JP2012526767A5 - - Google Patents
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- Publication number
- JP2012526767A5 JP2012526767A5 JP2012510280A JP2012510280A JP2012526767A5 JP 2012526767 A5 JP2012526767 A5 JP 2012526767A5 JP 2012510280 A JP2012510280 A JP 2012510280A JP 2012510280 A JP2012510280 A JP 2012510280A JP 2012526767 A5 JP2012526767 A5 JP 2012526767A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- pharmaceutically acceptable
- acceptable salt
- composition according
- tautomer
- 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
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- 150000003839 salts Chemical group 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 9
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 6
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 5
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 4
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 4
- 229910019142 PO4 Inorganic materials 0.000 claims 4
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 4
- 239000010452 phosphate Substances 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 3
- 229940125904 compound 1 Drugs 0.000 claims 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 2
- 229910002651 NO3 Inorganic materials 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 0.000 claims 2
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 2
- 229940125782 compound 2 Drugs 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 claims 2
- 150000002688 maleic acid derivatives Chemical class 0.000 claims 2
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 2
- 229940095064 tartrate Drugs 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010055113 Breast cancer metastatic Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome 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
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 150000001558 benzoic acid derivatives Chemical class 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 150000001860 citric acid derivatives Chemical class 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 208000006178 malignant mesothelioma Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 230000000683 nonmetastatic effect Effects 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 208000037964 urogenital cancer Diseases 0.000 claims 1
- KSGXQBZTULBEEQ-UHFFFAOYSA-N CCCCCCOC(NC(c(cc1)ccc1NCc1nc2cc(C(N(CCC(OCC)=O)c3ncccc3)=O)ccc2[n]1C)=N)=O Chemical compound CCCCCCOC(NC(c(cc1)ccc1NCc1nc2cc(C(N(CCC(OCC)=O)c3ncccc3)=O)ccc2[n]1C)=N)=O KSGXQBZTULBEEQ-UHFFFAOYSA-N 0.000 description 2
- ULXXDDBFHOBEHA-CWDCEQMOSA-N CN(C)C/C=C/C(Nc(c(O[C@@H]1COCC1)c1)cc2c1ncnc2Nc(cc1Cl)ccc1F)=O Chemical compound CN(C)C/C=C/C(Nc(c(O[C@@H]1COCC1)c1)cc2c1ncnc2Nc(cc1Cl)ccc1F)=O ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 description 2
- ZMADHQHIRBTTMZ-ZIADKAODSA-N CN(C(CN1CCN(C)CC1)=O)c(cc1)ccc1N/C(/c1ccccc1)=C(/c1ccc(C(O)OC)cc1N1)\C1=O Chemical compound CN(C(CN1CCN(C)CC1)=O)c(cc1)ccc1N/C(/c1ccccc1)=C(/c1ccc(C(O)OC)cc1N1)\C1=O ZMADHQHIRBTTMZ-ZIADKAODSA-N 0.000 description 1
- YBSJFWOBGCMAKL-UHFFFAOYSA-N C[n](c(CNc(cc1)ccc1C(N)=N)nc1c2)c1ccc2C(N(CCC(O)=O)c1ccccn1)=O Chemical compound C[n](c(CNc(cc1)ccc1C(N)=N)nc1c2)c1ccc2C(N(CCC(O)=O)c1ccccn1)=O YBSJFWOBGCMAKL-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09160202.9 | 2009-05-14 | ||
| EP09160202 | 2009-05-14 | ||
| PCT/EP2010/056504 WO2010130758A1 (en) | 2009-05-14 | 2010-05-11 | New combination therapy in treatment of cancer and fibrotic diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012526767A JP2012526767A (ja) | 2012-11-01 |
| JP2012526767A5 true JP2012526767A5 (cg-RX-API-DMAC7.html) | 2013-06-27 |
Family
ID=41119563
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012510280A Pending JP2012526767A (ja) | 2009-05-14 | 2010-05-11 | 癌及び線維性疾患の処置における新規な併用療法 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20120136004A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2429527A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2012526767A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2010130758A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2647375A1 (en) * | 2009-05-14 | 2013-10-09 | Boehringer Ingelheim International Gmbh | Combination of vargatef and dabigatran for the treatment of oncological and fibrotic diseases |
| CN103476770B (zh) * | 2010-11-25 | 2017-02-15 | 拉蒂欧制药有限责任公司 | 阿法替尼盐和多晶型物 |
| CN102649778A (zh) * | 2011-02-23 | 2012-08-29 | 苏州波锐生物医药科技有限公司 | 喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途 |
| CN105777656B (zh) * | 2014-12-25 | 2018-02-02 | 深圳海王医药科技研究院有限公司 | 萘普替尼对甲苯磺酸盐的β晶型及制备方法和含有其的药物组合物 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2738741B1 (fr) * | 1995-09-19 | 1997-12-05 | Oreal | Composition pour la teinture des fibres keratiniques, contenant un antagoniste de substance p |
| DE10063435A1 (de) * | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US7019012B2 (en) * | 2000-12-20 | 2006-03-28 | Boehringer Ingelheim International Pharma Gmbh & Co. Kg | Quinazoline derivatives and pharmaceutical compositions containing them |
| DE10233500A1 (de) * | 2002-07-24 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylen]-6-methoxycarbonyl-2-indolinon-Monoethansulfonat und dessen Verwendung als Arzneimittel |
| PE20060777A1 (es) * | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| EP2340837B1 (en) * | 2005-11-11 | 2017-03-15 | Boehringer Ingelheim International GmbH | Combination treatment of cancer comprising egfr/her2 inhibitors |
| WO2007057397A1 (en) * | 2005-11-15 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Treatment of cancer |
| EP2043632A2 (en) * | 2006-07-17 | 2009-04-08 | Boehringer Ingelheim International GmbH | New indications for direct thrombin inhibitors |
| PT2068880E (pt) * | 2006-09-18 | 2012-07-12 | Boehringer Ingelheim Int | Método para tratamento do cancro apresentando mutações no egfr |
| EP2647375A1 (en) * | 2009-05-14 | 2013-10-09 | Boehringer Ingelheim International Gmbh | Combination of vargatef and dabigatran for the treatment of oncological and fibrotic diseases |
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2010
- 2010-05-11 JP JP2012510280A patent/JP2012526767A/ja active Pending
- 2010-05-11 WO PCT/EP2010/056504 patent/WO2010130758A1/en not_active Ceased
- 2010-05-11 US US13/318,395 patent/US20120136004A1/en not_active Abandoned
- 2010-05-11 EP EP10719343A patent/EP2429527A1/en not_active Withdrawn
-
2013
- 2013-11-06 US US14/073,030 patent/US20140066456A1/en not_active Abandoned