JP2014533277A5 - - Google Patents

Info

Publication number

JP2014533277A5

JP2014533277A5 JP2014541310A JP2014541310A JP2014533277A5 JP 2014533277 A5 JP2014533277 A5 JP 2014533277A5 JP 2014541310 A JP2014541310 A JP 2014541310A JP 2014541310 A JP2014541310 A JP 2014541310A JP 2014533277 A5 JP2014533277 A5 JP 2014533277A5

Authority

JP

Japan

Prior art keywords

combination

administered

inhibitor

subject

pharmaceutical

Prior art date

2012-11-09

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 239000000203 mixture Substances 0.000 claims 28
• 101001034652 Homo sapiens Insulin-like growth factor 1 receptor Proteins 0.000 claims 22
• 102100039688 Insulin-like growth factor 1 receptor Human genes 0.000 claims 22
• 239000003112 inhibitor Substances 0.000 claims 22
• 229940124302 mTOR inhibitor Drugs 0.000 claims 22
• 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 22
• 239000003814 drug Substances 0.000 claims 18
• 206010028980 Neoplasm Diseases 0.000 claims 15
• 239000000825 pharmaceutical preparation Substances 0.000 claims 13
• 229940127557 pharmaceutical product Drugs 0.000 claims 13
• 201000011510 cancer Diseases 0.000 claims 9
• 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 9
• 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 9
• 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 7
• 229960005167 everolimus Drugs 0.000 claims 7
• 238000009472 formulation Methods 0.000 claims 6
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
• -1 SAR543 Chemical compound 0.000 claims 2
• 239000002246 antineoplastic agent Substances 0.000 claims 2
• 229940127089 cytotoxic agent Drugs 0.000 claims 2
• 230000000762 glandular Effects 0.000 claims 2
• 238000000034 method Methods 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
• GYLDXIAOMVERTK-UHFFFAOYSA-N 5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine Chemical compound C12=C(N)N=CN=C2N(C(C)C)N=C1C1=CC=C(OC(N)=N2)C2=C1 GYLDXIAOMVERTK-UHFFFAOYSA-N 0.000 claims 1
• 206010052399 Neuroendocrine tumour 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
• 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
• 239000012635 anticancer drug combination Substances 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
• JROFGZPOBKIAEW-UHFFFAOYSA-N chembl2132692 Chemical compound N1C=2C(OC)=CC=CC=2C=C1C(=C1C(N)=NC=NN11)N=C1C1CCC(C(O)=O)CC1 JROFGZPOBKIAEW-UHFFFAOYSA-N 0.000 claims 1
• 229940000425 combination drug Drugs 0.000 claims 1
• 238000002648 combination therapy Methods 0.000 claims 1
• 150000001875 compounds Chemical class 0.000 claims 1
• 239000002254 cytotoxic agent Substances 0.000 claims 1
• 231100000599 cytotoxic agent Toxicity 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
• 230000003176 fibrotic effect Effects 0.000 claims 1
• 208000016065 neuroendocrine neoplasm Diseases 0.000 claims 1
• 201000011519 neuroendocrine tumor Diseases 0.000 claims 1
• 230000005855 radiation Effects 0.000 claims 1
• 229950009216 sapanisertib Drugs 0.000 claims 1
• QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical group 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
• 238000011301 standard therapy Methods 0.000 claims 1
• 229960000235 temsirolimus Drugs 0.000 claims 1
• 208000008732 thymoma Diseases 0.000 claims 1
• 230000003442 weekly effect Effects 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