JP2017530154A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017530154A5 JP2017530154A5 JP2017517705A JP2017517705A JP2017530154A5 JP 2017530154 A5 JP2017530154 A5 JP 2017530154A5 JP 2017517705 A JP2017517705 A JP 2017517705A JP 2017517705 A JP2017517705 A JP 2017517705A JP 2017530154 A5 JP2017530154 A5 JP 2017530154A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- ring
- hydroxy
- substituted
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 226
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 104
- 125000005842 heteroatom Chemical group 0.000 claims description 88
- 229910052760 oxygen Inorganic materials 0.000 claims description 88
- 229910052717 sulfur Inorganic materials 0.000 claims description 88
- 229910052739 hydrogen Inorganic materials 0.000 claims description 77
- 229910052799 carbon Inorganic materials 0.000 claims description 72
- 125000000623 heterocyclic group Chemical group 0.000 claims description 61
- 125000004432 carbon atom Chemical group C* 0.000 claims description 55
- 239000001257 hydrogen Substances 0.000 claims description 55
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 55
- 125000005843 halogen group Chemical group 0.000 claims description 49
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims description 46
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims description 46
- -1 haloC 1 -C 3 alkyl Chemical group 0.000 claims description 44
- 150000002431 hydrogen Chemical group 0.000 claims description 38
- 229910052736 halogen Inorganic materials 0.000 claims description 33
- 150000002367 halogens Chemical group 0.000 claims description 33
- 125000004043 oxo group Chemical group O=* 0.000 claims description 33
- 229920006395 saturated elastomer Polymers 0.000 claims description 33
- 150000001875 compounds Chemical class 0.000 claims description 32
- 102100020683 Beta-klotho Human genes 0.000 claims description 31
- 102100031734 Fibroblast growth factor 19 Human genes 0.000 claims description 31
- 101001139095 Homo sapiens Beta-klotho Proteins 0.000 claims description 31
- 101000846394 Homo sapiens Fibroblast growth factor 19 Proteins 0.000 claims description 31
- 150000003839 salts Chemical class 0.000 claims description 30
- 125000003118 aryl group Chemical group 0.000 claims description 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 22
- 229910052757 nitrogen Inorganic materials 0.000 claims description 22
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 17
- 239000007787 solid Substances 0.000 claims description 15
- 150000001204 N-oxides Chemical class 0.000 claims description 11
- 125000002619 bicyclic group Chemical group 0.000 claims description 11
- 125000004122 cyclic group Chemical group 0.000 claims description 11
- 125000001475 halogen functional group Chemical group 0.000 claims description 11
- 125000003566 oxetanyl group Chemical group 0.000 claims description 11
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 claims description 11
- 125000006413 ring segment Chemical group 0.000 claims description 11
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 239000012472 biological sample Substances 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 9
- 230000036210 malignancy Effects 0.000 claims description 9
- WWXYIWRCALKTTD-UHFFFAOYSA-N 6-[[acetyl(methyl)amino]methyl]-N-(5-cyanopyridin-2-yl)-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound CN(Cc1cc2CCCN(C(=O)Nc3ccc(cn3)C#N)c2nc1C=O)C(C)=O WWXYIWRCALKTTD-UHFFFAOYSA-N 0.000 claims description 2
- 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
- DNJLKERWZGKXBF-UHFFFAOYSA-N N-(5-cyanopyridin-2-yl)-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound O=Cc1ccc2CCCN(C(=O)Nc3ccc(cn3)C#N)c2n1 DNJLKERWZGKXBF-UHFFFAOYSA-N 0.000 claims description 2
- HXNZAVZZAPTZBP-UHFFFAOYSA-N N-(5-cyanopyridin-2-yl)-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound OCc1cc2CCCN(C(=O)Nc3ccc(cn3)C#N)c2nc1C=O HXNZAVZZAPTZBP-UHFFFAOYSA-N 0.000 claims description 2
- GBJIYJAVKBUOHN-UHFFFAOYSA-N N-[5-cyano-4-(2-methoxyethoxy)pyridin-2-yl]-6-(difluoromethyl)-7-formyl-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound COCCOc1cc(NC(=O)N2CCCc3cc(C(F)F)c(C=O)nc23)ncc1C#N GBJIYJAVKBUOHN-UHFFFAOYSA-N 0.000 claims description 2
- RVTLBVODLXUYNU-UHFFFAOYSA-N N-[5-cyano-4-(2-methoxyethoxy)pyridin-2-yl]-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound COCCOc1cc(NC(=O)N2CCCc3cc(CO)c(C=O)nc23)ncc1C#N RVTLBVODLXUYNU-UHFFFAOYSA-N 0.000 claims description 2
- LGFNXKJQQVMYQI-UHFFFAOYSA-N N-[5-cyano-4-(2-methoxyethoxy)pyridin-2-yl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound COCCOc1cc(NC(=O)N2CCCc3cc(CN4CCN(C)CC4=O)c(C=O)nc23)ncc1C#N LGFNXKJQQVMYQI-UHFFFAOYSA-N 0.000 claims description 2
- SYRAVIOIIKVUFT-UHFFFAOYSA-N N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound COCCNc1cc(NC(=O)N2CCCc3cc(CO)c(C=O)nc23)ncc1C#N SYRAVIOIIKVUFT-UHFFFAOYSA-N 0.000 claims description 2
- BHKDKKZMPODMIQ-UHFFFAOYSA-N N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-formyl-6-[(4-methyl-2-oxopiperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound COCCNc1cc(NC(=O)N2CCCc3cc(CN4CCN(C)CC4=O)c(C=O)nc23)ncc1C#N BHKDKKZMPODMIQ-UHFFFAOYSA-N 0.000 claims description 2
- JDSIDNMVOWOKBD-MRXNPFEDSA-N N-[5-cyano-4-[(3R)-oxolan-3-yl]oxypyridin-2-yl]-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound C(#N)C=1C(=CC(=NC1)NC(=O)N1CCCC2=CC(=C(N=C12)C=O)CO)O[C@H]1COCC1 JDSIDNMVOWOKBD-MRXNPFEDSA-N 0.000 claims description 2
- JDSIDNMVOWOKBD-INIZCTEOSA-N N-[5-cyano-4-[(3S)-oxolan-3-yl]oxypyridin-2-yl]-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound C(#N)C=1C(=CC(=NC1)NC(=O)N1CCCC2=CC(=C(N=C12)C=O)CO)O[C@@H]1COCC1 JDSIDNMVOWOKBD-INIZCTEOSA-N 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
- 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
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 20
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- 206010073069 Hepatic cancer Diseases 0.000 claims 1
- 229940001468 citrate Drugs 0.000 claims 1
- 150000001860 citric acid derivatives Chemical class 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 229940049920 malate Drugs 0.000 claims 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 1
- 229940095064 tartrate Drugs 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 description 66
- 125000006615 aromatic heterocyclic group Chemical group 0.000 description 6
- BVCRERJDOOBZOH-UHFFFAOYSA-N bicyclo[2.2.1]heptanyl Chemical group C1C[C+]2CC[C-]1C2 BVCRERJDOOBZOH-UHFFFAOYSA-N 0.000 description 6
- 125000000753 cycloalkyl group Chemical group 0.000 description 6
- KVIZTDNKHOCNAM-UHFFFAOYSA-N 4-methylpiperazin-2-one Chemical compound CN1CCNC(=O)C1 KVIZTDNKHOCNAM-UHFFFAOYSA-N 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000001516 cell proliferation assay Methods 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000013642 negative control Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2014088094 | 2014-10-03 | ||
| CNPCT/CN2014/088094 | 2014-10-03 | ||
| PCT/US2015/053677 WO2016054483A1 (en) | 2014-10-03 | 2015-10-02 | Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019161051A Division JP6794514B2 (ja) | 2014-10-03 | 2019-09-04 | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017530154A JP2017530154A (ja) | 2017-10-12 |
| JP2017530154A5 true JP2017530154A5 (enExample) | 2018-11-15 |
| JP6585167B2 JP6585167B2 (ja) | 2019-10-02 |
Family
ID=54330059
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017517705A Active JP6585167B2 (ja) | 2014-10-03 | 2015-10-02 | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
| JP2019161051A Active JP6794514B2 (ja) | 2014-10-03 | 2019-09-04 | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019161051A Active JP6794514B2 (ja) | 2014-10-03 | 2019-09-04 | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US20180185341A1 (enExample) |
| EP (1) | EP3200786B1 (enExample) |
| JP (2) | JP6585167B2 (enExample) |
| ES (1) | ES2756748T3 (enExample) |
| PL (1) | PL3200786T3 (enExample) |
| WO (1) | WO2016054483A1 (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 |
| JP7103952B2 (ja) * | 2016-05-20 | 2022-07-20 | 江▲蘇▼豪森▲薬▼▲業▼集▲団▼有限公司 | Ｆｇｆｒ４阻害剤、その製造方法及び応用 |
| WO2018055503A1 (en) | 2016-09-20 | 2018-03-29 | Novartis Ag | Combination comprising a pd-1 antagonist and an fgfr4 inhibitor |
| PL3534902T3 (pl) * | 2016-11-02 | 2023-03-27 | Novartis Ag | Skojarzenia inhibitorów fgfr4 i sekwestrantów kwasów żółciowych |
| TWI723480B (zh) * | 2018-07-27 | 2021-04-01 | 大陸商北京加科思新藥研發有限公司 | 用作fgfr4抑制劑的稠環衍生物 |
| MX2021009863A (es) | 2019-03-21 | 2021-11-12 | Onxeo | Una molecula dbait en combinacion con inhibidor de quinasa para el tratamiento del cancer. |
| WO2021089791A1 (en) | 2019-11-08 | 2021-05-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
Family Cites Families (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5143854A (en) | 1989-06-07 | 1992-09-01 | Affymax Technologies N.V. | Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof |
| US5424186A (en) | 1989-06-07 | 1995-06-13 | Affymax Technologies N.V. | Very large scale immobilized polymer synthesis |
| GB9420999D0 (en) | 1994-10-18 | 1994-12-07 | Smithkline Beecham Plc | Novel compounds |
| US6140338A (en) | 1996-07-29 | 2000-10-31 | Banyu Pharmaceutical, Co., Ltd. | Chemokine receptor antagonists |
| US6048861A (en) | 1997-12-17 | 2000-04-11 | Merck & Co., Inc. | Integrin receptor antagonists |
| AU2832399A (en) | 1998-02-10 | 1999-08-30 | Novartis Ag | B cell inhibitors |
| US7115750B1 (en) | 1999-09-20 | 2006-10-03 | Takeda Pharmaceutical Company Limited | Melanin concentrating hormone antagonist |
| US6407241B1 (en) | 1999-11-08 | 2002-06-18 | Merck & Co., Inc. | Process and intermediates for the preparation of imidazolidinone αv integrin antagonists |
| YU32502A (sh) * | 1999-11-08 | 2004-12-31 | Merck & Co.Inc. | Postupak i intermedijeri za proizvodnju imidazolidinonskih antagonista alfa v integrina |
| AU2003211951A1 (en) | 2002-02-14 | 2003-09-04 | Ono Pharmaceutical Co., Ltd. | N-carbamoyl nitrogen-containing fused ring compounds and drugs containing these compounds as the active ingredient |
| US20060004010A1 (en) | 2002-07-10 | 2006-01-05 | Hiromu Habashita | Ccr4 antagonist and medical use thereof |
| CA2488739A1 (en) * | 2002-08-30 | 2004-03-11 | Eisai Co., Ltd. | Nitrogen-containing aromatic derivatives |
| US7098332B2 (en) | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| AU2003303231A1 (en) | 2002-12-20 | 2004-07-14 | Warner-Lambert Company Llc | Benzoxazines and derivatives thereof as inhibitors of pi3ks |
| EP1631260A2 (en) | 2003-02-28 | 2006-03-08 | Transform Pharmaceuticals, Inc. | Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen |
| BRPI0408332A (pt) | 2003-03-14 | 2006-03-21 | Ono Pharmaceutical Co | derivados heterocìclicos contendo nitrogênio e medicamentos contendo os mesmos como ingrediente ativo |
| JP2006522814A (ja) | 2003-04-11 | 2006-10-05 | タイゲン・バイオテクノロジー | アミノキノリン化合物 |
| JP4895811B2 (ja) | 2003-09-11 | 2012-03-14 | ケミア，インコーポレイテッド | サイトカイン阻害剤 |
| WO2007009883A1 (en) | 2005-07-15 | 2007-01-25 | F. Hoffmann-La Roche Ag | Novel heteroaryl fused cyclic amines |
| JP2009531274A (ja) * | 2005-12-07 | 2009-09-03 | オーエスアイ・ファーマスーティカルズ・インコーポレーテッド | キナーゼ阻害性ピロロピリジン化合物 |
| CA2634047C (en) | 2005-12-21 | 2016-04-12 | Novartis Ag | Pyrimidinyl aryl urea derivatives being fgf inhibitors |
| CN101405002A (zh) | 2005-12-29 | 2009-04-08 | 詹森药业有限公司 | 激肽原2受体拮抗剂 |
| CA2637988A1 (en) | 2006-02-10 | 2007-11-29 | Genentech, Inc. | Anti-fgf19 antibodies and methods using same |
| 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 |
| JP2009539815A (ja) * | 2006-06-09 | 2009-11-19 | アストラゼネカ アクチボラグ | 固形腫瘍の治療用のａ５ｂ１アンタゴニストとしてのＮ−（ベンゾイル）−Ｏ−［２−（ピリジン−２−イルアミノ）エチル］−Ｌ−チロシン誘導体と関連化合物 |
| WO2007146230A2 (en) | 2006-06-14 | 2007-12-21 | Merck & Co., Inc. | Non-nucleoside reverse transcriptase inhibitors |
| EP1918376A1 (en) | 2006-11-03 | 2008-05-07 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | FGFR4 promotes cancer cell resistance in response to chemotherapeutic drugs |
| TW200843766A (en) | 2007-03-09 | 2008-11-16 | Novartis Ag | Treatment of melanoma |
| TWI524898B (zh) | 2007-04-02 | 2016-03-11 | 建南德克公司 | 克羅梭（ｋｌｏｔｈｏ）ｂｅｔａ調節劑之用途 |
| WO2009079008A1 (en) | 2007-12-19 | 2009-06-25 | Yangbo Feng | Benzopyrans and analogs as rho kinase inhibitors |
| FR2933702A1 (fr) | 2008-07-08 | 2010-01-15 | Sanofi Aventis | Antagonistes specifiques du recepteur fgf-r4 |
| WO2010026291A1 (en) | 2008-09-03 | 2010-03-11 | Licentia Ltd. | Materials and methods for inhibiting cancer cell invasion related to fgfr4 |
| JPWO2010027002A1 (ja) | 2008-09-05 | 2012-02-02 | 塩野義製薬株式会社 | Ｐｉ３ｋ阻害活性を有する縮環モルホリン誘導体 |
| JP5683484B2 (ja) | 2008-12-19 | 2015-03-11 | ジェネンテック， インコーポレイテッド | 化合物と使用法 |
| GB0906472D0 (en) * | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (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 |
| CA2779303A1 (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 |
| CN102971304A (zh) | 2010-02-01 | 2013-03-13 | 日本化学医药株式会社 | Gpr119激动剂 |
| 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 |
| SG186850A1 (en) | 2010-07-29 | 2013-02-28 | Rigel Pharmaceuticals Inc | Ampk-activating heterocyclic compounds and methods for using the same |
| WO2012061337A1 (en) * | 2010-11-02 | 2012-05-10 | Exelixis, Inc. | Fgfr2 modulators |
| 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 |
| JP6033835B2 (ja) | 2011-03-18 | 2016-11-30 | ルピン アトランティス ホールディングス エスエー | カルシウム感知受容体モジュレーターとしてのベンゾ［ｂ］［１，４］オキサジン誘導体 |
| MX342240B (es) | 2011-04-07 | 2016-09-21 | Genentech Inc | Anticuerpos anti-fgfr4 y metodos de uso. |
| GB201118656D0 (en) * | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| PL2872491T3 (pl) | 2012-07-11 | 2021-12-13 | Blueprint Medicines Corporation | Inhibitory receptora czynnika wzrostu fibroblastów |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2906541B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2922572A1 (en) | 2012-11-23 | 2015-09-30 | 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 |
| EP2968337B1 (en) | 2013-03-15 | 2021-07-21 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| AR095464A1 (es) | 2013-03-15 | 2015-10-21 | Celgene Avilomics Res Inc | Compuestos de heteroarilo y usos de los mismos |
| DK2986610T5 (en) | 2013-04-19 | 2018-12-10 | Incyte Holdings Corp | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| WO2015006492A1 (en) | 2013-07-09 | 2015-01-15 | 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 |
| WO2015057938A1 (en) | 2013-10-18 | 2015-04-23 | Eisai R&D Management Co., Ltd. | Pyrimidine fgfr4 inhibitors |
| EP3060560A1 (en) | 2013-10-25 | 2016-08-31 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| KR101862493B1 (ko) | 2013-10-25 | 2018-05-29 | 노파르티스 아게 | Fgfr4 억제제로서의 고리-융합된 비시클릭 피리딜 유도체 |
| EP3155005A4 (en) | 2014-06-16 | 2018-07-11 | NGM Biopharmaceuticals, Inc. | Methods and uses for modulating bile acid homeostasis and treatment of bile acid disorders and diseases |
| ES2756748T3 (es) * | 2014-10-03 | 2020-04-27 | Novartis Ag | Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4 |
| US9802917B2 (en) * | 2015-03-25 | 2017-10-31 | Novartis Ag | 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 |
| EP3273959A1 (en) * | 2015-03-25 | 2018-01-31 | Novartis Ag | Pharmaceutical combinations |
| PL3534902T3 (pl) | 2016-11-02 | 2023-03-27 | Novartis Ag | Skojarzenia inhibitorów fgfr4 i sekwestrantów kwasów żółciowych |
-
2015
- 2015-10-02 ES ES15781518T patent/ES2756748T3/es active Active
- 2015-10-02 PL PL15781518T patent/PL3200786T3/pl unknown
- 2015-10-02 EP EP15781518.4A patent/EP3200786B1/en active Active
- 2015-10-02 US US15/516,443 patent/US20180185341A1/en not_active Abandoned
- 2015-10-02 JP JP2017517705A patent/JP6585167B2/ja active Active
- 2015-10-02 WO PCT/US2015/053677 patent/WO2016054483A1/en not_active Ceased
-
2018
- 2018-11-13 US US16/190,087 patent/US10463653B2/en active Active
-
2019
- 2019-02-28 US US16/289,612 patent/US10507201B2/en active Active
- 2019-09-04 JP JP2019161051A patent/JP6794514B2/ja active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017530154A5 (enExample) | ||
| JP6664385B2 (ja) | Ｂｕｂ１阻害薬としてのベンジル置換インダゾール類 | |
| RU2686323C2 (ru) | Новые соединения и композиции для ингибирования fasn | |
| JP7215687B2 (ja) | キナーゼ阻害活性を有する化合物、その製造方法及び用途 | |
| JP6952695B2 (ja) | インフルエンザウイルス複製の阻害剤、その適用方法および使用 | |
| JP6387488B2 (ja) | 非選択的キナーゼ阻害剤 | |
| JP2021063119A (ja) | 噴霧乾燥製剤 | |
| JP6021805B2 (ja) | 腫瘍治療剤 | |
| JP2010528026A5 (enExample) | ||
| TW202521536A (zh) | Ｃｄｋ抑制劑 | |
| CN107922431A (zh) | Hpk1抑制剂及其使用方法 | |
| RU2013109143A (ru) | Бензимидазол- и азабензимидазолсодержащие соединения, которые ингибируют киназу анапластической лимфомы | |
| JP2014513110A5 (enExample) | ||
| AU2014337154A1 (en) | Co-crystals of (s)-N-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as DNA-PK inhibitors | |
| WO2015058067A1 (en) | Co-crystals of (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors | |
| KR20110036620A (ko) | Ｓｍｏ 억제제로서의 피리다진 유도체 | |
| JP2016525076A5 (enExample) | ||
| CN105308036A (zh) | 用于激酶调节的化合物和方法及其适应症 | |
| JP2016526540A5 (enExample) | ||
| TW201028393A (en) | Kinase inhibitors and methods of their use | |
| JP2017527586A (ja) | 癌の治療に有用な縮合二環式（ヘテロ）芳香族化合物 | |
| JP2013173787A (ja) | 薬剤耐性癌の処置方法 | |
| TW201731841A (zh) | 6‐芳基或6‐異芳基‐4‐嗎啉‐4‐芳基‐吡啶‐2‐酮化合物 | |
| WO2015026935A2 (en) | Hdac8 inhibitors for treating cancer | |
| JP2017536342A5 (enExample) |