JP2013511525A5 - - Google Patents
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- Publication number
- JP2013511525A5 JP2013511525A5 JP2012539983A JP2012539983A JP2013511525A5 JP 2013511525 A5 JP2013511525 A5 JP 2013511525A5 JP 2012539983 A JP2012539983 A JP 2012539983A JP 2012539983 A JP2012539983 A JP 2012539983A JP 2013511525 A5 JP2013511525 A5 JP 2013511525A5
- Authority
- JP
- Japan
- Prior art keywords
- combination
- cancer
- administered
- dimethyl
- trioxo
- Prior art date
- 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
- 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 11
- 229960005167 everolimus Drugs 0.000 claims 11
- -1 2-fluoro-4-iodo-phenylamino Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- 208000032839 leukemia Diseases 0.000 claims 4
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000000389 T-cell leukemia Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims 2
- 238000012423 maintenance Methods 0.000 claims 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 150000003462 sulfoxides Chemical class 0.000 claims 2
- OQUFJVRYDFIQBW-UHFFFAOYSA-N trametinib dimethyl sulfoxide Chemical compound CS(C)=O.CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 OQUFJVRYDFIQBW-UHFFFAOYSA-N 0.000 claims 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 1
- IMXHGCRIEAKIBU-UHFFFAOYSA-N 4-[6-[4-(methoxycarbonylamino)phenyl]-4-(4-morpholinyl)-1-pyrazolo[3,4-d]pyrimidinyl]-1-piperidinecarboxylic acid methyl ester Chemical compound C1=CC(NC(=O)OC)=CC=C1C1=NC(N2CCOCC2)=C(C=NN2C3CCN(CC3)C(=O)OC)C2=N1 IMXHGCRIEAKIBU-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- KVLFRAWTRWDEDF-IRXDYDNUSA-N AZD-8055 Chemical compound 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 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 201000007815 Bannayan-Riley-Ruvalcaba syndrome Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005969 Bone giant cell tumour Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims 1
- 208000036566 Erythroleukaemia Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000005726 Inflammatory Breast Neoplasms Diseases 0.000 claims 1
- 206010021980 Inflammatory carcinoma of the breast Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000035490 Megakaryoblastic Acute Leukemia Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims 1
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 claims 1
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims 1
- 206010061934 Salivary gland cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 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
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000021841 acute erythroid leukemia Diseases 0.000 claims 1
- 208000013593 acute megakaryoblastic leukemia Diseases 0.000 claims 1
- 208000020700 acute megakaryocytic leukemia Diseases 0.000 claims 1
- 201000011143 bone giant cell tumor Diseases 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethyl sulfoxide Natural products CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000004653 inflammatory breast carcinoma Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- VDOCQQKGPJENHJ-UHFFFAOYSA-N methyl n-[4-[4-morpholin-4-yl-1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]pyrazolo[3,4-d]pyrimidin-6-yl]phenyl]carbamate Chemical compound C1=CC(NC(=O)OC)=CC=C1C1=NC(N2CCOCC2)=C(C=NN2C3CCN(CC=4C=NC=CC=4)CC3)C2=N1 VDOCQQKGPJENHJ-UHFFFAOYSA-N 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 210000000440 neutrophil Anatomy 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 210000004180 plasmocyte Anatomy 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 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 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 229960001302 ridaforolimus Drugs 0.000 claims 1
- 150000003839 salts Chemical class 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
- 229960002930 sirolimus Drugs 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229960000235 temsirolimus Drugs 0.000 claims 1
- 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 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 230000002861 ventricular Effects 0.000 claims 1
- 201000005102 vulva cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26181309P | 2009-11-17 | 2009-11-17 | |
| US61/261,813 | 2009-11-17 | ||
| PCT/US2010/056931 WO2011062930A1 (en) | 2009-11-17 | 2010-11-17 | Combination |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013511525A JP2013511525A (ja) | 2013-04-04 |
| JP2013511525A5 true JP2013511525A5 (enExample) | 2013-12-26 |
| JP5834370B2 JP5834370B2 (ja) | 2015-12-16 |
Family
ID=44059949
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012539983A Expired - Fee Related JP5834370B2 (ja) | 2009-11-17 | 2010-11-17 | 組合せ |
Country Status (17)
| Country | Link |
|---|---|
| US (4) | US20120283279A1 (enExample) |
| EP (1) | EP2501379B1 (enExample) |
| JP (1) | JP5834370B2 (enExample) |
| KR (1) | KR20120117779A (enExample) |
| CN (2) | CN104382906A (enExample) |
| AU (1) | AU2010322105B2 (enExample) |
| BR (1) | BR112012011677A8 (enExample) |
| CA (1) | CA2781063A1 (enExample) |
| EA (1) | EA022637B1 (enExample) |
| ES (1) | ES2578191T3 (enExample) |
| IL (1) | IL219786A (enExample) |
| MX (1) | MX2012005758A (enExample) |
| PL (1) | PL2501379T3 (enExample) |
| PT (1) | PT2501379E (enExample) |
| SG (1) | SG10201407558TA (enExample) |
| WO (1) | WO2011062930A1 (enExample) |
| ZA (1) | ZA201203444B (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2640390A4 (en) * | 2010-11-17 | 2014-08-06 | Glaxosmithkline Ip No 2 Ltd | METHODS OF TREATING CANCER |
| TWI505828B (zh) | 2010-12-20 | 2015-11-01 | 葛蘭素史克智慧財產（第二）有限公司 | 新穎醫藥組成物 |
| HK1201828A1 (en) * | 2011-11-08 | 2015-09-11 | Intellikine, Llc | Treatment regimens using multiple pharmaceutical agents |
| WO2014059095A1 (en) * | 2012-10-12 | 2014-04-17 | Glaxosmithkline Llc | Combinations |
| CA2946759A1 (en) * | 2014-04-25 | 2015-10-29 | Memorial Sloan-Kettering Cancer Center | Treatment of h-ras-driven tumors |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004004644A2 (en) * | 2002-07-05 | 2004-01-15 | Beth Israel Deaconess Medical Center | Combination of mtor inhibitor and a tyrosine kinase inhibitor for the treatment of neoplasms |
| US7378423B2 (en) * | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| PT1761528E (pt) * | 2004-06-11 | 2008-04-15 | Japan Tobacco Inc | Derivados de 5-amino-2,4,7-trioxo-3,4,7,8-tetra-hidro-2hpirido[ 2,3-d]pirimidina e compostos relacionados para o tratamento do cancro |
| BRPI0818426A2 (pt) * | 2007-10-15 | 2017-06-13 | Astrazeneca Ab | produto de combinação, uso de um produto de combinação, e, método para tratar câncer |
-
2010
- 2010-11-17 JP JP2012539983A patent/JP5834370B2/ja not_active Expired - Fee Related
- 2010-11-17 AU AU2010322105A patent/AU2010322105B2/en not_active Ceased
- 2010-11-17 EA EA201290339A patent/EA022637B1/ru not_active IP Right Cessation
- 2010-11-17 WO PCT/US2010/056931 patent/WO2011062930A1/en not_active Ceased
- 2010-11-17 KR KR1020127015509A patent/KR20120117779A/ko not_active Abandoned
- 2010-11-17 BR BR112012011677A patent/BR112012011677A8/pt not_active IP Right Cessation
- 2010-11-17 CN CN201410535441.1A patent/CN104382906A/zh active Pending
- 2010-11-17 US US13/509,955 patent/US20120283279A1/en not_active Abandoned
- 2010-11-17 MX MX2012005758A patent/MX2012005758A/es active IP Right Grant
- 2010-11-17 CA CA2781063A patent/CA2781063A1/en not_active Abandoned
- 2010-11-17 PL PL10832068.0T patent/PL2501379T3/pl unknown
- 2010-11-17 PT PT108320680T patent/PT2501379E/pt unknown
- 2010-11-17 EP EP10832068.0A patent/EP2501379B1/en active Active
- 2010-11-17 ES ES10832068.0T patent/ES2578191T3/es active Active
- 2010-11-17 CN CN2010800616827A patent/CN102724979A/zh active Pending
- 2010-11-17 SG SG10201407558TA patent/SG10201407558TA/en unknown
-
2012
- 2012-05-11 ZA ZA2012/03444A patent/ZA201203444B/en unknown
- 2012-05-14 IL IL219786A patent/IL219786A/en not_active IP Right Cessation
-
2014
- 2014-06-19 US US14/309,262 patent/US20140303195A1/en not_active Abandoned
-
2015
- 2015-09-24 US US14/863,709 patent/US20160008368A1/en not_active Abandoned
-
2016
- 2016-11-16 US US15/352,813 patent/US20170065593A1/en not_active Abandoned
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