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
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) | EP3974420B1 (ar) |
| JP (4) | 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) | MX2017003940A (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) |
Families Citing this family (11)
| 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 |
| CA3079617A1 (en) | 2017-10-20 | 2019-04-25 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| AU2018360581A1 (en) | 2017-10-31 | 2020-06-11 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| CA3090130A1 (en) | 2018-02-02 | 2019-08-08 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| CN113950478B (zh) * | 2019-06-04 | 2024-02-02 | 勃林格殷格翰国际有限公司 | 作为nr2b负向调节剂的嘌呤衍生物及其作为药物的用途，特别是用于治疗抑郁病症 |
| 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 |
| AU2021390209A1 (en) | 2020-12-04 | 2023-06-22 | Novartis Ag | Dosage regimen for a nr2b-nmda receptor nam for the treatment of depression |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| EP4313042A1 (en) * | 2021-03-26 | 2024-02-07 | Novartis AG | Novel cyclopenta[c]pyrrol negative allosteric modulators of nr2b |
| KR20230160906A (ko) * | 2021-03-26 | 2023-11-24 | 노파르티스 아게 | NR2B의 신규 시클로펜타[c]피롤 음성 알로스테릭 조정제 |
| WO2023233357A1 (en) | 2022-06-02 | 2023-12-07 | Novartis Ag | Subcutaneous administration of onfasprodil and dosing methods for use in the treatment of depression disorders |
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| DE4341403A1 (de) | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung |
| US5726172A (en) * | 1996-01-16 | 1998-03-10 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| US6369076B1 (en) * | 1999-10-29 | 2002-04-09 | Merck & Co. Inc. | 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists |
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| US7696241B2 (en) | 2004-03-04 | 2010-04-13 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
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| FR2945533B1 (fr) * | 2009-05-12 | 2011-05-27 | Sanofi Aventis | Derives de cyclopenta°c!pyrrolyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
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| HUE046820T2 (hu) | 2014-03-26 | 2020-03-30 | Hoffmann La Roche | Biciklusos vegyületek autotaxin (ATX) és lizofoszfatidsav (LPA) termelésgátlókként |
| 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 WO PCT/US2015/051694 patent/WO2016049165A1/en active Application Filing
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active IP Right Grant
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en unknown
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 MX MX2017003940A patent/MX2017003940A/es active IP Right Grant
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-25 AR ARP150103084A patent/AR103199A1/es active IP Right Grant
- 2015-09-25 UY UY0001036326A patent/UY36326A/es active IP Right Grant
- 2015-09-25 TW TW104131936A patent/TWI687407B/zh active
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2017
- 2017-02-13 ZA ZA2017/01061A patent/ZA201701061B/en unknown
- 2017-02-28 CL CL2017000474A patent/CL2017000474A1/es unknown
- 2017-03-02 IL IL250909A patent/IL250909B/en active IP Right Grant
- 2017-03-15 CO CONC2017/0002494A patent/CO2017002494A2/es unknown
- 2017-03-17 PH PH12017500513A patent/PH12017500513A1/en unknown
- 2017-03-24 GT GT201700062A patent/GT201700062A/es unknown
- 2017-04-24 EC ECIEPI201725302A patent/ECSP17025302A/es unknown
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2019
- 2019-01-23 US US16/255,500 patent/US10781174B2/en active Active
- 2019-01-23 JP JP2019008873A patent/JP6772307B2/ja active Active
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2020
- 2020-06-15 CY CY20201100542T patent/CY1123533T1/el unknown
- 2020-06-17 HR HRP20200959TT patent/HRP20200959T1/hr unknown
- 2020-08-12 US US16/991,684 patent/US20200369610A1/en not_active Abandoned
- 2020-09-30 JP JP2020166129A patent/JP7216060B2/ja active Active
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2022
- 2022-05-03 US US17/735,386 patent/US20220274925A1/en active Pending
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2023
- 2023-01-19 JP JP2023006525A patent/JP2023052515A/ja active Pending
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