1, 3 -dihydro -2H -imidazol -2 -one derivatives having PDEIV and cytokinin inhibiting activity
PCT No. PCT/EP96/01393 Sec. 371 Date Sep. 29, 1997 Sec. 102(e) Date Sep. 29, 1997 PCT Filed Mar. 28, 1996 PCT Pub. No. WO96/31487 PCT Pub. Date Oct. 10, 1996The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and...
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creator | E. J. E. FREYNE G. S. M. DIELS J. I. ANDRES-GIL |
description | PCT No. PCT/EP96/01393 Sec. 371 Date Sep. 29, 1997 Sec. 102(e) Date Sep. 29, 1997 PCT Filed Mar. 28, 1996 PCT Pub. No. WO96/31487 PCT Pub. Date Oct. 10, 1996The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1-6alkyloxy is a bivalent radical of formula Alk is C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof. |
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ANDRES-GIL</creatorcontrib><description>PCT No. PCT/EP96/01393 Sec. 371 Date Sep. 29, 1997 Sec. 102(e) Date Sep. 29, 1997 PCT Filed Mar. 28, 1996 PCT Pub. No. WO96/31487 PCT Pub. Date Oct. 10, 1996The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1-6alkyloxy is a bivalent radical of formula Alk is C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.</description><edition>6</edition><language>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>1998</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=19980506&DB=EPODOC&CC=CN&NR=1181073A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25544,76293</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19980506&DB=EPODOC&CC=CN&NR=1181073A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>E. 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Date Oct. 10, 1996The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1-6alkyloxy is a bivalent radical of formula Alk is C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.</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>1998</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqFirEKwjAQQLM4iPoN3gcYMGbQVWqlLuIgjpazOe1hvZQmFOLXW8Hd6fF4b6yuZgEWtOM6uc6DXhWg-cUO374ZDLQXAkcd9xi5pwA19iwPOO3ywwVQHFQp-icLC7DUfOP4zVgNN8c0VaM7NoFmP07UfJ-fs0JT60sKLVYkFMvsaMzGLNd2a_8fH3uoOO4</recordid><startdate>19980506</startdate><enddate>19980506</enddate><creator>E. J. E. 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FREYNE</creatorcontrib><creatorcontrib>G. S. M. DIELS</creatorcontrib><creatorcontrib>J. I. ANDRES-GIL</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>E. J. E. FREYNE</au><au>G. S. M. DIELS</au><au>J. I. ANDRES-GIL</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>1, 3 -dihydro -2H -imidazol -2 -one derivatives having PDEIV and cytokinin inhibiting activity</title><date>1998-05-06</date><risdate>1998</risdate><abstract>PCT No. PCT/EP96/01393 Sec. 371 Date Sep. 29, 1997 Sec. 102(e) Date Sep. 29, 1997 PCT Filed Mar. 28, 1996 PCT Pub. No. WO96/31487 PCT Pub. Date Oct. 10, 1996The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 each independently are hydrogen; C1-6alkyl; difluoromethyl; trifluoromethyl; C3-6cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C1-6alkylsulfonyl; arylsulfonyl; or substituted C1-10alkyl; R3 is hydrogen, halo or C1-6alkyloxy is a bivalent radical of formula Alk is C1-4alkanediyl; -A-B- is a bivalent radical of formula: -CR6=CR7- or -CHR6-CHR7-; L is hydrogen; optionally substituted C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C3-6alkenyl; optionally substituted piperidinyl; C1-6alkylsulfonyl or arylsulfonyl; aryl is optionally substituted phenyl; Het1 is morpholinyl or optionally substituted pyridinyl, -furanyl, -thienyl, -hydroxypyridinyl, -imidazolyl, -thiazolyl, -oxazolyl, -isoquinolinyl, -quinolinonyl, -piperidinyl, -piperazinyl; and Het2 is morpholinyl or optionally substituted piperidinyl, -piperazinyl, -pyridinyl, -furanyl or -thienyl; having PDE IV and cytokine inhibiting activity. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions thereof.</abstract><edition>6</edition><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 | 1, 3 -dihydro -2H -imidazol -2 -one derivatives having PDEIV and cytokinin inhibiting activity |
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