JP2010513447A5 - - Google Patents
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- Publication number
- JP2010513447A5 JP2010513447A5 JP2009542223A JP2009542223A JP2010513447A5 JP 2010513447 A5 JP2010513447 A5 JP 2010513447A5 JP 2009542223 A JP2009542223 A JP 2009542223A JP 2009542223 A JP2009542223 A JP 2009542223A JP 2010513447 A5 JP2010513447 A5 JP 2010513447A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- group
- heterocyclyl
- 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.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 24
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000003118 aryl group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 8
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 125000001475 halogen functional group Chemical group 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- -1 -O- (CH 2 ) n -OR x Chemical group 0.000 claims 6
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006553 (C3-C8) cycloalkenyl group Chemical group 0.000 claims 1
- PIGSMPOINQICAJ-UHFFFAOYSA-N 1-[2-fluoro-4-[6-(1-tritylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]-3-propan-2-ylurea Chemical compound C1=C(F)C(NC(=O)NC(C)C)=CC=C1C1=CN=C2N1C=C(C1=CN(N=C1)C(C=1C=CC=CC=1)(C=1C=CC=CC=1)C=1C=CC=CC=1)C=C2 PIGSMPOINQICAJ-UHFFFAOYSA-N 0.000 claims 1
- KWAOMFSRFDBBRI-UHFFFAOYSA-N 1-[2-fluoro-4-[6-(1h-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]-3-propan-2-ylurea Chemical compound C1=C(F)C(NC(=O)NC(C)C)=CC=C1C1=CN=C2N1C=C(C1=CNN=C1)C=C2 KWAOMFSRFDBBRI-UHFFFAOYSA-N 0.000 claims 1
- TUEVVYKIUZPSKK-UHFFFAOYSA-N 1-cyclohexyl-3-[2-fluoro-4-[6-(1-tritylpyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]urea Chemical compound FC1=CC(C=2N3C=C(C=CC3=NC=2)C2=CN(N=C2)C(C=2C=CC=CC=2)(C=2C=CC=CC=2)C=2C=CC=CC=2)=CC=C1NC(=O)NC1CCCCC1 TUEVVYKIUZPSKK-UHFFFAOYSA-N 0.000 claims 1
- LTIBDLOGEYRZBY-UHFFFAOYSA-N 1-cyclohexyl-3-[2-fluoro-4-[6-(1h-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]phenyl]urea Chemical compound FC1=CC(C=2N3C=C(C=CC3=NC=2)C2=CNN=C2)=CC=C1NC(=O)NC1CCCCC1 LTIBDLOGEYRZBY-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- ZAKUXPKAPWYKQK-UHFFFAOYSA-N 3h-oxathiadiazole Chemical group N1SOC=N1 ZAKUXPKAPWYKQK-UHFFFAOYSA-N 0.000 claims 1
- 108091008794 FGF receptors Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical group C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- YDJQQPMRODCRSH-UHFFFAOYSA-N n-[4-[6-[3-(4-fluorophenyl)-1-tritylpyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]phenyl]methanesulfonamide Chemical compound C1=CC(NS(=O)(=O)C)=CC=C1C1=CN=C2N1C=C(C=1C(=NN(C=1)C(C=1C=CC=CC=1)(C=1C=CC=CC=1)C=1C=CC=CC=1)C=1C=CC(F)=CC=1)C=C2 YDJQQPMRODCRSH-UHFFFAOYSA-N 0.000 claims 1
- XWEKHLNARXFFBD-UHFFFAOYSA-N n-[4-[6-[5-(4-fluorophenyl)-1h-pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]phenyl]methanesulfonamide Chemical compound C1=CC(NS(=O)(=O)C)=CC=C1C1=CN=C2N1C=C(C=1C(=NNC=1)C=1C=CC(F)=CC=1)C=C2 XWEKHLNARXFFBD-UHFFFAOYSA-N 0.000 claims 1
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical group C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical compound N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 150000003536 tetrazoles Chemical group 0.000 claims 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical group C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 1
- 150000003852 triazoles Chemical group 0.000 claims 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87154306P | 2006-12-22 | 2006-12-22 | |
| US60/871,543 | 2006-12-22 | ||
| GB0625826.3 | 2006-12-22 | ||
| GB0625826A GB0625826D0 (en) | 2006-12-22 | 2006-12-22 | New compounds |
| US97958707P | 2007-10-12 | 2007-10-12 | |
| GB0720000.9 | 2007-10-12 | ||
| US60/979,587 | 2007-10-12 | ||
| GB0720000A GB0720000D0 (en) | 2007-10-12 | 2007-10-12 | New compounds |
| US98103907P | 2007-10-18 | 2007-10-18 | |
| US60/981,039 | 2007-10-18 | ||
| PCT/GB2007/004934 WO2008078091A1 (en) | 2006-12-22 | 2007-12-21 | Bicyclic heterocyclic compounds as fgfr inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010513447A JP2010513447A (ja) | 2010-04-30 |
| JP2010513447A5 true JP2010513447A5 (cg-RX-API-DMAC7.html) | 2011-02-10 |
| JP5442448B2 JP5442448B2 (ja) | 2014-03-12 |
Family
ID=39260738
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009542223A Expired - Fee Related JP5442448B2 (ja) | 2006-12-22 | 2007-12-21 | Ｆｇｆｒインヒビターとしての二環式ヘテロ環式化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8895745B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2114941B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP5442448B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN101679408B (cg-RX-API-DMAC7.html) |
| AR (1) | AR064491A1 (cg-RX-API-DMAC7.html) |
| AU (1) | AU2007337886C1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2672172C (cg-RX-API-DMAC7.html) |
| HR (1) | HRP20150642T1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2009006706A (cg-RX-API-DMAC7.html) |
| NO (1) | NO343370B1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2008078091A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (160)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| AR059898A1 (es) | 2006-03-15 | 2008-05-07 | Janssen Pharmaceutica Nv | Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2 |
| MX2009006706A (es) | 2006-12-22 | 2009-07-02 | Astex Therapeutics Ltd | Compuestos heterociclicos biciclicos como inhibidores del receptor del factor de crecimiento de fibroblastos. |
| JP5442449B2 (ja) | 2006-12-22 | 2014-03-12 | アステックス、セラピューティックス、リミテッド | 新規化合物 |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| WO2009033703A1 (en) | 2007-09-14 | 2009-03-19 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones |
| ATE516272T1 (de) | 2007-09-14 | 2011-07-15 | Ortho Mcneil Janssen Pharm | 1,3-disubstituierte 4-(aryl-x-phenyl)-1h-pyridin- 2-one |
| RS51660B (sr) | 2007-09-14 | 2011-10-31 | Ortho-Mcneil-Janssen Pharmaceuticals Inc. | 1`,3`-disupstituisani-4-fenil-3,4,5,6-tetrahidro-2h, 1`h-[1,4`] bipiridinil-2`-oni |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| US8367662B2 (en) * | 2007-10-17 | 2013-02-05 | Novartis Ag | Organic compounds |
| EP2220083B1 (en) | 2007-11-14 | 2017-07-19 | Janssen Pharmaceuticals, Inc. | Imidazo[1,2-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| GB0810902D0 (en) * | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| US8518911B2 (en) | 2008-08-05 | 2013-08-27 | Merck Sharp & Dohme Corp. | Pyrazolo[1,5-a]pyridines as MARK inhibitors |
| EP2344470B1 (en) | 2008-09-02 | 2013-11-06 | Janssen Pharmaceuticals, Inc. | 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors |
| AU2009304293B2 (en) | 2008-10-16 | 2012-04-26 | Addex Pharma S.A. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
| JP5690277B2 (ja) * | 2008-11-28 | 2015-03-25 | ジャンセン ファーマシューティカルズ， インコーポレイテッド． | 代謝型グルタミン酸受容体の調節因子としてのインドールおよびベンゾオキサジン誘導体 |
| AU2010226490A1 (en) * | 2009-03-20 | 2011-10-06 | Amgen Inc. | Inhibitors of PI3 kinase |
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| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
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| KR20120035158A (ko) | 2009-05-12 | 2012-04-13 | 얀센 파마슈티칼즈, 인코포레이티드 | 1,２,４?트리아졸로［４,３?ａ］피리딘 유도체 및 ｍＧｌｕＲ２ 수용체의 양성 알로스테릭 조절자로서의 그의 용도 |
| AU2010284254B2 (en) * | 2009-08-17 | 2015-09-17 | Intellikine, Llc | Heterocyclic compounds and uses thereof |
| FR2950345B1 (fr) * | 2009-09-18 | 2011-09-23 | Sanofi Aventis | Derives acetyleniques de 5-phenyl-pyrazolopyridine, leur preparation et leur application en therapeutique |
| FR2950344B1 (fr) * | 2009-09-18 | 2011-11-25 | Sanofi Aventis | Derives de 5-phenyl-pyrazolopyridine, leur preparation et leur aplication en therapeutique. |
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| EP2619204A4 (en) * | 2010-09-21 | 2014-08-27 | Merck Sharp & Dohme | TRIAZOLOPYRAZINONE AS P2X7 RECEPTOR ANTAGONISTS |
| CN103298809B (zh) | 2010-11-08 | 2016-08-31 | 杨森制药公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途 |
| EP2643320B1 (en) | 2010-11-08 | 2015-03-04 | Janssen Pharmaceuticals, Inc. | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| CA2814996C (en) | 2010-11-08 | 2019-10-01 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| GB201020179D0 (en) * | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| DK2663539T3 (en) * | 2011-01-13 | 2016-11-07 | Bayer Ip Gmbh | PROCESS FOR THE PREPARATION OF 2,2-difluoroethylamine of 2,2-difluoro-1-chloroethane and ammonia |
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| CN102432472A (zh) * | 2011-11-03 | 2012-05-02 | 浙江工业大学 | 一种2，2-二氟丙烷-1，3-二胺的制备方法 |
| EA028085B1 (ru) | 2012-01-06 | 2017-10-31 | Эбайд Терапьютикс, Инк. | Карбаматные соединения и их применение |
| 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 |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| JP6182593B2 (ja) | 2012-04-20 | 2017-08-16 | アドヴィーナス セラピューティクス リミテッド | 置換ヘテロ二環化合物、組成物及び医薬並びにそれらの用途 |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| EP3495367B1 (en) | 2012-06-13 | 2020-09-30 | Incyte Holdings Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| BR112015000653A2 (pt) | 2012-07-11 | 2019-11-05 | Blueprint Medicines Corp | compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos |
| BR112015000675B1 (pt) * | 2012-07-13 | 2022-07-12 | UCB Biopharma SRL | Derivados de imidazopiridina como moduladores da atividade de tnf |
| US20150203589A1 (en) | 2012-07-24 | 2015-07-23 | The Trustees Of Columbia University In The City Of New York | Fusion proteins and methods thereof |
| CN102786543B (zh) * | 2012-07-24 | 2016-04-27 | 上海瑞博化学有限公司 | 咪唑并[1，2-a]吡啶-6-硼酸频哪醇酯及其衍生物的制备方法 |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| AU2013324396B2 (en) | 2012-09-28 | 2018-10-04 | Vanderbilt University | Fused heterocyclic compounds as selective BMP inhibitors |
| US8871754B2 (en) | 2012-11-19 | 2014-10-28 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| PT2925757T (pt) | 2012-11-19 | 2018-01-09 | Novartis Ag | Compostos e composições para o tratamento de doenças parasitárias |
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| AR095464A1 (es) | 2013-03-15 | 2015-10-21 | Celgene Avilomics Res Inc | Compuestos de heteroarilo y usos de los mismos |
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| EA036160B1 (ru) | 2013-03-15 | 2020-10-08 | Селджен Кар Ллс | Гетероарильные соединения и их применение |
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| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
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| CN109999033B (zh) | 2014-01-21 | 2022-12-23 | 詹森药业有限公司 | 包括代谢型谷氨酸能受体亚型2的正别构调节物或正位激动剂的组合及其用途 |
| HRP20191646T1 (hr) | 2014-01-21 | 2019-12-13 | Janssen Pharmaceutica Nv | Kombinacije koje sadržavaju pozitivne alosteričke modulatore ili ortosteričke agoniste metabotropnog glutamatergičnog receptora podtip 2 i njihova uporaba |
| RU2715236C2 (ru) | 2014-03-26 | 2020-02-26 | Астекс Терапьютикс Лтд | Комбинации |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| RU2658821C1 (ru) | 2014-08-18 | 2018-06-25 | Эйсай Ар Энд Ди Менеджмент Ко., Лтд. | Соль моноциклического производного пиридина и ее кристалл |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
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