Title:
特定の縮合ピロールカルボキサニリド類;新種のGABA脳受容体リガンド
Document Type and Number:
Japanese Patent JP3542356
Kind Code:
B2
Abstract:
The present invention encompasses structures of the formula (I) and the pharmaceutically acceptable non-toxic salts thereof wherein T is halogen, hydrogen, hydroxyl, amino or straight or branched chain lower alkoxy having 1-6 carbon atoms; X is hydrogen, hydroxyl or straight or branched chain lower alkyl having 1-6 carbon atoms; W is phenyl substituted with a 3,4-methylenedioxy, 3,4-ethylenedioxy, or 3,4-isopropylidenedioxy group, or a 2-naphthyridinyl group which may be substituted with halogen; and represents wherein Y represents nitrogen or C-R4; Z represents N-R7 or a carbon atom substituted with R8 and R9, i.e., C(R8)(R9); n is 1, 2, 3, or 4; R3 is hydrogen, phenyl, 2, 3 or 4-pyridyl, straight or branched chain lower alkyl having 1-6 carbon atoms, or phenylalkyl or 2, 3 or 4-pyridylalkyl where each alkyl is straight or branched chain lower alkyl having 1-6 carbon atoms; R4 is halogen or trifluoromethyl; or -OR10, - COR10, -CO2R10, -OCOR10, or -R10, where R10 is hydrogen, phenyl, 2, 3 or 4-pyridyl, straight or branched chain lower alkyl having 1-6 carbon atoms, or phenylalkyl or 2, 3 or 4-pyridylalkyl where each alkyl is straight or branched chain lower alkyl having 1-6 carbon atoms; or -CONR11R12 or -(CH2)mNR11R12, where m is 0, 1, or 2; R11 represents hydrogen, straight or branched chain lower alkyl having 1-6 carbon atoms; and R12 is hydrogen, phenyl, 2, 3 or 4-pyridyl, straight or branched chain lower alkyl having 1-6 carbon atoms, or phenylalkyl or 2, 3 or 4-pyridylalkyl where each alkyl is straight or branched chain lower alkyl having 1-6 carbon atoms; or NR11R12 forms a heterocyclic group which is morpholyl, piperidyl, pyrrolidyl, or N-alkyl piperazyl; R5 and R6 are the same or different and represent hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms; R7 is hydrogen, phenyl, 2, 3 or 4-pyridyl, straight or branched chain lower alkyl having 1-6 carbon atoms, or phenylalkyl or 2, 3 or 4-pyridylalkyl where each alkyl is straight or branched chain lower alkyl having 1-6 carbon atoms; R8 is hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; and R9 is -COR13, -CO2R13 or -R13, where R13 is hydrogen, phenyl, 2, 3 or 4-pyridyl, straight or branched chain lower alkyl having 1-6 carbon atoms, or phenylalkyl or 2, 3, or 4-pyridylalkyl where each alkyl is straight or branched chain lower alkyl having 1-6 carbon atoms; or - CONR14R15 or - (CH2)kNR14R15, where k is 0, 1, or 2; R14 represents hydrogen, straight or branched chain lower alkyl having 1-6 carbon atoms; and R15 is hydrogen, phenyl, 2, 3, or 4-pyridyl, straight or branched chain lower alkyl having 1-6 carbon atoms, or phenylalkyl or 2, 3 or 4-pyridylalkyl where each alkyl is straight or branched chain lower alkyl having 1-6 carbon atoms; or NR14R15 forms a heterocyclic group which is morpholyl, piperidyl, pyrrolidyl, or N-alkyl piperazyl; or (b) T and X are as defined above; W is phenyl, 2 or 3-thienyl, 2, 3, or 4-pyridyl or 6-quinolinyl, each of which may be mono or disubstituted with halogen, cyano, hydroxy, straight or branched chain lower alkyl having 1-6 carbon atoms, amino, mono or dialkylamino where each alkyl is independently straight or branched chain lower alkyl having 1-6 carbon atoms, straight or branched chain lower alkoxy having 1-6 carbon atoms, or NR1COR2, COR2, CONR1R2 where R1 and R2 are the same or different and represent hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; and represents or a compound of the formula:
Inventors:
Arbo, Pamela
Hatchson, alan
Hatchson, alan
Application Number:
JP51280795A
Publication Date:
July 14, 2004
Filing Date:
October 26, 1994
Export Citation:
Assignee:
NEUROGEN CORPORATION
International Classes:
A61K31/40; A61K31/403; A61K31/404; A61K31/41; A61K31/4375; A61K31/4439; A61K31/4709; A61K31/55; A61P25/00; A61P25/08; A61P25/20; A61P39/02; A61P43/00; C07D401/12; C07D209/08; C07D209/42; C07D209/52; C07D307/84; C07D401/14; C07D403/12; C07D403/14; C07D405/12; C07D409/04; C07D409/12; C07D413/04; C07D413/12; C07D471/04; C07D471/12; (IPC1-7): C07D209/42; A61K31/403; A61K31/404; A61K31/4375; A61K31/4439; A61K31/4709; A61P25/00; A61P43/00; C07D209/52; C07D401/12; C07D405/12; C07D409/12; C07D471/04
Attorney, Agent or Firm:
Hidekazu Miyoshi
Yasuo Miyoshi
Yasuo Miyoshi