RU2007101653A - Производные 1-азабицикло[3.3.1]нонанов - Google Patents
Производные 1-азабицикло[3.3.1]нонанов Download PDFInfo
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- RU2007101653A RU2007101653A RU2007101653/04A RU2007101653A RU2007101653A RU 2007101653 A RU2007101653 A RU 2007101653A RU 2007101653/04 A RU2007101653/04 A RU 2007101653/04A RU 2007101653 A RU2007101653 A RU 2007101653A RU 2007101653 A RU2007101653 A RU 2007101653A
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- Prior art keywords
- acid addition
- free base
- addition salt
- pharmaceutically acceptable
- acceptable acid
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 12
- 239000002253 acid Substances 0.000 claims 11
- 239000012458 free base Substances 0.000 claims 11
- 238000011282 treatment Methods 0.000 claims 8
- 230000002265 prevention Effects 0.000 claims 5
- 230000003340 mental effect Effects 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 230000004770 neurodegeneration Effects 0.000 claims 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims 4
- 208000020016 psychiatric disease Diseases 0.000 claims 4
- 102000015296 acetylcholine-gated cation-selective channel activity proteins Human genes 0.000 claims 3
- 108040006409 acetylcholine-gated cation-selective channel activity proteins Proteins 0.000 claims 3
- 230000004913 activation Effects 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000008177 pharmaceutical agent Substances 0.000 claims 2
- HMOACHBGHRNVLN-UHFFFAOYSA-N 1-azabicyclo[3.3.1]nonan-4-ol Chemical compound C1CCC2C(O)CCN1C2 HMOACHBGHRNVLN-UHFFFAOYSA-N 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000008024 pharmaceutical diluent Substances 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 239000007858 starting material Substances 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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Claims (14)
1. Соединение формулы I
где А представляет собой О или N(R1);
Y представляет собой группу формулы
где левая связь присоединена к группе А, и правая связь присоединена к группе R;
R представляет собой замещенный или незамещенный С5-С10арил, замещенный или незамещенный гетеро-С5-С10арил, группу N(R1)(R4) или группу N(R2)(CHR3R4);
R1 представляет собой водород, С1-С4алкил или CF3;
R2 представляет собой водород, С1-С4алкил или CF3;
R3 представляет собой водород, С1-С4алкил или CF3;
R4 представляет собой замещенный или незамещенный С5-С10арил или замещенный или незамещенный С5-С10гетероарил;
в форме свободного основания или в форме кислотной аддитивной соли.
2. Соединение формулы I по п.1, где А представляет собой кислород.
3. Соединение формулы I по п.1, где Y представляет собой одну из следующих групп:
4. Способ получения соединения формулы I по п.1 или его соли, которые включает стадию реакции соединения формулы II
где Y и R являются такими, как определено в п.1, и Z представляет собой уходящую группу, с соединением формулы III
и превращение полученного таким образом соединения формулы I в свободное основание или в форму кислотной аддитивной соли.
5. Соединение по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли для применения в качестве фармацевтического средства.
6. Соединение по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли для применения для профилактики и лечения психических и нейродегенеративных заболеваний.
7. Фармацевтическая композиция, включающая соединение по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли вместе с фармацевтическим носителем или разбавителем.
8. Применение соединения по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли в качестве фармацевтического средства для профилактики и лечения психических и нейродегенеративных заболеваний.
9. Применение соединения по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли для изготовления лекарственного средства для профилактики и лечения психических и нейродегенеративных заболеваний.
10. Способ профилактики и лечения психических и нейродегенеративных заболеваний у пациента, нуждающегося в таком лечении, который включает введение такому пациенту терапевтически эффективного количества соединения по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли.
11. Соединение по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли для применения для лечения или профилактики заболевания или состояния, в котором играет роль или участвует активация α7 nAChR.
12. Применение соединения по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли в качестве фармацевтического средства для лечения или профилактики заболевания или состояния, в котором играет роль или участвует активация α7 nAChR.
13. Способ лечения или профилактики заболевания или состояния, в котором играет роль или участвует активация α7 nAChR, у субъекта, нуждающегося в таком лечении, который включает введение такому пациенту терапевтически эффективного количества соединения по любому одному из пп.1-3 в форме свободного основания или в форме фармацевтически приемлемой кислотной аддитивной соли.
14. Продукт, полученный в соответствии со способом по п.2, характеризующийся тем, что (-)-1-азабицикло[3.3.1]нонан-4-ол используют в качестве исходного материала.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US58102004P | 2004-06-18 | 2004-06-18 | |
| US60/581,020 | 2004-06-18 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2007101653A true RU2007101653A (ru) | 2008-07-27 |
| RU2445313C2 RU2445313C2 (ru) | 2012-03-20 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2007101653/04A RU2445313C2 (ru) | 2004-06-18 | 2005-06-17 | Производные 1-азабицикло[3.3.1]нонанов |
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| Country | Link |
|---|---|
| US (3) | US20070249657A1 (ru) |
| EP (2) | EP2336129A1 (ru) |
| JP (1) | JP4944772B2 (ru) |
| KR (3) | KR101343654B1 (ru) |
| CN (1) | CN1964968A (ru) |
| AR (1) | AR049401A1 (ru) |
| AT (1) | ATE506362T1 (ru) |
| AU (1) | AU2005254689B2 (ru) |
| BR (1) | BRPI0510940A (ru) |
| CA (1) | CA2566155C (ru) |
| CY (1) | CY1111528T1 (ru) |
| DE (1) | DE602005027567D1 (ru) |
| DK (1) | DK1761533T3 (ru) |
| EC (1) | ECSP067053A (ru) |
| ES (1) | ES2364971T3 (ru) |
| HR (1) | HRP20110535T1 (ru) |
| IL (2) | IL179611A (ru) |
| MA (1) | MA28684B1 (ru) |
| MX (1) | MXPA06014697A (ru) |
| MY (1) | MY147262A (ru) |
| NO (1) | NO20070339L (ru) |
| NZ (1) | NZ551198A (ru) |
| PE (1) | PE20060437A1 (ru) |
| PL (1) | PL1761533T3 (ru) |
| PT (1) | PT1761533E (ru) |
| RU (1) | RU2445313C2 (ru) |
| SG (1) | SG153834A1 (ru) |
| SI (1) | SI1761533T1 (ru) |
| TN (1) | TNSN06407A1 (ru) |
| TW (1) | TWI370128B (ru) |
| WO (1) | WO2005123732A1 (ru) |
| ZA (1) | ZA200609255B (ru) |
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| GB0415746D0 (en) | 2004-07-14 | 2004-08-18 | Novartis Ag | Organic compounds |
| GB0521508D0 (en) | 2005-10-21 | 2005-11-30 | Novartis Ag | Organic compounds |
| GB0525673D0 (en) * | 2005-12-16 | 2006-01-25 | Novartis Ag | Organic compounds |
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| CN103180321A (zh) | 2010-09-23 | 2013-06-26 | Abbvie公司 | 氮杂金刚烷衍生物的一水合物 |
| BR112013018726A2 (pt) | 2011-01-27 | 2016-10-25 | Novartis Ag | uso de ativadores de alfa 7 do receptor nicotínico de acetilcolina |
| CN103561740A (zh) * | 2011-03-18 | 2014-02-05 | 诺瓦提斯公司 | 用于帕金森病中多巴胺诱导的运动障碍的α7烟碱性乙酰胆碱受体活化剂和mGluR5拮抗剂的组合 |
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| KR101879921B1 (ko) | 2013-01-15 | 2018-07-18 | 노파르티스 아게 | 기면증의 치료를 위한 알파 7 니코틴성 아세틸콜린 수용체 작용물질의 용도 |
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| JP6338223B2 (ja) * | 2013-01-15 | 2018-06-06 | ノバルティス アーゲー | アルファ７ニコチン性アセチルコリン受容体アゴニストの使用 |
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| CN118812532A (zh) | 2019-02-05 | 2024-10-22 | 斯基霍克疗法公司 | 用于调节剪接的方法和组合物 |
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- 2005-06-16 AR ARP050102477A patent/AR049401A1/es unknown
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