Compound for adjusting functional activity of vascular endothelial cell, its preparation method as well as usage

Compound for adjusting functional activity of vascular endothelial cell, its preparation method as well as usage

  • CN 1,415,619 A
  • Filed: 11/01/2001
  • Published: 05/07/2003
  • Est. Priority Date: 11/01/2001
  • Status: Active Application
First Claim
Patent Images

1. general formula I aShown compound, its derivative, its isomer, raceme or optical isomer, medicinal acid addition salt, pharmaceutical salts or its solvate, Wherein:

  • R 1'"'"', R 2'"'"', R 3'"'"' represent hydrogen atom, C respectively 1-20Saturated or undersaturated straight or branched aliphatic hydrocarbon, C 3-20Cycloalkyl group, replace C 3-20Cycloalkyl group, C 4-20Aryl radical, replace C 5-20Aryl radical, C 3-20Heterocycle alkyl, replacement C 3-20Heterocycle alkyl, beta-hydroxy C 2-20Alkyl, β

    -C 1-10Alkane carbonyl oxygen C 2-10Alkyl, β

    -C 5-14Virtue carbonyl oxygen base C 2-10Alkyl, beta substitution C 5-14Virtue carbonyl oxygen base C 2-10Alkyl, β

    -C 1-10Alkoxy C 2-10Alkyl, β

    -C 4-10Aryloxy C 2-10Alkyl, beta substitution C 4-10Aryloxy C 2-10Alkyl, β

    -sulfydryl C 2-20Alkyl, β

    -C 1-10Alkylthio C 2-10Alkyl, β

    -C 4-10Arylthio C 2-10Alkyl, beta substitution C 4-10Arylthio C 2-10Alkyl, beta-amino C 2-20Alkyl, β

    -C 1-10Alkylamino radical C 2-10Alkyl, β

    -C 4-14Aryl amine C 2-10Alkyl, beta substitution C 4-14Aryl amine C 2-10Alkyl, β

    -C 1-10Alkyl amide C 2-10Alkyl, β

    -C 5-14Aromatic amide C 2-10Alkyl, beta substitution C 5-14Aromatic amide C 1-10Alkyl, γ

    -hydroxyl C 2-20Alkyl, γ

    -C 1-10Alkane carbonyl oxygen C 2-10Alkyl, γ

    -C 5-14Virtue carbonyl oxygen base C 2-10Alkyl, γ

    -replacement C 5-14Virtue carbonyl oxygen base C 2-10Alkyl, γ

    -C 1-10Aryloxy C 2-10Alkyl, γ

    -replacement C 5-10Aryloxy C 2-10Alkyl, γ

    -sulfydryl C 2-20Alkyl, γ

    -C 1-10Alkylthio C 2-10Alkyl, γ

    -C 4-10Arylthio C 2-10Alkyl, γ

    -replacement C 5-10Arylthio C 2-10Alkyl, gamma-amino C 2-20Alkyl, γ

    -C 1-10Alkylamino radical C 2-10Alkyl, γ

    -C 4-14Aryl amine C 2-10Alkyl, γ

    -replacement C 4-14Aryl amine C 2-10Alkyl, γ

    -C 1-10Alkyl amide C 2-10Alkyl, γ

    -C 5-14Aromatic amide C 2-10Alkyl, γ

    -replacement C 5-14Aromatic amide C 2-10Alkyl;

    Or R 1'"'"' and R 2'"'"' or R 3'"'"' generate 3-9 unit ring texture, particularly morpholine ring, piperazine ring, piperidine ring, pyrroline ring, tetrahydroglyoxaline ring, pyrazoline ring, thiazoline ring, high morpholine ring, high piperazine ring, high piperidine ring, the piperazine ring of replacement, the N-(C of replacement 4-6Aryl) the tetrahydroglyoxaline ring of the pyrroline ring of the piperidine ring of piperazine ring, replacement, replacement, replacement, the N-(C of replacement 4-6Aryl) the pyrazoline ring of tetrahydroglyoxaline ring, replacement, the N-(C of replacement 4-6Aryl) the high piperazine ring of the high morpholine ring of the thiazoline ring of pyrazoline ring, replacement, replacement, replacement, the N-(C of replacement 4-5Aryl) the high piperidine ring of high piperazine ring, replacement, wherein, each substituting group that has substituent group is selected from;

    halogen, hydroxyl, cyano group, nitro, C 1-10Alkyl, C 4-6Aryl, C 1-6Alkoxyl group, C 1-6Alkylthio, one, two or three halo C 1-6Alkyl, amino, C 1-10Hydroxylamine base, C 1-10Alkylacyloxy, C 6-10Aryl acyloxy or C 1-10The hydrocarbon amide group;

    Y represents cyano group, carboxyl, phosphonate group, C 1-10Alkoxy carbonyl, C 3-10The C of heterocyclic oxy group carbonyl, replacement 3-10Heterocyclic oxy group carbonyl, C 4-10The C of aryloxycarbonyl, replacement 4-10Aryloxycarbonyl, carbamyl, C 1-10Alkylamino radical carbonyl, C 3-10The C of heterocycle amido carbonyl, replacement 3-10Heterocycle amido carbonyl, C 4-10Aryl amine carbonyl, replacement C 4-10Aryl amine carbonyl, single C 1-10Alkoxyl group phosphono, single C 3-10Heterocyclic oxy group phosphono, the list (C of replacement 3-10Heterocyclic oxy group) phosphono, single C 4-10Aryloxy phosphono, the list (C of replacement 4-10Aryloxy) phosphono, two (C 1-10Alkoxyl group) phosphono, two (C 3-10Heterocyclic oxy group) phosphono, the two (C of replacement 3-10Heterocyclic oxy group) phosphono, two (C 4-10Aryloxy) phosphono, the two (C of replacement 4-10Aryloxy) phosphono, single C 1-10Alkylamino radical phosphono, single C 4-10Heterocycle amido phosphono, the list (C of replacement 4-10The heterocycle amido) phosphono, single C 4-10Aryl amine phosphono, the list (C of replacement 5-10Aryl amine) phosphono, two (C 1-10Alkylamino radical) phosphono, two (C 4-10The heterocycle amido) phosphono, the two (C of replacement 4-10The heterocycle amido) phosphono, two (C 4-10Aryl amine) phosphono, the two (C of replacement 5-10Aryl amine) phosphono, (C 1-10Alkylamino radical) (C 1-10Alkoxyl group) phosphono, (C 4-10The heterocycle amido) (C 1-10Alkoxyl group) the phosphono, (C of replacement 4-10The heterocycle amido) (C 1-10Alkoxyl group) phosphono, (C 4-10Aryl amine) (C 1-10Alkoxyl group) the phosphono, (C of replacement 5-10Aryl amine) (C 1-10Alkoxyl group) phosphono, (C 1-10Alkylamino radical) (C 3-10Heterocyclic oxy group) phosphono, (C 4-10The heterocycle amido) (C 3-10Heterocyclic oxy group) the phosphono, (C of replacement 4-10The heterocycle amido) (C 3-10Heterocyclic oxy group) phosphono, (C 4-10Aryl amine) (C 3-10Heterocyclic oxy group) the phosphono, (C of replacement 5-10Aryl amine) (C 3-10Heterocyclic oxy group) phosphono, (C 1-10Alkylamino radical) (the C of replacement 3-10Heterocyclic oxy group) phosphono, (C 4-10The heterocycle amido) (the C of replacement 3-10Heterocyclic oxy group) the phosphono, (C of replacement 4-10The heterocycle amido) (the C of replacement 3-10Heterocyclic oxy group) phosphono, (C 4-10Aryl amine) (the C of replacement 3-10Heterocyclic oxy group) the phosphono, (C of replacement 5-10Aryl amine) (the C of replacement 3-10Heterocyclic oxy group) phosphono, (C 1-10Alkylamino radical) (C 4-10Aryloxy) phosphono, (C 4-10The heterocycle amido) (C 4-10Aryloxy) the phosphono, (C of replacement 4-10The heterocycle amido) (C 4-10Aryloxy) phosphono, (C 4-10Aryl amine) (C 4-10Aryloxy) the phosphono, (C of replacement 5-10Aryl amine) (C 4-10Aryloxy) phosphono, (C 1-10Alkylamino radical) (the C of replacement 4-10Aryloxy) phosphono, (C 4-10The heterocycle amido) (the C of replacement 4-10Aryloxy) the phosphono, (C of replacement 4-10The heterocycle amido) (the C of replacement 4-10Aryloxy) phosphono, (C 4-10Aryl amine) (the C of replacement 4-10Aryloxy) the phosphono, (C of replacement 5-10Aryl amine) (the C of replacement 4-10Aryloxy) phosphono, imidazolyl, pyrazolyl, triazol radical, tetrazole Ji, oxazolyl, thiazolyl, imidazolinyl, pyrazolinyl, oxazolinyl, thiazolinyl;

    substituted radical in wherein said " dibasic phosphono " can be identical;

    also can be different;

    heterocycle refers to contain 1-3 and is selected from N, O or heteroatomic list of S or annelated heterocycles;

    each substituting group that has substituent group is selected from;

    halogen, hydroxyl, cyano group;

    nitro, C 1-6Alkyl, C 4-6Aryl, C 1-6Alkoxyl group, C 1-6Alkylthio, one, two or three halo C 1-6Alkyl, amino, C 1-10The hydroxylamine base, C 1-10Alkylacyloxy, C 6-10Aryl acyloxy or C 1-10The hydrocarbon amide group.

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