H]([C@H](C)[C@@H](O)CC1=O)C(=C[C@@H]4CC[C@@H](O)[C@H](C4)OC)C ZDQSOHOQTUFQEM-XCXYXIJFSA-N 0.000 claims 1
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
• 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
• 150000001875 compounds Chemical class 0.000 claims 1
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
• 229910052736 halogen Inorganic materials 0.000 claims 1
• 150000002367 halogens Chemical class 0.000 claims 1
• 229910052760 oxygen Inorganic materials 0.000 claims 1
• 239000001301 oxygen Substances 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 125000004076 pyridyl group Chemical group 0.000 claims 1
• QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 1
• 229960000235 temsirolimus Drugs 0.000 claims 1
• 229950009819 zotarolimus Drugs 0.000 claims 1
• CGTADGCBEXYWNE-JUKNQOCSSA-N zotarolimus Chemical compound N1([C@H]2CC[C@@H](C[C@@H](C)[C@H]3OC(=O)[C@@H]4CCCCN4C(=O)C(=O)[C@@]4(O)[C@H](C)CC[C@H](O4)C[C@@H](/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C3)OC)C[C@H]2OC)C=NN=N1 CGTADGCBEXYWNE-JUKNQOCSSA-N 0.000 claims 1