JP2017524019A5 - - Google Patents
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- Publication number
- JP2017524019A5 JP2017524019A5 JP2017508504A JP2017508504A JP2017524019A5 JP 2017524019 A5 JP2017524019 A5 JP 2017524019A5 JP 2017508504 A JP2017508504 A JP 2017508504A JP 2017508504 A JP2017508504 A JP 2017508504A JP 2017524019 A5 JP2017524019 A5 JP 2017524019A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- ylmethyl
- triazole
- imidazol
- chloro
- 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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- 125000005843 halogen group Chemical group 0.000 claims description 131
- 125000000217 alkyl group Chemical group 0.000 claims description 55
- 125000003545 alkoxy group Chemical group 0.000 claims description 53
- 150000001875 compounds Chemical class 0.000 claims description 47
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 45
- 229910052736 halogen Inorganic materials 0.000 claims description 43
- 150000002367 halogens Chemical class 0.000 claims description 43
- 150000003839 salts Chemical class 0.000 claims description 37
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 36
- 239000012453 solvate Substances 0.000 claims description 36
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 32
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 31
- 125000001424 substituent group Chemical group 0.000 claims description 31
- 150000001204 N-oxides Chemical class 0.000 claims description 29
- 201000010099 disease Diseases 0.000 claims description 23
- 208000035475 disorder Diseases 0.000 claims description 21
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 239000001257 hydrogen Substances 0.000 claims description 20
- -1 3,5-dicyclopropyl- [1,2,4] triazol-1-ylmethyl Chemical group 0.000 claims description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims description 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 9
- 108010054200 NR2B NMDA receptor Proteins 0.000 claims description 8
- 229910052731 fluorine Inorganic materials 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- 229910052801 chlorine Inorganic materials 0.000 claims description 7
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 208000026106 cerebrovascular disease Diseases 0.000 claims description 6
- 206010015037 epilepsy Diseases 0.000 claims description 6
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- 208000028552 Treatment-Resistant Depressive disease Diseases 0.000 claims description 5
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- 208000002193 Pain Diseases 0.000 claims description 4
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- 125000004189 3,4-dichlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(Cl)C([H])=C1* 0.000 claims 1
- YUDVHEROTXDJBH-UHFFFAOYSA-N C1(CCC1)C=1N(C=CN=1)CC=1N=NN(C=1)C1=CC(=C(C=C1)Cl)Cl Chemical compound C1(CCC1)C=1N(C=CN=1)CC=1N=NN(C=1)C1=CC(=C(C=C1)Cl)Cl YUDVHEROTXDJBH-UHFFFAOYSA-N 0.000 claims 1
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- 208000028867 ischemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 238000000034 method Methods 0.000 description 6
- JRLJHLTZFBRDJM-UHFFFAOYSA-N 1-(3,4-dichlorophenyl)triazole Chemical compound C1=C(Cl)C(Cl)=CC=C1N1N=NC=C1 JRLJHLTZFBRDJM-UHFFFAOYSA-N 0.000 description 1
- XCUYCJFGWDLGRI-UHFFFAOYSA-N FC(C=1C=C(C=CC=1F)N1N=NC(=C1)CC1=NNC=C1)F Chemical compound FC(C=1C=C(C=CC=1F)N1N=NC(=C1)CC1=NNC=C1)F XCUYCJFGWDLGRI-UHFFFAOYSA-N 0.000 description 1
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- 230000002490 cerebral effect Effects 0.000 description 1
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| USRE49517E1 (en) | 2014-08-15 | 2023-05-02 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| PT3180329T (pt) | 2014-08-15 | 2020-06-08 | Janssen Pharmaceuticals Inc | Triazóis como inibidores do recetor nr2b |
| HRP20200410T1 (hr) | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| CN109071488B (zh) | 2016-02-10 | 2021-08-13 | 詹森药业有限公司 | 取代的1,2,3-三唑作为nr2b-选择性nmda调节剂 |
| TW201819376A (zh) | 2016-10-06 | 2018-06-01 | 比利時商健生藥品公司 | 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途 |
| IL267195B2 (en) | 2016-12-14 | 2024-05-01 | Sk Biopharmaceuticals Co Ltd | Use of carbamate compounds for prevention, alleviation or treatment of bipolar disorder |
| US11447503B2 (en) | 2019-06-14 | 2022-09-20 | Janssen Pharmaceutica Nv | Pyridine carbamates and their use as GLUN2B receptor modulators |
| JP7346441B2 (ja) | 2018-04-04 | 2023-09-19 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ピリジン及びピリミジン並びにｇｌｕｎ２ｂ受容体調節物質としてのそれらの使用 |
| MX2021015500A (es) | 2019-06-14 | 2022-02-10 | Janssen Pharmaceutica Nv | Pirazolo-pirazinas sustituidas y su uso como moduladores del receptor glun2b. |
| CA3142998A1 (en) | 2019-06-14 | 2020-12-17 | Janssen Pharmaceutica Nv | Pyrazine carbamates and their use as glun2b receptor modulators |
| TW202112774A (zh) | 2019-06-14 | 2021-04-01 | 比利時商健生藥品公司 | 經取代之吡唑并－吡啶醯胺及其作為ｇｌｕｎ２ｂ受體調節劑之用途 |
| JP2022536424A (ja) | 2019-06-14 | 2022-08-16 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ヘテロ芳香族ピラゾロピリジン及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用 |
| KR20220020917A (ko) | 2019-06-14 | 2022-02-21 | 얀센 파마슈티카 엔.브이. | 치환된 피라졸로[4,3-b]피리딘 및 GLUN2B 수용체 조절제로서의 이들의 용도 |
| PH12021552839A1 (en) | 2019-06-14 | 2022-10-03 | Janssen Pharmaceutica Nv | Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators |
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| US6610723B2 (en) * | 2001-01-29 | 2003-08-26 | Hoffmann-La Roche Inc. | Imidazole derivatives |
| EP1490364B1 (en) | 2002-03-28 | 2007-09-26 | Eisai R&D Management Co., Ltd. | 7-azaindoles as inhibitors of c-jun n-terminal kinases for the treatment of neurodegenerative disorders |
| US7005432B2 (en) * | 2002-05-16 | 2006-02-28 | Hoffman-La Roche Inc. | Substituted imidazol-pyridazine derivatives |
| TW200604183A (en) | 2004-02-18 | 2006-02-01 | Astrazeneca Ab | Triazole compounds and their use as metabotropic glutamate receptor antagonists |
| US7807704B2 (en) | 2006-03-30 | 2010-10-05 | Chemocentryx, Inc. | Bicyclic, nitrogen-containing compounds modulating CXCR4 and/or CCXCKR2 |
| PE20090717A1 (es) | 2007-05-18 | 2009-07-18 | Smithkline Beecham Corp | Derivados de quinolina como inhibidores de la pi3 quinasa |
| KR20100017372A (ko) | 2007-05-25 | 2010-02-16 | 애보트 게엠베하 운트 콤파니 카게 | 향대사성 글루타메이트 수용체 2（ｍｇｌｕ2 수용체）의 포지티브 조절자로서의 헤테로사이클릭 화합물 |
| EP2194045A4 (en) | 2007-08-30 | 2011-09-21 | Takeda Pharmaceutical | Substituted pyrazole derivative |
| EP2215073A4 (en) | 2007-10-31 | 2011-04-06 | Merck Sharp & Dohme | SLEEP MODULATION WITH NR2B RECEPTOR ANTAGONISTS |
| RU2499598C2 (ru) | 2008-03-27 | 2013-11-27 | Евотек Интернациональ Гмбх | Способы лечения нарушений с применением селективного антагониста nr2b-подтипа nmda рецепторов |
| WO2010016490A1 (ja) | 2008-08-05 | 2010-02-11 | 第一三共株式会社 | イミダゾピリジン－２－オン誘導体 |
| US9643922B2 (en) * | 2008-08-18 | 2017-05-09 | Yale University | MIF modulators |
| AU2009304293B2 (en) | 2008-10-16 | 2012-04-26 | Addex Pharma S.A. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
| EP3037421A3 (en) | 2008-11-25 | 2016-11-30 | University Of Rochester | Mlk inhibitors and methods of use |
| WO2010108187A2 (en) * | 2009-03-20 | 2010-09-23 | Brandeis University | Compounds and methods for treating mammalian gastrointestinal microbial infections |
| WO2011156245A2 (en) | 2010-06-09 | 2011-12-15 | Merck Sharp & Dohme Corp. | Positive allosteric modulators of mglur2 |
| WO2013130855A1 (en) | 2012-03-02 | 2013-09-06 | Takeda Pharmaceutical Company Limited | Indazole derivatives |
| WO2014124651A1 (en) | 2013-02-15 | 2014-08-21 | Københavns Universitet | Pyrrolidine-2-carboxylic acid derivatives as iglur antagonists |
| EP2970200A1 (en) | 2013-03-13 | 2016-01-20 | Abbvie Inc. | Pyridine cdk9 kinase inhibitors |
| PT3180329T (pt) | 2014-08-15 | 2020-06-08 | Janssen Pharmaceuticals Inc | Triazóis como inibidores do recetor nr2b |
| USRE49517E1 (en) | 2014-08-15 | 2023-05-02 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| HRP20200410T1 (hr) | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| CN109071488B (zh) | 2016-02-10 | 2021-08-13 | 詹森药业有限公司 | 取代的1,2,3-三唑作为nr2b-选择性nmda调节剂 |
| TW201819376A (zh) | 2016-10-06 | 2018-06-01 | 比利時商健生藥品公司 | 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途 |
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2018
- 2018-04-27 US US15/964,794 patent/US10323021B2/en active Active
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