JP2015508096A5 - - Google Patents
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- Publication number
- JP2015508096A5 JP2015508096A5 JP2014558256A JP2014558256A JP2015508096A5 JP 2015508096 A5 JP2015508096 A5 JP 2015508096A5 JP 2014558256 A JP2014558256 A JP 2014558256A JP 2014558256 A JP2014558256 A JP 2014558256A JP 2015508096 A5 JP2015508096 A5 JP 2015508096A5
- Authority
- JP
- Japan
- Prior art keywords
- trifluoromethyl
- amino
- bipyrimidinyl
- morpholin
- methyl
- 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
- 150000001875 compounds Chemical class 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 16
- 206010028980 Neoplasm Diseases 0.000 claims 12
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 208000034578 Multiple myelomas Diseases 0.000 claims 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 3
- 208000003174 Brain Neoplasms Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 3
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 3
- 208000017604 Hodgkin disease Diseases 0.000 claims 3
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 3
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 3
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 3
- 206010038389 Renal cancer Diseases 0.000 claims 3
- 206010039491 Sarcoma Diseases 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 3
- 210000004100 adrenal gland Anatomy 0.000 claims 3
- 201000005188 adrenal gland cancer Diseases 0.000 claims 3
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 3
- 210000004556 brain Anatomy 0.000 claims 3
- 210000000481 breast Anatomy 0.000 claims 3
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 3
- 210000001072 colon Anatomy 0.000 claims 3
- 208000029742 colonic neoplasm Diseases 0.000 claims 3
- 201000004101 esophageal cancer Diseases 0.000 claims 3
- 210000003238 esophagus Anatomy 0.000 claims 3
- 206010017758 gastric cancer Diseases 0.000 claims 3
- 208000005017 glioblastoma Diseases 0.000 claims 3
- 210000003734 kidney Anatomy 0.000 claims 3
- 201000010982 kidney cancer Diseases 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 210000004185 liver Anatomy 0.000 claims 3
- 201000007270 liver cancer Diseases 0.000 claims 3
- 208000014018 liver neoplasm Diseases 0.000 claims 3
- 210000004072 lung Anatomy 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 3
- 210000001672 ovary Anatomy 0.000 claims 3
- 210000000496 pancreas Anatomy 0.000 claims 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 3
- 210000002307 prostate Anatomy 0.000 claims 3
- 206010038038 rectal cancer Diseases 0.000 claims 3
- 210000000664 rectum Anatomy 0.000 claims 3
- 201000001275 rectum cancer Diseases 0.000 claims 3
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 3
- 210000002784 stomach Anatomy 0.000 claims 3
- 201000011549 stomach cancer Diseases 0.000 claims 3
- 239000000126 substance Substances 0.000 claims 3
- 201000002510 thyroid cancer Diseases 0.000 claims 3
- 210000003932 urinary bladder Anatomy 0.000 claims 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims 3
- 210000001215 vagina Anatomy 0.000 claims 3
- 206010046885 vaginal cancer Diseases 0.000 claims 3
- 208000013139 vaginal neoplasm Diseases 0.000 claims 3
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- -1 2′-amino-2-morpholino-4 ′-(trifluoromethyl)-[4,5′-bipyrimidin] -6-yl Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- BDAGIHXWWSANSR-UHFFFAOYSA-N methanoic acid Natural products OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 claims 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims 2
- CUZHYMLWMBVXNZ-NEPJUHHUSA-N (3ar,6ar)-3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]oxazol-2-one Chemical compound FC(F)(F)C1=NC(N)=NC=C1C1=CC(N2C(O[C@H]3COC[C@H]32)=O)=NC(N2CCOCC2)=N1 CUZHYMLWMBVXNZ-NEPJUHHUSA-N 0.000 claims 1
- YDFWDRYMAKYLOY-YRGRVCCFSA-N (3ar,6r,6ar)-3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-6-hydroxy-4,5,6,6a-tetrahydro-3ah-cyclopenta[d][1,3]oxazol-2-one Chemical compound FC(F)(F)C1=NC(N)=NC=C1C1=CC(N2C(O[C@H]3[C@H](O)CC[C@H]32)=O)=NC(N2CCOCC2)=N1 YDFWDRYMAKYLOY-YRGRVCCFSA-N 0.000 claims 1
- YDFWDRYMAKYLOY-OBJOEFQTSA-N (3as,6s,6as)-3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-6-hydroxy-4,5,6,6a-tetrahydro-3ah-cyclopenta[d][1,3]oxazol-2-one Chemical compound FC(F)(F)C1=NC(N)=NC=C1C1=CC(N2C(O[C@@H]3[C@@H](O)CC[C@@H]32)=O)=NC(N2CCOCC2)=N1 YDFWDRYMAKYLOY-OBJOEFQTSA-N 0.000 claims 1
- RAFZQDWSGKEORO-QGZVFWFLSA-N (4r)-3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-4-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one Chemical compound OC[C@]1(C)COC(=O)N1C1=CC(C=2C(=NC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 RAFZQDWSGKEORO-QGZVFWFLSA-N 0.000 claims 1
- RAFZQDWSGKEORO-KRWDZBQOSA-N (4s)-3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-4-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one Chemical compound OC[C@@]1(C)COC(=O)N1C1=CC(C=2C(=NC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 RAFZQDWSGKEORO-KRWDZBQOSA-N 0.000 claims 1
- BRPIFAODBNJVGK-GXFFZTMASA-N (4s,5r)-3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-5-(2-hydroxyethyl)-4-methyl-1,3-oxazolidin-2-one Chemical compound C[C@H]1[C@@H](CCO)OC(=O)N1C1=CC(C=2C(=NC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 BRPIFAODBNJVGK-GXFFZTMASA-N 0.000 claims 1
- RAFZQDWSGKEORO-UHFFFAOYSA-N 3-[6-[2-amino-4-(trifluoromethyl)pyrimidin-5-yl]-2-morpholin-4-ylpyrimidin-4-yl]-4-(hydroxymethyl)-4-methyl-1,3-oxazolidin-2-one Chemical compound OCC1(C)COC(=O)N1C1=CC(C=2C(=NC(N)=NC=2)C(F)(F)F)=NC(N2CCOCC2)=N1 RAFZQDWSGKEORO-UHFFFAOYSA-N 0.000 claims 1
- OSWFIVFLDKOXQC-UHFFFAOYSA-N 4-(3-methoxyphenyl)aniline Chemical compound COC1=CC=CC(C=2C=CC(N)=CC=2)=C1 OSWFIVFLDKOXQC-UHFFFAOYSA-N 0.000 claims 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 229910052805 deuterium Inorganic materials 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 235000019253 formic acid Nutrition 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000007962 solid dispersion Substances 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261602954P | 2012-02-24 | 2012-02-24 | |
| US61/602,954 | 2012-02-24 | ||
| US201261736707P | 2012-12-13 | 2012-12-13 | |
| US61/736,707 | 2012-12-13 | ||
| PCT/IB2013/051443 WO2013124826A1 (en) | 2012-02-24 | 2013-02-22 | Oxazolidin- 2 -one compounds and uses thereof as pi3ks inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015508096A JP2015508096A (ja) | 2015-03-16 |
| JP2015508096A5 true JP2015508096A5 (https=) | 2016-04-21 |
| JP6154404B2 JP6154404B2 (ja) | 2017-06-28 |
Family
ID=48142031
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014558256A Active JP6154404B2 (ja) | 2012-02-24 | 2013-02-22 | オキサゾリジン−２−オン化合物およびｐｉ３ｋ阻害剤としてのその使用 |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US8865894B2 (https=) |
| EP (1) | EP2817307B1 (https=) |
| JP (1) | JP6154404B2 (https=) |
| KR (1) | KR101640698B1 (https=) |
| CN (1) | CN104144926B (https=) |
| AP (1) | AP2014007835A0 (https=) |
| AR (1) | AR090121A1 (https=) |
| AU (1) | AU2013223713C1 (https=) |
| BR (1) | BR112014020672B1 (https=) |
| CA (1) | CA2865372A1 (https=) |
| CO (1) | CO7051028A2 (https=) |
| CR (1) | CR20140397A (https=) |
| DO (1) | DOP2014000194A (https=) |
| EA (1) | EA026031B1 (https=) |
| ES (1) | ES2598118T3 (https=) |
| GE (1) | GEP20156389B (https=) |
| GT (1) | GT201400178A (https=) |
| HK (1) | HK1199643A1 (https=) |
| IL (1) | IL233936A (https=) |
| MX (1) | MX353341B (https=) |
| NI (1) | NI201400089A (https=) |
| NZ (1) | NZ629198A (https=) |
| PE (1) | PE20142456A1 (https=) |
| PH (1) | PH12014501900A1 (https=) |
| PL (1) | PL2817307T3 (https=) |
| PT (1) | PT2817307T (https=) |
| SG (1) | SG11201404794XA (https=) |
| TW (1) | TW201339155A (https=) |
| UY (1) | UY34632A (https=) |
| WO (1) | WO2013124826A1 (https=) |
| ZA (1) | ZA201405446B (https=) |
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|---|---|---|---|---|
| KR20140069235A (ko) | 2011-09-27 | 2014-06-09 | 노파르티스 아게 | 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온 |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| WO2014043208A1 (en) * | 2012-09-11 | 2014-03-20 | Medivation Prostate Therapeutics, Inc. | Formulations of enzalutamide |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| EP2970240B1 (en) | 2013-03-14 | 2018-01-10 | Novartis AG | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| SG10201900002QA (en) | 2014-01-24 | 2019-02-27 | Dana Farber Cancer Institue Inc | Antibody molecules to pd-1 and uses thereof |
| EP3099717B1 (en) | 2014-01-31 | 2019-03-27 | Novartis AG | Antibody molecules to tim-3 and uses thereof |
| US20150259420A1 (en) | 2014-03-14 | 2015-09-17 | Novartis Ag | Antibody molecules to lag-3 and uses thereof |
| AP2016009374A0 (en) | 2014-03-24 | 2016-08-31 | Novartis Ag | Monobactam organic compounds for the treatment of bacterial infections |
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| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| TWI716362B (zh) | 2014-10-14 | 2021-01-21 | 瑞士商諾華公司 | 針對ｐｄ－ｌ１之抗體分子及其用途 |
| US10023576B2 (en) | 2014-10-22 | 2018-07-17 | Bristol-Myers Squibb Company | Heteroaryl substituted pyrrolotriazine amine compounds as PI3K inhibitors |
| US10214537B2 (en) | 2014-10-22 | 2019-02-26 | Bristol-Myers Squibb Company | Bicyclic heteroaryl amine compounds |
| WO2016100882A1 (en) | 2014-12-19 | 2016-06-23 | Novartis Ag | Combination therapies |
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| EP3878465A1 (en) | 2015-07-29 | 2021-09-15 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
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| CN118307674A (zh) | 2017-06-22 | 2024-07-09 | 诺华股份有限公司 | 针对cd73的抗体分子及其用途 |
| WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
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| AR126019A1 (es) | 2018-05-30 | 2023-09-06 | Novartis Ag | Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación |
| US20210214459A1 (en) | 2018-05-31 | 2021-07-15 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| CN109134558A (zh) * | 2018-09-21 | 2019-01-04 | 常州方圆制药有限公司 | 一种提高1-N-乙基庆大霉素Cla收率的合成方法 |
| CN109970764B (zh) * | 2019-03-26 | 2021-11-09 | 上海吉奉生物科技有限公司 | 一种（S）-1,1,5,5-四甲基二氢恶唑并[3,4-c]恶唑-3-酮的合成方法 |
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