RU2499598C2 - Способы лечения нарушений с применением селективного антагониста nr2b-подтипа nmda рецепторов - Google Patents
Способы лечения нарушений с применением селективного антагониста nr2b-подтипа nmda рецепторов Download PDFInfo
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- RU2499598C2 RU2499598C2 RU2010143864/15A RU2010143864A RU2499598C2 RU 2499598 C2 RU2499598 C2 RU 2499598C2 RU 2010143864/15 A RU2010143864/15 A RU 2010143864/15A RU 2010143864 A RU2010143864 A RU 2010143864A RU 2499598 C2 RU2499598 C2 RU 2499598C2
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4008708P | 2008-03-27 | 2008-03-27 | |
| US61/040,087 | 2008-03-27 | ||
| PCT/EP2009/002241 WO2009118187A1 (en) | 2008-03-27 | 2009-03-26 | Methods for treating disorders using nmda nr2b-subtype selective antagonist |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2010143864A RU2010143864A (ru) | 2012-05-10 |
| RU2499598C2 true RU2499598C2 (ru) | 2013-11-27 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
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| RU2010143864/15A RU2499598C2 (ru) | 2008-03-27 | 2009-03-26 | Способы лечения нарушений с применением селективного антагониста nr2b-подтипа nmda рецепторов |
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| EP (1) | EP2254580A1 (enExample) |
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| CA (1) | CA2719749A1 (enExample) |
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| WO (1) | WO2009118187A1 (enExample) |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2735277C2 (ru) * | 2015-06-01 | 2020-10-29 | Руджен Холдингс (Кайман) Лимитед | 3,3-дифторпиперидинкарбаматные гетероциклические соединения в качестве антагонистов nr2b nmda-рецептора |
| US11000526B2 (en) | 2016-11-22 | 2021-05-11 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
Families Citing this family (17)
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| US9387212B2 (en) | 2012-04-20 | 2016-07-12 | Ucb Biopharma Sprl | Methods for treating Parkinson's disease |
| US11232319B2 (en) * | 2014-05-16 | 2022-01-25 | The Trustees Of The University Of Pennsylvania | Applications of automatic anatomy recognition in medical tomographic imagery based on fuzzy anatomy models |
| US10155727B2 (en) | 2014-08-15 | 2018-12-18 | Janssen Pharmaceuticals, Inc. | Pyrazoles |
| HUE049277T2 (hu) | 2014-08-15 | 2020-09-28 | Janssen Pharmaceuticals Inc | Triazolok mint NR2B receptor inhibitorok |
| HRP20200410T1 (hr) | 2015-07-09 | 2020-08-21 | Janssen Pharmaceutica Nv | Supstituirani 4-azaindoli i njihova upotreba kao modulatora glun2b receptora |
| KR20180108822A (ko) | 2016-02-10 | 2018-10-04 | 얀센 파마슈티카 엔.브이. | Nr2b-선택적 nmda 조절제로서 치환된 1,2,3-트라이아졸 |
| US10487055B2 (en) | 2016-06-01 | 2019-11-26 | Rhode Island Board Of Education | Diindole compounds useful in treatment of nervous system disorders |
| TW201819376A (zh) | 2016-10-06 | 2018-06-01 | 比利時商健生藥品公司 | 經取代之１Ｈ－咪唑並［４，５－ｂ］吡啶－２（３Ｈ）－酮及其作為ＧＬＵＮ２Ｂ受體調節劑之用途 |
| US10732235B2 (en) * | 2018-03-29 | 2020-08-04 | Siemens Healthcare Gmbh | Magnetic resonance method and apparatus using atlas-based masking for quantitative susceptibility mapping |
| EP3774732A4 (en) | 2018-04-04 | 2022-02-09 | Janssen Pharmaceutica NV | PYRIDINE AND SUBSTITUTED PYRIMIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS |
| EP3983074A1 (en) | 2019-06-14 | 2022-04-20 | Janssen Pharmaceutica NV | Pyridine carbamates and their use as glun2b receptor modulators |
| SG11202112405VA (en) | 2019-06-14 | 2021-12-30 | Janssen Pharmaceutica Nv | Substituted heteroaromatic pyrazolo-pyridines and their use as glun2b receptor modulators |
| MX2021015500A (es) | 2019-06-14 | 2022-02-10 | Janssen Pharmaceutica Nv | Pirazolo-pirazinas sustituidas y su uso como moduladores del receptor glun2b. |
| MX2021015506A (es) | 2019-06-14 | 2022-02-10 | Janssen Pharmaceutica Nv | Amidas de pirazolo-piridina sustituidas y su uso como moduladores del receptor glun2b. |
| CN113950357A (zh) | 2019-06-14 | 2022-01-18 | 詹森药业有限公司 | 吡嗪氨基甲酸酯及其作为GluN2B受体调节剂的用途 |
| CA3143102A1 (en) | 2019-06-14 | 2020-12-17 | Janssen Pharmaceutica Nv | Substituted pyrazolo[4,3-b]pyridines and their use as glun2b receptor modulators |
| JP7667097B2 (ja) | 2019-06-14 | 2025-04-22 | ヤンセン ファーマシューティカ エヌ．ベー． | 置換ピラゾロ－ピリジンアミド及びｇｌｕｎ２ｂ受容体調節因子としてのその使用 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2173151C2 (ru) * | 1997-12-18 | 2001-09-10 | Форбз Меди-Тек Инк. | Способ и композиция для профилактики и задержки начала болезни альцгеймера |
| WO2003097637A1 (en) * | 2002-05-16 | 2003-11-27 | F. Hoffmann-La Roche Ag | (imidazol-1-yl-methyl)-pyridazine as nmda receptor blocker |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997032581A1 (en) * | 1996-03-08 | 1997-09-12 | F. Hoffmann-La Roche Ag | Use of 4-phenyl-3,6-dihydro-2h-pyridyl derivatives as nmda receptor subtype blockers |
| US6015824A (en) * | 1998-02-10 | 2000-01-18 | Hoffmann-La Roche Ag | Pyrrolidine and piperidine derivatives and treatment of neurodegenerative disorders |
| TWI254043B (en) * | 1999-06-08 | 2006-05-01 | Hoffmann La Roche | Ethanesulfonyl-piperidine derivatives having good affinity to N-methyl-D-aspartate (NMDA) receptor |
| DE60007697T2 (de) * | 1999-07-21 | 2004-12-09 | F. Hoffmann-La Roche Ag | Triazolderivate |
| AU2001273942B2 (en) * | 2000-04-20 | 2005-09-01 | F. Hoffmann-La Roche Ag | Pyrrolidine and piperidine derivatives and their use for the treament of neurodegenerative disorders |
| US6432985B2 (en) * | 2000-04-25 | 2002-08-13 | Hoffmann-La Roche Inc. | Neuroprotective substituted piperidine compounds with activity as NMDA NR2B subtype selective antagonists |
| US7022882B2 (en) * | 2000-10-06 | 2006-04-04 | The Regents Of The University Of California | NMDA receptor channel blocker with neuroprotective activity |
| JP2009503520A (ja) * | 2005-07-29 | 2009-01-29 | リージェンツ オブ ザ ユニバーシティ オブ ミネソタ | ベータアミロイド受容体及びその使用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2173151C2 (ru) * | 1997-12-18 | 2001-09-10 | Форбз Меди-Тек Инк. | Способ и композиция для профилактики и задержки начала болезни альцгеймера |
| WO2003097637A1 (en) * | 2002-05-16 | 2003-11-27 | F. Hoffmann-La Roche Ag | (imidazol-1-yl-methyl)-pyridazine as nmda receptor blocker |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2735277C2 (ru) * | 2015-06-01 | 2020-10-29 | Руджен Холдингс (Кайман) Лимитед | 3,3-дифторпиперидинкарбаматные гетероциклические соединения в качестве антагонистов nr2b nmda-рецептора |
| US11136328B2 (en) | 2015-06-01 | 2021-10-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists |
| US11000526B2 (en) | 2016-11-22 | 2021-05-11 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
| US11752155B2 (en) | 2016-11-22 | 2023-09-12 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
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| ZA201006587B (en) | 2012-02-29 |
| JP2011516417A (ja) | 2011-05-26 |
| CN101977606A (zh) | 2011-02-16 |
| IL207835A0 (en) | 2010-12-30 |
| RU2010143864A (ru) | 2012-05-10 |
| CA2719749A1 (en) | 2009-10-01 |
| NZ588698A (en) | 2012-06-29 |
| MX2010009649A (es) | 2010-12-17 |
| JP2016094430A (ja) | 2016-05-26 |
| US20110053951A1 (en) | 2011-03-03 |
| EP2254580A1 (en) | 2010-12-01 |
| WO2009118187A1 (en) | 2009-10-01 |
| KR20100135847A (ko) | 2010-12-27 |
| AU2009228660A1 (en) | 2009-10-01 |
| BRPI0909378A2 (pt) | 2015-10-06 |
| JP2014098018A (ja) | 2014-05-29 |
| AU2009228660B2 (en) | 2012-11-29 |
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