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 | |
| US60/979,587 | 2007-10-12 | ||
| GB0720000.9 | 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 (enExample) | 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 (enExample) |
| EP (1) | EP2114941B1 (enExample) |
| JP (1) | JP5442448B2 (enExample) |
| CN (1) | CN101679408B (enExample) |
| AR (1) | AR064491A1 (enExample) |
| AU (1) | AU2007337886C1 (enExample) |
| CA (1) | CA2672172C (enExample) |
| HR (1) | HRP20150642T1 (enExample) |
| MX (1) | MX2009006706A (enExample) |
| NO (1) | NO343370B1 (enExample) |
| WO (1) | WO2008078091A1 (enExample) |
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 |
| US8895745B2 (en) | 2006-12-22 | 2014-11-25 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| CA2672213C (en) | 2006-12-22 | 2016-02-16 | Astex Therapeutics Limited | Bicyclic amine derivatives as protein tyrosine kinase inhibitors |
| 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 |
| MX2010002536A (es) | 2007-09-14 | 2010-08-10 | Ortho Mcneil Janssen Pharm | 4-fenil-3,4,5,6-tetrahidro-2h, 1'h-[1,4]bipiridinil-2'-onas 1',3'-disubstituidas. |
| CA2697399C (en) | 2007-09-14 | 2016-01-19 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | 1,3-disubstituted 4-(aryl-x-phenyl)-1h-pyridin-2-ones |
| US8722894B2 (en) | 2007-09-14 | 2014-05-13 | Janssen Pharmaceuticals, Inc. | 1,3-disubstituted-4-phenyl-1H-pyridin-2-ones |
| 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 |
| PL2212323T3 (pl) | 2007-10-17 | 2013-01-31 | Novartis Ag | Pochodne imidazo[1,2-a]pirydyny użyteczne jako inhibitory ALK |
| MX2010005110A (es) | 2007-11-14 | 2010-09-09 | Ortho Mcneil Janssen Pharm | Derivados de imidazo[1,2-a]piridina y su uso como moduladores alostericos positivos de los receptores de glutamato metabotropico 2. |
| GB0810902D0 (en) * | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| WO2010017046A1 (en) | 2008-08-05 | 2010-02-11 | Merck & Co., Inc. | Pyrazolo[1,5-a]pyridines as mark inhibitors |
| BRPI0918055A2 (pt) | 2008-09-02 | 2015-12-01 | Addex Pharmaceuticals Sa | derivados de 3-azabiciclo[3,1,0]hexila como moduladores de receptores metabotrópicos de glutamato. |
| JP5656848B2 (ja) | 2008-10-16 | 2015-01-21 | 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モジュレーターとしてのインドールおよびベンゾモルホリンの誘導体 |
| CA2744138C (en) * | 2008-11-28 | 2015-08-11 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors |
| MX2011009796A (es) * | 2009-03-20 | 2011-12-14 | Amgen Inc | Inhibidores de la cinasa pi3. |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| 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 |
| SG176021A1 (en) | 2009-05-12 | 2011-12-29 | Janssen Pharmaceuticals Inc | 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders |
| ES2409006T3 (es) | 2009-05-12 | 2013-06-24 | Janssen Pharmaceuticals Inc. | Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de los receptores mGluR2 |
| UA111579C2 (uk) * | 2009-08-17 | 2016-05-25 | Інтеллікіне Ллк | ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ |
| 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. |
| GB201007286D0 (en) * | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| US20130196986A1 (en) * | 2010-09-21 | 2013-08-01 | Marc Labroli | Triazolopyrazinones as p2x7 receptor antagonists |
| US9012448B2 (en) | 2010-11-08 | 2015-04-21 | Janssen Pharmaceuticals, Inc. | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors |
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| PL2649069T3 (pl) | 2010-11-08 | 2016-01-29 | Janssen Pharmaceuticals Inc | Pochodne 1,2,4-triazolo[4,3-a]pirydyny i ich zastosowanie jako dodatnich allosterycznych modulatorów receptorów mGluR2 |
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| MX350788B (es) | 2012-01-06 | 2017-09-13 | Abide Therapeutics Inc | Compuestos de carbamato y preparación y uso de los mismos. |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| 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 |
| 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 |
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| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| 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 |
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| US20150203589A1 (en) | 2012-07-24 | 2015-07-23 | The Trustees Of Columbia University In The City Of New York | Fusion proteins and methods thereof |
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| DK3395814T3 (da) | 2013-10-25 | 2022-07-04 | Blueprint Medicines Corp | Hæmmere af fibroblastvækstfaktorreceptoren |
| MX374758B (es) | 2013-12-13 | 2025-03-06 | Hoffmann La Roche | Inhibidores de tirosina cinasa de bruton. |
| PT3096790T (pt) | 2014-01-21 | 2019-10-15 | Janssen Pharmaceutica Nv | Combinações compreendendo moduladores alostéricos positivos ou agonistas ortostéricos do recetor glutamatérgico metabotrópico do subtipo 2 e seu uso |
| EA202192105A3 (ru) | 2014-02-04 | 2022-02-28 | Янссен Фармацевтика Нв | Комбинации, содержащие положительные аллостерические модуляторы или ортостерические агонисты метаботропного глутаматергического рецептора 2 подтипа, и их применение |
| BR112016022062B1 (pt) | 2014-03-26 | 2023-04-11 | Astex Therapeutics Limited | Combinação, composição farmacêutica, uso de uma combinação ou de uma composição farmacêutica, e, produto farmacêutico |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| PL3122358T3 (pl) | 2014-03-26 | 2021-06-14 | Astex Therapeutics Ltd. | Połączenia inhibitorów fgfr i cmet w leczeniu nowotworu |
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2007
- 2007-12-21 US US12/520,481 patent/US8895745B2/en active Active
- 2007-12-21 HR HRP20150642TT patent/HRP20150642T1/hr unknown
- 2007-12-21 MX MX2009006706A patent/MX2009006706A/es active IP Right Grant
- 2007-12-21 CA CA2672172A patent/CA2672172C/en active Active
- 2007-12-21 WO PCT/GB2007/004934 patent/WO2008078091A1/en not_active Ceased
- 2007-12-21 AR ARP070105856A patent/AR064491A1/es active IP Right Grant
- 2007-12-21 EP EP07848659.4A patent/EP2114941B1/en active Active
- 2007-12-21 JP JP2009542223A patent/JP5442448B2/ja not_active Expired - Fee Related
- 2007-12-21 AU AU2007337886A patent/AU2007337886C1/en not_active Ceased
- 2007-12-21 CN CN200780047672.6A patent/CN101679408B/zh not_active Expired - Fee Related
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2009
- 2009-07-13 NO NO20092657A patent/NO343370B1/no unknown