ES2822830T3 - Antagonistas selectivos de NR2B - Google Patents
Antagonistas selectivos de NR2B Download PDFInfo
- Publication number
- ES2822830T3 ES2822830T3 ES16787974T ES16787974T ES2822830T3 ES 2822830 T3 ES2822830 T3 ES 2822830T3 ES 16787974 T ES16787974 T ES 16787974T ES 16787974 T ES16787974 T ES 16787974T ES 2822830 T3 ES2822830 T3 ES 2822830T3
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- Prior art keywords
- compound
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- column
- alkyl
- pharmaceutically acceptable
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- 239000005557 antagonist Substances 0.000 title description 4
- 102000034527 Retinoid X Receptors Human genes 0.000 title 1
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract description 22
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 21
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- 125000004076 pyridyl group Chemical group 0.000 claims abstract description 8
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- 238000010189 synthetic method Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- VNNOMGVHZFZWLD-RXMQYKEDSA-N tert-butyl n-[(4r)-3-oxo-1,2-oxazolidin-4-yl]carbamate Chemical compound CC(C)(C)OC(=O)N[C@@H]1CONC1=O VNNOMGVHZFZWLD-RXMQYKEDSA-N 0.000 description 1
- 108091008646 testicular receptors Proteins 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000009466 transformation Effects 0.000 description 1
- 229950005135 traxoprodil Drugs 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- GPRLSGONYQIRFK-MNYXATJNSA-N triton Chemical compound [3H+] GPRLSGONYQIRFK-MNYXATJNSA-N 0.000 description 1
- 229960000281 trometamol Drugs 0.000 description 1
- 238000010626 work up procedure Methods 0.000 description 1
- 239000011701 zinc Substances 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/09—Geometrical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3309DE2015 | 2015-10-14 | ||
| PCT/US2016/056716 WO2017066368A1 (en) | 2015-10-14 | 2016-10-13 | Selective nr2b antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2822830T3 true ES2822830T3 (es) | 2021-05-05 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES16787974T Active ES2822830T3 (es) | 2015-10-14 | 2016-10-13 | Antagonistas selectivos de NR2B |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10501451B2 (enExample) |
| EP (1) | EP3362447B1 (enExample) |
| JP (1) | JP6843853B2 (enExample) |
| KR (1) | KR20180064507A (enExample) |
| CN (1) | CN108368101B (enExample) |
| AU (1) | AU2016340239A1 (enExample) |
| BR (1) | BR112018007181A2 (enExample) |
| CA (1) | CA3001894A1 (enExample) |
| EA (1) | EA201890764A1 (enExample) |
| ES (1) | ES2822830T3 (enExample) |
| IL (1) | IL258611A (enExample) |
| MX (1) | MX2018004257A (enExample) |
| WO (1) | WO2017066368A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2018004256A (es) * | 2015-10-14 | 2018-05-16 | Squibb Bristol Myers Co | Antagonistas de receptor de n-metil-d-aspartato subtipo 2b (nr2b) selectivos. |
| EA202191014A1 (ru) * | 2018-10-17 | 2021-11-09 | Бёрингер Ингельхайм Интернациональ Гмбх | Производные 4-пиразин-2-илметил-морфолина и их применение в качестве лекарственного средства |
| TW202035396A (zh) * | 2018-10-17 | 2020-10-01 | 德商百靈佳殷格翰國際股份有限公司 | 4-吡啶基甲基-嗎啉衍生物及其作為藥物之用途 |
| CN112888684B (zh) * | 2018-10-17 | 2023-10-10 | 勃林格殷格翰国际有限公司 | 4-嘧啶-5-基甲基-吗啉衍生物及其作为药物的用途 |
| US12398143B2 (en) | 2019-06-04 | 2025-08-26 | Boehringer Ingelheim International Gmbh | Imidazopyrazine derivatives and the use thereof as medicament |
| EP4255419A1 (en) * | 2020-12-04 | 2023-10-11 | Novartis AG | Dosage regimen for a nr2b-nmda receptor nam for the treatment of depression |
| CN113620896A (zh) * | 2021-08-31 | 2021-11-09 | 青岛科技大学 | 2-(2-氯苯基)甲基-4,4-二甲基-3-异恶唑酮的制备方法 |
| CN116063200A (zh) * | 2022-12-12 | 2023-05-05 | 华南理工大学 | 一种异噁唑啉宠物用杀虫剂氟雷拉纳中间体及其制备方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| US7022728B2 (en) | 2001-03-09 | 2006-04-04 | Abbott Laboratories | Benzimidazoles that are useful in treating male sexual dysfunction |
| JPWO2003035641A1 (ja) | 2001-10-22 | 2005-02-10 | 塩野義製薬株式会社 | 新規カルバモイルピロリドン誘導体 |
| KR20060017839A (ko) | 2003-06-04 | 2006-02-27 | 머크 앤드 캄파니 인코포레이티드 | Ｎｍｄａ／ｎｒ2ｂ 길항제로서 3-플루오로-피페리딘 |
| MXPA06003748A (es) | 2003-10-08 | 2006-06-14 | Pfizer | Compuestos de lactama condensada. |
| US20070185168A1 (en) * | 2004-04-07 | 2007-08-09 | Takai Haruki S | Piperidine derivatives |
| JPWO2006137465A1 (ja) * | 2005-06-24 | 2009-01-22 | 塩野義製薬株式会社 | 含窒素複素環誘導体 |
| EP2520567A3 (en) | 2006-02-23 | 2012-12-12 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
| KR20100045983A (ko) | 2007-06-29 | 2010-05-04 | 에모리 유니버시티 | 신경보호를 위한 ｎｍｄａ 수용체 길항물질 |
| JP2009067784A (ja) * | 2007-08-21 | 2009-04-02 | Shionogi & Co Ltd | 環式基で置換された含窒素複素環誘導体を含有する鎮痛剤 |
| SG10201501050RA (en) * | 2010-02-11 | 2015-04-29 | Univ Northwestern | Secondary Structure Stabilized NMDA Receptor Modulators And Uses Thereof |
| US9221796B2 (en) * | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
| US9187506B2 (en) | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
-
2016
- 2016-10-13 CA CA3001894A patent/CA3001894A1/en not_active Abandoned
- 2016-10-13 CN CN201680073103.8A patent/CN108368101B/zh active Active
- 2016-10-13 EP EP16787974.1A patent/EP3362447B1/en active Active
- 2016-10-13 EA EA201890764A patent/EA201890764A1/ru unknown
- 2016-10-13 AU AU2016340239A patent/AU2016340239A1/en not_active Abandoned
- 2016-10-13 ES ES16787974T patent/ES2822830T3/es active Active
- 2016-10-13 KR KR1020187013128A patent/KR20180064507A/ko active Pending
- 2016-10-13 JP JP2018519276A patent/JP6843853B2/ja not_active Expired - Fee Related
- 2016-10-13 US US15/767,385 patent/US10501451B2/en active Active
- 2016-10-13 WO PCT/US2016/056716 patent/WO2017066368A1/en not_active Ceased
- 2016-10-13 MX MX2018004257A patent/MX2018004257A/es unknown
- 2016-10-13 BR BR112018007181A patent/BR112018007181A2/pt not_active Application Discontinuation
-
2018
- 2018-04-10 IL IL258611A patent/IL258611A/en unknown
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2019
- 2019-12-09 US US16/707,382 patent/US10954225B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US10954225B2 (en) | 2021-03-23 |
| CN108368101B (zh) | 2022-03-15 |
| EP3362447A1 (en) | 2018-08-22 |
| MX2018004257A (es) | 2018-05-16 |
| CN108368101A (zh) | 2018-08-03 |
| BR112018007181A2 (pt) | 2018-10-16 |
| EA201890764A1 (ru) | 2018-09-28 |
| IL258611A (en) | 2018-06-28 |
| EP3362447B1 (en) | 2020-08-26 |
| US20200115370A1 (en) | 2020-04-16 |
| US10501451B2 (en) | 2019-12-10 |
| JP6843853B2 (ja) | 2021-03-17 |
| AU2016340239A1 (en) | 2018-05-31 |
| KR20180064507A (ko) | 2018-06-14 |
| WO2017066368A1 (en) | 2017-04-20 |
| CA3001894A1 (en) | 2017-04-20 |
| JP2018530582A (ja) | 2018-10-18 |
| US20180312495A1 (en) | 2018-11-01 |
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