N-substituted anilines

Compounds of the formula wherein R1 is hydrogen or -(CH2)mCOOR2; R2 is hydrogen, (R6)2N(CH2)2-, R6COOCH2- or -CH2CON(CH2CH2OH)2; R3 is hydrogen, nitro, hydroxy, amino, CH3(CH2) nS(O)0-2-, CH3(CH2)n-, CH3(CH2)nO- ,R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-, R5NHCONH-, [CH3(CH2)n]2NCO- , CH3(CH2)nCHOH...

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Hauptverfasser: RU-JEN LEE HAN, MATTHEW CARSON, RONALD ANDREW LEMAHIEU, VINCENT STEWART MADISON
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creator RU-JEN LEE HAN
MATTHEW CARSON
RONALD ANDREW LEMAHIEU
VINCENT STEWART MADISON
description Compounds of the formula wherein R1 is hydrogen or -(CH2)mCOOR2; R2 is hydrogen, (R6)2N(CH2)2-, R6COOCH2- or -CH2CON(CH2CH2OH)2; R3 is hydrogen, nitro, hydroxy, amino, CH3(CH2) nS(O)0-2-, CH3(CH2)n-, CH3(CH2)nO- ,R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-, R5NHCONH-, [CH3(CH2)n]2NCO- , CH3(CH2)nCHOHCH2O-, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, (R6O)2PO(CH2)pO- , (HO) (R6O)PO(CH2)pO-, R6[O(CH2)2]qO- , R7(CH2)pO-, or -O(CH2)p-pyridinium(OH); R4 is CH3(CH2) n- , CH3(CH2)nO- , CF3SO2NH-, R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-R5NHCONH-, [CH3(CH2)n]2NCO-, CH3(CH2)nCHOHCH2O-, carboxy, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, R6[O(CH2)2]qO- , or R7(CH2)pO-; R5 is CH3(CH2)n-, 1-adamantyl or diphenylmethyl; R6 is lower alkyl; R7 is 1- or 2 -naphthyloxy, 1-, 2- or 3-pyridinyloxy, 2,3- or 3,4-dihydroxyphenyl, 6,7-dihydroxy-2-naphthyl, phenyl, phenoxy or substituted phenyl or phenoxy, wherein the substituent is selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, nitro, amino, halo, R6 S(O)0-2-, carboxy, carboxy-lower alkyl or phenyl; R8 is hydrogen or lower alkyl; n is an integer from 0 to 17; m is an integer from 1 to 3; t is an integer from 1 to 10; p is an integer from 2 to 18, and q is an integer from 1 to 6; and when R2 is hydrogen, a pharmaceutically acceptable salt thereof with a base, are potent inhibitors of phospholipases A2 (PLA2's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.
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R4 is CH3(CH2) n- , CH3(CH2)nO- , CF3SO2NH-, R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-R5NHCONH-, [CH3(CH2)n]2NCO-, CH3(CH2)nCHOHCH2O-, carboxy, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, R6[O(CH2)2]qO- , or R7(CH2)pO-; R5 is CH3(CH2)n-, 1-adamantyl or diphenylmethyl; R6 is lower alkyl; R7 is 1- or 2 -naphthyloxy, 1-, 2- or 3-pyridinyloxy, 2,3- or 3,4-dihydroxyphenyl, 6,7-dihydroxy-2-naphthyl, phenyl, phenoxy or substituted phenyl or phenoxy, wherein the substituent is selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, nitro, amino, halo, R6 S(O)0-2-, carboxy, carboxy-lower alkyl or phenyl; R8 is hydrogen or lower alkyl; n is an integer from 0 to 17; m is an integer from 1 to 3; t is an integer from 1 to 10; p is an integer from 2 to 18, and q is an integer from 1 to 6; and when R2 is hydrogen, a pharmaceutically acceptable salt thereof with a base, are potent inhibitors of phospholipases A2 (PLA2's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.</description><edition>5</edition><language>eng</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; 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R2 is hydrogen, (R6)2N(CH2)2-, R6COOCH2- or -CH2CON(CH2CH2OH)2; R3 is hydrogen, nitro, hydroxy, amino, CH3(CH2) nS(O)0-2-, CH3(CH2)n-, CH3(CH2)nO- ,R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-, R5NHCONH-, [CH3(CH2)n]2NCO- , CH3(CH2)nCHOHCH2O-, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, (R6O)2PO(CH2)pO- , (HO) (R6O)PO(CH2)pO-, R6[O(CH2)2]qO- , R7(CH2)pO-, or -O(CH2)p-pyridinium&lt;+&gt;(OH&lt;-&gt;); R4 is CH3(CH2) n- , CH3(CH2)nO- , CF3SO2NH-, R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-R5NHCONH-, [CH3(CH2)n]2NCO-, CH3(CH2)nCHOHCH2O-, carboxy, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, R6[O(CH2)2]qO- , or R7(CH2)pO-; R5 is CH3(CH2)n-, 1-adamantyl or diphenylmethyl; R6 is lower alkyl; R7 is 1- or 2 -naphthyloxy, 1-, 2- or 3-pyridinyloxy, 2,3- or 3,4-dihydroxyphenyl, 6,7-dihydroxy-2-naphthyl, phenyl, phenoxy or substituted phenyl or phenoxy, wherein the substituent is selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, nitro, amino, halo, R6 S(O)0-2-, carboxy, carboxy-lower alkyl or phenyl; 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MATTHEW CARSON ; RONALD ANDREW LEMAHIEU ; VINCENT STEWART MADISON</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_AU666199BB23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1996</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>RU-JEN LEE HAN</creatorcontrib><creatorcontrib>MATTHEW CARSON</creatorcontrib><creatorcontrib>RONALD ANDREW LEMAHIEU</creatorcontrib><creatorcontrib>VINCENT STEWART MADISON</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>RU-JEN LEE HAN</au><au>MATTHEW CARSON</au><au>RONALD ANDREW LEMAHIEU</au><au>VINCENT STEWART MADISON</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>N-substituted anilines</title><date>1996-02-01</date><risdate>1996</risdate><abstract>Compounds of the formula wherein R1 is hydrogen or -(CH2)mCOOR2; R2 is hydrogen, (R6)2N(CH2)2-, R6COOCH2- or -CH2CON(CH2CH2OH)2; R3 is hydrogen, nitro, hydroxy, amino, CH3(CH2) nS(O)0-2-, CH3(CH2)n-, CH3(CH2)nO- ,R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-, R5NHCONH-, [CH3(CH2)n]2NCO- , CH3(CH2)nCHOHCH2O-, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, (R6O)2PO(CH2)pO- , (HO) (R6O)PO(CH2)pO-, R6[O(CH2)2]qO- , R7(CH2)pO-, or -O(CH2)p-pyridinium&lt;+&gt;(OH&lt;-&gt;); R4 is CH3(CH2) n- , CH3(CH2)nO- , CF3SO2NH-, R5COO-, R5OOC- ,R5HNCOO-, R5NHCO-, R5CONH-R5NHCONH-, [CH3(CH2)n]2NCO-, CH3(CH2)nCHOHCH2O-, carboxy, (2-quinolinyl)methoxy, oleyloxy, linoleyloxy, R8OOC(CH2)tO-, R6[O(CH2)2]qO- , or R7(CH2)pO-; R5 is CH3(CH2)n-, 1-adamantyl or diphenylmethyl; R6 is lower alkyl; R7 is 1- or 2 -naphthyloxy, 1-, 2- or 3-pyridinyloxy, 2,3- or 3,4-dihydroxyphenyl, 6,7-dihydroxy-2-naphthyl, phenyl, phenoxy or substituted phenyl or phenoxy, wherein the substituent is selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, nitro, amino, halo, R6 S(O)0-2-, carboxy, carboxy-lower alkyl or phenyl; R8 is hydrogen or lower alkyl; n is an integer from 0 to 17; m is an integer from 1 to 3; t is an integer from 1 to 10; p is an integer from 2 to 18, and q is an integer from 1 to 6; and when R2 is hydrogen, a pharmaceutically acceptable salt thereof with a base, are potent inhibitors of phospholipases A2 (PLA2's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.</abstract><edition>5</edition><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 N-substituted anilines
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