R 1 and R 2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl, R 3 is aryl or ar(lower)alkyl, both of which may have one or more suitable substituent(s), or heterocyclic(lower)alkyl, R 4 is carboxy or protected carboxy, A is oxygen or sulfur atom, Y is carbonyl, thiocarbonyl or sulfonyl and Z is lower alkylene,
and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them in admixture with pharmaceutically acceptable carriers.
摘要:
New compound of the formula: wherein A' is a group of the formula: in which R 3 is hydrogen or alkyl, R 4 is hydrogen, halogen, alkyl, alkoxy, acyloxymethyl, or substituted or unsubstituted heterocyclic-thiomethyl, R 5 is carboxy or protected carboxy, and X is -S- or -0-, provided that when A' is a group of the formula: R 5 then R 4 is hydrogen, halogen, alkoxy or carbamoyloxy- methyl protected by an amino-protecting group, and R 3 and R 5 are each as defined above, or a salt thereof or a hydrate thereof and processes for their preparation.
摘要:
The present invention relates to novel indole derivatives and a pharmaceutically acceptable salt thereof which have pharmacological activities such as inhibitory activity on testosteron 5a-reductase and the like, to process for preparation thereof, to a pharmaceutical composition comprising the same and to a use of the same for manufacturing a medicament.
摘要:
New compound of the formula: wherein A' is a group of the formula: in which R 3 is hydrogen or alkyl,
R 4 is hydrogen, halogen, alkyl, alkoxy, acyloxymethyl, or substituted or unsubstituted heterocyclic-thiomethyl, R 5 is carboxy or protected carboxy, and X is -S- or -0-,
provided that when A' is a group of the formula: R 5 then R 4 is hydrogen, halogen, alkoxy or carbamoyloxy- methyl protected by an amino-protecting group, and R 3 and R 5 are each as defined above, or a salt thereof or a hydrate thereof and processes for their preparation.
wherein R 1 is carboxy or protected carboxy, R 2 is hydrogen, lower alkyl or halogen, R 3 is aryl or ar(lower)alkyl, each of which may have suitable substituent(s), [substituted carbamoyl]-(lower)alkyl, or a group of the formula :
is heterocyclic group containing nitrogen atom, and n is 0 or 1, R 11 is hydrogen or lower alkyl, A is lower alkylene which may be substituted by oxo, or lower alkenylene, Q is carbonyl or lower alkylene, X is
in which R 4 is hydrogen or lower alkyl, and R 5 is hydrogen, lower alkyl or Y-Z-R 3 , Y is bond or lower alkylene, Z is lower alkylene, lower alkenylene, -0-or
in which R 6 is hydrogen, lower alkyl, ar(lower)alkyl which may have suitable substituent(s) or amino protective group, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them.
R 1 is carboxy or protected carboxy, R 2 is hydrogen, lower alkyl or halogen, R 3 is aryl or ar(lower)alkyl, each of which may have suitable substituent(s), [substituted carbamoyl]-(lower)alkyl, or a group of the formula :
is heterocyclic group containing nitrogen atom, and n is 0 or 1, R 11 is hydrogen or lower alkyl, A is lower alkylene which may be substituted by oxo, or lower alkenylene, Q is carbonyl or lower alkylene, X is
in which R 4 is hydrogen or lower alkyl, and R 5 is hydrogen, lower alkyl or Y-Z-R 3 , Y is bond or lower alkylene, Z is lower alkylene, lower alkenylene, -0-or
in which R 6 is hydrogen, lower alkyl, ar(lower)alkyl which may have suitable substituent(s) or amino protective group, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them.
摘要:
compound of the formula: in which R 1 and R 2 are each hydrogen, halogen, lower alkoxy or halo(lower)alkyl, R 3 is aryl or ar(lower)alkyl, both of which may have one or more suitable substituent(s), or heterocyclic(lower)alkyl, R 4 is carboxy or protected carboxy, A is oxygen or sulfur atom, Y is carbonyl, thiocarbonyl or sulfonyl and Z is lower alkylene, and pharmaceutically acceptable salts thereof, processes for their preparation and pharmaceutical compositions comprising them in admixture with pharmaceutically acceptable carriers.
摘要:
The present invention provides compounds of the general formula: wherein R 1 is a hydroxyl or protected hydroxyl group or a carboxyl group or a lower alkoxycarbonyl or benzyloxy radical, R 2 is a hydrogen or halogen atom or a halo(lower)alkyl radical, R 3 is a hydrogen atom, a hydroxyl group or a lower alkoxy radical and A is a lower alkylene radical; and the pharmaceutically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them and is also concerned with the use thereof.