JP2011500623A5 - - Google Patents
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- Publication number
- JP2011500623A5 JP2011500623A5 JP2010529359A JP2010529359A JP2011500623A5 JP 2011500623 A5 JP2011500623 A5 JP 2011500623A5 JP 2010529359 A JP2010529359 A JP 2010529359A JP 2010529359 A JP2010529359 A JP 2010529359A JP 2011500623 A5 JP2011500623 A5 JP 2011500623A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- independently selected
- optionally
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000001424 substituent group Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 10
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000003282 alkyl amino group Chemical group 0.000 claims 7
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 6
- -1 carboxy, carbonyl Chemical group 0.000 claims 6
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 3
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 3
- 150000008064 anhydrides Chemical group 0.000 claims 3
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 3
- 125000005647 linker group Chemical group 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 150000003462 sulfoxides Chemical class 0.000 claims 3
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 210000000988 bone and bone Anatomy 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 102100034134 Activin receptor type-1B Human genes 0.000 claims 1
- 101710173011 Activin receptor type-1B Proteins 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 206010006956 Calcium deficiency Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000032544 Cicatrix Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000018565 Hemochromatosis Diseases 0.000 claims 1
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 101000712674 Homo sapiens TGF-beta receptor type-1 Proteins 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 206010023330 Keloid scar Diseases 0.000 claims 1
- 206010027398 Mesenteric fibrosis Diseases 0.000 claims 1
- 208000029578 Muscle disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010034665 Peritoneal fibrosis Diseases 0.000 claims 1
- 206010051246 Photodermatosis Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 102100033456 TGF-beta receptor type-1 Human genes 0.000 claims 1
- 208000025865 Ulcer Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 230000004221 bone function Effects 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=O 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000009251 neurologic dysfunction Effects 0.000 claims 1
- 208000015015 neurological dysfunction Diseases 0.000 claims 1
- 230000011164 ossification Effects 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000008845 photoaging Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 231100000241 scar Toxicity 0.000 claims 1
- 230000037387 scars Effects 0.000 claims 1
- 230000000638 stimulation Effects 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07118726.4 | 2007-10-17 | ||
| EP07118726 | 2007-10-17 | ||
| EP08151336.8 | 2008-02-12 | ||
| EP08151336 | 2008-02-12 | ||
| PCT/EP2008/063841 WO2009050183A2 (en) | 2007-10-17 | 2008-10-15 | Imidazo [1, 2-a] pyridine derivatives useful as alk inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011500623A JP2011500623A (ja) | 2011-01-06 |
| JP2011500623A5 true JP2011500623A5 (cg-RX-API-DMAC7.html) | 2011-12-01 |
| JP5456681B2 JP5456681B2 (ja) | 2014-04-02 |
Family
ID=39944334
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010529359A Expired - Fee Related JP5456681B2 (ja) | 2007-10-17 | 2008-10-15 | ＡＬＫ阻害剤として有用なイミダゾ［１，２−ａ］ピリジン誘導体 |
Country Status (23)
Families Citing this family (83)
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| US8343966B2 (en) * | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
| CN102159559A (zh) * | 2008-07-18 | 2011-08-17 | 赛诺菲-安万特 | 新型咪唑并[1,2-a]吡啶衍生物、其制备方法、其作为药物的用途、其药物组合物和新型用途特别是作为MET抑制剂的新型用途 |
| FR2945806B1 (fr) * | 2009-05-19 | 2013-04-05 | Sanofi Aventis | Nouveaux derives imidazo[1,2-a]pyridine,procede de preparation,medicaments,compositions pharmaceutiques et utilisation notamment comme inhibiteurs de met |
| CA2760778A1 (en) * | 2009-05-13 | 2010-11-18 | Amgen Inc. | Heteroaryl compounds as pikk inhibitors |
| EP2454262B1 (en) * | 2009-07-15 | 2014-05-14 | Abbott Laboratories | Pyrrolopyrazine inhibitors of kinases |
| UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| WO2011146287A1 (en) | 2010-05-20 | 2011-11-24 | Takeda Pharmaceutical Company Limited | Pyrazolo[4,3-b]pyridine-7-amine inhibitors of alk5 |
| CN102443009B (zh) * | 2010-09-30 | 2014-04-16 | 山东轩竹医药科技有限公司 | 并环激酶抑制剂 |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| PH12013502695A1 (en) * | 2011-07-01 | 2019-06-14 | Bayer Ip Gmbh | Hydroxymethylaryl-substituted pyrrolotriazines as alk1 inhibitors |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| ES2790358T3 (es) | 2011-12-28 | 2020-10-27 | Global Blood Therapeutics Inc | Compuestos de heteroaril aldehído sustituido y métodos para su uso en el aumento de la oxigenación tisular |
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| US10280168B2 (en) | 2012-03-30 | 2019-05-07 | Agency For Science, Technology And Research | Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof |
| BR112014030812B1 (pt) | 2012-06-13 | 2022-11-08 | Incyte Holdings Corporation | Compostos tricíclicos substituídos como inibidores de fgfr, seus usos, composição farmacêutica e método para inibir uma enzima fgfr |
| US9738636B2 (en) | 2012-09-28 | 2017-08-22 | Vanderbilt University | Fused heterocyclic compounds as selective BMP inhibitors |
| US9981939B2 (en) | 2013-03-15 | 2018-05-29 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| EP2970196B1 (en) | 2013-03-15 | 2020-11-25 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| US9422279B2 (en) | 2013-03-15 | 2016-08-23 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
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| US8952171B2 (en) | 2013-03-15 | 2015-02-10 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
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| US10266551B2 (en) | 2013-03-15 | 2019-04-23 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
| US20140274961A1 (en) | 2013-03-15 | 2014-09-18 | Global Blood Therapeutics, Inc. | Compounds and uses thereof for the modulation of hemoglobin |
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| TWI663160B (zh) | 2016-05-12 | 2019-06-21 | 全球血液治療公司 | 用於合成2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)-吡啶-3-基)甲氧基)苯甲醛之方法 |
| US11352328B2 (en) | 2016-07-12 | 2022-06-07 | Arisan Therapeutics Inc. | Heterocyclic compounds for the treatment of arenavirus |
| WO2018053126A1 (en) * | 2016-09-14 | 2018-03-22 | Vanderbilt University | Inhibition of bmp signaling, compounds, compositions and uses thereof |
| TW202332423A (zh) | 2016-10-12 | 2023-08-16 | 美商全球血液治療公司 | 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| KR20200115620A (ko) | 2018-01-29 | 2020-10-07 | 메르크 파텐트 게엠베하 | Gcn2 억제제 및 이의 용도 |
| EP3765460A1 (en) | 2018-03-14 | 2021-01-20 | Vanderbilt University | Inhibition of bmp signaling, compounds, compositions and uses thereof |
| TW201946630A (zh) | 2018-05-04 | 2019-12-16 | 美商英塞特公司 | Fgfr抑制劑之鹽 |
| SG11202010636VA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Solid forms of an fgfr inhibitor and processes for preparing the same |
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| JP7300057B2 (ja) * | 2019-07-26 | 2023-06-28 | シージーンテック （スーチョウ， チャイナ） カンパニー リミテッド | Ｆｇｆｒとｖｅｇｆｒ二重阻害剤としてのピリジン誘導体 |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3153456A1 (en) | 2019-10-02 | 2021-04-08 | Stefanie Fluckiger-Mangual | Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
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| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| CN111116582B (zh) * | 2019-12-18 | 2022-07-29 | 大连大学 | 一种mGluR2拮抗剂 |
| EP4076456B1 (en) * | 2019-12-19 | 2024-05-01 | Université de Strasbourg | Sigma-1 receptor ligands and therapeutic uses thereof |
| CN115052663A (zh) | 2020-01-08 | 2022-09-13 | 辛瑟斯治疗股份有限公司 | Alk5抑制剂缀合物及其用途 |
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| WO2021147699A1 (zh) * | 2020-01-21 | 2021-07-29 | 四川科伦博泰生物医药股份有限公司 | 吡啶并杂环类化合物、其制备方法及用途 |
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| EP4182322B1 (en) | 2020-07-15 | 2024-04-24 | Chiesi Farmaceutici S.p.A. | Pyrido oxazine derivatives as alk5 inhibitors |
| JP2023533850A (ja) | 2020-07-15 | 2023-08-04 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | Ａｌｋ５阻害剤としてのピリドオキサジンアミノ誘導体 |
| WO2022136221A1 (en) | 2020-12-23 | 2022-06-30 | Chiesi Farmaceutici S.P.A. | Pyrido oxazine derivatives as alk5 inhibitors |
| KR20230134545A (ko) * | 2021-01-26 | 2023-09-21 | 씨젠테크 (쑤저우, 차이나) 컴퍼니 리미티드 | 메틸피라졸로로 치환된 피리도 이미다졸계 화합물의결정형 및 이의 제조방법 |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313611A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
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| EP1790650B1 (en) * | 2004-08-31 | 2014-03-26 | Msd Kk | NEW SUBSTITUTED IMIDAZOLE DERIVATIVES |
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| DOP2006000051A (es) * | 2005-02-24 | 2006-08-31 | Lilly Co Eli | Inhibidores de vegf-r2 y métodos |
| HRP20150642T1 (hr) | 2006-12-22 | 2015-08-14 | Astex Therapeutics Limited | BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a |
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2008
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- 2008-10-15 BR BRPI0817434-2A patent/BRPI0817434A2/pt not_active IP Right Cessation
- 2008-10-15 EP EP08838625A patent/EP2212323B1/en active Active
- 2008-10-15 AR ARP080104492A patent/AR068877A1/es unknown
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- 2008-10-15 PL PL08838625T patent/PL2212323T3/pl unknown
- 2008-10-15 US US12/679,549 patent/US8367662B2/en not_active Expired - Fee Related
- 2008-10-15 PE PE2008001769A patent/PE20091383A1/es not_active Application Discontinuation
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- 2008-10-15 WO PCT/EP2008/063841 patent/WO2009050183A2/en not_active Ceased
- 2008-10-15 ES ES08838625T patent/ES2393430T3/es active Active
- 2008-10-15 PT PT08838625T patent/PT2212323E/pt unknown
- 2008-10-15 CA CA2703037A patent/CA2703037A1/en not_active Abandoned
- 2008-10-15 AU AU2008313773A patent/AU2008313773B2/en not_active Ceased
- 2008-10-16 TW TW097139735A patent/TW200922570A/zh unknown
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2010
- 2010-03-25 IL IL204720A patent/IL204720A0/en unknown
- 2010-04-01 ZA ZA2010/02334A patent/ZA201002334B/en unknown
- 2010-04-08 MA MA32756A patent/MA31766B1/fr unknown
- 2010-04-16 TN TN2010000167A patent/TN2010000167A1/fr unknown
- 2010-05-11 CO CO10056124A patent/CO6270321A2/es not_active Application Discontinuation