ES2791186T3 - Triazoles como inhibidores de receptores NR2B - Google Patents
Triazoles como inhibidores de receptores NR2B Download PDFInfo
- Publication number
- ES2791186T3 ES2791186T3 ES15777754T ES15777754T ES2791186T3 ES 2791186 T3 ES2791186 T3 ES 2791186T3 ES 15777754 T ES15777754 T ES 15777754T ES 15777754 T ES15777754 T ES 15777754T ES 2791186 T3 ES2791186 T3 ES 2791186T3
- Authority
- ES
- Spain
- Prior art keywords
- phenyl
- ylmethyl
- triazole
- imidazol
- methyl
- 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.)
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- 108010038912 Retinoid X Receptors Proteins 0.000 title description 16
- 150000003852 triazoles Chemical class 0.000 title description 6
- 108091006082 receptor inhibitors Proteins 0.000 title description 2
- 102000034527 Retinoid X Receptors Human genes 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 claims abstract description 222
- 150000001875 compounds Chemical class 0.000 claims abstract description 142
- 150000003839 salts Chemical class 0.000 claims abstract description 76
- 125000001424 substituent group Chemical group 0.000 claims abstract description 75
- 229910052736 halogen Inorganic materials 0.000 claims abstract description 74
- 150000002367 halogens Chemical class 0.000 claims abstract description 69
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 64
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 55
- 239000012453 solvate Substances 0.000 claims abstract description 36
- 150000001204 N-oxides Chemical class 0.000 claims abstract description 31
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 30
- 239000001257 hydrogen Substances 0.000 claims abstract description 30
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims abstract description 26
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 25
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims abstract description 19
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 15
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract description 15
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims abstract description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract description 10
- 125000005842 heteroatom Chemical group 0.000 claims abstract description 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract description 7
- 229910052760 oxygen Inorganic materials 0.000 claims abstract description 6
- 229910052717 sulfur Inorganic materials 0.000 claims abstract description 5
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims abstract description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 32
- -1 3,5-dicyclopropyl- [1,2,4] triazol-1-ylmethyl Chemical group 0.000 claims description 107
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- 238000000034 method Methods 0.000 claims description 17
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
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- 108020003175 receptors Proteins 0.000 claims description 11
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- 239000004480 active ingredient Substances 0.000 claims description 6
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- 125000006002 1,1-difluoroethyl group Chemical group 0.000 claims description 4
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 4
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- AQLRWJVRJUSCJS-UHFFFAOYSA-N 1-[[1-(4-chlorophenyl)triazol-4-yl]methyl]-3,5-dimethyl-1,2,4-triazole Chemical compound N1=C(C)N=C(C)N1CC1=CN(C=2C=CC(Cl)=CC=2)N=N1 AQLRWJVRJUSCJS-UHFFFAOYSA-N 0.000 claims description 2
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Classifications
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
Landscapes
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- Chemical & Material Sciences (AREA)
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- Psychiatry (AREA)
- Psychology (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
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| US201462037831P | 2014-08-15 | 2014-08-15 | |
| US201562146656P | 2015-04-13 | 2015-04-13 | |
| PCT/US2015/045412 WO2016025917A1 (en) | 2014-08-15 | 2015-08-14 | Triazoles as nr2b receptor inhibitors |
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| ES2791186T3 true ES2791186T3 (es) | 2020-11-03 |
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| PT (1) | PT3180329T (https=) |
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| ES2791252T3 (es) | 2014-08-15 | 2020-11-03 | Janssen Pharmaceuticals Inc | Pirazoles |
| WO2016025917A1 (en) | 2014-08-15 | 2016-02-18 | Janssen Pharmaceuticals, Inc. | Triazoles as nr2b receptor inhibitors |
| HRP20200410T1 (hr) | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| BR112018016329A2 (pt) | 2016-02-10 | 2018-12-18 | Janssen Pharmaceutica Nv | 1,2,3-triazóis substituídos como moduladores de nmda seletivos para nr2b |
| 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 |
| MX2019006940A (es) * | 2016-12-14 | 2019-09-06 | Sk Biopharmaceuticals Co Ltd | Uso de compuestos de carbamato para prevencion, alivio o tratamiento del trastorno bipolar. |
| WO2019193516A2 (en) | 2018-04-04 | 2019-10-10 | Janssen Pharmaceutica Nv | Substituted pyridine and pyrimidines and their use as glun2b receptor modulators |
| CN113993868A (zh) | 2019-06-14 | 2022-01-28 | 詹森药业有限公司 | 取代的吡唑并吡啶酰胺以及它们作为glun2b受体调节剂的用途 |
| MX2021015508A (es) | 2019-06-14 | 2022-01-31 | Janssen Pharmaceutica Nv | Carbamatos de piridina y su uso como moduladores del receptor glun2b. |
| KR20220024403A (ko) | 2019-06-14 | 2022-03-03 | 얀센 파마슈티카 엔.브이. | 치환된 피라졸로-피라진 및 이들의 glun2b 수용체 조절제로서의 용도 |
| CN113950357A (zh) | 2019-06-14 | 2022-01-18 | 詹森药业有限公司 | 吡嗪氨基甲酸酯及其作为GluN2B受体调节剂的用途 |
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| JP7667097B2 (ja) | 2019-06-14 | 2025-04-22 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ピラゾロ－ピリジンアミド及びｇｌｕｎ２ｂ受容体調節因子としてのその使用 |
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| TWI443090B (zh) | 2007-05-25 | 2014-07-01 | Abbvie Deutschland | 作為代謝性麩胺酸受體２（ｍｇｌｕ２ 受體）之正向調節劑之雜環化合物 |
| CN101842357A (zh) | 2007-08-30 | 2010-09-22 | 武田药品工业株式会社 | 取代的吡唑衍生物 |
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| US9643922B2 (en) * | 2008-08-18 | 2017-05-09 | Yale University | MIF modulators |
| RU2517181C2 (ru) | 2008-10-16 | 2014-05-27 | Орто-Макнейл-Янссен Фармасьютикалз, Инк. | Производные индола и бензоморфолина в качестве модулятора метаботропных глутаматных рецепторов |
| CA2744498C (en) | 2008-11-25 | 2017-10-24 | University Of Rochester | Mlk inhibitors and methods of use |
| US8969342B2 (en) * | 2009-03-20 | 2015-03-03 | Brandeis University | Compounds and methods for treating mammalian gastrointestinal microbial infections |
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| 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 |
| TW201444820A (zh) | 2013-03-13 | 2014-12-01 | Abbvie Inc | 吡啶ｃｄｋ９激酶抑制劑 |
| ES2791252T3 (es) | 2014-08-15 | 2020-11-03 | Janssen Pharmaceuticals Inc | Pirazoles |
| WO2016025917A1 (en) | 2014-08-15 | 2016-02-18 | Janssen Pharmaceuticals, Inc. | Triazoles as nr2b receptor inhibitors |
| HRP20200410T1 (hr) | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| BR112018016329A2 (pt) | 2016-02-10 | 2018-12-18 | Janssen Pharmaceutica Nv | 1,2,3-triazóis substituídos como moduladores de nmda seletivos para nr2b |
| 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 |
-
2015
- 2015-08-14 WO PCT/US2015/045412 patent/WO2016025917A1/en not_active Ceased
- 2015-08-14 PT PT157777541T patent/PT3180329T/pt unknown
- 2015-08-14 PL PL15777754T patent/PL3180329T3/pl unknown
- 2015-08-14 HU HUE15777754A patent/HUE049277T2/hu unknown
- 2015-08-14 ES ES15777754T patent/ES2791186T3/es active Active
- 2015-08-14 US US15/503,864 patent/US9981950B2/en active Active
- 2015-08-14 DK DK15777754.1T patent/DK3180329T3/da active
- 2015-08-14 EP EP15777754.1A patent/EP3180329B1/en active Active
- 2015-08-14 JP JP2017508504A patent/JP6605020B2/ja active Active
-
2018
- 2018-04-27 US US15/964,794 patent/US10323021B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US20180282305A1 (en) | 2018-10-04 |
| JP2017524019A (ja) | 2017-08-24 |
| EP3180329B1 (en) | 2020-03-18 |
| PT3180329T (pt) | 2020-06-08 |
| HUE049277T2 (hu) | 2020-09-28 |
| EP3180329A1 (en) | 2017-06-21 |
| JP6605020B2 (ja) | 2019-11-13 |
| WO2016025917A1 (en) | 2016-02-18 |
| US20170226087A1 (en) | 2017-08-10 |
| DK3180329T3 (da) | 2020-04-06 |
| US9981950B2 (en) | 2018-05-29 |
| PL3180329T3 (pl) | 2020-08-24 |
| US10323021B2 (en) | 2019-06-18 |
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