JP2014511840A5 - - Google Patents
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- Publication number
- JP2014511840A5 JP2014511840A5 JP2014501220A JP2014501220A JP2014511840A5 JP 2014511840 A5 JP2014511840 A5 JP 2014511840A5 JP 2014501220 A JP2014501220 A JP 2014501220A JP 2014501220 A JP2014501220 A JP 2014501220A JP 2014511840 A5 JP2014511840 A5 JP 2014511840A5
- Authority
- JP
- Japan
- Prior art keywords
- dihydro
- oxo
- phenyl
- trifluoropropyl
- succinamide
- 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
- BDBIBRDNIFFYLE-UHFFFAOYSA-N n'-(3,3,3-trifluoropropyl)butanediamide Chemical compound NC(=O)CCC(=O)NCCC(F)(F)F BDBIBRDNIFFYLE-UHFFFAOYSA-N 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 21
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 4
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- -1 3,3,3-trifluoropropyl Chemical group 0.000 claims 3
- 238000001144 powder X-ray diffraction data Methods 0.000 claims 3
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 2
- CZRZGKHVNFKAIZ-UHFFFAOYSA-N C(CCC(=O)N)(=O)NCCCF Chemical compound C(CCC(=O)N)(=O)NCCCF CZRZGKHVNFKAIZ-UHFFFAOYSA-N 0.000 claims 2
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 2
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 229960002448 dasatinib Drugs 0.000 claims 2
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 2
- 229960003957 dexamethasone Drugs 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 229960001603 tamoxifen Drugs 0.000 claims 2
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 239000004359 castor oil Substances 0.000 claims 1
- 235000019438 castor oil Nutrition 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 238000004088 simulation Methods 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 *[C@@]([C@@](*)C(N[C@]1N=C(c2ccccc2)c(cccc2)c2N(*)C1=O)=O)C(N)=O Chemical compound *[C@@]([C@@](*)C(N[C@]1N=C(c2ccccc2)c(cccc2)c2N(*)C1=O)=O)C(N)=O 0.000 description 2
- AYOUDDAETNMCBW-GSHUGGBRSA-N CN(c(cccc1)c1C(c1ccccc1)=N[C@@H]1NC([C@H](CCC(F)(F)F)[C@H](CCC(F)(F)F)C(N)=O)=O)C1=O Chemical compound CN(c(cccc1)c1C(c1ccccc1)=N[C@@H]1NC([C@H](CCC(F)(F)F)[C@H](CCC(F)(F)F)C(N)=O)=O)C1=O AYOUDDAETNMCBW-GSHUGGBRSA-N 0.000 description 2
- WJEXAUOGHKSGBR-GCKMJXCFSA-N NC([C@@H](CCC(F)(F)F)[C@@H](CCC(F)(F)F)C(N[C@H]1N=C(c2ccccc2)c(cccc2)c2NC1=O)=O)=O Chemical compound NC([C@@H](CCC(F)(F)F)[C@@H](CCC(F)(F)F)C(N[C@H]1N=C(c2ccccc2)c(cccc2)c2NC1=O)=O)=O WJEXAUOGHKSGBR-GCKMJXCFSA-N 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161466238P | 2011-03-22 | 2011-03-22 | |
| US61/466,238 | 2011-03-22 | ||
| PCT/US2012/030021 WO2012129353A1 (en) | 2011-03-22 | 2012-03-22 | Bis(fluoroalkyl)-1,4-benzodiazepinone compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014511840A JP2014511840A (ja) | 2014-05-19 |
| JP2014511840A5 true JP2014511840A5 (https=) | 2014-07-31 |
| JP5873923B2 JP5873923B2 (ja) | 2016-03-01 |
Family
ID=45894701
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014501220A Active JP5873923B2 (ja) | 2011-03-22 | 2012-03-22 | ビス（フルオロアルキル）−１，４−ベンゾジアゼピノン化合物 |
Country Status (32)
| Country | Link |
|---|---|
| US (2) | US8629136B2 (https=) |
| EP (1) | EP2688873B1 (https=) |
| JP (1) | JP5873923B2 (https=) |
| KR (1) | KR101948347B1 (https=) |
| CN (1) | CN103717576B (https=) |
| AR (2) | AR085471A1 (https=) |
| AU (1) | AU2012230904B2 (https=) |
| BR (1) | BR112013024059B1 (https=) |
| CA (1) | CA2830902C (https=) |
| CL (1) | CL2013002690A1 (https=) |
| CO (1) | CO6771446A2 (https=) |
| CY (1) | CY1116423T1 (https=) |
| DK (1) | DK2688873T3 (https=) |
| EA (1) | EA022530B1 (https=) |
| ES (1) | ES2534080T3 (https=) |
| HR (1) | HRP20150273T1 (https=) |
| IL (1) | IL228534A (https=) |
| MA (1) | MA35036B1 (https=) |
| MX (1) | MX2013010420A (https=) |
| MY (1) | MY161233A (https=) |
| PE (1) | PE20140626A1 (https=) |
| PH (1) | PH12013501738B1 (https=) |
| PL (1) | PL2688873T3 (https=) |
| PT (1) | PT2688873E (https=) |
| RS (1) | RS53843B1 (https=) |
| SG (1) | SG193555A1 (https=) |
| SI (1) | SI2688873T1 (https=) |
| SM (1) | SMT201500091B (https=) |
| TN (1) | TN2013000372A1 (https=) |
| TW (1) | TWI530489B (https=) |
| UY (1) | UY33961A (https=) |
| WO (1) | WO2012129353A1 (https=) |
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| US9242940B2 (en) | 2012-09-21 | 2016-01-26 | Bristol-Myers Squibb Company | N-substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds |
| WO2014047370A1 (en) * | 2012-09-21 | 2014-03-27 | Bristol-Myers Squibb Company | Fluoroalkyl dibenzodiazepinone compounds |
| CN105308030A (zh) | 2012-09-21 | 2016-02-03 | 百时美施贵宝公司 | 烷基、氟烷基-1,4-苯并二氮杂*酮化合物 |
| TWI614238B (zh) * | 2012-09-21 | 2018-02-11 | 必治妥美雅史谷比公司 | 雙（氟烷基）－１，４－苯并二氮呯酮化合物及其前藥 |
| JP2015531792A (ja) * | 2012-09-21 | 2015-11-05 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | １，４−ベンゾジアゼピノン化合物のプロドラッグ |
| CN104797569A (zh) | 2012-09-21 | 2015-07-22 | 百时美施贵宝公司 | 取代的1,5-苯并二氮杂*酮化合物 |
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| CN1386118A (zh) | 2000-06-01 | 2002-12-18 | 布里斯托尔-迈尔斯斯奎布药品公司 | 作为Aβ蛋白产生抑制剂的被环状琥珀酸酯取代的内酰胺类化合物 |
| US7001901B2 (en) | 2002-08-27 | 2006-02-21 | Bristol-Myers Squibb Company | Tetrazolylpropionamides as inhibitors of Aβ protein production |
| NZ538870A (en) | 2002-09-20 | 2007-04-27 | Arrow Therapeutics Ltd | Benzodiazepine derivatives and pharmaceutical compositions containing them |
| EP1592684B1 (en) | 2003-02-04 | 2008-07-30 | F. Hoffmann-La Roche Ag | Malonamide derivatives as gamma-secretase inhibitors |
| GB0312365D0 (en) | 2003-05-30 | 2003-07-02 | Univ Aston | Novel 3-substituted-1, 4-benzodiazepines |
| KR100838852B1 (ko) | 2003-09-09 | 2008-06-16 | 에프. 호프만-라 로슈 아게 | 감마-세크리테이즈의 활성을 차단하는 말론아미드 유도체 |
| EP1795198A1 (en) | 2005-12-09 | 2007-06-13 | Hubrecht Laboratorium | Treatment of Barret's esophagus |
| CA2644136A1 (en) | 2006-02-27 | 2007-09-07 | The Johns Hopkins University | Cancer treatment with gamma-secretase inhibitors |
| ES2398531T3 (es) | 2006-03-27 | 2013-03-20 | F. Hoffmann-La Roche Ag | Derivados de malonamida como inhibidores de gamma secretasa |
| AU2007299129A1 (en) | 2006-09-20 | 2008-03-27 | F. Hoffmann-La Roche Ag | 4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]diazepine derivatives |
| JP5385904B2 (ja) | 2007-08-14 | 2014-01-08 | イーライ リリー アンド カンパニー | γ−セクレターゼ阻害剤 |
| MA33076B1 (fr) | 2008-01-11 | 2012-03-01 | Hoffmann La Roche | Utilisation d'un inhibiteur de la gamma-secretase pour le traitement du cancer |
| WO2011060051A1 (en) | 2009-11-12 | 2011-05-19 | University Of Massachusetts | Methods for treating glioblastoma |
| US20120225860A1 (en) | 2011-03-02 | 2012-09-06 | John Frederick Boylan | Method for administration of a gamma secretase inhibitor |
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