HUP0400570A2 - Feniletenil- vagy feniletinil-heteroaril-származékok mint glutamát receptor antagonisták, alkalmazásuk, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Feniletenil- vagy feniletinil-heteroaril-származékok mint glutamát receptor antagonisták, alkalmazásuk, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0400570A2 HUP0400570A2 HU0400570A HUP0400570A HUP0400570A2 HU P0400570 A2 HUP0400570 A2 HU P0400570A2 HU 0400570 A HU0400570 A HU 0400570A HU P0400570 A HUP0400570 A HU P0400570A HU P0400570 A2 HUP0400570 A2 HU P0400570A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- hydrogen atom
- alkyl
- alkyl group
- atom
- Prior art date
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- 238000002360 preparation method Methods 0.000 title abstract 3
- 238000000034 method Methods 0.000 title abstract 2
- -1 Phenylethenyl Chemical group 0.000 title 1
- 239000003825 glutamate receptor antagonist Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 14
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 14
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 abstract 5
- 125000005843 halogen group Chemical group 0.000 abstract 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 102000012777 Metabotropic Glutamate 5 Receptor Human genes 0.000 abstract 1
- 108010065028 Metabotropic Glutamate 5 Receptor Proteins 0.000 abstract 1
- 125000001589 carboacyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
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- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
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- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/14—Ortho-condensed systems
Abstract
A találmány tárgya (I) általános képletű vegyületek[mely képletbenRl, R2, R3, R4 és R5 jelentése egymástól függetlenül hidrogénatom, 1-6szénatomos alkil-, -(CH2)n halogén-, 1-6 szénatomos alkoxi-, -(CH2)nNRR1, -(CH2)n-N(R)-C(O)-1-6 szénatomos alkil-, aril-csoport vagyhelyettesítetlen vagy egy vagy több 1-6 szénatomos alkilcsoporttalhelyettesített heteroaril-csoport; R, R' és R" jelentése egymástólfüggetlenül hidrogénatom vagy 1-6 szénatomos alkilcsoport; A jelentése-CH=CH- vagy -C<C-; és B jelentése (Bl), (B2), (B3), (B4), (B5) vagy(B6) általános képletű csoport; ahol R6 jelentése hidrogénatom, 1-6szénatomos alkilcsoport, -(CH2)n-C(O)OR csoport vagy halogénatom; R7jelentése hidrogénatom, 1-6 szénatomos alkilcsoport, -(CH2)n-C(O)OR'csoport, halogénatom, nitrocsoport vagy helyettesítetlen vagy 1-6szénatomos alkil- vagy cikloalkilcsoporttal helyettesített heteroaril-csoport; R8 jelentése hidrogénatom, 1-6 szénatomos alkilcsoport, -(CH2)n-OH, -(CH2)n-C(O)OR" csoport vagy arilcsoport; R9 jelentése 1-6szénatomos alkilcsoport; Rl0 jelentése hidrogénatom, 1-6 szénatomosalkilcsoport vagy halogénatom; Rl1 jelentése hidrogénatom vagy 1-6szénatomos alkilcsoport; R12 jelentése -(CH2)n-N(R)-C(O)-(1-6szénatomos)- alkilcsoport; R13 jelentése hidrogénatom vagy 1-6szénatomos alkilcsoport; R14, R15, R16 és Rl7 jelentése egymástólfüggetlenül hidrogénatom, 1-6 szénatomos alkilcsoport, -(CH2)nhalogéncsoport vagy 1-6 szénatomos alkoxicsoport; R18, Rl9 és R20jelentése egymástól függetlenül hidrogénatom, 1-6 szénatomosalkilcsoport, -(CH2)n halogéncsoport vagy 1-6 szénatomosalkoxicsoport; R21 jelentése hidrogénatom vagy 1-6 szénatomosalkilcsoport; R22 jelentése hidrogénatom, 1-6 szénatomos alkilcsoportvagy egy vagy több hidroxilcsoporttal és/vagy halogénatommalhelyettesített 1-6 szénatomos alkilcsoport; R23 jelentésehidrogénatom, 1-6 szénatomos alkil-, 1-6 szénatomos alkanoil- vagynitrocsoport; R24, R25 és R26 jelentése egymástól függetlenülhidrogénatom vagy 1-6 szénatomos alkilcsoport] és gyógyászatilagalkalmas sóik felhasználása mGluR5 receptor által közvetítettrendellenességek kezelésére vagy megelőzésére alkalmas gyógyászatikészítmények előállítására. A találmány kiterjed a vegyületekelőállítási eljárására is. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP00126615 | 2000-12-04 | ||
PCT/EP2001/013714 WO2002046166A1 (en) | 2000-12-04 | 2001-11-26 | Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP0400570A2 true HUP0400570A2 (hu) | 2004-06-28 |
HUP0400570A3 HUP0400570A3 (en) | 2004-09-28 |
Family
ID=8170567
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0400570A HUP0400570A3 (en) | 2000-12-04 | 2001-11-26 | Phenylethenyl or phenylethinyl heteroaril derivatives as glutamate receptor antagonists, their use, process for their preparation and pharmaceutical compositions containing them |
Country Status (32)
Country | Link |
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US (4) | US6706707B2 (hu) |
EP (1) | EP1349839B8 (hu) |
JP (2) | JP4077317B2 (hu) |
KR (1) | KR100515549B1 (hu) |
CN (1) | CN1257894C (hu) |
AR (1) | AR035401A1 (hu) |
AT (1) | ATE288898T1 (hu) |
AU (2) | AU2956702A (hu) |
BG (1) | BG107877A (hu) |
BR (1) | BR0115871A (hu) |
CA (1) | CA2430696C (hu) |
CZ (1) | CZ20031795A3 (hu) |
DE (1) | DE60108900T2 (hu) |
DK (1) | DK1349839T3 (hu) |
EC (1) | ECSP034640A (hu) |
ES (1) | ES2248410T3 (hu) |
HK (1) | HK1063318A1 (hu) |
HR (1) | HRP20030429A2 (hu) |
HU (1) | HUP0400570A3 (hu) |
IL (2) | IL155999A0 (hu) |
MA (1) | MA26971A1 (hu) |
MX (1) | MXPA03004862A (hu) |
NO (1) | NO324326B1 (hu) |
NZ (1) | NZ525917A (hu) |
PL (1) | PL366222A1 (hu) |
PT (1) | PT1349839E (hu) |
RS (1) | RS43903A (hu) |
RU (1) | RU2284323C9 (hu) |
SI (1) | SI1349839T1 (hu) |
SK (1) | SK8402003A3 (hu) |
WO (1) | WO2002046166A1 (hu) |
ZA (1) | ZA200303870B (hu) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8536229B2 (en) | 2001-12-04 | 2013-09-17 | Novartis Ag | Acetylene derivatives having MGluR 5 antagonistic activity |
Families Citing this family (48)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2004014881A2 (en) | 2002-08-09 | 2004-02-19 | Astra Zeneca Ab | '1,2,4'oxadiazoles as modulators of metabotropic glutamate receptor-5 |
EP1581525A2 (en) | 2002-08-09 | 2005-10-05 | AstraZeneca AB | Compounds having an activity at metabotropic glutamate receptors |
MXPA05001592A (es) * | 2002-08-09 | 2005-05-05 | Astrazeneca Ab | Oxadiazoles como moduladores de receptor-5 de glutamato metabotropico. |
ITMI20030151A1 (it) * | 2003-01-30 | 2004-07-31 | Recordati Ind Chimica E Farma Ceutica S P A | Uso di antagonisti selettivi del recettore mglu5 per il trattamento di disfunzioni neuromuscolari del tratto urinario inferiore. |
PT1603877E (pt) | 2003-03-04 | 2009-02-11 | Addex Pharma Sa | Novos derivados de aminopiridina como antagonistas de mglur5 |
JP4610480B2 (ja) | 2003-03-07 | 2011-01-12 | アステラス製薬株式会社 | 2,6−ジ置換スチリルを有する含窒素ヘテロ環誘導体 |
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US8536229B2 (en) | 2001-12-04 | 2013-09-17 | Novartis Ag | Acetylene derivatives having MGluR 5 antagonistic activity |
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