JP2013536208A5 - - Google Patents
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- JP2013536208A5 JP2013536208A5 JP2013525161A JP2013525161A JP2013536208A5 JP 2013536208 A5 JP2013536208 A5 JP 2013536208A5 JP 2013525161 A JP2013525161 A JP 2013525161A JP 2013525161 A JP2013525161 A JP 2013525161A JP 2013536208 A5 JP2013536208 A5 JP 2013536208A5
- Authority
- JP
- Japan
- Prior art keywords
- syk
- groups
- chemical reaction
- acyl
- osteoclasts
- 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
- 238000006243 chemical reaction Methods 0.000 description 8
- 125000002252 acyl group Chemical group 0.000 description 5
- -1 araliphatic Chemical group 0.000 description 5
- 210000002997 osteoclast Anatomy 0.000 description 4
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 3
- 210000003630 histaminocyte Anatomy 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
- 125000006239 protecting group Chemical group 0.000 description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 3
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 description 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 2
- 125000003710 aryl alkyl group Chemical group 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- YRTCKZIKGWZNCU-UHFFFAOYSA-N furo[3,2-b]pyridine Chemical class C1=CC=C2OC=CC2=N1 YRTCKZIKGWZNCU-UHFFFAOYSA-N 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 231100000189 neurotoxic Toxicity 0.000 description 2
- 230000002887 neurotoxic effect Effects 0.000 description 2
- 210000001331 nose Anatomy 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 102000013455 Amyloid beta-Peptides Human genes 0.000 description 1
- 108010090849 Amyloid beta-Peptides Proteins 0.000 description 1
- 208000006386 Bone Resorption Diseases 0.000 description 1
- 101100481408 Danio rerio tie2 gene Proteins 0.000 description 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 description 1
- 101000996834 Homo sapiens Linker for activation of T-cells family member 2 Proteins 0.000 description 1
- 101000818543 Homo sapiens Tyrosine-protein kinase ZAP-70 Proteins 0.000 description 1
- 102000009438 IgE Receptors Human genes 0.000 description 1
- 108010073816 IgE Receptors Proteins 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- 102100034238 Linker for activation of T-cells family member 2 Human genes 0.000 description 1
- 101100268648 Mus musculus Abl1 gene Proteins 0.000 description 1
- 101100481410 Mus musculus Tek gene Proteins 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 description 1
- 102000038030 PI3Ks Human genes 0.000 description 1
- 108091007960 PI3Ks Proteins 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 102000029797 Prion Human genes 0.000 description 1
- 108091000054 Prion Proteins 0.000 description 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 1
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 1
- 101150094745 Ptk2b gene Proteins 0.000 description 1
- 108050003452 SH2 domains Proteins 0.000 description 1
- 102000014400 SH2 domains Human genes 0.000 description 1
- 108060006706 SRC Proteins 0.000 description 1
- 102000001332 SRC Human genes 0.000 description 1
- 102100021125 Tyrosine-protein kinase ZAP-70 Human genes 0.000 description 1
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 125000001931 aliphatic group Chemical group 0.000 description 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 125000003435 aroyl group Chemical group 0.000 description 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 1
- 235000003704 aspartic acid Nutrition 0.000 description 1
- 230000035578 autophosphorylation Effects 0.000 description 1
- 210000003651 basophil Anatomy 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 description 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- LHHCSNFAOIFYRV-DOVBMPENSA-N boceprevir Chemical compound O=C([C@@H]1[C@@H]2[C@@H](C2(C)C)CN1C(=O)[C@@H](NC(=O)NC(C)(C)C)C(C)(C)C)NC(C(=O)C(N)=O)CC1CCC1 LHHCSNFAOIFYRV-DOVBMPENSA-N 0.000 description 1
- 230000024279 bone resorption Effects 0.000 description 1
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 210000004899 c-terminal region Anatomy 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 description 1
- 125000001589 carboacyl group Chemical group 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 150000001735 carboxylic acids Chemical class 0.000 description 1
- 239000012876 carrier material Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000005754 cellular signaling Effects 0.000 description 1
- 230000002596 correlated effect Effects 0.000 description 1
- 230000016396 cytokine production Effects 0.000 description 1
- 230000003436 cytoskeletal effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 210000002257 embryonic structure Anatomy 0.000 description 1
- 210000002919 epithelial cell Anatomy 0.000 description 1
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 108020001507 fusion proteins Proteins 0.000 description 1
- 102000037865 fusion proteins Human genes 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 230000009033 hematopoietic malignancy Effects 0.000 description 1
- 210000003958 hematopoietic stem cell Anatomy 0.000 description 1
- 210000000777 hematopoietic system Anatomy 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 125000000623 heterocyclic group Chemical group 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 102000006495 integrins Human genes 0.000 description 1
- 108010044426 integrins Proteins 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000003032 molecular docking Methods 0.000 description 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 description 1
- 210000003928 nasal cavity Anatomy 0.000 description 1
- 239000007923 nasal drop Substances 0.000 description 1
- 229940100662 nasal drops Drugs 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 102000037979 non-receptor tyrosine kinases Human genes 0.000 description 1
- 108091008046 non-receptor tyrosine kinases Proteins 0.000 description 1
- 125000003232 p-nitrobenzoyl group Chemical group [N+](=O)([O-])C1=CC=C(C(=O)*)C=C1 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 238000007634 remodeling Methods 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
- 150000003460 sulfonic acids Chemical class 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000003944 tolyl group Chemical group 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10008928 | 2010-08-27 | ||
| EP10008928.3 | 2010-08-27 | ||
| PCT/EP2011/003831 WO2012025187A2 (en) | 2010-08-27 | 2011-07-29 | Furopyridine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013536208A JP2013536208A (ja) | 2013-09-19 |
| JP2013536208A5 true JP2013536208A5 (https=) | 2015-08-06 |
| JP5789300B2 JP5789300B2 (ja) | 2015-10-07 |
Family
ID=44501791
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013525161A Expired - Fee Related JP5789300B2 (ja) | 2010-08-27 | 2011-07-29 | フロピリジン誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9006440B2 (https=) |
| EP (1) | EP2609100B1 (https=) |
| JP (1) | JP5789300B2 (https=) |
| KR (1) | KR20130108318A (https=) |
| CN (1) | CN103052640B (https=) |
| AR (1) | AR082727A1 (https=) |
| AU (1) | AU2011295441B2 (https=) |
| BR (1) | BR112013004624A2 (https=) |
| CA (1) | CA2809333C (https=) |
| EA (1) | EA201300283A1 (https=) |
| ES (1) | ES2545352T3 (https=) |
| IL (1) | IL224870A (https=) |
| MX (1) | MX2013002199A (https=) |
| SG (1) | SG187956A1 (https=) |
| WO (1) | WO2012025187A2 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012118632A1 (en) | 2011-02-28 | 2012-09-07 | Ning Xi | Substituted quinoline compounds and methods of use |
| HRP20161578T1 (hr) * | 2012-02-09 | 2016-12-30 | Merck Patent Gmbh | Derivati furo[3, 2-b]piridina kao inhibitori tbk1 i ikk |
| AU2013224420B2 (en) * | 2012-02-21 | 2016-12-15 | Merck Patent Gmbh | Furopyridine derivatives |
| WO2014022117A1 (en) | 2012-07-28 | 2014-02-06 | Calitor Sciences, Llc | Substituted pyrazolone compounds and methods of use |
| US8975282B2 (en) | 2012-07-28 | 2015-03-10 | Sunshine Lake Pharma Co., Ltd. | Substituted pyrazolone compounds and methods of use |
| CZ2014295A3 (cs) * | 2014-04-30 | 2015-10-14 | Masarykova Univerzita | Substituované furo[3,2-b]pyridiny pro použití jako léčiva |
| EP3313834A1 (en) * | 2015-06-29 | 2018-05-02 | Merck Patent GmbH | Tbk/ikk inhibitor compounds and uses thereof |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | 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 |
| JP7564888B2 (ja) * | 2020-05-01 | 2024-10-09 | ギリアード サイエンシーズ， インコーポレイテッド | Ｃｄ７３阻害性２，４－ジオキソピリミジン化合物 |
| JP2025531008A (ja) | 2022-08-09 | 2025-09-19 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | フロピリミジン誘導体 |
| WO2024033280A1 (en) | 2022-08-09 | 2024-02-15 | Merck Patent Gmbh | Furopyridin and furopyrimidin, inhibitors of pi4k, for use in the treatment of parasite infection and malaria |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE247469T1 (de) * | 1995-06-07 | 2003-09-15 | Pfizer | Heterocyclische kondensierte pyrimidin-derivate |
| US6187777B1 (en) | 1998-02-06 | 2001-02-13 | Amgen Inc. | Compounds and methods which modulate feeding behavior and related diseases |
| US20020004511A1 (en) | 2000-06-28 | 2002-01-10 | Luzzio Michael Joseph | Thiophene derivatives useful as anticancer agents |
| WO2008118823A2 (en) | 2007-03-26 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20090118276A1 (en) * | 2007-11-02 | 2009-05-07 | Wyeth | Thienopyrimidines, thienopyridines, and pyrrolopyrimidines as b-raf inhibitors |
| BRPI0908573A2 (pt) * | 2008-03-05 | 2012-12-25 | Methylgene Inc | inibidores da atividade de proteÍna tirosina quinase |
| SG2014015085A (en) | 2008-04-16 | 2014-06-27 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
-
2011
- 2011-07-29 AU AU2011295441A patent/AU2011295441B2/en not_active Ceased
- 2011-07-29 CN CN201180041050.9A patent/CN103052640B/zh not_active Expired - Fee Related
- 2011-07-29 WO PCT/EP2011/003831 patent/WO2012025187A2/en not_active Ceased
- 2011-07-29 KR KR20137007836A patent/KR20130108318A/ko not_active Withdrawn
- 2011-07-29 EP EP11738631.8A patent/EP2609100B1/en not_active Not-in-force
- 2011-07-29 MX MX2013002199A patent/MX2013002199A/es not_active Application Discontinuation
- 2011-07-29 SG SG2013013990A patent/SG187956A1/en unknown
- 2011-07-29 EA EA201300283A patent/EA201300283A1/ru unknown
- 2011-07-29 US US13/819,166 patent/US9006440B2/en not_active Expired - Fee Related
- 2011-07-29 CA CA2809333A patent/CA2809333C/en not_active Expired - Fee Related
- 2011-07-29 ES ES11738631T patent/ES2545352T3/es active Active
- 2011-07-29 BR BR112013004624A patent/BR112013004624A2/pt not_active IP Right Cessation
- 2011-07-29 JP JP2013525161A patent/JP5789300B2/ja not_active Expired - Fee Related
- 2011-08-26 AR ARP110103112 patent/AR082727A1/es unknown
-
2013
- 2013-02-21 IL IL224870A patent/IL224870A/en active IP Right Grant
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