JP2011515370A5 - - Google Patents
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- Publication number
- JP2011515370A5 JP2011515370A5 JP2011500221A JP2011500221A JP2011515370A5 JP 2011515370 A5 JP2011515370 A5 JP 2011515370A5 JP 2011500221 A JP2011500221 A JP 2011500221A JP 2011500221 A JP2011500221 A JP 2011500221A JP 2011515370 A5 JP2011515370 A5 JP 2011515370A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- ray powder
- powder diffraction
- substantially pure
- pure crystalline
- 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.)
- Pending
Links
- 238000000634 powder X-ray diffraction Methods 0.000 claims 9
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- 125000004174 2-benzimidazolyl group Chemical group [H]N1C(*)=NC2=C([H])C([H])=C([H])C([H])=C12 0.000 claims 3
- PDQDKDDEHHXEMI-UHFFFAOYSA-N 2-hydroxypropanoic acid 1H-quinolin-2-one Chemical compound CC(O)C(O)=O.O=C1NC2=C(C=CC=C2)C=C1 PDQDKDDEHHXEMI-UHFFFAOYSA-N 0.000 claims 3
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 3
- VIDDDLSZDPUIHF-UHFFFAOYSA-N 5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]quinolin-4-amine Chemical compound C1CN(C)CCN1C1=CC=C(N=C(N2)C=3C(=C4C(F)=CC=CC4=NC=3)N)C2=C1 VIDDDLSZDPUIHF-UHFFFAOYSA-N 0.000 claims 3
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010004593 Bile duct cancer Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 1
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 1
- 208000031852 Gastrointestinal stromal cancer Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 101000851007 Homo sapiens Vascular endothelial growth factor receptor 2 Proteins 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas 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
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 1
- 208000026900 bile duct neoplasm Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000000649 small cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3774608P | 2008-03-19 | 2008-03-19 | |
| US61/037,746 | 2008-03-19 | ||
| PCT/EP2009/053222 WO2009115562A2 (en) | 2008-03-19 | 2009-03-18 | Crystalline forms and two solvated forms of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]quinolin-2(1h)-one lactic acid salts |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011515370A JP2011515370A (ja) | 2011-05-19 |
| JP2011515370A5 true JP2011515370A5 (https=) | 2012-04-12 |
Family
ID=40622140
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011500221A Pending JP2011515370A (ja) | 2008-03-19 | 2009-03-18 | ４−アミノ−５−フルオロ−３−［５−（４−メチルピペラジン−１−イル）−１ｈ−ベンズイミダゾール−２−イル］キノリン−２（１ｈ）−オン乳酸塩の結晶形態及び２つの溶媒和物形態 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US8563556B2 (https=) |
| EP (1) | EP2257544B1 (https=) |
| JP (1) | JP2011515370A (https=) |
| KR (1) | KR20100137517A (https=) |
| CN (1) | CN101970425B (https=) |
| AR (1) | AR070924A1 (https=) |
| AU (1) | AU2009227003B2 (https=) |
| BR (1) | BRPI0909762A2 (https=) |
| CA (1) | CA2718076A1 (https=) |
| CL (1) | CL2009000651A1 (https=) |
| CO (1) | CO6321253A2 (https=) |
| EC (1) | ECSP10010555A (https=) |
| IL (1) | IL208020A0 (https=) |
| MA (1) | MA32230B1 (https=) |
| MX (1) | MX2010010152A (https=) |
| MY (1) | MY150554A (https=) |
| NZ (2) | NZ600887A (https=) |
| PE (1) | PE20091628A1 (https=) |
| PH (2) | PH12012502568A1 (https=) |
| RU (1) | RU2497820C2 (https=) |
| SG (1) | SG188919A1 (https=) |
| TW (1) | TWI426072B (https=) |
| WO (1) | WO2009115562A2 (https=) |
| ZA (1) | ZA201006263B (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20091628A1 (es) | 2008-03-19 | 2009-11-19 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona |
| CN102834094B (zh) | 2010-04-16 | 2015-05-06 | 诺华有限公司 | 有机化合物的组合产品及其制药用途 |
| BR112012026289A2 (pt) | 2010-04-16 | 2016-07-12 | Novartis Ag | composto orgânico para uso no tratamento de câncer do fígado |
| AR081776A1 (es) * | 2010-06-30 | 2012-10-17 | Novartis Ag | Composiciones farmaceuticas que comprenden monohidrato de lactato de 4-amino-5-fluoro-3-[6-(4-metil-piperazin-1-il)-1h-bencimidazol-2-il]-1h-quinolin-2-ona, proceso para la produccion de la composicion |
| AU2012229107A1 (en) | 2011-03-17 | 2013-09-19 | Novartis Ag | FGFR and ligands thereof as biomarkers for breast cancer in HR positive subjects |
| MX2013013437A (es) | 2011-05-19 | 2013-12-06 | Novartis Ag | 4-amino-5-fluoro-3- [6- (4-metil-piperazin-1-il) -1h-bencimidazol-2-il] -1h-quinolin-2-ona parea usarse en el tratamiento de un carcinoma adenoide quistico. |
| JP2014526506A (ja) | 2011-09-15 | 2014-10-06 | ノバルティス アーゲー | 中等度肝障害患者の癌治療における４−アミノ−５−フルオロ−３−［６−（４−メチルピペラジン−１−イル）−１ｈ−ベンゾイミダゾール−２−イル］−１ｈ−キノリン−２−オンの使用 |
| WO2013063003A1 (en) | 2011-10-28 | 2013-05-02 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
| EP2809312A1 (en) | 2012-01-31 | 2014-12-10 | Novartis AG | Combination of a rtk inhibitor with an anti - estrogen and use thereof for the treatment of cancer |
| IN2014DN10801A (https=) | 2012-07-11 | 2015-09-04 | Novartis Ag | |
| WO2014058785A1 (en) | 2012-10-10 | 2014-04-17 | Novartis Ag | Combination therapy |
| EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
| PE20170255A1 (es) | 2014-01-24 | 2017-03-22 | Dana Farber Cancer Inst Inc | Moleculas de anticuerpo que se unen a pd-1 y usos de las mismas |
| HUE045065T2 (hu) | 2014-01-31 | 2019-12-30 | Novartis Ag | TIM-3 antitest molekulák és felhasználásaik |
| KR102442436B1 (ko) | 2014-03-14 | 2022-09-15 | 노파르티스 아게 | Lag-3에 대한 항체 분자 및 그의 용도 |
| 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 |
| EP4245376A3 (en) | 2014-10-14 | 2023-12-13 | Novartis AG | Antibody molecules to pd-l1 and uses thereof |
| EP3233918A1 (en) | 2014-12-19 | 2017-10-25 | Novartis AG | Combination therapies |
| EA035817B1 (ru) | 2015-03-10 | 2020-08-14 | Адуро Байотек, Инк. | Композиции и способы для активации сигналинга, зависимого от "гена стимулятора интерферона" |
| HRP20211058T8 (hr) | 2015-07-29 | 2021-11-26 | Novartis Ag | Kombinirane terapije koje sadrže molekule antitijela protiv lag-3 |
| EP3878465A1 (en) | 2015-07-29 | 2021-09-15 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
| EP3328418A1 (en) | 2015-07-29 | 2018-06-06 | Novartis AG | Combination therapies comprising antibody molecules to pd-1 |
| PE20181326A1 (es) | 2015-11-03 | 2018-08-20 | Janssen Biotech Inc | Anticuerpos que se unen especificamente a pd-1 y sus usos |
| ES2986067T3 (es) | 2015-12-17 | 2024-11-08 | Novartis Ag | Moléculas de anticuerpos frente a PD-1 y usos de las mismas |
| EP3507367A4 (en) | 2016-07-05 | 2020-03-25 | Aduro BioTech, Inc. | CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF |
| UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
| US12398209B2 (en) | 2018-01-22 | 2025-08-26 | Janssen Biotech, Inc. | Methods of treating cancers with antagonistic anti-PD-1 antibodies |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60115069T2 (de) | 2000-09-11 | 2006-08-03 | Chiron Corp., Emeryville | Chinolinonderivate als tyrosin-kinase inhibitoren |
| EP1539754A4 (en) | 2002-08-23 | 2009-02-25 | Novartis Vaccines & Diagnostic | BENZIMIDAZOCHINOLINONE AND ITS USE |
| US20050256157A1 (en) | 2002-08-23 | 2005-11-17 | Chiron Corporation | Combination therapy with CHK1 inhibitors |
| US7825132B2 (en) | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| CN100377709C (zh) * | 2002-11-13 | 2008-04-02 | 希龙公司 | 受体酪氨酸激酶抑制剂的制药用途及相关检测方法 |
| SG148864A1 (en) | 2002-11-13 | 2009-01-29 | Chiron Corp | Methods of treating cancer and related methods |
| US20050209247A1 (en) * | 2003-11-07 | 2005-09-22 | Chiron Corporation | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
| EP1718306A2 (en) * | 2004-02-20 | 2006-11-08 | Chiron Corporation | Modulation of inflammatory and metastatic processes |
| EP2301546B1 (en) * | 2005-01-27 | 2014-09-10 | Novartis AG | Treatment of metastasized tumors |
| BRPI0611375A2 (pt) * | 2005-05-23 | 2010-08-31 | Novartis Ag | formas cristalinas e outras de sais de ácido láctico de 4-amino-5-flúor-3-[6-(4-metilpiperazin-1-il)-1h-benzimid azol-2-il]-1h-quinolin-2-ona |
| NZ567550A (en) * | 2005-11-29 | 2011-08-26 | Novartis Ag | Formulations of lactic acid salts of 4-amino-5-fluoro-3-[6-(4-methyl-piperazin-1-yl)-1 H-benzimidazol-2-yl]1H-quinolin-2-one |
| PE20091628A1 (es) | 2008-03-19 | 2009-11-19 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona |
| US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
-
2009
- 2009-03-17 PE PE2009000395A patent/PE20091628A1/es not_active Application Discontinuation
- 2009-03-17 AR ARP090100957A patent/AR070924A1/es unknown
- 2009-03-18 MY MYPI20104156 patent/MY150554A/en unknown
- 2009-03-18 CA CA2718076A patent/CA2718076A1/en not_active Abandoned
- 2009-03-18 BR BRPI0909762A patent/BRPI0909762A2/pt not_active IP Right Cessation
- 2009-03-18 MX MX2010010152A patent/MX2010010152A/es not_active Application Discontinuation
- 2009-03-18 CL CL2009000651A patent/CL2009000651A1/es unknown
- 2009-03-18 CN CN200980108402.0A patent/CN101970425B/zh not_active Expired - Fee Related
- 2009-03-18 AU AU2009227003A patent/AU2009227003B2/en not_active Ceased
- 2009-03-18 RU RU2010142396/04A patent/RU2497820C2/ru not_active IP Right Cessation
- 2009-03-18 JP JP2011500221A patent/JP2011515370A/ja active Pending
- 2009-03-18 SG SG2013020011A patent/SG188919A1/en unknown
- 2009-03-18 TW TW098108804A patent/TWI426072B/zh not_active IP Right Cessation
- 2009-03-18 WO PCT/EP2009/053222 patent/WO2009115562A2/en not_active Ceased
- 2009-03-18 NZ NZ600887A patent/NZ600887A/xx not_active IP Right Cessation
- 2009-03-18 NZ NZ587829A patent/NZ587829A/xx not_active IP Right Cessation
- 2009-03-18 EP EP09721534.7A patent/EP2257544B1/en active Active
- 2009-03-18 US US12/922,213 patent/US8563556B2/en not_active Expired - Fee Related
- 2009-03-18 KR KR1020107023196A patent/KR20100137517A/ko not_active Ceased
-
2010
- 2010-09-01 ZA ZA2010/06263A patent/ZA201006263B/en unknown
- 2010-09-06 IL IL208020A patent/IL208020A0/en not_active IP Right Cessation
- 2010-10-15 MA MA33250A patent/MA32230B1/fr unknown
- 2010-10-19 CO CO10129430A patent/CO6321253A2/es not_active Application Discontinuation
- 2010-10-19 EC EC2010010555A patent/ECSP10010555A/es unknown
-
2012
- 2012-12-26 PH PH12012502568A patent/PH12012502568A1/en unknown
- 2012-12-26 PH PH12012502569A patent/PH12012502569A1/en unknown
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