JP2018509446A5 - - Google Patents
Download PDFInfo
- 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 |
|---|---|---|---|
| CN2015000202 | 2015-03-25 | ||
| CNPCT/CN2015/000202 | 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 (https=) | 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 (https=) |
| EP (1) | EP3274349B1 (https=) |
| JP (1) | JP6696995B2 (https=) |
| KR (1) | KR102606643B1 (https=) |
| CN (1) | CN107406448B (https=) |
| AR (1) | AR104060A1 (https=) |
| AU (2) | AU2016238437B2 (https=) |
| CA (1) | CA2977326C (https=) |
| ES (1) | ES2803028T3 (https=) |
| MX (1) | MX2017012293A (https=) |
| PL (1) | PL3274349T3 (https=) |
| RU (1) | RU2720456C2 (https=) |
| TW (1) | TWI699206B (https=) |
| WO (1) | WO2016151500A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6585167B2 (ja) * | 2014-10-03 | 2019-10-02 | ノバルティス アーゲー | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
| CN113234072B (zh) * | 2016-05-20 | 2022-11-04 | 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 |
| CA3075720A1 (en) * | 2017-10-02 | 2019-04-11 | 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 |
| WO2019085860A1 (zh) * | 2017-10-31 | 2019-05-09 | 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 |
| AU2020298246A1 (en) * | 2019-06-21 | 2022-01-27 | 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 |
| CA2261633A1 (en) | 1996-07-29 | 1998-02-05 | Banyu Pharmaceutical Co., Ltd. | Chemokine receptor antagonists |
| ES2241192T3 (es) | 1997-12-17 | 2005-10-16 | MERCK & CO., INC. (A NEW JERSEY CORP.) | Antagonistas del receptor de integrina. |
| AR015514A1 (es) | 1998-02-10 | 2001-05-02 | Novartis Ag | Compuesto de amida, proceso para su preparacion y composicion farmaceutica que lo contiene |
| EP1218336A2 (en) | 1999-09-20 | 2002-07-03 | Takeda Chemical Industries, Ltd. | Melanin concentrating hormone antagonist |
| JPWO2003068753A1 (ja) | 2002-02-14 | 2005-06-02 | 小野薬品工業株式会社 | Ｎ−カルバモイル窒素含有縮合環化合物およびその化合物を有効成分として含有する薬剤 |
| US20060004010A1 (en) | 2002-07-10 | 2006-01-05 | Hiromu Habashita | Ccr4 antagonist and medical use thereof |
| AU2003303231A1 (en) | 2002-12-20 | 2004-07-14 | Warner-Lambert Company Llc | Benzoxazines and derivatives thereof as inhibitors of pi3ks |
| US7098332B2 (en) * | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| WO2004080966A1 (ja) | 2003-03-14 | 2004-09-23 | Ono Pharmaceutical Co., Ltd. | 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 |
| EP1613322A4 (en) | 2003-04-11 | 2008-08-13 | Taigen Biotechnology Co Ltd | AMINOQUINOLINE COMPOUNDS |
| US7749999B2 (en) | 2003-09-11 | 2010-07-06 | Itherx Pharmaceuticals, Inc. | Alpha-ketoamides and derivatives thereof |
| CN101223167B (zh) | 2005-07-15 | 2011-08-31 | 弗·哈夫曼-拉罗切有限公司 | 杂芳基稠合的环状胺 |
| BRPI0620408B8 (pt) | 2005-12-21 | 2021-05-25 | Novartis Ag | derivados de pirimidinil aril uréia sendo inibidores de fgf, seus usos, e preparação farmacêutica |
| EP1976528A2 (en) | 2005-12-29 | 2008-10-08 | Janssen Pharmaceutica, N.V. | Prokineticin 2 receptor antagonists |
| KR20090008217A (ko) | 2006-03-10 | 2009-01-21 | 오노 야꾸힝 고교 가부시키가이샤 | 질소 함유 복소환 유도체 및 이들을 유효 성분으로 하는 약제 |
| WO2007146230A2 (en) | 2006-06-14 | 2007-12-21 | Merck & Co., Inc. | Non-nucleoside reverse transcriptase inhibitors |
| CA2679268A1 (en) | 2007-03-09 | 2008-09-18 | Novartis Ag | Treatment of melanoma |
| WO2009079008A1 (en) | 2007-12-19 | 2009-06-25 | Yangbo Feng | Benzopyrans and analogs as rho kinase inhibitors |
| US20110172217A1 (en) | 2008-09-05 | 2011-07-14 | Shionogi & Co., Ltd. | Ring-fused morpholine derivative having pi3k-inhibiting activity |
| RU2561109C2 (ru) | 2008-12-19 | 2015-08-20 | Дженентек, Инк. | Соединения и способы применения |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| CA2761009A1 (en) | 2009-05-04 | 2010-11-11 | Plexxikon, Inc. | Compounds and methods for inhibition of renin, and indications therefor |
| US9556201B2 (en) | 2009-10-29 | 2017-01-31 | Glaxosmithkline Llc | Bicyclic pyridines and analogs as sirtuin modulators |
| CN102596916B (zh) | 2009-10-30 | 2015-06-17 | 诺瓦提斯公司 | 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 |
| KR20120130104A (ko) | 2010-02-01 | 2012-11-28 | 닛뽕 케미파 가부시키가이샤 | Ｇｐｒ119 작동약 |
| 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 |
| BR112013002112B1 (pt) | 2010-07-29 | 2021-04-06 | Rigel Pharmaceuticals, Inc. | Composto, composição farmacêutica, e, uso de um composto, ou de um respectivo sal farmaceuticamente aceitável, ou de uma composição |
| 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 |
| AP2013007153A0 (en) | 2011-03-18 | 2013-09-30 | 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 |
| SMT202100451T1 (it) | 2012-07-11 | 2021-09-14 | Blueprint Medicines Corp | Inibitori del recettore di crescita dei fibroblasti |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US20150290235A1 (en) | 2012-11-23 | 2015-10-15 | 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 |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| EP3019491A4 (en) | 2013-07-09 | 2016-12-21 | Dana Farber Cancer Inst Inc | KINASEHEMMER FOR THE TREATMENT OF DISEASES |
| AR097455A1 (es) | 2013-08-28 | 2016-03-16 | Astellas Pharma Inc | Composición farmacéutica que contiene compuesto de pirimidina como un ingrediente activo |
| MX378288B (es) | 2013-10-18 | 2025-03-10 | Eisai R&D Man Co Ltd | Inhibidores de pirimidina del fgfr4. |
| CA2928042C (en) | 2013-10-25 | 2022-05-10 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| 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 WO PCT/IB2016/051633 patent/WO2016151500A1/en not_active Ceased
- 2016-03-23 KR KR1020177026470A patent/KR102606643B1/ko active Active
- 2016-03-23 PL PL16712082T patent/PL3274349T3/pl unknown
- 2016-03-23 EP EP16712082.3A patent/EP3274349B1/en active Active
- 2016-03-23 AU AU2016238437A patent/AU2016238437B2/en active Active
- 2016-03-23 RU RU2017133243A patent/RU2720456C2/ru active
- 2016-03-23 ES ES16712082T patent/ES2803028T3/es active Active
- 2016-03-23 JP JP2017549754A patent/JP6696995B2/ja active Active
- 2016-03-23 CA CA2977326A patent/CA2977326C/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 CN CN201680018234.6A patent/CN107406448B/zh active Active
- 2016-03-24 TW TW105109283A patent/TWI699206B/zh active
-
2019
- 2019-02-07 AU AU2019200936A patent/AU2019200936A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018509446A5 (https=) | ||
| JP2014507455A5 (https=) | ||
| JP2016501250A5 (https=) | ||
| RU2017133243A (ru) | Частицы n-(5-циано-4-((2-метоксиэтил)амино)пиридин-2-ил)-7-формил-6-((4-метил-2-оксопиперазин-1-ил)метил)-3,4-дигидро-1,8-нафтиридин-1(2h)-карбоксамида | |
| JP2014506907A5 (https=) | ||
| JP2010539110A5 (https=) | ||
| JP2012532112A5 (https=) | ||
| JP2020528889A5 (https=) | ||
| JP2019517487A5 (https=) | ||
| JP2014503525A5 (https=) | ||
| JP2019532078A5 (https=) | ||
| JP2013510120A5 (https=) | ||
| JP2020537657A5 (https=) | ||
| JP2017533968A5 (https=) | ||
| JP2014037426A5 (https=) | ||
| JP2013545785A5 (https=) | ||
| JP2013508373A5 (https=) | ||
| JP2012521994A5 (https=) | ||
| JP2008506720A5 (https=) | ||
| RU2012103487A (ru) | Ингибирующие jak соединения на основе пиразолопиримидина и способы | |
| JP2013533879A5 (https=) | ||
| JP2019514956A5 (https=) | ||
| JP2009507909A5 (https=) | ||
| SG11201909094VA (en) | 4-pyridone compound or salt thereof, and pharmaceutical composition and formulation including same | |
| JP2013509392A5 (https=) |