Antiulcer acylated 2-hydroxy-3-phenyl-1,3-di:amino-propane cpds. - prepd. e.g. by reacting the corresp non-acylated di:amine with reactive carboxylic acid deriv
Acylated diaminopropane derivs. of formula (I) and their acid addition salts are new: In (I) R1 is 1-20C alkyl, 2-7C alkenyl, 1,3-pentadien-1-yl, 3-7C cycloalkyl or 4-8C cycloalkylmethyl (both opt. substd. by CH3), 5-7C cycloalkenyl or 6-8C cycloalkenylmethyl (both opt. substd. by CH3), adamantyl, a...
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creator | HUESCHENS,ROLF,.DR MILKOWSKI,WOLFGANG,.DR HEINEMANN,HENNING,.DR WOLF,KLAUS-ULLRICH,DR ZEUGNER,HORST,.DR LIEPMANN,HANS,.DR HEMPEL,REINHARD,DR.MED HELL,INSA,DR |
description | Acylated diaminopropane derivs. of formula (I) and their acid addition salts are new: In (I) R1 is 1-20C alkyl, 2-7C alkenyl, 1,3-pentadien-1-yl, 3-7C cycloalkyl or 4-8C cycloalkylmethyl (both opt. substd. by CH3), 5-7C cycloalkenyl or 6-8C cycloalkenylmethyl (both opt. substd. by CH3), adamantyl, adamantylmethyl, benzyl or phenethyl (both opt. 3,4-dimethoxy substd.), phenyl substd. by 2 CH3O's, 3,4-methylenedioxy, 3,4-ethylenedioxy, 3,4-ethylenedioxy, 2-F, 4-F, or by 2-CF3, or R1 is 2-, 3- or 4-pyridyl, or furyl. R2=H, 1-3C alkyl or methoxyethyl. R3 and R4 = H, halo, 1-3C alkyl or alkoxy. The following cpds. are excluded: (a) R1=3,4-dimethoxy 2-F-, or 2-CF3-phenyl or 2-furyl; R2=CH3; R3=H and R4=4-Cl; (b) R1=3,4-dimethoxyphenyl; R2=CH3 and R3+R4 = 3,4-dimethoxy). The cpd. are made e.g. by reacting the corresp. unacylated diamine with a reactive deriv. of R1COOH. (I) are useful for treating ulcers and have no effects on gastric secretion or the CNS. The usual adult dose is 150-450 mg (orally) per day. The cpd. N-acetyl-N2-methyl-N2-(4-chlorophenyl)-2-hydroxy-1,3-diaminopropa- ne has 7-day oral LD50 in mice of 2.26g/kg. |
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fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_DE2720968A1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>DE2720968A1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_DE2720968A13</originalsourceid><addsrcrecordid>eNqNzjsOwjAQBNA0FAi4wx6AjUgi8esiCOIA9MjYS2LJ2NbGBHwbjoqLiJpqmqeZmWaf2gb9NJIYhIxGBFJQYhcVu3fECn1HNhoslhUqvRcPbR16dl5YAulVnwOCZ_IqB8rbHG4RmIQM2rYQumQcM_UerLP4GxibCF46dKMfkhV8S6tGy_RFJ0ash3k2uQvT02LMWQan5nI4I3l3Tc1CkqVwPTblplzt1tu6qP4gX8y0Uno</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Antiulcer acylated 2-hydroxy-3-phenyl-1,3-di:amino-propane cpds. - prepd. e.g. by reacting the corresp non-acylated di:amine with reactive carboxylic acid deriv</title><source>esp@cenet</source><creator>HUESCHENS,ROLF,.DR ; MILKOWSKI,WOLFGANG,.DR ; HEINEMANN,HENNING,.DR ; WOLF,KLAUS-ULLRICH,DR ; ZEUGNER,HORST,.DR ; LIEPMANN,HANS,.DR ; HEMPEL,REINHARD,DR.MED ; HELL,INSA,DR</creator><creatorcontrib>HUESCHENS,ROLF,.DR ; MILKOWSKI,WOLFGANG,.DR ; HEINEMANN,HENNING,.DR ; WOLF,KLAUS-ULLRICH,DR ; ZEUGNER,HORST,.DR ; LIEPMANN,HANS,.DR ; HEMPEL,REINHARD,DR.MED ; HELL,INSA,DR</creatorcontrib><description>Acylated diaminopropane derivs. of formula (I) and their acid addition salts are new: In (I) R1 is 1-20C alkyl, 2-7C alkenyl, 1,3-pentadien-1-yl, 3-7C cycloalkyl or 4-8C cycloalkylmethyl (both opt. substd. by CH3), 5-7C cycloalkenyl or 6-8C cycloalkenylmethyl (both opt. substd. by CH3), adamantyl, adamantylmethyl, benzyl or phenethyl (both opt. 3,4-dimethoxy substd.), phenyl substd. by 2 CH3O's, 3,4-methylenedioxy, 3,4-ethylenedioxy, 3,4-ethylenedioxy, 2-F, 4-F, or by 2-CF3, or R1 is 2-, 3- or 4-pyridyl, or furyl. R2=H, 1-3C alkyl or methoxyethyl. R3 and R4 = H, halo, 1-3C alkyl or alkoxy. The following cpds. are excluded: (a) R1=3,4-dimethoxy 2-F-, or 2-CF3-phenyl or 2-furyl; R2=CH3; R3=H and R4=4-Cl; (b) R1=3,4-dimethoxyphenyl; R2=CH3 and R3+R4 = 3,4-dimethoxy). The cpd. are made e.g. by reacting the corresp. unacylated diamine with a reactive deriv. of R1COOH. (I) are useful for treating ulcers and have no effects on gastric secretion or the CNS. The usual adult dose is 150-450 mg (orally) per day. The cpd. N-acetyl-N2-methyl-N2-(4-chlorophenyl)-2-hydroxy-1,3-diaminopropa- ne has 7-day oral LD50 in mice of 2.26g/kg.</description><edition>2</edition><language>eng ; ger</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>1978</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=19781123&DB=EPODOC&CC=DE&NR=2720968A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76294</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19781123&DB=EPODOC&CC=DE&NR=2720968A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>HUESCHENS,ROLF,.DR</creatorcontrib><creatorcontrib>MILKOWSKI,WOLFGANG,.DR</creatorcontrib><creatorcontrib>HEINEMANN,HENNING,.DR</creatorcontrib><creatorcontrib>WOLF,KLAUS-ULLRICH,DR</creatorcontrib><creatorcontrib>ZEUGNER,HORST,.DR</creatorcontrib><creatorcontrib>LIEPMANN,HANS,.DR</creatorcontrib><creatorcontrib>HEMPEL,REINHARD,DR.MED</creatorcontrib><creatorcontrib>HELL,INSA,DR</creatorcontrib><title>Antiulcer acylated 2-hydroxy-3-phenyl-1,3-di:amino-propane cpds. - prepd. e.g. by reacting the corresp non-acylated di:amine with reactive carboxylic acid deriv</title><description>Acylated diaminopropane derivs. of formula (I) and their acid addition salts are new: In (I) R1 is 1-20C alkyl, 2-7C alkenyl, 1,3-pentadien-1-yl, 3-7C cycloalkyl or 4-8C cycloalkylmethyl (both opt. substd. by CH3), 5-7C cycloalkenyl or 6-8C cycloalkenylmethyl (both opt. substd. by CH3), adamantyl, adamantylmethyl, benzyl or phenethyl (both opt. 3,4-dimethoxy substd.), phenyl substd. by 2 CH3O's, 3,4-methylenedioxy, 3,4-ethylenedioxy, 3,4-ethylenedioxy, 2-F, 4-F, or by 2-CF3, or R1 is 2-, 3- or 4-pyridyl, or furyl. R2=H, 1-3C alkyl or methoxyethyl. R3 and R4 = H, halo, 1-3C alkyl or alkoxy. The following cpds. are excluded: (a) R1=3,4-dimethoxy 2-F-, or 2-CF3-phenyl or 2-furyl; R2=CH3; R3=H and R4=4-Cl; (b) R1=3,4-dimethoxyphenyl; R2=CH3 and R3+R4 = 3,4-dimethoxy). The cpd. are made e.g. by reacting the corresp. unacylated diamine with a reactive deriv. of R1COOH. (I) are useful for treating ulcers and have no effects on gastric secretion or the CNS. The usual adult dose is 150-450 mg (orally) per day. The cpd. N-acetyl-N2-methyl-N2-(4-chlorophenyl)-2-hydroxy-1,3-diaminopropa- ne has 7-day oral LD50 in mice of 2.26g/kg.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1978</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNzjsOwjAQBNA0FAi4wx6AjUgi8esiCOIA9MjYS2LJ2NbGBHwbjoqLiJpqmqeZmWaf2gb9NJIYhIxGBFJQYhcVu3fECn1HNhoslhUqvRcPbR16dl5YAulVnwOCZ_IqB8rbHG4RmIQM2rYQumQcM_UerLP4GxibCF46dKMfkhV8S6tGy_RFJ0ash3k2uQvT02LMWQan5nI4I3l3Tc1CkqVwPTblplzt1tu6qP4gX8y0Uno</recordid><startdate>19781123</startdate><enddate>19781123</enddate><creator>HUESCHENS,ROLF,.DR</creator><creator>MILKOWSKI,WOLFGANG,.DR</creator><creator>HEINEMANN,HENNING,.DR</creator><creator>WOLF,KLAUS-ULLRICH,DR</creator><creator>ZEUGNER,HORST,.DR</creator><creator>LIEPMANN,HANS,.DR</creator><creator>HEMPEL,REINHARD,DR.MED</creator><creator>HELL,INSA,DR</creator><scope>EVB</scope></search><sort><creationdate>19781123</creationdate><title>Antiulcer acylated 2-hydroxy-3-phenyl-1,3-di:amino-propane cpds. - prepd. e.g. by reacting the corresp non-acylated di:amine with reactive carboxylic acid deriv</title><author>HUESCHENS,ROLF,.DR ; MILKOWSKI,WOLFGANG,.DR ; HEINEMANN,HENNING,.DR ; WOLF,KLAUS-ULLRICH,DR ; ZEUGNER,HORST,.DR ; LIEPMANN,HANS,.DR ; HEMPEL,REINHARD,DR.MED ; HELL,INSA,DR</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_DE2720968A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; ger</language><creationdate>1978</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>HUESCHENS,ROLF,.DR</creatorcontrib><creatorcontrib>MILKOWSKI,WOLFGANG,.DR</creatorcontrib><creatorcontrib>HEINEMANN,HENNING,.DR</creatorcontrib><creatorcontrib>WOLF,KLAUS-ULLRICH,DR</creatorcontrib><creatorcontrib>ZEUGNER,HORST,.DR</creatorcontrib><creatorcontrib>LIEPMANN,HANS,.DR</creatorcontrib><creatorcontrib>HEMPEL,REINHARD,DR.MED</creatorcontrib><creatorcontrib>HELL,INSA,DR</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>HUESCHENS,ROLF,.DR</au><au>MILKOWSKI,WOLFGANG,.DR</au><au>HEINEMANN,HENNING,.DR</au><au>WOLF,KLAUS-ULLRICH,DR</au><au>ZEUGNER,HORST,.DR</au><au>LIEPMANN,HANS,.DR</au><au>HEMPEL,REINHARD,DR.MED</au><au>HELL,INSA,DR</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Antiulcer acylated 2-hydroxy-3-phenyl-1,3-di:amino-propane cpds. - prepd. e.g. by reacting the corresp non-acylated di:amine with reactive carboxylic acid deriv</title><date>1978-11-23</date><risdate>1978</risdate><abstract>Acylated diaminopropane derivs. of formula (I) and their acid addition salts are new: In (I) R1 is 1-20C alkyl, 2-7C alkenyl, 1,3-pentadien-1-yl, 3-7C cycloalkyl or 4-8C cycloalkylmethyl (both opt. substd. by CH3), 5-7C cycloalkenyl or 6-8C cycloalkenylmethyl (both opt. substd. by CH3), adamantyl, adamantylmethyl, benzyl or phenethyl (both opt. 3,4-dimethoxy substd.), phenyl substd. by 2 CH3O's, 3,4-methylenedioxy, 3,4-ethylenedioxy, 3,4-ethylenedioxy, 2-F, 4-F, or by 2-CF3, or R1 is 2-, 3- or 4-pyridyl, or furyl. R2=H, 1-3C alkyl or methoxyethyl. R3 and R4 = H, halo, 1-3C alkyl or alkoxy. The following cpds. are excluded: (a) R1=3,4-dimethoxy 2-F-, or 2-CF3-phenyl or 2-furyl; R2=CH3; R3=H and R4=4-Cl; (b) R1=3,4-dimethoxyphenyl; R2=CH3 and R3+R4 = 3,4-dimethoxy). The cpd. are made e.g. by reacting the corresp. unacylated diamine with a reactive deriv. of R1COOH. (I) are useful for treating ulcers and have no effects on gastric secretion or the CNS. The usual adult dose is 150-450 mg (orally) per day. The cpd. N-acetyl-N2-methyl-N2-(4-chlorophenyl)-2-hydroxy-1,3-diaminopropa- ne has 7-day oral LD50 in mice of 2.26g/kg.</abstract><edition>2</edition><oa>free_for_read</oa></addata></record> |
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title | Antiulcer acylated 2-hydroxy-3-phenyl-1,3-di:amino-propane cpds. - prepd. e.g. by reacting the corresp non-acylated di:amine with reactive carboxylic acid deriv |
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