AR100733A1 - Derivados de difluoroetilpiridina como antagonistas del receptor nmda nr2b - Google Patents
Derivados de difluoroetilpiridina como antagonistas del receptor nmda nr2bInfo
- Publication number
- AR100733A1 AR100733A1 ARP150101773A ARP150101773A AR100733A1 AR 100733 A1 AR100733 A1 AR 100733A1 AR P150101773 A ARP150101773 A AR P150101773A AR P150101773 A ARP150101773 A AR P150101773A AR 100733 A1 AR100733 A1 AR 100733A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- optionally substituted
- alkoxy
- fluorine atoms
- Prior art date
Links
- 102000034527 Retinoid X Receptors Human genes 0.000 title abstract 3
- 108010038912 Retinoid X Receptors Proteins 0.000 title abstract 3
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 8
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 6
- 125000001153 fluoro group Chemical group F* 0.000 abstract 6
- 150000005829 chemical entities Chemical class 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- -1 -CO2R7 Chemical group 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 230000008485 antagonism Effects 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000002464 receptor antagonist Substances 0.000 abstract 1
- 229940044551 receptor antagonist Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Antagonistas del receptor selectivo del subtipo NR2B. También se describen composiciones farmacéuticas que comprenden una entidad química de fórmula (1), y métodos para tratar distintas enfermedades y trastornos asociados con el antagonismo del subtipo NR2B, por ejemplo, enfermedades y trastornos del SNC tales como la depresión, mediante la administración de una entidad química de la fórmula (1). Reivindicación 1: Una entidad química caracterizada porque es de fórmula (1), donde: uno de Y y Z es N, y el otro es C(R²); X es hidrógeno, halógeno, C₁₋₆ alquilo, C₃₋₆ cicloalquilo, C₁₋₄ alcoxi, -CO₂R⁷, -CN, -SR⁷, -S(O)₂R⁷, -NO₂, o -N(R⁷)(R⁸), donde dicho C₁₋₆ alquilo está opcionalmente sustituido con entre uno y seis átomos de flúor y dicho C₁₋₄ alcoxi está opcionalmente sustituido con entre uno y seis átomos de flúor; R¹ es hidrógeno, halógeno, C₁₋₄ alquilo, C₁₋₄ alcoxi, -CN, -NO₂, -N(R⁷)(R⁸), -CO₂R⁷, -C(O)N(R⁷)(R⁸) o C₃₋₆ cicloalquilo, donde dicho C₁₋₄ alquilo está opcionalmente sustituido con entre uno y tres átomos de flúor y dicho C₁₋₄ alcoxi está opcionalmente sustituido con entre uno y tres átomos de flúor; R² es hidrógeno, halógeno, C₁₋₄ alquilo, ciclopropilo o C₁₋₄ alcoxi donde dicho C₁₋₄ alquilo está opcionalmente sustituido con entre uno y tres átomos de flúor y dicho C₁₋₄ alcoxi está opcionalmente sustituido con entre uno y tres átomos de flúor; R³ es hidrógeno, -F, -Cl, -CH₃, -CF₃ o -OCH₃; R⁴ es hidrógeno, -F, -Cl, C₁₋₃ alquilo o ciclopropilo, donde dicho C₁₋₃ alquilo está opcionalmente sustituido con entre uno y tres átomos de flúor; R⁵ es hidrógeno o -CH₃; R⁶ es hidrógeno, -F o -CH₃; cada instancia de R⁷ en forma independiente es C₁₋₄ alquilo; y cada instancia de R⁸ en forma independiente es hidrógeno o C₁₋₄ alquilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462007762P | 2014-06-04 | 2014-06-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR100733A1 true AR100733A1 (es) | 2016-10-26 |
Family
ID=53776925
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150101773A AR100733A1 (es) | 2014-06-04 | 2015-06-04 | Derivados de difluoroetilpiridina como antagonistas del receptor nmda nr2b |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10030026B2 (es) |
| EP (1) | EP3152213B1 (es) |
| JP (1) | JP2017516836A (es) |
| CN (1) | CN106795163B (es) |
| AR (1) | AR100733A1 (es) |
| AU (1) | AU2015271719A1 (es) |
| CA (1) | CA2950285A1 (es) |
| TW (1) | TW201609741A (es) |
| WO (1) | WO2015187845A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201609741A (zh) | 2014-06-04 | 2016-03-16 | 盧郡控股（開曼）有限公司 | 作為ｎｒ２ｂ ｎｍｄａ受體拮抗劑之二氟乙基吡啶衍生物 |
| WO2016044323A1 (en) | 2014-09-15 | 2016-03-24 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
| EP3253761A4 (en) | 2015-02-04 | 2018-06-20 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists |
| MX380424B (es) | 2015-06-01 | 2025-03-12 | Rugen Holdings Cayman Ltd | Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b. |
| WO2018098128A1 (en) * | 2016-11-22 | 2018-05-31 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| BR112019010880A2 (pt) * | 2016-11-28 | 2019-10-01 | Praxis Precision Medicines, Inc. | compostos e seus métodos de uso |
| ES2897050T3 (es) * | 2017-12-08 | 2022-02-28 | Boehringer Ingelheim Int | Derivados de imidazopiridina y el uso de los mismos como medicamento |
| EP3870292A4 (en) | 2018-10-26 | 2022-11-09 | The Research Foundation for The State University of New York | COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE L-DOPA-INDUCED DYSKINESIA |
| WO2020171129A1 (ja) | 2019-02-20 | 2020-08-27 | 住友化学株式会社 | エーテル化合物及びそれを含有する有害節足動物防除組成物 |
| US12398143B2 (en) | 2019-06-04 | 2025-08-26 | Boehringer Ingelheim International Gmbh | Imidazopyrazine derivatives and the use thereof as medicament |
| CN112941036B (zh) * | 2021-02-08 | 2023-06-09 | 吉林惠康生物药业有限公司 | 一种提高狂犬病毒在人二倍体细胞中复制水平的方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA005974B1 (ru) * | 2001-02-23 | 2005-08-25 | Мерк Энд Ко., Инк. | N-замещенные неарильные гетероциклические антагонисты nmda/nr2b |
| CA2527093C (en) | 2003-06-04 | 2009-10-20 | Merck & Co., Inc. | 3-fluoro-piperidines as nmda/nr2b antagonists |
| US7592360B2 (en) | 2003-06-04 | 2009-09-22 | Merck & Co., Inc. | 3-fluoro-piperidines as NMDA/NR2B antagonists |
| WO2006113471A2 (en) | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl nmda/nr2b antagonists |
| WO2010015637A1 (en) | 2008-08-06 | 2010-02-11 | Novartis Ag | New antiviral modified nucleosides |
| PE20151436A1 (es) | 2013-01-29 | 2015-10-10 | Naurex Inc | Moduladores de receptores nmda de espiro-lactama y sus usos |
| TW201609741A (zh) | 2014-06-04 | 2016-03-16 | 盧郡控股（開曼）有限公司 | 作為ｎｒ２ｂ ｎｍｄａ受體拮抗劑之二氟乙基吡啶衍生物 |
| WO2016044323A1 (en) | 2014-09-15 | 2016-03-24 | Rugen Holdings (Cayman) Limited | Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists |
-
2015
- 2015-06-03 TW TW104118008A patent/TW201609741A/zh unknown
- 2015-06-03 WO PCT/US2015/034009 patent/WO2015187845A1/en not_active Ceased
- 2015-06-03 US US15/315,812 patent/US10030026B2/en not_active Expired - Fee Related
- 2015-06-03 CN CN201580029736.4A patent/CN106795163B/zh not_active Expired - Fee Related
- 2015-06-03 EP EP15745595.7A patent/EP3152213B1/en active Active
- 2015-06-03 AU AU2015271719A patent/AU2015271719A1/en not_active Abandoned
- 2015-06-03 JP JP2016571288A patent/JP2017516836A/ja active Pending
- 2015-06-03 CA CA2950285A patent/CA2950285A1/en not_active Abandoned
- 2015-06-04 AR ARP150101773A patent/AR100733A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2015271719A1 (en) | 2016-12-01 |
| EP3152213A1 (en) | 2017-04-12 |
| US20170101412A1 (en) | 2017-04-13 |
| US10030026B2 (en) | 2018-07-24 |
| JP2017516836A (ja) | 2017-06-22 |
| TW201609741A (zh) | 2016-03-16 |
| CN106795163B (zh) | 2019-07-30 |
| EP3152213B1 (en) | 2018-10-31 |
| CN106795163A (zh) | 2017-05-31 |
| CA2950285A1 (en) | 2015-12-10 |
| WO2015187845A1 (en) | 2015-12-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |