ANNELATED AZAHETEROCYCLIC AMIDES, WHICH INCLUDE PYRIMIDINE FRAGMENT, METHOD OF OBTAINING AND THEIR APPLICATION
FIELD: chemistry. ^ SUBSTANCE: present invention relates to new annelated azaheterocyclic amides, including a pyrimidine fragment, with the general formula 1, method of obtaining them and their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of P13K kinas...
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creator | IVASHCHENKO ALEKSANDR VASIL'EVICH KHVAT ALEKSANDR VIKTOROVICH KRAVCHENKO DMITRIJ VLADIMIROVICH SAVCHUK NIKOLAJ FILIPPOVICH TKACHENKO SERGEJ EVGEN'EVICH ALJAB'EV SERGEJ BORISOVICH RYZHOVA ELENA ALEKSANDROVNA OKUN' IL'JA MATUSOVICH IVASHCHENKO ANDREJ ALEKSANDROVICH |
description | FIELD: chemistry. ^ SUBSTANCE: present invention relates to new annelated azaheterocyclic amides, including a pyrimidine fragment, with the general formula 1, method of obtaining them and their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of P13K kinase, in compounds with the general formula 1: , where: X represents an oxygen atom, sulphur atom or not necessarily substituted at the nitrogen NH group, where the substitute is selected from lower alkyls and possibly a substituted aryl; Y represents an atom of nitrogen or substituted at the carbon atom CH group, where the substitute is selected from lower alkyls; Z represents an oxygen atom; R1 represents a hydrogen atom or not necessarily substituted C1-C6alkyl, or Z represents a nitrogen atom, which is together with a carbon atom, with which it is joined, form through Z and R1 annelated imidazole cycle; R2 and R3 independently from each other represent hydrogen, not necessarily substituted with C1-C6alkyl, C3-C6cycloalkyl, not necessarily substituted with phenyl, not necessarily substituted with 6-member aza-heteroaryl, under the condition, when Y represents a nitrogen atom, or R2 and R3 independently from each other represent not necessarily substituted C1-C6alkyl, not necessarily substituted with phenyl, not necessarily substituted with 5-7-member heterocycle with 1-2 heteroatoms, selected from nitrogen and oxygen, and possibly annelated with a phenyl ring, under the condition, when Y does not necessarily represent a substituted carbon atom at the CH group, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents a substituted aminoC1-C6alkyl and not necessarily substituted 5-6-member aza-heterocycloalkyl, under the condition, when Y represents a group which is substituted at the CH atom, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents phenyl which is not necessarily substituted, pyridyl which is not necessarily substituted, pyrimidinyl which is not necessarily substituted, under the conditions, when R1 represents a substituted aminoC1-C6alkyl, substituted C2-C3hydroxyalkyl and aza-heterocycloalkyl not necessarily substituted, Y represents a group with CH substituted, and X represents an oxygen atom, sulphur, and the substitute of the above indicated substituted alkyl, phenyl, heterocycle, pyridyl, pyrimidyl are selected from groups of hydroxyl-, cyano-groups, hydrogen, lower alkyl |
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fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_RU2345996C1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>RU2345996C1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_RU2345996C13</originalsourceid><addsrcrecordid>eNqNjDsKwkAQQNNYiHqHOUAs_ELKcXeSHUhmwzpBYhOCrJXEQLw_pvAAVq94j7dMBhShEpUs4B0dKQVvWlOyAazY0jWFm2PjgMWUjSWo28CzYCHIAxYViaZQkTpvwefgL4osLAWgWFBHHADrev6hspd1snj2ryluflwlkJMat43ju4vT2D_iED9daPaH4ynLzmZ3-CP5AuIqNts</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>ANNELATED AZAHETEROCYCLIC AMIDES, WHICH INCLUDE PYRIMIDINE FRAGMENT, METHOD OF OBTAINING AND THEIR APPLICATION</title><source>esp@cenet</source><creator>IVASHCHENKO ALEKSANDR VASIL'EVICH ; KHVAT ALEKSANDR VIKTOROVICH ; KRAVCHENKO DMITRIJ VLADIMIROVICH ; SAVCHUK NIKOLAJ FILIPPOVICH ; TKACHENKO SERGEJ EVGEN'EVICH ; ALJAB'EV SERGEJ BORISOVICH ; RYZHOVA ELENA ALEKSANDROVNA ; OKUN' IL'JA MATUSOVICH ; IVASHCHENKO ANDREJ ALEKSANDROVICH</creator><creatorcontrib>IVASHCHENKO ALEKSANDR VASIL'EVICH ; KHVAT ALEKSANDR VIKTOROVICH ; KRAVCHENKO DMITRIJ VLADIMIROVICH ; SAVCHUK NIKOLAJ FILIPPOVICH ; TKACHENKO SERGEJ EVGEN'EVICH ; ALJAB'EV SERGEJ BORISOVICH ; RYZHOVA ELENA ALEKSANDROVNA ; OKUN' IL'JA MATUSOVICH ; IVASHCHENKO ANDREJ ALEKSANDROVICH</creatorcontrib><description>FIELD: chemistry. ^ SUBSTANCE: present invention relates to new annelated azaheterocyclic amides, including a pyrimidine fragment, with the general formula 1, method of obtaining them and their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of P13K kinase, in compounds with the general formula 1: , where: X represents an oxygen atom, sulphur atom or not necessarily substituted at the nitrogen NH group, where the substitute is selected from lower alkyls and possibly a substituted aryl; Y represents an atom of nitrogen or substituted at the carbon atom CH group, where the substitute is selected from lower alkyls; Z represents an oxygen atom; R1 represents a hydrogen atom or not necessarily substituted C1-C6alkyl, or Z represents a nitrogen atom, which is together with a carbon atom, with which it is joined, form through Z and R1 annelated imidazole cycle; R2 and R3 independently from each other represent hydrogen, not necessarily substituted with C1-C6alkyl, C3-C6cycloalkyl, not necessarily substituted with phenyl, not necessarily substituted with 6-member aza-heteroaryl, under the condition, when Y represents a nitrogen atom, or R2 and R3 independently from each other represent not necessarily substituted C1-C6alkyl, not necessarily substituted with phenyl, not necessarily substituted with 5-7-member heterocycle with 1-2 heteroatoms, selected from nitrogen and oxygen, and possibly annelated with a phenyl ring, under the condition, when Y does not necessarily represent a substituted carbon atom at the CH group, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents a substituted aminoC1-C6alkyl and not necessarily substituted 5-6-member aza-heterocycloalkyl, under the condition, when Y represents a group which is substituted at the CH atom, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents phenyl which is not necessarily substituted, pyridyl which is not necessarily substituted, pyrimidinyl which is not necessarily substituted, under the conditions, when R1 represents a substituted aminoC1-C6alkyl, substituted C2-C3hydroxyalkyl and aza-heterocycloalkyl not necessarily substituted, Y represents a group with CH substituted, and X represents an oxygen atom, sulphur, and the substitute of the above indicated substituted alkyl, phenyl, heterocycle, pyridyl, pyrimidyl are selected from groups of hydroxyl-, cyano-groups, hydrogen, lower alkyls, possibly mono- or di-substituted lower alkyl sulfamoyl, carbamoyl, C1-C6alkoxycarbonyl, amino, mono- or di-lower alkyl-amine, N-(lower alkyl), N-(phenylC1-C6alkyl)amine, phenyl, possibly substituted with a halogen atom, C1-C6alkyl, haloid-C1-C6alkyl; phenylC1-C6alkyl, saturated or non-saturated 5-6-member heterocycle containing 1-2-heteroatoms, selected from nitrogen, oxygen and sulphur, and possible condensation with a benzene ring R4 represents hydrogen or a lower alkyl. ^ EFFECT: obtaining new annelated aza-heterocyclic amides, including a pyrimidine fragment, with the general formula with the possibility of their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of PI3K kinase. ^ 16 cl, 5 tbl, 5 ex</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>2009</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=20090210&DB=EPODOC&CC=RU&NR=2345996C1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76290</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20090210&DB=EPODOC&CC=RU&NR=2345996C1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>IVASHCHENKO ALEKSANDR VASIL'EVICH</creatorcontrib><creatorcontrib>KHVAT ALEKSANDR VIKTOROVICH</creatorcontrib><creatorcontrib>KRAVCHENKO DMITRIJ VLADIMIROVICH</creatorcontrib><creatorcontrib>SAVCHUK NIKOLAJ FILIPPOVICH</creatorcontrib><creatorcontrib>TKACHENKO SERGEJ EVGEN'EVICH</creatorcontrib><creatorcontrib>ALJAB'EV SERGEJ BORISOVICH</creatorcontrib><creatorcontrib>RYZHOVA ELENA ALEKSANDROVNA</creatorcontrib><creatorcontrib>OKUN' IL'JA MATUSOVICH</creatorcontrib><creatorcontrib>IVASHCHENKO ANDREJ ALEKSANDROVICH</creatorcontrib><title>ANNELATED AZAHETEROCYCLIC AMIDES, WHICH INCLUDE PYRIMIDINE FRAGMENT, METHOD OF OBTAINING AND THEIR APPLICATION</title><description>FIELD: chemistry. ^ SUBSTANCE: present invention relates to new annelated azaheterocyclic amides, including a pyrimidine fragment, with the general formula 1, method of obtaining them and their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of P13K kinase, in compounds with the general formula 1: , where: X represents an oxygen atom, sulphur atom or not necessarily substituted at the nitrogen NH group, where the substitute is selected from lower alkyls and possibly a substituted aryl; Y represents an atom of nitrogen or substituted at the carbon atom CH group, where the substitute is selected from lower alkyls; Z represents an oxygen atom; R1 represents a hydrogen atom or not necessarily substituted C1-C6alkyl, or Z represents a nitrogen atom, which is together with a carbon atom, with which it is joined, form through Z and R1 annelated imidazole cycle; R2 and R3 independently from each other represent hydrogen, not necessarily substituted with C1-C6alkyl, C3-C6cycloalkyl, not necessarily substituted with phenyl, not necessarily substituted with 6-member aza-heteroaryl, under the condition, when Y represents a nitrogen atom, or R2 and R3 independently from each other represent not necessarily substituted C1-C6alkyl, not necessarily substituted with phenyl, not necessarily substituted with 5-7-member heterocycle with 1-2 heteroatoms, selected from nitrogen and oxygen, and possibly annelated with a phenyl ring, under the condition, when Y does not necessarily represent a substituted carbon atom at the CH group, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents a substituted aminoC1-C6alkyl and not necessarily substituted 5-6-member aza-heterocycloalkyl, under the condition, when Y represents a group which is substituted at the CH atom, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents phenyl which is not necessarily substituted, pyridyl which is not necessarily substituted, pyrimidinyl which is not necessarily substituted, under the conditions, when R1 represents a substituted aminoC1-C6alkyl, substituted C2-C3hydroxyalkyl and aza-heterocycloalkyl not necessarily substituted, Y represents a group with CH substituted, and X represents an oxygen atom, sulphur, and the substitute of the above indicated substituted alkyl, phenyl, heterocycle, pyridyl, pyrimidyl are selected from groups of hydroxyl-, cyano-groups, hydrogen, lower alkyls, possibly mono- or di-substituted lower alkyl sulfamoyl, carbamoyl, C1-C6alkoxycarbonyl, amino, mono- or di-lower alkyl-amine, N-(lower alkyl), N-(phenylC1-C6alkyl)amine, phenyl, possibly substituted with a halogen atom, C1-C6alkyl, haloid-C1-C6alkyl; phenylC1-C6alkyl, saturated or non-saturated 5-6-member heterocycle containing 1-2-heteroatoms, selected from nitrogen, oxygen and sulphur, and possible condensation with a benzene ring R4 represents hydrogen or a lower alkyl. ^ EFFECT: obtaining new annelated aza-heterocyclic amides, including a pyrimidine fragment, with the general formula with the possibility of their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of PI3K kinase. ^ 16 cl, 5 tbl, 5 ex</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>2009</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjDsKwkAQQNNYiHqHOUAs_ELKcXeSHUhmwzpBYhOCrJXEQLw_pvAAVq94j7dMBhShEpUs4B0dKQVvWlOyAazY0jWFm2PjgMWUjSWo28CzYCHIAxYViaZQkTpvwefgL4osLAWgWFBHHADrev6hspd1snj2ryluflwlkJMat43ju4vT2D_iED9daPaH4ynLzmZ3-CP5AuIqNts</recordid><startdate>20090210</startdate><enddate>20090210</enddate><creator>IVASHCHENKO ALEKSANDR VASIL'EVICH</creator><creator>KHVAT ALEKSANDR VIKTOROVICH</creator><creator>KRAVCHENKO DMITRIJ VLADIMIROVICH</creator><creator>SAVCHUK NIKOLAJ FILIPPOVICH</creator><creator>TKACHENKO SERGEJ EVGEN'EVICH</creator><creator>ALJAB'EV SERGEJ BORISOVICH</creator><creator>RYZHOVA ELENA ALEKSANDROVNA</creator><creator>OKUN' IL'JA MATUSOVICH</creator><creator>IVASHCHENKO ANDREJ ALEKSANDROVICH</creator><scope>EVB</scope></search><sort><creationdate>20090210</creationdate><title>ANNELATED AZAHETEROCYCLIC AMIDES, WHICH INCLUDE PYRIMIDINE FRAGMENT, METHOD OF OBTAINING AND THEIR APPLICATION</title><author>IVASHCHENKO ALEKSANDR VASIL'EVICH ; KHVAT ALEKSANDR VIKTOROVICH ; KRAVCHENKO DMITRIJ VLADIMIROVICH ; SAVCHUK NIKOLAJ FILIPPOVICH ; TKACHENKO SERGEJ EVGEN'EVICH ; ALJAB'EV SERGEJ BORISOVICH ; RYZHOVA ELENA ALEKSANDROVNA ; OKUN' IL'JA MATUSOVICH ; IVASHCHENKO ANDREJ ALEKSANDROVICH</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_RU2345996C13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; rus</language><creationdate>2009</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>IVASHCHENKO ALEKSANDR VASIL'EVICH</creatorcontrib><creatorcontrib>KHVAT ALEKSANDR VIKTOROVICH</creatorcontrib><creatorcontrib>KRAVCHENKO DMITRIJ VLADIMIROVICH</creatorcontrib><creatorcontrib>SAVCHUK NIKOLAJ FILIPPOVICH</creatorcontrib><creatorcontrib>TKACHENKO SERGEJ EVGEN'EVICH</creatorcontrib><creatorcontrib>ALJAB'EV SERGEJ BORISOVICH</creatorcontrib><creatorcontrib>RYZHOVA ELENA ALEKSANDROVNA</creatorcontrib><creatorcontrib>OKUN' IL'JA MATUSOVICH</creatorcontrib><creatorcontrib>IVASHCHENKO ANDREJ ALEKSANDROVICH</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>IVASHCHENKO ALEKSANDR VASIL'EVICH</au><au>KHVAT ALEKSANDR VIKTOROVICH</au><au>KRAVCHENKO DMITRIJ VLADIMIROVICH</au><au>SAVCHUK NIKOLAJ FILIPPOVICH</au><au>TKACHENKO SERGEJ EVGEN'EVICH</au><au>ALJAB'EV SERGEJ BORISOVICH</au><au>RYZHOVA ELENA ALEKSANDROVNA</au><au>OKUN' IL'JA MATUSOVICH</au><au>IVASHCHENKO ANDREJ ALEKSANDROVICH</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>ANNELATED AZAHETEROCYCLIC AMIDES, WHICH INCLUDE PYRIMIDINE FRAGMENT, METHOD OF OBTAINING AND THEIR APPLICATION</title><date>2009-02-10</date><risdate>2009</risdate><abstract>FIELD: chemistry. ^ SUBSTANCE: present invention relates to new annelated azaheterocyclic amides, including a pyrimidine fragment, with the general formula 1, method of obtaining them and their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of P13K kinase, in compounds with the general formula 1: , where: X represents an oxygen atom, sulphur atom or not necessarily substituted at the nitrogen NH group, where the substitute is selected from lower alkyls and possibly a substituted aryl; Y represents an atom of nitrogen or substituted at the carbon atom CH group, where the substitute is selected from lower alkyls; Z represents an oxygen atom; R1 represents a hydrogen atom or not necessarily substituted C1-C6alkyl, or Z represents a nitrogen atom, which is together with a carbon atom, with which it is joined, form through Z and R1 annelated imidazole cycle; R2 and R3 independently from each other represent hydrogen, not necessarily substituted with C1-C6alkyl, C3-C6cycloalkyl, not necessarily substituted with phenyl, not necessarily substituted with 6-member aza-heteroaryl, under the condition, when Y represents a nitrogen atom, or R2 and R3 independently from each other represent not necessarily substituted C1-C6alkyl, not necessarily substituted with phenyl, not necessarily substituted with 5-7-member heterocycle with 1-2 heteroatoms, selected from nitrogen and oxygen, and possibly annelated with a phenyl ring, under the condition, when Y does not necessarily represent a substituted carbon atom at the CH group, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents a substituted aminoC1-C6alkyl and not necessarily substituted 5-6-member aza-heterocycloalkyl, under the condition, when Y represents a group which is substituted at the CH atom, and X represents an oxygen atom, sulphur atom, or R2 represents hydrogen, and R3 represents phenyl which is not necessarily substituted, pyridyl which is not necessarily substituted, pyrimidinyl which is not necessarily substituted, under the conditions, when R1 represents a substituted aminoC1-C6alkyl, substituted C2-C3hydroxyalkyl and aza-heterocycloalkyl not necessarily substituted, Y represents a group with CH substituted, and X represents an oxygen atom, sulphur, and the substitute of the above indicated substituted alkyl, phenyl, heterocycle, pyridyl, pyrimidyl are selected from groups of hydroxyl-, cyano-groups, hydrogen, lower alkyls, possibly mono- or di-substituted lower alkyl sulfamoyl, carbamoyl, C1-C6alkoxycarbonyl, amino, mono- or di-lower alkyl-amine, N-(lower alkyl), N-(phenylC1-C6alkyl)amine, phenyl, possibly substituted with a halogen atom, C1-C6alkyl, haloid-C1-C6alkyl; phenylC1-C6alkyl, saturated or non-saturated 5-6-member heterocycle containing 1-2-heteroatoms, selected from nitrogen, oxygen and sulphur, and possible condensation with a benzene ring R4 represents hydrogen or a lower alkyl. ^ EFFECT: obtaining new annelated aza-heterocyclic amides, including a pyrimidine fragment, with the general formula with the possibility of their application in the form of free bases or their pharmaceutically accepted salts as inhibitors of PI3K kinase. ^ 16 cl, 5 tbl, 5 ex</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 | ANNELATED AZAHETEROCYCLIC AMIDES, WHICH INCLUDE PYRIMIDINE FRAGMENT, METHOD OF OBTAINING AND THEIR APPLICATION |
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