JP2013536208A5 - - Google Patents
Download PDFInfo
- Publication number
- 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 |
|---|---|---|---|
| EP10008928.3 | 2010-08-27 | ||
| EP10008928 | 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 |
|---|---|---|---|---|
| RU2568258C2 (ru) | 2011-02-28 | 2015-11-20 | Саншайн Лейк Фарма Ко., Лтд | Замещенные соединения хинолина и способы их использования |
| US9045493B2 (en) * | 2012-02-09 | 2015-06-02 | Merck Patent Gmbh | Furo[3,2-b]- and thieno[3,2-b]pyridin derivatives |
| CA2863717C (en) * | 2012-02-21 | 2021-09-28 | Lars Burgdorf | Furopyridine derivatives |
| US8975282B2 (en) | 2012-07-28 | 2015-03-10 | Sunshine Lake Pharma Co., Ltd. | Substituted pyrazolone compounds and methods of use |
| JP6342392B2 (ja) | 2012-07-28 | 2018-06-13 | カリター・サイエンシーズ・エルエルシー | 置換型ピラゾロン化合物及び使用方法 |
| CZ305472B6 (cs) * | 2014-04-30 | 2015-10-14 | Masarykova Univerzita | Substituované furo[3,2-b]pyridiny pro použití jako léčiva |
| MX2017015357A (es) * | 2015-06-29 | 2018-03-16 | Merck Patent Gmbh | Compuestos inhibidores de serina/treonina-proteina cinasa (tbk)/inhibidor de cinasa de factor nuclear kappa-b subunidad epsilon (ikk-epsilon) y usos de los mismos. |
| EA202192575A1 (ru) | 2019-03-21 | 2022-01-14 | Онксео | Соединения dbait в сочетании с ингибиторами киназ для лечения рака |
| CN114761006A (zh) | 2019-11-08 | 2022-07-15 | Inserm(法国国家健康医学研究院) | 对激酶抑制剂产生耐药性的癌症的治疗方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| IL297327B2 (en) * | 2020-05-01 | 2026-01-01 | Gilead Sciences Inc | 4,2-dioxopyrimidine compounds CD73 inhibitors |
| 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 |
|---|---|---|---|---|
| JP3290666B2 (ja) * | 1995-06-07 | 2002-06-10 | ファイザー・インコーポレーテッド | 複素環式の縮合環ピリミジン誘導体 |
| 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 |
| US7834024B2 (en) | 2007-03-26 | 2010-11-16 | 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 |
| NZ588355A (en) * | 2008-03-05 | 2012-03-30 | Methylgene Inc | Inhibitors of protein tyrosine kinase activity |
| SG165655A1 (en) | 2008-04-16 | 2010-11-29 | 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 EA EA201300283A patent/EA201300283A1/ru unknown
- 2011-07-29 SG SG2013013990A patent/SG187956A1/en unknown
- 2011-07-29 WO PCT/EP2011/003831 patent/WO2012025187A2/en not_active Ceased
- 2011-07-29 EP EP11738631.8A patent/EP2609100B1/en not_active Not-in-force
- 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 MX MX2013002199A patent/MX2013002199A/es not_active Application Discontinuation
- 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 JP JP2013525161A patent/JP5789300B2/ja not_active Expired - Fee Related
- 2011-07-29 KR KR20137007836A patent/KR20130108318A/ko not_active Withdrawn
- 2011-07-29 ES ES11738631T patent/ES2545352T3/es active Active
- 2011-07-29 BR BR112013004624A patent/BR112013004624A2/pt not_active IP Right Cessation
- 2011-08-26 AR ARP110103112 patent/AR082727A1/es unknown
-
2013
- 2013-02-21 IL IL224870A patent/IL224870A/en active IP Right Grant
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013536208A5 (https=) | ||
| KR102553943B1 (ko) | 세포배양배지에 알부민, 히알루론산, 또는 콜라겐을 유효성분으로 포함하는 화장용 조성물 | |
| EP3007556B1 (en) | Cell stabilization | |
| JP2013538214A5 (https=) | ||
| ES2969240T3 (es) | Medio para formar colonias y uso de este | |
| AU2011272137B2 (en) | Novel peptide and use thereof | |
| US20240299391A1 (en) | Compounds and methods for treatment of diamond blackfan anemia | |
| US11844779B2 (en) | PKC-Delta-I inhibitor formulations and uses thereof | |
| CN105939717A (zh) | 治疗和预防同种抗体驱动的慢性移植物抗宿主病的方法 | |
| JP2011246442A (ja) | 光老化抑制剤および皮膚菲薄化抑制剤 | |
| Chen et al. | Metabolic reprogramming: a new option for the treatment of spinal cord injury | |
| KR101508323B1 (ko) | 세포 배양액 | |
| US12569494B2 (en) | Compositions and methods to promote thymic regeneration | |
| JP7360171B2 (ja) | Ｂリンパ球活性の調節及び臓器保護のためのピルフェニドン誘導体 | |
| US10668027B1 (en) | Method of treating Acanthamoeba infection using allopurinol | |
| US20210024928A1 (en) | C/ebp alpha sarna compositions and methods of use | |
| EP4342479A1 (en) | Composition containing function-reinforced stem cell for prevention or treatment of atopic dermatitis | |
| EP3139944B1 (en) | Dsg2-derived short peptide for use in treating ocular angiogenic diseases | |
| US12508243B2 (en) | Compositions and methods for treating cancer and improving epithelial homeostasis | |
| JP2023054511A (ja) | 皮膚幹細胞増殖促進剤及び皮膚再生促進剤 | |
| WO2004000245A1 (ja) | 細胞への塩基性アミノ酸取り込み促進剤および化粧料もしくは医薬組成物 | |
| US9655901B1 (en) | Methods of treating Nfa-1 organism infection using allopurinol | |
| US11975051B1 (en) | Therapeutic peptides and uses thereof | |
| US20230201226A1 (en) | Combination therapy for reducing drug-induced nephrotoxicity, dyslipidemia and hyperglycemia | |
| RU2775721C2 (ru) | 6-6-конденсированные бициклические гетероарильные соединения и их применение в качестве ингибиторов lats |