1-phenylpyrazole-3-carboxamides acting on neurotensin receptors
1-Phenyl pyrazole-3-carboxamides of formula (I), their salts, quaternary ammonium salts formed with tertiary amines, and their solvates, are new. R1 = TCN, C(NH2)=NOH, C(=NOH)NH(CH2)rNR5R6, TC(NR12R13)=NR14, C(NH2)=NO(CH2)rNR5R6, TCONRaRb, TCONR7Rc, YCOOR7, ORd, TNR5R6 (provided R5 and R6 are not bo...
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| creator | JEANARLES MOLIMARD ROBERT BOIGEGRAIN BERNARD LABEEUW FRANCIS JEANJEAN DANIELLE GULLY |
| description | 1-Phenyl pyrazole-3-carboxamides of formula (I), their salts, quaternary ammonium salts formed with tertiary amines, and their solvates, are new. R1 = TCN, C(NH2)=NOH, C(=NOH)NH(CH2)rNR5R6, TC(NR12R13)=NR14, C(NH2)=NO(CH2)rNR5R6, TCONRaRb, TCONR7Rc, YCOOR7, ORd, TNR5R6 (provided R5 and R6 are not both H when T is a direct bond), TN(R7)CORe, SO2NRaRb, TN(R7)SO2R'7, TNR27R28; NRaRb = NR5R6, NR9(CH2)sCR7R8(CH2)tNR5R6, NR21(CH)sCR7R8(CH2)tNR22R23R24Q , a gp. of formula (i)-(v), NR7(CH2)qCN, NR7(CH2)qC(NR12R13)=NR14, NR7(CH2)qCONH2, NR7(CH2)qCOOR7, NR21(CH2)sCR7R8(CH2)tNR25R26; Rc = XOR7, CH2R20COOR7 or (CH2)4CH(NH2)COOR7; Rd = XNR5R6, YCONR5R6, YCOOR7, YSO2NR5R6, or a gp. of formula (vi) or (vii); Re = R16, YNR5R6, YNHCOR16, CH(R17)NR5R6, YNR22R23R24Q, a gp. (vi), (CH2)qCN, (CH2)qC(NR12R13)=NR14 or NR18R19; R2, R3 = H, 1-6C alkyl, (3-8C cycloalkyl)-methyl, 3-8C cycloalkyl, halo, nitro, CF3, OR4, NR5R6, pyrrol-1-yl, cyano or carbamoyl; or R2+R3 = trimethylene, tetramethylene, or pentamethylene; R4 = H, 1-6C alkyl, 3-4C alkenyl, 3-8C cycloalkyl, (3-8C cycloalkyl)methyl, (1-4C alkoxy)(1-4C alkylene), or benzyl; R5, R6 = H, 1-6C alkyl, 3-8C alkenyl, (3-8C cycloalkyl)methyl, or benzyl; or NR5R6 = pyrrolidine, piperidine, morpholine, thiomorpholine, (4-R9)-piperazine, aziridine, azetidine or perhydroazepine ring; R5', R6' = H or 1-6C alkyl; or NR5'R6' = pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine or (4-(1-6C alkyl)-piperazine; R7' = 1-4C alkyl; phenyl opt. substd by one or more 1-4C alkyl; or XNR5R6; R7 = H, 1-4C alkyl, or benzyl; R8 = H, 1-4C alkyl or OH; or CR7R8 = 3-5C cycloalkane; R9 = H, 1-4C alkyl, benzyl, XOH, XNR5'R6' or 3-8C alkenyl; R10 = H, 1-4C alkyl, benzyl, carbamoyl, or cyano; R11 = H, 1-4C alkyl, XOH, or XNR5'R6'; R12, R13 = H or 1-4C alkyl; R14 = H; or may be 1-4C alkyl when R12 = H and R13 = alkyl; or R13+R14 = Z; R15 = H, 1-4C alkyl or (CH2)sNR5R6; R16 = H, 1-8C alkyl, 3-8C cycloalkyl, phenyl, or piperid-2-, -3- or -4-yl; R17 = 1-6C alkyl, phenyl, benzyl, hydroxy-(1-4C alkyl), or amino(1-4C alkyl); R18, R19 = H or 1-4C alkyl; R18 may also be (CH2)qNR5R6; or NR18R19 = pyrrolidine, piperidine, morpholine, thiomorpholine or (4-R9)-piperazine; R20 = H, 1-4C alkyl, benzyl, hydroxyphenylmethyl, hydroxy(1-4C alkyl), mercapto(1-4C alkyl), (CH2)3NHC(=NH)NH2, (CH2)4NH2, or CH2-Im; Im = imidazol-4-yl; R21 = 1-4C alkyl, allyl, or benzyl; R22, R23 = 1-6C alkyl; or NR22R23 = pyrrolidine, piperidine, morpholine, or perhydroazepine |
| format | Patent |
| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_AU709119BB2</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>AU709119BB2</sourcerecordid><originalsourceid>FETCH-epo_espacenet_AU709119BB23</originalsourceid><addsrcrecordid>eNrjZLA31C3ISM2rzCmoLEqsys9J1TXWTU4sSsqvSMzNTEktVkhMLsnMS1fIz1PISy0tyi9JzSvOzFMoSk1OLSjJLyrmYWBNS8wpTuWF0twMCm6uIc4euqkF-fGpxQWJyal5qSXxjqHmBpaGhpZOTkbGRCgBAGcvMTU</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>1-phenylpyrazole-3-carboxamides acting on neurotensin receptors</title><source>esp@cenet</source><creator>JEANARLES MOLIMARD ; ROBERT BOIGEGRAIN ; BERNARD LABEEUW ; FRANCIS JEANJEAN ; DANIELLE GULLY</creator><creatorcontrib>JEANARLES MOLIMARD ; ROBERT BOIGEGRAIN ; BERNARD LABEEUW ; FRANCIS JEANJEAN ; DANIELLE GULLY</creatorcontrib><description>1-Phenyl pyrazole-3-carboxamides of formula (I), their salts, quaternary ammonium salts formed with tertiary amines, and their solvates, are new. R1 = TCN, C(NH2)=NOH, C(=NOH)NH(CH2)rNR5R6, TC(NR12R13)=NR14, C(NH2)=NO(CH2)rNR5R6, TCONRaRb, TCONR7Rc, YCOOR7, ORd, TNR5R6 (provided R5 and R6 are not both H when T is a direct bond), TN(R7)CORe, SO2NRaRb, TN(R7)SO2R'7, TNR27R28; NRaRb = NR5R6, NR9(CH2)sCR7R8(CH2)tNR5R6, NR21(CH)sCR7R8(CH2)tN<+>R22R23R24Q<-> , a gp. of formula (i)-(v), NR7(CH2)qCN, NR7(CH2)qC(NR12R13)=NR14, NR7(CH2)qCONH2, NR7(CH2)qCOOR7, NR21(CH2)sCR7R8(CH2)tNR25R26; Rc = XOR7, CH2R20COOR7 or (CH2)4CH(NH2)COOR7; Rd = XNR5R6, YCONR5R6, YCOOR7, YSO2NR5R6, or a gp. of formula (vi) or (vii); Re = R16, YNR5R6, YNHCOR16, CH(R17)NR5R6, YN<+>R22R23R24Q<->, a gp. (vi), (CH2)qCN, (CH2)qC(NR12R13)=NR14 or NR18R19; R2, R3 = H, 1-6C alkyl, (3-8C cycloalkyl)-methyl, 3-8C cycloalkyl, halo, nitro, CF3, OR4, NR5R6, pyrrol-1-yl, cyano or carbamoyl; or R2+R3 = trimethylene, tetramethylene, or pentamethylene; R4 = H, 1-6C alkyl, 3-4C alkenyl, 3-8C cycloalkyl, (3-8C cycloalkyl)methyl, (1-4C alkoxy)(1-4C alkylene), or benzyl; R5, R6 = H, 1-6C alkyl, 3-8C alkenyl, (3-8C cycloalkyl)methyl, or benzyl; or NR5R6 = pyrrolidine, piperidine, morpholine, thiomorpholine, (4-R9)-piperazine, aziridine, azetidine or perhydroazepine ring; R5', R6' = H or 1-6C alkyl; or NR5'R6' = pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine or (4-(1-6C alkyl)-piperazine; R7' = 1-4C alkyl; phenyl opt. substd by one or more 1-4C alkyl; or XNR5R6; R7 = H, 1-4C alkyl, or benzyl; R8 = H, 1-4C alkyl or OH; or CR7R8 = 3-5C cycloalkane; R9 = H, 1-4C alkyl, benzyl, XOH, XNR5'R6' or 3-8C alkenyl; R10 = H, 1-4C alkyl, benzyl, carbamoyl, or cyano; R11 = H, 1-4C alkyl, XOH, or XNR5'R6'; R12, R13 = H or 1-4C alkyl; R14 = H; or may be 1-4C alkyl when R12 = H and R13 = alkyl; or R13+R14 = Z; R15 = H, 1-4C alkyl or (CH2)sNR5R6; R16 = H, 1-8C alkyl, 3-8C cycloalkyl, phenyl, or piperid-2-, -3- or -4-yl; R17 = 1-6C alkyl, phenyl, benzyl, hydroxy-(1-4C alkyl), or amino(1-4C alkyl); R18, R19 = H or 1-4C alkyl; R18 may also be (CH2)qNR5R6; or NR18R19 = pyrrolidine, piperidine, morpholine, thiomorpholine or (4-R9)-piperazine; R20 = H, 1-4C alkyl, benzyl, hydroxyphenylmethyl, hydroxy(1-4C alkyl), mercapto(1-4C alkyl), (CH2)3NHC(=NH)NH2, (CH2)4NH2, or CH2-Im; Im = imidazol-4-yl; R21 = 1-4C alkyl, allyl, or benzyl; R22, R23 = 1-6C alkyl; or NR22R23 = pyrrolidine, piperidine, morpholine, or perhydroazepine; R24 = 1-4C alkyl, benzyl, allyl, hydroxy(1-4C alkyl), or (1-4C alkoxy)(1-4C alkyl); Q<-> = an anion; R25 = H or 1-6C alkyl; R26 = (1-4C alkoxy)carbonyl, benzyloxycarbonyl, or (1-4C alkyl)carbonyl; R27 = H, 1-4C alkyl, (1-4C alkyl)carbonyl, CO(CH2)rOH, or SO2R'7; R28 = XNR5R6; s, t = 0-3, with the proviso that (s+t) in the same group is 1 or more; r = 2-5; q = 1-5; T = a direct bond or 2-7C alkylene; X = 2-7C alkylene; Y = 2-7C alkylene; Z = 2-6C alkylene; AECN = a 4-7 membered saturated heterocycle, opt. substd by one or more 1-4C alkyl; NHAA(OH) = NHC(Xa)(Xa')COOH; Xa = H, and Xa' = H, 1-5C alkyl or a non-aromatic 3-15C carbocycle; or CXaXa' = a 3-15C non-aromatic carbocycle; and NGNL = piperazine, imidazolidine or imidazoline, all opt. substd. by 1 or more 1-4C alkyl. A number of intermediates for the preparation of these compounds are also claimed.</description><edition>6</edition><language>eng</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; 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>1999</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=19990819&DB=EPODOC&CC=AU&NR=709119B2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19990819&DB=EPODOC&CC=AU&NR=709119B2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>JEANARLES MOLIMARD</creatorcontrib><creatorcontrib>ROBERT BOIGEGRAIN</creatorcontrib><creatorcontrib>BERNARD LABEEUW</creatorcontrib><creatorcontrib>FRANCIS JEANJEAN</creatorcontrib><creatorcontrib>DANIELLE GULLY</creatorcontrib><title>1-phenylpyrazole-3-carboxamides acting on neurotensin receptors</title><description>1-Phenyl pyrazole-3-carboxamides of formula (I), their salts, quaternary ammonium salts formed with tertiary amines, and their solvates, are new. R1 = TCN, C(NH2)=NOH, C(=NOH)NH(CH2)rNR5R6, TC(NR12R13)=NR14, C(NH2)=NO(CH2)rNR5R6, TCONRaRb, TCONR7Rc, YCOOR7, ORd, TNR5R6 (provided R5 and R6 are not both H when T is a direct bond), TN(R7)CORe, SO2NRaRb, TN(R7)SO2R'7, TNR27R28; NRaRb = NR5R6, NR9(CH2)sCR7R8(CH2)tNR5R6, NR21(CH)sCR7R8(CH2)tN<+>R22R23R24Q<-> , a gp. of formula (i)-(v), NR7(CH2)qCN, NR7(CH2)qC(NR12R13)=NR14, NR7(CH2)qCONH2, NR7(CH2)qCOOR7, NR21(CH2)sCR7R8(CH2)tNR25R26; Rc = XOR7, CH2R20COOR7 or (CH2)4CH(NH2)COOR7; Rd = XNR5R6, YCONR5R6, YCOOR7, YSO2NR5R6, or a gp. of formula (vi) or (vii); Re = R16, YNR5R6, YNHCOR16, CH(R17)NR5R6, YN<+>R22R23R24Q<->, a gp. (vi), (CH2)qCN, (CH2)qC(NR12R13)=NR14 or NR18R19; R2, R3 = H, 1-6C alkyl, (3-8C cycloalkyl)-methyl, 3-8C cycloalkyl, halo, nitro, CF3, OR4, NR5R6, pyrrol-1-yl, cyano or carbamoyl; or R2+R3 = trimethylene, tetramethylene, or pentamethylene; R4 = H, 1-6C alkyl, 3-4C alkenyl, 3-8C cycloalkyl, (3-8C cycloalkyl)methyl, (1-4C alkoxy)(1-4C alkylene), or benzyl; R5, R6 = H, 1-6C alkyl, 3-8C alkenyl, (3-8C cycloalkyl)methyl, or benzyl; or NR5R6 = pyrrolidine, piperidine, morpholine, thiomorpholine, (4-R9)-piperazine, aziridine, azetidine or perhydroazepine ring; R5', R6' = H or 1-6C alkyl; or NR5'R6' = pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine or (4-(1-6C alkyl)-piperazine; R7' = 1-4C alkyl; phenyl opt. substd by one or more 1-4C alkyl; or XNR5R6; R7 = H, 1-4C alkyl, or benzyl; R8 = H, 1-4C alkyl or OH; or CR7R8 = 3-5C cycloalkane; R9 = H, 1-4C alkyl, benzyl, XOH, XNR5'R6' or 3-8C alkenyl; R10 = H, 1-4C alkyl, benzyl, carbamoyl, or cyano; R11 = H, 1-4C alkyl, XOH, or XNR5'R6'; R12, R13 = H or 1-4C alkyl; R14 = H; or may be 1-4C alkyl when R12 = H and R13 = alkyl; or R13+R14 = Z; R15 = H, 1-4C alkyl or (CH2)sNR5R6; R16 = H, 1-8C alkyl, 3-8C cycloalkyl, phenyl, or piperid-2-, -3- or -4-yl; R17 = 1-6C alkyl, phenyl, benzyl, hydroxy-(1-4C alkyl), or amino(1-4C alkyl); R18, R19 = H or 1-4C alkyl; R18 may also be (CH2)qNR5R6; or NR18R19 = pyrrolidine, piperidine, morpholine, thiomorpholine or (4-R9)-piperazine; R20 = H, 1-4C alkyl, benzyl, hydroxyphenylmethyl, hydroxy(1-4C alkyl), mercapto(1-4C alkyl), (CH2)3NHC(=NH)NH2, (CH2)4NH2, or CH2-Im; Im = imidazol-4-yl; R21 = 1-4C alkyl, allyl, or benzyl; R22, R23 = 1-6C alkyl; or NR22R23 = pyrrolidine, piperidine, morpholine, or perhydroazepine; R24 = 1-4C alkyl, benzyl, allyl, hydroxy(1-4C alkyl), or (1-4C alkoxy)(1-4C alkyl); Q<-> = an anion; R25 = H or 1-6C alkyl; R26 = (1-4C alkoxy)carbonyl, benzyloxycarbonyl, or (1-4C alkyl)carbonyl; R27 = H, 1-4C alkyl, (1-4C alkyl)carbonyl, CO(CH2)rOH, or SO2R'7; R28 = XNR5R6; s, t = 0-3, with the proviso that (s+t) in the same group is 1 or more; r = 2-5; q = 1-5; T = a direct bond or 2-7C alkylene; X = 2-7C alkylene; Y = 2-7C alkylene; Z = 2-6C alkylene; AECN = a 4-7 membered saturated heterocycle, opt. substd by one or more 1-4C alkyl; NHAA(OH) = NHC(Xa)(Xa')COOH; Xa = H, and Xa' = H, 1-5C alkyl or a non-aromatic 3-15C carbocycle; or CXaXa' = a 3-15C non-aromatic carbocycle; and NGNL = piperazine, imidazolidine or imidazoline, all opt. substd. by 1 or more 1-4C alkyl. A number of intermediates for the preparation of these compounds are also claimed.</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</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>1999</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLA31C3ISM2rzCmoLEqsys9J1TXWTU4sSsqvSMzNTEktVkhMLsnMS1fIz1PISy0tyi9JzSvOzFMoSk1OLSjJLyrmYWBNS8wpTuWF0twMCm6uIc4euqkF-fGpxQWJyal5qSXxjqHmBpaGhpZOTkbGRCgBAGcvMTU</recordid><startdate>19990819</startdate><enddate>19990819</enddate><creator>JEANARLES MOLIMARD</creator><creator>ROBERT BOIGEGRAIN</creator><creator>BERNARD LABEEUW</creator><creator>FRANCIS JEANJEAN</creator><creator>DANIELLE GULLY</creator><scope>EVB</scope></search><sort><creationdate>19990819</creationdate><title>1-phenylpyrazole-3-carboxamides acting on neurotensin receptors</title><author>JEANARLES MOLIMARD ; ROBERT BOIGEGRAIN ; BERNARD LABEEUW ; FRANCIS JEANJEAN ; DANIELLE GULLY</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_AU709119BB23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1999</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</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>JEANARLES MOLIMARD</creatorcontrib><creatorcontrib>ROBERT BOIGEGRAIN</creatorcontrib><creatorcontrib>BERNARD LABEEUW</creatorcontrib><creatorcontrib>FRANCIS JEANJEAN</creatorcontrib><creatorcontrib>DANIELLE GULLY</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>JEANARLES MOLIMARD</au><au>ROBERT BOIGEGRAIN</au><au>BERNARD LABEEUW</au><au>FRANCIS JEANJEAN</au><au>DANIELLE GULLY</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>1-phenylpyrazole-3-carboxamides acting on neurotensin receptors</title><date>1999-08-19</date><risdate>1999</risdate><abstract>1-Phenyl pyrazole-3-carboxamides of formula (I), their salts, quaternary ammonium salts formed with tertiary amines, and their solvates, are new. R1 = TCN, C(NH2)=NOH, C(=NOH)NH(CH2)rNR5R6, TC(NR12R13)=NR14, C(NH2)=NO(CH2)rNR5R6, TCONRaRb, TCONR7Rc, YCOOR7, ORd, TNR5R6 (provided R5 and R6 are not both H when T is a direct bond), TN(R7)CORe, SO2NRaRb, TN(R7)SO2R'7, TNR27R28; NRaRb = NR5R6, NR9(CH2)sCR7R8(CH2)tNR5R6, NR21(CH)sCR7R8(CH2)tN<+>R22R23R24Q<-> , a gp. of formula (i)-(v), NR7(CH2)qCN, NR7(CH2)qC(NR12R13)=NR14, NR7(CH2)qCONH2, NR7(CH2)qCOOR7, NR21(CH2)sCR7R8(CH2)tNR25R26; Rc = XOR7, CH2R20COOR7 or (CH2)4CH(NH2)COOR7; Rd = XNR5R6, YCONR5R6, YCOOR7, YSO2NR5R6, or a gp. of formula (vi) or (vii); Re = R16, YNR5R6, YNHCOR16, CH(R17)NR5R6, YN<+>R22R23R24Q<->, a gp. (vi), (CH2)qCN, (CH2)qC(NR12R13)=NR14 or NR18R19; R2, R3 = H, 1-6C alkyl, (3-8C cycloalkyl)-methyl, 3-8C cycloalkyl, halo, nitro, CF3, OR4, NR5R6, pyrrol-1-yl, cyano or carbamoyl; or R2+R3 = trimethylene, tetramethylene, or pentamethylene; R4 = H, 1-6C alkyl, 3-4C alkenyl, 3-8C cycloalkyl, (3-8C cycloalkyl)methyl, (1-4C alkoxy)(1-4C alkylene), or benzyl; R5, R6 = H, 1-6C alkyl, 3-8C alkenyl, (3-8C cycloalkyl)methyl, or benzyl; or NR5R6 = pyrrolidine, piperidine, morpholine, thiomorpholine, (4-R9)-piperazine, aziridine, azetidine or perhydroazepine ring; R5', R6' = H or 1-6C alkyl; or NR5'R6' = pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine or (4-(1-6C alkyl)-piperazine; R7' = 1-4C alkyl; phenyl opt. substd by one or more 1-4C alkyl; or XNR5R6; R7 = H, 1-4C alkyl, or benzyl; R8 = H, 1-4C alkyl or OH; or CR7R8 = 3-5C cycloalkane; R9 = H, 1-4C alkyl, benzyl, XOH, XNR5'R6' or 3-8C alkenyl; R10 = H, 1-4C alkyl, benzyl, carbamoyl, or cyano; R11 = H, 1-4C alkyl, XOH, or XNR5'R6'; R12, R13 = H or 1-4C alkyl; R14 = H; or may be 1-4C alkyl when R12 = H and R13 = alkyl; or R13+R14 = Z; R15 = H, 1-4C alkyl or (CH2)sNR5R6; R16 = H, 1-8C alkyl, 3-8C cycloalkyl, phenyl, or piperid-2-, -3- or -4-yl; R17 = 1-6C alkyl, phenyl, benzyl, hydroxy-(1-4C alkyl), or amino(1-4C alkyl); R18, R19 = H or 1-4C alkyl; R18 may also be (CH2)qNR5R6; or NR18R19 = pyrrolidine, piperidine, morpholine, thiomorpholine or (4-R9)-piperazine; R20 = H, 1-4C alkyl, benzyl, hydroxyphenylmethyl, hydroxy(1-4C alkyl), mercapto(1-4C alkyl), (CH2)3NHC(=NH)NH2, (CH2)4NH2, or CH2-Im; Im = imidazol-4-yl; R21 = 1-4C alkyl, allyl, or benzyl; R22, R23 = 1-6C alkyl; or NR22R23 = pyrrolidine, piperidine, morpholine, or perhydroazepine; R24 = 1-4C alkyl, benzyl, allyl, hydroxy(1-4C alkyl), or (1-4C alkoxy)(1-4C alkyl); Q<-> = an anion; R25 = H or 1-6C alkyl; R26 = (1-4C alkoxy)carbonyl, benzyloxycarbonyl, or (1-4C alkyl)carbonyl; R27 = H, 1-4C alkyl, (1-4C alkyl)carbonyl, CO(CH2)rOH, or SO2R'7; R28 = XNR5R6; s, t = 0-3, with the proviso that (s+t) in the same group is 1 or more; r = 2-5; q = 1-5; T = a direct bond or 2-7C alkylene; X = 2-7C alkylene; Y = 2-7C alkylene; Z = 2-6C alkylene; AECN = a 4-7 membered saturated heterocycle, opt. substd by one or more 1-4C alkyl; NHAA(OH) = NHC(Xa)(Xa')COOH; Xa = H, and Xa' = H, 1-5C alkyl or a non-aromatic 3-15C carbocycle; or CXaXa' = a 3-15C non-aromatic carbocycle; and NGNL = piperazine, imidazolidine or imidazoline, all opt. substd. by 1 or more 1-4C alkyl. A number of intermediates for the preparation of these compounds are also claimed.</abstract><edition>6</edition><oa>free_for_read</oa></addata></record> |
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| subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS 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-phenylpyrazole-3-carboxamides acting on neurotensin receptors |
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