Phenylethanolaminotetralincarboxamide derivatives

C - Chemistry – Metallurgy – 07 – C

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C07C 235/20 (2006.01) A61K 31/16 (2006.01) A61K 31/395 (2006.01) A61K 31/445 (2006.01) A61K 31/5375 (2006.01) C07C 235/06 (2006.01) C07D 295/185 (2006.01)

Patent

CA 2251090

Phenylethanolaminotetralincarboxamide derivative represented by general formula (I) and pharmacologically acceptable salts thereof, wherein A represents lower alkylene; B represents amino, di(lower alkyl)amino or 3- to 7-membered alicyclic amino which may bear oxygen on the ring; the asterisked carbon atom represents a carbon atom with an R- or S-configuration or a mixture of such atoms; and the carbon atom labeled with (S) represents a carbon atom with an S-configuration. These compounds have selective .beta.2-adrenergic receptor stimulating effects while reducing the burden on the heart, such as tachycardia, and are useful as preventives for threatened abortion and premature birth, bronchodilator, and agents for remission and lithagogue for urinary calculus.

Dérivé de phényléthanolaminotétralincarboxamide représenté par la formule générale (I) et des sels pharmacologiquement acceptables de ceux-ci. Dans la formule (I), A représente alkylène inférieur; B représente amino, di(alkyle inférieur)amino ou amino alicyclique à 3 à 7 éléments qui peut porter oxygène sur le cycle; l'atome de carbone marqué d'un astérisque représente un atome de carbone à configuration R- ou S- ou un mélange de ces atomes; et l'atome de carbone marqué d'un (S) représente un atome de carbone à configuration S. Ces composés comprennent un récepteur adrénergique- beta 2 sélectif stimulant les effets tout en réduisant la charge du coeur, telle que la tachychardie, et sont utiles en tant qu'agents de prévention du risque d'avortement, d'accouchement prématuré, en tant qu'agents de bronchodilatation, de rémission et agent pour l'expulsion des calculs urinaires.

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