65938-77-4Relevant articles and documents
Butyne diol derivatives
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, (2008/06/13)
The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula I and especially their use as endothelin receptor antagonists.
Indole derivatives useful as endothelin receptor antagonists
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, (2008/06/13)
PCT No. PCT/EP97/01882 Sec. 371 Date Oct. 5, 1998 Sec. 102(e) Date Oct. 5, 1998 PCT Filed Apr. 11, 1997 PCT Pub. No. WO97/43260 PCT Pub. Date Nov. 20, 1997Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl [optionally substituted by CO2H or CO2(C1-6 alkyl)], C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6, alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCOR10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or CONHSO2(C1-6alkyl); Ar1-3 independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.