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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- 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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- 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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- 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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| US9981950B2 (en) | 2014-08-15 | 2018-05-29 | Janssen Pharmaceuticals, Inc. | Triazoles as NR2B receptor inhibitors |
| BR112018000468A2 (pt) | 2015-07-09 | 2018-09-18 | Janssen Pharmaceutica Nv | 4-azaindóis substituídos e seu uso como moduladores do receptor de glun2b |
| MA44008A (fr) | 2016-02-10 | 2018-12-19 | Janssen Pharmaceutica Nv | 1,2,3-triazoles substitués utilisés comme modulateurs de nmda sélectifs de 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 |
| JP7208139B2 (ja) | 2016-12-14 | 2023-01-18 | エスケー バイオファーマスティカルズ カンパニー リミテッド | 双極性障害の予防、軽減又は治療のためのカルバメート化合物の使用 |
| EP3774732A4 (en) | 2018-04-04 | 2022-02-09 | Janssen Pharmaceutica NV | PYRIDINE AND SUBSTITUTED PYRIMIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS |
| BR112021025132A2 (pt) | 2019-06-14 | 2022-01-25 | Janssen Pharmaceutica Nv | Carbamatos de piridina e seu uso como moduladores do receptor glun2b |
| MX2021015511A (es) | 2019-06-14 | 2022-01-31 | Janssen Pharmaceutica Nv | Carbamatos de pirazina y sus usos como moduladores del receptor glun2b. |
| JP2022536773A (ja) | 2019-06-14 | 2022-08-18 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ピラゾロピラジン及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用 |
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| CN113993583A (zh) | 2019-06-14 | 2022-01-28 | 詹森药业有限公司 | 取代的吡唑并[4,3-b]吡啶及其作为GLUN2B受体调节剂的用途 |
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| US9434743B2 (en) | 2012-03-02 | 2016-09-06 | 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 |
| WO2016025918A1 (en) | 2014-08-15 | 2016-02-18 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| US9981950B2 (en) | 2014-08-15 | 2018-05-29 | Janssen Pharmaceuticals, Inc. | Triazoles as NR2B receptor inhibitors |
| BR112018000468A2 (pt) | 2015-07-09 | 2018-09-18 | Janssen Pharmaceutica Nv | 4-azaindóis substituídos e seu uso como moduladores do receptor de glun2b |
| MA44008A (fr) | 2016-02-10 | 2018-12-19 | Janssen Pharmaceutica Nv | 1,2,3-triazoles substitués utilisés comme modulateurs de nmda sélectifs de 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 |
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2015
- 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 PL PL15777754T patent/PL3180329T3/pl unknown
- 2015-08-14 JP JP2017508504A patent/JP6605020B2/ja active Active
- 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 ES ES15777754T patent/ES2791186T3/es active Active
- 2015-08-14 HU HUE15777754A patent/HUE049277T2/hu unknown
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2018
- 2018-04-27 US US15/964,794 patent/US10323021B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3180329A1 (en) | 2017-06-21 |
| US9981950B2 (en) | 2018-05-29 |
| HUE049277T2 (hu) | 2020-09-28 |
| US10323021B2 (en) | 2019-06-18 |
| JP6605020B2 (ja) | 2019-11-13 |
| PT3180329T (pt) | 2020-06-08 |
| US20180282305A1 (en) | 2018-10-04 |
| US20170226087A1 (en) | 2017-08-10 |
| DK3180329T3 (da) | 2020-04-06 |
| JP2017524019A (ja) | 2017-08-24 |
| PL3180329T3 (pl) | 2020-08-24 |
| WO2016025917A1 (en) | 2016-02-18 |
| EP3180329B1 (en) | 2020-03-18 |
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