KR920703037A - 5-HT₃antagonists for the Treatment of Hypotension, Goji, and bradycardia Associated with Myocardial Instability - Google Patents

Abstract

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Description

5-HT ₃ antagonist for the treatment of hypotension, goji and bradycardia associated with myocardial instability

[Brief Description of Drawings]

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Claims (13)

An effective and / or prophylactic amount of a 5-HT ₃ receptor antagonist is administered to a mammal, such as a human, by administering to a mammal in need of treatment and / or prevention of goji and bradycardia associated with myocardial stability and / or hypotension. A method of treating and / or preventing goji and bradycardia and / or hypotension associated with myocardial instability, Use of 5-HT ₃ receptor antagonists in the treatment and / or prevention of goji, bradycardia and / or hypotension associated with myocardial instability. A pharmaceutical composition for use in the treatment and / or prophylaxis of goji, bradycardia and / or hypotension associated with myocardial instability, consisting of 5-HT ₃ receptor antagonists, and pharmaceutically acceptable excipients. The method, use or composition according to any one of claims 1, 2 or 3, wherein the 5-HT ₃ receptor antagonist is of formula (I), or a pharmaceutically acceptable salt thereof; X-A-R (I) Wherein X is a phenyl group or a monocyclic 5- or 6-membered heteroaryl group, one of which is optionally fused to a saturated or unsaturated 5-7 membered carbocyclic or heterocyclic ring; A is a binding moiety; And R is a saturated azabicyclic moiety or an imidazolyl group moiety. The method, use or composition according to claim 4, wherein X is the following partial-formulas (a), (b), (c), (d), (f) or (g): Wherein Ra to Re and Rg are selected from hydrogen, halogen or hydroxy; R ₁ is hydrogen and R ₂ is hydrogen or C _1-4 alkyl; Both R ₁ and R ₂ are a bond; R ₃ to R ₄ are individually hydrogen or C _1-6 alkyl; And R ₄ together with R ₂ can be C _2-7 polymethylene when R ₁ is hydrogen; R ₈ and R ₉ are C _2-6 polymethylene or C _2-5 polymethylene individually selected from hydrogen or C _1-6 alkyl or interrupted by —O— bonds with R ₈ and R ₉ together; R ₁₈ is hydrogen, C _1-6 alkoxy, C _3-8 alkyloxy or C _3-8 during Colo cycloalkyl C _1-4 alkyloxy group, or; R ₁₈ is bonded to Y such that YR ₁₈ is NB = N, wherein B is N or CH; R ₁₁ is hydrogen, halo, C _1-6 alkoxy or C _1-6 alkyl; R ₁₈ and R ₁₁ are joined to -OCH (RuRv) -E-, wherein E is (CH ₂ ) _n or NRwCO (CH ₂ ) _n , where n is 1 or 2 and m is 0 or 1, and Ru , Rv and Rw are individually selected from hydrogen or C _1-6 alkyl; R ₁₂ is amino optionally substituted by hydrogen C _1-6 alkoxy or C _1-6 alkyl group or R ₁₂ is alkanoylamino; And R ₁₃ is halo, C _1-6 alkyl, C _1-6 alkoxy or C _1-6 alkylthio; R ₁₄ is hydrogen C _1-6 alkyl; And L is CH or N. The method, use or composition according to claim 4 or 5, wherein A is a group of CONH (amide), COO (ester), NHCONH (urade), CONHCONH (extended uraide), or formula (h): Wherein the dashed circle represents two double bonds at any position in the 5-membered ring; Two of G, H and I are selected from oxygen, sulfur, nitrogen and carbon, the other being oxygen, sulfur or nitrogen; And E is C _1-5 alkylene which is a bond or optionally substituted by phenyl or hydroxy. The method, use or composition according to claim 6, wherein R is the following partial-formula (i), (j) or (k): In which Z is (CH ₂ ) _n where n is 2 or 3, or Z is CH ₂ —O—CH ₂ ; p and q are individually 1 to 3; And R ₁₅ or R ₁₆ is methyl or ethyl, preferably methyl. 8. The compound of claim 7, wherein R is endo-9-azabicyclo [3.2.1] non-3-yl, endo-8-azabicyclo [3.2.1] oct-3-yl, 9-aza-3-oxabi The method, use or composition which is cyclo [3.2.1] non-7-yl or 3-quinuclidinyl. The method, use or composition according to claim 8, wherein the compound of formula (I) is MDL 72222, ICS 205930, Granissetron or PU 46470A. The method, use or composition according to claim 4 or 5, wherein A is -CO- (R ₂ ) ₂ -and R is an imidazolyl moiety. The method, use or composition according to claim 10, wherein R is 5-methyl-4-imidazolyl. The method, use or composition according to claim 11, wherein the compound of formula (I) is ondansetron. The method, use or composition of claim 1, wherein the 5-HT ₃ receptor antagonist is described herein by reference to a written patent publication relating to 5-HT ₃ receptor antagonist. ※ Note: The disclosure is based on the initial application.