Claims
- 1. A method of treating a central nervous system disorder in a warm-blooded animal in need thereof comprising administering to the warm-blooded animal a therapeutically effective amount of a compound of formula (I) a N-oxide form, a pharmaceutically acceptable addition salt or a stereochemically isomeric form thereof, wherein:n is zero, 1, 2, 3, 4, 5, or 6; p is zero, 1, 2, 3 or 4; q is zero, 1, 2, 3 or 4; r is zero, 1, 2, 3, 4 or 5; R1 and R2 each independently are hydrogen; C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or a radical of formula: wherein: R9, R10, R11 and R12 each independently are hydrogen, halo, halomethyl, or C1-6alkyl; m is zero, 1, 2, or 3; R13, R14, R15 and R16 each independently are hydrogen, C1-6alkyl, aryl or arylcarbonyl; or R15 and R16 taken together may form a bivalent radical C4-5alkanediyl; R17 is hydrogen; C1-6alkyl; C1-6alkylcarbonyl; halomethylcarbonyl; C1-6alkyloxycarbonyl; aryl; di(aryl)methyl; C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; each R3 independently is halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R4 independently is halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6alkyl)amino, C1-6alkylcarbonylamino, aminosulfonyl, mono- or di(C1-6alkyl)aminosulfonyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl; each R5 independently is C1-6alkyl, cyano or halomethyl; X is CR6R7, NR8, O, S, S(═O) or S(═O)2; wherein R6 and R7 each independently are hydrogen, hydroxy, C1-6alkyl, halomethyl, C1-6alkyloxy or R6 and R7 taken together may form methylene; mono- or di(cyano)methylene; a bivalent radical of formula —(CH2)2—, —(CH2)3—, —(CH2)4—, —(CH2)5—, —O—(CH2)2—O—, —O—(CH2)3—O—; or, together with the carbon atom to which they are attached, a carbonyl; R8 is hydrogen, C1-6alkyl, C1-6alkylcarbonyl, arylcarbonyl, arylC1-6alkylcarbonyl, C1-6alkylsulfonyl, arylsulfonyl or arylC1-6alkylsulfonyl; aryl is phenyl; or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl;provided that the compound is other than (±)-3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]furan-2-methanamine oxalic acid.
- 2. The method of claim 1 wherein the compound is other than 3,3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]furan-2-methanamine.
- 3. The method of claim 2 wherein R13, R14, R15 and R16 each independently are hydrogen or C1-6alkyl.
- 4. The method of claim 3 wherein X is CR6R7 or O.
- 5. The method of claim 5 wherein R1 and R2 both are C1-6alkyl or R1 and R2 are taken together with the nitrogen atom to which they are attached and form a morpholinyl ring; a radical of formula (c) or a radical of formula (e).
- 6. The method of claim 5 wherein the substituents on carbon atoms 3a and 12b have the trans configuration.
- 7. The method of claim 6 wherein r, p and q are zero.
- 8. The method of claim 6 wherein p is 1 and R3 is halo, C1-6alkyl or C1-6alkyloxy.
- 9. The method of claim 6 wherein q is 1 and R4 is halo, C1-6alkyl or C1-6alkyloxy.
- 10. The method of claim 1 wherein the compound is 3,3a,8,12b-tetrahydro-N,N-dimethyl-2H-dibenzo[3,4:6,7]cyclohepta[1,2-b]furan-2-methanamine; a stereochemically isomeric form or a pharmaceutically acceptable addition salt thereof, or an N-oxide form thereof.
- 11. The method of claim 1 wherein the disorder is selected from the group consisting of anxiety, depression, mild depression, bipolar disorder, sleep-disorder, sexual disorder, psychosis, borderline psychosis, schizophrenia, migraine, personality disorder, obsessive-compulsive disorder, social phobia, panic attack, organic mental disorder, mental disorder in children, aggression, memory disorder, attitude disorder in older people, addiction, obesity, bulimia, and addictive properties of drugs of abuse.
- 12. The method of claim 1 wherein the disorder is selected from the group consisting of anxiety, psychosis, depression, migraine and addictive properties of drugs of abuse.
Priority Claims (1)
Number |
Date |
Country |
Kind |
96200990 |
Apr 1996 |
EP |
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CROSS REFERENCE TO RELATED APPLICATIONS
This application is a continuation of application Ser. No. 09/155,840, filed Oct. 6, 1998 U.S. Pat. No. 6,057,441, which was a National Stage application under 35 U.S.C. § 371 of PCT/EP97/01829, filed Apr. 9, 1997, which claims priority from EP 96.200.990.8, filed Apr. 12, 1996.
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Continuations (1)
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Number |
Date |
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Parent |
09/155840 |
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US |
Child |
09/533625 |
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US |