http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-057990-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D407-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4164 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
| filingDate | 2006-11-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2008-01-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-057990-A1 |
| titleOfInvention | IMIDAZOLINS 4,4,5,5 TETRASUSTITUIDAS AND A PROCESS FOR SYNTHESIS |
| abstract | The compounds described show activity as antitumor agents. These imidazolines are inhibitors of the interaction between P53 and MDM2 (proteins). Claim 1: A compound of formula (1), wherein X1 and X2 are halogen, acetylene, cyano, trifluoromethyl or nitro; R1 and R2 are selected from the group consisting of -H, -CH3, - CH2CH3, -CH2OH and -CH2OCH3 with the proviso that they are not both hydrogen; R3 is -H or -C (= O) -R7; and when R6 is hydrogen then, R4 is -OCH3, -OCH2CH3, -OCH2CH2F, -OCH2CH2OCH3, or -OCH (CH3) 2; R5 is -H, -halogen, -CH3, -CF3, -OCH3, -C (CH3) 2, -cyclopropyl, cyano, -C (CH3) 3, -C (CH3) 2OR (where R is -H , -CH3, -CH2-CH3, -C (CH3) 2CH-OR (where R is -H, -CH3, -CH (CH3) 2, -CH2CH2OH or - CH2CH2OCH3), -C (CH3) 2CN, -C (CH3) 2COR (where R is -CH3), -C (CH3) 2COOR (where R is -H, -CH3, -CH2CH3 or -CH- (CH3) 2), -C (CH3 ) 2CONRaRb (where Ra is -H, -CH3, and Rb is -H or -CH3), -SR (where R is -CH3 or -CH2CH3), or -SO2R (where R is - CH3 , -CH2CH3, 1-pyrrolidine, -NH-tert-butyl or -N (CH3) 2); and when R6 is not hydrogen then R4 is -OCH3, -OCH2CH3, -OCH2CH2F, -OCH2CH2OCH3, or -OCH (CH3) 2; R5 is hydrogen, -CI, -OCH3, tert-butyl or -N (CH3) 2; R6 is -CI, cyclopropyl, -SO2R (where R is -CH3, -CH2CH3, 1-pyrrolidine, -NH -terc-butyl, -NH2, or -N (CH3) 2); and R7 is selected from the group consisting of i) -CH3, -CH (CH3) 2, -CH2CH (CH3) 2, cyclopropyl, cyclobutyl, - CH2CH2Ph, 2-furanyl, phenyl or phenyl substituted by chlorine, -OCH3 or cyano, ii) 4-morpholinyl, 1-piperidinyl, 4-thiomorpholinyl or 4-thiomorpholinyl-1,1-dioxide, iii) -NRc2 (where Rc is hydrogen, -CH3, -CH2CH3. -CH2CH2OH, -CH2CH2OCH3 or -CH2CH (OH) CH2OH), iv) a substituted piperazine of the formula (2), in which R is selected from the group consisting of a) hydrogen, b) lower alkyl, c) -CH (CH3) 2, d) -CH (CH2CH3) 2, e) cyclopentyl, f) -CH2CH (OH) CH3, g) -CH2CF3, h) -CH2CH (OH) CF3, i) -CH2C (CH3) 2OH, j) -CH2- [4-N-methylpiperidinyl], k) -CH2CH2Rd (where Rd is -OH, -OCH3, -OCH2CH2OH, -OCH2CH2OCH3, -CN, -CF3, -SO2CH3, -SO2NH2, -SO2N ( CH3) 2, -CONH2, -CON (CH3) 2, -NH2, -NHCOCH3, -NHSO2CH3, -N (CH3) 2, -N (CH2CH3) 2, -N (CH2CH2CH3) 2, 1-pyrrolidinyl, 1- piperidinyl, 4-morpholinyl, 2-isothiazolidinyl-1-1-dioxide, or 2-tetrahydrofuranyl), l) -CH2CH2CH2Re (where Re is -OH, -OCH3, -SO2CH3, -SO2CH2CH3, -SO2N (CH3) 2, -CN, -N (CH3) 2, -N (CH2CH2CH3) 2, 1-imidazolyl, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, -COOCH3, -COOCH2CH3, -COOC (CH3) 3, -CON (CH3 ) 2, -CO-Rf (where Rf is -CH3, -CH2CH3, cyclopropyl, phenyl, 2-thienyl, 3-thienyl, 2-furanyl, 3-furanyl), -COCH2-Rg (where Rg is 1-1, -NHCH2CH2OH, -N HCH2CH2OCH3, -NHCH2CH2N (CH3) 2, 1-piperidinyl, 1- (piperidinyl-4-methanol), 4-morpholinyl, or -N (CH3) - (3- (1-methylpyrrolidinyl)), m) CH2CORh (in the that Rh is -OCH3, -OCH2CH3, -NH2, - NHCH2CH (CH3) 2, -NHCH2CF3, -NH-cyclopropyl, -NH-tert-butyl, -NHCH2CH2CH2OH, -N (CH3) 2, -N (CH2CH3) 2 , -N (CH2CH2OH) 2, -N (CH2CH2OCH3) 2, -N (CH3) CH2CH2OH, -N (CH3) CH2CH2OCH3, - NHCH2CH2OCH3, 1-pyrrolidinyl, 1-piperidinyl, 1- (piperidinyl-4-methanol), 1- (piperidinyl-3-carboxamide), 4-morpholinyl, 4-thiomorpholinyl, 4-thiomorpholinyl-1,1-dioxide, 1-piperazinyl, 1- (4-acetylpiperazinyl), 1- (3-oxopiperazinyl), n) -SO2Ri (where Ri is -CH3, -CH2CH3, -CH (CH3) 2, phenyl, 4-methylphenyl, 4-propylphenyl, -CF3, 2-thienyl, 3-thienyl, -NH2, -NHCH3, -N (CH3) 2, -NHCH2CH2OCH3, -N (CH2CH2OCH3) 2, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazil-4-ethanol, 1- (4- acetylpiperazinyl), 1- (3-oxopiperazinyl) ), or) -CORj (where Rj is -CH3, -CH2CH3, -CH (CH3) 2, 2-tetrahydrofuranyl, 2-thienyl, 3-thienyl, -NH2, -NHCH3, -N (CH3) 2,1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl-4-ethanol, 1- (4- acetylpiperazinyl), or 1- (3-oxopiperazinyl)), p) 4-tetrahydro-2H-thiopyranyl-1, 1-dioxide, q) 4-piperidinyl-1-acetyl, r) 4-piperidinyl-1-dimethylcarboxamide, and s) 3-tetrahydro-thiophenyl-1,1-dioxide; v) a substituted oxopiperazine of the formula (3), wherein R is -H, -CH3, -CH2CH3, -CH2CH2CH3, -CH2CH2OH or -CH2CH2OCH3; and vi) a substituted piperidine of the formula (4), in which R is -H, -COOCH3, -COOCH2CH3, -CONH2, -OH, -CH2OH, -CH2CH2OH, -CH2N (CH2CH3) 2, -CH2- ( 1-piperazinyl), -CH2- (1- (3- oxopiperazinyl)), - NH2, -NHCOCH3, -NHCOCH2NH2, -NHCOCH2NHCH3, -NHCOCH2N (CH3) 2, -NHCOCH2N (CH2CH2OH) 2, -NHCOCH2N (CH2CH2N3 (CH2CH2CH3) , -NHCOCH2NHCH2CH2OH, -NHCOCH2- (1- (4-acetylpiperazinyl)), -NHCOCH2- (1- (3-oxopiperazinyl)), -NHCOCH2- (1- piperidinecarboxamide), -NHCOCH2- (N, N-diethyl-1 -piperidinylcarboxamide), -NHCOCH2- (1- (3-hydroxypiperidinyl)), -NHCOCH2- (1- (piperidinyl-4-methanol)), -NHCON (CH3) 2, -NHCSNHCH3, -NHCSNHPh, -NHCH2CONH2, 1 - 1 pyrrolidinyl, 1-piperidinyl, 1- (4- methylpiperazinyl), or 4-morpholinyl; and pharmaceutically acceptable salts and esters thereof. |
| priorityDate | 2005-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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