Indole derivatives as 5-HT receptor antagonist
First Claim
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1. A compound of formula (I) or a salt thereof:
- ##STR11## wherein;
P1 is pyridyl;
P2 is phenyl;
A is a bond or a chain of 1 to 5 atoms optionally substituted by C1-6 alkyl;
R1 and R2 groups are each independently hydrogen, C1-6 alkyl optionally substituted by NR12 R13, C2-6 alkenyl, C2-6 alkynyl, cyano, halogen, CF3, NR12 R13, CHO, OCF3, COR14, CH2 OR14 or OR14 where R12, R13 and R14 are independently hydrogen or C1-6 alkyl;
n and m are independently 0, 1 or 2;
R3 is hydrogen or C1-6 alkyl;
R4 is a group of formula (i);
##STR12## in which;
R6 and R7 are independently hydrogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C1-6 alkylthio, C1-6 alkoxy or halogen, or a pharmaceutically acceptable salt thereof.
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Abstract
A compound of formula (I) or a salt thereof: ##STR1## wherein: P1 is pyridyl;
P2 is phenyl;
A is a bond or a chain of 1 to 5 atoms optionally substituted by C1-6 alkyl;
R1 and R2 groups are each independently hydrogen, C1-6 alkyl optionally substituted by NR12 R13, C2-6 alkenyl, C2-6 alkynyl, cyano, halogen, CF3, NR12 R13, CHO, OCF3, COR14, CH2 OR14 or OR14 where R12, R13 and R14 are independently hydrogen or C1-6 alkyl;
n and m are independently 0, 1 or 2;
R3 is hydrogen or C1-6 alkyl;
R4 is a group of formula (i): ##STR2## in which: R6 and R7 are independently hydrogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C1-6 alkylthio, C1-6 alkoxy or halogen.
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Citations
14 Claims
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1. A compound of formula (I) or a salt thereof:
- ##STR11## wherein;
P1 is pyridyl;P2 is phenyl; A is a bond or a chain of 1 to 5 atoms optionally substituted by C1-6 alkyl; R1 and R2 groups are each independently hydrogen, C1-6 alkyl optionally substituted by NR12 R13, C2-6 alkenyl, C2-6 alkynyl, cyano, halogen, CF3, NR12 R13, CHO, OCF3, COR14, CH2 OR14 or OR14 where R12, R13 and R14 are independently hydrogen or C1-6 alkyl; n and m are independently 0, 1 or 2; R3 is hydrogen or C1-6 alkyl; R4 is a group of formula (i);
##STR12## in which;
R6 and R7 are independently hydrogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C1-6 alkylthio, C1-6 alkoxy or halogen, or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 9, 10, 11, 12, 13, 14)
- ##STR11## wherein;
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8. A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, which process comprises:
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(a) the coupling of a compound of formula (II);
##STR13## with a compound of formula (HI);
space="preserve" listing-type="equation">D--R.sup.4 '"'"' (III)wherein A, P1 and P2 are as defined in formula (I) , C and D contain the appropriate functional group(s) necessary to form the moiety -NR3 '"'"'CO when coupled, the variables R1 '"'"', R2 '"'"', R3 '"'"' and R4 '"'"' are R1, R2, R3 and R4 respectively, as defined in formula (I), or groups convertible thereto, and thereafter optionally and as necessary and in any appropriate order, converting any R1 '"'"', R2 '"'"', R3 '"'"' and R4 '"'"', when other than R1, R2, R3 and R4 respectively to R1, R2, R3 and R4, interconverting R1, R2, R3 and R4 and forming a pharmaceutically acceptable salt thereof;
or(b) the coupling of a compound of formula (IV);
##STR14## with a compound of formula (V);
##STR15## wherein P1, P2, R1 '"'"', R2 '"'"', R3 '"'"' and R4 '"'"' are as defined above and E and G contain the appropriate functional group(s) necessary to form the A moiety when coupled and thereafter optionally and as necessary and in any appropriate order, converting any R1 '"'"', R2 '"'"', R3 '"'"' and R4 '"'"', when other than R1, R2, R3 and R4 respectively to R1, R2, R3 and R4, interconverting R1, R2, R3 and R4 and forming a pharmaceutically acceptable salt.
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Specification