http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-20010082510-A
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-08 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/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-18 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/A61P21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F7-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D521-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-28 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/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D223-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D223-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 |
| filingDate | 2000-08-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4adcd31e3b2ff98f8bcc39b8eb11755a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2e6de93399b16fca8512d7b71b40edec http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d1b625e5fb6dbd07db96e144cad27535 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_950de802da23d33641f68d1e4492a703 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0924238925f2d489ab6de51c25dbd740 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8f6977df5a366198752fcb938255a3f3 |
| publicationDate | 2001-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | KR-20010082510-A |
| titleOfInvention | 1,2,4,5-tetrahydro-benzo[d]azepines |
| abstract | The present invention relates to pharmaceutically acceptable salts of 1,2,4,5-tetrahydro-benzo [d] azepine derivatives of the general formula (1) or racemic and optically active forms thereof:n n n n n n n n n n Wheren n n R 1 is hydrogen, lower alkyl, oxygen, halogen; Or -OR, -O (C 3 -C 6 ) cycloalkyl, -O (CHR) n- (C 3 -C 6 ) cycloalkyl, -O (CHR) n CN, -O (CHR) n CF 3 , -O (CHR) (CHR) n NR 2 , -O (CHR) (CHR) n OR, -O (CHR) n -lower alkenyl, -OCF 3 , -OCF 2 -R, -OCF 2 -lower egg Kenyl, -OCHRF, -OCHF-lower alkenyl, -OCF 2 CRF 2 , -OCF 2 Br, -O (CHR) n CF 2 Br, -O (CHR) n -phenyl, wherein the phenyl group is optionally 1 to Three lower alkyl, lower alkoxy, halogen, nitro or cyano groups may be substituted independently of one another), -O (CHR) (CHR) n -morpholino, -O (CHR) (CHR) n- Pyrrolidino, -O (CHR) (CHR) n -piperidino, -O (CHR) (CHR) n -imidazolo, -O (CHR) (CHR) n -triazolo, -O (CHR) n -pyridino, —O (CHR) (CHR) n —OSi-lower alkyl, —O (CHR) (CHR) n OS (O) 2 —lower alkyl, —O (CH 2 ) n CH = CF 2 , -O (CHR) n -2,2-dimethyl- [1,3] dioxolane, -O (CHR) n -CHOR-CH 2 OR, -O (CHR) n -CHOR- (CHR) n -CH 2 OR; Or -SR or -S (CHR) n COOR; Or -NR 2 , -N (R) (CHR) (CHR) n OR, -N (R) (CHR) n CF 3 , -N (R) (CHR) (CHR) n -morpholino, -N (R) (CHR) (CHR) n -imidazolo, -N (R) (CHR) (CHR) n -pyrrolidino, -N (R) (CHR) (CHR) n -pyrrolidine-2 -On, -N (R) (CHR) (CHR) n -piperidino, -N (R) (CHR) (CHR) n -triazolo, -N (R) (CHR) n -pyridino and;n n n n is 1 to 6;n n n R, independently of one another when one or more R is present, means hydrogen, lower alkyl or lower alkenyl;n n n R 2 means nitro or cyano;n n n R 3 is piperazino optionally substituted with hydrogen, lower alkyl, ═O, ═S, —SR, —S (O) 2 —lower alkyl, — (C 3 -C 6 ) cycloalkyl, or lower alkyl; Or -CONR 2 ,-(CHR) n CONR 2 ,-(CHR) n OR,-(CH 2 ) n -CF 3 , -CF 3 ,-(CHR) n OC (O) CF 3 ,-(CHR) n COOR,-(CHR) n SC 6 H 5 , wherein the phenyl group can be optionally substituted independently of one another by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups,-(CHR ) n -1,3-dioxo-1,3-dihydro-isoindole,-(CHR) n -tetrahydro-pyran-2-yloxy or-(CHR) n -S-lower alkyl; Or -NR 2 , -NRCO-lower alkyl, -NRCHO, -N (R) (CHR) n CN, -N (R) (CHR) n CF 3 , -N (R) (CHR) (CHR) n- OR, -N (R) C (O) (CHR) n O-lower alkyl, -N (R) (CHR) n -lower alkyl, -N (R) (CHR) (CHR) n -OR, -N (R) (CHR) (CHR) n- O-phenyl, wherein the phenyl group may be optionally substituted independently of one another by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups,- N (R) (CHR) n -lower alkenyl, -N (R) (CHR) (CHR) n -O- (CHR) n OR, -N (R) (CHR) n C (O) O-lower Alkyl, -N (R) (CHR) n C (O) NR-lower alkyl, -N (R) (CH 2 ) n -2,2-dimethyl- [1,3] dioxolane, -N (R) (CHR) (CHR) n morpholino, -N (R) (CHR) n -pyridino, -N (R) (CHR) (CHR) n -piperidino, -N (R) (CHR) ( CHR) n -pyrrolidino, -N (R) (CHR) (CHR) n -O-pyridino, -N (R) (CHR) (CHR) n imidazolo, -N (R) (CHR) n -CR 2- (CHR) n -OR, -N (R) (CHR) n -CR 2 -OR, -N (R) (CHR) n -CHOR-CH 2 OR, -N (R) (CHR ) n -CHOR- (CHR) n -CH 2 OR; Or —OR, —O (CHR) n CF 3 , —OCF 3 , —O (CHR) (CHR) n —O-phenyl, wherein the phenyl group optionally comprises 1 to 3 lower alkyl, lower alkoxy, halogen, nitro Or a cyano group, each independently), -O (CHR) (CHR) n- O-lower alkyl, -O (CHR) n -pyridino or -O (CHR) (CHR) n- Morpholino;n n n R 4 is hydrogen, lower alkyl, lower alkenyl or nitro; Or -OR, -OCF 3 , -OCF 2 -R, -OCF 2 -lower alkenyl, -OCHRF, -OCHF-lower alkenyl, -O (CHR) n CF 3 ; Or-(CHR) n CHRF,-(CHR) n CF 2 R,-(CHR) n CF 3 ,-(C 3 -C 6 ) cycloalkyl,-(CHR) n (C 3 -C 6 ) cycloalkyl -(CHR) n CN,-(CHR) n -phenyl, wherein the phenyl group may be optionally substituted independently of one another by one to three lower alkyl, lower alkoxy, halogen, nitro or cyano groups, -(CHR) (CHR) n OR,-(CHR) n CHORCH 2 OR,-(CHR) (CHR) n NR 2 ,-(CHR) n COOR,-(CHR) (CHR) n OSi-lower alkyl, -(CHR) (CHR) n -OS (O) 2 -lower alkyl,-(CH 2 ) n -CH = CF 2 , -CF 3 , -CF 2 -R, -CF 2 -lower alkenyl, -CHRF , -CHF-lower alkenyl,-(CHR) n -2,2-dimethyl- [1,3] dioxolane,-(CH 2 ) n -2-oxo-azpan-1-yl,-(CHR) (CHR) n -morpholino,-(CHR) n -pyridino,-(CHR) (CHR) n -imidazolo,-(CHR) (CHR) n -triazolo,-(CH 2 ) n OH optionally substituted by - (CHR) (CHR) n-pyrrolidino, - (CHR) (CHR) n -3- hydroxy-pyrrolidino or - (CHR) (CHR) n-piperidino; Or -NR 2 , -N (R) (CHR) n -pyridino, -N (R) C (O) O-lower alkyl, -N (CH 2 CF 3 ) C (O) O-lower alkyl,- N [C (O) O-lower alkyl] 2 , -NR-NR-C (O) O-lower alkyl, or -N (R) (CHR) n CF 3 , -NRCF 3 , -NRCF 2 -R,- NRCF 2 -lower alkenyl, -NRCHRF, -NRCHF-lower alkenyl; Or absent when X is -N = or = N-; Or R 4 and R 1 or R 3 and R 4 are group-(CH 2 ) 3-5 -,-(CH 2 ) 2 -N =, -CH = NN =, -CH = CH-N =, -NH Interconnected to —CH═CH— or —NR—CH 2 —CH 2 — and together with the N and C atoms to which they are attached form an additional ring;n n n R 5 and R 6 mean hydrogen, lower alkyl, lower alkoxy, amino, nitro, —SO 2 NH 2 or halogen; orn n n R 5 and R 6 are interconnected to the group —O—CH 2 —O and together with the C atom to which they are attached form an additional 5-membered ring;n n n R 7 and R 8 mean hydrogen, lower alkyl, lower alkoxy, amino, nitro or halogen;n n n R 9 and R 10 mean hydrogen or lower alkyl;n n n R 11 and R 12 mean hydrogen, lower alkyl, hydroxy, lower alkoxy, lower alkoxycarbonyloxy or lower alkanoyloxy;n n n R 13 and R 14 mean hydrogen, tritium or lower alkyl;n n n R 15 and R 16 mean hydrogen, tritium, lower alkyl, hydroxy, lower alkoxy, lower alkoxycarbonyloxy or lower alkanoyloxy, or together form an oxo group;n n n X means -N =, = N-, -N <,> C = or = C <;n n n Y means -N =, = N-, -NH-, -CH = or = CH-;n n n The dotted line may be a bond.n n n Surprisingly, compounds of formula 1 have been found to be useful in the treatment of diseases associated with these receptors because they are antagonists at metabotropic glutamate receptors. |
| priorityDate | 1999-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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