7-AZAINDOLE DERIVATIVES

7-Azaindole derivatives (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. 7-Azaindole derivatives of formula (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. R : indazole-3-, -4- or -7-yl, imidazo[1,2-a]...

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Hauptverfasser: DORSCH, DIETER, KARAPETYAN, GNUNI AMATUNU, MERKUL, EUGEN, MUELLER, THOMAS, J.J, SIRRENBERG, CHRISTIAN
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description 7-Azaindole derivatives (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. 7-Azaindole derivatives of formula (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. R : indazole-3-, -4- or -7-yl, imidazo[1,2-a]pyrimidin-3- or -5-yl, quinolin-4-, -5- or -8-yl, isoquinolin-1-, -4 - or -5-yl, 1H-pyrrolo [3,2-c]pyridine-3 -, -4- or -7-yl, 1H-pyrrolo[2,3-c] pyridine-3-, -4- or -7-yl, furo[2,3-c]pyridine-3-, -4- or -7- yl, furo[3,2-b]pyridine-3- or -7-yl, 2,6-naphthyridin-1-or-4-yl or amino-quinoline-4-, -5 - or -8-yl (all optionally mono- or di-substituted by R 5>-), 1,8-naphthyridin-4-yl (optionally substituted by R 5>at 7th position) or 1,8-naphthyridin-4-yl (optionally substituted by A, Hal, CN, -[C(R 6>) 2] n-Cyc, OR 6>, N(R 6>) 2, SO 2A Or SO 2Ar 1>); R 1> : H or A1a; R 2> : H, A1a or -[C(R 6>) 2] n-Ar 1>; R 3> : H, A, Hal, CN, -[C(R 6>) 2] n-Ar 1>, -[C(R 6>) 2] n-Het, -[C(R 6>) 2] n-Cyc, OR 6>or N(R 6>) 2; R 5> : A, Hal, CN, -[C(R 6>) 2] n-Ar 1>, -[C(R 6>) 2] n-Het, -[C(R 6>) 2] n-Cyc, OR 6>. N(R 6>) 2, SO 2A or SO 2Ar 1>; R 6> : H or A1a; A : 1-6C-alkyl (where one or two CH 2groups are optionally replaced by O, N, S and/or -CH=CH, and 1-7 H atoms are replaced by F); A1a : 1-4C-alkyl; Cyc : 3-7C-cycloalkyl; Ar 1> : phenyl (optionally substituted by 1-3 Hal, A, -[C(R 6>) 2] n-OR 6>, N(R 6>) 2, CN, COOR 6>, CON(R 6>) 2, NR 6>COA, NR 6>SO 2A, COR 6>, SO 2N(R 6>) 2and/or S(O) nA); Het : optionally saturated mono-or bicyclic aryl heterocycle with 1-4 N, O and/or S (optionally mono- or di-substituted by Hal, A, -[C(R 6>) 2] nOR 6>, N(R 6>) 2, NO 2, CN, COOR 6>, CON(R 6>) 2, NR 6>COA, NR 6>SO 2A, COR 6>, SO 2NR 6>and/or S(O) n), preferably furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, thiadiazolyl, pyridazinyl or pyrazinyl (optionally substituted by 1 or 2 A); Hal : F, Cl, Br or I; and n : 0-2. Independent claims are included for: (1) the preparation of (I); and (2) the use of (I) for treating tumor, tumor growth, tumor metastasis and/or AIDS. [Image] ACTIVITY : Cytostatic; Anti-HIV; Antiinflammatory; Vasotropic; Neuroprotective; Nootropic; Antiarteriosclerotic; Antiarthritic; Osteopathic; Vulnerary. MECHANISM OF ACTION : 3-Phosphoinositide-dependent kinase 1 inhibitor; IkappaB kinase-epsilon inhibitor; Transforming growth factor-beta inhibitor; Serine/threonine-protein kinase 1 inhibitor. The
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fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_EP2670748B1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>EP2670748B1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_EP2670748B13</originalsourceid><addsrcrecordid>eNrjZBA313WMcvT0c_H3cVVwcQ3yDHMM8QxzDeZhYE1LzClO5YXS3AwKbq4hzh66qQX58anFBYnJqXmpJfGuAUZm5gbmJhZOhsZEKAEAk3sfDQ</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>7-AZAINDOLE DERIVATIVES</title><source>esp@cenet</source><creator>DORSCH, DIETER ; KARAPETYAN, GNUNI AMATUNU ; MERKUL, EUGEN ; MUELLER, THOMAS, J.J ; SIRRENBERG, CHRISTIAN</creator><creatorcontrib>DORSCH, DIETER ; KARAPETYAN, GNUNI AMATUNU ; MERKUL, EUGEN ; MUELLER, THOMAS, J.J ; SIRRENBERG, CHRISTIAN</creatorcontrib><description>7-Azaindole derivatives (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. 7-Azaindole derivatives of formula (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. R : indazole-3-, -4- or -7-yl, imidazo[1,2-a]pyrimidin-3- or -5-yl, quinolin-4-, -5- or -8-yl, isoquinolin-1-, -4 - or -5-yl, 1H-pyrrolo [3,2-c]pyridine-3 -, -4- or -7-yl, 1H-pyrrolo[2,3-c] pyridine-3-, -4- or -7-yl, furo[2,3-c]pyridine-3-, -4- or -7- yl, furo[3,2-b]pyridine-3- or -7-yl, 2,6-naphthyridin-1-or-4-yl or amino-quinoline-4-, -5 - or -8-yl (all optionally mono- or di-substituted by R 5&gt;-), 1,8-naphthyridin-4-yl (optionally substituted by R 5&gt;at 7th position) or 1,8-naphthyridin-4-yl (optionally substituted by A, Hal, CN, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;, N(R 6&gt;) 2, SO 2A Or SO 2Ar 1&gt;); R 1&gt; : H or A1a; R 2&gt; : H, A1a or -[C(R 6&gt;) 2] n-Ar 1&gt;; R 3&gt; : H, A, Hal, CN, -[C(R 6&gt;) 2] n-Ar 1&gt;, -[C(R 6&gt;) 2] n-Het, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;or N(R 6&gt;) 2; R 5&gt; : A, Hal, CN, -[C(R 6&gt;) 2] n-Ar 1&gt;, -[C(R 6&gt;) 2] n-Het, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;. N(R 6&gt;) 2, SO 2A or SO 2Ar 1&gt;; R 6&gt; : H or A1a; A : 1-6C-alkyl (where one or two CH 2groups are optionally replaced by O, N, S and/or -CH=CH, and 1-7 H atoms are replaced by F); A1a : 1-4C-alkyl; Cyc : 3-7C-cycloalkyl; Ar 1&gt; : phenyl (optionally substituted by 1-3 Hal, A, -[C(R 6&gt;) 2] n-OR 6&gt;, N(R 6&gt;) 2, CN, COOR 6&gt;, CON(R 6&gt;) 2, NR 6&gt;COA, NR 6&gt;SO 2A, COR 6&gt;, SO 2N(R 6&gt;) 2and/or S(O) nA); Het : optionally saturated mono-or bicyclic aryl heterocycle with 1-4 N, O and/or S (optionally mono- or di-substituted by Hal, A, -[C(R 6&gt;) 2] nOR 6&gt;, N(R 6&gt;) 2, NO 2, CN, COOR 6&gt;, CON(R 6&gt;) 2, NR 6&gt;COA, NR 6&gt;SO 2A, COR 6&gt;, SO 2NR 6&gt;and/or S(O) n), preferably furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, thiadiazolyl, pyridazinyl or pyrazinyl (optionally substituted by 1 or 2 A); Hal : F, Cl, Br or I; and n : 0-2. Independent claims are included for: (1) the preparation of (I); and (2) the use of (I) for treating tumor, tumor growth, tumor metastasis and/or AIDS. [Image] ACTIVITY : Cytostatic; Anti-HIV; Antiinflammatory; Vasotropic; Neuroprotective; Nootropic; Antiarteriosclerotic; Antiarthritic; Osteopathic; Vulnerary. MECHANISM OF ACTION : 3-Phosphoinositide-dependent kinase 1 inhibitor; IkappaB kinase-epsilon inhibitor; Transforming growth factor-beta inhibitor; Serine/threonine-protein kinase 1 inhibitor. The ability of (I) to inhibit Transforming growth factor-beta was tested using in vitro. The results showed that 5-(1H-pyrrolo[2,3-b]pyridin-3-yl)-isoquinoline exhibited an IC 5 0value of 0.5 nm to 1 mu M.</description><language>eng ; fre ; ger</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&amp;date=20160928&amp;DB=EPODOC&amp;CC=EP&amp;NR=2670748B1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,309,781,886,25568,76551</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20160928&amp;DB=EPODOC&amp;CC=EP&amp;NR=2670748B1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>DORSCH, DIETER</creatorcontrib><creatorcontrib>KARAPETYAN, GNUNI AMATUNU</creatorcontrib><creatorcontrib>MERKUL, EUGEN</creatorcontrib><creatorcontrib>MUELLER, THOMAS, J.J</creatorcontrib><creatorcontrib>SIRRENBERG, CHRISTIAN</creatorcontrib><title>7-AZAINDOLE DERIVATIVES</title><description>7-Azaindole derivatives (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. 7-Azaindole derivatives of formula (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. R : indazole-3-, -4- or -7-yl, imidazo[1,2-a]pyrimidin-3- or -5-yl, quinolin-4-, -5- or -8-yl, isoquinolin-1-, -4 - or -5-yl, 1H-pyrrolo [3,2-c]pyridine-3 -, -4- or -7-yl, 1H-pyrrolo[2,3-c] pyridine-3-, -4- or -7-yl, furo[2,3-c]pyridine-3-, -4- or -7- yl, furo[3,2-b]pyridine-3- or -7-yl, 2,6-naphthyridin-1-or-4-yl or amino-quinoline-4-, -5 - or -8-yl (all optionally mono- or di-substituted by R 5&gt;-), 1,8-naphthyridin-4-yl (optionally substituted by R 5&gt;at 7th position) or 1,8-naphthyridin-4-yl (optionally substituted by A, Hal, CN, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;, N(R 6&gt;) 2, SO 2A Or SO 2Ar 1&gt;); R 1&gt; : H or A1a; R 2&gt; : H, A1a or -[C(R 6&gt;) 2] n-Ar 1&gt;; R 3&gt; : H, A, Hal, CN, -[C(R 6&gt;) 2] n-Ar 1&gt;, -[C(R 6&gt;) 2] n-Het, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;or N(R 6&gt;) 2; R 5&gt; : A, Hal, CN, -[C(R 6&gt;) 2] n-Ar 1&gt;, -[C(R 6&gt;) 2] n-Het, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;. N(R 6&gt;) 2, SO 2A or SO 2Ar 1&gt;; R 6&gt; : H or A1a; A : 1-6C-alkyl (where one or two CH 2groups are optionally replaced by O, N, S and/or -CH=CH, and 1-7 H atoms are replaced by F); A1a : 1-4C-alkyl; Cyc : 3-7C-cycloalkyl; Ar 1&gt; : phenyl (optionally substituted by 1-3 Hal, A, -[C(R 6&gt;) 2] n-OR 6&gt;, N(R 6&gt;) 2, CN, COOR 6&gt;, CON(R 6&gt;) 2, NR 6&gt;COA, NR 6&gt;SO 2A, COR 6&gt;, SO 2N(R 6&gt;) 2and/or S(O) nA); Het : optionally saturated mono-or bicyclic aryl heterocycle with 1-4 N, O and/or S (optionally mono- or di-substituted by Hal, A, -[C(R 6&gt;) 2] nOR 6&gt;, N(R 6&gt;) 2, NO 2, CN, COOR 6&gt;, CON(R 6&gt;) 2, NR 6&gt;COA, NR 6&gt;SO 2A, COR 6&gt;, SO 2NR 6&gt;and/or S(O) n), preferably furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, thiadiazolyl, pyridazinyl or pyrazinyl (optionally substituted by 1 or 2 A); Hal : F, Cl, Br or I; and n : 0-2. Independent claims are included for: (1) the preparation of (I); and (2) the use of (I) for treating tumor, tumor growth, tumor metastasis and/or AIDS. [Image] ACTIVITY : Cytostatic; Anti-HIV; Antiinflammatory; Vasotropic; Neuroprotective; Nootropic; Antiarteriosclerotic; Antiarthritic; Osteopathic; Vulnerary. MECHANISM OF ACTION : 3-Phosphoinositide-dependent kinase 1 inhibitor; IkappaB kinase-epsilon inhibitor; Transforming growth factor-beta inhibitor; Serine/threonine-protein kinase 1 inhibitor. The ability of (I) to inhibit Transforming growth factor-beta was tested using in vitro. The results showed that 5-(1H-pyrrolo[2,3-b]pyridin-3-yl)-isoquinoline exhibited an IC 5 0value of 0.5 nm to 1 mu M.</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>eNrjZBA313WMcvT0c_H3cVVwcQ3yDHMM8QxzDeZhYE1LzClO5YXS3AwKbq4hzh66qQX58anFBYnJqXmpJfGuAUZm5gbmJhZOhsZEKAEAk3sfDQ</recordid><startdate>20160928</startdate><enddate>20160928</enddate><creator>DORSCH, DIETER</creator><creator>KARAPETYAN, GNUNI AMATUNU</creator><creator>MERKUL, EUGEN</creator><creator>MUELLER, THOMAS, J.J</creator><creator>SIRRENBERG, CHRISTIAN</creator><scope>EVB</scope></search><sort><creationdate>20160928</creationdate><title>7-AZAINDOLE DERIVATIVES</title><author>DORSCH, DIETER ; KARAPETYAN, GNUNI AMATUNU ; MERKUL, EUGEN ; MUELLER, THOMAS, J.J ; SIRRENBERG, CHRISTIAN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_EP2670748B13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre ; ger</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>DORSCH, DIETER</creatorcontrib><creatorcontrib>KARAPETYAN, GNUNI AMATUNU</creatorcontrib><creatorcontrib>MERKUL, EUGEN</creatorcontrib><creatorcontrib>MUELLER, THOMAS, J.J</creatorcontrib><creatorcontrib>SIRRENBERG, CHRISTIAN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>DORSCH, DIETER</au><au>KARAPETYAN, GNUNI AMATUNU</au><au>MERKUL, EUGEN</au><au>MUELLER, THOMAS, J.J</au><au>SIRRENBERG, CHRISTIAN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>7-AZAINDOLE DERIVATIVES</title><date>2016-09-28</date><risdate>2016</risdate><abstract>7-Azaindole derivatives (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. 7-Azaindole derivatives of formula (I) and their salts, tautomers or stereoisomers, including their mixtures in all ratios, are new. R : indazole-3-, -4- or -7-yl, imidazo[1,2-a]pyrimidin-3- or -5-yl, quinolin-4-, -5- or -8-yl, isoquinolin-1-, -4 - or -5-yl, 1H-pyrrolo [3,2-c]pyridine-3 -, -4- or -7-yl, 1H-pyrrolo[2,3-c] pyridine-3-, -4- or -7-yl, furo[2,3-c]pyridine-3-, -4- or -7- yl, furo[3,2-b]pyridine-3- or -7-yl, 2,6-naphthyridin-1-or-4-yl or amino-quinoline-4-, -5 - or -8-yl (all optionally mono- or di-substituted by R 5&gt;-), 1,8-naphthyridin-4-yl (optionally substituted by R 5&gt;at 7th position) or 1,8-naphthyridin-4-yl (optionally substituted by A, Hal, CN, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;, N(R 6&gt;) 2, SO 2A Or SO 2Ar 1&gt;); R 1&gt; : H or A1a; R 2&gt; : H, A1a or -[C(R 6&gt;) 2] n-Ar 1&gt;; R 3&gt; : H, A, Hal, CN, -[C(R 6&gt;) 2] n-Ar 1&gt;, -[C(R 6&gt;) 2] n-Het, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;or N(R 6&gt;) 2; R 5&gt; : A, Hal, CN, -[C(R 6&gt;) 2] n-Ar 1&gt;, -[C(R 6&gt;) 2] n-Het, -[C(R 6&gt;) 2] n-Cyc, OR 6&gt;. N(R 6&gt;) 2, SO 2A or SO 2Ar 1&gt;; R 6&gt; : H or A1a; A : 1-6C-alkyl (where one or two CH 2groups are optionally replaced by O, N, S and/or -CH=CH, and 1-7 H atoms are replaced by F); A1a : 1-4C-alkyl; Cyc : 3-7C-cycloalkyl; Ar 1&gt; : phenyl (optionally substituted by 1-3 Hal, A, -[C(R 6&gt;) 2] n-OR 6&gt;, N(R 6&gt;) 2, CN, COOR 6&gt;, CON(R 6&gt;) 2, NR 6&gt;COA, NR 6&gt;SO 2A, COR 6&gt;, SO 2N(R 6&gt;) 2and/or S(O) nA); Het : optionally saturated mono-or bicyclic aryl heterocycle with 1-4 N, O and/or S (optionally mono- or di-substituted by Hal, A, -[C(R 6&gt;) 2] nOR 6&gt;, N(R 6&gt;) 2, NO 2, CN, COOR 6&gt;, CON(R 6&gt;) 2, NR 6&gt;COA, NR 6&gt;SO 2A, COR 6&gt;, SO 2NR 6&gt;and/or S(O) n), preferably furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyrimidinyl, triazolyl, tetrazolyl, thiadiazolyl, pyridazinyl or pyrazinyl (optionally substituted by 1 or 2 A); Hal : F, Cl, Br or I; and n : 0-2. Independent claims are included for: (1) the preparation of (I); and (2) the use of (I) for treating tumor, tumor growth, tumor metastasis and/or AIDS. [Image] ACTIVITY : Cytostatic; Anti-HIV; Antiinflammatory; Vasotropic; Neuroprotective; Nootropic; Antiarteriosclerotic; Antiarthritic; Osteopathic; Vulnerary. MECHANISM OF ACTION : 3-Phosphoinositide-dependent kinase 1 inhibitor; IkappaB kinase-epsilon inhibitor; Transforming growth factor-beta inhibitor; Serine/threonine-protein kinase 1 inhibitor. The ability of (I) to inhibit Transforming growth factor-beta was tested using in vitro. The results showed that 5-(1H-pyrrolo[2,3-b]pyridin-3-yl)-isoquinoline exhibited an IC 5 0value of 0.5 nm to 1 mu M.</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 7-AZAINDOLE DERIVATIVES
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