Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1991-05-15
1992-06-30
Morris, Patricia L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
548343, A61K 31415, C07D23390
Patent
active
051263610
ABSTRACT:
Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl.
Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position.
Furthermore, the compounds have remarkable antitumor activities and therefore can provide novel antitumor agents.
REFERENCES:
patent: 4924000 (1990-05-01), Hesse et al.
Matsuda Akira
Minakawa Noriaki
Sasaki Takuma
Ueda Tohru
Yanagi Yoshikazu
Miltenberger Lenora
Morris Patricia L.
Yamasa Shoyu Kabushiki Kaisha
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