JP2012526766A5 - - Google Patents
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- Publication number
- JP2012526766A5 JP2012526766A5 JP2012510279A JP2012510279A JP2012526766A5 JP 2012526766 A5 JP2012526766 A5 JP 2012526766A5 JP 2012510279 A JP2012510279 A JP 2012510279A JP 2012510279 A JP2012510279 A JP 2012510279A JP 2012526766 A5 JP2012526766 A5 JP 2012526766A5
- 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
Links
- 150000003839 salts Chemical group 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 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
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 5
- 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
- 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
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 2
- 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
- 206010028980 Neoplasm Diseases 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
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 2
- CCIVGXIOQKPBKL-UHFFFAOYSA-N ethanesulfonic acid Chemical class CCS(O)(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-N 0.000 claims 2
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 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 class 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
- 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
- 229910002651 NO3 Inorganic materials 0.000 claims 1
- NHNBFGGVMKEFGY-UHFFFAOYSA-N Nitrate Chemical compound [O-][N+]([O-])=O NHNBFGGVMKEFGY-UHFFFAOYSA-N 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
- 201000011510 cancer Diseases 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
- 150000002823 nitrates Chemical class 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
- UGEWTLXHMYKLCO-UHFFFAOYSA-N CCCCCCOC(NC(c(cc1)ccc1NCc1nc2cc(C(N(CCC(O)=O)c3ccccn3)=O)ccc2[n]1C)=N)=O Chemical compound CCCCCCOC(NC(c(cc1)ccc1NCc1nc2cc(C(N(CCC(O)=O)c3ccccn3)=O)ccc2[n]1C)=N)=O UGEWTLXHMYKLCO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09160203.7 | 2009-05-14 | ||
| EP09160203 | 2009-05-14 | ||
| PCT/EP2010/056503 WO2010130757A1 (en) | 2009-05-14 | 2010-05-11 | New combination therapy in treatment of oncological and fibrotic diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012526766A JP2012526766A (ja) | 2012-11-01 |
| JP2012526766A5 true JP2012526766A5 (enExample) | 2013-06-27 |
Family
ID=41016957
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012510279A Pending JP2012526766A (ja) | 2009-05-14 | 2010-05-11 | 腫瘍性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) | US20120142703A1 (enExample) |
| EP (2) | EP2647375A1 (enExample) |
| JP (1) | JP2012526766A (enExample) |
| WO (1) | WO2010130757A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170065529A1 (en) | 2015-09-09 | 2017-03-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical dosage form for immediate release of an indolinone derivative |
| WO2009147212A1 (en) | 2008-06-06 | 2009-12-10 | Boehringer Ingelheim International Gmbh | Capsule pharmaceutical dosage form comprising a suspension formulation of an indolinone derivative |
| UA107560C2 (uk) * | 2008-06-06 | 2015-01-26 | Фармацевтична лікарська форма для негайного вивільнення похідної індолінону | |
| US20120136004A1 (en) * | 2009-05-14 | 2012-05-31 | Boehringer Ingelheim International Gmbh | New combination therapy in treatment of cancer and fibrotic diseases |
| 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 |
| CN103102352B (zh) * | 2011-11-15 | 2015-08-12 | 山东亨利医药科技有限责任公司 | 酪氨酸激酶抑制剂吲哚满酮衍生物 |
| CN103130775B (zh) * | 2011-11-22 | 2015-09-30 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的吲哚满酮衍生物 |
| JP2015524825A (ja) * | 2012-08-17 | 2015-08-27 | キャンサー・セラピューティクス・シーアールシー・ピーティーワイ・リミテッド | Ｖｅｇｆｒ３阻害剤 |
| US9238644B2 (en) * | 2012-08-17 | 2016-01-19 | Cancer Therapeutics Crc Pty Limited | VEGFR3 inhibitors |
| CN103768067A (zh) * | 2012-10-23 | 2014-05-07 | 杨子娇 | 一类治疗房角狭窄的化合物及其用途 |
| WO2014138727A1 (en) * | 2013-03-08 | 2014-09-12 | Board Of Regents, The University Of Texas System | Suppression of malignant mesothelioma by overexpression or stimulation of endothelial protein c receptors (epcr) |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| UA75054C2 (uk) | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу |
| DE10063435A1 (de) | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| EA009664B1 (ru) | 2002-03-07 | 2008-02-28 | Бёрингер Ингельхайм Фарма Гмбх Унд Ко. Кг | Предназначенная для перорального применения лекарственная форма для этилового эфира 3-[(2-{[4-(гексилоксикарбониламиноиминометил)фениламино]метил}-1-метил-1h-бензимидазол-5-карбонил)пиридин-2-иламино]пропионовой кислоты и его солей |
| 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 |
| DE10237423A1 (de) | 2002-08-16 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verwendung von LCK-Inhibitoren für die Behandlung von immunologischen Erkrankungen |
| US20050043233A1 (en) * | 2003-04-29 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis |
| DE10339862A1 (de) | 2003-08-29 | 2005-03-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-[(2-{[4-(Hexyloxycarbonylamino-imino-methyl)- phenylamino]-methyl}-1-methyl-1H-benzimidazol-5-carbonyl)-pyridin-2-yl-amino]-propionsäure-ethylester-Methansulfonat und dessen Verwendung als Arzneimittel |
| DE10349113A1 (de) | 2003-10-17 | 2005-05-12 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung von Aminocrotonylverbindungen |
| PE20060777A1 (es) * | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| PL1948180T3 (pl) | 2005-11-11 | 2013-09-30 | Boehringer Ingelheim Int | Terapia skojarzona raka polegająca na podawaniu inhibitorów EGFR/HER2 |
| CA2833852C (en) | 2005-11-11 | 2014-10-21 | Boehringer Ingelheim International Gmbh | Quinazoline derivatives for the treatment of cancer diseases |
| WO2007057397A1 (en) * | 2005-11-15 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Treatment of cancer |
| EP1870400A1 (en) | 2006-06-08 | 2007-12-26 | Boehringer Ingelheim Pharma GmbH & Co. KG | Salts and crystalline salt forms of an 2-indolinone derivative |
| CA2657269A1 (en) * | 2006-07-17 | 2008-01-24 | Boehringer Ingelheim International Gmbh | New indications for direct thrombin inhibitors |
| US20120136004A1 (en) * | 2009-05-14 | 2012-05-31 | Boehringer Ingelheim International Gmbh | New combination therapy in treatment of cancer and fibrotic diseases |
-
2010
- 2010-05-11 WO PCT/EP2010/056503 patent/WO2010130757A1/en not_active Ceased
- 2010-05-11 EP EP13174888.1A patent/EP2647375A1/en not_active Withdrawn
- 2010-05-11 JP JP2012510279A patent/JP2012526766A/ja active Pending
- 2010-05-11 EP EP10721441A patent/EP2429520A1/en not_active Ceased
- 2010-05-11 US US13/318,289 patent/US20120142703A1/en not_active Abandoned
-
2014
- 2014-03-06 US US14/198,726 patent/US20140187563A1/en not_active Abandoned
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