PE20170893A1 - N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostericos negativos de nr2b - Google Patents
N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostericos negativos de nr2bInfo
- Publication number
- PE20170893A1 PE20170893A1 PE2017000506A PE2017000506A PE20170893A1 PE 20170893 A1 PE20170893 A1 PE 20170893A1 PE 2017000506 A PE2017000506 A PE 2017000506A PE 2017000506 A PE2017000506 A PE 2017000506A PE 20170893 A1 PE20170893 A1 PE 20170893A1
- Authority
- PE
- Peru
- Prior art keywords
- alkylaryl
- oxyaril
- pirrol
- negative allosteric
- octahydro cyclopenta
- Prior art date
Links
- 102000034527 Retinoid X Receptors Human genes 0.000 title abstract 2
- 108010038912 Retinoid X Receptors Proteins 0.000 title abstract 2
- 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 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000020925 Bipolar disease Diseases 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000005346 substituted cycloalkyl group Chemical group 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
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- 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
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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)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Pain & Pain Management (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
Se refiere al N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol de formula general (I), donde L1 es -C(O)-, -C(O)-C1-C3alquilenilo, entre otros; R1 es cicloalquilo, arilo o heteroarilo opcionalmente sustituido; X es O, S, entre otros; Y e Y´ son H, halogeno, entre otros; L2 es un enlace, -(CH2)n-, entre otros; R2 es fenilo, naftilo, entre otros; n es 1, 2 o 3. Es un compuesto seleccionado: 2-((3aR, 5s, 6aS)-5-(3, 4-difluorofenoxi)hexahidrociclopenta[c]pirrol-2(1H)-il)-1-(4-hidroxifenil)etanona. Tambien se refiere a una composicion y una combinacion. Dicho compuesto es un modulador alosterico negativo de NR2B, siendo util en el tratamiento de trastorno bipolar, trastorno obsesivo, entre otros
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462056284P | 2014-09-26 | 2014-09-26 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20170893A1 true PE20170893A1 (es) | 2017-07-12 |
Family
ID=55581945
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2017000506A PE20170893A1 (es) | 2014-09-26 | 2015-09-23 | N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostericos negativos de nr2b |
Country Status (40)
Country | Link |
---|---|
US (4) | US10239835B2 (es) |
EP (4) | EP3683207B1 (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) | ES2956546T3 (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 (11)
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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 |
KR20200074164A (ko) | 2017-10-20 | 2020-06-24 | 반더빌트유니버시티 | 무스카린성 아세틸콜린 수용체 m4의 길항제 |
US11352344B2 (en) | 2017-10-31 | 2022-06-07 | 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 |
US11376258B2 (en) | 2019-06-04 | 2022-07-05 | Boehringer Ingelheim International Gmbh | Purine derivatives and the use thereof as medicament |
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 |
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 |
UY39688A (es) * | 2021-03-26 | 2022-10-31 | Novartis Ag | Moduladores Alostéricos Negativos Novedosos de 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 |
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CA2937616A1 (en) | 2014-03-26 | 2015-10-01 | 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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2015
- 2015-09-22 JO JOP/2015/0237A patent/JO3579B1/ar active
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active 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 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en unknown
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active IP Right Grant
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en active Application Filing
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 MX MX2017003940A patent/MX2017003940A/es active IP Right Grant
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
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- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
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- 2015-09-25 UY UY0001036326A patent/UY36326A/es active IP Right Grant
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- 2015-09-25 TW TW104131936A patent/TWI687407B/zh active
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2017
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2019
- 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
-
2022
- 2022-05-03 US US17/735,386 patent/US20220274925A1/en active Pending
-
2023
- 2023-01-19 JP JP2023006525A patent/JP2023052515A/ja active Pending
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