New heterocyclic substd. piperazine derivs
Pyrrolidinyl-, piperidinyl- and hexamethyleneimino-substd. piperazine derivs. (I) and their tautomers, stereoisomers (including mixtures) and salts are new. Ra = 3-pyrrolidinyl, 3- or 4-piperidinyl or 3- or 4- hexamethyleneiminyl opt. monosubstd. by 1-5C alkyl or aryl-1-3C alkyl (opt. monosubstd. on...
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| creator | GUTH, BRIAN., 88447 WARTHAUSEN, DE HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE PIEPER, HELMUT. DR., 88400 BIBERACH, DE WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE |
| description | Pyrrolidinyl-, piperidinyl- and hexamethyleneimino-substd. piperazine derivs. (I) and their tautomers, stereoisomers (including mixtures) and salts are new. Ra = 3-pyrrolidinyl, 3- or 4-piperidinyl or 3- or 4- hexamethyleneiminyl opt. monosubstd. by 1-5C alkyl or aryl-1-3C alkyl (opt. monosubstd. on or in alkyl part by COOH, 1-3C alkoxycarbonyl, CONH2, CONH(1-3C alkyl), CON(1-3C alkyl)2, vinyl or ethynyl); or, when this substit. is not on a C atom alpha to N, by OH, 1-3C alkoxy, NH2, NH(1-3C alkyl) or N(1-3C alkyl)2; or 1-6C alkanoyl; benzoyl; allyloxycarbonyl; 1-5C alkoxycarbonyl; or phenyl-1-3C alkoxycarbonyl; Rb, Rc = H; 1-5C alkyl; aryl; or aryl-1-5C alkyl; or together with the ethylene bridge between them form o-phenylene; and the piperazinylene gp. in (I) can contain 1 or 2 CO gps. in place of 1 or 2 CH2 gps.; Y1 = -A1-; -CO-; -CO-CO-; -A1-CO-; -CO-A1-; -SO2-A2-; -A2-SO2-; -CO-A1-CO-; -CO-NR1-CO-; -CO-NR1-A2-; -CO-NR1-A2-CO-; -CO-A2-NR1-CO-; -CO-A2-O-; or -CO-A2-NR1; R1 = H; 1-5C alkyl; aryl; or aryl-1-3C alkyl; A1 = 1-5C n-alkylene opt. monosubstd. by 1-5C alkyl, cyclohexyl-1-3C alkyl, aryl, aryl-1-3C alkyl or, when not alpha to a N atom, R1O; A2 = 1-4C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl or aryl-1-3C alkyl; Y2= phenylene; cyclohexylene; pyridinylene; 3- or 4- piperidinylene or 1,4-piperazinylene opt. contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom, and in the case of 4-piperidinylene opt. 4-substd. by R1O (N, O or O,O acetal or N, O or N,N bond must not be formed in linkage with Y1 or Y3); 1,4-ketopiperazinylene opt. monosubstd. alpha to CO gp. by 1-5C alkyl (opt. substd. by phenyl, R1O-phenyl, 1-3C alkoxycarbonyl or COOH); -NR1-B- linked to Y1 via the N atom; or -O-B- linked to Y1 via the O atom; B = phenylene; cyclohexylene; pyridinylene; or piperidinylene linked via the 3- or 4-position with the NR1 or O of Y2 and opt contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom; Y3 = -CO-; -A2-CO-; -CH2-CH(NHR2)-CO-; -NR2-A3-CO-; -CH2-NR2-A3-CO-; -O-A3-CO-; -CO-A3-CO-; or -CO-NR1-A3-CO-; A3 = 1-3C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl, pyridyl or aryl-1-3C alkyl; R2 = H; 1-5C alkyl; aryl-1-3C alkyl; aryl; 1-5C alkoxycarbonyl; 1-5C alkylsulphonyl; aryl-1-3C alkylsulphonyl or arylsulphonyl; formyl opt. monosubstd. by 1-4C alkyl, aryl or aryl-1-3C alkyl; and -A2-CO-, -NR2-A3-CO- and -O-A3-CO- are linked with Y2 via A2, NR2 and O, respectively, and -NR2-A3-CO-, -CH2-NR2-A3-CO- and -O-A3-CO- cannot be linked with a N at |
| format | Patent |
| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_DE19526678A1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>DE19526678A1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_DE19526678A13</originalsourceid><addsrcrecordid>eNrjZNDySy1XyEgtSS3KT65MzslMViguTSouSdFTKMgsSC1KrMrMS1VISS3KLCvmYWBNS8wpTuWF0twMim6uIc4euqkF-fGpxQWJyal5qSXxLq6GlqZGZmbmFo6GxsSoAQBHiSlK</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>New heterocyclic substd. piperazine derivs</title><source>esp@cenet</source><creator>GUTH, BRIAN., 88447 WARTHAUSEN, DE ; HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE ; LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE ; PIEPER, HELMUT. DR., 88400 BIBERACH, DE ; WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE ; AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE</creator><creatorcontrib>GUTH, BRIAN., 88447 WARTHAUSEN, DE ; HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE ; LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE ; PIEPER, HELMUT. DR., 88400 BIBERACH, DE ; WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE ; AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE</creatorcontrib><description>Pyrrolidinyl-, piperidinyl- and hexamethyleneimino-substd. piperazine derivs. (I) and their tautomers, stereoisomers (including mixtures) and salts are new. Ra = 3-pyrrolidinyl, 3- or 4-piperidinyl or 3- or 4- hexamethyleneiminyl opt. monosubstd. by 1-5C alkyl or aryl-1-3C alkyl (opt. monosubstd. on or in alkyl part by COOH, 1-3C alkoxycarbonyl, CONH2, CONH(1-3C alkyl), CON(1-3C alkyl)2, vinyl or ethynyl); or, when this substit. is not on a C atom alpha to N, by OH, 1-3C alkoxy, NH2, NH(1-3C alkyl) or N(1-3C alkyl)2; or 1-6C alkanoyl; benzoyl; allyloxycarbonyl; 1-5C alkoxycarbonyl; or phenyl-1-3C alkoxycarbonyl; Rb, Rc = H; 1-5C alkyl; aryl; or aryl-1-5C alkyl; or together with the ethylene bridge between them form o-phenylene; and the piperazinylene gp. in (I) can contain 1 or 2 CO gps. in place of 1 or 2 CH2 gps.; Y1 = -A1-; -CO-; -CO-CO-; -A1-CO-; -CO-A1-; -SO2-A2-; -A2-SO2-; -CO-A1-CO-; -CO-NR1-CO-; -CO-NR1-A2-; -CO-NR1-A2-CO-; -CO-A2-NR1-CO-; -CO-A2-O-; or -CO-A2-NR1; R1 = H; 1-5C alkyl; aryl; or aryl-1-3C alkyl; A1 = 1-5C n-alkylene opt. monosubstd. by 1-5C alkyl, cyclohexyl-1-3C alkyl, aryl, aryl-1-3C alkyl or, when not alpha to a N atom, R1O; A2 = 1-4C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl or aryl-1-3C alkyl; Y2= phenylene; cyclohexylene; pyridinylene; 3- or 4- piperidinylene or 1,4-piperazinylene opt. contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom, and in the case of 4-piperidinylene opt. 4-substd. by R1O (N, O or O,O acetal or N, O or N,N bond must not be formed in linkage with Y1 or Y3); 1,4-ketopiperazinylene opt. monosubstd. alpha to CO gp. by 1-5C alkyl (opt. substd. by phenyl, R1O-phenyl, 1-3C alkoxycarbonyl or COOH); -NR1-B- linked to Y1 via the N atom; or -O-B- linked to Y1 via the O atom; B = phenylene; cyclohexylene; pyridinylene; or piperidinylene linked via the 3- or 4-position with the NR1 or O of Y2 and opt contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom; Y3 = -CO-; -A2-CO-; -CH2-CH(NHR2)-CO-; -NR2-A3-CO-; -CH2-NR2-A3-CO-; -O-A3-CO-; -CO-A3-CO-; or -CO-NR1-A3-CO-; A3 = 1-3C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl, pyridyl or aryl-1-3C alkyl; R2 = H; 1-5C alkyl; aryl-1-3C alkyl; aryl; 1-5C alkoxycarbonyl; 1-5C alkylsulphonyl; aryl-1-3C alkylsulphonyl or arylsulphonyl; formyl opt. monosubstd. by 1-4C alkyl, aryl or aryl-1-3C alkyl; and -A2-CO-, -NR2-A3-CO- and -O-A3-CO- are linked with Y2 via A2, NR2 and O, respectively, and -NR2-A3-CO-, -CH2-NR2-A3-CO- and -O-A3-CO- cannot be linked with a N atom of Y2; E = OH; 1-6C alkoxy; phenyl-1-3C alkoxy; 3-9C cycloalkoxy (in which a 5-8C cycloalkyl ring is opt. mono- or disubstd. by 1-3C alkyl); 5-8C cycloalkoxy where a CH2 gp. in the 3- or 4-position of the cycloalkyl ring is (a) replaced by O or (b) replaced by imino opt. monosubstd. by alkyl, phenyl-1-3C alkyl, phenyl-1-3C alkoxy-carbonyl or 2-6C alkanoyl (the cycloalkane ring can also be opt. mono- or disubstd. by 1-3C alkyl); 4-7C cycloalkenyloxy; or 3-5C alkenyloxy or alkynyloxy both opt. substd. by phenyl ("provided that no C-O bonds are present where the C carries a double or triple bond"); 3-8C cycloalkyl-1-3C alkoxy; 8-10C bicycloalkoxy opt. mono- or disubstd. in bicycloalkyl gp. by 1-3C alkyl; 1,3-dihydro-3-oxo-1-isobenzofuranyloxy; or R5-CO-O-C(R R )-O-; or alpha -amino gp. of a natural amino acid or its 1-6C alkyl, 2-6C alkenyl, 5-7C cycloalkyl, phenyl or phenyl-1-3C alkyl ester; R3 = H; 1=6C alkyl; 3-7C cycloalkyl; or phenyl; R4 = H or 1-6C alkyl; R5 = 1-5C alkyl; 1-5C alkoxy; 5-7C cycloalkyl; or 5-7C cycloalkoxy.</description><edition>6</edition><language>eng ; ger</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>1997</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=19970123&DB=EPODOC&CC=DE&NR=19526678A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76289</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19970123&DB=EPODOC&CC=DE&NR=19526678A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>GUTH, BRIAN., 88447 WARTHAUSEN, DE</creatorcontrib><creatorcontrib>HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE</creatorcontrib><creatorcontrib>LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE</creatorcontrib><creatorcontrib>PIEPER, HELMUT. DR., 88400 BIBERACH, DE</creatorcontrib><creatorcontrib>WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE</creatorcontrib><creatorcontrib>AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE</creatorcontrib><title>New heterocyclic substd. piperazine derivs</title><description>Pyrrolidinyl-, piperidinyl- and hexamethyleneimino-substd. piperazine derivs. (I) and their tautomers, stereoisomers (including mixtures) and salts are new. Ra = 3-pyrrolidinyl, 3- or 4-piperidinyl or 3- or 4- hexamethyleneiminyl opt. monosubstd. by 1-5C alkyl or aryl-1-3C alkyl (opt. monosubstd. on or in alkyl part by COOH, 1-3C alkoxycarbonyl, CONH2, CONH(1-3C alkyl), CON(1-3C alkyl)2, vinyl or ethynyl); or, when this substit. is not on a C atom alpha to N, by OH, 1-3C alkoxy, NH2, NH(1-3C alkyl) or N(1-3C alkyl)2; or 1-6C alkanoyl; benzoyl; allyloxycarbonyl; 1-5C alkoxycarbonyl; or phenyl-1-3C alkoxycarbonyl; Rb, Rc = H; 1-5C alkyl; aryl; or aryl-1-5C alkyl; or together with the ethylene bridge between them form o-phenylene; and the piperazinylene gp. in (I) can contain 1 or 2 CO gps. in place of 1 or 2 CH2 gps.; Y1 = -A1-; -CO-; -CO-CO-; -A1-CO-; -CO-A1-; -SO2-A2-; -A2-SO2-; -CO-A1-CO-; -CO-NR1-CO-; -CO-NR1-A2-; -CO-NR1-A2-CO-; -CO-A2-NR1-CO-; -CO-A2-O-; or -CO-A2-NR1; R1 = H; 1-5C alkyl; aryl; or aryl-1-3C alkyl; A1 = 1-5C n-alkylene opt. monosubstd. by 1-5C alkyl, cyclohexyl-1-3C alkyl, aryl, aryl-1-3C alkyl or, when not alpha to a N atom, R1O; A2 = 1-4C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl or aryl-1-3C alkyl; Y2= phenylene; cyclohexylene; pyridinylene; 3- or 4- piperidinylene or 1,4-piperazinylene opt. contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom, and in the case of 4-piperidinylene opt. 4-substd. by R1O (N, O or O,O acetal or N, O or N,N bond must not be formed in linkage with Y1 or Y3); 1,4-ketopiperazinylene opt. monosubstd. alpha to CO gp. by 1-5C alkyl (opt. substd. by phenyl, R1O-phenyl, 1-3C alkoxycarbonyl or COOH); -NR1-B- linked to Y1 via the N atom; or -O-B- linked to Y1 via the O atom; B = phenylene; cyclohexylene; pyridinylene; or piperidinylene linked via the 3- or 4-position with the NR1 or O of Y2 and opt contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom; Y3 = -CO-; -A2-CO-; -CH2-CH(NHR2)-CO-; -NR2-A3-CO-; -CH2-NR2-A3-CO-; -O-A3-CO-; -CO-A3-CO-; or -CO-NR1-A3-CO-; A3 = 1-3C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl, pyridyl or aryl-1-3C alkyl; R2 = H; 1-5C alkyl; aryl-1-3C alkyl; aryl; 1-5C alkoxycarbonyl; 1-5C alkylsulphonyl; aryl-1-3C alkylsulphonyl or arylsulphonyl; formyl opt. monosubstd. by 1-4C alkyl, aryl or aryl-1-3C alkyl; and -A2-CO-, -NR2-A3-CO- and -O-A3-CO- are linked with Y2 via A2, NR2 and O, respectively, and -NR2-A3-CO-, -CH2-NR2-A3-CO- and -O-A3-CO- cannot be linked with a N atom of Y2; E = OH; 1-6C alkoxy; phenyl-1-3C alkoxy; 3-9C cycloalkoxy (in which a 5-8C cycloalkyl ring is opt. mono- or disubstd. by 1-3C alkyl); 5-8C cycloalkoxy where a CH2 gp. in the 3- or 4-position of the cycloalkyl ring is (a) replaced by O or (b) replaced by imino opt. monosubstd. by alkyl, phenyl-1-3C alkyl, phenyl-1-3C alkoxy-carbonyl or 2-6C alkanoyl (the cycloalkane ring can also be opt. mono- or disubstd. by 1-3C alkyl); 4-7C cycloalkenyloxy; or 3-5C alkenyloxy or alkynyloxy both opt. substd. by phenyl ("provided that no C-O bonds are present where the C carries a double or triple bond"); 3-8C cycloalkyl-1-3C alkoxy; 8-10C bicycloalkoxy opt. mono- or disubstd. in bicycloalkyl gp. by 1-3C alkyl; 1,3-dihydro-3-oxo-1-isobenzofuranyloxy; or R5-CO-O-C(R R )-O-; or alpha -amino gp. of a natural amino acid or its 1-6C alkyl, 2-6C alkenyl, 5-7C cycloalkyl, phenyl or phenyl-1-3C alkyl ester; R3 = H; 1=6C alkyl; 3-7C cycloalkyl; or phenyl; R4 = H or 1-6C alkyl; R5 = 1-5C alkyl; 1-5C alkoxy; 5-7C cycloalkyl; or 5-7C cycloalkoxy.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1997</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZNDySy1XyEgtSS3KT65MzslMViguTSouSdFTKMgsSC1KrMrMS1VISS3KLCvmYWBNS8wpTuWF0twMim6uIc4euqkF-fGpxQWJyal5qSXxLq6GlqZGZmbmFo6GxsSoAQBHiSlK</recordid><startdate>19970123</startdate><enddate>19970123</enddate><creator>GUTH, BRIAN., 88447 WARTHAUSEN, DE</creator><creator>HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE</creator><creator>LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE</creator><creator>PIEPER, HELMUT. DR., 88400 BIBERACH, DE</creator><creator>WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE</creator><creator>AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE</creator><scope>EVB</scope></search><sort><creationdate>19970123</creationdate><title>New heterocyclic substd. piperazine derivs</title><author>GUTH, BRIAN., 88447 WARTHAUSEN, DE ; HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE ; LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE ; PIEPER, HELMUT. DR., 88400 BIBERACH, DE ; WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE ; AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_DE19526678A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; ger</language><creationdate>1997</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>GUTH, BRIAN., 88447 WARTHAUSEN, DE</creatorcontrib><creatorcontrib>HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE</creatorcontrib><creatorcontrib>LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE</creatorcontrib><creatorcontrib>PIEPER, HELMUT. DR., 88400 BIBERACH, DE</creatorcontrib><creatorcontrib>WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE</creatorcontrib><creatorcontrib>AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>GUTH, BRIAN., 88447 WARTHAUSEN, DE</au><au>HIMMELSBACH, FRANK. DR., 88441 MITTELBIBERACH, DE</au><au>LINZ, GUENTER. DR., 88441 MITTELBIBERACH, DE</au><au>PIEPER, HELMUT. DR., 88400 BIBERACH, DE</au><au>WEISENBERGER, JOHANNES. DR., 88400 BIBERACH, DE</au><au>AUSTEL, VOLKHARD, .. DR., 88400 BIBERACH, DE</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>New heterocyclic substd. piperazine derivs</title><date>1997-01-23</date><risdate>1997</risdate><abstract>Pyrrolidinyl-, piperidinyl- and hexamethyleneimino-substd. piperazine derivs. (I) and their tautomers, stereoisomers (including mixtures) and salts are new. Ra = 3-pyrrolidinyl, 3- or 4-piperidinyl or 3- or 4- hexamethyleneiminyl opt. monosubstd. by 1-5C alkyl or aryl-1-3C alkyl (opt. monosubstd. on or in alkyl part by COOH, 1-3C alkoxycarbonyl, CONH2, CONH(1-3C alkyl), CON(1-3C alkyl)2, vinyl or ethynyl); or, when this substit. is not on a C atom alpha to N, by OH, 1-3C alkoxy, NH2, NH(1-3C alkyl) or N(1-3C alkyl)2; or 1-6C alkanoyl; benzoyl; allyloxycarbonyl; 1-5C alkoxycarbonyl; or phenyl-1-3C alkoxycarbonyl; Rb, Rc = H; 1-5C alkyl; aryl; or aryl-1-5C alkyl; or together with the ethylene bridge between them form o-phenylene; and the piperazinylene gp. in (I) can contain 1 or 2 CO gps. in place of 1 or 2 CH2 gps.; Y1 = -A1-; -CO-; -CO-CO-; -A1-CO-; -CO-A1-; -SO2-A2-; -A2-SO2-; -CO-A1-CO-; -CO-NR1-CO-; -CO-NR1-A2-; -CO-NR1-A2-CO-; -CO-A2-NR1-CO-; -CO-A2-O-; or -CO-A2-NR1; R1 = H; 1-5C alkyl; aryl; or aryl-1-3C alkyl; A1 = 1-5C n-alkylene opt. monosubstd. by 1-5C alkyl, cyclohexyl-1-3C alkyl, aryl, aryl-1-3C alkyl or, when not alpha to a N atom, R1O; A2 = 1-4C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl or aryl-1-3C alkyl; Y2= phenylene; cyclohexylene; pyridinylene; 3- or 4- piperidinylene or 1,4-piperazinylene opt. contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom, and in the case of 4-piperidinylene opt. 4-substd. by R1O (N, O or O,O acetal or N, O or N,N bond must not be formed in linkage with Y1 or Y3); 1,4-ketopiperazinylene opt. monosubstd. alpha to CO gp. by 1-5C alkyl (opt. substd. by phenyl, R1O-phenyl, 1-3C alkoxycarbonyl or COOH); -NR1-B- linked to Y1 via the N atom; or -O-B- linked to Y1 via the O atom; B = phenylene; cyclohexylene; pyridinylene; or piperidinylene linked via the 3- or 4-position with the NR1 or O of Y2 and opt contg. 1 CO gp. in place of 1 CH2 gp. adjacent to a N atom; Y3 = -CO-; -A2-CO-; -CH2-CH(NHR2)-CO-; -NR2-A3-CO-; -CH2-NR2-A3-CO-; -O-A3-CO-; -CO-A3-CO-; or -CO-NR1-A3-CO-; A3 = 1-3C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl, pyridyl or aryl-1-3C alkyl; R2 = H; 1-5C alkyl; aryl-1-3C alkyl; aryl; 1-5C alkoxycarbonyl; 1-5C alkylsulphonyl; aryl-1-3C alkylsulphonyl or arylsulphonyl; formyl opt. monosubstd. by 1-4C alkyl, aryl or aryl-1-3C alkyl; and -A2-CO-, -NR2-A3-CO- and -O-A3-CO- are linked with Y2 via A2, NR2 and O, respectively, and -NR2-A3-CO-, -CH2-NR2-A3-CO- and -O-A3-CO- cannot be linked with a N atom of Y2; E = OH; 1-6C alkoxy; phenyl-1-3C alkoxy; 3-9C cycloalkoxy (in which a 5-8C cycloalkyl ring is opt. mono- or disubstd. by 1-3C alkyl); 5-8C cycloalkoxy where a CH2 gp. in the 3- or 4-position of the cycloalkyl ring is (a) replaced by O or (b) replaced by imino opt. monosubstd. by alkyl, phenyl-1-3C alkyl, phenyl-1-3C alkoxy-carbonyl or 2-6C alkanoyl (the cycloalkane ring can also be opt. mono- or disubstd. by 1-3C alkyl); 4-7C cycloalkenyloxy; or 3-5C alkenyloxy or alkynyloxy both opt. substd. by phenyl ("provided that no C-O bonds are present where the C carries a double or triple bond"); 3-8C cycloalkyl-1-3C alkoxy; 8-10C bicycloalkoxy opt. mono- or disubstd. in bicycloalkyl gp. by 1-3C alkyl; 1,3-dihydro-3-oxo-1-isobenzofuranyloxy; or R5-CO-O-C(R R )-O-; or alpha -amino gp. of a natural amino acid or its 1-6C alkyl, 2-6C alkenyl, 5-7C cycloalkyl, phenyl or phenyl-1-3C alkyl ester; R3 = H; 1=6C alkyl; 3-7C cycloalkyl; or phenyl; R4 = H or 1-6C alkyl; R5 = 1-5C alkyl; 1-5C alkoxy; 5-7C cycloalkyl; or 5-7C cycloalkoxy.</abstract><edition>6</edition><oa>free_for_read</oa></addata></record> |
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| language | eng ; ger |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY |
| title | New heterocyclic substd. piperazine derivs |
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