KR840007406A - 중추 신경계에 활성을 나타내는 복소환 화합물의 제조방법 - Google Patents
중추 신경계에 활성을 나타내는 복소환 화합물의 제조방법 Download PDFInfo
- Publication number
- KR840007406A KR840007406A KR1019840000249A KR840000249A KR840007406A KR 840007406 A KR840007406 A KR 840007406A KR 1019840000249 A KR1019840000249 A KR 1019840000249A KR 840000249 A KR840000249 A KR 840000249A KR 840007406 A KR840007406 A KR 840007406A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- halogen atom
- hydrogen
- atom
- converted
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 3
- 210000003169 central nervous system Anatomy 0.000 title 1
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 150000001412 amines Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 239000007858 starting material Substances 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 150000002576 ketones Chemical class 0.000 claims 2
- AAILEWXSEQLMNI-UHFFFAOYSA-N 1h-pyridazin-6-one Chemical compound OC1=CC=CN=N1 AAILEWXSEQLMNI-UHFFFAOYSA-N 0.000 claims 1
- NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical compound CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Classifications
-
- 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
- C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
- C07D237/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Biomedical Technology (AREA)
- Public Health (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Catalysts (AREA)
- Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
- Saccharide Compounds (AREA)
- Non-Silver Salt Photosensitive Materials And Non-Silver Salt Photography (AREA)
- Polymerisation Methods In General (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (3)
- 기을 함유한 X1또는 X2기가 케톤 형태인 화합물을 출발물질로 하여, 상기 케톤을 상응하는 염소화 유도체로 전환시킨 후 이를 아민(식중 R1및 R2는 -(CH2)nOH 기(n=1~4)를 나타내거나가 복소원으로 하나의 질소원자를 함유하며 3 또는 4위치에 -(CH2)mOH기(m은 0,1 또는 2이다)를 갖는 5 또는 6원 포화복소환을 형성한다)과 반응시키고, 필요하다면 수득된 히드록시화 유도체를 산클로라이드와 반응시켜 에스테르화함을 특징으로 하는 하기 일반식(I)의 화합물 및 그의 약학적으로 무독한 산과의 염의 제조방법.상기식중, -X1은 N 또는기를 나타내고; -X2는 N 또는기를 나타내며, X1과 X2는 서로 다르고; -R1및 R2는 -(CH2)nOH (n=1~4)를 나타내거나,가 복소원으로서 하나의 질소 원자를 함유하며 I) a -(CH2)mOR6기(m은 1,0 또는 2이고, R6는 수소 또는또는기이며, R7은 저급알킬, 시클로알킬기 또는 할로겐원자에 의해 치환될 수 있는 페닐기를 나타내며, R8및 R9는 각각 수소 또는 저급 알킬을 독립적으로 나타낸다); ii) 옥소(=0)기; iii) 스피로-1,3-디옥솔란-2-일기로부터 선택된 3 또는 4위치의 치환체를 갖는 5 또는 6원포화복소환을 구성하며; -Ar은기(R3는 수소, 할로겐원자, 저급 알킬기, 저급알콕시기, 트리플루오로메틸기, 히드록실기, 니트로기 또는 시아노기를 나타내며, R4는 수소원자 또는 할로겐원자를 나타낸다) 또는 할로겐원자에 의해 비치환 또는 모노 치환된 나프틸기를 나타내고; -R5는 수소 또는 할로겐원자를 나타내며, X2가 질소원자를 나타낼 때 R5는 단지 할로겐원자일 수 있다.
- 제1항에 있어서, 출발물질을 3-피리다지논으로 하고, 이를 상응하는 6-아릴-3-클로로-피리다진으로 전환시킨 후 아민기로 치환시킴을 특징으로 하는 방법.
- 제1항에 있어서, 출발물질을 6-아릴-피리미딘-2-온으로 하고, 이를 상응하는 2-클로로-6-아릴 피리미딘으로 전환시킨 후 아민로 치환시킴을 특징으로 하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR8300954A FR2539741A1 (fr) | 1983-01-21 | 1983-01-21 | Composes a noyau heterocyclique diazote, leur procede de preparation et les medicaments, actifs sur le systeme nerveux central, qui en contiennent |
| FR8300954 | 1983-01-21 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR840007406A true KR840007406A (ko) | 1984-12-07 |
| KR910000640B1 KR910000640B1 (ko) | 1991-01-31 |
Family
ID=9285183
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019840000249A KR910000640B1 (ko) | 1983-01-21 | 1984-01-20 | 중추 신경계에 활성을 나타내는 복소환 화합물의 제조방법 |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US4624952A (ko) |
| EP (1) | EP0114770B1 (ko) |
| JP (1) | JPS59137469A (ko) |
| KR (1) | KR910000640B1 (ko) |
| AT (1) | ATE28453T1 (ko) |
| AU (1) | AU563160B2 (ko) |
| CA (1) | CA1217490A (ko) |
| CS (1) | CS242894B2 (ko) |
| DD (1) | DD216014A5 (ko) |
| DE (1) | DE3464909D1 (ko) |
| DK (1) | DK25684A (ko) |
| EG (1) | EG16212A (ko) |
| ES (1) | ES8407040A1 (ko) |
| FI (1) | FI79537C (ko) |
| FR (1) | FR2539741A1 (ko) |
| GR (1) | GR79766B (ko) |
| HU (1) | HU191586B (ko) |
| IE (1) | IE56569B1 (ko) |
| IL (1) | IL70740A (ko) |
| MA (1) | MA20007A1 (ko) |
| NO (1) | NO159170C (ko) |
| NZ (1) | NZ206906A (ko) |
| OA (1) | OA07638A (ko) |
| PH (1) | PH21060A (ko) |
| PL (1) | PL143224B1 (ko) |
| PT (1) | PT77966B (ko) |
| SG (1) | SG2189G (ko) |
| SU (1) | SU1342415A3 (ko) |
| YU (1) | YU10384A (ko) |
| ZA (1) | ZA84342B (ko) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5001125A (en) * | 1984-03-26 | 1991-03-19 | Janssen Pharmaceutica N.V. | Anti-virally active pyridazinamines |
| FR2567518B1 (fr) * | 1984-07-11 | 1987-11-13 | Sanofi Sa | Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent |
| DE3517617A1 (de) * | 1985-05-15 | 1986-11-20 | Lentia GmbH Chem. u. pharm. Erzeugnisse - Industriebedarf, 8000 München | Neue pyridaziniumverbindungen, verfahren zu deren herstellung und diese enthaltende fungizide und algizide mittel |
| US5106973A (en) * | 1987-11-23 | 1992-04-21 | Janssen Pharmaceutica N.V. | Pyridzainamine derivatives |
| FI895821A0 (fi) * | 1988-12-07 | 1989-12-05 | Wellcome Found | Farmaceutiskt aktiva cns foereningar. |
| US5656631A (en) * | 1989-02-07 | 1997-08-12 | Sanofi | Pyridazine derivatives |
| FR2676444B1 (fr) * | 1991-05-16 | 1995-03-10 | Sanofi Elf | Nouveaux derives d'amino-3 pyridazines actifs sur le systeme nerveux central, procede de preparation et compositions pharmaceutiques en contenant. |
| US5958934A (en) * | 1996-05-23 | 1999-09-28 | Syntex (U.S.A.) Inc. | Aryl pyrimidine derivatives and uses thereof |
| TW440563B (en) * | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
| US5952331A (en) * | 1996-05-23 | 1999-09-14 | Syntex (Usa) Inc. | Aryl pyrimidine derivatives |
| WO2008096746A1 (ja) * | 2007-02-06 | 2008-08-14 | Takeda Pharmaceutical Company Limited | スピロ化合物およびその用途 |
| CN107973791B (zh) | 2015-04-29 | 2020-04-07 | 南京圣和药业股份有限公司 | 稠环或三环芳基嘧啶化合物用作激酶抑制剂 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1345880A (en) * | 1971-06-18 | 1974-02-06 | Cepbepe | Pyridazine derivatives |
| US4302455A (en) * | 1980-04-14 | 1981-11-24 | Merck & Co., Inc. | 2-(4-Aminopiperidino)pyrazines |
| FR2510997A1 (fr) * | 1981-08-10 | 1983-02-11 | Sanofi Sa | Nouveaux derives de la methyl-4 phenyl-6 pyridazine, procede pour leur preparation et medicaments actifs sur le systeme nerveux central en contenant |
| FR2511366A1 (fr) * | 1981-08-11 | 1983-02-18 | Sanofi Sa | Nouveaux derives de la pyridazine, leur procede de preparation et les medicaments, actifs sur le systeme nerveux central, qui en contiennent |
-
1983
- 1983-01-21 FR FR8300954A patent/FR2539741A1/fr active Granted
-
1984
- 1984-01-12 CA CA000445186A patent/CA1217490A/en not_active Expired
- 1984-01-12 AU AU23236/84A patent/AU563160B2/en not_active Ceased
- 1984-01-13 MA MA20228A patent/MA20007A1/fr unknown
- 1984-01-16 PT PT77966A patent/PT77966B/pt not_active IP Right Cessation
- 1984-01-16 GR GR73515A patent/GR79766B/el unknown
- 1984-01-16 US US06/570,832 patent/US4624952A/en not_active Expired - Fee Related
- 1984-01-17 ZA ZA84342A patent/ZA84342B/xx unknown
- 1984-01-17 ES ES528921A patent/ES8407040A1/es not_active Expired
- 1984-01-18 EP EP84400101A patent/EP0114770B1/en not_active Expired
- 1984-01-18 AT AT84400101T patent/ATE28453T1/de not_active IP Right Cessation
- 1984-01-18 IE IE102/84A patent/IE56569B1/en not_active IP Right Cessation
- 1984-01-18 DE DE8484400101T patent/DE3464909D1/de not_active Expired
- 1984-01-19 DD DD84259497A patent/DD216014A5/de not_active IP Right Cessation
- 1984-01-19 CS CS84424A patent/CS242894B2/cs unknown
- 1984-01-20 NZ NZ206906A patent/NZ206906A/en unknown
- 1984-01-20 OA OA58210A patent/OA07638A/xx unknown
- 1984-01-20 DK DK25684A patent/DK25684A/da not_active Application Discontinuation
- 1984-01-20 IL IL70740A patent/IL70740A/xx unknown
- 1984-01-20 PH PH30134A patent/PH21060A/en unknown
- 1984-01-20 NO NO840214A patent/NO159170C/no unknown
- 1984-01-20 PL PL1984245836A patent/PL143224B1/pl unknown
- 1984-01-20 YU YU00103/84A patent/YU10384A/xx unknown
- 1984-01-20 HU HU84246A patent/HU191586B/hu not_active IP Right Cessation
- 1984-01-20 KR KR1019840000249A patent/KR910000640B1/ko active IP Right Grant
- 1984-01-20 FI FI840238A patent/FI79537C/fi not_active IP Right Cessation
- 1984-01-20 SU SU843696574A patent/SU1342415A3/ru active
- 1984-01-21 EG EG40/84A patent/EG16212A/xx active
- 1984-01-21 JP JP59009383A patent/JPS59137469A/ja active Pending
-
1989
- 1989-01-11 SG SG21/89A patent/SG2189G/en unknown
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