1-arylphthalazine antagonists of excitatory amino acid receptors

US6048853A · kind A · utility

Assignee

• Bearsden Bio, Inc. · US

Inventors

• Mark Anthony Collins · Raleigh, US
• Jeffrey Claude Pelletier · Whitemarsh, US

Key dates

• Filing date: Jan 18, 1996
• Grant date: Apr 11, 2000
• Expiry date: Jan 18, 2016

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D237/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Substituted 1-arylphthalazine compositions with the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently PA2 a) H, PA2 b) HO, PA2 c) R.sup.11 O--, PA2 d) halogen, PA2 e) C1-C3-alkyl, PA2 f) CF.sub.3, PA2 g) R.sup.12 CO.sub.2 --, or PA2 h) R.sup.12 CONH--; PA1 R.sup.1 and R.sup.2, or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 can be taken together to be PA2 a) --OCH.sub.2 O--, or PA2 b) --OCH.sub.2 CH.sub.2 O--; PA1 R.sup.5 is PA2 a) H, PA2 b) C1-C6-alkyl, PA2 c) C3-C6-alkenyl, PA2 d) C3-C6-alkynyl, PA2 e) C3-C6-cycloalkyl, PA2 f) phenyl or substituted phenyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alky, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and CO.sub.2 R.sup.12, or PA2 g) phenyl-C1-C3-alkyl or substituted phenyl-C1-C3-alkyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alkyl, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and --CO.sub.2 R.sup.12 ; PA1 R.sup.6 is PA2 a) R.sup.10 R.sup.11 N--, PA2 b) R.sup.10 NHC(NH)--, PA2 c) R.sup.12 CONH--, PA2 d) 1-pyrrolidino or P…