http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1407769-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0d269c8e41f178194d858c230c9f85e3 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-42 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-42 |
filingDate | 2002-10-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9cd0023d97b42645b84557ab4deb6566 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c4568e95a8f38fd251ac39c617fba1c8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ea6408278af45e34c99ab96b59d6377e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b677f69c12e78982e759681cd30a34db http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fa6d8b508c4764e1a6d7d2dc3559038d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4456af5dcb2e9178323b8221a89c3afe |
publicationDate | 2004-04-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | EP-1407769-A1 |
titleOfInvention | Indole derivatives as beta-2 agonists |
abstract | Indole derivatives (I) are new. Indole derivatives of formula (I) and their salts and/or isomers, tautomers, solvates and isotopic variations are new. [Image] n : 0-4; R1, R2H or 1-4C alkyl; R3H or 1-6C alkyl optionally substituted by OH, and R4-R8H , OH, 1-6C alkyl, 1-6C alkoxy, 1-6C hydroxyalkyl, 1-6C thioalkyl, halo or trifluoromethyl. Independent claims are also included for (1) preparation of (I); (2) intermediate acid compounds of formula (II), and (3) intermediate ester compounds of formula (IV). [Image] Ra>acid protecting 1-4C alkyl. ACTIVITY : Antiasthmatic; Antiallergic; Antibacterial; Fungicide; Protozoacide; Virucide; Respiratory-Gen.; Antiinflammatory; Hypotensive; Antidepressant; Neuroprotective; Nootropic; Antiparkinsonian; Muscular-Gen.; Antiarteriosclerotic; Anticonvulsant; Tocolytic; Cardiovascular-Gen.; CNS-Gen.; Dermatological; Antipsoriatic; Ophthalmological; Antiulcer; Gastrointestinal-Gen. MECHANISM OF ACTION : beta -2 agonist. In a n assay using Chinese hamster ovary cells recombinantly expressing the human beta -2 adrenergic receptor, results showed that (I) e.g. 5-[(2R)-2-([(2R)-2-hydroxy-2-[4-hydroxy-3-(hydroxymethyl)phenyl]ethyl]amino)propyl]-N-(2-methoxybenzyl)-1H-indole-2-carboxamide (Ia) exhibited a beta -2 Cyclic Adenosine Monophosphate EC50 values of 0.02-0.9 nM. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7737126-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-7985740-B2 |
priorityDate | 2002-10-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 535.