Heterocyclic-substituted alkanamides useful as renin inhibitors

Heterocyclic-substituted alkanamides useful as renin inhibitors

  • CN 101,171,230 A
  • Filed: 03/10/2006
  • Published: 04/30/2008
  • Est. Priority Date: 03/11/2005
  • Status: Active Application
First Claim
Patent Images

1. following formula:

  • compound(1) WhereinR 1Be a) optional by the saturated heterocyclic of following groups replacement one or many;

    C 1-8-alkyloyl, C 2-6Thiazolinyl, C 2-6Alkynyl, C 1-6Alkoxyl group, C 1-6Alkoxy-C 1-6Alkoxyl group, C 1-6Alkoxy-C 1-6Alkyl, C 1-6Alkoxycarbonyl amino, C 1-6Alkyl, C 0-6Alkyl-carbonyl-amino, C 1-6The alkyl-carbonyl oxygen base, C 1-6Alkylenedioxy group, optional N-one or N, N-two-C 1-6-alkylating amino, aryl, optional N-one or N, N-two-C 1-6-alkylating formamyl, the carboxyl of optionally esterify, cyano group, C 3-8Cycloalkyloxy, C 3-8Cycloalkyl-C 0-6Alkyl, halogen, halo-C 1-6Alkoxyl group, halo-C 1-6Alkyl, heteroaryl, undersaturated, fractional saturation or saturated heterocyclic radical, hydroxyl, nitro is by the oxide compound or the oxo base of carbon atom bonding;

    Or B) the azepan base-, azetidinyl-, aziridinyl-, two 

    alkyl-, the Dioxepane base-, dioxolanyl-, the dithiane base-, the dithiolane base-, furyl-, the oxathiane base-, the oxepane alkyl-, THP trtrahydropyranyl-, tetrahydrofuran base-, the tetrahydrochysene thiophenyl-, tetrahydro thiapyran base-, the thia suberyl-, or dicyclo saturated heterocyclyl-C 1-4Alkyl, the optional following groups that is selected from of described each group replaces one or many;

    C 1-8Alkyloyl, C 2-6Thiazolinyl, C 2-6Alkynyl, C 1-6Alkoxyl group, C 1-6Alkoxy-C 1-6Alkoxyl group, C 1-6Alkoxy-C 1-6Alkyl, C 1-6Alkoxycarbonyl amino, C 1-6Alkyl, C 0-6Alkyl-carbonyl-amino, C 1-6The alkyl-carbonyl oxygen base, C 1-6Alkylenedioxy group, optional N-one or N, N-two-C 1-6-alkylating amino, aryl, optional N--or N, N-two-C 1-6-alkylating formamyl, the carboxyl of optionally esterify, cyano group, C 3-8Cycloalkyloxy, C 3-8Cycloalkyl-C 0-6Alkyl, halogen, halo-C 1-6Alkoxyl group, halo-C 1-6Alkyl, heteroaryl, unsaturated, fractional saturation or saturated heterocyclyl, hydroxyl, nitro, oxide compound or oxo base;

    Or C) the optional C that is selected from following group replacement one or many 2-8Alkynyl;

    C 1-8Alkyloyl, C 2-6Thiazolinyl, C 2-6Alkynyl, C 1-6Alkoxyl group, C 1-6Alkoxy-C 1-6Alkoxyl group, C 1-6Alkoxy-C 1-6Alkyl, C 1-6Alkoxycarbonyl amino, C 1-6Alkyl, C 0-6Alkyl-carbonyl-amino, C 1-6The alkyl-carbonyl oxygen base, C 1-6Alkylenedioxy group, optional N-one or N, N-two-C 1-6-alkylating amino, aryl, optional N-one or N, N-two-C 1-6-alkylating formamyl, the carboxyl of optionally esterify, cyano group, C 3-8Cycloalkyloxy, C 3-8Cycloalkyl-C 0-6Alkyl, halogen, halo-C 1-6-alkoxyl group, halo-C 1-6Alkyl, heteroaryl, unsaturated, fractional saturation or saturated heterocyclyl, hydroxyl, nitro or oxo base;

    Or R 2Be to be selected from a following 1-4 group independently of one another;

    C 1-8Alkyloyl is being higher than the C that carries alkyloyl on the position of α

    1-8Alkyloyl-C 2-4Alkoxyl group, C 1-8Alkanoylamino-C 1-4Alkoxyl group, N-C 1-4Alkanoylamino-C 1-4Alkyl, C 1-8Alkyloyl oxygen base-C 1-4Alkyl, N '"'"'-C 2-8Alkyloyl Piperazino-C 1-4Alkoxyl group, N '"'"'-C 2-8Alkyloyl Piperazino-C 1-4Alkyl, C 1-8Alkane alkylsulfonyl-C 1-4Alkoxyl group, C 1-8Alkane alkylsulfonyl-C 1-4Alkyl, C 1-8Alkane sulfuryl amino-C 1-4Alkoxyl group, C 1-4Alkane sulfuryl amino-C 1-4Alkyl, C 1-8Alkane alkylsulfonyl-C 1-4(hydroxyl) alkoxyl group, C 2-8Thiazolinyl oxygen base, C 2-8Thiazolinyl oxygen base-C 1-4Alkoxyl group, C 2-8Thiazolinyl oxygen base-C 1-4Alkyl, C 1-8Alkoxyl group, C 1-6Alkoxy-C 1-6Alkyloyl, C 1-4Alkoxy-C 2-4Thiazolinyl, C 1-4Alkoxy-C 2-4Thiazolinyl oxygen base, C 1-4Alkoxy-C 1-4Alkoxyl group, C 1-4Alkoxy-C 1-4Alkoxy-C 1-4Alkyl, C 1-4Alkoxy-C 1-4Alkyl, C 1-4Alkoxy carbonyl-C 1-4Alkoxyl group, C 1-4Alkoxy carbonyl-C 1-4Alkyl, C 1-8Alkoxycarbonyl amino-C 1-4Alkoxyl group, C 1-8Alkoxycarbonyl amino-C 1-4Alkyl, C 1-8Alkyl, C 1-4Alkylamino, N, N-two-C 1-4Alkylamino, C 1-4Alkylamino-C 1-4Alkoxyl group, N, N-two-C 1-4Alkylamino-C 1-4Alkoxyl group, C 1-4Alkylamino-C 1-4Alkyl, N, N-two-C 1-4Alkylamino-C 1-4Alkyl, N-one-or N, N-two-C 1-4Alkyl-carbamoyl-C 1-4Alkoxyl group, N-one-or N, N-two-C 1-4Alkyl-carbamoyl-C 1-4Alkyl, N '"'"'-C 1-4Alkyl piperazine sub-base-C 1-4Alkoxyl group, N '"'"'-C 1-4Alkyl piperazine sub-base-C 1-4Alkyl, C 1-4Alkylthio-C 1-4Alkoxyl group, C 1-4Alkylthio-C 1-4(hydroxyl) alkoxyl group, C 1-4Alkylthio-C 1-4Alkyl, amino-C 2-4 alkoxyl groups, amino-C 1-4Alkyl, formamyl-C 1-4Alkoxyl group, formamyl-C 1-8Alkyl, carboxyl-C 1-4Alkoxyl group, carboxyl-C 1-4Alkyl, cyano group-C 1-4Alkoxyl group, cyano group-C 1-4Alkyl, C 3-8Cycloalkyloxy, C 3-8Cycloalkyloxy-C 1-4Alkoxyl group, C 3-8Cycloalkyloxy-C 1-4Alkyl, C 3-8Cycloalkyl, S, S-dioxo thiomorpholine generation-C 1-4Alkoxyl group, S.S-dioxo thiomorpholine generation-C 1-4Alkyl, halogen, halo-C 1-4Alkoxyl group, halo-C 1-4Alkyl, halo-C 2-8(hydroxyl) alkoxyl group, hydroxyl, hydroxyl-C 2-8Alkoxyl group, hydroxyl-C 2-8Alkyl, imidazolyl sulfenyl-C 1-4Alkoxyl group, imidazolyl sulfenyl-C 1-4Alkyl, the morpholino-C of optional N-oxidation 1-4Alkoxyl group, morpholino-C 1-4Alkyl, S-oxo thiomorpholine generation-C 1-4Alkoxyl group, S-oxo thiomorpholine generation-C 1-4Alkyl, Piperazino-C 1-4Alkoxyl group, Piperazino-C 1-4Alkyl, piperidino-(1-position only)-C 1-4Alkoxyl group, piperidino-(1-position only)-C 1-4Alkyl, optional part hydrogenant pyridyl-or N-pyridine oxide base-C 1-4Alkoxyl group, optional part hydrogenant pyridyl-or N-pyridine oxide base-C 1-4Alkyl, the pyridyl sulfenyl-C of optional N-oxidation 1-4Alkoxyl group, the pyridyl sulfenyl-C of optional N-oxidation 1-4Alkyl, pyrimidine-based sulfur-base-C 1-4Alkoxyl group, pyrimidine-based sulfur-base-C 1-4Alkyl, pyrrolidino-C 1-4Alkoxyl group, pyrrolidino-C 1-4Alkyl, thiazolinyl sulfenyl-C 1-4Alkoxyl group, thiazolinyl sulfenyl-C 1-4Alkyl, thiazolyl-C 1-4Alkoxyl group, thiazolyl sulfenyl-C 1-4Alkoxyl group, thiazolyl sulfenyl-C 1-4Alkyl, thiomorpholine generation-C 1-4Alkoxyl group, thiomorpholine generation-C 1-4Alkyl, three fluoro-C 1-8Alkane alkylsulfonyl-C 1-4Alkoxyl group, three fluoro-C 1-8Alkane sulfuryl amino-C 1-4Alkyl, unsubstituted or by following groups one, two or trisubstd phenyl or naphthyl;

    C 1-4Alkoxyl group, C 1-4Alkyl, C 1-4Alkylamino, two-C 1-4Alkylamino, halogen, hydroxyl and/or trifluoromethyl and unsubstituted or by following groups one, two or trisubstd phenyl-or naphthyl-C 1-4Alkoxyl group;

    C 1-4Alkoxyl group, C 1-4Alkyl, C 1-4Alkylamino, two-C 1-4Alkylamino, halogen, hydroxyl and/or trifluoromethyl, And salt, prodrug, or wherein one or more atoms are by its stable non radioactive isotope alternate compound, especially pharmacologically acceptable salt;

    R wherein 1Be to choose wantonly except N-ethanoyl piperidin-4-yl that replaces or the compound of the choosing the oxo-piperidine base that replaces wantonly.

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