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Amino-thiazole and oxazole derivatives

Assignee: Akzo NV
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Filing: 1987-04-17
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Granted: —
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Expires: 2007-04-17
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Abstract

Abstract The present invention relates to new amino-thiazole and amino-­oxazole derivatives of the general formula: wherein: R represents hydrogen, a lower alkyl group with 1 to 4 carbon atoms, a lower alkenyl group, a phenyl-alkyl (1-4 C), furanyl-alkyl (1-4 C) or thienyl-alkyl (1-4 C) group; X represents sulphur or oxygen; R₁ and R₂ represent hydrogen or alkyl (1-4 C), and the dotted line represents an optional extra bond, as well as pharmaceutically acceptable acid addition salts thereof, having potent dopamine-agonist activity.

Inventors

  • 👤 Duncan Robertson Rae
  • 👤 Samuel George Gibson

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-02 23:15
CPC Classifications
C; C07; C07D; C07D413/00; C07D413/02; C07D413/04; A; A61; A61P; A61P25/00; A61P25/24; A61P25/26; A61P9/00; A61P9/12; C07D417/00; C07D417/02; C07D417/04

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 73 words
Amino-thiazole and amino-oxazole derivatives of the general formula: wherein: R represents hydrogen, a lower alkyl group with 1 to 4 carbon atoms, a lower alkenyl group, a phenyl alkyl (1-4 C), furanyl alkyl (1-4 C) or thienyl alkyl (1-4 C) group; X represents sulphur or oxygen; R₁ and R₂ represent hydrogen or alkyl (1-4 C), and the dotted line represents an optional extra bond, as well as pharmaceutically acceptable acid addition salts thereof.
Claim 2
Dependent Claim 73 words
Amino-thiazole and amino-oxazole derivatives of the general formula: wherein: R represents hydrogen, a lower alkyl group with 1 to 4 carbon atoms, a lower alkenyl group, a phenyl alkyl (1-4 C), furanyl alkyl (1-4 C) or thienyl alkyl (1-4 C) group; X represents sulphur or oxygen; R₁ and R₂ represent hydrogen or alkyl (1-4 C), and the dotted line represents an optional extra bond, as well as pharmaceutically acceptable acid addition salts thereof.
Claim 3
Dependent Claim 19 words
Compounds according to claim 1, in which the dotted line is an extra bond, and pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim 17 words
Compounds according to claim 1, in which X represents a sulphur atom, and pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim 18 words
Compounds according to claim 1, in which R₁ and R₂ represent both hydrogen and pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim 20 words
Compounds according to claims 2, 3 or 4 in which R represents a methyl, ethyl, n.propyl, allyl or cyclopropylmethyl group.
Claim 7
Dependent Claim 12 words
The compound according to claim 1: 4-(1-ethyl-1,2,5,6-tetrahydropyrid-3-yl)-thiazole-2-amine and pharmaceutically acceptable salts thereof.
Claim 8
Dependent Claim 12 words
The compound according to claim 1: 4-(1-propyl-1,2,5,6-tetrahydropyrid-3-yl)-thiazole-2-amine and pharmaceutically acceptable salts thereof.
Claim 9
Dependent Claim 18 words
Pharmaceutical composition containing the compound of claim 1 together with one or more pharmaceutically acceptable carriers or diluents.
Claim 10
Dependent Claim 29 words
A process for the preparation of a compound claimed in claim 1, characterized in that the compound is prepared by methods in actual use or described in the literature.
Claim 11
Dependent Claim 100 words
Process according to claim 9, characterised in that a compound of the formula II wherein X and R, have the afore said meanings, A⁻ is any suitable anion, such as a halogen or hydroxy anion, and R₃ and R₄ have the same meaning as R₁ and R₂ but may in addition represent an amino-protecting group or an aliphatic acyl group with 1-4 carbon atoms, is partially or completely hydrogenated, after which, if present, the N-protecting group is removed or the N-acyl group is reduced, after which the compound thus obtained may be converted into a pharmaceutically acceptable acid addition salt.

References Cited (Backward Citations)

DE2132431A1 Cited
EP0111904A2 Cited
EP0149884A2 Cited

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