The present invention relates to novel 2-amino-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid derivatives useful for prophylaxis and therapy of allergic diseases such as allergic asthma, allergic dermatitis and hay fever, which have the following formula: ##STR1## wherein A is ##STR2## (R, R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl and m is 0 or 1, with the proviso that when m is 1, R.sup.1 is hydrogen) or R--Co-- (R has the same meaning as defined above), or a physiologically acceptable salt thereof, and to a method for preparing the same.

Takeda Chemical Industries, Ltd.

2-amino-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid derivatives

The invention provides hydrazine derivatives of the formula ##STR1##wherein R.sup.1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R.sup.2 is an acyl group derived from an .alpha.-, .beta.-, .gamma.- or .delta.-(amino, hydroxy or thiol)carboxylic acid in which the amino, hydroxy or thiol group is optionally lower alkylated or the amino group is optionally acylated, sulphonylated or amidated and in which any functional group present in a side-chain is optionally protected, or a group of the formula Het(CH.sub.2).sub.m CO; R.sup.3 is hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl-lower alkenyl, aryl or heterocyclyl; R.sup.4 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula X-aryl, X-heteroaryl or --(CH.sub.2).sub.n --CH.dbd.CR.sup.5 R.sup.6 ; R.sup.5 and R.sup.6 together are lower alkylene in which one CH.sub.2 group is optionally replaced by a hetero atom; Het is heterocyclyl; X is a spacer group; m is 0, 1, 2, 3 or 4; and n is 1 or 2; and their pharmaceutically acceptable salts inhibit the release of tumour necrosis factor alpha (TNF-.alpha.) from cells. They can be used as medicaments, especially in the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumours, cachexia, cardiovascular diseases, fever, haemorrhage and sepsis.

carboxylic acid/חום

2-amino-5-oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acid derivatives

Compounds as inhibitor of tumor necrosis factor alpha release

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