JP2013505940A5 - - Google Patents
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- Publication number
- JP2013505940A5 JP2013505940A5 JP2012531020A JP2012531020A JP2013505940A5 JP 2013505940 A5 JP2013505940 A5 JP 2013505940A5 JP 2012531020 A JP2012531020 A JP 2012531020A JP 2012531020 A JP2012531020 A JP 2012531020A JP 2013505940 A5 JP2013505940 A5 JP 2013505940A5
- Authority
- JP
- Japan
- Prior art keywords
- chloro
- methyl
- administered
- combination
- fluoro
- 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
- -1 2-fluoro-4-iodo-phenylamino Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- YFQJOPFTGMHYNV-YDALLXLXSA-N n-[(2s)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide;hydrochloride Chemical compound Cl.CN1N=CC(Cl)=C1C1=C(Cl)SC(C(=O)N[C@H](CN)CC=2C=C(F)C=CC=2)=C1 YFQJOPFTGMHYNV-YDALLXLXSA-N 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethyl sulfoxide Natural products CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 3
- 238000002648 combination therapy Methods 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000012423 maintenance Methods 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 1
- RGJSVKAUQGSGDN-UHFFFAOYSA-N 4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide;hydrochloride Chemical compound Cl.CN1N=CC(Cl)=C1C1=CSC(C(N)=O)=C1 RGJSVKAUQGSGDN-UHFFFAOYSA-N 0.000 claims 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical class N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- PGNUBDXGTOZIHC-UHFFFAOYSA-N 4-chloro-1-methylpyrazole Chemical compound CN1C=C(Cl)C=N1 PGNUBDXGTOZIHC-UHFFFAOYSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm 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
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- METKIMKYRPQLGS-UHFFFAOYSA-N atenolol Chemical compound CC(C)NCC(O)COC1=CC=C(CC(N)=O)C=C1 METKIMKYRPQLGS-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical compound 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 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24502709P | 2009-09-23 | 2009-09-23 | |
| US61/245,027 | 2009-09-23 | ||
| PCT/US2010/049952 WO2011038085A1 (en) | 2009-09-23 | 2010-09-23 | Combination |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015246841A Division JP6148320B2 (ja) | 2009-09-23 | 2015-12-18 | 組合せ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013505940A JP2013505940A (ja) | 2013-02-21 |
| JP2013505940A5 true JP2013505940A5 (enExample) | 2013-11-14 |
| JP5890310B2 JP5890310B2 (ja) | 2016-03-22 |
Family
ID=43796199
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012531020A Expired - Fee Related JP5890310B2 (ja) | 2009-09-23 | 2010-09-23 | 組合せ |
| JP2015246841A Expired - Fee Related JP6148320B2 (ja) | 2009-09-23 | 2015-12-18 | 組合せ |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015246841A Expired - Fee Related JP6148320B2 (ja) | 2009-09-23 | 2015-12-18 | 組合せ |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US20120283278A1 (enExample) |
| EP (1) | EP2480085B1 (enExample) |
| JP (2) | JP5890310B2 (enExample) |
| KR (1) | KR101739158B1 (enExample) |
| CN (1) | CN102762098B (enExample) |
| AU (1) | AU2010298280B2 (enExample) |
| BR (1) | BR112012006485A2 (enExample) |
| CA (1) | CA2775125C (enExample) |
| EA (2) | EA201270453A1 (enExample) |
| ES (1) | ES2527831T3 (enExample) |
| IL (1) | IL218801A (enExample) |
| MX (1) | MX2012003547A (enExample) |
| SG (1) | SG179144A1 (enExample) |
| WO (1) | WO2011038085A1 (enExample) |
| ZA (1) | ZA201201940B (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP2913048A1 (en) | 2014-02-27 | 2015-09-02 | ratiopharm GmbH | Pharmaceutical composition comprising trametinib |
| US20230172936A1 (en) * | 2020-05-11 | 2023-06-08 | Cleave Therapeutics, Inc. | VCP/p97 INHIBITOR FOR THE TREATMENT OF CANCER |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7378423B2 (en) * | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| DE602005004286T2 (de) * | 2004-06-11 | 2009-01-02 | Japan Tobacco Inc. | 5-amino-2,4,7-trioxo-3,4,7,8-tetrahydro-2h-pyridoä2,3-düpyrimidinderivate und verwandte verbindungen zur behandlung von krebs |
| JP3821154B1 (ja) * | 2005-03-16 | 2006-09-13 | いすゞ自動車株式会社 | 排気ガス浄化方法及び排気ガス浄化システム |
| UY30892A1 (es) * | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
-
2010
- 2010-09-23 EA EA201270453A patent/EA201270453A1/ru unknown
- 2010-09-23 MX MX2012003547A patent/MX2012003547A/es active IP Right Grant
- 2010-09-23 CA CA2775125A patent/CA2775125C/en not_active Expired - Fee Related
- 2010-09-23 WO PCT/US2010/049952 patent/WO2011038085A1/en not_active Ceased
- 2010-09-23 SG SG2012018164A patent/SG179144A1/en unknown
- 2010-09-23 EP EP10819438.2A patent/EP2480085B1/en active Active
- 2010-09-23 ES ES10819438.2T patent/ES2527831T3/es active Active
- 2010-09-23 JP JP2012531020A patent/JP5890310B2/ja not_active Expired - Fee Related
- 2010-09-23 BR BR112012006485A patent/BR112012006485A2/pt active Search and Examination
- 2010-09-23 CN CN201080052973.XA patent/CN102762098B/zh not_active Expired - Fee Related
- 2010-09-23 AU AU2010298280A patent/AU2010298280B2/en not_active Ceased
- 2010-09-23 KR KR1020127010301A patent/KR101739158B1/ko not_active Expired - Fee Related
- 2010-09-23 US US13/497,580 patent/US20120283278A1/en not_active Abandoned
-
2012
- 2012-03-15 ZA ZA2012/01940A patent/ZA201201940B/en unknown
- 2012-03-22 IL IL218801A patent/IL218801A/en not_active IP Right Cessation
-
2014
- 2014-06-27 US US14/317,775 patent/US20140309243A1/en not_active Abandoned
-
2015
- 2015-09-25 EA EA201500882A patent/EA201500882A1/ru unknown
- 2015-12-18 JP JP2015246841A patent/JP6148320B2/ja not_active Expired - Fee Related
-
2016
- 2016-02-02 US US15/013,228 patent/US20160143913A1/en not_active Abandoned
-
2018
- 2018-03-27 US US15/936,659 patent/US20180214451A1/en not_active Abandoned
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