MX374657B - Moduladores alostéricos negativos de nr2b de n-alquilaril-5-oxiaril-octahidro-ciclopenta [c] pirrol. - Google Patents
Moduladores alostéricos negativos de nr2b de n-alquilaril-5-oxiaril-octahidro-ciclopenta [c] pirrol.Info
- Publication number
- MX374657B MX374657B MX2017003940A MX2017003940A MX374657B MX 374657 B MX374657 B MX 374657B MX 2017003940 A MX2017003940 A MX 2017003940A MX 2017003940 A MX2017003940 A MX 2017003940A MX 374657 B MX374657 B MX 374657B
- Authority
- MX
- Mexico
- Prior art keywords
- oxyaryl
- alkylaryl
- nr2b
- allosteric modulators
- negative allosteric
- Prior art date
Links
- 229940126662 negative allosteric modulator Drugs 0.000 title abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 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
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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 Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se refiere a moduladores alostéricos negativos de los receptores NR2B de N-alquilaril-5-oxiaril-octadihidrociclopent[c]pirrol que son útiles en el tratamiento de enfermedades neurológicas, que tienen la fórmula I: (ver Fórmula) en donde R1, R2, L1, L2, X, Y y Y' se describen en la presente. En un aspecto se describen los compuestos de fórmula I y las sales farmacéuticamente aceptables, profármacos, solvatos, hidratos, tautómeros o estereoisómeros de los mismos, en donde L1 es alquilo de C1-C5 lineal o ramificado, sustituido opcionalmente con uno o más sustituyentes seleccionados del grupo que consiste en OH, OR10, NH2, NHR10 y N(R10)(R10'), siempre que no más de un oxígeno o nitrógeno esté unido a cualquier carbono.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462056284P | 2014-09-26 | 2014-09-26 | |
| PCT/US2015/051694 WO2016049165A1 (en) | 2014-09-26 | 2015-09-23 | N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2017003940A MX2017003940A (es) | 2018-03-01 |
| MX374657B true MX374657B (es) | 2025-03-06 |
Family
ID=55581945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017003940A MX374657B (es) | 2014-09-26 | 2015-09-23 | Moduladores alostéricos negativos de nr2b de n-alquilaril-5-oxiaril-octahidro-ciclopenta [c] pirrol. |
Country Status (40)
| Country | Link |
|---|---|
| US (4) | US10239835B2 (es) |
| EP (4) | EP4282412A3 (es) |
| JP (5) | JP6473227B2 (es) |
| KR (1) | KR102479356B1 (es) |
| CN (1) | CN106795111B (es) |
| AP (1) | AP2017009832A0 (es) |
| AR (1) | AR103199A1 (es) |
| AU (1) | AU2015320721B2 (es) |
| BR (1) | BR112017006093B1 (es) |
| CA (1) | CA2962569C (es) |
| CL (1) | CL2017000474A1 (es) |
| CO (1) | CO2017002494A2 (es) |
| CR (1) | CR20170114A (es) |
| CU (1) | CU24482B1 (es) |
| CY (1) | CY1123533T1 (es) |
| DK (1) | DK3197868T3 (es) |
| EA (1) | EA034937B1 (es) |
| EC (1) | ECSP17025302A (es) |
| ES (3) | ES2911004T3 (es) |
| GT (1) | GT201700062A (es) |
| HR (1) | HRP20200959T1 (es) |
| HU (1) | HUE049698T2 (es) |
| IL (1) | IL250909B (es) |
| JO (1) | JO3579B1 (es) |
| LT (1) | LT3197868T (es) |
| MX (1) | MX374657B (es) |
| MY (1) | MY182342A (es) |
| NZ (1) | NZ729569A (es) |
| PE (1) | PE20170893A1 (es) |
| PH (1) | PH12017500513A1 (es) |
| PL (1) | PL3197868T3 (es) |
| PT (1) | PT3197868T (es) |
| RS (1) | RS60497B1 (es) |
| SG (1) | SG11201702023QA (es) |
| SI (1) | SI3197868T1 (es) |
| TN (1) | TN2017000076A1 (es) |
| TW (1) | TWI687407B (es) |
| UY (1) | UY36326A (es) |
| WO (1) | WO2016049165A1 (es) |
| ZA (1) | ZA201701061B (es) |
Families Citing this family (16)
| 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 |
| CN118063442A (zh) | 2017-10-20 | 2024-05-24 | 范德比尔特大学 | 毒蕈碱性乙酰胆碱受体m4的拮抗剂 |
| KR20200081424A (ko) | 2017-10-31 | 2020-07-07 | 반더빌트유니버시티 | 무스카린성 아세틸콜린 수용체 m4의 길항제 |
| 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 |
| CA3091805A1 (en) | 2018-03-05 | 2019-09-12 | Arcus Biosciences, Inc. | Arginase inhibitors |
| EP3980420B1 (en) | 2019-06-04 | 2023-04-19 | Boehringer Ingelheim International GmbH | Imidazopyrazine derivatives and the use thereof as medicament |
| 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 |
| 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 |
| KR20230116865A (ko) * | 2020-12-04 | 2023-08-04 | 노파르티스 아게 | 우울증의 치료를 위한 nr2b-nmda 수용체 nam의 투여요법 |
| 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 |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| EP4313042A4 (en) * | 2021-03-26 | 2025-01-15 | Novartis AG | NEW CYCLOPENTA[C PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B |
| EP4313041A4 (en) * | 2021-03-26 | 2025-01-15 | Novartis AG | NEW CYCLOPENTAL[C PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B |
| EP4531851A1 (en) | 2022-06-02 | 2025-04-09 | Novartis AG | Subcutaneous administration of onfasprodil and dosing methods for use in the treatment of depression disorders |
| EP4649143A1 (en) | 2023-01-12 | 2025-11-19 | Novartis AG | Engineered ketoreductase polypeptides |
| WO2025120013A1 (en) | 2023-12-06 | 2025-06-12 | Novartis Ag | Compositions and methods for treating depression disorders |
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| FR2945534B1 (fr) * | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| MX2012007935A (es) | 2010-01-07 | 2012-08-15 | Du Pont | Compuestos heterociclicos fungicidas. |
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| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
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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 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
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