SUBSTITUTED 1-PHENYPYRAZOLE-3-CARBOXYAMIDES AS ACTIVE SUBSTANCES IN RESPECT TO NEUROTENSIN RCEPTORS, THEIR PRODUCTION AND PHARMACEUTIC COMPOSITIONS CONTAINING THEM

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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Hauptverfasser:	LABEEUW BERNARD, BOIGEGRAIN ROBERT, GULLY DANIELLE, MOLIMARD JEANARLES, JEANJEAN FRANCIS
Format:	Patent
Sprache:	eng ; pol
Schlagworte:	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
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creator	LABEEUW BERNARD BOIGEGRAIN ROBERT GULLY DANIELLE MOLIMARD JEANARLES JEANJEAN FRANCIS
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
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fullrecord	<record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_PL188077BB1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>PL188077BB1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_PL188077BB13</originalsourceid><addsrcrecordid>eNqNi01qw0AMhb3JIrS5gw4QQ0wWyVaW1VoQS8OMJsTdhFCmq9IE0hvlorVLD1B48Hg_37J6pNwmF8_OHTR16FnHMEZ8swPX25owtnYacZCOE-Akcjky_FKoNJWiEDkFJgc3UM7RnDXNNXFwi2kN3rNECNG6PPGmgNpB6DEOSJxdCMiGYEnmMU1BHUVFX2dyeK4WH5fPe1n9-VMFL-zU1-V2PZf77fJevsr3ORya_X6z27Vts_3H5QduukaS</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>SUBSTITUTED 1-PHENYPYRAZOLE-3-CARBOXYAMIDES AS ACTIVE SUBSTANCES IN RESPECT TO NEUROTENSIN RCEPTORS, THEIR PRODUCTION AND PHARMACEUTIC COMPOSITIONS CONTAINING THEM</title><source>esp@cenet</source><creator>LABEEUW BERNARD ; BOIGEGRAIN ROBERT ; GULLY DANIELLE ; MOLIMARD JEANARLES ; JEANJEAN FRANCIS</creator><creatorcontrib>LABEEUW BERNARD ; BOIGEGRAIN ROBERT ; GULLY DANIELLE ; MOLIMARD JEANARLES ; JEANJEAN FRANCIS</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>7</edition><language>eng ; pol</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>2004</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=20041231&DB=EPODOC&CC=PL&NR=188077B1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20041231&DB=EPODOC&CC=PL&NR=188077B1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>LABEEUW BERNARD</creatorcontrib><creatorcontrib>BOIGEGRAIN ROBERT</creatorcontrib><creatorcontrib>GULLY DANIELLE</creatorcontrib><creatorcontrib>MOLIMARD JEANARLES</creatorcontrib><creatorcontrib>JEANJEAN FRANCIS</creatorcontrib><title>SUBSTITUTED 1-PHENYPYRAZOLE-3-CARBOXYAMIDES AS ACTIVE SUBSTANCES IN RESPECT TO NEUROTENSIN RCEPTORS, THEIR PRODUCTION AND PHARMACEUTIC COMPOSITIONS CONTAINING THEM</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>2004</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNi01qw0AMhb3JIrS5gw4QQ0wWyVaW1VoQS8OMJsTdhFCmq9IE0hvlorVLD1B48Hg_37J6pNwmF8_OHTR16FnHMEZ8swPX25owtnYacZCOE-Akcjky_FKoNJWiEDkFJgc3UM7RnDXNNXFwi2kN3rNECNG6PPGmgNpB6DEOSJxdCMiGYEnmMU1BHUVFX2dyeK4WH5fPe1n9-VMFL-zU1-V2PZf77fJevsr3ORya_X6z27Vts_3H5QduukaS</recordid><startdate>20041231</startdate><enddate>20041231</enddate><creator>LABEEUW BERNARD</creator><creator>BOIGEGRAIN ROBERT</creator><creator>GULLY DANIELLE</creator><creator>MOLIMARD JEANARLES</creator><creator>JEANJEAN FRANCIS</creator><scope>EVB</scope></search><sort><creationdate>20041231</creationdate><title>SUBSTITUTED 1-PHENYPYRAZOLE-3-CARBOXYAMIDES AS ACTIVE SUBSTANCES IN RESPECT TO NEUROTENSIN RCEPTORS, THEIR PRODUCTION AND PHARMACEUTIC COMPOSITIONS CONTAINING THEM</title><author>LABEEUW BERNARD ; BOIGEGRAIN ROBERT ; GULLY DANIELLE ; MOLIMARD JEANARLES ; JEANJEAN FRANCIS</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_PL188077BB13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; pol</language><creationdate>2004</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>LABEEUW BERNARD</creatorcontrib><creatorcontrib>BOIGEGRAIN ROBERT</creatorcontrib><creatorcontrib>GULLY DANIELLE</creatorcontrib><creatorcontrib>MOLIMARD JEANARLES</creatorcontrib><creatorcontrib>JEANJEAN FRANCIS</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>LABEEUW BERNARD</au><au>BOIGEGRAIN ROBERT</au><au>GULLY DANIELLE</au><au>MOLIMARD JEANARLES</au><au>JEANJEAN FRANCIS</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>SUBSTITUTED 1-PHENYPYRAZOLE-3-CARBOXYAMIDES AS ACTIVE SUBSTANCES IN RESPECT TO NEUROTENSIN RCEPTORS, THEIR PRODUCTION AND PHARMACEUTIC COMPOSITIONS CONTAINING THEM</title><date>2004-12-31</date><risdate>2004</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>7</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	SUBSTITUTED 1-PHENYPYRAZOLE-3-CARBOXYAMIDES AS ACTIVE SUBSTANCES IN RESPECT TO NEUROTENSIN RCEPTORS, THEIR PRODUCTION AND PHARMACEUTIC COMPOSITIONS CONTAINING THEM
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