KR940007021A - 흥분성 아미노산 수용체 길항물질 - Google Patents
흥분성 아미노산 수용체 길항물질 Download PDFInfo
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- KR940007021A KR940007021A KR1019930017398A KR930017398A KR940007021A KR 940007021 A KR940007021 A KR 940007021A KR 1019930017398 A KR1019930017398 A KR 1019930017398A KR 930017398 A KR930017398 A KR 930017398A KR 940007021 A KR940007021 A KR 940007021A
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- Prior art keywords
- alkyl
- chr
- hydrogen
- pharmaceutically acceptable
- phenyl
- Prior art date
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- 229940123511 Excitatory amino acid receptor antagonist Drugs 0.000 title abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000002252 acyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- -1 hydroxy, amino, bromo, iodo Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- NSENYWQRQUNUGD-UHFFFAOYSA-N 1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinolin-2-ium-3-carboxylate Chemical compound C1CCCC2CNC(C(=O)O)CC21 NSENYWQRQUNUGD-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000004299 tetrazol-5-yl group Chemical group [H]N1N=NC(*)=N1 0.000 claims 1
- NENLYAQPNATJSU-UHFFFAOYSA-N 1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline Chemical class C1NCCC2CCCCC21 NENLYAQPNATJSU-UHFFFAOYSA-N 0.000 abstract 2
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 238000010189 synthetic method Methods 0.000 abstract 1
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- 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
- C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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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
- A61K31/47—Quinolines; Isoquinolines
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- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
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Abstract
본 발명은 흥분성 아미노산수용체 길항물질제로서 유용하고 신경질환의 치료에 유용한 신규한 데카하이드로이소퀴놀린 화합물을 제공한다. 본 발명은 또한 데카하이드로이소퀴놀린 뿐 아니라, 그의 합성에 신규한 중간체의 제조를 위한 합성 방법을 제공한다.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (4)
- 하기 일반식(Ⅰ)의 화합물 또는 그의 약학적으로 허요가능한 염:상기식에서, R1은 수소, C1-C10알킬, 아릴알킬, 알콕시카보닐 또는 아실이고; R2는 수소, C1-C6알킬, 치환된 알킬, 사이클로알킬 또는 아릴 알킬이고, R3는 CO2H, SO2H, CONHSO2R8또는 일반식의 그룹이고, W는 (CH2)n, S, SO 또는 CO2이고, Y는 CHR7, NR4, O, S, SO 또는 SO2이고, Z는 NR6, CHR7,또는 CH이거나, 또는 W 및 Y는 함께 HC=CH 또는 C≡C이거나, 또는 Y 및 Z는 함께 HC=CH 또는 C≡C이고, R4는 수소, C1-C4알킬, 페닐 또는 아실이고, R5는 수소, C1-C4알킬, CF3, 페닐, 하이드록시, 아미노, 브로모, 요오도 또는 클로로이고, R6은 아실이고, R7은 독립적으로 수소, C1-C4알킬, 페닐 또는 치환된 페닐이고, R8은 C1-C4알킬 또는 테트라졸-5-일이고, n은 0.1 또는 2이고, 단 Y가 NR4, O, S, SO 또는 SO2일때, W는 (CH2)n이고, Z는 CHR7또는 CH이고, 또한 W가 S, SO 또는 SO2일때, Y는 CHR7이고, Z는 CHR7 또는 CH이거나, 또는 Y 및 Z는 함께 HC=CH 또는 C≡C이고, 또한 W 및 Z가 CH2일때, Y가 S가 아니고, 또한 W 및 Y가 함께 HC=CH 또는 C≡C일때, Z는 CHR7이다.
- 제1항에 있어서, 6-[2-(1(2)H-테트라졸-5-일)에틸]데카하이드로이소퀴놀린-3-카복실산 화합물 또는 그의 약학적 허용가능한 염.
- (3S, 4aR, 6R, 8aR)-6-[2(1C2)H-테트라졸-5-일)에틸]데카하이드로 이소퀴놀린-3-카복실산인 화합물 또는 그의 약학적으로 허용가능한 염.
- 하나 이상의 약학적으로 허용가능한 담체, 희석제 또는 부형제와 함께 활성성분으로서 제1항 내지 제3항중 어느 한 항에 청구된 화합물을 포함하는 약학 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US939,780 | 1978-09-05 | ||
| US07/939,780 US5284957A (en) | 1992-09-03 | 1992-09-03 | Excitatory amino acid receptor antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR940007021A true KR940007021A (ko) | 1994-04-26 |
| KR100274367B1 KR100274367B1 (ko) | 2000-12-15 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019930017398A KR100274367B1 (ko) | 1992-09-03 | 1993-09-01 | 흥분성 아미노산 수용체 길항물질 |
Country Status (27)
| Country | Link |
|---|---|
| US (7) | US5284957A (ko) |
| EP (1) | EP0590789B9 (ko) |
| JP (1) | JP3601840B2 (ko) |
| KR (1) | KR100274367B1 (ko) |
| CN (1) | CN1043762C (ko) |
| AT (1) | ATE234287T1 (ko) |
| AU (1) | AU656482B2 (ko) |
| BR (1) | BR9303495A (ko) |
| CA (2) | CA2104909C (ko) |
| CZ (1) | CZ285049B6 (ko) |
| DE (1) | DE69332754T2 (ko) |
| DK (1) | DK0590789T3 (ko) |
| ES (1) | ES2194844T3 (ko) |
| FI (1) | FI933810A (ko) |
| HK (1) | HK1013989A1 (ko) |
| HU (2) | HU224015B1 (ko) |
| IL (1) | IL106809A (ko) |
| MX (1) | MX9305294A (ko) |
| MY (1) | MY131442A (ko) |
| NO (1) | NO304072B1 (ko) |
| NZ (1) | NZ248513A (ko) |
| PH (1) | PH31250A (ko) |
| PL (1) | PL173809B1 (ko) |
| PT (1) | PT590789E (ko) |
| RU (1) | RU2117661C1 (ko) |
| SG (1) | SG45319A1 (ko) |
| ZA (1) | ZA936231B (ko) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2087812B1 (es) * | 1993-07-02 | 1997-03-16 | Lilly Co Eli | Derivados de decahidroisoquinolina utiles como antagonistas de los receptrores de los aminoacidos excitadores. |
| US5580877A (en) * | 1994-04-25 | 1996-12-03 | Merck Sharp & Dohme Ltd. | Pyrazolo-quinoline derivatives for treating cerebral ischemia |
| US5446051A (en) * | 1994-05-31 | 1995-08-29 | Eli Lilly And Company | Aryl-spaced decahydroisoquinoline-3-carboxylic acids as excitatory amino acid receptor antagonists |
| US5723414A (en) * | 1996-01-24 | 1998-03-03 | Rohm And Haas Company | 5-aryl-isoxazolinones and herbicidal use thereof |
| PT807633E (pt) * | 1996-05-15 | 2003-02-28 | Pfizer | Novas pirimidin-4-onas substituidas em 2,3, e fundidas com heteroarilo em (5,6) |
| DE69722613T2 (de) | 1996-05-15 | 2004-05-13 | Pfizer Inc. | 2,3,6-trisubstituierte 4(3h)-chinazolinone |
| AU734657B2 (en) | 1997-04-07 | 2001-06-21 | Eli Lilly And Company | Pharmacological agents |
| US6627755B1 (en) | 1997-06-09 | 2003-09-30 | Pfizer Inc | Quinazolin-4-one AMPA antagonists |
| US6323208B1 (en) | 1997-09-05 | 2001-11-27 | Pfizer Inc | Atropisomers of 2,3-disubstituted-(5.6)-heteroaryl fused-pyrimidin-4-ones |
| IL125950A0 (en) * | 1997-09-05 | 1999-04-11 | Pfizer Prod Inc | Methods of administering ampa receptor antagonists to treat dyskinesias associated with dopamine agonist therapy |
| WO1999044612A1 (en) | 1998-03-02 | 1999-09-10 | Cocensys, Inc. | Substituted quinazolines and analogs and the use thereof |
| WO2001002367A2 (en) * | 1999-07-06 | 2001-01-11 | Eli Lilly And Company | Diester prodrugs of a decahydroisoquinoline-3-carboxylic acid |
| EA004290B1 (ru) * | 1999-07-06 | 2004-02-26 | Эли Лилли Энд Компани | СЕЛЕКТИВНЫЕ АНТАГОНИСТЫ РЕЦЕПТОРА iGluR5 ДЛЯ ЛЕЧЕНИЯ МИГРЕНИ |
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| DK704488D0 (da) * | 1988-12-19 | 1988-12-19 | Novo Industri As | Nye n-substituerede azaheterocykliske carboxylsyrer |
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| US5192751A (en) * | 1992-07-24 | 1993-03-09 | Eli Lilly And Company | Use of competitive NMDA receptor antagonists in the treatment of urinary incontinence |
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1992
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