http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-031858-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_afc5d8c9ee6673323cee3e2d19bc5146 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D223-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D223-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-10 |
| filingDate | 2001-07-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2003-10-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-031858-A1 |
| titleOfInvention | ESPIROBENZOAZEPINAS SUBSTITUTED NON-PEPTIDIC, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USE OF SUCH COMPOUNDS IN THE MANUFACTURE OF MEDICINES, PROCESS TO PREPARE SUCH COMPOSITIONS AND INTERMEDIARY USES IN THE PREPARATION OF SUCH COMPOUNDS |
| abstract | Non-peptide substituted spirobenzoazepines of Formula (1) or its optical isomers, enantiomers, diastereomers, racemates, or pharmaceutically acceptable salts, wherein: R1 is one to three members independently selected from hydrogen, halogen, amino, substituted amino, hydroxy, alkyloxy , phenyl, substituted phenyl, alkylthio, arylthio, alkyl sulfoxide, aryl sulfoxide, alkyl sulfone, and aryl sulfone; -R2-R3- is -N (C (O) R ') - CH2- or -CH2-N (C (O) R') -, where R 'is selected from alkyl, substituted alkyl, phenyl, substituted phenyl, heteroaryl, substituted heteroaryl, and -Bp-G-Eq-W wherein B is selected from (CH2) m, NH and O; G is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; E is O, S, NH, (CH2) iN (R ") CO or (CH2) iCONR" wherein R "is selected from hydrogen, alkyl and substituted alkyl; W is one to three members independently selected from hydrogen, alkyl, substituted alkyl, amino, substituted amino, alkylthiophenyl, alkyl-sulfoxidophenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; p is independently 0 or 1; q is independently 0 or 1; m is independently 1, 2 or 3; and i is independently 0, 1, 2 or 3; R4 is one or two members independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, phenyl and substituted phenyl; R5 is selected from hydrogen, alkyl, substituted alkyl, aldehyde, carboxyl, alkoxycarbonyl, substituted alkoxycarbonyl, - (CH2) kNZ1Z2 and -CONZ1Z2 wherein k is an integer of 1-4, and Z1 and Z2 are independently selected from hydrogen, alkyl , substituted alkyl, heterocyclyl, substituted heterocyclyl, aminocarbonyl and substituted aminocarbonyl, or N, Z1 and Z2 together form heterocyclyl, substituted heterocyclyl, heteroaryl or substituted heteroaryl; a represents a single or double bond provided that when R1 is iodine, bromine, alkylthio, arylthio, alkyl sulfone or aryl sulfone, a is a double bond; A is selected from aryl, naphthyl and heteroaryl; X is selected from CH, CH2, CHOH and C = O; and n is 1, 2 or 3. These compounds are useful as antagonists of vasopressin receptors to treat conditions associated with vasopressin receptor activity such as those involving increased vascular resistance and heart failure. Also described are pharmaceutical compositions comprising said compounds, the use of such compounds in the manufacture of medicaments to treat conditions such as hypertension, congestive heart failure, heart failure, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal insufficiency, cerebral edema and ischemia, apopletic attack, thrombosis or water retention, a process for preparing said pharmaceutical composition and useful intermediates in the preparation of such compounds. |
| priorityDate | 2001-07-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 26.