DERIVES DE BENZODIAZEPINE
1355170 Benzodiazepines F HOFFMANNLA ROCHE & CO AG 12 May 1972 [13 May 1971] 22368/72 Heading C2C Compounds of the general Formula (I) (B = CO, CH 2 ; R = H, halogen, CF 3 , NO 2 , amino, C 1-7 alkyl, 1-adamantylcarbonylamino, t-alkylcarbonylamino; R 1 = H, C 1-7 alkyl, hydroxyalkyl or aminoalky...
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| creator | E. BROGER G.F. FIELD L.H. STERNBACH |
| description | 1355170 Benzodiazepines F HOFFMANNLA ROCHE & CO AG 12 May 1972 [13 May 1971] 22368/72 Heading C2C Compounds of the general Formula (I) (B = CO, CH 2 ; R = H, halogen, CF 3 , NO 2 , amino, C 1-7 alkyl, 1-adamantylcarbonylamino, t-alkylcarbonylamino; R 1 = H, C 1-7 alkyl, hydroxyalkyl or aminoalkyl, C 2-7 alkenyl or alkynyl, cycloalkyl-(C 1-7 alkyl), C 1-7 alkylamino- (C 1-7 alkyl), di-(C 1-7 alkyl)amino-C 1-7 alkyl; R 2 = thiazolyl, isothiazolyl, pyrazolyl, 1-(C 1-7 alkyl)pyrazolyl, imidazolyl, 1-(C 1-7 alkyl)imidazolyl; R 3,4 = H or R 3+4 = C-N bond; R 5 =H, OH; provided that (i) when B = CO, R 3+4 = C-N bond, (ii) when B = CH 2 , R = halogen, NO 2 , amino, 1-adamantylcarbonylamino, talkylcarbonylamino, (iii) when B = CO, R 1 =H and R 2 = thiazolyl, R = amino, 1-adamantylcarbonylamino, t-alkylcarbonylamino and (iv) when R 5 = OH, B = CO and R 1 = C 1-7 alkyl) and their acid addition salts are prepared by standard methods, e.g. cyclizing an aminoacetamidophenyl ketone or reacting a 2-halo-5- nitrophenyl ketone with ethylene diamine or a derivative thereof, optionally followed by introduction of a 1-substituent, reduction of NO 2 to NH 3 and replacement of the latter by halogen and/or reduction of a 4,5-double bond. The preparation of α-(1-methyl-5-pyrazolyl)-5- chloro-2-nitrobenzyl alcohol, 5-chloro-2-nitrophenyl 1-methyl-5-pyrazolyl ketone, 2-amino-5- chlorophenyl 1-methyl-5-pyrazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-5-pyrazolyl ketone, α-(o-nitrophenyl)-2-thiazolylmethanol, o-nitrophenyl 2-thiazolyl ketone, o-aminophenyl 2-thiazolyl ketone, 2-bromoacetamidophenyl 2-thiazolyl ketone, 5-(2-thiazolyl)-1,3-dihydro-2H- 1,4-benzodiazepin-2-one, α-(2-thiazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 2- thiazolyl ketone, α-(1-methyl-5-pyrazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-5-pyrazolyl ketone, α-(1-methyl-2-imidazolyl)-5-chloro-2-nitrobenzyl alcohol, 5-chloro-2- nitrophenyl 1-methyl-2-imidazolyl ketone, 2-amino 5-chlorophenyl 1-methyl-2-imidazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-2-imidazolyl ketone, α-(1-methyl-2-imidazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-2-imidazolyl ketone, α-(5-chloro-2-nitrophenyl)-2-thiazolylmethanol, 5-chloro-2-nitrophenyl 2-thiazolyl ketone, 2-amino-5-chlorophenyl 2- thiazolyl ketone, 2-(2-bromoacetamido)-5-chlorophenyl 2-thiazolyl ketone, 7-chloro-5-(2-thiazolyl)- 1,3-dihydro-2H-1,4-benzodiazepin-2-one, α-(5- |
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_BE783475A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>BE783475A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_BE783475A3</originalsourceid><addsrcrecordid>eNrjZJB0cQ3yDHMNVnBxVXBy9Yvyd_F0jHIN8PRz5WFgTUvMKU7lhdLcDHJuriHOHrqpBfnxqcUFicmpeakl8U6u5hbGJuamjsYEFQAAWw8evA</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>DERIVES DE BENZODIAZEPINE</title><source>esp@cenet</source><creator>E. BROGER ; G.F. FIELD ; L.H. STERNBACH</creator><creatorcontrib>E. BROGER ; G.F. FIELD ; L.H. STERNBACH</creatorcontrib><description>1355170 Benzodiazepines F HOFFMANNLA ROCHE & CO AG 12 May 1972 [13 May 1971] 22368/72 Heading C2C Compounds of the general Formula (I) (B = CO, CH 2 ; R = H, halogen, CF 3 , NO 2 , amino, C 1-7 alkyl, 1-adamantylcarbonylamino, t-alkylcarbonylamino; R 1 = H, C 1-7 alkyl, hydroxyalkyl or aminoalkyl, C 2-7 alkenyl or alkynyl, cycloalkyl-(C 1-7 alkyl), C 1-7 alkylamino- (C 1-7 alkyl), di-(C 1-7 alkyl)amino-C 1-7 alkyl; R 2 = thiazolyl, isothiazolyl, pyrazolyl, 1-(C 1-7 alkyl)pyrazolyl, imidazolyl, 1-(C 1-7 alkyl)imidazolyl; R 3,4 = H or R 3+4 = C-N bond; R 5 =H, OH; provided that (i) when B = CO, R 3+4 = C-N bond, (ii) when B = CH 2 , R = halogen, NO 2 , amino, 1-adamantylcarbonylamino, talkylcarbonylamino, (iii) when B = CO, R 1 =H and R 2 = thiazolyl, R = amino, 1-adamantylcarbonylamino, t-alkylcarbonylamino and (iv) when R 5 = OH, B = CO and R 1 = C 1-7 alkyl) and their acid addition salts are prepared by standard methods, e.g. cyclizing an aminoacetamidophenyl ketone or reacting a 2-halo-5- nitrophenyl ketone with ethylene diamine or a derivative thereof, optionally followed by introduction of a 1-substituent, reduction of NO 2 to NH 3 and replacement of the latter by halogen and/or reduction of a 4,5-double bond. The preparation of α-(1-methyl-5-pyrazolyl)-5- chloro-2-nitrobenzyl alcohol, 5-chloro-2-nitrophenyl 1-methyl-5-pyrazolyl ketone, 2-amino-5- chlorophenyl 1-methyl-5-pyrazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-5-pyrazolyl ketone, α-(o-nitrophenyl)-2-thiazolylmethanol, o-nitrophenyl 2-thiazolyl ketone, o-aminophenyl 2-thiazolyl ketone, 2-bromoacetamidophenyl 2-thiazolyl ketone, 5-(2-thiazolyl)-1,3-dihydro-2H- 1,4-benzodiazepin-2-one, α-(2-thiazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 2- thiazolyl ketone, α-(1-methyl-5-pyrazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-5-pyrazolyl ketone, α-(1-methyl-2-imidazolyl)-5-chloro-2-nitrobenzyl alcohol, 5-chloro-2- nitrophenyl 1-methyl-2-imidazolyl ketone, 2-amino 5-chlorophenyl 1-methyl-2-imidazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-2-imidazolyl ketone, α-(1-methyl-2-imidazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-2-imidazolyl ketone, α-(5-chloro-2-nitrophenyl)-2-thiazolylmethanol, 5-chloro-2-nitrophenyl 2-thiazolyl ketone, 2-amino-5-chlorophenyl 2- thiazolyl ketone, 2-(2-bromoacetamido)-5-chlorophenyl 2-thiazolyl ketone, 7-chloro-5-(2-thiazolyl)- 1,3-dihydro-2H-1,4-benzodiazepin-2-one, α-(5- isothiazolyl)-5-chloro-2-nitrobenzyl alcohol, 5-chloro-2-nitrophenyl 5-isothiazolyl ketone, α-(5-isothiazolyl)-2-chloro-5-nitrobenzyl alcohol, 2-chloro- 5-nitrophenyl 5-isothiazolyl ketone, 2-amino-5- iodophenyl 2-thiazolyl ketone, 2-(2-bromoacetamido)-5-iodophenyl 2-thiazolyl ketone and 7-iodo-5- (2-thiazolyl)-1,3-dihydro-2H-1,4-benzodiazepin-2- one is described. The compounds (I) and their salts are anticonvulsants, muscle relaxants and sedatives, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.</description><language>fre</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>1972</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=19721116&DB=EPODOC&CC=BE&NR=783475A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76293</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19721116&DB=EPODOC&CC=BE&NR=783475A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>E. BROGER</creatorcontrib><creatorcontrib>G.F. FIELD</creatorcontrib><creatorcontrib>L.H. STERNBACH</creatorcontrib><title>DERIVES DE BENZODIAZEPINE</title><description>1355170 Benzodiazepines F HOFFMANNLA ROCHE & CO AG 12 May 1972 [13 May 1971] 22368/72 Heading C2C Compounds of the general Formula (I) (B = CO, CH 2 ; R = H, halogen, CF 3 , NO 2 , amino, C 1-7 alkyl, 1-adamantylcarbonylamino, t-alkylcarbonylamino; R 1 = H, C 1-7 alkyl, hydroxyalkyl or aminoalkyl, C 2-7 alkenyl or alkynyl, cycloalkyl-(C 1-7 alkyl), C 1-7 alkylamino- (C 1-7 alkyl), di-(C 1-7 alkyl)amino-C 1-7 alkyl; R 2 = thiazolyl, isothiazolyl, pyrazolyl, 1-(C 1-7 alkyl)pyrazolyl, imidazolyl, 1-(C 1-7 alkyl)imidazolyl; R 3,4 = H or R 3+4 = C-N bond; R 5 =H, OH; provided that (i) when B = CO, R 3+4 = C-N bond, (ii) when B = CH 2 , R = halogen, NO 2 , amino, 1-adamantylcarbonylamino, talkylcarbonylamino, (iii) when B = CO, R 1 =H and R 2 = thiazolyl, R = amino, 1-adamantylcarbonylamino, t-alkylcarbonylamino and (iv) when R 5 = OH, B = CO and R 1 = C 1-7 alkyl) and their acid addition salts are prepared by standard methods, e.g. cyclizing an aminoacetamidophenyl ketone or reacting a 2-halo-5- nitrophenyl ketone with ethylene diamine or a derivative thereof, optionally followed by introduction of a 1-substituent, reduction of NO 2 to NH 3 and replacement of the latter by halogen and/or reduction of a 4,5-double bond. The preparation of α-(1-methyl-5-pyrazolyl)-5- chloro-2-nitrobenzyl alcohol, 5-chloro-2-nitrophenyl 1-methyl-5-pyrazolyl ketone, 2-amino-5- chlorophenyl 1-methyl-5-pyrazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-5-pyrazolyl ketone, α-(o-nitrophenyl)-2-thiazolylmethanol, o-nitrophenyl 2-thiazolyl ketone, o-aminophenyl 2-thiazolyl ketone, 2-bromoacetamidophenyl 2-thiazolyl ketone, 5-(2-thiazolyl)-1,3-dihydro-2H- 1,4-benzodiazepin-2-one, α-(2-thiazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 2- thiazolyl ketone, α-(1-methyl-5-pyrazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-5-pyrazolyl ketone, α-(1-methyl-2-imidazolyl)-5-chloro-2-nitrobenzyl alcohol, 5-chloro-2- nitrophenyl 1-methyl-2-imidazolyl ketone, 2-amino 5-chlorophenyl 1-methyl-2-imidazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-2-imidazolyl ketone, α-(1-methyl-2-imidazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-2-imidazolyl ketone, α-(5-chloro-2-nitrophenyl)-2-thiazolylmethanol, 5-chloro-2-nitrophenyl 2-thiazolyl ketone, 2-amino-5-chlorophenyl 2- thiazolyl ketone, 2-(2-bromoacetamido)-5-chlorophenyl 2-thiazolyl ketone, 7-chloro-5-(2-thiazolyl)- 1,3-dihydro-2H-1,4-benzodiazepin-2-one, α-(5- isothiazolyl)-5-chloro-2-nitrobenzyl alcohol, 5-chloro-2-nitrophenyl 5-isothiazolyl ketone, α-(5-isothiazolyl)-2-chloro-5-nitrobenzyl alcohol, 2-chloro- 5-nitrophenyl 5-isothiazolyl ketone, 2-amino-5- iodophenyl 2-thiazolyl ketone, 2-(2-bromoacetamido)-5-iodophenyl 2-thiazolyl ketone and 7-iodo-5- (2-thiazolyl)-1,3-dihydro-2H-1,4-benzodiazepin-2- one is described. The compounds (I) and their salts are anticonvulsants, muscle relaxants and sedatives, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1972</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZJB0cQ3yDHMNVnBxVXBy9Yvyd_F0jHIN8PRz5WFgTUvMKU7lhdLcDHJuriHOHrqpBfnxqcUFicmpeakl8U6u5hbGJuamjsYEFQAAWw8evA</recordid><startdate>19721116</startdate><enddate>19721116</enddate><creator>E. BROGER</creator><creator>G.F. FIELD</creator><creator>L.H. STERNBACH</creator><scope>EVB</scope></search><sort><creationdate>19721116</creationdate><title>DERIVES DE BENZODIAZEPINE</title><author>E. BROGER ; G.F. FIELD ; L.H. STERNBACH</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_BE783475A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>fre</language><creationdate>1972</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>E. BROGER</creatorcontrib><creatorcontrib>G.F. FIELD</creatorcontrib><creatorcontrib>L.H. STERNBACH</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>E. BROGER</au><au>G.F. FIELD</au><au>L.H. STERNBACH</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>DERIVES DE BENZODIAZEPINE</title><date>1972-11-16</date><risdate>1972</risdate><abstract>1355170 Benzodiazepines F HOFFMANNLA ROCHE & CO AG 12 May 1972 [13 May 1971] 22368/72 Heading C2C Compounds of the general Formula (I) (B = CO, CH 2 ; R = H, halogen, CF 3 , NO 2 , amino, C 1-7 alkyl, 1-adamantylcarbonylamino, t-alkylcarbonylamino; R 1 = H, C 1-7 alkyl, hydroxyalkyl or aminoalkyl, C 2-7 alkenyl or alkynyl, cycloalkyl-(C 1-7 alkyl), C 1-7 alkylamino- (C 1-7 alkyl), di-(C 1-7 alkyl)amino-C 1-7 alkyl; R 2 = thiazolyl, isothiazolyl, pyrazolyl, 1-(C 1-7 alkyl)pyrazolyl, imidazolyl, 1-(C 1-7 alkyl)imidazolyl; R 3,4 = H or R 3+4 = C-N bond; R 5 =H, OH; provided that (i) when B = CO, R 3+4 = C-N bond, (ii) when B = CH 2 , R = halogen, NO 2 , amino, 1-adamantylcarbonylamino, talkylcarbonylamino, (iii) when B = CO, R 1 =H and R 2 = thiazolyl, R = amino, 1-adamantylcarbonylamino, t-alkylcarbonylamino and (iv) when R 5 = OH, B = CO and R 1 = C 1-7 alkyl) and their acid addition salts are prepared by standard methods, e.g. cyclizing an aminoacetamidophenyl ketone or reacting a 2-halo-5- nitrophenyl ketone with ethylene diamine or a derivative thereof, optionally followed by introduction of a 1-substituent, reduction of NO 2 to NH 3 and replacement of the latter by halogen and/or reduction of a 4,5-double bond. The preparation of α-(1-methyl-5-pyrazolyl)-5- chloro-2-nitrobenzyl alcohol, 5-chloro-2-nitrophenyl 1-methyl-5-pyrazolyl ketone, 2-amino-5- chlorophenyl 1-methyl-5-pyrazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-5-pyrazolyl ketone, α-(o-nitrophenyl)-2-thiazolylmethanol, o-nitrophenyl 2-thiazolyl ketone, o-aminophenyl 2-thiazolyl ketone, 2-bromoacetamidophenyl 2-thiazolyl ketone, 5-(2-thiazolyl)-1,3-dihydro-2H- 1,4-benzodiazepin-2-one, α-(2-thiazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 2- thiazolyl ketone, α-(1-methyl-5-pyrazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-5-pyrazolyl ketone, α-(1-methyl-2-imidazolyl)-5-chloro-2-nitrobenzyl alcohol, 5-chloro-2- nitrophenyl 1-methyl-2-imidazolyl ketone, 2-amino 5-chlorophenyl 1-methyl-2-imidazolyl ketone, 2-(2- bromoacetamido)-5-chlorophenyl 1-methyl-2-imidazolyl ketone, α-(1-methyl-2-imidazolyl)-2-chloro- 5-nitrobenzyl alcohol, 2-chloro-5-nitrophenyl 1- methyl-2-imidazolyl ketone, α-(5-chloro-2-nitrophenyl)-2-thiazolylmethanol, 5-chloro-2-nitrophenyl 2-thiazolyl ketone, 2-amino-5-chlorophenyl 2- thiazolyl ketone, 2-(2-bromoacetamido)-5-chlorophenyl 2-thiazolyl ketone, 7-chloro-5-(2-thiazolyl)- 1,3-dihydro-2H-1,4-benzodiazepin-2-one, α-(5- isothiazolyl)-5-chloro-2-nitrobenzyl alcohol, 5-chloro-2-nitrophenyl 5-isothiazolyl ketone, α-(5-isothiazolyl)-2-chloro-5-nitrobenzyl alcohol, 2-chloro- 5-nitrophenyl 5-isothiazolyl ketone, 2-amino-5- iodophenyl 2-thiazolyl ketone, 2-(2-bromoacetamido)-5-iodophenyl 2-thiazolyl ketone and 7-iodo-5- (2-thiazolyl)-1,3-dihydro-2H-1,4-benzodiazepin-2- one is described. The compounds (I) and their salts are anticonvulsants, muscle relaxants and sedatives, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier.</abstract><oa>free_for_read</oa></addata></record> |
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| title | DERIVES DE BENZODIAZEPINE |
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