AR103199A1 - N-alquilaril-5-oxiaril-octahidrociclopenta[c]pirrol moduladores alóstericos negativos de nr2b - Google Patents
N-alquilaril-5-oxiaril-octahidrociclopenta[c]pirrol moduladores alóstericos negativos de nr2bInfo
- Publication number
- AR103199A1 AR103199A1 ARP150103084A ARP150103084A AR103199A1 AR 103199 A1 AR103199 A1 AR 103199A1 AR P150103084 A ARP150103084 A AR P150103084A AR P150103084 A ARP150103084 A AR P150103084A AR 103199 A1 AR103199 A1 AR 103199A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- optionally substituted
- substituents selected
- alkylenyl
- Prior art date
Links
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 1
- 102000034527 Retinoid X Receptors Human genes 0.000 title 1
- 108010038912 Retinoid X Receptors Proteins 0.000 title 1
- 229940126662 negative allosteric modulator Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000005466 alkylenyl group Chemical group 0.000 abstract 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- 101100240516 Caenorhabditis elegans nhr-10 gene Proteins 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 150000001768 cations Chemical class 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 239000002184 metal Substances 0.000 abstract 2
- 229910052751 metal Inorganic materials 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 101100509371 Arabidopsis thaliana CHR11 gene Proteins 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 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
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- 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)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicación 1: Un compuesto de formula (1), o una sal farmacéuticamente aceptable, profármaco, solvato, hidrato, tautómero o esteroisómero del mismo, caracterizado porque: L¹ es alquilo C₁₋₅ lineal o ramificado opcionalmente sustituido con uno o más sustituyentes seleccionados del grupo que consiste en OH, OR¹⁰, NH₂, NHR¹⁰, y N(R¹⁰)(R¹⁰) que no estén unidos más de uno de oxígeno o de nitrógeno a cualquier carbono; o, L¹ está seleccionado de un grupo que consiste en -C(O)-, -C(O)-C₁₋₃ alquilenilo-, -C(O)O-C₁₋₃ alquilenilo-, -S(O)₂-, -S(O)₂NH-, -C(O)NH-, -C(O)NR¹⁰-, y un enlace; cada R¹⁰ y R¹⁰ son independientemente seleccionados a partir del grupo H; los alquilos C₁₋₆ pueden ser opcionalmente sustituidos con uno o más sustituyentes seleccionados del grupo que consiste en OH, O-C₁₋₅ alquilo, OPO₃⁻²M₂, OP(O)(OH)₂, OC(O)alquilo y OC(O)O-alquilo donde M es un catión metálico monovalente; y el cicloalquilo puede ser opcionalmente sustituido por uno o más sustituyentes seleccionados del grupo OH y alquilos O-C₁₋₅ mientras no más de un oxígeno esté adherido a alguna molécula de carbono; o R¹⁰ y R¹⁰ puede formar un heterociclo junto con el nitrógeno al cual están unidos; R¹ es un cicloalquilo, arilo o heteroarilo, que puede ser sustituido opcionalmente con uno o mas sustituyentes seleccionados del grupo que consiste en OH, CN, halógeno, alquilarilos C₁₋₆, alquilarilos O-C₁₋₆, O-R¹⁰, OPO₃⁻²M₂, OP(O)(OH)₂, SH, S-R¹⁰, alquilos C₁₋₅, alquilos ramificados, NH₂, NHR¹⁰, NHS(O)₂R¹⁰, N(R¹⁰)(NR¹⁰), y NHCOR¹⁰ donde M es un catión metálico monovalente; X es seleccionado a partir de O, S, -S(O)-, y -S(O)₂; Y e Y son independientemente H, halógeno o alquilo C₁₋₅; L² es un enlace, -(CH₂)ₙ- o -(CHR¹¹)ₙ; cada R¹¹ es seleccionado independientemente a partir de un grupo que consiste en H, alquilenilos C₁₋₅, alquilenilo CO-C₁₋₅, y alquilenilo-CO; R² es un fenilo, naftilo, heteroarilo o heteroarilo bicíclico, de los cuales pueden ser sustituidos opcionalmente con uno o más sustituyentes seleccionados de un grupo que consiste de halógeno, hidróxido (OH), alquilo C₁₋₆, OR¹⁰, CN, NH₂, NHR¹⁰, N(R¹⁰)(R¹⁰), -nitro, SH, SR¹⁰, SOR¹⁰, SO₂R¹⁰, SO₂NHR¹⁰, SO₂N(R¹⁰)(R¹⁰), CONH₂, CONR¹⁰, y CON(R¹⁰)(R¹⁰); y n es 1, 2 ó 3.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462056284P | 2014-09-26 | 2014-09-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR103199A1 true AR103199A1 (es) | 2017-04-26 |
Family
ID=55581945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150103084A AR103199A1 (es) | 2014-09-26 | 2015-09-25 | N-alquilaril-5-oxiaril-octahidrociclopenta[c]pirrol moduladores alóstericos negativos de nr2b |
Country Status (40)
| Country | Link |
|---|---|
| US (4) | US10239835B2 (es) |
| EP (4) | EP3197868B1 (es) |
| JP (4) | 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) | ES2791327T3 (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) | MX2017003940A (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 (13)
| 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 |
| EP3703680B1 (en) | 2017-10-31 | 2024-05-15 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| AU2019216492A1 (en) | 2018-02-02 | 2020-08-20 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
| EA202092086A1 (ru) | 2018-03-05 | 2021-02-09 | Аркус Байосайенсиз, Инк. | Ингибиторы аргиназы |
| 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 |
| IL303357A (en) | 2020-12-04 | 2023-08-01 | Novartis Ag | Dosing regimen for the 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 |
| US20240199576A1 (en) * | 2021-03-26 | 2024-06-20 | Novartis Ag | Novel cyclopenta[c]pyrrol negative allosteric modulators of nr2b |
| CR20230458A (es) * | 2021-03-26 | 2023-10-27 | Novartis Ag | Nuevos moduladores alostéricos negativos ciclopenta[c]pirrol de NR2B |
| 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 |
| WO2024150146A1 (en) | 2023-01-12 | 2024-07-18 | Novartis Ag | Engineered ketoreductase polypeptides |
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| EP3036221B1 (en) * | 2013-09-26 | 2018-11-07 | Cadent Therapeutics, Inc. | Selective octahydro-cyclopenta[c]pyrrole negative modulators of nr2b |
| AU2015238537B2 (en) | 2014-03-26 | 2019-08-01 | F. Hoffmann-La Roche Ag | Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors |
| 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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