KR940005581A - Angiotensin II Antagonist - Google Patents

Abstract

The present invention antagonizes angiotensin II at receptor sites in the body and, therefore, kidney damage and recurrent stenosis due to renal failure, glaucoma, nonsteroidal anti-inflammatory agents associated with hypertension, congestive heart failure, mental illness, diabetic or hypertensive nephropathy Novel, efficacious and effective novel phenyl and heterocyclic derivatives useful for treating conditions associated with excessive or irregular angiotensin II activity, such as pharmaceutical preparations comprising them and their use for antagonizing angiotensin II receptors in mammals Provides

Description

Angiotensin II Antagonists

Since this is an open matter, no full text was included.

Claims (4)

A compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof. Wherein R ₁ is CO ₂ H, SO ₃ H, PO ₃ H ₂ , CONHSO ₂ R ₅ or 5-tetrazolyl; R ₂ is H, —OH, —OCOCH ₃ , halo, C ₁ -C ₄ alkyl, amino, acetamido or C ₁ -C ₄ alkoxy; X is _{- (CH 2) m NHCO-,} - (CH 2) m CONH-, -O-, -NH-, -CH 2 -, - (CH 2) mCO-, or -CO (CH _{2) m} - ego ; R ₃ is C ₄ -C ₉ straight alkyl, C ₄ -C ₉ straight trifluoroalkyl, C ₄ -C ₉ straight alkenyl or C ₄ -C ₉ straight trifluoro alkenyl; R ₄ is -CONH (C ₁ -C ₄ alkyl), -CONH (C ₁ -C ₄ trifluoroalkyl), -CONH (hydroxy-C ₁ -C ₄ alkyl), R ₅ is phenyl, C ₁ -C ₄ alkyl substituted phenyl, C ₁ -C ₅ alkyl or C ₁ -C ₅ trifluoroalkyl, R ₆ is (CH ₂ ) _p R ₁ or C ₁ -C ₄ alkyl ego; R ₇ is H or CH ₃ ; R ₈ is H or — (CH ₂ ) _q R ₁₂ and R ₉ is 0 or S; R ₁₀ is H, — (CH) pR ₁ , C ₁ -C ₇ alkyl, C ₁ -C ₇ trifluoro alkyl, halo, substituted or unsubstituted phenyl, 3-pyridyl, 2-pyrimidyl, furanyl , Oxazolyl, isoxazolyl, substituted or unsubstituted fused bicyclic group, substituted or unsubstituted fused tricyclic group, or 4,4-ethylenedioxy when m is 0; R ₁₁ is H, OH, C ₁ -C ₇ alkoxy, CO ₂ H, SO ₃ H, PO ₃ H ₂ , CONHS0 ₂ R ₅ , or tetrazolyl; R ₁₂ is OH, NH ₂ or CO ₂ H; Y is the R group of natural amino acids; X 'is -0-,-(CH ₂ ) _p -or -S-: m is independently 0 or 1: p is independently 0, 1, 2, 3 or 4; q is 1, 2, 3 or 4; Provided that when R ₄ is group (g) or (h) and R ₁₀ is H, the carboxy of group (h) or tetrazolyl of group (g) is in the 2 or 3 position. A compound of formula la or a pharmaceutically acceptable salt or solvate thereof. Wherein R ₃ is C ₄ -C ₉ straight alkyl, R ₁₀ is unsubstituted or p-substituted phenyl, substituted or unsubstituted fused bicyclic group or substituted or unsubstituted fused tricyclic group; m is 0 or 1; X 'is -0-, -S- or (CH ₂ ) _p ; P is 0, 1, 3 or 4. (R) -1- [1-oxo-2- [4- (2-sulfobenzoyl) amino-lH-imidazol-1-yl) octyl) -4- (cis)-(4-carboxymethylphenoxy- L-proline or a pharmaceutically acceptable salt or solvate thereof. A pharmaceutical formulation for treating hypertension, comprising the compound as claimed in any one of claims 1 to 3 as an active substance, together with one or more pharmaceutically acceptable carriers, excipients or diluents. ※ Note: The disclosure is based on the initial application.