5-Substituted 7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines, their use as a medicament and pharmaceutical compositions
5-Substitutované 7-[4-(2-pyridyl)fenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidiny jsou silnými inhibitory proteinkináz, a to zejména cyklin-dependentních kináz CDK2 a CDK5, a vykazují antileukemické, proapooptotické, antiangiogenní i protinádorové účinky. Vynález se dále týká způsobů jejich př...
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creator | Kryštof Vladimír Pospíšil Tomáš Vollmar Angelika Strnad Miroslav Havlíček Libor Šturc Antonín Jorda Radek Zahler Stefan |
description | 5-Substitutované 7-[4-(2-pyridyl)fenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidiny jsou silnými inhibitory proteinkináz, a to zejména cyklin-dependentních kináz CDK2 a CDK5, a vykazují antileukemické, proapooptotické, antiangiogenní i protinádorové účinky. Vynález se dále týká způsobů jejich přípravy, farmaceutických přípravků obsahujících tyto sloučeniny a jejich použití pro léčbu, a to zejména onemocnění spojených s proliferací, apoptózou, angiogenezí a záněty, jako jsou leukemie a metastázující solidní nádory.
5-substituted-7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines are potent inhibitors of protein kinases, especially cyclin-dependent kinases such as CDK2 and CDK5, and display antileukemic, pro-apoptotic, antiangiogenic and anticancer activities. The invention also relates to processes for their preparation, to pharmaceutical compositions and to their use as medicaments, particularly in the treatment of disorders involving cell proliferation, apoptosis, angiogenesis and inflammation, such as leukemia and metastatic solid cancer. |
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5-substituted-7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines are potent inhibitors of protein kinases, especially cyclin-dependent kinases such as CDK2 and CDK5, and display antileukemic, pro-apoptotic, antiangiogenic and anticancer activities. The invention also relates to processes for their preparation, to pharmaceutical compositions and to their use as medicaments, particularly in the treatment of disorders involving cell proliferation, apoptosis, angiogenesis and inflammation, such as leukemia and metastatic solid cancer.</description><language>cze ; eng</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>2016</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=20161123&DB=EPODOC&CC=CZ&NR=2015324A3$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20161123&DB=EPODOC&CC=CZ&NR=2015324A3$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Kryštof Vladimír</creatorcontrib><creatorcontrib>Pospíšil Tomáš</creatorcontrib><creatorcontrib>Vollmar Angelika</creatorcontrib><creatorcontrib>Strnad Miroslav</creatorcontrib><creatorcontrib>Havlíček Libor</creatorcontrib><creatorcontrib>Šturc Antonín</creatorcontrib><creatorcontrib>Jorda Radek</creatorcontrib><creatorcontrib>Zahler Stefan</creatorcontrib><title>5-Substituted 7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines, their use as a medicament and pharmaceutical compositions</title><description>5-Substitutované 7-[4-(2-pyridyl)fenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidiny jsou silnými inhibitory proteinkináz, a to zejména cyklin-dependentních kináz CDK2 a CDK5, a vykazují antileukemické, proapooptotické, antiangiogenní i protinádorové účinky. Vynález se dále týká způsobů jejich přípravy, farmaceutických přípravků obsahujících tyto sloučeniny a jejich použití pro léčbu, a to zejména onemocnění spojených s proliferací, apoptózou, angiogenezí a záněty, jako jsou leukemie a metastázující solidní nádory.
5-substituted-7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines are potent inhibitors of protein kinases, especially cyclin-dependent kinases such as CDK2 and CDK5, and display antileukemic, pro-apoptotic, antiangiogenic and anticancer activities. The invention also relates to processes for their preparation, to pharmaceutical compositions and to their use as medicaments, particularly in the treatment of disorders involving cell proliferation, apoptosis, angiogenesis and inflammation, such as leukemia and metastatic solid cancer.</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>2016</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNizFqw0AQANWkCEn-sGUMPnB0EqmNSUhvVzHGbHRrtHB3e2hXxfkX_rEVyANSDQwzj82td_v5R41tNgrw7o6de21dqROHGldlpFxjIhtrxMRZTs47VimTlBqXCq8S5ditvQun3ylx4Ey6BhuJJ5iVABUQEgUeMFE2wBygjDglHGi2xUYYJBVRNpasz83DBaPSyx-fGvj8OOy-HBU5k5blymTn3Xe7eet92229_0dyB_J0Ty4</recordid><startdate>20161123</startdate><enddate>20161123</enddate><creator>Kryštof Vladimír</creator><creator>Pospíšil Tomáš</creator><creator>Vollmar Angelika</creator><creator>Strnad Miroslav</creator><creator>Havlíček Libor</creator><creator>Šturc Antonín</creator><creator>Jorda Radek</creator><creator>Zahler Stefan</creator><scope>EVB</scope></search><sort><creationdate>20161123</creationdate><title>5-Substituted 7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines, their use as a medicament and pharmaceutical compositions</title><author>Kryštof Vladimír ; Pospíšil Tomáš ; Vollmar Angelika ; Strnad Miroslav ; Havlíček Libor ; Šturc Antonín ; Jorda Radek ; Zahler Stefan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CZ2015324A33</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>cze ; eng</language><creationdate>2016</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>Kryštof Vladimír</creatorcontrib><creatorcontrib>Pospíšil Tomáš</creatorcontrib><creatorcontrib>Vollmar Angelika</creatorcontrib><creatorcontrib>Strnad Miroslav</creatorcontrib><creatorcontrib>Havlíček Libor</creatorcontrib><creatorcontrib>Šturc Antonín</creatorcontrib><creatorcontrib>Jorda Radek</creatorcontrib><creatorcontrib>Zahler Stefan</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Kryštof Vladimír</au><au>Pospíšil Tomáš</au><au>Vollmar Angelika</au><au>Strnad Miroslav</au><au>Havlíček Libor</au><au>Šturc Antonín</au><au>Jorda Radek</au><au>Zahler Stefan</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>5-Substituted 7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines, their use as a medicament and pharmaceutical compositions</title><date>2016-11-23</date><risdate>2016</risdate><abstract>5-Substitutované 7-[4-(2-pyridyl)fenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidiny jsou silnými inhibitory proteinkináz, a to zejména cyklin-dependentních kináz CDK2 a CDK5, a vykazují antileukemické, proapooptotické, antiangiogenní i protinádorové účinky. Vynález se dále týká způsobů jejich přípravy, farmaceutických přípravků obsahujících tyto sloučeniny a jejich použití pro léčbu, a to zejména onemocnění spojených s proliferací, apoptózou, angiogenezí a záněty, jako jsou leukemie a metastázující solidní nádory.
5-substituted-7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines are potent inhibitors of protein kinases, especially cyclin-dependent kinases such as CDK2 and CDK5, and display antileukemic, pro-apoptotic, antiangiogenic and anticancer activities. The invention also relates to processes for their preparation, to pharmaceutical compositions and to their use as medicaments, particularly in the treatment of disorders involving cell proliferation, apoptosis, angiogenesis and inflammation, such as leukemia and metastatic solid cancer.</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 | 5-Substituted 7-[4-(2-pyridyl)phenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidines, their use as a medicament and pharmaceutical compositions |
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