JO3579B1 - مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول - Google Patents
مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرولInfo
- Publication number
- JO3579B1 JO3579B1 JOP/2015/0237A JOP20150237A JO3579B1 JO 3579 B1 JO3579 B1 JO 3579B1 JO P20150237 A JOP20150237 A JO P20150237A JO 3579 B1 JO3579 B1 JO 3579B1
- Authority
- JO
- Jordan
- Prior art keywords
- oxyaryl
- alkylaryl
- nr2b
- allosteric modulators
- octahydro
- Prior art date
Links
- 229940126662 negative allosteric modulator Drugs 0.000 title abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 102000034527 Retinoid X Receptors Human genes 0.000 abstract 1
- 108010038912 Retinoid X Receptors Proteins 0.000 abstract 1
Classifications
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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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P25/22—Anxiolytics
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
يتعلق الاختراع الحالي بمُعدِلات تفاغرية سالبة لمستقبلات <span dir="LTR">NR2B</span> من المركب <span dir="LTR">N</span>-ألكيل أريل-5- أوكسي أريل-ثامن هيدرو-خماسي الحلقة [<span dir="LTR">c</span>] بيرول مفيدة في علاج الأمراض العصبية ذات الصيغة <span dir="LTR">I</span>: <span dir="LTR">(I)</span> <span dir="LTR"><img src="file:///C:/Users/Darwish.Q/AppData/Local/Temp/msohtmlclip1/01/clip_image002.gif" /></span> حيث <span dir="LTR">R<sub>1</sub></span>، <span dir="LTR">R<sub>2</sub></span>، <span dir="LTR">L<sub>1</sub></span>، <span dir="LTR">L<sub>2</sub></span>، <span dir="LTR">X</span>، <span dir="LTR">Y</span>، و <span dir="LTR">Y`</span> كما وصفت في الوصف التفصيلي.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462056284P | 2014-09-26 | 2014-09-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3579B1 true JO3579B1 (ar) | 2020-07-05 |
Family
ID=55581945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2015/0237A JO3579B1 (ar) | 2014-09-26 | 2015-09-22 | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
Country Status (40)
| Country | Link |
|---|---|
| US (4) | US10239835B2 (ar) |
| EP (4) | EP3683207B1 (ar) |
| JP (5) | JP6473227B2 (ar) |
| KR (1) | KR102479356B1 (ar) |
| CN (1) | CN106795111B (ar) |
| AP (1) | AP2017009832A0 (ar) |
| AR (1) | AR103199A1 (ar) |
| AU (1) | AU2015320721B2 (ar) |
| BR (1) | BR112017006093B1 (ar) |
| CA (1) | CA2962569C (ar) |
| CL (1) | CL2017000474A1 (ar) |
| CO (1) | CO2017002494A2 (ar) |
| CR (1) | CR20170114A (ar) |
| CU (1) | CU24482B1 (ar) |
| CY (1) | CY1123533T1 (ar) |
| DK (1) | DK3197868T3 (ar) |
| EA (1) | EA034937B1 (ar) |
| EC (1) | ECSP17025302A (ar) |
| ES (3) | ES2791327T3 (ar) |
| GT (1) | GT201700062A (ar) |
| HR (1) | HRP20200959T1 (ar) |
| HU (1) | HUE049698T2 (ar) |
| IL (1) | IL250909B (ar) |
| JO (1) | JO3579B1 (ar) |
| LT (1) | LT3197868T (ar) |
| MX (1) | MX374657B (ar) |
| MY (1) | MY182342A (ar) |
| NZ (1) | NZ729569A (ar) |
| PE (1) | PE20170893A1 (ar) |
| PH (1) | PH12017500513A1 (ar) |
| PL (1) | PL3197868T3 (ar) |
| PT (1) | PT3197868T (ar) |
| RS (1) | RS60497B1 (ar) |
| SG (1) | SG11201702023QA (ar) |
| SI (1) | SI3197868T1 (ar) |
| TN (1) | TN2017000076A1 (ar) |
| TW (1) | TWI687407B (ar) |
| UY (1) | UY36326A (ar) |
| WO (1) | WO2016049165A1 (ar) |
| ZA (1) | ZA201701061B (ar) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3579B1 (ar) * | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
| US12600726B2 (en) | 2017-07-12 | 2026-04-14 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| IL310346A (en) | 2017-10-20 | 2024-03-01 | Univ Vanderbilt | Muscarinic acetylcholine M4 receptor antagonists |
| AU2018360581A1 (en) | 2017-10-31 | 2020-06-11 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| CN111788182B (zh) | 2018-02-02 | 2023-09-26 | 范德堡大学 | 毒蕈碱性乙酰胆碱受体m4的拮抗剂 |
| CN111818928A (zh) | 2018-03-05 | 2020-10-23 | 艾库斯生物科学有限公司 | 精氨酸酶抑制剂 |
| TW202112378A (zh) * | 2019-06-04 | 2021-04-01 | 德商百靈佳殷格翰國際股份有限公司 | 嘌呤衍生物及其作為藥物之用途 |
| CN113906033B (zh) | 2019-06-04 | 2024-04-02 | 勃林格殷格翰国际有限公司 | 咪唑并吡嗪衍生物及其作为药剂的用途 |
| CN111481543A (zh) * | 2020-05-21 | 2020-08-04 | 苏州健雄职业技术学院 | Nr2b负变构调节剂联合gaba受体调节剂在制备治疗阿尔兹海默症的药物中的用途 |
| CN116744922A (zh) * | 2020-12-04 | 2023-09-12 | 诺华股份有限公司 | Nr2b-nmda受体nam在治疗抑郁症中的剂量方案 |
| MX2023006567A (es) * | 2020-12-04 | 2023-06-16 | Novartis Ag | Regimen de dosificacion para un nam del receptor nr2b-nmda para el tratamiento de la depresion. |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| CN117120053A (zh) * | 2021-03-26 | 2023-11-24 | 诺华股份有限公司 | 新的环戊二烯并[c]吡咯NR2B负变构调节剂 |
| EP4313041A4 (en) * | 2021-03-26 | 2025-01-15 | Novartis AG | NEW CYCLOPENTAL[C PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B |
| AU2023278502A1 (en) | 2022-06-02 | 2025-01-02 | Novartis Ag | Subcutaneous administration of onfasprodil and dosing methods for use in the treatment of depression disorders |
| IL322082A (en) | 2023-01-12 | 2025-09-01 | Novartis Ag | Engineered ketoreductase polypeptides |
| TW202539663A (zh) | 2023-12-06 | 2025-10-16 | 瑞士商諾華公司 | 用於治療抑鬱障礙之組成物和方法 |
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| JO3579B1 (ar) * | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
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2015
- 2015-09-22 JO JOP/2015/0237A patent/JO3579B1/ar active
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en not_active IP Right Cessation
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en not_active Ceased
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
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