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4-aminoethoxy indolone derivatives
| Details |
Inventors: Mewshaw, Richard Eric;
Assignee: American Home Products Corporation (Madison, NJ)
Primary Examiner: Raymond; Richard L.
Assistant Examiner: Sripada; Pavanaram K.
Attorney, Agent or Firm: Barrett; Rebecca R.
A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or lower alkoxy; R.sub.1 is hydrogen, lower alkyl or aryl(lower)alkyl; R.sub.2 is hydrogen, lower alkyl or --(CH.sub.2).sub.n X.sub.p Ar, where X is oxygen or carbonyl; Ar is cycloalkyl, aryl or arylaryl, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R.sub.1 and R.sub.2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3,4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs. |
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DETAILED DESCRIPTION What is claimed is: 1.
A compound of the formula I: ##STR5## in which: Y is hydrogen, halogen or alkoxy of 1 to 6 carbon atoms; R.
sub.
1 is hydrogen, alkyl of 1 to 6 carbon atoms or arylalkyl of 7 to 12 carbon atoms; R.
sub.
2 is hydrogen, alkyl of 1 to 6 carbon atoms or --(CH.
sub.
2).
sub.
n X.
sub.
p Ar, where X is oxygen or carbonyl; Ar is cycloalkyl of 5 to 7 carbon atoms, aryl of 6 to 12 carbon atoms, haloaryl of 6 to 12 carbon atoms or arylaryl of 12 to 16 carbon atoms, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R.
sub.
1 and R.
sub.
2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl moiety; n is one of the integers 1,2,3,4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof.
2.
A compound of claim 1 in which Y is hydrogen, chlorine, fluorine or alkyl of 1 to 3 carbon atoms; R.
sub.
1 is hydrogen, alkyl of 1 to 3 carbon atoms or arylalkyl of 7 to 8 carbon atoms; R.
sub.
2 is hydrogen, alkyl of 1 to 3 carbon atoms or --(CH.
sub.
2).
sub.
n X.
sub.
p Ar, where X is carbonyl, Ar is cycloalkyl of 5 to 7 carbon atoms, aryl of 6 to 12 carbon atoms, haloaryl of 6 to 12 carbon atoms, biphenyl, oxindolyl or indolyl; or R.
sub.
1 and R.
sub.
2 taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3 or 4; p is 0 or 1; or a pharmaceutically acceptable salt thereof.
3.
The compound of claim 1 which is 4-(2-benzylaminoethoxy)-1,3-dihydro-indol-2-one or a pharmaceutically acceptable salt thereof.
4.
The compound of claim 1 which 4-(2-methylamino-ethoxy)-1,3-dihydro-indol-2-one or a pharmaceutically acceptable salt thereof.
5.
The compound of claim 1 which is 4-(2-amino-ethoxy)-1,3-dihydro-indol-2-one or a pharmaceutically acceptable salt thereof.
6.
The compound of claim 1 which is 7-chloro-4-?2-(4-fluoro-benzylamino)!-ethoxy!-1,3-dihydro-indol-2-one or a pharmaceutically acceptable salt thereof
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Gene Therapy 
