COMPOSTO DE ARILSULFONAMIDAS E ANÁLOGOS, BEM COMO COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS

Aryl sulphonamides (I) and their salts are new: R1-A-D-E-G-L-R2 (I) R1 = 6-10C aryl; quinolyl; isoquinolyl; or a group of formula (a); Q = group of formula (i)-(vii): a = 1 or 2; R3 = H; 2-6C alkenyl; 1-6C alkyl; 1-6C acyl; -(CO)b-NR4R5 or -NR6-SO2-R7; b = 0 or 1; R4, R5 = H; phenyl; 1-6C acyl; 4-7C...

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Hauptverfasser: KLAUS-HELMUT MOHRS, MICHAEL MATZKE, ARNO FRIEDL, JOACHIM MITTENDORF, JEAN-MARIE-VIKTOR DE VRY, FRANK MAULER, MICHAEL-HAROLD ROCK, JOACHIM SCHUMACHER, ERVIN HORVATH, REINHARD JORK, JUERGEN DRESSEL, JUERGEN FRANZ, PETER SPREYER, SIEGFRIED RADDATZ, VERENA VOEHRINGER, JOERG KELDENICH
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creator KLAUS-HELMUT MOHRS
MICHAEL MATZKE
ARNO FRIEDL
JOACHIM MITTENDORF
JEAN-MARIE-VIKTOR DE VRY
FRANK MAULER
MICHAEL-HAROLD ROCK
JOACHIM SCHUMACHER
ERVIN HORVATH
REINHARD JORK
JUERGEN DRESSEL
JUERGEN FRANZ
PETER SPREYER
SIEGFRIED RADDATZ
VERENA VOEHRINGER
JOERG KELDENICH
description Aryl sulphonamides (I) and their salts are new: R1-A-D-E-G-L-R2 (I) R1 = 6-10C aryl; quinolyl; isoquinolyl; or a group of formula (a); Q = group of formula (i)-(vii): a = 1 or 2; R3 = H; 2-6C alkenyl; 1-6C alkyl; 1-6C acyl; -(CO)b-NR4R5 or -NR6-SO2-R7; b = 0 or 1; R4, R5 = H; phenyl; 1-6C acyl; 4-7C cycloacyl; benzoyl; or 1-6C alkyl optionally substituted by NH2, NH(1-6C alkyl) or N(1-6C alkyl)2; or NR4R5 = 5- or 6-membered saturated heterocycle optionally containing S and/or O and/or NR8; R6 = H; phenyl; 1-6C alkyl; or 1-6C acyl; R7 = phenyl or 1-6C alkyl; R8 = H; 1-6C alkyl; or 1-6C acyl; rings in R1 and alkenyl, alkenyl and acyl groups in R3 are optionally geminally substituted by 1 or more halo, COOH, OH, phenyl, 1-6C alkoxy, 1-6C alkoxycarbonyl or 1-8C alkyl (itself optionally substituted by halo, 1-6C alkylsulphonyloxy, N3, NH2, NH(1-6C alkyl), N(1-6C alkyl)2 or OH); A, E = bond or 1-4C alkylene; D = O ; S(O)c; or N(R9); c = 0-2; R9 = H; 1-6C alkyl; or 1-6C acyl; G = divalent 6-10C aryl or 5-7-membered heteroaryl (containing 1-3 S, N and/O) optionally substituted by 1 or more OH, CF3, COOH, halo, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 1-6C alkoxycarbonyl, -CO-O-(CH2)d-NR4R5, -NR6-SO2R7, -(CH2)e-(CO)f-NR14R15 and/or OR16; R14, R15 = R4 and R5 or -(CH2)g-NR4R5; d, g = 1-4; e, f = 0 or 1; R16 = 6-10C aryl; L = O; NH; N(R19)-SO2; N(R20)-SO; N(R21)-SO2O; N(R22)-SO2-N(R23); N(R24)-CO; SO2-N(R25); OSO2; N(R26)-P(O)(OR27); or N(OH)-SO2 (bonding to G is via the left hand atom); R19-R27 = H or 1-4C alkyl or R19 = SO2R2; R2 = 6-10C aryl or 5-7-membered saturated or aromatic heterocycle (containing 1-3 S, N and/or O) optionally substituted by 1 or more halo, CF3, NO2, NH2 and/or 1-6C alkyl; a group of formula (b): morpholinyl; 3-8C cycloalkyl; 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl optionally substituted by 1 or more halo, CF3, OH, CN, N3, 1-6C alkoxy (optionally substituted by 1 or more F); phthalimido and/or NR4R5; or phenyl or 5- or 6-membered heteroaryl (containing 1-3 S, N and/O) and both optionally substituted by 1 or more halo, NO2, OH, 1-6C alkyl, 1-6C alkoxy and/or NR30R31; or L and R2 together form a group of formula (c): R30, R31 = H; 1-6C alkyl; or 1-6C acyl. Also claimed are (1) starting materials of formula (II) (see 'Preparation'); (2) compounds of formulae (XV): R48-SO2-(CH2)h-U-(CH2)i-CR49R50-CF2-R51 (XV) R48 = leaving group; U = O or single bond; R49, R50 = H; F; Cl; or CF3; R51 = H; F; Cl; or Br; h = 1 or 2; i = 0 or 1; compounds are
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fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_BR9807848B1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>BR9807848B1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_BR9807848B13</originalsourceid><addsrcrecordid>eNrjZIhz9vcN8A8O8VdwcVVwDPL0CQ71cfP3c_T1dHEMVgAK-R1u9PF39w_WUXBy9VUAqvZXgGjxPNx-uNlfwc0xyNfR-XBXaIinsyNQQ2gw0Cj_YAVf12Bf_2AeBta0xJziVF4ozc2g4OYa4uyhm1qQH59aXJCYnJqXWhLvFGRpYWBuYWLhZGhMhBIAEVw1Vg</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>COMPOSTO DE ARILSULFONAMIDAS E ANÁLOGOS, BEM COMO COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS</title><source>esp@cenet</source><creator>KLAUS-HELMUT MOHRS ; MICHAEL MATZKE ; ARNO FRIEDL ; JOACHIM MITTENDORF ; JEAN-MARIE-VIKTOR DE VRY ; FRANK MAULER ; MICHAEL-HAROLD ROCK ; JOACHIM SCHUMACHER ; ERVIN HORVATH ; REINHARD JORK ; JUERGEN DRESSEL ; JUERGEN FRANZ ; PETER SPREYER ; SIEGFRIED RADDATZ ; VERENA VOEHRINGER ; JOERG KELDENICH</creator><creatorcontrib>KLAUS-HELMUT MOHRS ; MICHAEL MATZKE ; ARNO FRIEDL ; JOACHIM MITTENDORF ; JEAN-MARIE-VIKTOR DE VRY ; FRANK MAULER ; MICHAEL-HAROLD ROCK ; JOACHIM SCHUMACHER ; ERVIN HORVATH ; REINHARD JORK ; JUERGEN DRESSEL ; JUERGEN FRANZ ; PETER SPREYER ; SIEGFRIED RADDATZ ; VERENA VOEHRINGER ; JOERG KELDENICH</creatorcontrib><description>Aryl sulphonamides (I) and their salts are new: R1-A-D-E-G-L-R2 (I) R1 = 6-10C aryl; quinolyl; isoquinolyl; or a group of formula (a); Q = group of formula (i)-(vii): a = 1 or 2; R3 = H; 2-6C alkenyl; 1-6C alkyl; 1-6C acyl; -(CO)b-NR4R5 or -NR6-SO2-R7; b = 0 or 1; R4, R5 = H; phenyl; 1-6C acyl; 4-7C cycloacyl; benzoyl; or 1-6C alkyl optionally substituted by NH2, NH(1-6C alkyl) or N(1-6C alkyl)2; or NR4R5 = 5- or 6-membered saturated heterocycle optionally containing S and/or O and/or NR8; R6 = H; phenyl; 1-6C alkyl; or 1-6C acyl; R7 = phenyl or 1-6C alkyl; R8 = H; 1-6C alkyl; or 1-6C acyl; rings in R1 and alkenyl, alkenyl and acyl groups in R3 are optionally geminally substituted by 1 or more halo, COOH, OH, phenyl, 1-6C alkoxy, 1-6C alkoxycarbonyl or 1-8C alkyl (itself optionally substituted by halo, 1-6C alkylsulphonyloxy, N3, NH2, NH(1-6C alkyl), N(1-6C alkyl)2 or OH); A, E = bond or 1-4C alkylene; D = O ; S(O)c; or N(R9); c = 0-2; R9 = H; 1-6C alkyl; or 1-6C acyl; G = divalent 6-10C aryl or 5-7-membered heteroaryl (containing 1-3 S, N and/O) optionally substituted by 1 or more OH, CF3, COOH, halo, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 1-6C alkoxycarbonyl, -CO-O-(CH2)d-NR4R5, -NR6-SO2R7, -(CH2)e-(CO)f-NR14R15 and/or OR16; R14, R15 = R4 and R5 or -(CH2)g-NR4R5; d, g = 1-4; e, f = 0 or 1; R16 = 6-10C aryl; L = O; NH; N(R19)-SO2; N(R20)-SO; N(R21)-SO2O; N(R22)-SO2-N(R23); N(R24)-CO; SO2-N(R25); OSO2; N(R26)-P(O)(OR27); or N(OH)-SO2 (bonding to G is via the left hand atom); R19-R27 = H or 1-4C alkyl or R19 = SO2R2; R2 = 6-10C aryl or 5-7-membered saturated or aromatic heterocycle (containing 1-3 S, N and/or O) optionally substituted by 1 or more halo, CF3, NO2, NH2 and/or 1-6C alkyl; a group of formula (b): morpholinyl; 3-8C cycloalkyl; 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl optionally substituted by 1 or more halo, CF3, OH, CN, N3, 1-6C alkoxy (optionally substituted by 1 or more F); phthalimido and/or NR4R5; or phenyl or 5- or 6-membered heteroaryl (containing 1-3 S, N and/O) and both optionally substituted by 1 or more halo, NO2, OH, 1-6C alkyl, 1-6C alkoxy and/or NR30R31; or L and R2 together form a group of formula (c): R30, R31 = H; 1-6C alkyl; or 1-6C acyl. Also claimed are (1) starting materials of formula (II) (see 'Preparation'); (2) compounds of formulae (XV): R48-SO2-(CH2)h-U-(CH2)i-CR49R50-CF2-R51 (XV) R48 = leaving group; U = O or single bond; R49, R50 = H; F; Cl; or CF3; R51 = H; F; Cl; or Br; h = 1 or 2; i = 0 or 1; compounds are excluded when a) U is a single bond, R49 = R50 = H or F and R51 = F; and b) U = O, R49 or R50 = Cl and i = 0; and (3) compounds of formulae (VXI) and (XVII): R48-SO2-CH2-CH2-CH2-CF3 (XVI) R48-SO2-CH2-CH2-CH2-CF2-CF3 (XVII).</description><language>por</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM ; 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>2013</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=20131105&amp;DB=EPODOC&amp;CC=BR&amp;NR=9807848B1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20131105&amp;DB=EPODOC&amp;CC=BR&amp;NR=9807848B1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>KLAUS-HELMUT MOHRS</creatorcontrib><creatorcontrib>MICHAEL MATZKE</creatorcontrib><creatorcontrib>ARNO FRIEDL</creatorcontrib><creatorcontrib>JOACHIM MITTENDORF</creatorcontrib><creatorcontrib>JEAN-MARIE-VIKTOR DE VRY</creatorcontrib><creatorcontrib>FRANK MAULER</creatorcontrib><creatorcontrib>MICHAEL-HAROLD ROCK</creatorcontrib><creatorcontrib>JOACHIM SCHUMACHER</creatorcontrib><creatorcontrib>ERVIN HORVATH</creatorcontrib><creatorcontrib>REINHARD JORK</creatorcontrib><creatorcontrib>JUERGEN DRESSEL</creatorcontrib><creatorcontrib>JUERGEN FRANZ</creatorcontrib><creatorcontrib>PETER SPREYER</creatorcontrib><creatorcontrib>SIEGFRIED RADDATZ</creatorcontrib><creatorcontrib>VERENA VOEHRINGER</creatorcontrib><creatorcontrib>JOERG KELDENICH</creatorcontrib><title>COMPOSTO DE ARILSULFONAMIDAS E ANÁLOGOS, BEM COMO COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS</title><description>Aryl sulphonamides (I) and their salts are new: R1-A-D-E-G-L-R2 (I) R1 = 6-10C aryl; quinolyl; isoquinolyl; or a group of formula (a); Q = group of formula (i)-(vii): a = 1 or 2; R3 = H; 2-6C alkenyl; 1-6C alkyl; 1-6C acyl; -(CO)b-NR4R5 or -NR6-SO2-R7; b = 0 or 1; R4, R5 = H; phenyl; 1-6C acyl; 4-7C cycloacyl; benzoyl; or 1-6C alkyl optionally substituted by NH2, NH(1-6C alkyl) or N(1-6C alkyl)2; or NR4R5 = 5- or 6-membered saturated heterocycle optionally containing S and/or O and/or NR8; R6 = H; phenyl; 1-6C alkyl; or 1-6C acyl; R7 = phenyl or 1-6C alkyl; R8 = H; 1-6C alkyl; or 1-6C acyl; rings in R1 and alkenyl, alkenyl and acyl groups in R3 are optionally geminally substituted by 1 or more halo, COOH, OH, phenyl, 1-6C alkoxy, 1-6C alkoxycarbonyl or 1-8C alkyl (itself optionally substituted by halo, 1-6C alkylsulphonyloxy, N3, NH2, NH(1-6C alkyl), N(1-6C alkyl)2 or OH); A, E = bond or 1-4C alkylene; D = O ; S(O)c; or N(R9); c = 0-2; R9 = H; 1-6C alkyl; or 1-6C acyl; G = divalent 6-10C aryl or 5-7-membered heteroaryl (containing 1-3 S, N and/O) optionally substituted by 1 or more OH, CF3, COOH, halo, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 1-6C alkoxycarbonyl, -CO-O-(CH2)d-NR4R5, -NR6-SO2R7, -(CH2)e-(CO)f-NR14R15 and/or OR16; R14, R15 = R4 and R5 or -(CH2)g-NR4R5; d, g = 1-4; e, f = 0 or 1; R16 = 6-10C aryl; L = O; NH; N(R19)-SO2; N(R20)-SO; N(R21)-SO2O; N(R22)-SO2-N(R23); N(R24)-CO; SO2-N(R25); OSO2; N(R26)-P(O)(OR27); or N(OH)-SO2 (bonding to G is via the left hand atom); R19-R27 = H or 1-4C alkyl or R19 = SO2R2; R2 = 6-10C aryl or 5-7-membered saturated or aromatic heterocycle (containing 1-3 S, N and/or O) optionally substituted by 1 or more halo, CF3, NO2, NH2 and/or 1-6C alkyl; a group of formula (b): morpholinyl; 3-8C cycloalkyl; 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl optionally substituted by 1 or more halo, CF3, OH, CN, N3, 1-6C alkoxy (optionally substituted by 1 or more F); phthalimido and/or NR4R5; or phenyl or 5- or 6-membered heteroaryl (containing 1-3 S, N and/O) and both optionally substituted by 1 or more halo, NO2, OH, 1-6C alkyl, 1-6C alkoxy and/or NR30R31; or L and R2 together form a group of formula (c): R30, R31 = H; 1-6C alkyl; or 1-6C acyl. Also claimed are (1) starting materials of formula (II) (see 'Preparation'); (2) compounds of formulae (XV): R48-SO2-(CH2)h-U-(CH2)i-CR49R50-CF2-R51 (XV) R48 = leaving group; U = O or single bond; R49, R50 = H; F; Cl; or CF3; R51 = H; F; Cl; or Br; h = 1 or 2; i = 0 or 1; compounds are excluded when a) U is a single bond, R49 = R50 = H or F and R51 = F; and b) U = O, R49 or R50 = Cl and i = 0; and (3) compounds of formulae (VXI) and (XVII): R48-SO2-CH2-CH2-CH2-CF3 (XVI) R48-SO2-CH2-CH2-CH2-CF2-CF3 (XVII).</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><subject>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</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>2013</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZIhz9vcN8A8O8VdwcVVwDPL0CQ71cfP3c_T1dHEMVgAK-R1u9PF39w_WUXBy9VUAqvZXgGjxPNx-uNlfwc0xyNfR-XBXaIinsyNQQ2gw0Cj_YAVf12Bf_2AeBta0xJziVF4ozc2g4OYa4uyhm1qQH59aXJCYnJqXWhLvFGRpYWBuYWLhZGhMhBIAEVw1Vg</recordid><startdate>20131105</startdate><enddate>20131105</enddate><creator>KLAUS-HELMUT MOHRS</creator><creator>MICHAEL MATZKE</creator><creator>ARNO FRIEDL</creator><creator>JOACHIM MITTENDORF</creator><creator>JEAN-MARIE-VIKTOR DE VRY</creator><creator>FRANK MAULER</creator><creator>MICHAEL-HAROLD ROCK</creator><creator>JOACHIM SCHUMACHER</creator><creator>ERVIN HORVATH</creator><creator>REINHARD JORK</creator><creator>JUERGEN DRESSEL</creator><creator>JUERGEN FRANZ</creator><creator>PETER SPREYER</creator><creator>SIEGFRIED RADDATZ</creator><creator>VERENA VOEHRINGER</creator><creator>JOERG KELDENICH</creator><scope>EVB</scope></search><sort><creationdate>20131105</creationdate><title>COMPOSTO DE ARILSULFONAMIDAS E ANÁLOGOS, BEM COMO COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS</title><author>KLAUS-HELMUT MOHRS ; MICHAEL MATZKE ; ARNO FRIEDL ; JOACHIM MITTENDORF ; JEAN-MARIE-VIKTOR DE VRY ; FRANK MAULER ; MICHAEL-HAROLD ROCK ; JOACHIM SCHUMACHER ; ERVIN HORVATH ; REINHARD JORK ; JUERGEN DRESSEL ; JUERGEN FRANZ ; PETER SPREYER ; SIEGFRIED RADDATZ ; VERENA VOEHRINGER ; JOERG KELDENICH</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_BR9807848B13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>por</language><creationdate>2013</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><topic>ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM</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>KLAUS-HELMUT MOHRS</creatorcontrib><creatorcontrib>MICHAEL MATZKE</creatorcontrib><creatorcontrib>ARNO FRIEDL</creatorcontrib><creatorcontrib>JOACHIM MITTENDORF</creatorcontrib><creatorcontrib>JEAN-MARIE-VIKTOR DE VRY</creatorcontrib><creatorcontrib>FRANK MAULER</creatorcontrib><creatorcontrib>MICHAEL-HAROLD ROCK</creatorcontrib><creatorcontrib>JOACHIM SCHUMACHER</creatorcontrib><creatorcontrib>ERVIN HORVATH</creatorcontrib><creatorcontrib>REINHARD JORK</creatorcontrib><creatorcontrib>JUERGEN DRESSEL</creatorcontrib><creatorcontrib>JUERGEN FRANZ</creatorcontrib><creatorcontrib>PETER SPREYER</creatorcontrib><creatorcontrib>SIEGFRIED RADDATZ</creatorcontrib><creatorcontrib>VERENA VOEHRINGER</creatorcontrib><creatorcontrib>JOERG KELDENICH</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>KLAUS-HELMUT MOHRS</au><au>MICHAEL MATZKE</au><au>ARNO FRIEDL</au><au>JOACHIM MITTENDORF</au><au>JEAN-MARIE-VIKTOR DE VRY</au><au>FRANK MAULER</au><au>MICHAEL-HAROLD ROCK</au><au>JOACHIM SCHUMACHER</au><au>ERVIN HORVATH</au><au>REINHARD JORK</au><au>JUERGEN DRESSEL</au><au>JUERGEN FRANZ</au><au>PETER SPREYER</au><au>SIEGFRIED RADDATZ</au><au>VERENA VOEHRINGER</au><au>JOERG KELDENICH</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>COMPOSTO DE ARILSULFONAMIDAS E ANÁLOGOS, BEM COMO COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS</title><date>2013-11-05</date><risdate>2013</risdate><abstract>Aryl sulphonamides (I) and their salts are new: R1-A-D-E-G-L-R2 (I) R1 = 6-10C aryl; quinolyl; isoquinolyl; or a group of formula (a); Q = group of formula (i)-(vii): a = 1 or 2; R3 = H; 2-6C alkenyl; 1-6C alkyl; 1-6C acyl; -(CO)b-NR4R5 or -NR6-SO2-R7; b = 0 or 1; R4, R5 = H; phenyl; 1-6C acyl; 4-7C cycloacyl; benzoyl; or 1-6C alkyl optionally substituted by NH2, NH(1-6C alkyl) or N(1-6C alkyl)2; or NR4R5 = 5- or 6-membered saturated heterocycle optionally containing S and/or O and/or NR8; R6 = H; phenyl; 1-6C alkyl; or 1-6C acyl; R7 = phenyl or 1-6C alkyl; R8 = H; 1-6C alkyl; or 1-6C acyl; rings in R1 and alkenyl, alkenyl and acyl groups in R3 are optionally geminally substituted by 1 or more halo, COOH, OH, phenyl, 1-6C alkoxy, 1-6C alkoxycarbonyl or 1-8C alkyl (itself optionally substituted by halo, 1-6C alkylsulphonyloxy, N3, NH2, NH(1-6C alkyl), N(1-6C alkyl)2 or OH); A, E = bond or 1-4C alkylene; D = O ; S(O)c; or N(R9); c = 0-2; R9 = H; 1-6C alkyl; or 1-6C acyl; G = divalent 6-10C aryl or 5-7-membered heteroaryl (containing 1-3 S, N and/O) optionally substituted by 1 or more OH, CF3, COOH, halo, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 1-6C alkoxycarbonyl, -CO-O-(CH2)d-NR4R5, -NR6-SO2R7, -(CH2)e-(CO)f-NR14R15 and/or OR16; R14, R15 = R4 and R5 or -(CH2)g-NR4R5; d, g = 1-4; e, f = 0 or 1; R16 = 6-10C aryl; L = O; NH; N(R19)-SO2; N(R20)-SO; N(R21)-SO2O; N(R22)-SO2-N(R23); N(R24)-CO; SO2-N(R25); OSO2; N(R26)-P(O)(OR27); or N(OH)-SO2 (bonding to G is via the left hand atom); R19-R27 = H or 1-4C alkyl or R19 = SO2R2; R2 = 6-10C aryl or 5-7-membered saturated or aromatic heterocycle (containing 1-3 S, N and/or O) optionally substituted by 1 or more halo, CF3, NO2, NH2 and/or 1-6C alkyl; a group of formula (b): morpholinyl; 3-8C cycloalkyl; 1-12C alkyl, 2-12C alkenyl or 2-12C alkynyl optionally substituted by 1 or more halo, CF3, OH, CN, N3, 1-6C alkoxy (optionally substituted by 1 or more F); phthalimido and/or NR4R5; or phenyl or 5- or 6-membered heteroaryl (containing 1-3 S, N and/O) and both optionally substituted by 1 or more halo, NO2, OH, 1-6C alkyl, 1-6C alkoxy and/or NR30R31; or L and R2 together form a group of formula (c): R30, R31 = H; 1-6C alkyl; or 1-6C acyl. Also claimed are (1) starting materials of formula (II) (see 'Preparation'); (2) compounds of formulae (XV): R48-SO2-(CH2)h-U-(CH2)i-CR49R50-CF2-R51 (XV) R48 = leaving group; U = O or single bond; R49, R50 = H; F; Cl; or CF3; R51 = H; F; Cl; or Br; h = 1 or 2; i = 0 or 1; compounds are excluded when a) U is a single bond, R49 = R50 = H or F and R51 = F; and b) U = O, R49 or R50 = Cl and i = 0; and (3) compounds of formulae (VXI) and (XVII): R48-SO2-CH2-CH2-CH2-CF3 (XVI) R48-SO2-CH2-CH2-CH2-CF2-CF3 (XVII).</abstract><oa>free_for_read</oa></addata></record>
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
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 COMPOSTO DE ARILSULFONAMIDAS E ANÁLOGOS, BEM COMO COMPOSIÇÃO FARMACÊUTICA E USO DOS MESMOS
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