RU2012138710A - Модуляция nmda-рецептора со стабилизированной вторичной структурой и его применение - Google Patents
Модуляция nmda-рецептора со стабилизированной вторичной структурой и его применение Download PDFInfo
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- RU2012138710A RU2012138710A RU2012138710/04A RU2012138710A RU2012138710A RU 2012138710 A RU2012138710 A RU 2012138710A RU 2012138710/04 A RU2012138710/04 A RU 2012138710/04A RU 2012138710 A RU2012138710 A RU 2012138710A RU 2012138710 A RU2012138710 A RU 2012138710A
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- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 title 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 18
- 150000001204 N-oxides Chemical class 0.000 claims abstract 4
- 150000003839 salts Chemical class 0.000 claims abstract 4
- 208000000044 Amnesia Diseases 0.000 claims abstract 2
- 208000026139 Memory disease Diseases 0.000 claims abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 2
- 208000010877 cognitive disease Diseases 0.000 claims abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 2
- 208000035475 disorder Diseases 0.000 claims abstract 2
- 230000001771 impaired effect Effects 0.000 claims abstract 2
- 230000006984 memory degeneration Effects 0.000 claims abstract 2
- 206010027175 memory impairment Diseases 0.000 claims abstract 2
- 208000023060 memory loss Diseases 0.000 claims abstract 2
- 208000004296 neuralgia Diseases 0.000 claims abstract 2
- 208000021722 neuropathic pain Diseases 0.000 claims abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract 2
- 201000000980 schizophrenia Diseases 0.000 claims abstract 2
- 0 *C(CCC1)(C(N*)=O)N1C(C1(*)N(*)CCC1)=O Chemical compound *C(CCC1)(C(N*)=O)N1C(C1(*)N(*)CCC1)=O 0.000 description 2
- ORDNBIQZKXYGTM-UHFFFAOYSA-N CC(C(C=O)N)O Chemical compound CC(C(C=O)N)O ORDNBIQZKXYGTM-UHFFFAOYSA-N 0.000 description 1
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0815—Tripeptides with the first amino acid being basic
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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
- A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
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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
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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
- A61P25/04—Centrally acting analgesics, e.g. opioids
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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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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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
- A61P25/22—Anxiolytics
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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
- A61P25/24—Antidepressants
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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
- 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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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Investigating Or Analysing Biological Materials (AREA)
Abstract
1. Соединение, представленное формулой:где Rпредставляет собой Н;Rпредставляет собой бензил;Rпредставляет собойRпредставляет собойRпредставляет собой H или CH;Rпредставляет собой H или CH;и их стереоизомеры, N-оксиды или фармацевтически приемлемые соли.2. Соединение по п.1, где Rи Rпредставляют собой СН3. Соединение по п.1, где Rпредставляет собой СН, а Rпредставляет собой Н.4. Соединение, представленное формулойгде Rпредставляет собой Н;Rпредставляет собой Н;Rпредставляет собойRпредставляет собойRпредставляет собой CH, а Rпредставляет собой H или Rпредставляет собой Н, а Rпредставляет собой CH;и их стереоизомеры, N-оксиды или фармацевтически приемлемые соли.5. Соединение, представленное формулойили6. Способ лечения когнитивного расстройства, связанного с потерей памяти или нарушением способности к обучению, где указанный способ включает введение пациенту, нуждающемуся в этом, эффективного количества соединения по одному из пп.1-5.7. Фармацевтически приемлемая композиция, содержащая соединение по любому из пп.1-5, и фармацевтически приемлемый наполнитель.8. Способ устранения невропатической боли у пациента, нуждающегося в этом, где указанный способ включает введение эффективного количества соединения по любому из пп.1-5.9. Способ лечения депрессии, расстройства, ассоциированного с навязчивыми состояниями, или шизофрении у пациента, нуждающегося в этом, где указанный способ включает введение эффективного количества соединения по любому из пп.1-5.
Claims (9)
1. Соединение, представленное формулой:
где R4 представляет собой Н;
R1 представляет собой бензил;
R5 представляет собой
R6 представляет собой
R2 представляет собой H или CH3;
R3 представляет собой H или CH3;
и их стереоизомеры, N-оксиды или фармацевтически приемлемые соли.
2. Соединение по п.1, где R2 и R3 представляют собой СН3.
3. Соединение по п.1, где R2 представляет собой СН3, а R3 представляет собой Н.
4. Соединение, представленное формулой
где R4 представляет собой Н;
R1 представляет собой Н;
R5 представляет собой
R6 представляет собой
R2 представляет собой CH3, а R3 представляет собой H или R2 представляет собой Н, а R3 представляет собой CH3;
и их стереоизомеры, N-оксиды или фармацевтически приемлемые соли.
5. Соединение, представленное формулой
6. Способ лечения когнитивного расстройства, связанного с потерей памяти или нарушением способности к обучению, где указанный способ включает введение пациенту, нуждающемуся в этом, эффективного количества соединения по одному из пп.1-5.
7. Фармацевтически приемлемая композиция, содержащая соединение по любому из пп.1-5, и фармацевтически приемлемый наполнитель.
8. Способ устранения невропатической боли у пациента, нуждающегося в этом, где указанный способ включает введение эффективного количества соединения по любому из пп.1-5.
9. Способ лечения депрессии, расстройства, ассоциированного с навязчивыми состояниями, или шизофрении у пациента, нуждающегося в этом, где указанный способ включает введение эффективного количества соединения по любому из пп.1-5.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30347210P | 2010-02-11 | 2010-02-11 | |
| US61/303,472 | 2010-02-11 | ||
| PCT/US2011/024583 WO2011100585A1 (en) | 2010-02-11 | 2011-02-11 | Secondary structure stabilized nmda receptor modulators and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2012138710A true RU2012138710A (ru) | 2014-03-20 |
| RU2566821C2 RU2566821C2 (ru) | 2015-10-27 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2012138710/04A RU2566821C2 (ru) | 2010-02-11 | 2011-02-11 | Модулятор nmda-рецептора со стабилизированной вторичной структурой и его применение |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9101612B2 (ru) |
| EP (1) | EP2542254B1 (ru) |
| JP (4) | JP5928828B2 (ru) |
| CN (2) | CN105037492A (ru) |
| AU (1) | AU2011215704B2 (ru) |
| BR (1) | BR112012020142A2 (ru) |
| CA (1) | CA2789331C (ru) |
| ES (1) | ES2706063T3 (ru) |
| IL (1) | IL221400A (ru) |
| MX (1) | MX2012009388A (ru) |
| RU (1) | RU2566821C2 (ru) |
| SG (3) | SG183265A1 (ru) |
| WO (1) | WO2011100585A1 (ru) |
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| KR20150110787A (ko) | 2013-01-29 | 2015-10-02 | 노렉스, 인크. | 스피로-락탐 nmda 수용체 조절인자 및 그의 용도 |
| KR20150110586A (ko) | 2013-01-29 | 2015-10-02 | 노렉스, 인크. | 스피로-락탐 nmda 수용체 조절인자 및 그의 용도 |
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2011
- 2011-02-11 CN CN201510222007.2A patent/CN105037492A/zh active Pending
- 2011-02-11 CN CN2011800146633A patent/CN102933226A/zh active Pending
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- 2011-02-11 SG SG2012059358A patent/SG183265A1/en unknown
- 2011-02-11 JP JP2012553046A patent/JP5928828B2/ja active Active
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- 2011-02-11 SG SG10201811584RA patent/SG10201811584RA/en unknown
- 2011-02-11 WO PCT/US2011/024583 patent/WO2011100585A1/en not_active Ceased
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| CN102933226A (zh) | 2013-02-13 |
| JP5928828B2 (ja) | 2016-06-01 |
| US9593145B2 (en) | 2017-03-14 |
| IL221400A (en) | 2016-07-31 |
| ES2706063T3 (es) | 2019-03-27 |
| JP6328169B2 (ja) | 2018-05-23 |
| US9101612B2 (en) | 2015-08-11 |
| WO2011100585A1 (en) | 2011-08-18 |
| CA2789331C (en) | 2017-11-07 |
| JP2013519683A (ja) | 2013-05-30 |
| SG10201501050RA (en) | 2015-04-29 |
| RU2566821C2 (ru) | 2015-10-27 |
| IL221400A0 (en) | 2012-10-31 |
| EP2542254A1 (en) | 2013-01-09 |
| US20160115197A1 (en) | 2016-04-28 |
| JP2016185948A (ja) | 2016-10-27 |
| AU2011215704A1 (en) | 2012-08-30 |
| EP2542254A4 (en) | 2013-07-10 |
| MX2012009388A (es) | 2012-10-01 |
| US20130053325A1 (en) | 2013-02-28 |
| SG10201811584RA (en) | 2019-01-30 |
| AU2011215704B2 (en) | 2015-07-23 |
| BR112012020142A2 (pt) | 2020-08-18 |
| EP2542254B1 (en) | 2018-09-26 |
| CA2789331A1 (en) | 2011-08-18 |
| CN105037492A (zh) | 2015-11-11 |
| JP2020117510A (ja) | 2020-08-06 |
| SG183265A1 (en) | 2012-09-27 |
| JP2018119004A (ja) | 2018-08-02 |
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