http://rdf.ncbi.nlm.nih.gov/pubchem/patent/HU-0501212-A2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_7042957c266a740dc593e92ea88eb60e |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-51 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/C07D243-02 |
| filingDate | 2005-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d68a60a8e0867d9af2b2cf7f52e54d1a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_aa9d949b27926eb62d46756fbe2f4a40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b6b7cc53aab3f8ae1b59385e9a3e715e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bbc9693b0016b728715981051e5d7850 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_aeb242eab2bf1063b1e7cd2a1946e3ce http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e52dedb866feb03a4fb367e6f662bbb1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_35e31dc503a6f18e92e27d4f3dd9ceef http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_49b4344069d6e02cfd1db564f14decb8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0c71bd8324f7789882fec5a5c21044d9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ed31c40d28946d4cba5b8e0635ec2476 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a37eb535d6103b480a85e6f07aa21e9d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_76a9ba6c96efc12994a4d40d5f1779b9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b3d86909354ae61710c9afb3cefc463b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb9fefd914e0f802f2c1892a2e9c2955 |
| publicationDate | 2007-09-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | HU-0501212-A2 |
| titleOfInvention | Optical isomers of dihydro-2,3-benzodiazepin, their stereoselective synthesis, pharmaceutical compositions containing them and their use |
| abstract | Enantiomeric dihydro-2,3-benzodiazepine derivatives or their acid addition salts are new. Enantiomeric dihydro-2,3-benzodiazepine derivatives of formula (I) or their acid addition salts are new. X : a halogen or chloro atom, or alkoxy; Y 1halogen or chloro atom; X+Y 1a methylenedioxy group; R : 1-4C alkyl (preferably methyl or ethyl). The configuration of the chiral carbon atom is R or S. Independent claims are included for the following: (1) new intermediate selected from enantiomeric dihydro-2,3-benzodiazepine derivatives of formula (V); enantiomeric benzo[b]pyran derivatives of formula (XII); hydrazone derivatives of formula (XIV); racemic and enantiomeric dihydro-2,3-benzodiazepine derivatives of formula (III); racemic and enantiomeric dihydro-2,3-benzodiazepine compounds of formula (VI); diastereomeric dihydro-2,3-benzodiazepine derivatives having high stereochemical purity of formula (VII); racemic or enantiomeric dihydro-2,3-benzodiazepine compounds of formula (VIII), or their acid addition salts with their optically active acids; (2) a pharmaceutical composition comprising the enantiomeric dihydro-2,3-benzodiazepine derivatives (I) and a carrier; and (3) preparation of the dihydro-2,3-benzodiazepine derivatives (I) (preferably (R)-(-)-7-acetyl-5-(4-amino-3-methylphenyl)-8-methyl-8,9-dihydro-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine; or (R)-(-)-3-acetyl-1-(4-amino-3-methylphenyl)-8-chloro-4-methyl-4,5-dihydro-3H-2,3-benzodiazepine) of high enantiomeric purity. V 1hydrogen atom or hydroxyl; L 1hydroxyl, or alkyl- or aryl-sulfonyl; R aa substituted arylene, alkylene or alkenylene (preferably cis- or trans-alkenylene, especially cis-ethenylene); R 1T 1 (preferably hydrogen atom); R 2T 1 (preferably methyl); R 3T 1 (preferably phenyl); T 1aliphatic or branched saturated or unsaturated alkyl, aryl or aralkyl (all optionally substituted), or hydrogen atom. The hydrazone compounds (XIV) are mixtures of E and Z isomers. [Image] [Image] [Image] [Image] ACTIVITY : Cerebroprotective; Vasotropic; Neuroprotective; Vulnerary; Anticonvulsant; Neuroleptic; Cytostatic; Muscular-Gen.; Relaxant; Antiparkinsonian; Nootropic; Antiinflammatory; CNS-Gen.; Analgesic; Antiemetic; Antimigraine; Antiaddictive; Tranquilizer. MECHANISM OF ACTION : Non-competitive antagonist of amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. The AMPA antagonistic efficacy of (R)-(-)-7-acetyl-5-(4-amino-3-methylphenyl)-8-methyl-8,9-dihydro-7H-1,3-dioxolo[4,5-h][2,3]benzodiazepine (A1) was evaluated in the chicken retina by using Spreading depression test method as described in Sheardown (1993). The compound (A1) was effective AMPA antagonist compound, because the effect of the AMPA receptor was blocked by 1.8 mu M (EC 50) value. |
| priorityDate | 2005-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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