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EP0196674A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Hydroxamates as modulators of arachidonic acid metabolic pathways

Assignee: USV Pharmaceutical Corp
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Filing: 1986-04-03
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Granted: —
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Expires: 2006-04-03
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Abstract

Abstract This invention relates to new chemical compounds possessing valuable pharmaceutical activity, particularly as lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: and salts thereof; wherein R 2 is H, lower alkyl, formyl or C 2 -C 10 alkanoyl; R and R, are each independently hydrogen, lower cycloalkyl, fused cycloalkyl or lower alkyl-substituted fused cycloalkyl, lower alkyl, phenyl, naphthyl or a nitrogen, oxygen, or sulfur heterocyclic ring or heterocyclic-lower alkyl; Z, Z, and Z 7 are each a chemical bond, or an alkylene chain or a mono- or di-substituted alkylene chain containing up to 6 carbon atoms in the principal chain and up to a total of about 10 carbon atoms, a lower cycloalkyl, a nitrogen oxygen, or sulfur heterocyclic ring or heterocyclic-lower alkyl, or a mono- or di-subsituted lower cycloalkyl or heterocyclic lower alkyl, and the substituents are hydrogen, lower alkyl, aryl, lower aralkyl, lower alkoxy, hydroxy, lower aralkoxy, aryloxy, carboxy, lower carbalkoxy, carbaryloxy, lower carbaralkoxy, amino, lower alkyl amino, amino loweralkyl, di-loweralkylamino or cyano; X and Y are each independently 0, S, CR 3 R 4 or a chemical bond; R 3 and R 4 are each independently H or lower alkyl; each R 5 is hydrogen, aryl, lower alkarayl, formyl, nitro, cyano, amino, lower aminoalkyl, lower alkylamino, lower aralkylamino, halo, trihalo alkyl, carbamoyl or aroyl; n is an integer from 0-2; and n, is an integer from 1-2.

Inventors

  • 👤 Fu-Chih Huang

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-04 10:54
CPC Classifications
C; C07; C07D; C07D215/00; C07D215/02; C07D215/12; C07D215/14

Claims Analysis

Total Claims: 21
Claim 1
Independent Claim 228 words
A compound of the formula: and salts thereof; wherein R 2 is H, lower alkyl, formyl or C 2 -C 10 alkanoyl; R and R 1 are each independently hydrogen, lower cycloalkyl, fused cycloalkyl or lower alkyl-substituted fused cycloalkyl, lower alkyl, phenyl, naphthyl or a nitrogen, oxygen, or sulfur heterocyclic ring or heterocyclic-lower alkyl; Z, Z 1 and Z 2 are each a chemical bond, or an alkylene chain or a mono- or di-substituted alkylene chain containing up to 6 carbon atoms in the principal chain and up to a total of about 10 carbon atoms, a lower cycloalkyl, a nitrogen, oxygen, or sulfur heterocyclic ring or heterocyclic-lower alkyl, or a mono- or di-substituted lower cycloalkyl or heterocyclic lower alkyl, and the substituents are hydrogen, lower alkyl, aryl, lower aralkyl, lower alkoxy, hydroxy, lower aralkoxy, aryloxy, carboxy, lower carbalkoxy, carbaryloxy, lower carbaralkoxy, amino, lower alkyl amino, amino loweralkyl, di-loweralkylamino or cyano; X and Y are each independently O, S, CR 3 R 4 or a chemical bond; R 3 and R 4 are each independently H or lower alkyl; Ar is phenyl or naphthyl or a nitrogen, oxygen, or sulfur heterocyclic; each R 5 is hydrogen, aryl, lower alkanoyl, formyl, nitro, cyano, amino, lower aminoalkyl, lower alkylamino, lower aralkylamino, halo, trihaloalkyl carbamoyl or aroyl; n is an integer from 0-2; and n 1 is an integer from 1-2.
Claim 2
Dependent Claim 228 words
A compound of the formula: and salts thereof; wherein R 2 is H, lower alkyl, formyl or C 2 -C 10 alkanoyl; R and R 1 are each independently hydrogen, lower cycloalkyl, fused cycloalkyl or lower alkyl-substituted fused cycloalkyl, lower alkyl, phenyl, naphthyl or a nitrogen, oxygen, or sulfur heterocyclic ring or heterocyclic-lower alkyl; Z, Z 1 and Z 2 are each a chemical bond, or an alkylene chain or a mono- or di-substituted alkylene chain containing up to 6 carbon atoms in the principal chain and up to a total of about 10 carbon atoms, a lower cycloalkyl, a nitrogen, oxygen, or sulfur heterocyclic ring or heterocyclic-lower alkyl, or a mono- or di-substituted lower cycloalkyl or heterocyclic lower alkyl, and the substituents are hydrogen, lower alkyl, aryl, lower aralkyl, lower alkoxy, hydroxy, lower aralkoxy, aryloxy, carboxy, lower carbalkoxy, carbaryloxy, lower carbaralkoxy, amino, lower alkyl amino, amino loweralkyl, di-loweralkylamino or cyano; X and Y are each independently O, S, CR 3 R 4 or a chemical bond; R 3 and R 4 are each independently H or lower alkyl; Ar is phenyl or naphthyl or a nitrogen, oxygen, or sulfur heterocyclic; each R 5 is hydrogen, aryl, lower alkanoyl, formyl, nitro, cyano, amino, lower aminoalkyl, lower alkylamino, lower aralkylamino, halo, trihaloalkyl carbamoyl or aroyl; n is an integer from 0-2; and n 1 is an integer from 1-2.
Claim 3
Dependent Claim 13 words
The compound according to Claim 1 wherein Ar is phenyl, naphthyl or pyridyl.
Claim 4
Dependent Claim 11 words
The compound according to Claim 1 wherein n l is 1.
Claim 5
Dependent Claim 19 words
The compound according to Claims 1-3 wherein R and R 1 are independently hydrogen, loweralkyl, phenyl, naphthyl or quinolyl.
Claim 6
Dependent Claim 14 words
The compound according to Claims 1-4 wherein R 2 is hydrogen or lower alkyl.
Claim 7
Dependent Claim 14 words
A compound according to Claims 1-5 wherein R 5 is hydrogen, halo or benzoyl.
Claim 8
Dependent Claim 195 words
The compound according to Claim 1 having the formula: and salts thereof wherein Ar is phenyl or naphthyl; Y is 0 or CR 3 R 4 ; X is 0 or C R 3 R 4 ; Z and Z 1 are independently a chemical bond or an alkylene chain having up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms; Z 2 is a chemical bond or an alkylene chain or a mono-substituted alkylene chain containing up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms and the substituents are hydrogen. lower alkyl, aryl, lower aralkyl, hydroxy, lower alkoxy, lower aralkoxy, aryloxy, carboxy, lower carbalkoxy, carbaryloxy, lower carbaralkoxy, lower carbalkoxy lower alkoxy, amino, lower alkylamino, diloweralkylamino or cyano; R and R 1 are each independently hydrogen, lower alkyl, lower cycloalkyl, phenyl, naphthyl or quinolyl; R 2 , R 3 and R 4 are each hydrogen or lower alkyl; each R S is hydrogen, aryl, lower alkanoyl, formyl, nitro, cyano, amino, lower aminoalkyl, lower alkylamino, lower aralkylamino, halo, trihaloalkyl, carbamoyl or aroyl; and n is an integer from 0-2.
Claim 9
Dependent Claim 188 words
The compound according to Claim 1 having the formula: and salts thereof; wherein R and R 1 are each independently hydrogen, lower alkyl, phenyl, naphthyl or a nitrogen, oxygen or sulfur heterocyclic ring; Z and Z 1 are independently a chemical bond or an alkylene chain having up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms; Z 2 is a chemical bond or an alkylene chain or a mono-substituted alkylene chain containing up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms and the substituents are hydrogen, lower alkyl, aryl, lower aralkyl, hydroxy, lower alkoxy, lower aralkoxy, aryloxy, carboxy, lower carbalkoxy, carbaryloxy, lower carbaralkoxy, lower carbalkoxy lower alkoxy, amino, lower alkylamino, diloweralkylamino or cyano; X and Y are each independently 0, S, or C R 3 R 4 ; R 3 and R 4 are each independently hydrogen or lower alkyl; n is 0, 1 or 2; and each R 5 is hydrogen, aryl, lower alkanoyl, formyl, nitro, cyano, amino, lower aminoalkyl, lower alkylamino, lower dialkylamino, halo, trihaloalkyl, carbamoyl or aroyl.
Claim 10
Dependent Claim 16 words
The compound according to Claims 1-8 wherein Y is 0 or CR 3 R 4 .
Claim 11
Dependent Claim 21 words
The compound according to Claims 1-9 wherein R and R 1 are each independently H, lower alkyl, phenyl, naphthyl or quinolyl.
Claim 12
Dependent Claim 185 words
The compound according to Claim 1 having the formula: and salts thereof; wherein n is 0 or 1; R and R 1 are each independently hydrogen, lower alkyl, phenyl, naphthyl or a nitrogen, oxygen or sulfur heterocyclic ring; Z and Z l are independently a chemical bond or an alkylene chain having up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms; Z 2 is a chemical bond or an alkylene chain or a mono-substituted alkylene chain containing up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms and the substituents are hydrogen, lower alkyl, aryl, lower aralkyl, hydroxy, lower alkoxy, lower aralkoxy, aryloxy, carboxy, lower carbalkoxy, carbaryloxy, lower carbaralkoxy, lower carbalkoxy lower alkoxy, amino, lower alkylamino, diloweralkylamino or cyano; X is independently 0, S, or CR 3 R 4 ; R 3 is independently hydrogen or lower alkyl; n is 0, 1 or 2; and each R 5 is hydrogen, aryl, lower alkanoyl, formyl, nitro, cyano, amino, lower aminoalkyl, lower alkylamino, lower dialkylamino, halo, trihaloalkyl, carbamoyl or aroyl.
Claim 13
Dependent Claim 16 words
The compound according to Claims 1-11 wherein X is 0 or CR 3 R 4 .
Claim 14
Dependent Claim 12 words
The compound according to Claims 1-12 wherein n is 0 or 1.
Claim 15
Dependent Claim 162 words
The compound according to Claim 1 having the formula: and salts thereof; wherein R and R 1 are each independently hydrogen, lower alkyl, phenyl, naphthyl or a nitrogen, oxygen or sulfur heterocyclic ring; Z and Z 1 are independently a chemical bond or an alkylene chain having up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms; Z 2 is a chemical bond or an alkylene chain or a mono-substituted alkylene chain containing up to 6 carbon atoms in the principal chain and up to a total of 10 carbon atoms and the substituents are hydrogen, lower alkyl, aryl, lower aralkyl, hydroxy, lower alkoxy, lower aralkoxy, aryloxy, carboxy, lower carbalkoxy, carbaryloxy, lower carbaralkoxy, lower carbalkoxy lower alkoxy, amino, lower alkylamino, diloweralkylamino or cyano; R 3 is independently hydrogen or lower alkyl; and each R5 is hydrogen, aryl, lower alkanoyl, formyl, nitro, cyano, amino, lower aminoalkyl, lower alkylamino, lower dialkylamino, halo, trihaloalkyl, carbamoyl or aroyl.
Claim 16
Dependent Claim 30 words
The compound according to Claims 1-14 wherein Z and Z 1 are each a chemical bond or an alkylene chain containing up to 3 carbon atoms in the normal chain.
Claim 17
Dependent Claim 23 words
The compound according to Claims 1-15 wherein Z 2 is an alkylene chain containing up to 5 carbon atoms in the normal chain.
Claim 18
Dependent Claim 35 words
The compound according to Claims 1-16 wherein R and R l are mono- or di-substituted with halo, hydroxy, lower alkyl, lower alkoxy, amino, cyano, lower alkyl, amino, lower aralkyl, aryloxy, lower aralkoxy, nitro or trihalomethyl.
Claim 19
Dependent Claim 76 words
The compound according to Claim 1 which is α-(4-benzyloxyphenyl)-N-benzyl- acetohydroxamate; α-methyl- α-(4-(2-methylpropyl)phenyl)-N-benzyl acetohydroxamate; α-methyl-α-(2-(6-methoxynaphthyl)-N-benzyl acetohydroxamate; α-(4-benzyloxyphenyl)-N-phenethyl acetohydroxamate; α-(4- (2-methylpropyl) phenyl- α-methyl-N- (2-phenethyl) - acetohydroxamate; α-(4-benzyloxyphenyl)-N-(3-phenylpropyl)acetohydroxamate; α-(4-benzyloxyphenyl)-N-methyl acetohydroxamate; α-(4-hydroxyphenyl)-N-(α-methylbenzyl)acetohydroxamate; α-(4-(2-methylpropyl)phenyl)-α-methyl-N-(α-methylbenzyl)acetohydroxamate; α-phenethyl-N-phenethyl acetohydroxamate; α-(4-benzyloxyphenyl)-N-(α-methylbenzyl)acetohydroxamate; α-(4-benzyloxyphenyl)-N-(1-benzylpropyl)acetohydroxamate; α-(3-(2-quinolinylmethoxy)phenyl)-N-(2-phenethyl)-acetohydroxamate; α-(5-benzyloxy-2-pyridyl)-N-benzyl-acetohydroxamate; α-(4-phenoxyphenyl)-N-pentyl-acetohydroxamate; α-(4-benzyloxyphenyl)-N-(5-pentanoic acid)-acetohydroxamate; α-(4-benzyloxybenzyl)-N-(2-phenethyl)acetohydroxamate; α-(4-benzyloxy-3-chlorophenyl)-N-(2-phenethyl)-acetohydroxamate; α-(4-benzyloxy-3-chlorophenyl)-N-(1-carbethoxy-2-phenethyl)acetohydroxamate; α-(3-benzyloxyphenyl)-N-(1-methyl-2-phenethyl)-acetohydroxamate; α-(2-pyridyl)-N-phenethyl acetohydroxamate; c(-(4-benzyloxyphenyl)-N-(2-pyridylmethyl)acetohydroxamate; α-(4-benzyloxyphenyl)-N-phenethyl-0-acetyl acetohydroxamate; N-hydroxy-N-phenethyl-4-benzyloxy-benzamide; N-Hydroxy-N-methyl-3-((quinolin-2-yl)methoxy)phenyl acetamide; N-Hydroxy-N-methyl-5-phenylvaleramide; N-Hydroxy-N-methyl-4-((quinolin-2-yl)methoxy)phenyl acetamide; N-Hydroxy-N-methyl-4-(4-methoxyphenyl)butyramide; N-Hydroxy-N-(2-phenethyl)-2-(3-benzyloxyphenyl) propionamide; N-(3-carboxypropyl)-N-hydroxy-4-phenylbutyramide; N-(2-phenethyl)-N-hydroxy-5-phenylvaleramide; N-Hydroxy-N-(2-methyl-2-(4-methoxyphenyl)ethyl-4-hydroxy-phenylacetamide; N-Hydroxy-N-(2-phenethyl)-2-(3-benzoylphenyl) propionamide; N-Hydroxy-N-(4-chlorophenethyl)-4-benzyloxyphenyl- acetamide; N-(3-carboxypropyl)-N-hydroxy-4-phenylbutyramide; N-Benzyl-N-hydroxy-4-phenylbutyramide; N-Hydroxy-N-[2-methyl-2-(4-benzyloxyphenyl)ethyl]-4-benzyloxyphenylacetamide; N-Hydroxy-N-(1-benzylpropyl)-4-phenylbutyramide; N -Hydroxy-N-(3-phenylpropyl)-3-phepylpropionamide; N-Hydroxy-N-(2-phenethyl)-3-phenoxypropionamide; N-Hydroxy-N-(2-phenethyl)-4-(4-methoxyphenyl)-butyramide; N-Hydroxy-N-propyl-2-(4-benzyloxyphenyl)acetamide; N-Hydroxy-N-methyl-2-(3-chloro-4-benzyloxy)phenyl)-acetamide; N-Hydroxy-N-(2-phenethyl)-4-methoxyphenylacetamide; or N-(t-Butyl)-N-hydroxy-4-benzylphenylacetamide.
Claim 20
Dependent Claim 17 words
A therapeutic composition comprising a compound according to any of Claims 1-18 and a pharmaceutical carrier therefor.
Claim 21
Independent Claim 28 words
A method of treating hypersensitive disease, inflammatory conditions or allergic responses comprising the administration of a therapeutically effective amount of a compound according to any of Claims 1-18.

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