JP2018509446A5 - - Google Patents
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- Publication number
- JP2018509446A5 JP2018509446A5 JP2017549754A JP2017549754A JP2018509446A5 JP 2018509446 A5 JP2018509446 A5 JP 2018509446A5 JP 2017549754 A JP2017549754 A JP 2017549754A JP 2017549754 A JP2017549754 A JP 2017549754A JP 2018509446 A5 JP2018509446 A5 JP 2018509446A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- naphthyridine
- methoxyethyl
- carboxamide
- pyridin
- 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 5-cyano-4-((2-methoxyethyl) amino) pyridin-2-yl Chemical group 0.000 claims description 38
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 30
- 239000002245 particle Substances 0.000 claims description 28
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 21
- 150000001860 citric acid derivatives Chemical class 0.000 claims description 16
- 238000000034 method Methods 0.000 claims description 13
- 239000011164 primary particle Substances 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 8
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 6
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 6
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 6
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims description 6
- 239000000725 suspension Substances 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims description 4
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 claims description 4
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims description 4
- YKYONYBAUNKHLG-UHFFFAOYSA-N propyl acetate Chemical compound CCCOC(C)=O YKYONYBAUNKHLG-UHFFFAOYSA-N 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 239000013078 crystal Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 238000002360 preparation method Methods 0.000 claims description 2
- 235000019260 propionic acid Nutrition 0.000 claims description 2
- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims description 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 2
- 239000002904 solvent Substances 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003917 carbamoyl group Chemical class [H]N([H])C(*)=O 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 description 3
- QYFLACRBFDPQEP-UHFFFAOYSA-N 2-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound C(=O)C1N(C2=NC=C(C=C2CC1)CN1C(CN(CC1)C)=O)C(=O)N QYFLACRBFDPQEP-UHFFFAOYSA-N 0.000 description 1
- KVIZTDNKHOCNAM-UHFFFAOYSA-N 4-methylpiperazin-2-one Chemical compound CN1CCNC(=O)C1 KVIZTDNKHOCNAM-UHFFFAOYSA-N 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 150000003857 carboxamides Chemical class 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 238000010899 nucleation Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2015/000202 | 2015-03-25 | ||
| CN2015000202 | 2015-03-25 | ||
| PCT/IB2016/051633 WO2016151500A1 (en) | 2015-03-25 | 2016-03-23 | Particles of n-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2- oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2h)-carboxamide |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018509446A JP2018509446A (ja) | 2018-04-05 |
| JP2018509446A5 true JP2018509446A5 (enExample) | 2019-05-09 |
| JP6696995B2 JP6696995B2 (ja) | 2020-05-20 |
Family
ID=55637404
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017549754A Active JP6696995B2 (ja) | 2015-03-25 | 2016-03-23 | Ｎ−（５−シアノ−４−（（２−メトキシエチル）アミノ）ピリジン−２−イル）−７−ホルミル−６−（（４−メチル−２−オキソピペラジン−１−イル）メチル）−３，４−ジヒドロ−１，８−ナフチリジン−１（２ｈ）−カルボキサミドの粒子 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9802917B2 (enExample) |
| EP (1) | EP3274349B1 (enExample) |
| JP (1) | JP6696995B2 (enExample) |
| KR (1) | KR102606643B1 (enExample) |
| CN (1) | CN107406448B (enExample) |
| AR (1) | AR104060A1 (enExample) |
| AU (2) | AU2016238437B2 (enExample) |
| CA (1) | CA2977326C (enExample) |
| ES (1) | ES2803028T3 (enExample) |
| MX (1) | MX2017012293A (enExample) |
| PL (1) | PL3274349T3 (enExample) |
| RU (1) | RU2720456C2 (enExample) |
| TW (1) | TWI699206B (enExample) |
| WO (1) | WO2016151500A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2756748T3 (es) | 2014-10-03 | 2020-04-27 | Novartis Ag | Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4 |
| CN113105454B (zh) * | 2016-05-20 | 2022-10-11 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂、其制备方法和应用 |
| CN107619388A (zh) | 2016-07-13 | 2018-01-23 | 南京天印健华医药科技有限公司 | 作为fgfr抑制剂的杂环化合物 |
| EP3691616A1 (en) * | 2017-10-02 | 2020-08-12 | Novartis AG | Method for preparing a pharmaceutical product |
| CN110234649B (zh) * | 2017-10-31 | 2021-10-15 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂的盐、晶体、制备方法及其用途 |
| CN110225913B (zh) * | 2017-10-31 | 2021-10-15 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂晶型及其制备方法 |
| CN109745321B (zh) * | 2017-11-08 | 2022-04-29 | 上海翰森生物医药科技有限公司 | 包含fgfr4抑制剂的药物组合物 |
| EP3986405A4 (en) * | 2019-06-21 | 2023-06-14 | Terns Pharmaceuticals, Inc. | Compounds for inhibiting fgfr4 |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9420999D0 (en) | 1994-10-18 | 1994-12-07 | Smithkline Beecham Plc | Novel compounds |
| AU3633997A (en) | 1996-07-29 | 1998-02-20 | Banyu Pharmaceutical Co., Ltd. | Chemokine receptor antagonists |
| SK9192000A3 (en) | 1997-12-17 | 2001-03-12 | Merck & Co Inc | Integrin receptor antagonists |
| WO1999041239A1 (en) | 1998-02-10 | 1999-08-19 | Novartis Ag | B cell inhibitors |
| US7115750B1 (en) | 1999-09-20 | 2006-10-03 | Takeda Pharmaceutical Company Limited | Melanin concentrating hormone antagonist |
| TW200305423A (en) | 2002-02-14 | 2003-11-01 | Ono Pharmaceutical Co | N-carbamoyl nitrogen-containing condensed ring compound and medicament containing same as active ingredient |
| WO2004007472A1 (ja) | 2002-07-10 | 2004-01-22 | Ono Pharmaceutical Co., Ltd. | Ｃｃｒ４アンタゴニストおよびその医薬用途 |
| US7098332B2 (en) * | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| WO2004056820A1 (en) | 2002-12-20 | 2004-07-08 | Warner-Lambert Company Llc | Benzoxazines and derivatives thereof as inhibitors of pi3ks |
| JP4736043B2 (ja) | 2003-03-14 | 2011-07-27 | 小野薬品工業株式会社 | 含窒素複素環誘導体およびそれらを有効成分とする薬剤 |
| CA2521619A1 (en) | 2003-04-11 | 2004-10-28 | Taigen Biotechnology | Aminoquinoline compounds |
| SG146624A1 (en) | 2003-09-11 | 2008-10-30 | Kemia Inc | Cytokine inhibitors |
| AU2006271781A1 (en) | 2005-07-15 | 2007-01-25 | F. Hoffmann-La Roche Ag | Novel heteroaryl fused cyclic amines |
| ME00011A (me) | 2005-12-21 | 2009-02-10 | Novartis Ag | Derivati pirimidinilaril uree kao fgf inhibitori |
| CA2635845A1 (en) | 2005-12-29 | 2007-07-12 | Janssen Pharmaceutica N.V. | Prokineticin 2 receptor antagonists |
| RU2008140144A (ru) | 2006-03-10 | 2010-04-20 | Оно Фармасьютикал Ко., Лтд. (Jp) | Азотосодержащее гетероциклическое производное и фармацевтическое средство, включающее такое производное в качестве активного ингредиента |
| WO2007146230A2 (en) | 2006-06-14 | 2007-12-21 | Merck & Co., Inc. | Non-nucleoside reverse transcriptase inhibitors |
| JP2010520881A (ja) | 2007-03-09 | 2010-06-17 | ノバルティス アーゲー | 黒色腫の処置 |
| EP2234618A4 (en) | 2007-12-21 | 2011-04-27 | Scripps Research Inst | BENZOPYRANE AND ANALOGUE AS RHO KINASE INHIBITORS |
| EP2341052A4 (en) | 2008-09-05 | 2011-10-12 | Shionogi & Co | RING-CONDENSED MORPHOLINE DERIVATIVITY WITH PI3K-INHIBITING EFFECT |
| EP2376085B1 (en) | 2008-12-19 | 2014-02-26 | Genentech, Inc. | Compounds and methods of use |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| SG175877A1 (en) | 2009-05-04 | 2011-12-29 | Plexxikon Inc | Compounds and methods for inhibition of renin, and indications therefor |
| WO2011059839A1 (en) | 2009-10-29 | 2011-05-19 | Sirtris Pharmaceuticals, Inc. | Bicyclic pyridines and analogs as sirtuin modulators |
| ES2524548T3 (es) | 2009-10-30 | 2014-12-10 | Novartis Ag | N-óxido de 3-(2,6-dicloro-3,5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperacin-1-il)-fenilamino]-pirimidin-4-il}-1-metil-urea |
| EP2532656A1 (en) | 2010-02-01 | 2012-12-12 | Nippon Chemiphar Co., Ltd. | Gpr119 agonist |
| WO2011111880A1 (ko) | 2010-03-08 | 2011-09-15 | 주식회사 메디젠텍 | 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 gsk3 이동에 의해 발생되는 질환의 치료 또는 예방용 약학적 조성물 |
| HUE052110T2 (hu) | 2010-07-29 | 2021-04-28 | Rigel Pharmaceuticals Inc | AMPK-t aktiváló heterociklusos vegyületek és alkalmazásuk |
| JP5620417B2 (ja) * | 2011-02-07 | 2014-11-05 | 中外製薬株式会社 | アミノピラゾール誘導体を含む医薬 |
| SG193331A1 (en) | 2011-03-18 | 2013-10-30 | Lupin Ltd | Benzo [b] [1, 4] oxazin derivatives as calcium sensing receptor modulators |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014079709A1 (en) | 2012-11-23 | 2014-05-30 | Ab Science | Use of small molecule inhibitors/activators in combination with (deoxy)nucleoside or (deoxy)nucleotide analogs for treatment of cancer and hematological malignancies or viral infections |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| AU2014287209B2 (en) | 2013-07-09 | 2019-01-24 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| TW201605452A (zh) | 2013-08-28 | 2016-02-16 | 安斯泰來製藥股份有限公司 | 以嘧啶化合物作爲有效成分之醫藥組成物 |
| SG11201602069WA (en) | 2013-10-18 | 2016-04-28 | Eisai R&D Man Co Ltd | Pyrimidine fgfr4 inhibitors |
| PT3395814T (pt) | 2013-10-25 | 2022-07-27 | Blueprint Medicines Corp | Inibidores do recetor do fator de crescimento de fibroblastos |
| CN105683188B (zh) * | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| MA38393B1 (fr) | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
-
2016
- 2016-03-18 US US15/073,766 patent/US9802917B2/en active Active
- 2016-03-23 MX MX2017012293A patent/MX2017012293A/es active IP Right Grant
- 2016-03-23 AR ARP160100792A patent/AR104060A1/es unknown
- 2016-03-23 WO PCT/IB2016/051633 patent/WO2016151500A1/en not_active Ceased
- 2016-03-23 CN CN201680018234.6A patent/CN107406448B/zh active Active
- 2016-03-23 RU RU2017133243A patent/RU2720456C2/ru active
- 2016-03-23 KR KR1020177026470A patent/KR102606643B1/ko active Active
- 2016-03-23 JP JP2017549754A patent/JP6696995B2/ja active Active
- 2016-03-23 EP EP16712082.3A patent/EP3274349B1/en active Active
- 2016-03-23 AU AU2016238437A patent/AU2016238437B2/en active Active
- 2016-03-23 ES ES16712082T patent/ES2803028T3/es active Active
- 2016-03-23 PL PL16712082T patent/PL3274349T3/pl unknown
- 2016-03-23 CA CA2977326A patent/CA2977326C/en active Active
- 2016-03-24 TW TW105109283A patent/TWI699206B/zh active
-
2019
- 2019-02-07 AU AU2019200936A patent/AU2019200936A1/en not_active Abandoned
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