JP2015500884A5 - - Google Patents

Info

Publication number

JP2015500884A5

JP2015500884A5 JP2014548915A JP2014548915A JP2015500884A5 JP 2015500884 A5 JP2015500884 A5 JP 2015500884A5 JP 2014548915 A JP2014548915 A JP 2014548915A JP 2014548915 A JP2014548915 A JP 2014548915A JP 2015500884 A5 JP2015500884 A5 JP 2015500884A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

group

composition according

mtor inhibitor

formula

Prior art date

2012-12-20

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.)

Withdrawn

Links

• Espacenet
• Global Dossier
• Discuss

• 239000008194 pharmaceutical composition Substances 0.000 claims 15
• 229940124302 mTOR inhibitor Drugs 0.000 claims 8
• 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 8
• 206010028980 Neoplasm Diseases 0.000 claims 7
• 206010021143 Hypoxia Diseases 0.000 claims 5
• 201000011510 cancer Diseases 0.000 claims 5
• 230000007954 hypoxia Effects 0.000 claims 5
• 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 4
• 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 4
• 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 4
• 125000003118 aryl group Chemical group 0.000 claims 4
• 150000001875 compounds Chemical class 0.000 claims 4
• 229960005167 everolimus Drugs 0.000 claims 4
• 239000000651 prodrug Substances 0.000 claims 4
• 229940002612 prodrug Drugs 0.000 claims 4
• 229960000235 temsirolimus Drugs 0.000 claims 4
• QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 claims 4
• 125000001072 heteroaryl group Chemical group 0.000 claims 3
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
• RGHYDLZMTYDBDT-UHFFFAOYSA-N 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone Chemical compound O=C1N(CC)C2=NC(N)=NC(C)=C2C=C1C=1C=CNN=1 RGHYDLZMTYDBDT-UHFFFAOYSA-N 0.000 claims 2
• BUROJSBIWGDYCN-GAUTUEMISA-N AP 23573 Chemical compound C1C[C@@H](OP(C)(C)=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 BUROJSBIWGDYCN-GAUTUEMISA-N 0.000 claims 2
• KVLFRAWTRWDEDF-IRXDYDNUSA-N AZD-8055 Chemical group C1=C(CO)C(OC)=CC=C1C1=CC=C(C(=NC(=N2)N3[C@H](COCC3)C)N3[C@H](COCC3)C)C2=N1 KVLFRAWTRWDEDF-IRXDYDNUSA-N 0.000 claims 2
• 206010003571 Astrocytoma Diseases 0.000 claims 2
• 206010029260 Neuroblastoma Diseases 0.000 claims 2
• 206010052399 Neuroendocrine tumour Diseases 0.000 claims 2
• 208000006265 Renal cell carcinoma Diseases 0.000 claims 2
• 125000003435 aroyl group Chemical group 0.000 claims 2
• JROFGZPOBKIAEW-HAQNSBGRSA-N chembl3120215 Chemical compound N1C=2C(OC)=CC=CC=2C=C1C(=C1C(N)=NC=NN11)N=C1[C@H]1CC[C@H](C(O)=O)CC1 JROFGZPOBKIAEW-HAQNSBGRSA-N 0.000 claims 2
• 229950006418 dactolisib Drugs 0.000 claims 2
• JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical compound O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims 2
• 229910052736 halogen Inorganic materials 0.000 claims 2
• 150000002367 halogens Chemical class 0.000 claims 2
• 125000000623 heterocyclic group Chemical group 0.000 claims 2
• 229910052739 hydrogen Inorganic materials 0.000 claims 2
• 150000002431 hydrogen Chemical class 0.000 claims 2
• 239000001257 hydrogen Substances 0.000 claims 2
• 230000002401 inhibitory effect Effects 0.000 claims 2
• 208000016065 neuroendocrine neoplasm Diseases 0.000 claims 2
• 201000011519 neuroendocrine tumor Diseases 0.000 claims 2
• 229910052760 oxygen Inorganic materials 0.000 claims 2
• ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 2
• 229960001302 ridaforolimus Drugs 0.000 claims 2
• 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 2
• 229960002930 sirolimus Drugs 0.000 claims 2
• 229910052717 sulfur Inorganic materials 0.000 claims 2
• 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
• 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 1
• 208000003174 Brain Neoplasms Diseases 0.000 claims 1
• -1 C 1 -C 6 alkyl Chemical group 0.000 claims 1
• 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
• 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 1
• 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 125000004093 cyano group Chemical group *C#N 0.000 claims 1
• YUCFVHQCAFKDQG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH] YUCFVHQCAFKDQG-UHFFFAOYSA-N 0.000 claims 1
• 201000000062 kidney sarcoma Diseases 0.000 claims 1
• 208000010658 metastatic prostate carcinoma Diseases 0.000 claims 1
• 229910052757 nitrogen Inorganic materials 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
• 150000003839 salts Chemical class 0.000 claims 1
• 230000004614 tumor growth Effects 0.000 claims 1