Medicinal compositions promoting bowel movement
AssigneeEisai Co., Ltd.
InventorsMasahiro Yasuda, Hitoshi Harada, Shuhei Miyazawa, Seiichi Kobayashi, Kokichi Harada, Takayuki Hida, Hisashi Shibata, Nobuyuki Yasuda, Osamu Asano, Yoshihiko Kotake
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Abstract
The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
Claims31
A defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism or a salt thereof.
A defecation-promoting agent comprising a compound having an adenosine A2b receptor antagonism or a salt thereof.
Use of a compound having an adenosine A2 receptor antagonism or a salt thereof for producing a defecation-promoting agent.
Use of a compound having an adenosine A2b receptor antagonism or a salt thereof for producing a defecation-promoting agent.
Use of an adenosine A2b receptor antagonist for a pharmaceutical preparation for treating, preventing or improving constipation.
A compound represented by the formula:
- 40
- (wherein A represents a phenyl group, pyridyl group, thienyl group or furyl group which may be substituted with one or two groups selected from a halogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group and a C1-6 alkoxy-carbonyl group;
- B represents a pyridyl group which may be substituted with one or more groups selected from a halogen atom, hydroxyl group, a C1-6 alkyl group and amino group;
- R represents a hydrogen atom, a morpholinyl group or a group represented by the formula —NR1aR1b (wherein R1a and R1b are the same as or different from each other and each represents a hydrogen atom, a C1-6 alkyl group, a C1-6 acyl group, a phenyl group or a C1-6 alkylsulfonyl group);
- and R2 represents a hydrogen atom or a group represented by the formula —NR2aR2b (wherein R2a and R2b are the same as or different from each other and each represents a hydrogen atom or a C1-6 alkyl group),
- provided that, in the above definition, the cases (i) where, A is a 4-fluorophenyl group;
- B is a 4-pyridyl group;
- R1 is an amino group;
- and R2 is a hydrogen atom, and (ii) where, A is a 4-fluorophenyl group;
- B is a 4-pyridyl group, R1 is an acetamide group;
- and R2 is a hydrogen atom are excluded) or a salt thereof.
A compound represented by the formula:
- 41
- (wherein A, R1 and R2 have the same meanings as defined in claim 16;
- and B′ represents a 1,2-dihydro-2-pyridinone-4-yl group which may be substituted with one or more groups selected from a halogen atom, hydroxyl group, a C1-6 alkyl group and amino group) or a salt thereof.
A method for promotion of defecation, by administering a pharmacologically effective amount of a compound having an adenosine A2 receptor antagonism or a salt thereof to a patient.
A method for promotion of defecation, by administering a pharmacologically effective amount of a compound having an adenosine A2b receptor antagonism or a salt thereof to a patient.
A method for treating, preventing or improving constipation, by administering a pharmacologically effective amount of a compound having an adenosine A2b receptor antagonism or a salt thereof to a patient.
Dependencies are inferred from the claim text.