http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-035493-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c902faf6ae746c51fc8010672fc22894 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 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/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 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/A61P25-20 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/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/G06T3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 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/A61P25-20 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/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-28 |
| filingDate | 2001-09-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-06-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-035493-A1 |
| titleOfInvention | DERIVATIVES OF AZEPINO (4,5B) INDOLINA SUBSTITUTED, PHARMACEUTICAL COMPOSITION AND THE USE OF SUCH DERIVATIVES TO PREPARE A MEDICINAL PRODUCT |
| abstract | Substituted azepino [4,5b] indoline derivatives, comprising a compound of Formula (1) in which R 1 is selected from the group consisting of hydrogen, C 1-8 alkyl and C 1-8 hydrocarbylene, each R 2 independently is selected from group consisting of C1-8 alkyl, and OH; R3 is hydrogen, C1-8 alkyl, Ar, Het, R7C (= O) -, R7OC (= O) -, R5R6NC (= O) -, R7C (= S) -, R7SC (= O) -, R5R6NC ( = S) -, R7SO2-, R5R6NSO2, R7S (= O) -, R5R6NS (= O) -, Rc hydrocarbylene C1-8, or Rc hydrocarbylene C1-8 C (= O) -; each R4, independently, is selected from the group consisting of Ar, C1-8 alkyl, ArO-, C1-8 alkoxy, Het, halo, OH, CN, NO2, CF3, CF3O, NRaRb, N = CRaRb, R7S, hydrocarbylene C1-8 Ar, and C1-8 ORa hydrocarbylene; each R 5 and R 6 is independently hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 1-8 haloalkyl, C 3-8 cycloalkenyl, Ar, or C 1-8 hydrocarbylene; or R5 and R6 together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino, or thiomorpholino ring, each R7 is independently hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C1-8 haloalkyl, C3-8 cycloalkenyl, Ar, or C1-8 hydrocarbylene Ar, Ra and Rb, independently, are selected from the group consisting of hydrogen, C1-8 alkyl, Ar, C1-3 Ar hydrocarbylene, SO2Ar, SO2 C1-4 alkyl, (C3-8 cycloalkyl) C1-8 alkyl, and Het; Rc is Ar, Het, R7CO2-, R7C (= O) -, R7OC (= O) -, R7O-, R7 C1-8 alkylene O-, R7S-, R7C (= S) -, R7S (= O) - , R7S (= O) 2-, R7SC (= O) -, R7C (= O) N (R7) -, R7C (= S) N (R7) -, R5R6N-, R5R6NC (= O) -, R5R6NC ( = S) -, R5R6NS (= O) -, R5R6NSO2-, R7S (= O) N (R7) -, R7SO2N (R7) -, or R7N (R7) C (= O) N (R7) -; each Ar is independently aryl or heteroaryl; p is 0, 1, 2, 3, or 4; and q is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; where Ar of R1, R3- R7, Ra, Rb and Rc is optionally substituted with one or more (for example 1, 2, 3, 4 or 5) substituents independently selected from halo, CN, NO2, ORe, methylenedioxy, ethylenedioxy, CF3, OCF3, SRe, SO2Re, NRfRg, CONRfRg, CORe, Re and hydrocarbylene Rd C1-8, each Rd is independently hydroxy, C1-8 alkoxy, cyano, SRh or C (= O) Rh, each Re is independently selected from group consisting of hydrogen, C1-8 alkyl, Ar, hydrocarbylene C1-3 Ar, SO2Ar, SO2 C1-4 alkyl, (C3-8 cycloalkyl) C1-8 alkyl and Het; where any Ar de Re is optionally substituted with one or more (for example 1, 2, 3, 4 or 5) substituents independently selected from halo, CN, NO2, ORd, methylenedioxy, ethylenedioxy, CF3, OCF3, SRf, SO2Rf, NRfRg , CONRfRg, CORf, Rf and hydrocarbylene Rd C1-8; each Rf and Rg is independently selected from the group consisting of hydrogen, C1-8 alkyl, Ar, hydrocarbylene Ar C1-3, SO2Ar, SO2 C1-4 alkyl, (C3-8 cycloalkyl) C1-8 alkyl and Het; and each Rh is independently hydrogen, C 1-8 alkyl, C 2-8 alkenyl, C 2-8 alkynyl, C 1-8 halolalkyl, C 3-8 cycloalkenyl, phenyl or C 1-8 hydrocarbylene (phenyl); or a pharmaceutically acceptable salt thereof; with the proviso that when (a) R1 is methyl; and (b) R3 hydrogen or - (CH2) 3NR5R6, where, R5 and R6 are each methyl; then p and q are not each 0, and pharmaceutical compositions containing said compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and / or conditions of a mammal in which the activity of a 5-HT receptor is involved. The compounds and salts are particularly useful for treating diseases of the central nervous system. It also refers to the use of such derivatives to prepare useful medications for treating a disease of the central nervous system. |
| priorityDate | 2000-09-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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