ACYLAMINO-SUBSTITUTED DERIVATIVES OF CONDENSED CYCLOPENTACARBOXYLIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICALS
FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula (I), where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, contain...
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| creator | PATEK MARSEL SHTROBEL' KHARTMUT VAJKHZEL' ALEKSANDRA KADERAJT DITER PERNERSHTORFER JOZEF SHEFER MATTIAS CHEHN' L. CHARLI SAFAROVA ALENA CHEKHTIZKIJ VERNGARD |
| description | FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula (I), where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R-O-, HN-C(O)- and NC-; Y is selected from the group, containing S, C(R)=C(R) and C(R)=N; Z is selected from the group, containing C(R); R, R, R, R, Rand Rindependently on each other group R, R, R, R, Rand Rare selected from the group, containing (C-C)-alkyl, (C-C)-alkenyl, (C-C)-cycloalkyl and (C-C)-cycloalkyl-(C-C)-alkyl-, and all of them can optionally have one or more similar or different substituents R; Rand Rrepresent hydrogen; Rand Rare selected independently on each other, from the group, containing hydrogen and , (C-C)-alkyl; R, R, Rand Rare selected independently on each other, from the group, containing hydrogen, halogen and ON-; Ris selected from the group, containing hydrogen and (C-C)-alkyl; one of the groups Rand Ris group of formula II: R-R-, and the other of groups Rand Ris selected from the group, containing hydrogen, halogen, R, HO-, R-O-, R-S(O)-, HN-, R-NH-, R-N(R)-, R-C(O)- and NC-; Ris chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R), O, S, with other chain members being similar or different groups C(R)(R), where two adjacent groups can be bound to each other by double bond; Ris selected from the group, containing hydrogen, R, R-O-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R, R-O-, R-S(O)-, R-C(O)-NH-, R-S(O)-NH-, R-C(O)-, HO-C(O)-, HN-C(O)-, R-NH-C(O)-, R-N(R)-S(O)-, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups Rand R, constitutes not less than 5; Ris selected from the group, containing hydrogen and (C-C)-alkyl; R, independently on each other group R, is selected from |
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_RU2529484C2</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>RU2529484C2</sourcerecordid><originalsourceid>FETCH-epo_espacenet_RU2529484C23</originalsourceid><addsrcrecordid>eNqNi0EKwjAQRbtxIeod5gLd1Aq6nE5SGkiTkEyKXZUicSVarPfHLDyAqwfv_b8t3kijxl4ZW4bYBFYcWQoQ0qsBWQ0ygG2BrBHShBxoJG2dNIyEvrHXUSsCJCUCoBHAnVQe0Lms890awACuQ98jychZ6rAvNvf5sabDj7sCWsnUlWl5TWld5lt6ps_kY3WqLvW5pur4x-QLO4E4ug</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>ACYLAMINO-SUBSTITUTED DERIVATIVES OF CONDENSED CYCLOPENTACARBOXYLIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICALS</title><source>esp@cenet</source><creator>PATEK MARSEL ; SHTROBEL' KHARTMUT ; VAJKHZEL' ALEKSANDRA ; KADERAJT DITER ; PERNERSHTORFER JOZEF ; SHEFER MATTIAS ; CHEHN' L. CHARLI ; SAFAROVA ALENA ; CHEKHTIZKIJ VERNGARD</creator><creatorcontrib>PATEK MARSEL ; SHTROBEL' KHARTMUT ; VAJKHZEL' ALEKSANDRA ; KADERAJT DITER ; PERNERSHTORFER JOZEF ; SHEFER MATTIAS ; CHEHN' L. CHARLI ; SAFAROVA ALENA ; CHEKHTIZKIJ VERNGARD</creatorcontrib><description>FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula (I), where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R-O-, HN-C(O)- and NC-; Y is selected from the group, containing S, C(R)=C(R) and C(R)=N; Z is selected from the group, containing C(R); R, R, R, R, Rand Rindependently on each other group R, R, R, R, Rand Rare selected from the group, containing (C-C)-alkyl, (C-C)-alkenyl, (C-C)-cycloalkyl and (C-C)-cycloalkyl-(C-C)-alkyl-, and all of them can optionally have one or more similar or different substituents R; Rand Rrepresent hydrogen; Rand Rare selected independently on each other, from the group, containing hydrogen and , (C-C)-alkyl; R, R, Rand Rare selected independently on each other, from the group, containing hydrogen, halogen and ON-; Ris selected from the group, containing hydrogen and (C-C)-alkyl; one of the groups Rand Ris group of formula II: R-R-, and the other of groups Rand Ris selected from the group, containing hydrogen, halogen, R, HO-, R-O-, R-S(O)-, HN-, R-NH-, R-N(R)-, R-C(O)- and NC-; Ris chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R), O, S, with other chain members being similar or different groups C(R)(R), where two adjacent groups can be bound to each other by double bond; Ris selected from the group, containing hydrogen, R, R-O-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R, R-O-, R-S(O)-, R-C(O)-NH-, R-S(O)-NH-, R-C(O)-, HO-C(O)-, HN-C(O)-, R-NH-C(O)-, R-N(R)-S(O)-, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups Rand R, constitutes not less than 5; Ris selected from the group, containing hydrogen and (C-C)-alkyl; R, independently on each other group R, is selected from the group, containing hydrogen, fluorine, (C-C)-alkyl and HO-, or two groups R, together with included into them chain members, form monocyclic ring with number of members 4, which is saturated and contains 1 ring heteromember, selected from the group, containing O; Ris selected from the group, containing (C-C)-alkyl, which can optionally have one substituent R; Ris selected independently on each other, from the group, containing hydrogen, Rand phenyl; Ris selected from the group, containing R-O- and R-N(R)-; Ris selected from the group, containing hydrogen and R; Ris selected from the group, containing hydrogen; Ris selected from the group, containing hydrogen; Ris selected from the group, containing HO-, R-O-, HN-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)-, HN-C(O)- and phenyl; R, independently on each other group R, is selected from the group, containing (C-C)-alkyl; Het, independently on each other group Het, is monocyclic heterocyclic ring with number of members 5, which contains 1 or 2 similar or different ring heteromembers, selected from the group, containing N and S, and ring is saturated or non-saturated and optionally substituted with one or more similar or different substituents, selected from the group, containing (C-C)-alkyl; m, independently on each other number m, is integer number, selected from the group, containing 0, 1 and 2; phenyl, independently on each other phenyl group, can optionally have one or more similar or different substituents, selected from the group, containing halogen and (C-C)-alkyl.EFFECT: invention also relates to method of obtaining compound of formula (I) and its application for manufacturing pharmaceutical for inhibiting receptor Edg-2.17 cl, 14 tbl, 362 ex
Изобретение относится к соединению формулы I, где кольцо A является циклоалкановым кольцом с числом членов от 3-х до 7-и, бензольным кольцом или моноциклическим 5-членным или 6-членным ароматическим гетероциклическим кольцом, содержащим 1 гетерочлен кольца, выбранный из группы, содержащей N и S, причем бензольное и гетероциклическое кольца могут необязательно иметь один или два одинаковых или разных заместителей, выбранных из группы, содержащей галоген, HO-, R-O-, HN-C(O)- и NC-; Y выбирают из группы, содержащей S, C(R)=C(R) и C(R)=N; Z выбирают из группы, содержащей C(R); R, R, R, R, Rи Rнезависимо от каждой другой группы R, R, R, R, Rи Rвыбирают из группы, содержащей (C-C)-алкил, (C-C)-алкенил, (C-C)-циклоалкил и (C-C)-циклоалкил-(C-C)-алкил-, причем все они могут необязательно иметь один или более одинаковых или разных заместителей R; Rи Rпредставляют собой водород; Rи Rвыбирают, независимо друг от друга, из группы, содержащей водород и (C-C)-алкил; R, R, Rи Rвыбирают, независимо друг от друга, из группы, содержащей водород, галоген и ON-; Rвыбирают из группы, содержащей водород и (C-C)-алкил; одна из групп Rи Rявляется группой формулы II: R-R-, а другую из групп Rи Rвыбирают из группы, содержащей водород, галоген, R, HO-, R-O-, R-S(O)-, HN-, R-NH-, R-N(R)-, R-C(O)- и NC-; Rявляется цепью, содержащей от 1 до 5 членов цепи, из которых 0 или 1 член цепи является гетерочленом цепи, выбранным из группы, содержащей N(R), O, S, тогда как другие члены цепи являются одинаковыми или разными группами C(R)(R), где две соседние группы C(R)(R) могут соединяться друг с другом двойной связью; Rвыбирают из группы, содержащей водород, R, R-O-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)- и моноциклическое, бициклическое или трициклическое кольцо с числом членов от 5-и до 10-и,</description><language>eng ; rus</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; 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>2014</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=20140927&DB=EPODOC&CC=RU&NR=2529484C2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76318</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20140927&DB=EPODOC&CC=RU&NR=2529484C2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>PATEK MARSEL</creatorcontrib><creatorcontrib>SHTROBEL' KHARTMUT</creatorcontrib><creatorcontrib>VAJKHZEL' ALEKSANDRA</creatorcontrib><creatorcontrib>KADERAJT DITER</creatorcontrib><creatorcontrib>PERNERSHTORFER JOZEF</creatorcontrib><creatorcontrib>SHEFER MATTIAS</creatorcontrib><creatorcontrib>CHEHN' L. CHARLI</creatorcontrib><creatorcontrib>SAFAROVA ALENA</creatorcontrib><creatorcontrib>CHEKHTIZKIJ VERNGARD</creatorcontrib><title>ACYLAMINO-SUBSTITUTED DERIVATIVES OF CONDENSED CYCLOPENTACARBOXYLIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICALS</title><description>FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula (I), where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R-O-, HN-C(O)- and NC-; Y is selected from the group, containing S, C(R)=C(R) and C(R)=N; Z is selected from the group, containing C(R); R, R, R, R, Rand Rindependently on each other group R, R, R, R, Rand Rare selected from the group, containing (C-C)-alkyl, (C-C)-alkenyl, (C-C)-cycloalkyl and (C-C)-cycloalkyl-(C-C)-alkyl-, and all of them can optionally have one or more similar or different substituents R; Rand Rrepresent hydrogen; Rand Rare selected independently on each other, from the group, containing hydrogen and , (C-C)-alkyl; R, R, Rand Rare selected independently on each other, from the group, containing hydrogen, halogen and ON-; Ris selected from the group, containing hydrogen and (C-C)-alkyl; one of the groups Rand Ris group of formula II: R-R-, and the other of groups Rand Ris selected from the group, containing hydrogen, halogen, R, HO-, R-O-, R-S(O)-, HN-, R-NH-, R-N(R)-, R-C(O)- and NC-; Ris chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R), O, S, with other chain members being similar or different groups C(R)(R), where two adjacent groups can be bound to each other by double bond; Ris selected from the group, containing hydrogen, R, R-O-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R, R-O-, R-S(O)-, R-C(O)-NH-, R-S(O)-NH-, R-C(O)-, HO-C(O)-, HN-C(O)-, R-NH-C(O)-, R-N(R)-S(O)-, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups Rand R, constitutes not less than 5; Ris selected from the group, containing hydrogen and (C-C)-alkyl; R, independently on each other group R, is selected from the group, containing hydrogen, fluorine, (C-C)-alkyl and HO-, or two groups R, together with included into them chain members, form monocyclic ring with number of members 4, which is saturated and contains 1 ring heteromember, selected from the group, containing O; Ris selected from the group, containing (C-C)-alkyl, which can optionally have one substituent R; Ris selected independently on each other, from the group, containing hydrogen, Rand phenyl; Ris selected from the group, containing R-O- and R-N(R)-; Ris selected from the group, containing hydrogen and R; Ris selected from the group, containing hydrogen; Ris selected from the group, containing hydrogen; Ris selected from the group, containing HO-, R-O-, HN-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)-, HN-C(O)- and phenyl; R, independently on each other group R, is selected from the group, containing (C-C)-alkyl; Het, independently on each other group Het, is monocyclic heterocyclic ring with number of members 5, which contains 1 or 2 similar or different ring heteromembers, selected from the group, containing N and S, and ring is saturated or non-saturated and optionally substituted with one or more similar or different substituents, selected from the group, containing (C-C)-alkyl; m, independently on each other number m, is integer number, selected from the group, containing 0, 1 and 2; phenyl, independently on each other phenyl group, can optionally have one or more similar or different substituents, selected from the group, containing halogen and (C-C)-alkyl.EFFECT: invention also relates to method of obtaining compound of formula (I) and its application for manufacturing pharmaceutical for inhibiting receptor Edg-2.17 cl, 14 tbl, 362 ex
Изобретение относится к соединению формулы I, где кольцо A является циклоалкановым кольцом с числом членов от 3-х до 7-и, бензольным кольцом или моноциклическим 5-членным или 6-членным ароматическим гетероциклическим кольцом, содержащим 1 гетерочлен кольца, выбранный из группы, содержащей N и S, причем бензольное и гетероциклическое кольца могут необязательно иметь один или два одинаковых или разных заместителей, выбранных из группы, содержащей галоген, HO-, R-O-, HN-C(O)- и NC-; Y выбирают из группы, содержащей S, C(R)=C(R) и C(R)=N; Z выбирают из группы, содержащей C(R); R, R, R, R, Rи Rнезависимо от каждой другой группы R, R, R, R, Rи Rвыбирают из группы, содержащей (C-C)-алкил, (C-C)-алкенил, (C-C)-циклоалкил и (C-C)-циклоалкил-(C-C)-алкил-, причем все они могут необязательно иметь один или более одинаковых или разных заместителей R; Rи Rпредставляют собой водород; Rи Rвыбирают, независимо друг от друга, из группы, содержащей водород и (C-C)-алкил; R, R, Rи Rвыбирают, независимо друг от друга, из группы, содержащей водород, галоген и ON-; Rвыбирают из группы, содержащей водород и (C-C)-алкил; одна из групп Rи Rявляется группой формулы II: R-R-, а другую из групп Rи Rвыбирают из группы, содержащей водород, галоген, R, HO-, R-O-, R-S(O)-, HN-, R-NH-, R-N(R)-, R-C(O)- и NC-; Rявляется цепью, содержащей от 1 до 5 членов цепи, из которых 0 или 1 член цепи является гетерочленом цепи, выбранным из группы, содержащей N(R), O, S, тогда как другие члены цепи являются одинаковыми или разными группами C(R)(R), где две соседние группы C(R)(R) могут соединяться друг с другом двойной связью; Rвыбирают из группы, содержащей водород, R, R-O-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)- и моноциклическое, бициклическое или трициклическое кольцо с числом членов от 5-и до 10-и,</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><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>2014</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNi0EKwjAQRbtxIeod5gLd1Aq6nE5SGkiTkEyKXZUicSVarPfHLDyAqwfv_b8t3kijxl4ZW4bYBFYcWQoQ0qsBWQ0ygG2BrBHShBxoJG2dNIyEvrHXUSsCJCUCoBHAnVQe0Lms890awACuQ98jychZ6rAvNvf5sabDj7sCWsnUlWl5TWld5lt6ps_kY3WqLvW5pur4x-QLO4E4ug</recordid><startdate>20140927</startdate><enddate>20140927</enddate><creator>PATEK MARSEL</creator><creator>SHTROBEL' KHARTMUT</creator><creator>VAJKHZEL' ALEKSANDRA</creator><creator>KADERAJT DITER</creator><creator>PERNERSHTORFER JOZEF</creator><creator>SHEFER MATTIAS</creator><creator>CHEHN' L. CHARLI</creator><creator>SAFAROVA ALENA</creator><creator>CHEKHTIZKIJ VERNGARD</creator><scope>EVB</scope></search><sort><creationdate>20140927</creationdate><title>ACYLAMINO-SUBSTITUTED DERIVATIVES OF CONDENSED CYCLOPENTACARBOXYLIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICALS</title><author>PATEK MARSEL ; SHTROBEL' KHARTMUT ; VAJKHZEL' ALEKSANDRA ; KADERAJT DITER ; PERNERSHTORFER JOZEF ; SHEFER MATTIAS ; CHEHN' L. CHARLI ; SAFAROVA ALENA ; CHEKHTIZKIJ VERNGARD</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_RU2529484C23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; rus</language><creationdate>2014</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><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>PATEK MARSEL</creatorcontrib><creatorcontrib>SHTROBEL' KHARTMUT</creatorcontrib><creatorcontrib>VAJKHZEL' ALEKSANDRA</creatorcontrib><creatorcontrib>KADERAJT DITER</creatorcontrib><creatorcontrib>PERNERSHTORFER JOZEF</creatorcontrib><creatorcontrib>SHEFER MATTIAS</creatorcontrib><creatorcontrib>CHEHN' L. CHARLI</creatorcontrib><creatorcontrib>SAFAROVA ALENA</creatorcontrib><creatorcontrib>CHEKHTIZKIJ VERNGARD</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>PATEK MARSEL</au><au>SHTROBEL' KHARTMUT</au><au>VAJKHZEL' ALEKSANDRA</au><au>KADERAJT DITER</au><au>PERNERSHTORFER JOZEF</au><au>SHEFER MATTIAS</au><au>CHEHN' L. CHARLI</au><au>SAFAROVA ALENA</au><au>CHEKHTIZKIJ VERNGARD</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>ACYLAMINO-SUBSTITUTED DERIVATIVES OF CONDENSED CYCLOPENTACARBOXYLIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICALS</title><date>2014-09-27</date><risdate>2014</risdate><abstract>FIELD: medicine, pharmaceutics.SUBSTANCE: invention relates to compound of formula (I), where ring A is cycloalkane ring with number of members from 3 to 7, benzene ring or monocyclic 5-member or 6-member aromatic heterocyclic ring, containing 1 heteromember of ring, selected from the group, containing N and S, and benzene and heterocyclic rings can optionally have one or two similar or different substituents, selected from the group, containing halogen, HO-, R-O-, HN-C(O)- and NC-; Y is selected from the group, containing S, C(R)=C(R) and C(R)=N; Z is selected from the group, containing C(R); R, R, R, R, Rand Rindependently on each other group R, R, R, R, Rand Rare selected from the group, containing (C-C)-alkyl, (C-C)-alkenyl, (C-C)-cycloalkyl and (C-C)-cycloalkyl-(C-C)-alkyl-, and all of them can optionally have one or more similar or different substituents R; Rand Rrepresent hydrogen; Rand Rare selected independently on each other, from the group, containing hydrogen and , (C-C)-alkyl; R, R, Rand Rare selected independently on each other, from the group, containing hydrogen, halogen and ON-; Ris selected from the group, containing hydrogen and (C-C)-alkyl; one of the groups Rand Ris group of formula II: R-R-, and the other of groups Rand Ris selected from the group, containing hydrogen, halogen, R, HO-, R-O-, R-S(O)-, HN-, R-NH-, R-N(R)-, R-C(O)- and NC-; Ris chain, containing from 1 to 5 chain members of which 0 or 1 chain member is heteromember of chain, selected from the group, containing N(R), O, S, with other chain members being similar or different groups C(R)(R), where two adjacent groups can be bound to each other by double bond; Ris selected from the group, containing hydrogen, R, R-O-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)- and monocyclic, bicyclic or tricyclic ring with number of members from 5 to 10, which is saturated or non-saturated and contains 0, 1, 2 or 3 similar or different ring heteromembers, selected from the group, containing N, N(R), O, S, and ring can optionally have on ring carbon atoms one or 2-3 similar or different substituents, selected from the group, containing halogen, R, R-O-, R-S(O)-, R-C(O)-NH-, R-S(O)-NH-, R-C(O)-, HO-C(O)-, HN-C(O)-, R-NH-C(O)-, R-N(R)-S(O)-, NC-, oxo, phenyl and Het; on condition that total number of C, N, O and S atoms, present in two groups Rand R, constitutes not less than 5; Ris selected from the group, containing hydrogen and (C-C)-alkyl; R, independently on each other group R, is selected from the group, containing hydrogen, fluorine, (C-C)-alkyl and HO-, or two groups R, together with included into them chain members, form monocyclic ring with number of members 4, which is saturated and contains 1 ring heteromember, selected from the group, containing O; Ris selected from the group, containing (C-C)-alkyl, which can optionally have one substituent R; Ris selected independently on each other, from the group, containing hydrogen, Rand phenyl; Ris selected from the group, containing R-O- and R-N(R)-; Ris selected from the group, containing hydrogen and R; Ris selected from the group, containing hydrogen; Ris selected from the group, containing hydrogen; Ris selected from the group, containing HO-, R-O-, HN-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)-, HN-C(O)- and phenyl; R, independently on each other group R, is selected from the group, containing (C-C)-alkyl; Het, independently on each other group Het, is monocyclic heterocyclic ring with number of members 5, which contains 1 or 2 similar or different ring heteromembers, selected from the group, containing N and S, and ring is saturated or non-saturated and optionally substituted with one or more similar or different substituents, selected from the group, containing (C-C)-alkyl; m, independently on each other number m, is integer number, selected from the group, containing 0, 1 and 2; phenyl, independently on each other phenyl group, can optionally have one or more similar or different substituents, selected from the group, containing halogen and (C-C)-alkyl.EFFECT: invention also relates to method of obtaining compound of formula (I) and its application for manufacturing pharmaceutical for inhibiting receptor Edg-2.17 cl, 14 tbl, 362 ex
Изобретение относится к соединению формулы I, где кольцо A является циклоалкановым кольцом с числом членов от 3-х до 7-и, бензольным кольцом или моноциклическим 5-членным или 6-членным ароматическим гетероциклическим кольцом, содержащим 1 гетерочлен кольца, выбранный из группы, содержащей N и S, причем бензольное и гетероциклическое кольца могут необязательно иметь один или два одинаковых или разных заместителей, выбранных из группы, содержащей галоген, HO-, R-O-, HN-C(O)- и NC-; Y выбирают из группы, содержащей S, C(R)=C(R) и C(R)=N; Z выбирают из группы, содержащей C(R); R, R, R, R, Rи Rнезависимо от каждой другой группы R, R, R, R, Rи Rвыбирают из группы, содержащей (C-C)-алкил, (C-C)-алкенил, (C-C)-циклоалкил и (C-C)-циклоалкил-(C-C)-алкил-, причем все они могут необязательно иметь один или более одинаковых или разных заместителей R; Rи Rпредставляют собой водород; Rи Rвыбирают, независимо друг от друга, из группы, содержащей водород и (C-C)-алкил; R, R, Rи Rвыбирают, независимо друг от друга, из группы, содержащей водород, галоген и ON-; Rвыбирают из группы, содержащей водород и (C-C)-алкил; одна из групп Rи Rявляется группой формулы II: R-R-, а другую из групп Rи Rвыбирают из группы, содержащей водород, галоген, R, HO-, R-O-, R-S(O)-, HN-, R-NH-, R-N(R)-, R-C(O)- и NC-; Rявляется цепью, содержащей от 1 до 5 членов цепи, из которых 0 или 1 член цепи является гетерочленом цепи, выбранным из группы, содержащей N(R), O, S, тогда как другие члены цепи являются одинаковыми или разными группами C(R)(R), где две соседние группы C(R)(R) могут соединяться друг с другом двойной связью; Rвыбирают из группы, содержащей водород, R, R-O-, R-NH-, R-N(R)-, R-C(O)-NH-, HO-C(O)- и моноциклическое, бициклическое или трициклическое кольцо с числом членов от 5-и до 10-и,</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS 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 | ACYLAMINO-SUBSTITUTED DERIVATIVES OF CONDENSED CYCLOPENTACARBOXYLIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICALS |
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