DERIVANTS OF 2, 4, 5-TRIPHENYLIMIDAZOLINE AS INACTIVATORS OF INTERACTION BETWEEN P53 AND MDM2 PROTEINS DESIGNED FOR APPLICATION AS ANTICANCER DRUGS
FIELD: chemistry. ^ SUBSTANCE: present invention refers to the field of organic chemistry, notably to derivatives of dihydroimidazole with the general formula (I) and to its pharmaceutically acceptable salts where X1 and X2 denote halogen; R1 and R2 are chosen from the group including -H, -CH3, -CH2...
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| creator | LOVEJ ALLEN DZHON SO SUNSAU VOVKULICH PITER MAJKL GREJVS BREHDFORD DZHEJMS KONG NORMAN PITSTSOLATO DZHAKOMO DIN TSIN'TSZI ROBERTS DZHON LOSON LJU TSZIN'TSZUN' VU BINKH TKHANKH |
| description | FIELD: chemistry. ^ SUBSTANCE: present invention refers to the field of organic chemistry, notably to derivatives of dihydroimidazole with the general formula (I) and to its pharmaceutically acceptable salts where X1 and X2 denote halogen; R1 and R2 are chosen from the group including -H, -CH3, -CH2CH3 on the condition that both R1 and R2 do not denote hydrogen; R3 denotes -H or -C(=O)-R7; and if R6 denotes hydrogen, then R4 denotes -OCH3, -OCH2CH3 or -OCH(CH3)2; R5 denotes -H, - halogen, -CF3, -OCH3, -C(CH3)2, - cyclopropyl, - cyano group, -C(CH3)3, -C(CH3)2OR (where R denotes -H), -C(CH3)2CH-OR (where R denotes -CH3), -C(CH3)2CN, -C(CH3)2COR (where R denotes -CH3), -SR (where R denotes -CH2CH3) or -SO2R (where R denotes -CH3, -CH2CH3, 1-pyrrolidine, -NH-tert-butyl); and if R6 does not denote hydrogen, then R4 denotes -OCH2CH3; R5 denotes hydrogen, -Cl, -OCH3, tert butyl; R6 denotes -Cl, cyclopropyl, -SO2R (where R denotes -CH3, 1-pyrrolidine, -NH-tert-butyl or -N(CH3)2); and R7 is chosen from the group including i) -CH3, -CH(CH3)2, -CH2CH(CH3)2, cyclopropyl, cyclobutyl, -CH2CH2Ph, 2-furanyl, phenyl or phenyl substituted with chlorine, -OCH3 or cyano group, ii) 1-piperidinyl, iii) -NRcÇè2 (where Rc denotes -CH2CH2OH, -CH2CH2OCH3 or -CH2CH(OH)CH2OH, iv) substituted piperazidine with the formula where R is chosen from the group including a) hydrogen, c) -CH(CH3)2, k) -CH2CH2Rd (where Rd denotes -OH, -OCH3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-morfolinil, 2-izotiazolidinil-1, 1-dioxide), l) -CH2CH2CH2Re (where Re denotes -OCH3, -SO2CH3, -SO2CH2CH3, -CN), m) -CH2-CO-Rh (where Rh denotes -NH2, 1-pyrrolidinyl, 4-morfolinil), n) -SO2Ri (where Ri denotes -CH3, -CH2CH3), o) -CORj (where Rj denotes -CH3, 2-tetrahydrofuranyl, -NH2, -N(CH3)2), p) 4-tetrahydro-2H-thiopiranyl-1,1-dioxide, q) 4-piperidinyl-1-acetyl, r) 4-piperidinyl-1-dimethylcarboxamide, and s) 3-tetrahydrothiophenyl-1,1-dioxide; v) substituted oxopiperazine with the formula where R denotes -H; and vi) substituted piperidine with the formula where R denotes -CONH2, -OH, -CH2OH, -CH2CH2OH, 1-pyrrolidinyl, 1-piperidinyl, 1-(4-methylpiperazinyl) or 4-morfolinil. Moreover, the invention refers to the pharmaceutical composition based on the compound with the formula (I), to application of the formula (I) compound for production of a drug, to the production process of the formula (I) compound. ^ EFFECT: new derivatives of dihydroimidazole that may be used as anticancer drugs. ^ 40 cl, 204 ex
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_RU2442779C2</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>RU2442779C2</sourcerecordid><originalsourceid>FETCH-epo_espacenet_RU2442779C23</originalsourceid><addsrcrecordid>eNqNjUEKwjAURLtxIeod_gHaTayIy5j82g_tT_hJFd2ISFyJCvUmXtgqHsDVMMObmXH2sii01RwDuApUDmUOiyIK-Rp531BLVh9cQ4ygAxBrEwc8OvnyxBHlEzmGNcYdIoNfzEGzhda2Cry4iMQBLAbaMFqonID2viGjv7VhdXgfHBsUsNJtwjQbXU7XPs1-OsmgwmjqIj3ux9Q_Tud0S8-jdKos1XK5Mmr-B_IGDchAcw</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>DERIVANTS OF 2, 4, 5-TRIPHENYLIMIDAZOLINE AS INACTIVATORS OF INTERACTION BETWEEN P53 AND MDM2 PROTEINS DESIGNED FOR APPLICATION AS ANTICANCER DRUGS</title><source>esp@cenet</source><creator>LOVEJ ALLEN DZHON ; SO SUNSAU ; VOVKULICH PITER MAJKL ; GREJVS BREHDFORD DZHEJMS ; KONG NORMAN ; PITSTSOLATO DZHAKOMO ; DIN TSIN'TSZI ; ROBERTS DZHON LOSON ; LJU TSZIN'TSZUN' ; VU BINKH TKHANKH</creator><creatorcontrib>LOVEJ ALLEN DZHON ; SO SUNSAU ; VOVKULICH PITER MAJKL ; GREJVS BREHDFORD DZHEJMS ; KONG NORMAN ; PITSTSOLATO DZHAKOMO ; DIN TSIN'TSZI ; ROBERTS DZHON LOSON ; LJU TSZIN'TSZUN' ; VU BINKH TKHANKH</creatorcontrib><description>FIELD: chemistry. ^ SUBSTANCE: present invention refers to the field of organic chemistry, notably to derivatives of dihydroimidazole with the general formula (I) and to its pharmaceutically acceptable salts where X1 and X2 denote halogen; R1 and R2 are chosen from the group including -H, -CH3, -CH2CH3 on the condition that both R1 and R2 do not denote hydrogen; R3 denotes -H or -C(=O)-R7; and if R6 denotes hydrogen, then R4 denotes -OCH3, -OCH2CH3 or -OCH(CH3)2; R5 denotes -H, - halogen, -CF3, -OCH3, -C(CH3)2, - cyclopropyl, - cyano group, -C(CH3)3, -C(CH3)2OR (where R denotes -H), -C(CH3)2CH-OR (where R denotes -CH3), -C(CH3)2CN, -C(CH3)2COR (where R denotes -CH3), -SR (where R denotes -CH2CH3) or -SO2R (where R denotes -CH3, -CH2CH3, 1-pyrrolidine, -NH-tert-butyl); and if R6 does not denote hydrogen, then R4 denotes -OCH2CH3; R5 denotes hydrogen, -Cl, -OCH3, tert butyl; R6 denotes -Cl, cyclopropyl, -SO2R (where R denotes -CH3, 1-pyrrolidine, -NH-tert-butyl or -N(CH3)2); and R7 is chosen from the group including i) -CH3, -CH(CH3)2, -CH2CH(CH3)2, cyclopropyl, cyclobutyl, -CH2CH2Ph, 2-furanyl, phenyl or phenyl substituted with chlorine, -OCH3 or cyano group, ii) 1-piperidinyl, iii) -NRcÇè2 (where Rc denotes -CH2CH2OH, -CH2CH2OCH3 or -CH2CH(OH)CH2OH, iv) substituted piperazidine with the formula where R is chosen from the group including a) hydrogen, c) -CH(CH3)2, k) -CH2CH2Rd (where Rd denotes -OH, -OCH3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-morfolinil, 2-izotiazolidinil-1, 1-dioxide), l) -CH2CH2CH2Re (where Re denotes -OCH3, -SO2CH3, -SO2CH2CH3, -CN), m) -CH2-CO-Rh (where Rh denotes -NH2, 1-pyrrolidinyl, 4-morfolinil), n) -SO2Ri (where Ri denotes -CH3, -CH2CH3), o) -CORj (where Rj denotes -CH3, 2-tetrahydrofuranyl, -NH2, -N(CH3)2), p) 4-tetrahydro-2H-thiopiranyl-1,1-dioxide, q) 4-piperidinyl-1-acetyl, r) 4-piperidinyl-1-dimethylcarboxamide, and s) 3-tetrahydrothiophenyl-1,1-dioxide; v) substituted oxopiperazine with the formula where R denotes -H; and vi) substituted piperidine with the formula where R denotes -CONH2, -OH, -CH2OH, -CH2CH2OH, 1-pyrrolidinyl, 1-piperidinyl, 1-(4-methylpiperazinyl) or 4-morfolinil. Moreover, the invention refers to the pharmaceutical composition based on the compound with the formula (I), to application of the formula (I) compound for production of a drug, to the production process of the formula (I) compound. ^ EFFECT: new derivatives of dihydroimidazole that may be used as anticancer drugs. ^ 40 cl, 204 ex
Настоящее изобретение относится к области органической химии, а именно к производным дигидроимидазола общей формулы (I) и к его фармацевтически приемлемым солям, где X1 и X2 обозначают галоген; R1 и R2 выбраны из группы, включающей -Н, -СН3, -СН2СН3, при условии, что R1 и R2 оба не обозначают водород; R3 обозначает -Н или -C(=O)-R7; и если R6 обозначает водород, то R4 обозначает -ОСН3, -ОСН2СН3 или -ОСН(СН3)2; R5 обозначает -Н, -галоген, -CF3, -ОСН3, -С(СН3)2, -циклопропил, -цианогруппу, -С(СН3)3, -С(СН3)2OR (где R обозначает -Н), -С(СН3)2СН-OR (где R обозначает -СН3), -С(СН3)2СН, -С(СН3)2COR (где R обозначает -СН3), -SR (где R обозначает -СН2СН3) или -SO2R (где R обозначает -СН3, -СН2СН3, 1-пирролидин, -NH-трет-бутил); и если R6 не обозначает водород, то R4 обозначает -ОСН2СН3; R5 обозначает водород, -Cl, -ОСН3, трет-бутил; R6 обозначает -Cl, циклопропил, -SO2R (где R обозначает -СН3, 1-пирролидин, -NH-трет-бутил или -N(СН3)2); и R7 выбран из группы, включающей i) -СН3, -СН(СН3)2, -СН2СН(СН3)2, циклопропил, циклобутил, -CH2CH2Ph, 2-фуранил, фенил или фенил, замещенный хлором, -ОСН3 или цианогруппой, ii) 1-пиперидинил, iii) -NRc 2 (где Rc обозначает -CH2CH2OH, -CH2CH2OCH3 или -СН2СН(ОН)CH2OH), iv) замещенный пиперазин формулы в которой R выбран из группы, включающей а) водород, с) -СН(СН3)2, k) -CH2CH2Rd (где Rd обозначает -ОН, -ОСН3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-морфолинил, 2-изотиазолидинил-1,1-диоксид), 1) -CH2CH2CH2Re (где Re обозначает -ОСН3, -SO2CH3, -SO2CH2CH3, -CN), m)-CH2-CO-Rh (где Rh обозначает -NH2, 1-пирролидинил, 4-морфолинил), n) -SO2R1 (где Ri обозначает -СН3, -СН2СН3), о) -CORj (где Rj обозначает -СН3, 2-тетрагидрофуранил, -NH2, -N(СН3)2), р) 4-тетрагидро-2Н-тиопиранил-1,1-диоксид, q) 4-пиперидинил-4-ацетил, r) 4-пиперидинил-1-диметилкарбоксамид, и s) 3-тетрагидротиофенил-1,1-диоксид; v) замещенный оксопиперазин формулы в которой R о</description><language>eng ; rus</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2012</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20120220&DB=EPODOC&CC=RU&NR=2442779C2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20120220&DB=EPODOC&CC=RU&NR=2442779C2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>LOVEJ ALLEN DZHON</creatorcontrib><creatorcontrib>SO SUNSAU</creatorcontrib><creatorcontrib>VOVKULICH PITER MAJKL</creatorcontrib><creatorcontrib>GREJVS BREHDFORD DZHEJMS</creatorcontrib><creatorcontrib>KONG NORMAN</creatorcontrib><creatorcontrib>PITSTSOLATO DZHAKOMO</creatorcontrib><creatorcontrib>DIN TSIN'TSZI</creatorcontrib><creatorcontrib>ROBERTS DZHON LOSON</creatorcontrib><creatorcontrib>LJU TSZIN'TSZUN'</creatorcontrib><creatorcontrib>VU BINKH TKHANKH</creatorcontrib><title>DERIVANTS OF 2, 4, 5-TRIPHENYLIMIDAZOLINE AS INACTIVATORS OF INTERACTION BETWEEN P53 AND MDM2 PROTEINS DESIGNED FOR APPLICATION AS ANTICANCER DRUGS</title><description>FIELD: chemistry. ^ SUBSTANCE: present invention refers to the field of organic chemistry, notably to derivatives of dihydroimidazole with the general formula (I) and to its pharmaceutically acceptable salts where X1 and X2 denote halogen; R1 and R2 are chosen from the group including -H, -CH3, -CH2CH3 on the condition that both R1 and R2 do not denote hydrogen; R3 denotes -H or -C(=O)-R7; and if R6 denotes hydrogen, then R4 denotes -OCH3, -OCH2CH3 or -OCH(CH3)2; R5 denotes -H, - halogen, -CF3, -OCH3, -C(CH3)2, - cyclopropyl, - cyano group, -C(CH3)3, -C(CH3)2OR (where R denotes -H), -C(CH3)2CH-OR (where R denotes -CH3), -C(CH3)2CN, -C(CH3)2COR (where R denotes -CH3), -SR (where R denotes -CH2CH3) or -SO2R (where R denotes -CH3, -CH2CH3, 1-pyrrolidine, -NH-tert-butyl); and if R6 does not denote hydrogen, then R4 denotes -OCH2CH3; R5 denotes hydrogen, -Cl, -OCH3, tert butyl; R6 denotes -Cl, cyclopropyl, -SO2R (where R denotes -CH3, 1-pyrrolidine, -NH-tert-butyl or -N(CH3)2); and R7 is chosen from the group including i) -CH3, -CH(CH3)2, -CH2CH(CH3)2, cyclopropyl, cyclobutyl, -CH2CH2Ph, 2-furanyl, phenyl or phenyl substituted with chlorine, -OCH3 or cyano group, ii) 1-piperidinyl, iii) -NRcÇè2 (where Rc denotes -CH2CH2OH, -CH2CH2OCH3 or -CH2CH(OH)CH2OH, iv) substituted piperazidine with the formula where R is chosen from the group including a) hydrogen, c) -CH(CH3)2, k) -CH2CH2Rd (where Rd denotes -OH, -OCH3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-morfolinil, 2-izotiazolidinil-1, 1-dioxide), l) -CH2CH2CH2Re (where Re denotes -OCH3, -SO2CH3, -SO2CH2CH3, -CN), m) -CH2-CO-Rh (where Rh denotes -NH2, 1-pyrrolidinyl, 4-morfolinil), n) -SO2Ri (where Ri denotes -CH3, -CH2CH3), o) -CORj (where Rj denotes -CH3, 2-tetrahydrofuranyl, -NH2, -N(CH3)2), p) 4-tetrahydro-2H-thiopiranyl-1,1-dioxide, q) 4-piperidinyl-1-acetyl, r) 4-piperidinyl-1-dimethylcarboxamide, and s) 3-tetrahydrothiophenyl-1,1-dioxide; v) substituted oxopiperazine with the formula where R denotes -H; and vi) substituted piperidine with the formula where R denotes -CONH2, -OH, -CH2OH, -CH2CH2OH, 1-pyrrolidinyl, 1-piperidinyl, 1-(4-methylpiperazinyl) or 4-morfolinil. Moreover, the invention refers to the pharmaceutical composition based on the compound with the formula (I), to application of the formula (I) compound for production of a drug, to the production process of the formula (I) compound. ^ EFFECT: new derivatives of dihydroimidazole that may be used as anticancer drugs. ^ 40 cl, 204 ex
Настоящее изобретение относится к области органической химии, а именно к производным дигидроимидазола общей формулы (I) и к его фармацевтически приемлемым солям, где X1 и X2 обозначают галоген; R1 и R2 выбраны из группы, включающей -Н, -СН3, -СН2СН3, при условии, что R1 и R2 оба не обозначают водород; R3 обозначает -Н или -C(=O)-R7; и если R6 обозначает водород, то R4 обозначает -ОСН3, -ОСН2СН3 или -ОСН(СН3)2; R5 обозначает -Н, -галоген, -CF3, -ОСН3, -С(СН3)2, -циклопропил, -цианогруппу, -С(СН3)3, -С(СН3)2OR (где R обозначает -Н), -С(СН3)2СН-OR (где R обозначает -СН3), -С(СН3)2СН, -С(СН3)2COR (где R обозначает -СН3), -SR (где R обозначает -СН2СН3) или -SO2R (где R обозначает -СН3, -СН2СН3, 1-пирролидин, -NH-трет-бутил); и если R6 не обозначает водород, то R4 обозначает -ОСН2СН3; R5 обозначает водород, -Cl, -ОСН3, трет-бутил; R6 обозначает -Cl, циклопропил, -SO2R (где R обозначает -СН3, 1-пирролидин, -NH-трет-бутил или -N(СН3)2); и R7 выбран из группы, включающей i) -СН3, -СН(СН3)2, -СН2СН(СН3)2, циклопропил, циклобутил, -CH2CH2Ph, 2-фуранил, фенил или фенил, замещенный хлором, -ОСН3 или цианогруппой, ii) 1-пиперидинил, iii) -NRc 2 (где Rc обозначает -CH2CH2OH, -CH2CH2OCH3 или -СН2СН(ОН)CH2OH), iv) замещенный пиперазин формулы в которой R выбран из группы, включающей а) водород, с) -СН(СН3)2, k) -CH2CH2Rd (где Rd обозначает -ОН, -ОСН3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-морфолинил, 2-изотиазолидинил-1,1-диоксид), 1) -CH2CH2CH2Re (где Re обозначает -ОСН3, -SO2CH3, -SO2CH2CH3, -CN), m)-CH2-CO-Rh (где Rh обозначает -NH2, 1-пирролидинил, 4-морфолинил), n) -SO2R1 (где Ri обозначает -СН3, -СН2СН3), о) -CORj (где Rj обозначает -СН3, 2-тетрагидрофуранил, -NH2, -N(СН3)2), р) 4-тетрагидро-2Н-тиопиранил-1,1-диоксид, q) 4-пиперидинил-4-ацетил, r) 4-пиперидинил-1-диметилкарбоксамид, и s) 3-тетрагидротиофенил-1,1-диоксид; v) замещенный оксопиперазин формулы в которой R о</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2012</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjUEKwjAURLtxIeod_gHaTayIy5j82g_tT_hJFd2ISFyJCvUmXtgqHsDVMMObmXH2sii01RwDuApUDmUOiyIK-Rp531BLVh9cQ4ygAxBrEwc8OvnyxBHlEzmGNcYdIoNfzEGzhda2Cry4iMQBLAbaMFqonID2viGjv7VhdXgfHBsUsNJtwjQbXU7XPs1-OsmgwmjqIj3ux9Q_Tud0S8-jdKos1XK5Mmr-B_IGDchAcw</recordid><startdate>20120220</startdate><enddate>20120220</enddate><creator>LOVEJ ALLEN DZHON</creator><creator>SO SUNSAU</creator><creator>VOVKULICH PITER MAJKL</creator><creator>GREJVS BREHDFORD DZHEJMS</creator><creator>KONG NORMAN</creator><creator>PITSTSOLATO DZHAKOMO</creator><creator>DIN TSIN'TSZI</creator><creator>ROBERTS DZHON LOSON</creator><creator>LJU TSZIN'TSZUN'</creator><creator>VU BINKH TKHANKH</creator><scope>EVB</scope></search><sort><creationdate>20120220</creationdate><title>DERIVANTS OF 2, 4, 5-TRIPHENYLIMIDAZOLINE AS INACTIVATORS OF INTERACTION BETWEEN P53 AND MDM2 PROTEINS DESIGNED FOR APPLICATION AS ANTICANCER DRUGS</title><author>LOVEJ ALLEN DZHON ; SO SUNSAU ; VOVKULICH PITER MAJKL ; GREJVS BREHDFORD DZHEJMS ; KONG NORMAN ; PITSTSOLATO DZHAKOMO ; DIN TSIN'TSZI ; ROBERTS DZHON LOSON ; LJU TSZIN'TSZUN' ; VU BINKH TKHANKH</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_RU2442779C23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; rus</language><creationdate>2012</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>LOVEJ ALLEN DZHON</creatorcontrib><creatorcontrib>SO SUNSAU</creatorcontrib><creatorcontrib>VOVKULICH PITER MAJKL</creatorcontrib><creatorcontrib>GREJVS BREHDFORD DZHEJMS</creatorcontrib><creatorcontrib>KONG NORMAN</creatorcontrib><creatorcontrib>PITSTSOLATO DZHAKOMO</creatorcontrib><creatorcontrib>DIN TSIN'TSZI</creatorcontrib><creatorcontrib>ROBERTS DZHON LOSON</creatorcontrib><creatorcontrib>LJU TSZIN'TSZUN'</creatorcontrib><creatorcontrib>VU BINKH TKHANKH</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>LOVEJ ALLEN DZHON</au><au>SO SUNSAU</au><au>VOVKULICH PITER MAJKL</au><au>GREJVS BREHDFORD DZHEJMS</au><au>KONG NORMAN</au><au>PITSTSOLATO DZHAKOMO</au><au>DIN TSIN'TSZI</au><au>ROBERTS DZHON LOSON</au><au>LJU TSZIN'TSZUN'</au><au>VU BINKH TKHANKH</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>DERIVANTS OF 2, 4, 5-TRIPHENYLIMIDAZOLINE AS INACTIVATORS OF INTERACTION BETWEEN P53 AND MDM2 PROTEINS DESIGNED FOR APPLICATION AS ANTICANCER DRUGS</title><date>2012-02-20</date><risdate>2012</risdate><abstract>FIELD: chemistry. ^ SUBSTANCE: present invention refers to the field of organic chemistry, notably to derivatives of dihydroimidazole with the general formula (I) and to its pharmaceutically acceptable salts where X1 and X2 denote halogen; R1 and R2 are chosen from the group including -H, -CH3, -CH2CH3 on the condition that both R1 and R2 do not denote hydrogen; R3 denotes -H or -C(=O)-R7; and if R6 denotes hydrogen, then R4 denotes -OCH3, -OCH2CH3 or -OCH(CH3)2; R5 denotes -H, - halogen, -CF3, -OCH3, -C(CH3)2, - cyclopropyl, - cyano group, -C(CH3)3, -C(CH3)2OR (where R denotes -H), -C(CH3)2CH-OR (where R denotes -CH3), -C(CH3)2CN, -C(CH3)2COR (where R denotes -CH3), -SR (where R denotes -CH2CH3) or -SO2R (where R denotes -CH3, -CH2CH3, 1-pyrrolidine, -NH-tert-butyl); and if R6 does not denote hydrogen, then R4 denotes -OCH2CH3; R5 denotes hydrogen, -Cl, -OCH3, tert butyl; R6 denotes -Cl, cyclopropyl, -SO2R (where R denotes -CH3, 1-pyrrolidine, -NH-tert-butyl or -N(CH3)2); and R7 is chosen from the group including i) -CH3, -CH(CH3)2, -CH2CH(CH3)2, cyclopropyl, cyclobutyl, -CH2CH2Ph, 2-furanyl, phenyl or phenyl substituted with chlorine, -OCH3 or cyano group, ii) 1-piperidinyl, iii) -NRcÇè2 (where Rc denotes -CH2CH2OH, -CH2CH2OCH3 or -CH2CH(OH)CH2OH, iv) substituted piperazidine with the formula where R is chosen from the group including a) hydrogen, c) -CH(CH3)2, k) -CH2CH2Rd (where Rd denotes -OH, -OCH3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-morfolinil, 2-izotiazolidinil-1, 1-dioxide), l) -CH2CH2CH2Re (where Re denotes -OCH3, -SO2CH3, -SO2CH2CH3, -CN), m) -CH2-CO-Rh (where Rh denotes -NH2, 1-pyrrolidinyl, 4-morfolinil), n) -SO2Ri (where Ri denotes -CH3, -CH2CH3), o) -CORj (where Rj denotes -CH3, 2-tetrahydrofuranyl, -NH2, -N(CH3)2), p) 4-tetrahydro-2H-thiopiranyl-1,1-dioxide, q) 4-piperidinyl-1-acetyl, r) 4-piperidinyl-1-dimethylcarboxamide, and s) 3-tetrahydrothiophenyl-1,1-dioxide; v) substituted oxopiperazine with the formula where R denotes -H; and vi) substituted piperidine with the formula where R denotes -CONH2, -OH, -CH2OH, -CH2CH2OH, 1-pyrrolidinyl, 1-piperidinyl, 1-(4-methylpiperazinyl) or 4-morfolinil. Moreover, the invention refers to the pharmaceutical composition based on the compound with the formula (I), to application of the formula (I) compound for production of a drug, to the production process of the formula (I) compound. ^ EFFECT: new derivatives of dihydroimidazole that may be used as anticancer drugs. ^ 40 cl, 204 ex
Настоящее изобретение относится к области органической химии, а именно к производным дигидроимидазола общей формулы (I) и к его фармацевтически приемлемым солям, где X1 и X2 обозначают галоген; R1 и R2 выбраны из группы, включающей -Н, -СН3, -СН2СН3, при условии, что R1 и R2 оба не обозначают водород; R3 обозначает -Н или -C(=O)-R7; и если R6 обозначает водород, то R4 обозначает -ОСН3, -ОСН2СН3 или -ОСН(СН3)2; R5 обозначает -Н, -галоген, -CF3, -ОСН3, -С(СН3)2, -циклопропил, -цианогруппу, -С(СН3)3, -С(СН3)2OR (где R обозначает -Н), -С(СН3)2СН-OR (где R обозначает -СН3), -С(СН3)2СН, -С(СН3)2COR (где R обозначает -СН3), -SR (где R обозначает -СН2СН3) или -SO2R (где R обозначает -СН3, -СН2СН3, 1-пирролидин, -NH-трет-бутил); и если R6 не обозначает водород, то R4 обозначает -ОСН2СН3; R5 обозначает водород, -Cl, -ОСН3, трет-бутил; R6 обозначает -Cl, циклопропил, -SO2R (где R обозначает -СН3, 1-пирролидин, -NH-трет-бутил или -N(СН3)2); и R7 выбран из группы, включающей i) -СН3, -СН(СН3)2, -СН2СН(СН3)2, циклопропил, циклобутил, -CH2CH2Ph, 2-фуранил, фенил или фенил, замещенный хлором, -ОСН3 или цианогруппой, ii) 1-пиперидинил, iii) -NRc 2 (где Rc обозначает -CH2CH2OH, -CH2CH2OCH3 или -СН2СН(ОН)CH2OH), iv) замещенный пиперазин формулы в которой R выбран из группы, включающей а) водород, с) -СН(СН3)2, k) -CH2CH2Rd (где Rd обозначает -ОН, -ОСН3, -CF3, -SO2CH3, -NH2, -NHCOCH3, -NHSO2CH3, 4-морфолинил, 2-изотиазолидинил-1,1-диоксид), 1) -CH2CH2CH2Re (где Re обозначает -ОСН3, -SO2CH3, -SO2CH2CH3, -CN), m)-CH2-CO-Rh (где Rh обозначает -NH2, 1-пирролидинил, 4-морфолинил), n) -SO2R1 (где Ri обозначает -СН3, -СН2СН3), о) -CORj (где Rj обозначает -СН3, 2-тетрагидрофуранил, -NH2, -N(СН3)2), р) 4-тетрагидро-2Н-тиопиранил-1,1-диоксид, q) 4-пиперидинил-4-ацетил, r) 4-пиперидинил-1-диметилкарбоксамид, и s) 3-тетрагидротиофенил-1,1-диоксид; v) замещенный оксопиперазин формулы в которой R о</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
| title | DERIVANTS OF 2, 4, 5-TRIPHENYLIMIDAZOLINE AS INACTIVATORS OF INTERACTION BETWEEN P53 AND MDM2 PROTEINS DESIGNED FOR APPLICATION AS ANTICANCER DRUGS |
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