Nitrogen-containing heterocyclic compounds, their production and use
View Patent ↗A compound of the formula: wherein one of A and D is N and the other is C, or both are N; B is N or C; m is 0-3; R 1 , R 2 and R 3 each is (i) H or (ii) a group bound via C, N, O or S; R 4 is a group bound via C; R 5 is H or a group bound via C or O; R 6 is H or a group bound via C; R 7 is a homo- or hetero-cyclic group which may be substituted; or a salt thereof possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful as a prophylactic or therapeutic agent for sex hormone-dependent diseases, and so forth.
1. A compound of formula
wherein m is an integer from 0 to 3;
R 1 , R 2 and R 3 each is (i) hydrogen or (ii) a group bound via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom;
wherein R 4 is a group of the formula: —(CH 2 ) n —NR 10 R 11 wherein n is an integer from 1 to 3; R 10 is hydrogen, a C 1-10 hydrocarbon group which may be substituted, a C 1-20 acyl group which may be substituted, a hydroxy group which may be substituted, a heterocyclic group which may be substituted, or a group of the formula: —S(O) t —R 12 wherein t is an integer from 0 to 2, and R 12 is hydrogen or a C 1-10 hydrocarbon group which may be substituted; and R 11 is hydrogen or a C 1-10 hydrocarbon group; or R 10 and R 11 form, taken together with the adjacent nitrogen atom, a cyclic amino group which may be substituted
R 5 re represents (i) hydrogen, (ii) halogen or (iii) a group via a carbon atom or an oxygen atom;
R 6 represents hydrogen or a group bound via a carbon atom;
R 7 represents a homocyclic group which may be substituted or a heterocyclic group which may be substituted; and each dotted line represents a single bond or a double bond; or a salt thereof.
2. A compound of claim 1 or a salt thereof, wherein R 4 is a N—C 1-6 alkyl-N-benzylaminomethyl group.
3. A pharmaceutical composition which comprises a compound of claim 1 or a salt thereof in a pharmaceutically acceptable carrier.
4. A method for treating prostatic cancer, uterine cancer, breast cancer, hysteromyoma, endometriosis, precocious puberty, premenstrual syndrome, multilocular ovary syndrome or wherein the method comprises administering to a mammal an effective amount of the compound of claim 1 or a salt thereof.
5. A method for treating prostatic cancer, uterine cancer or breast cancer, wherein the method comprises administering to a mammal an effective amount of the compound of claim 1 or a salt thereof.
6. A method for treating endometriosis, hysteromyoma or precocious puberty, wherein the method comprises administering to a mammal an effective amount of the compound of claim 1 or a salt thereof.
7. A method for regulating pregnancy, wherein the method comprises administering to a mammal an effective amount of the compound of claim 1 or a salt thereof.
8. A method for regulating menstruation cycle, wherein the method comprises administering to a mammal an effective amount of the compound of claim 1 or a salt thereof.