Troponyl-oxamic acid derivatives

Claim 2

A compound of formula I ##STR4## in which R 1 and R 4 are the same or different selected from the group consisting of hydrogen, halo, trifluoromethyl, lower alkoxy, lower alkyl, phenyl, hydroxy, phenoxy, mercapto, (2-carboxyphenyl)thio, NR 7 R 8 wherein R 7 and R 8 each is hydrogen or lower alkyl or R 7 is lower alkyl and R 8 is p-toluenesulfonyl, and a radical of formula NR 9 COCOOR 10 wherein R 9 and R 10 each is hydrogen or lower alkyl; and R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, halo, trifluoromethyl, lower alkoxy, lower alkyl, phenyl, hydroxy, phenoxy, mercapto, (2-carboxyphenyl)thio and NR 7 R 8 wherein R 7 and R 8 each is hydrogen or lower alkyl or R 7 is lower alkyl and R 8 is p-toluenesulfonyl; with the proviso that at least one of R 1 and R 4 must be a radical of formula NR 9 COCOOR 10 wherein R 9 and R 10 are as defined herein; or a therapeutically acceptable salt thereof.

Claim 3

A compound of formula 1 ##STR5## in which a. R 1 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 4 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy; b. R 4 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 1 , R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy; or c. R 1 and R 4 are a radical of formula NR 9 COCOOR 10 wherein R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy; or a therapeutically acceptable salt thereof.

Claim 4

A compound of formula 1 ##STR5## in which a. R 1 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 4 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy; b. R 4 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 1 , R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy; or c. R 1 and R 4 are a radical of formula NR 9 COCOOR 10 wherein R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy; or a therapeutically acceptable salt thereof.

Claim 5

A compound of formula 1 ##STR6## in which a. R 1 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 4 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least three of R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen; b. R 4 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 1 , R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least three of R 1 , R 2 , R 3 , R 5 and R 6 are hydrogen; or c. R 1 and R 4 are a radical of formula NR 9 COCOOR 10 wherein R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least two of R 2 , R 3 , R 5 and R 6 are hydrogen, or a therapeutically acceptable salt thereof.

Claim 6

A compound of formula 1 ##STR6## in which a. R 1 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 4 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least three of R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen; b. R 4 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 1 , R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least three of R 1 , R 2 , R 3 , R 5 and R 6 are hydrogen; or c. R 1 and R 4 are a radical of formula NR 9 COCOOR 10 wherein R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 5 and R 6 are the same or different selected from the group consisting of hydrogen, lower alkoxy and hydroxy, with the proviso that at least two of R 2 , R 3 , R 5 and R 6 are hydrogen, or a therapeutically acceptable salt thereof.

Claim 7

A compound of formula 1 ##STR7## in which a. R 1 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen; or b. R 1 and R 4 are a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 5 and R 6 are hydrogen, or a therapeutically acceptable salt thereof.

Claim 8

A compound of formula 1 ##STR7## in which a. R 1 is a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen; or b. R 1 and R 4 are a radical of formula NR 9 COCOOR 10 in which R 9 and R 10 each is hydrogen or lower alkyl, and R 2 , R 3 , R 5 and R 6 are hydrogen, or a therapeutically acceptable salt thereof.

Claim 9

[(2-Oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 10

[(2-Oxo-3,5,7-cycloheptatrien-1-yl)-N-methylamino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 11

[(3-Bromo-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 12

[(5-Chloro-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 13

[(3-Phenoxy-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 14

[(7-Phenoxy-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 15

[(5-Hydroxy-4-oxo-2,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 16

[(3-Hydroxy-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 17

2,2'[(2-Oxo-3,5,7-cycloheptatrien-1,5-diyl)diimino]bis[2-oxo-acetic acid] diethyl ester, as claimed in claim 1.

Claim 18

[(5-Methoxy-4-oxo-2,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid Methyl Ester, as claimed in claim 1.

Claim 19

[(2-Oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid pentyl ester, as claimed in claim 1.

Claim 20

[(2-Oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid 1-methylethyl ester, as claimed in claim 1.

Claim 21

[(2-Oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid, 1,1-dimethylethyl ester, as claimed in claim 1.

Claim 22

[(2-Oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid, as claimed in claim 1.

Claim 23

[[3-[N-[(4-Methylphenyl)sulfonyl]-N-methylamino]-2-oxo-3,5,7-cycloheptatrien-1-yl]amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 24

[(3-Methylamino-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 25

[(3-Methoxy-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 26

[(6-Methoxy-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 27

[(4-Methoxy-2-oxo-3,5,7-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 28

[[7-oxo-4-[(2-carboxyphenyl)thio]-1,3,5-cycloheptatrien-1-yl)amino]oxo-acetic acid ethyl ester, as claimed in claim 1.

Claim 29

A method for suppressing allergic manifestations of anaphylactic reactions and atopic hypersensitivity in a mammal which comprises administering to said mammal an effective amount of a compound of claim 1, or a therapeutically acceptable salt thereof.

Claim 30

A pharmaceutical composition useful in suppressing allergic manifestations of anaphylactic reactions and atopic hypersensitivity comprising a compound of claim 1, or a therapeutically acceptable salt thereof, and a pharmaceutically acceptable carrier.