Buhlmayer Peter (Arlesheim CHX) Furet Pascal (Thann FRX)
출원인 / 주소
Ciba-Geigy Corporation (Tarrytown NY 02)
인용정보
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초록▼
The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula [Figure] (I) wherein the substituents are defined in the specification; or salts thereof; to processes for the preparation thereof; and to the use thereof as well as to pharmaceutical compositions that
The invention relates to substituted 3-amino-1-arylalkyl-benzazepin-2-ones of the general formula [Figure] (I) wherein the substituents are defined in the specification; or salts thereof; to processes for the preparation thereof; and to the use thereof as well as to pharmaceutical compositions that comprise compounds of formula (I) or pharmaceutically acceptable salts thereof.
대표청구항▼
A compound of the formula [Figure] (I) wherein Ar is aryl; X is C1-C2alkylene or a direct bond; R1 is selected from the group consisting of hydrogen; lower alkyl; aryl-lower alkyl; and an acyl selected from the group consisting of lower alkanoyl, aryl-lower alkanoyl and aroyl, each of which is eithe
A compound of the formula [Figure] (I) wherein Ar is aryl; X is C1-C2alkylene or a direct bond; R1 is selected from the group consisting of hydrogen; lower alkyl; aryl-lower alkyl; and an acyl selected from the group consisting of lower alkanoyl, aryl-lower alkanoyl and aroyl, each of which is either unsubstituted or independently substituted by 1-3 substituents independently selected from the group consisting of lower alkyl, aryl-lower alkyl, lower alkoxy-lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy, aryl-lower alkoxy, C3-C7cycloalkyl, C3-C7cycloalkyl-lower alkyl, nitro, halogen, trifluoromethyl, and amino, where said amino may be unsubstituted, mono- or independently di-substituted by lower alkyl, aryl-lower alkyl or aryl, or disubstituted by lower alkylene or lower alkyleneoxy-lower alkylene; R2 is lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkoxy-lower alkyl, aryl-lower alkyl or C3-C7cycloalkyl-lower alkyl; R3 is carboxy; 5-tetrazolyl, PO2H2, PO3H2 or SO3H2; alkoxycarbonyl; lower alkoxy-lower alkoxycarbonyl; aryl-lower alkoxycarbonyl; aryloxycarbonyl; carbamoyl; carbamoyl that (i) is monosubstituted by hydroxy, lower alkanesulfonyl, halo-lower alkanesulfonyl or by arylsulfonyl, (ii) is monosubstituted or disubstituted, the substituents independently selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl and phenyl-lower alkyl, or (iii) is disubstituted by lower alkylene or by lower alkylene-X1-lower alkylene, wherein X1 is selected from the group consisting of O, S and NH; the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of: lower alkyl, aryl-lower alkyl, lower alkoxy-lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy, aryl-lower alkoxy, C3-C7cycloalkyl, C3-C7cycloalkyl-lower alkyl, nitro, halogen, trifluoromethyl, and amino, where said amino may be unsubstituted, mono- or independently di-substituted by lower alkyl, aryl-lower alkyl or by aryl, or disubstituted by lower alkylene or lower alkyleneoxy-lower alkylene; “aryl”in each case above is an independently-selected “carbocyclic or heterocyclic aryl”which may be independently substituted by 1-3 substituents independently selected from the group consisting of lower alkyl, “carbocyclic or heterocyclic aryl”-lower alkyl, lower alkoxy-lower alkyl, lower alkoxy, lower alkoxy-lower alkoxy, “carbocyclic or heterocyclic aryl”-lower alkoxy, C3-C7cycloalkyl, C3-C7cycloalkyl-lower alkyl, nitro, halogen, trifluoromethyl, and amino, where said amino may be unsubstituted, mono- or independently di-substituted by lower alkyl, “carbocyclic or heterocyclic aryl”-lower alkyl or “carbocyclic or heterocyclic aryl”, or disubstituted by lower alkylene or lower alkyleneoxy-lower alkylene: and “carbocyclic or heterocyclic aryl”is selected from the group consisting of phenyl, naphthyl, pyrrolyl, pyridyl, furyl, thienyl, imidazolyl, isoxazolyl, and thiazolyl; a stereoisomer or a metal, mineral, ammonium, or organic salt thereof. A method of treating pathological symptoms of the human body that are brought about by modulation of the AT2-receptor, which comprises administering a therapeutically effective amount of a compound of formula I according to claim 1, or of a stereoisomer or pharmaceutically acceptable salt thereof.
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