http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EA-001002-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D493-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-93 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D493-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-93 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D493-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4035 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-535 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-048 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-343 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4525 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-495 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4465 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4523 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-443 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-445 |
| filingDate | 1997-04-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_aeb75a5e0d22f7924875aafa6e44664d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5c007c0e46d541bbffe24e61f7e4da1a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0e63f0b7aed744c7357ac51f86bf33b5 |
| publicationDate | 2000-08-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EA-001002-B1 |
| titleOfInvention | SUBSTITUTED TETRACYCLIC DERIVATIVES OF TETRAHYDROFURANE |
| abstract | 1. A compound of formula a N-oxide form thereof, 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; R<1> and R<2> each independently are hydrogen; C1-6 alkyl; C1-6 alkylcarbonyl; halomethylcarbonyl; C1-6 alkyl substituted with hydroxy, C1-6 alkyloxy group, carboxyl, C1-6 alkylcarbonyloxy, C1-6 alkyloxycarbonyl or aryl; or R<1> and R<2> taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or a radical of formula: wherein: R<9>, R<10>, R<11> and R<12> each independently are hydrogen, halo, halomethyl, or C1-6 alkyl; m is zero, 1, 2, or 3; R<13>, R<14>, R<15> and R<16> each independently are hydrogen, C1-6alkyl, aryl or arylcarbonyl; or R<15> and R<16> taken together may form a bivalent radical C4-5alkanediyl; R<17> is hydrogen; C1-6 alkyl; C1-6 alkylcarbonyl; halomethylcarbonyl; C1-6 alkyloxycarbonyl; aryl; di(aryl)methyl; C1-6 alkyl substituted with hydroxy, C1-6 alkyloxy, carboxyl, C1-6 alkylcarbonyloxy, C1-6 alkyloxycarbonyl or aryl; each R<3> independently is halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6 alkyl)amino group, C1-6 alkylcarbonylamino group, aminosulfonyl, mono- or di(C1-6 alkyl)aminosulfonyl, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylcarbonyl, C1-6 alkyloxycarbonyl; each R<4> independently is halo, cyano, hydroxy, halomethyl, halomethoxy, carboxyl, nitro, amino, mono- or di(C1-6 alkyl)amino group, C1-6 alkylcarbonylamino group, aminosulfonyl, mono- or di(C1-6 alkyl)aminosulfonyl, C1-6 alkyl, C1-6 alkyloxy, C1-6 alkylcarbonyl, C1-6 alkyloxycarbonyl; each R<5> independently is C1-6 alkyl, cyano or halomethyl; X is CR<6>R<7>, NR<8>, O, S, S(=O) or S(=O)2; wherein R<6> and R<7> each independently are hydrogen, hydroxy, C1-6 alkyl, halomethyl, C1-6 alkyloxy, or R<6> and R<7> 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, they form carbonyl; R<8> is hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl, arylcarbonyl, aryl C1-6 alkylcarbonyl, C1-6 alkylsulfonyl, arylsulfonyl or aryl C1-6 alkylsulfonyl; aryl is phenyl; or phenyl substituted with 1, 2, or 3 substituents selected from halo, hydroxy, C1-6 alkyl or halomethyl;provided that the compound is other than (a)3, 3a, 8, 12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]furan-2-methanamine and (b) (+-)-3, 3a,8,12b-tetrahydro-N-methyl-2H-dibenzo[3,4:6,7]-cyclohepta[1,2-b]furan-2-methanamine oxalic acid. 2. A compound as claimed in claim 1, wherein R<13>, R<14>, R<15> and R<16> each independently are hydrogen or C1-6 alkyl. 3. A compound as claimed in any of claims 1-2, wherein X is CR<6>R<7> or O. 4. A compound as claimed in any of claims 1-3, wherein R<1> and R<2> both are C1-6 alkyl or R<1> and R<2> taken together with the nitrogen atom to which they are attached, form a morpholinyl ring; a radical of formula (c) or a radical of formula (e). 5. A compound as claimed in any of claims 1-4, wherein the substituents on carbon atoms 3a and 12b have the trans-configuration. 6. A compound as claimed in any of claims 1-5, wherein r, p and q are zero. 7. A compound as claimed in any of claims 1-6, wherein p is 1, R<3> is halo, C1-6 alkyl or C1-6 alkyloxy. 8. A compound as claimed in any of claims 1-6, wherein q is 1, R<4> is halo, C1-6 alkyl or C1-6 alkyloxy. 9. A compound as claimed in claim 1, wherein 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 thereof or a pharmaceutically acceptable addition salt thereof, or an N-oxide form thereof. 10. A composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound as claimed in any of claims 1-9. 11. The use of a compound as claimed in any of claims 1-9 for treatment or prevention of central nerve system disorders. 12. A process of preparing a compound as described in claim 1, characterized in that: an intermediate of formula (II) is N-alkylated with an intermediate of formula (III): wherein in the intermediates (II) and (III) radicals from R<1> to R<5>, n, p, q, r and X are defined as in claim 1, and W is a suitable leaving group; in a reaction-inert solvent and, optionally, in the presence of a suitable base; 13. A method as claimed in claim 12, characterised in that one prepared compound is converted into another using art-known transformations, and further, if desired, converting the compounds of formula (I), into a therapeutically active non-toxic acid addition salts by treatment with an acid, or into a therapeutically active non-toxic base addition salt by treatment with a base, or conversely, converting the acid addition salt form into the free base by treatment with alkali, or converting the base addition salt into the free acid by treatment with acid; and, if desired, preparing stereochemically isomeric forms thereof or N-oxide forms thereof. |
| priorityDate | 1996-04-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 129.