PYRAZOLE CONDENSED RING DERIVATIVE
PURPOSE:To obtain a new compound composed of a pyrazole condensed ring derivative having a specific structure, excellent in inhibiting action on manifestation of androgenic action and therapeutic effects on prostatic hypertrophy, prostatic cancer, etc., and having long duration of activity and high...
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| creator | YAMADA SATOSHI MIYAJIMA KEISUKE YAMAUCHI TAKESHI KIYOKAWA HIROSHI KISHI KAZUMASA TATSUMI KUNIHIKO KIYONO KUNIHIKO EDAMATSU HIROSHI |
| description | PURPOSE:To obtain a new compound composed of a pyrazole condensed ring derivative having a specific structure, excellent in inhibiting action on manifestation of androgenic action and therapeutic effects on prostatic hypertrophy, prostatic cancer, etc., and having long duration of activity and high oral absorptivity. CONSTITUTION:A benzoic acid derivative expressed by formula I [R and R are H or lower alkyl; R and R are H, lower alkyl, lower alkoxy, halogen, etc.; (m) is 1 or 2; (n) is 1, 2 or 3] is esterified and then reduced. The produced hydroxyl group is further halogenated and the resultant benzyl halide derivative expressed by formula II (X is halogen) reacts with a cyanogen compound and the formed acetonitrile derivative then reacts with a formic acid ester to afford a compound expressed by formula III, which reacts with semicarbazides to provide a compound expressed by formula IV. The prepared compound further reacts with an orthoformic acid ester to afford the new pyrazole condensed ring derivative, expressed by the formula V (A is CH or N) and capable of inhibiting the manifestation of androgenic action. |
| format | Patent |
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CONSTITUTION:A benzoic acid derivative expressed by formula I [R and R are H or lower alkyl; R and R are H, lower alkyl, lower alkoxy, halogen, etc.; (m) is 1 or 2; (n) is 1, 2 or 3] is esterified and then reduced. The produced hydroxyl group is further halogenated and the resultant benzyl halide derivative expressed by formula II (X is halogen) reacts with a cyanogen compound and the formed acetonitrile derivative then reacts with a formic acid ester to afford a compound expressed by formula III, which reacts with semicarbazides to provide a compound expressed by formula IV. The prepared compound further reacts with an orthoformic acid ester to afford the new pyrazole condensed ring derivative, expressed by the formula V (A is CH or N) and capable of inhibiting the manifestation of androgenic action.</description><edition>5</edition><language>eng</language><subject>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>1994</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=19941108&DB=EPODOC&CC=JP&NR=H06312987A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25555,76308</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19941108&DB=EPODOC&CC=JP&NR=H06312987A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>YAMADA SATOSHI</creatorcontrib><creatorcontrib>MIYAJIMA KEISUKE</creatorcontrib><creatorcontrib>YAMAUCHI TAKESHI</creatorcontrib><creatorcontrib>KIYOKAWA HIROSHI</creatorcontrib><creatorcontrib>KISHI KAZUMASA</creatorcontrib><creatorcontrib>TATSUMI KUNIHIKO</creatorcontrib><creatorcontrib>KIYONO KUNIHIKO</creatorcontrib><creatorcontrib>EDAMATSU HIROSHI</creatorcontrib><title>PYRAZOLE CONDENSED RING DERIVATIVE</title><description>PURPOSE:To obtain a new compound composed of a pyrazole condensed ring derivative having a specific structure, excellent in inhibiting action on manifestation of androgenic action and therapeutic effects on prostatic hypertrophy, prostatic cancer, etc., and having long duration of activity and high oral absorptivity. CONSTITUTION:A benzoic acid derivative expressed by formula I [R and R are H or lower alkyl; R and R are H, lower alkyl, lower alkoxy, halogen, etc.; (m) is 1 or 2; (n) is 1, 2 or 3] is esterified and then reduced. The produced hydroxyl group is further halogenated and the resultant benzyl halide derivative expressed by formula II (X is halogen) reacts with a cyanogen compound and the formed acetonitrile derivative then reacts with a formic acid ester to afford a compound expressed by formula III, which reacts with semicarbazides to provide a compound expressed by formula IV. The prepared compound further reacts with an orthoformic acid ester to afford the new pyrazole condensed ring derivative, expressed by the formula V (A is CH or N) and capable of inhibiting the manifestation of androgenic action.</description><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>1994</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZFAKiAxyjPL3cVVw9vdzcfULdnVRCPL0c1dwcQ3yDHMM8Qxz5WFgTUvMKU7lhdLcDIpuriHOHrqpBfnxqcUFicmpeakl8V4BHgZmxoZGlhbmjsbEqAEAUNgi3w</recordid><startdate>19941108</startdate><enddate>19941108</enddate><creator>YAMADA SATOSHI</creator><creator>MIYAJIMA KEISUKE</creator><creator>YAMAUCHI TAKESHI</creator><creator>KIYOKAWA HIROSHI</creator><creator>KISHI KAZUMASA</creator><creator>TATSUMI KUNIHIKO</creator><creator>KIYONO KUNIHIKO</creator><creator>EDAMATSU HIROSHI</creator><scope>EVB</scope></search><sort><creationdate>19941108</creationdate><title>PYRAZOLE CONDENSED RING DERIVATIVE</title><author>YAMADA SATOSHI ; MIYAJIMA KEISUKE ; YAMAUCHI TAKESHI ; KIYOKAWA HIROSHI ; KISHI KAZUMASA ; TATSUMI KUNIHIKO ; KIYONO KUNIHIKO ; EDAMATSU HIROSHI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_JPH06312987A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1994</creationdate><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>YAMADA SATOSHI</creatorcontrib><creatorcontrib>MIYAJIMA KEISUKE</creatorcontrib><creatorcontrib>YAMAUCHI TAKESHI</creatorcontrib><creatorcontrib>KIYOKAWA HIROSHI</creatorcontrib><creatorcontrib>KISHI KAZUMASA</creatorcontrib><creatorcontrib>TATSUMI KUNIHIKO</creatorcontrib><creatorcontrib>KIYONO KUNIHIKO</creatorcontrib><creatorcontrib>EDAMATSU HIROSHI</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>YAMADA SATOSHI</au><au>MIYAJIMA KEISUKE</au><au>YAMAUCHI TAKESHI</au><au>KIYOKAWA HIROSHI</au><au>KISHI KAZUMASA</au><au>TATSUMI KUNIHIKO</au><au>KIYONO KUNIHIKO</au><au>EDAMATSU HIROSHI</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PYRAZOLE CONDENSED RING DERIVATIVE</title><date>1994-11-08</date><risdate>1994</risdate><abstract>PURPOSE:To obtain a new compound composed of a pyrazole condensed ring derivative having a specific structure, excellent in inhibiting action on manifestation of androgenic action and therapeutic effects on prostatic hypertrophy, prostatic cancer, etc., and having long duration of activity and high oral absorptivity. CONSTITUTION:A benzoic acid derivative expressed by formula I [R and R are H or lower alkyl; R and R are H, lower alkyl, lower alkoxy, halogen, etc.; (m) is 1 or 2; (n) is 1, 2 or 3] is esterified and then reduced. The produced hydroxyl group is further halogenated and the resultant benzyl halide derivative expressed by formula II (X is halogen) reacts with a cyanogen compound and the formed acetonitrile derivative then reacts with a formic acid ester to afford a compound expressed by formula III, which reacts with semicarbazides to provide a compound expressed by formula IV. The prepared compound further reacts with an orthoformic acid ester to afford the new pyrazole condensed ring derivative, expressed by the formula V (A is CH or N) and capable of inhibiting the manifestation of androgenic action.</abstract><edition>5</edition><oa>free_for_read</oa></addata></record> |
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| subjects | 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 | PYRAZOLE CONDENSED RING DERIVATIVE |
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