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 (enExample) | 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 (enExample) |
| EP (1) | EP2257544B1 (enExample) |
| JP (1) | JP2011515370A (enExample) |
| KR (1) | KR20100137517A (enExample) |
| CN (1) | CN101970425B (enExample) |
| AR (1) | AR070924A1 (enExample) |
| AU (1) | AU2009227003B2 (enExample) |
| BR (1) | BRPI0909762A2 (enExample) |
| CA (1) | CA2718076A1 (enExample) |
| CL (1) | CL2009000651A1 (enExample) |
| CO (1) | CO6321253A2 (enExample) |
| EC (1) | ECSP10010555A (enExample) |
| IL (1) | IL208020A0 (enExample) |
| MA (1) | MA32230B1 (enExample) |
| MX (1) | MX2010010152A (enExample) |
| MY (1) | MY150554A (enExample) |
| NZ (2) | NZ600887A (enExample) |
| PE (1) | PE20091628A1 (enExample) |
| PH (2) | PH12012502569A1 (enExample) |
| RU (1) | RU2497820C2 (enExample) |
| SG (1) | SG188919A1 (enExample) |
| TW (1) | TWI426072B (enExample) |
| WO (1) | WO2009115562A2 (enExample) |
| ZA (1) | ZA201006263B (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR070924A1 (es) | 2008-03-19 | 2010-05-12 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales del acido lactico de 4- amino -5- fluoro-3-(5-(4-metilpiperazin-1-il ) -1h- bencimidazol-2-il) quinolin -2-(1h) - ona |
| WO2011128405A1 (en) | 2010-04-16 | 2011-10-20 | Novartis Ag | Combination of organic compounds |
| PL2558095T3 (pl) | 2010-04-16 | 2019-06-28 | Novartis Ag | Związek organiczny, przeznaczony do stosowania w leczeniu raka wątroby |
| 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. |
| KR20140062485A (ko) | 2011-09-15 | 2014-05-23 | 노파르티스 아게 | 중등도 간 손상 환자의 암 치료에 있어서 4-아미노-5-플루오로-3-[6-(4-메틸피페라진-1-일)-1h-벤즈이미다졸-2-일]-1h-퀴놀린-2-온의 용도 |
| WO2013063003A1 (en) | 2011-10-28 | 2013-05-02 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
| JP2015505562A (ja) | 2012-01-31 | 2015-02-23 | ノバルティス アーゲー | Ｒｔｋ阻害剤と抗エストロゲン剤との組合せ、およびがん治療のためのその使用 |
| BR112015000349A2 (pt) | 2012-07-11 | 2017-06-27 | Novartis Ag | método de tratamento de tumores estromais gastrointestinais |
| 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 |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
| LT3116909T (lt) | 2014-03-14 | 2020-02-10 | Novartis Ag | Antikūno molekulės prieš lag-3 ir jų panaudojimas |
| 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 |
| EP3206711B1 (en) | 2014-10-14 | 2023-05-31 | Novartis AG | Antibody molecules to pd-l1 and uses thereof |
| EP3233918A1 (en) | 2014-12-19 | 2017-10-25 | Novartis AG | Combination therapies |
| PE20171448A1 (es) | 2015-03-10 | 2017-10-02 | Aduro Biotech Inc | Composiciones y metodos para activar la senalizacion dependiente del estimulador del gen de interferon |
| WO2017019897A1 (en) | 2015-07-29 | 2017-02-02 | Novartis Ag | Combination therapies comprising antibody molecules to tim-3 |
| CN114272371A (zh) | 2015-07-29 | 2022-04-05 | 诺华股份有限公司 | 包含抗pd-1抗体分子的联合疗法 |
| EP3317301B1 (en) | 2015-07-29 | 2021-04-07 | Novartis AG | Combination therapies comprising antibody molecules to lag-3 |
| CA3004138A1 (en) | 2015-11-03 | 2017-05-11 | Janssen Biotech, Inc. | Antibodies specifically binding pd-1 and tim-3 and their uses |
| ES2986067T3 (es) | 2015-12-17 | 2024-11-08 | Novartis Ag | Moléculas de anticuerpos frente a PD-1 y usos de las mismas |
| WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds 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 |
|---|---|---|---|---|
| ATE309996T1 (de) * | 2000-09-11 | 2005-12-15 | Chiron Corp | Chinolinonderivate als tyrosin-kinase inhibitoren |
| US20050256157A1 (en) * | 2002-08-23 | 2005-11-17 | Chiron Corporation | Combination therapy with CHK1 inhibitors |
| EP1539754A4 (en) * | 2002-08-23 | 2009-02-25 | Novartis Vaccines & Diagnostic | BENZIMIDAZOCHINOLINONE AND ITS USE |
| US7825132B2 (en) * | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| US7838527B2 (en) * | 2002-11-13 | 2010-11-23 | Novartis Vaccines And Diagnostics, Inc. | Methods of treating cancer and related methods |
| 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 |
| JP4890255B2 (ja) * | 2003-11-07 | 2012-03-07 | ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド | 改良された薬物特性を有するキノリノン化合物の薬学的に受容可能な塩 |
| RU2377988C2 (ru) * | 2004-02-20 | 2010-01-10 | Новартис Вэксинес Энд Дайэгностикс, Инк. | Модуляция воспалительных и метастатических процессов |
| SG173317A1 (en) * | 2005-01-27 | 2011-08-29 | Novartis Vaccines & Diagnostic | Treatment of metastasized tumors |
| AU2006249847B2 (en) * | 2005-05-23 | 2012-12-20 | Novartis Ag | Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one lactic acid salts |
| 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 |
| AR070924A1 (es) | 2008-03-19 | 2010-05-12 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales del acido lactico de 4- amino -5- fluoro-3-(5-(4-metilpiperazin-1-il ) -1h- bencimidazol-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 AR ARP090100957A patent/AR070924A1/es unknown
- 2009-03-17 PE PE2009000395A patent/PE20091628A1/es not_active Application Discontinuation
- 2009-03-18 CA CA2718076A patent/CA2718076A1/en not_active Abandoned
- 2009-03-18 NZ NZ600887A patent/NZ600887A/xx not_active IP Right Cessation
- 2009-03-18 CN CN200980108402.0A patent/CN101970425B/zh not_active Expired - Fee Related
- 2009-03-18 SG SG2013020011A patent/SG188919A1/en unknown
- 2009-03-18 BR BRPI0909762A patent/BRPI0909762A2/pt not_active IP Right Cessation
- 2009-03-18 RU RU2010142396/04A patent/RU2497820C2/ru not_active IP Right Cessation
- 2009-03-18 AU AU2009227003A patent/AU2009227003B2/en not_active Ceased
- 2009-03-18 EP EP09721534.7A patent/EP2257544B1/en active Active
- 2009-03-18 MY MYPI20104156 patent/MY150554A/en unknown
- 2009-03-18 MX MX2010010152A patent/MX2010010152A/es not_active Application Discontinuation
- 2009-03-18 KR KR1020107023196A patent/KR20100137517A/ko not_active Ceased
- 2009-03-18 JP JP2011500221A patent/JP2011515370A/ja active Pending
- 2009-03-18 WO PCT/EP2009/053222 patent/WO2009115562A2/en not_active Ceased
- 2009-03-18 TW TW098108804A patent/TWI426072B/zh not_active IP Right Cessation
- 2009-03-18 CL CL2009000651A patent/CL2009000651A1/es unknown
- 2009-03-18 NZ NZ587829A patent/NZ587829A/xx not_active IP Right Cessation
- 2009-03-18 US US12/922,213 patent/US8563556B2/en not_active Expired - Fee Related
-
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 PH12012502569A patent/PH12012502569A1/en unknown
- 2012-12-26 PH PH12012502568A patent/PH12012502568A1/en unknown
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