JP2008519814A5 - - Google Patents
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- Publication number
- JP2008519814A5 JP2008519814A5 JP2007540715A JP2007540715A JP2008519814A5 JP 2008519814 A5 JP2008519814 A5 JP 2008519814A5 JP 2007540715 A JP2007540715 A JP 2007540715A JP 2007540715 A JP2007540715 A JP 2007540715A JP 2008519814 A5 JP2008519814 A5 JP 2008519814A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heteroaryl
- aryl
- alkoxy
- nr4r5
- 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.)
- Abandoned
Links
- 125000001072 heteroaryl group Chemical group 0.000 claims 69
- 125000003118 aryl group Chemical group 0.000 claims 60
- 229910052739 hydrogen Inorganic materials 0.000 claims 43
- 239000001257 hydrogen Substances 0.000 claims 43
- 150000002431 hydrogen Chemical class 0.000 claims 35
- -1 methylenedioxy Chemical group 0.000 claims 31
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 26
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 24
- 125000005842 heteroatom Chemical group 0.000 claims 23
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 19
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 150000001412 amines Chemical class 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 3
- 238000003556 assay Methods 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 210000002569 neuron Anatomy 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 238000003756 stirring Methods 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 238000010438 heat treatment Methods 0.000 claims 2
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 2
- 208000014674 injury Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 2
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 230000008733 trauma Effects 0.000 claims 2
- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- KZPYGQFFRCFCPP-UHFFFAOYSA-N 1,1'-bis(diphenylphosphino)ferrocene Chemical compound [Fe+2].C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1 KZPYGQFFRCFCPP-UHFFFAOYSA-N 0.000 claims 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- OZNPSODUPVRWJM-UHFFFAOYSA-N 3-[[(6-chloro-5-quinolin-5-ylpyridin-3-yl)amino]methyl]phenol Chemical compound OC1=CC=CC(CNC=2C=C(C(Cl)=NC=2)C=2C3=CC=CN=C3C=CC=2)=C1 OZNPSODUPVRWJM-UHFFFAOYSA-N 0.000 claims 1
- IOJWUTDVJYMWHJ-UHFFFAOYSA-N 3-[[(6-quinolin-5-ylpyrazin-2-yl)amino]methyl]phenol Chemical compound OC1=CC=CC(CNC=2N=C(C=NC=2)C=2C3=CC=CN=C3C=CC=2)=C1 IOJWUTDVJYMWHJ-UHFFFAOYSA-N 0.000 claims 1
- 125000006291 3-hydroxybenzyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])* 0.000 claims 1
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims 1
- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 208000030507 AIDS Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- ZOXJGFHDIHLPTG-UHFFFAOYSA-N Boron Chemical compound [B] ZOXJGFHDIHLPTG-UHFFFAOYSA-N 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000027089 Parkinsonian disease Diseases 0.000 claims 1
- 206010034010 Parkinsonism Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 201000001068 Prinzmetal angina Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 238000002266 amputation Methods 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 210000003050 axon Anatomy 0.000 claims 1
- 230000028600 axonogenesis Effects 0.000 claims 1
- 229910052796 boron Inorganic materials 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 150000001721 carbon Chemical class 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 230000005779 cell damage Effects 0.000 claims 1
- 208000037887 cell injury Diseases 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 208000025245 disorder of lacrimal gland Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000027993 eye symptom Diseases 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 125000005549 heteroarylene group Chemical group 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- LTISYOKGGULSJJ-UHFFFAOYSA-N n-[(4-chloro-3-fluorophenyl)methyl]-5-quinolin-5-ylpyridin-3-amine Chemical compound C1=C(Cl)C(F)=CC(CNC=2C=C(C=NC=2)C=2C3=CC=CN=C3C=CC=2)=C1 LTISYOKGGULSJJ-UHFFFAOYSA-N 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000014511 neuron projection development Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 239000012299 nitrogen atmosphere Substances 0.000 claims 1
- 230000003287 optical effect Effects 0.000 claims 1
- 229910052763 palladium Inorganic materials 0.000 claims 1
- YJVFFLUZDVXJQI-UHFFFAOYSA-L palladium(ii) acetate Chemical compound [Pd+2].CC([O-])=O.CC([O-])=O YJVFFLUZDVXJQI-UHFFFAOYSA-L 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 230000008929 regeneration Effects 0.000 claims 1
- 238000011069 regeneration method Methods 0.000 claims 1
- 229960001755 resorcinol Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 239000012321 sodium triacetoxyborohydride Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 238000010626 work up procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0425026A GB0425026D0 (en) | 2004-11-12 | 2004-11-12 | Compounds which bind to the active site of protein kinase enzymes |
| GBGB0500245.6A GB0500245D0 (en) | 2004-11-12 | 2005-01-07 | Compounds which bind to the active site of protein kinase enzymes |
| PCT/GB2005/004358 WO2006051311A1 (en) | 2004-11-12 | 2005-11-11 | Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008519814A JP2008519814A (ja) | 2008-06-12 |
| JP2008519814A5 true JP2008519814A5 (https=) | 2008-12-25 |
Family
ID=35788166
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007540715A Abandoned JP2008519814A (ja) | 2004-11-12 | 2005-11-11 | プロテインキナーゼ酵素の活性部位と結合する窒素複素環式芳香族化合物 |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1814856A1 (https=) |
| JP (1) | JP2008519814A (https=) |
| CA (1) | CA2585490A1 (https=) |
| WO (1) | WO2006051311A1 (https=) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8211919B2 (en) | 2005-09-02 | 2012-07-03 | Astellas Pharma Inc. | Amide derivatives as rock inhibitors |
| JP5252404B2 (ja) * | 2006-08-16 | 2013-07-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ピラジン化合物、その使用及び調製方法 |
| US8071779B2 (en) | 2006-12-18 | 2011-12-06 | Inspire Pharmaceuticals, Inc. | Cytoskeletal active rho kinase inhibitor compounds, composition and use |
| GEP20125379B (en) | 2007-05-03 | 2012-01-10 | Pfizer Ltd | 2 -pyridine carboxamide derivatives as sodium channel modulators |
| CA2697081C (en) | 2007-08-22 | 2013-04-23 | Irm Llc | 5-(4-(haloalkoxy)phenyl)pyrimidine-2-amine compounds and compositions as kinase inhibitors |
| TWI504395B (zh) | 2009-03-10 | 2015-10-21 | Substituted 3-amino-2-mercaptoquinoline as a KCNQ2 / 3 modifier | |
| TWI461197B (zh) | 2009-03-12 | 2014-11-21 | 2-mercaptoquinoline-3-carboxamide as a KCNQ2 / 3 modifier | |
| TW201038565A (en) | 2009-03-12 | 2010-11-01 | Gruenenthal Gmbh | Substituted 2-mercapto-3-aminopyridines as KCNQ2/3 modulators |
| TWI475020B (zh) | 2009-03-12 | 2015-03-01 | The substituted nicotine amide as a KCNQ2 / 3 modifier | |
| HRP20140371T1 (hr) | 2009-05-15 | 2014-05-23 | Novartis Ag | Arilpiridini kao inhibitori sinteze aldosterona |
| SI2440547T1 (sl) * | 2009-06-12 | 2023-05-31 | Abivax | Nove kemične molekule, ki zavirajo mehanizem spajanja za zdravljenje bolezni, ki so posledica napak pri spajanju |
| US10253020B2 (en) | 2009-06-12 | 2019-04-09 | Abivax | Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging |
| SI2531492T1 (sl) | 2010-02-05 | 2016-08-31 | Heptares Therapeutics Limited | Derivati 1,2,4-triazin-4-amina |
| JP5605727B2 (ja) | 2010-04-06 | 2014-10-15 | Ｊｎｃ株式会社 | セレンテラジン類縁体及びセレンテラミド類縁体 |
| TW201211007A (en) | 2010-08-27 | 2012-03-16 | Gruenenthal Gmbh | Substituted 2-amino-quinoline-3-carboxamides as KCNQ2/3 modulators |
| SI2609086T1 (sl) | 2010-08-27 | 2015-04-30 | Gruenenthal Gmbh | Substituirani 2-okso in 2-tiokso-dihidrokinolin-3-karboksamidi kot KCNQ2/3 modulatorji |
| DK2609083T3 (da) | 2010-08-27 | 2015-03-30 | Gruenenthal Gmbh | Substituerede 2-oxy-quinolin-3-carboxamider som KCNQ2/3 modulatorer |
| MX2013002295A (es) | 2010-09-01 | 2013-05-09 | Gruenenthal Gmbh | 1-oxo-dihidroisoquinolin-3-carboxamidas sustituidas como moduladores de kcnq2/3. |
| JP2013542967A (ja) * | 2010-11-17 | 2013-11-28 | ノバルティス アーゲー | ３−（アミノアリール）−ピリジン化合物 |
| EP2817292B1 (en) | 2012-02-22 | 2019-12-18 | Sanford-Burnham Medical Research Institute | Sulfonamide compounds and uses as tnap inhibitors |
| EP2757161A1 (en) | 2013-01-17 | 2014-07-23 | Splicos | miRNA-124 as a biomarker of viral infection |
| US20160339018A1 (en) | 2013-04-24 | 2016-11-24 | Kyushu University, National University Corporation | Therapeutic agent for ocular fundus disease |
| AU2015206652A1 (en) | 2014-01-14 | 2016-08-04 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| EP2974729A1 (en) | 2014-07-17 | 2016-01-20 | Abivax | Quinoline derivatives for use in the treatment of inflammatory diseases |
| LT3319959T (lt) | 2015-07-06 | 2021-12-27 | Alkermes, Inc. | Histono deacetilazės hetero-halogeno inhibitoriai |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| WO2017064119A1 (en) | 2015-10-13 | 2017-04-20 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion |
| EP4088719A1 (en) | 2015-10-13 | 2022-11-16 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion |
| US11168068B2 (en) | 2016-07-18 | 2021-11-09 | Janssen Pharmaceutica Nv | Tau PET imaging ligands |
| RS62959B1 (sr) | 2017-01-11 | 2022-03-31 | Alkermes Inc | Biciklični inhibitori histon-deacetilaze |
| US11225475B2 (en) | 2017-08-07 | 2022-01-18 | Alkermes, Inc. | Substituted pyridines as inhibitors of histone deacetylase |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| EP3669873A1 (en) | 2018-12-20 | 2020-06-24 | Abivax | Quinoline derivatives for use ine the traeatment of inflammation diseases |
| SG11202107614PA (en) | 2019-01-18 | 2021-08-30 | Astrazeneca Ab | Pcsk9 inhibitors and methods of use thereof |
| AU2020209216A1 (en) | 2019-01-18 | 2021-08-26 | Astrazeneca Ab | PCSK9 inhibitors and methods of use thereof |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| TW202115024A (zh) | 2019-08-14 | 2021-04-16 | 美商英塞特公司 | 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物 |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| US11993580B1 (en) | 2022-12-02 | 2024-05-28 | Neumora Therapeutics, Inc. | Methods of treating neurological disorders |
| PY2404093A (es) * | 2023-01-30 | 2024-10-03 | Eurofarma Laboratorios S A | Hidrazidas bloqueadoras de nav 1.7 y/o nav 1.8, sus procesos de obtención, composiciones, usos, métodos de tratamiento de los mismos y kits |
| WO2025224050A1 (en) | 2024-04-22 | 2025-10-30 | Institut National de la Santé et de la Recherche Médicale | Methods of treatment of patients suffering from hypomelanosis of ito |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60023926T2 (de) * | 1999-09-10 | 2006-07-20 | Merck & Co., Inc. | Tyrosin kinase inhibitoren |
| CA2423050A1 (en) * | 2000-09-20 | 2002-03-28 | Ortho-Mcneil Pharmaceutical, Inc. | Pyrazine derivatives as modulators of tyrosine kinases |
| DE60317198T2 (de) * | 2002-05-23 | 2008-12-04 | Cytopia Research Pty. Ltd., Richmond | Proteinkinaseinhibitoren |
| CA2530389A1 (en) * | 2003-07-02 | 2005-01-13 | Biofocus Discovery Limited | Pyrazine and pyridine derivatives as rho kinase inhibitors |
-
2005
- 2005-11-11 EP EP05809312A patent/EP1814856A1/en not_active Withdrawn
- 2005-11-11 JP JP2007540715A patent/JP2008519814A/ja not_active Abandoned
- 2005-11-11 WO PCT/GB2005/004358 patent/WO2006051311A1/en not_active Ceased
- 2005-11-11 CA CA002585490A patent/CA2585490A1/en not_active Abandoned
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