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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- 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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- 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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- 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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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- 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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- 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
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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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| Application Number | Title | Priority Date | Filing Date |
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| RU2012138710/04A RU2566821C2 (ru) | 2010-02-11 | 2011-02-11 | Модулятор nmda-рецептора со стабилизированной вторичной структурой и его применение |
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| Country | Link |
|---|---|
| US (2) | US9101612B2 (ru) |
| EP (1) | EP2542254B1 (ru) |
| JP (4) | JP5928828B2 (ru) |
| CN (2) | CN102933226A (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) | SG10201811584RA (ru) |
| WO (1) | WO2011100585A1 (ru) |
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| EP2331571B1 (en) | 2008-09-18 | 2015-08-26 | Northwestern University | Nmda receptor modulators and uses thereof |
| US8951968B2 (en) | 2009-10-05 | 2015-02-10 | Northwestern University | Methods of treating depression and other related diseases |
| KR101692275B1 (ko) | 2010-02-11 | 2017-01-04 | 노오쓰웨스턴 유니버시티 | ２차 구조 안정화된 ｎｍｄａ 수용체 조절제 및 그의 용도 |
| SG10201811584RA (en) | 2010-02-11 | 2019-01-30 | Univ Northwestern | Secondary Structure Stabilized NMDA Receptor Modulators And Uses Thereof |
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| CA2898863A1 (en) | 2013-01-29 | 2014-08-07 | Naurex, Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
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| EA201591404A1 (ru) | 2013-01-29 | 2016-01-29 | Аптиникс Инк. | Спиролактамные модуляторы рецептора nmda и их применение |
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| AU2011215704B2 (en) | 2015-07-23 |
| EP2542254A1 (en) | 2013-01-09 |
| CA2789331A1 (en) | 2011-08-18 |
| IL221400A0 (en) | 2012-10-31 |
| IL221400A (en) | 2016-07-31 |
| JP6328169B2 (ja) | 2018-05-23 |
| SG10201501050RA (en) | 2015-04-29 |
| CN102933226A (zh) | 2013-02-13 |
| JP2013519683A (ja) | 2013-05-30 |
| WO2011100585A1 (en) | 2011-08-18 |
| JP2018119004A (ja) | 2018-08-02 |
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| RU2566821C2 (ru) | 2015-10-27 |
| BR112012020142A2 (pt) | 2020-08-18 |
| SG183265A1 (en) | 2012-09-27 |
| ES2706063T3 (es) | 2019-03-27 |
| MX2012009388A (es) | 2012-10-01 |
| CA2789331C (en) | 2017-11-07 |
| CN105037492A (zh) | 2015-11-11 |
| JP2020117510A (ja) | 2020-08-06 |
| US9101612B2 (en) | 2015-08-11 |
| US20160115197A1 (en) | 2016-04-28 |
| US20130053325A1 (en) | 2013-02-28 |
| AU2011215704A1 (en) | 2012-08-30 |
| JP5928828B2 (ja) | 2016-06-01 |
| US9593145B2 (en) | 2017-03-14 |
| EP2542254A4 (en) | 2013-07-10 |
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