RU2001106634A - Новые 4-амино-1-арил-пиридин-2-оны с антиконвульсивным действием и способ их получения - Google Patents
Новые 4-амино-1-арил-пиридин-2-оны с антиконвульсивным действием и способ их полученияInfo
- Publication number
- RU2001106634A RU2001106634A RU2001106634/04A RU2001106634A RU2001106634A RU 2001106634 A RU2001106634 A RU 2001106634A RU 2001106634/04 A RU2001106634/04 A RU 2001106634/04A RU 2001106634 A RU2001106634 A RU 2001106634A RU 2001106634 A RU2001106634 A RU 2001106634A
- Authority
- RU
- Russia
- Prior art keywords
- pyridin
- amino
- general formula
- compounds
- alkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
-
- 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
- C07D213/46—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Claims (12)
1. Новые соединения общей формулы 1
где n = 0,1,2,3,4,5;
X обозначает водород, С1-С4-алкил, С1-С4-алкокси, трифтор-
метил, трифторметокси или галоген;
А обозначает амино, С1-С4-алкиламино, С1-С4-диалкиламино, морфолино, пиперидино или пирролидино, за исключением соединений, в которых n равно 0 и А обозначает метиламино или диметиламино.
2. Соединения по п.1, представляющие собой
4-амино-1-фенилпиридин-2-он,
4-амино-1-(2-хлорфенил)пиридин-2-он,
4-амино-1-(4-хлорфенил)пиридин-2-он,
4-амино-1-(2-метилфенил)пиридин-2-он,
4-амино-1-(3-метилфенил)пиридин-2-он,
4-амино-1-(4-метилфенил)пиридин-2-он,
4-амино-1-(4-метоксифенил)пиридин-2-он,
4-амино-1-(4-трифторметоксифенил)пиридин-2-он,
4-амино-1-(2,6-дихлорфенил)пиридин-2-он,
4-амино-1-(2-фторфенил)пиридин-2-он,
4-амино-1-(4-фторфенил)пиридин-2-он,
4-амино-1-(2,6-дифторфенил)пиридин-2-он,
4-амино-1-(2-хлор-4-фторфенил)пиридин-2-он,
1-(2-хлорфенил)-4-диметиламино-пиридин-2-он,
1-(2-хлорфенил)-4-(4-морфолино)пиридин-2-он.
3. Способ получения соединений общей формулы 1, отличающийся тем, что соединение общей формулы 2
где n = 0,1,2,3,4,5;
X обозначает водород, С1-С4-алкил, С1-С4-алкокси, трифторметил, трифторметокси или галоген;
R обозначает С1-С4-алкил,
нагревают в щелочной среде в течение 0,1-10 ч при 50-150°С и затем нагревают с сильными кислотами в течение 10-30 мин при 100-200°С.
4. Способ получения соединений общей формулы 1 по п.3, отличающийся тем, что используют предпочтительно 5-50%-ный раствор едкого натра.
5. Способ получения соединений общей формулы 1 по п.3, отличающийся тем, что нагревание в щелочной среде предпочтительно проводят в пределах одного часа.
6. Способ получения соединений общей формулы 1 по п.3, отличающийся тем, что используют предпочтительно 50-98%-ную серную кислоту.
7. Способ получения соединений общей формулы 1, где А обозначает С1-С4-алкиламино, С1-С4-диалкиламино, морфолино, пиперидино или пирролидино, отличающийся тем, что соединение общей формулы 2
где n = 0,1,2,3,4,5;
Х обозначает водород, С1-С4-алкил, С1-С4-алкокси, трифторметил, трифторметокси или галоген;
R обозначает С1-С4-алкил,
нагревают в щелочной среде в течение 0,1-10 ч при 50-150°С, затем нагревают с сильными кислотами в течение 10-30 мин при 100-200°С и затем алкилируют в щелочной среде.
8. Способ получения соединений общей формулы 1 по п.7, отличающийся тем, что алкилирование проводят предпочтительно диметилсульфатом, метилиодидом, 1,4-дибромбутаном, 1,5-дибромпентаном или ди-(2-хлорэтиловым) эфиром.
9. Фармацевтические композиции, отличающиеся тем, что они содержат в качестве активного вещества по меньшей мере одно соединение общей формулы 1 и в случае необходимости фармацевтические носители и вспомогательные вещества.
10. фармацевтические композиции по п.9, отличающиеся тем, что они содержат в качестве активного вещества по меньшей мере одно из соединений по п.2.
11. Соединения общей формулы 1 по п.1, для приготовления лекарственных средств для лечения различных форм эпилептических заболеваний.
12. Соединения по п.2 для приготовления лекарственных средств для лечения различных форм эпилептических заболевании.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19835918.7 | 1998-08-07 | ||
| DE19835918A DE19835918A1 (de) | 1998-08-07 | 1998-08-07 | Neue antikonvulsiv wirkende 4-Amino-1-aryl-pyridin-2-one und Verfahren zu deren Herstellung |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2001106634A true RU2001106634A (ru) | 2004-02-27 |
Family
ID=7876889
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2001106634/04A RU2001106634A (ru) | 1998-08-07 | 1999-07-28 | Новые 4-амино-1-арил-пиридин-2-оны с антиконвульсивным действием и способ их получения |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US6071911A (ru) |
| EP (1) | EP1102748A1 (ru) |
| JP (1) | JP2002522420A (ru) |
| KR (1) | KR20010074802A (ru) |
| CN (1) | CN1322197A (ru) |
| AR (1) | AR021186A1 (ru) |
| AU (1) | AU5507499A (ru) |
| BG (1) | BG105196A (ru) |
| BR (1) | BR9912849A (ru) |
| CA (1) | CA2279692C (ru) |
| DE (1) | DE19835918A1 (ru) |
| HU (1) | HUP0103204A3 (ru) |
| IL (1) | IL141200A0 (ru) |
| NO (1) | NO20010575L (ru) |
| NZ (1) | NZ509914A (ru) |
| PL (1) | PL346013A1 (ru) |
| RU (1) | RU2001106634A (ru) |
| SK (1) | SK2002001A3 (ru) |
| TR (1) | TR200100370T2 (ru) |
| WO (1) | WO2000007988A1 (ru) |
| ZA (1) | ZA200100999B (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2320973T3 (es) | 2000-06-12 | 2009-06-01 | EISAI R&D MANAGEMENT CO., LTD. | Compuestos de 1,2-dihidropiridina, procedimiento para su preparacion y uso de los mismos. |
| GB0129260D0 (en) | 2001-12-06 | 2002-01-23 | Eisai London Res Lab Ltd | Pharmaceutical compositions and their uses |
| MY148809A (en) | 2004-07-06 | 2013-05-31 | Eisai R&D Man Co Ltd | Crystals of 1,2-dihydropyridine compound and their production process |
| KR20210107644A (ko) | 2018-12-14 | 2021-09-01 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 1,2-디하이드로피리딘 화합물의 수성 기반 약학적 제형 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS51118768A (en) * | 1975-02-19 | 1976-10-18 | Shigeo Senda | Method for preparing 4-amino-2-pyridone derivatives |
| EP0110091B1 (de) * | 1982-10-27 | 1987-01-21 | Degussa Aktiengesellschaft | 2-Amino-3-Acylamino-6-benzylamino-pyridin-Derivate mit anti-epileptischer Wirkung |
-
1998
- 1998-08-07 DE DE19835918A patent/DE19835918A1/de not_active Withdrawn
-
1999
- 1999-07-28 SK SK200-2001A patent/SK2002001A3/sk unknown
- 1999-07-28 CN CN99811849A patent/CN1322197A/zh active Pending
- 1999-07-28 WO PCT/EP1999/005399 patent/WO2000007988A1/de not_active Application Discontinuation
- 1999-07-28 BR BR9912849-7A patent/BR9912849A/pt not_active IP Right Cessation
- 1999-07-28 AU AU55074/99A patent/AU5507499A/en not_active Abandoned
- 1999-07-28 KR KR1020017001574A patent/KR20010074802A/ko not_active Application Discontinuation
- 1999-07-28 HU HU0103204A patent/HUP0103204A3/hu unknown
- 1999-07-28 PL PL99346013A patent/PL346013A1/xx unknown
- 1999-07-28 JP JP2000563622A patent/JP2002522420A/ja active Pending
- 1999-07-28 IL IL14120099A patent/IL141200A0/xx unknown
- 1999-07-28 RU RU2001106634/04A patent/RU2001106634A/ru unknown
- 1999-07-28 EP EP99941472A patent/EP1102748A1/de not_active Withdrawn
- 1999-07-28 TR TR2001/00370T patent/TR200100370T2/xx unknown
- 1999-07-28 NZ NZ509914A patent/NZ509914A/xx unknown
- 1999-08-05 CA CA002279692A patent/CA2279692C/en not_active Expired - Fee Related
- 1999-08-06 US US09/370,640 patent/US6071911A/en not_active Expired - Fee Related
- 1999-08-06 AR ARP990103952A patent/AR021186A1/es not_active Application Discontinuation
-
2001
- 2001-01-30 BG BG105196A patent/BG105196A/xx unknown
- 2001-02-02 NO NO20010575A patent/NO20010575L/no unknown
- 2001-02-06 ZA ZA200100999A patent/ZA200100999B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20010074802A (ko) | 2001-08-09 |
| AU5507499A (en) | 2000-02-28 |
| NO20010575L (no) | 2001-04-04 |
| JP2002522420A (ja) | 2002-07-23 |
| BR9912849A (pt) | 2001-05-08 |
| SK2002001A3 (en) | 2002-01-07 |
| CN1322197A (zh) | 2001-11-14 |
| CA2279692A1 (en) | 2000-02-07 |
| NO20010575D0 (no) | 2001-02-02 |
| AR021186A1 (es) | 2002-07-03 |
| ZA200100999B (en) | 2001-12-14 |
| HUP0103204A3 (en) | 2002-06-28 |
| TR200100370T2 (tr) | 2001-08-21 |
| DE19835918A1 (de) | 2000-02-10 |
| NZ509914A (en) | 2002-11-26 |
| HUP0103204A2 (hu) | 2002-04-29 |
| PL346013A1 (en) | 2002-01-14 |
| BG105196A (en) | 2001-12-29 |
| US6071911A (en) | 2000-06-06 |
| IL141200A0 (en) | 2002-02-10 |
| EP1102748A1 (de) | 2001-05-30 |
| WO2000007988A1 (de) | 2000-02-17 |
| CA2279692C (en) | 2003-10-07 |
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