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 (enExample) | 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 (enExample) |
| JP (1) | JP2008519814A (enExample) |
| CA (1) | CA2585490A1 (enExample) |
| WO (1) | WO2006051311A1 (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8211919B2 (en) | 2005-09-02 | 2012-07-03 | Astellas Pharma Inc. | Amide derivatives as rock inhibitors |
| US8318723B2 (en) * | 2006-08-16 | 2012-11-27 | Boehringer Ingelheim International Gmbh | Pyrazine compounds, their use and methods of preparation |
| US8071779B2 (en) * | 2006-12-18 | 2011-12-06 | Inspire Pharmaceuticals, Inc. | Cytoskeletal active rho kinase inhibitor compounds, composition and use |
| KR20100007956A (ko) | 2007-05-03 | 2010-01-22 | 화이자 리미티드 | 나트륨 채널 조절제로서의 2-피리딘 카복스아마이드 유도체 |
| MX2010002004A (es) | 2007-08-22 | 2010-03-11 | Irm Llc | Compuestos de 5-(4-(halo-alcoxi)-fenil)-pirimidin-2-amina y composiciones con inhibidores de cinasa. |
| 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 | |
| TWI475020B (zh) | 2009-03-12 | 2015-03-01 | The substituted nicotine amide as a KCNQ2 / 3 modifier | |
| TW201038565A (en) | 2009-03-12 | 2010-11-01 | Gruenenthal Gmbh | Substituted 2-mercapto-3-aminopyridines as KCNQ2/3 modulators |
| SG175925A1 (en) * | 2009-05-15 | 2011-12-29 | Novartis Ag | Aryl pyridine as aldosterone synthase inhibitors |
| WO2010143169A2 (en) * | 2009-06-12 | 2010-12-16 | Société Splicos | Compounds useful for treating aids |
| US10253020B2 (en) | 2009-06-12 | 2019-04-09 | Abivax | Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging |
| US8809525B2 (en) | 2010-02-05 | 2014-08-19 | Heptares Therapeutics Limited | 1,2,4-triazine-4-amine derivatives |
| 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 |
| HUE024870T2 (en) | 2010-08-27 | 2016-02-29 | Gruenenthal Gmbh | Substituted 2-oxo and 2-thioxo-dihydroquinoline-3-carboxamides as modulators of KCNQ2 / 3 |
| TW201211007A (en) | 2010-08-27 | 2012-03-16 | Gruenenthal Gmbh | Substituted 2-amino-quinoline-3-carboxamides as KCNQ2/3 modulators |
| RU2595894C2 (ru) | 2010-08-27 | 2016-08-27 | Грюненталь Гмбх | Замещенные 2-окси-хинолин-3-карбоксамиды в качестве модуляторов kcnq2/3 |
| MX2013002295A (es) | 2010-09-01 | 2013-05-09 | Gruenenthal Gmbh | 1-oxo-dihidroisoquinolin-3-carboxamidas sustituidas como moduladores de kcnq2/3. |
| EP2640702A1 (en) * | 2010-11-17 | 2013-09-25 | Novartis AG | 3-(aminoaryl)-pyridine compounds |
| BR112014020773A2 (pt) | 2012-02-22 | 2020-10-27 | Sanford-Burnham Medical Research Institute | compostos de sulfonamida e seus usos como inibidores tnap |
| EP2757161A1 (en) | 2013-01-17 | 2014-07-23 | Splicos | miRNA-124 as a biomarker of viral infection |
| EP2990040B1 (en) | 2013-04-24 | 2019-12-04 | Kyushu University, National University Corporation | Therapeutic agent for eyeground disease |
| TN2016000270A1 (en) | 2014-01-14 | 2017-10-06 | Millennium Pharm Inc | Heteroaryls and uses thereof. |
| JP2017502092A (ja) | 2014-01-14 | 2017-01-19 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | ヘテロアリール及びその使用 |
| EP2974729A1 (en) | 2014-07-17 | 2016-01-20 | Abivax | Quinoline derivatives for use in the treatment of inflammatory diseases |
| EP3319968A1 (en) | 2015-07-06 | 2018-05-16 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| ES2899906T3 (es) | 2015-07-06 | 2022-03-15 | Alkermes Inc | Inhibidores bicíclicos de histona desacetilasa |
| US12048761B2 (en) | 2015-10-13 | 2024-07-30 | Inserm (Institut National De La Santé Et De La Recherche Medicale) | 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 |
| ES2875562T3 (es) | 2017-01-11 | 2021-11-10 | Alkermes Inc | Inhibidores bicíclicos de histona desacetilasa |
| 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 |
| EA202191890A1 (ru) | 2019-01-18 | 2022-02-03 | Астразенека Аб | Ингибиторы pcsk9 и способы их применения |
| 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 |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| PH12022550361A1 (en) | 2019-08-14 | 2023-02-27 | Incyte Corp | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| PE20221905A1 (es) | 2019-10-11 | 2022-12-23 | Incyte Corp | Aminas biciclicas como inhibidoras de la cdk2 |
| 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 |
| EP4626878A1 (en) | 2022-12-02 | 2025-10-08 | Neumora Therapeutics, Inc. | Methods of treating neurological disorders |
| AR131658A1 (es) * | 2023-01-30 | 2025-04-16 | 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 sus 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 |
|---|---|---|---|---|
| ATE309241T1 (de) * | 1999-09-10 | 2005-11-15 | Merck & Co Inc | Tyrosin kinase inhibitoren |
| PT1330452E (pt) * | 2000-09-20 | 2009-01-22 | Ortho Mcneil Pharm Inc | Derivados de pirazina como moduladores de tirosina-cinases |
| US7122550B2 (en) * | 2002-05-23 | 2006-10-17 | Cytopia Pty Ltd | Protein kinase inhibitors |
| JP2007516196A (ja) * | 2003-07-02 | 2007-06-21 | ガラパゴス エヌブイ | Rhoキナーゼ阻害剤としてのピラジン及びピラリジン誘導体 |
-
2005
- 2005-11-11 JP JP2007540715A patent/JP2008519814A/ja not_active Abandoned
- 2005-11-11 EP EP05809312A patent/EP1814856A1/en not_active Withdrawn
- 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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