N-acylpiperazine derivative, anti-ulcer drug, and antibacterial drug
AssigneeShiseido Company, Ltd.
InventorsChikao Nishino, Fumitaka Sato, Hirotada Fukunishi
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Abstract
An N-acylpiperazine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein R.sub.1 represents a pyridylcarbonyloxy lower alkyl group, a benzoylamino lower alkyl group, benzyl group, carbamoyl group, pyridyl group, or diphenylmethyl group; R.sub.2 represents a lower alkyl group or a lower alkoxy group; n represents an integer of 0 to 2; R.sub.3 represents a hydrogen atom, an alkenyl group, or benzyl group; and m represents an integer of 1 to 3. The N-acylpiperazine derivative or a salt thereof has an anti-ulcer effect, an antibacterial activity against Helicobacter pyroli, and high safety to be available for prevention or cure of various ulcers.
Claims23
An N-acylpiperazine compound or a pharmaceutically acceptable salt thereof expressed by the following formula 1:
- ##STR20## wherein R.sub.1 represents a pyridylcarbonyloxy lower alkyl group,
- an unsubstituted or a substituted benzyl group, wherein said substituted benzyl group is a piperonyl,
- an unsubstituted or a substituted carbamoyl group, wherein said substituted carbamoyl group is a lower alkyl carbamoyl group,
- a pyridyl group,
- a diphenylemthyl group, or
- a benzoylamino lower alkyl group having the formula of:
- ##STR21## wherein Y represents an unsubstituted or a substituted phenyl group, wherein said substituted phenyl group is 3,4-methylenedioxyphenyl, and q represents an integer of 1 to 4;
- R.sub.2 represents a lower alkyl or lower alkoxy group;
- n represents an integer of 0 to 2;
- R.sub.3 represents an alkenyl group, or an unsubstituted or a substituted benzyl group, wherein said substituted benzyl group has a halogen atom;
- and
- m represents an integer of 1 to 3.
An N-acylpiperazine compound or a pharmaceutically acceptable salt thereof, which is expressed by the following formula 3:
- ##STR24## wherein R.sub.1 represents an unsubstituted or a substituted carbamoyl group, wherein said substituted carbamoyl group is a lower alkyl carbamoyl group,
- an unsubstituted or a substituted benzyl group, wherein said substituted benzyl group is a piperonyl, or a pyridyl group;
- R.sub.2 represents a lower alkyl group;
- Rb represents a halogen atom;
- and
- l represents 0 or 1.
A method for treating peptic ulcers in mammals, which comprises administering to said mammals an effective amount of N-acylpiperazine compound or a pharmaceutically acceptable salt thereof having the following formula 4:
- ##STR25## wherein R.sub.1 represents an unsubstituted or a substituted benzyl group, or diphenylmethyl group, and R.sub.2 represents a lower alkyl group, wherein said substituted benzyl group is a piperonyl.
A method for inhibiting acid secretion in stomach of mammals, which comprises administering to said mammals an effective amount of N-acylpiperazine compound or a pharmaceutically acceptable salt thereof having the following formula 4:
- ##STR26## wherein R.sub.1 represents an unsubstituted or a substituted benzyl group, or diphenylmethyl group, and R.sub.2 represents a lower alkyl group, wherein said substituted benzyl group is a piperonyl.
A method for inhibiting the growth of Helicobacter pyroli in stomach of mammals, which comprises administering to said mammals an effective amount of N-acylpiperazine compound or a pharmaceutically acceptable salt thereof having the following formula 4:
- ##STR27## wherein R.sub.1 represents an unsubstituted or a substituted benzyl group, or diphenylmethyl group, and R.sub.2 represents a lower alkyl group, wherein said substituted benzyl group is a piperonyl.
A method of preventing peptic ulcers in mammals, which comprises administering to said mammals an effective amount of N-acylpiperazine compound or a pharmaceutically acceptable salt thereof having the following formula 4:
- ##STR28## wherein R.sub.1 represents an unsubstituted or a substituted benzyl group, or diphenylmethyl group, and R.sub.2 represents a lower alkyl group, wherein said substituted benzyl group is a piperonyl.
A method of preventing peptic ulcers according to 22, wherein said peptic ulcers are gastric ulcers in man.
Dependencies are inferred from the claim text.