EA201790713A1 - N-АЛКИЛАРИЛ-5-ОКСОАРИЛОКТАГИДРОЦИКЛОПЕНТА[c]ПИРРОЛЬНЫЕ НЕГАТИВНЫЕ АЛОСТЕРИЧЕСКИЕ МОДУЛЯТОРЫ NR2B - Google Patents
N-АЛКИЛАРИЛ-5-ОКСОАРИЛОКТАГИДРОЦИКЛОПЕНТА[c]ПИРРОЛЬНЫЕ НЕГАТИВНЫЕ АЛОСТЕРИЧЕСКИЕ МОДУЛЯТОРЫ NR2BInfo
- Publication number
- EA201790713A1 EA201790713A1 EA201790713A EA201790713A EA201790713A1 EA 201790713 A1 EA201790713 A1 EA 201790713A1 EA 201790713 A EA201790713 A EA 201790713A EA 201790713 A EA201790713 A EA 201790713A EA 201790713 A1 EA201790713 A1 EA 201790713A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- nr2b
- modulators
- oxyoryloktaghydro
- alkilaril
- alosteric
- 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
- NNHOUIKFCCIVCI-UHFFFAOYSA-N cyclopenta[c]pyrrole Chemical compound N1=CC2=CC=CC2=C1 NNHOUIKFCCIVCI-UHFFFAOYSA-N 0.000 title 1
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 102000007399 Nuclear hormone receptor Human genes 0.000 abstract 1
- 108020005497 Nuclear hormone receptor Proteins 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 229940126662 negative allosteric modulator Drugs 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 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
- 239000000126 substance Substances 0.000 abstract 1
- 125000001424 substituent 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
-
- 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)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (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)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Изобретение относится к N-алкиларил-5-оксиарилоктадигидроциклопент[с]пиррольным негативным аллостерическим модуляторам рецепторов NR2B, применимым для лечения неврологических заболеваний, описывающихся формулой Iв которой R,R, L,L, X, Y и Y' описаны в настоящем изобретении. В одном объекте описаны соединения формулы I и их фармацевтически приемлемые соли, пролекарства, сольваты, гидраты, таутомеры или стереоизомеры, в которой Lозначает линейный или разветвленный С-С-алкил, необязательно замещенный одним или большим количеством заместителей, выбранных из группы, включающей ОН, OR, NH, NHRи N(R)(R') при условии, что к любому атому углерода присоединен не более чем один атом кислорода или азота.
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 |
---|---|
EA201790713A1 true EA201790713A1 (ru) | 2017-07-31 |
EA034937B1 EA034937B1 (ru) | 2020-04-08 |
Family
ID=55581945
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201790713A EA034937B1 (ru) | 2014-09-26 | 2015-09-23 | N-алкиларил-5-оксоарилоктагидроциклопента[c]пиррольные негативные алостерические модуляторы nr2b |
Country Status (40)
Country | Link |
---|---|
US (4) | US10239835B2 (ru) |
EP (4) | EP4282412A3 (ru) |
JP (4) | JP6473227B2 (ru) |
KR (1) | KR102479356B1 (ru) |
CN (1) | CN106795111B (ru) |
AP (1) | AP2017009832A0 (ru) |
AR (1) | AR103199A1 (ru) |
AU (1) | AU2015320721B2 (ru) |
BR (1) | BR112017006093B1 (ru) |
CA (1) | CA2962569C (ru) |
CL (1) | CL2017000474A1 (ru) |
CO (1) | CO2017002494A2 (ru) |
CR (1) | CR20170114A (ru) |
CU (1) | CU24482B1 (ru) |
CY (1) | CY1123533T1 (ru) |
DK (1) | DK3197868T3 (ru) |
EA (1) | EA034937B1 (ru) |
EC (1) | ECSP17025302A (ru) |
ES (3) | ES2956546T3 (ru) |
GT (1) | GT201700062A (ru) |
HR (1) | HRP20200959T1 (ru) |
HU (1) | HUE049698T2 (ru) |
IL (1) | IL250909B (ru) |
JO (1) | JO3579B1 (ru) |
LT (1) | LT3197868T (ru) |
MX (1) | MX2017003940A (ru) |
MY (1) | MY182342A (ru) |
NZ (1) | NZ729569A (ru) |
PE (1) | PE20170893A1 (ru) |
PH (1) | PH12017500513A1 (ru) |
PL (1) | PL3197868T3 (ru) |
PT (1) | PT3197868T (ru) |
RS (1) | RS60497B1 (ru) |
SG (1) | SG11201702023QA (ru) |
SI (1) | SI3197868T1 (ru) |
TN (1) | TN2017000076A1 (ru) |
TW (1) | TWI687407B (ru) |
UY (1) | UY36326A (ru) |
WO (1) | WO2016049165A1 (ru) |
ZA (1) | ZA201701061B (ru) |
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 |
EP3697759A4 (en) | 2017-10-20 | 2021-05-12 | Vanderbilt University | MUSCARINIAN ACETYLCHOLINE RECEPTOR ANTAGONISTS M4 |
KR20200081424A (ko) | 2017-10-31 | 2020-07-07 | 반더빌트유니버시티 | 무스카린성 아세틸콜린 수용체 m4의 길항제 |
AU2019216492A1 (en) | 2018-02-02 | 2020-08-20 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
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 |
TW202237103A (zh) | 2020-12-04 | 2022-10-01 | 瑞士商諾華公司 | 用於治療抑鬱症的nr2b-nmda受體nam之劑量方案 |
JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
JP2024512066A (ja) * | 2021-03-26 | 2024-03-18 | ノバルティス アーゲー | NR2Bの負のアロステリックモジュレーターである新規なシクロペンタ[c]ピロール |
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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JP2008507543A (ja) | 2004-07-22 | 2008-03-13 | グラクソ グループ リミテッド | 抗細菌剤 |
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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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CN105916843B (zh) * | 2013-09-26 | 2019-09-20 | 科登特治疗公司 | 八氢环戊二烯并[c]吡咯类选择性NR2B负性调节剂 |
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 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en active Application Filing
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 MX MX2017003940A patent/MX2017003940A/es active IP Right Grant
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en unknown
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
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