JP2016503010A5 - - Google Patents
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- Publication number
- JP2016503010A5 JP2016503010A5 JP2015547524A JP2015547524A JP2016503010A5 JP 2016503010 A5 JP2016503010 A5 JP 2016503010A5 JP 2015547524 A JP2015547524 A JP 2015547524A JP 2015547524 A JP2015547524 A JP 2015547524A JP 2016503010 A5 JP2016503010 A5 JP 2016503010A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- crystalline
- ylethynyl
- pyridazin
- imidazo
- 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
- -1 imidazo [1,2-b] pyridazin-3-ylethynyl Chemical group 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 9
- 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 8
- 238000000034 method Methods 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 230000008018 melting Effects 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- SNIABFMMCKVXSY-UHFFFAOYSA-N benzoylazanium;chloride Chemical compound Cl.NC(=O)C1=CC=CC=C1 SNIABFMMCKVXSY-UHFFFAOYSA-N 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 210000004214 philadelphia chromosome Anatomy 0.000 claims 1
- PHXJVRSECIGDHY-UHFFFAOYSA-N ponatinib Chemical compound C1CN(C)CCN1CC(C(=C1)C(F)(F)F)=CC=C1NC(=O)C1=CC=C(C)C(C#CC=2N3N=CC=CC3=NC=2)=C1 PHXJVRSECIGDHY-UHFFFAOYSA-N 0.000 claims 1
- BWTNNZPNKQIADY-UHFFFAOYSA-N ponatinib hydrochloride Chemical compound Cl.C1CN(C)CCN1CC(C(=C1)C(F)(F)F)=CC=C1NC(=O)C1=CC=C(C)C(C#CC=2N3N=CC=CC3=NC=2)=C1 BWTNNZPNKQIADY-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261736543P | 2012-12-12 | 2012-12-12 | |
| US61/736,543 | 2012-12-12 | ||
| US201261737007P | 2012-12-13 | 2012-12-13 | |
| US61/737,007 | 2012-12-13 | ||
| US201361788208P | 2013-03-15 | 2013-03-15 | |
| US61/788,208 | 2013-03-15 | ||
| PCT/US2013/074571 WO2014093579A2 (en) | 2012-12-12 | 2013-12-12 | Crystalline forms of 3-(imidazo[1,2-b] pyridazin-3-ylethynyl)-4-methyl-n-(4-[(4-methylpiperazin-1-yl) methyl]-3-(trifluoromethyl)phenyl)benzamide and its mono hydrochloride salt |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018129624A Division JP7042175B2 (ja) | 2012-12-12 | 2018-07-09 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016503010A JP2016503010A (ja) | 2016-02-01 |
| JP2016503010A5 true JP2016503010A5 (enExample) | 2017-01-26 |
| JP6447508B2 JP6447508B2 (ja) | 2019-01-09 |
Family
ID=50929140
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015547524A Active JP6447508B2 (ja) | 2012-12-12 | 2013-12-12 | ３−（イミダゾ［１，２−ｂ］ピリダジン−３−イルエチニル）−４−メチル−Ｎ−｛４−［（４−メチルピペラジン−１−イル）メチル］−３−（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
| JP2018129624A Active JP7042175B2 (ja) | 2012-12-12 | 2018-07-09 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
| JP2021203538A Active JP7352841B2 (ja) | 2012-12-12 | 2021-12-15 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
| JP2023150905A Pending JP2023179498A (ja) | 2012-12-12 | 2023-09-19 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
| JP2025171607A Pending JP2026010061A (ja) | 2012-12-12 | 2025-10-10 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018129624A Active JP7042175B2 (ja) | 2012-12-12 | 2018-07-09 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
| JP2021203538A Active JP7352841B2 (ja) | 2012-12-12 | 2021-12-15 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
| JP2023150905A Pending JP2023179498A (ja) | 2012-12-12 | 2023-09-19 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
| JP2025171607A Pending JP2026010061A (ja) | 2012-12-12 | 2025-10-10 | ３－（イミダゾ［１，２－ｂ］ピリダジン－３－イルエチニル）－４－メチル－Ｎ－｛４－［（４－メチルピペラジン－１－イル）メチル］－３－（トリフルオロメチル）フェニル｝ベンズアミドおよびその一塩酸塩の結晶形 |
Country Status (9)
| Country | Link |
|---|---|
| US (9) | US9493470B2 (enExample) |
| JP (5) | JP6447508B2 (enExample) |
| CN (2) | CN105188701A (enExample) |
| CA (3) | CA2815506C (enExample) |
| CL (1) | CL2015001643A1 (enExample) |
| HK (1) | HK1218878A1 (enExample) |
| MX (11) | MX391445B (enExample) |
| NZ (1) | NZ709648A (enExample) |
| WO (2) | WO2014093579A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1973545T3 (da) | 2005-12-23 | 2013-02-25 | Ariad Pharma Inc | Bicykliske heteroarylforbindelser |
| TWI568722B (zh) | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物 |
| CA2815506C (en) | 2012-12-12 | 2018-12-11 | Ariad Pharmaceuticals, Inc. | Crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride |
| EP3016954B1 (en) * | 2013-07-04 | 2018-10-31 | Sandoz AG | Crystalline forms of ponatinib hydrochloride |
| CN104496995A (zh) * | 2014-01-06 | 2015-04-08 | 广东东阳光药业有限公司 | 制备3-乙炔基咪唑并[1,2-b]哒嗪的方法 |
| EA201991197A1 (ru) * | 2016-12-15 | 2020-01-13 | Ариад Фармасьютикалз, Инк. | БЕНЗИМИДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ c-Kit |
| US10221184B2 (en) | 2017-01-20 | 2019-03-05 | Apicore Us Llc | Polymorphs of ponatinib hydrochloride |
| US11072620B2 (en) | 2017-06-20 | 2021-07-27 | Apotex Inc. | Crystalline forms of Ponatinib hydrochloride |
| ES2941266T3 (es) * | 2018-04-02 | 2023-05-19 | Stealth Biotherapeutics Inc | Dipéptidos cristalinos útiles en la síntesis elamipretide |
| EP3781568A1 (en) | 2018-06-22 | 2021-02-24 | Johnson Matthey Public Limited Company | Form of ponatinib |
| US12240869B2 (en) | 2018-11-01 | 2025-03-04 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2020223235A1 (en) | 2019-04-29 | 2020-11-05 | Incyte Corporation | Mini-tablet dosage forms of ponatinib |
| CN111004240B (zh) * | 2019-12-13 | 2020-12-01 | 山东铂源药业有限公司 | 一种泊那替尼中间体3-乙炔基咪唑并[1,2-b]哒嗪的合成方法 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5099067A (en) * | 1988-08-05 | 1992-03-24 | Northwestern University | Use of ammonium formate as a hydrogen transfer reagent for reduction of chiral nitro compounds with retention of configuration |
| JP4903963B2 (ja) | 1999-11-08 | 2012-03-28 | シェーリング コーポレイション | Ｎ−（４−ヒドロキシ−フェニル）−ｎ’−（４’−アミノフェニル）−ピペラジンを調製するためのプロセス |
| HN2001000008A (es) | 2000-01-21 | 2003-12-11 | Inc Agouron Pharmaceuticals | Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo |
| DE10021246A1 (de) | 2000-04-25 | 2001-10-31 | Schering Ag | Substituierte Benzoesäureamide und deren Verwendung als Arzneimittel |
| IL159811A0 (en) | 2001-07-13 | 2004-06-20 | Neurogen Corp | Heteroaryl substituted fused bicyclic heteroaryl compounds as gabaa receptor ligands |
| AR041992A1 (es) | 2002-11-06 | 2005-06-08 | Smithkline Beecham Corp | Compuesto de piridinil benzoheterociclico, composicion farmaceutica que lo comprende y su uso para prepararla |
| GB0230089D0 (en) | 2002-12-24 | 2003-01-29 | Astrazeneca Ab | Therapeutic agents |
| TW200529849A (en) | 2003-11-28 | 2005-09-16 | Novartis Ag | Diaryl urea derivatives in the treatment of protein kinase dependent diseases |
| EP1694691A1 (en) | 2003-12-05 | 2006-08-30 | Biovitrum Ab | Improved synthesis of 2-substituted adenosines |
| ATE415970T1 (de) | 2003-12-24 | 2008-12-15 | Astrazeneca Ab | Pyrimidine mit tie2 (tek) aktivität |
| EP1737462B1 (en) | 2003-12-24 | 2008-07-30 | AstraZeneca AB | Pyrimidines with tie2 (tek) activity |
| AU2005231980B2 (en) | 2004-04-07 | 2011-09-08 | Merck Serono Sa | 1,1'-(1,2-ethynediyl)bis-benzene derivatives as PTP 1-B inhibitors |
| EP1771169A1 (en) | 2004-07-14 | 2007-04-11 | PTC Therapeutics, Inc. | Methods for treating hepatitis c |
| US7776869B2 (en) | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| GB0502418D0 (en) | 2005-02-05 | 2005-03-16 | Astrazeneca Ab | Compounds |
| US20080194552A1 (en) | 2005-03-31 | 2008-08-14 | Astrazeneca Ab | Aminopyrimidine Derivatives With Tie2 Inhibiting Activity |
| JP2009502734A (ja) | 2005-07-29 | 2009-01-29 | アステラス製薬株式会社 | Ｌｃｋ阻害剤としての縮合複素環 |
| US8071609B2 (en) | 2005-08-11 | 2011-12-06 | Ariad Pharmaceuticals, Inc. | Unsaturated heterocyclic derivatives |
| DK1973545T3 (da) | 2005-12-23 | 2013-02-25 | Ariad Pharma Inc | Bicykliske heteroarylforbindelser |
| SI1973545T1 (sl) * | 2005-12-23 | 2013-04-30 | Ariad Pharmaceuticals, Inc. | Spojine bicikličnega heteroarila |
| ES2555515T3 (es) | 2006-05-08 | 2016-01-04 | Ariad Pharmaceuticals, Inc. | Compuestos de heteroarilo monocíclico |
| WO2007133560A2 (en) | 2006-05-08 | 2007-11-22 | Ariad Pharmaceuticals, Inc. | Acetylenic heteroaryl compounds |
| EP2107054A1 (en) | 2008-04-01 | 2009-10-07 | Università Degli Studi Di Milano - Bicocca | Antiproliferative compounds and therapeutic uses thereof |
| WO2010124047A1 (en) | 2009-04-23 | 2010-10-28 | Wyeth Llc | Bisaryl alkynylamides as negative allosteric modulators of metabotropic glutamate receptor 5 (mglur5) |
| US8329724B2 (en) * | 2009-08-03 | 2012-12-11 | Hoffmann-La Roche Inc. | Process for the manufacture of pharmaceutically active compounds |
| CA2777128A1 (en) * | 2009-10-30 | 2011-05-05 | Ariad Pharmaceuticals, Inc. | Methods and compositions for treating cancer |
| WO2012139027A1 (en) | 2011-04-07 | 2012-10-11 | Ariad Pharmaceuticals, Inc. | Methods and compositions for treating neurodegenerative diseases |
| CA2832465A1 (en) | 2011-04-07 | 2013-07-04 | Ariad Pharmaceuticals, Inc. | Methods and compositions for treating parkinson's disease |
| WO2013162727A1 (en) | 2012-04-25 | 2013-10-31 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
| CA2815506C (en) * | 2012-12-12 | 2018-12-11 | Ariad Pharmaceuticals, Inc. | Crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride |
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2013
- 2013-05-09 CA CA2815506A patent/CA2815506C/en active Active
- 2013-05-09 CA CA3022250A patent/CA3022250A1/en not_active Abandoned
- 2013-05-09 CA CA3167093A patent/CA3167093A1/en active Pending
- 2013-12-12 CN CN201380072027.5A patent/CN105188701A/zh active Pending
- 2013-12-12 MX MX2018010998A patent/MX391445B/es unknown
- 2013-12-12 CN CN202210369530.8A patent/CN115043843A/zh active Pending
- 2013-12-12 HK HK16106954.3A patent/HK1218878A1/zh unknown
- 2013-12-12 WO PCT/US2013/074571 patent/WO2014093579A2/en not_active Ceased
- 2013-12-12 JP JP2015547524A patent/JP6447508B2/ja active Active
- 2013-12-12 WO PCT/US2013/074585 patent/WO2014093583A2/en not_active Ceased
- 2013-12-12 NZ NZ709648A patent/NZ709648A/en unknown
- 2013-12-12 MX MX2015007578A patent/MX359147B/es active IP Right Grant
- 2013-12-12 US US14/651,577 patent/US9493470B2/en active Active
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2015
- 2015-06-12 MX MX2021002253A patent/MX2021002253A/es unknown
- 2015-06-12 CL CL2015001643A patent/CL2015001643A1/es unknown
- 2015-06-12 MX MX2021002256A patent/MX2021002256A/es unknown
- 2015-06-12 MX MX2021002259A patent/MX2021002259A/es unknown
- 2015-06-12 MX MX2021002258A patent/MX2021002258A/es unknown
- 2015-06-12 MX MX2021002254A patent/MX2021002254A/es unknown
- 2015-06-12 MX MX2021002257A patent/MX2021002257A/es unknown
- 2015-06-12 MX MX2021002255A patent/MX2021002255A/es unknown
- 2015-06-12 MX MX2021002264A patent/MX2021002264A/es unknown
- 2015-06-12 MX MX2021002261A patent/MX2021002261A/es unknown
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2016
- 2016-11-02 US US15/341,898 patent/US10125136B2/en active Active
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2018
- 2018-07-09 JP JP2018129624A patent/JP7042175B2/ja active Active
- 2018-09-28 US US16/146,143 patent/US10662197B2/en active Active
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2020
- 2020-05-22 US US16/881,790 patent/US11279705B2/en active Active
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2021
- 2021-05-12 US US17/318,832 patent/US11192897B2/en active Active
- 2021-05-12 US US17/318,876 patent/US11384086B2/en active Active
- 2021-05-12 US US17/318,772 patent/US11192896B2/en active Active
- 2021-05-12 US US17/318,677 patent/US11192895B2/en active Active
- 2021-12-15 JP JP2021203538A patent/JP7352841B2/ja active Active
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2023
- 2023-02-27 US US18/175,272 patent/US20240083902A1/en not_active Abandoned
- 2023-09-19 JP JP2023150905A patent/JP2023179498A/ja active Pending
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2025
- 2025-10-10 JP JP2025171607A patent/JP2026010061A/ja active Pending