Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Patent
1997-09-12
1999-07-06
Kumar, Shailendra
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
514522, 514535, 514539, 514540, 514541, 514542, 514562, 514564, 514595, 514596, 514597, 514598, 514925, 514927, 558417, 560 17, 560 29, 560 34, 562431, 562439, 564 48, 564 49, 564 50, A61K 3744, C07C 59235
Patent
active
059198249
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to aminophenol derivatives having binding inhibition against cholecystokinin receptors including gastrin receptor and useful as therapeutic agents for digestive diseases and central nervous system diseases.
BACKGROUND ART
Cholecystokinin (CCK) is a brain/gastrointestinal tract hormone and has a close connection with the central nervous system and the gastrointestinal tract. CCK receptors are categorized into two groups: CCK-A receptor which is found primarily within components of the digestive tract such as the pancreas or the biliary system and CCK-B receptor which is found in the brain. CCK-A receptor is considered to significantly participate in control of gastrointestinal motility and pancreatic juice system. CCK-B receptor is considered to significantly participate in appetite regulation and psychic activities.
On the other hand, Gastrin, known as a hormone stimulating gastric acid secretion and CCK have in common five C-terminal amino acid residues. Therefore, both are called members of the gastrin/CCK family. Gastrin receptor, which may be found in the gastrointestinal tract, pancreas, and the biliary system, are primarily found in gastric mucosal cells (parietal cells) and participate in the control of gastric acid and pepsin secretion. The gene encoding CCK-B receptor and gastrin receptor were cloned, and as a result, it was found that the amino acid sequences of the two receptors are identical (Y-M. Lee, et al., J. Biological Chem. 268 (11) 8164-8169, 1993).
As described hereinbefore, there are two groups of CCK receptors, and the CCK-B receptor is considered to be identical to the gastrin receptor. Various diseases are considered to manifest themselves through these receptors.
Accordingly, development of compounds having strong binding inhibition against one of CCK-A or gastrin (CCK-B) group of receptors is desired.
Accordingly, a general object of the present invention is to provide a compound exhibiting strong binding inhibition against members of either the gastrin (CCK-B) receptor or the CCK-A receptor.
DISCLOSURE OF THE INVENTION
The present inventors synthesized a vast number of aminophenol derivatives and investigated each derivative's action on CCK-A receptor and gastrin receptor. As a result, they found that the compounds represented by the following formula (1) have stronger gastrin receptor binding inhibition or CCK-A receptor binding inhibition than previously known compounds and thus are useful as medicines. The present invention was accomplished based on this finding.
Accordingly, the present invention provides a compound represented by the following formula (1): ##STR2## wherein X represents an oxygen atom or a sulfur atom, A represents a linear or branched alkylene group, other, each independently represent a hydrogen atom or an alkyl group, aryl group, a cycloalkyl group which may have a substituent, or a group --N(R.sup.6)R.sup.7 wherein R6 and R.sup.7 are identical to or different from each other, each independently representing a hydrogen atom, an alkyl group which may have a substituent, an alkoxyl group, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, a pyridyl group which may have a substituent, a thiazolyl group which may have a substituent, or R.sup.6 and R.sup.7, together with the adjacent nitrogen atom, form a saturated or unsaturated heterocyclic ring which may have a substituent; a salt thereof; or an optical isomer of the compound or the salt.
The present invention also provides a medicine which contains as an active component a compound of formula (1), a salt thereof, or an optical isomer of the compound or the salt.
The present invention also provides an anti-cholecystokinin agent and an anti-gastrin agent containing, as an active component, a compound of formula (1), a salt thereof, or an optical isomer of the compound or the salt.
The present invention also provides a preventive and therapeutic agent for peptic ulcers, gastritis, rectal/colonic cancer, Zollinger-Elli
REFERENCES:
patent: 4645678 (1987-02-01), Nofre et al.
patent: 5382590 (1995-01-01), Bourzat et al.
patent: 5663204 (1997-09-01), Dubroeucq et al.
Kawagoe Keiichi
Takeda Yasuyuki
Yokohama Shuichi
Yokomizo Aki
Yokomizo Yoshihiro
Daiichi Pharmaceutical Co. Ltd.
Kumar Shailendra
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