Medicaments

Use of an adenosine A1 agonist for the manufacture of a medicament for the treatment of emesis wherein the adenosine A1 agonist is selected from:

• a compound of formula (I):
• 5
• wherein X represents O or CH2;
• R2 represents C1 3alkyl, CI3alkoxy, halogen or hydrogen;
• R3 represents H, phenyl (optionally substituted by halogen), a 5 or 6 membered heteroaryl group, C1-6 alkoxy, C1-6 alkylO(CH2)n where n is 0-6, C3-7cycloalkyl, C1-6 hydroxyalkyl, halogen or a C1-6 straight or branched alkyl, C1-6 alkenyl or C1-6 alkynyl group optionally substituted by one or more halogens;
• Y and Z represent O, N, CH, N(C1-6 alkyl);
• W represents CH, O, N, S, N(C1-6 alkyl);
• and wherein at least one of W and Z represents a heteroatom (and when Y, Z and/or W is N, the presence or absence of an additional H would be apparent to a person skilled in the art);
• with the proviso that when W represents CH, Z represents N and Y represents O, R3 cannot be H;
• R4 and R5 independently represent H or a C1-6 straight chain or branched alkyl group;
• R1 represents hydrogen or a group selected from:
• (1) -(alk)n -(C3-7) cycloalkyl, including bridged cycloalkyl, said cycloalkyl group optionally substituted by one or more substituents selected from OH, halogen, -(C1-3) alkoxy, wherein (alk) represents C1-3 alkylene and n represents 0 or 1;
• (2) an aliphatic heterocyclic group of 4 to 6 membered rings containing at least one heteroatom selected from O, N or S. optionally substituted by one or more substituents selected from the group consisting of -(C1-3)alkyl, —CO2—(C1-4)alkyl, —CO(C1-3alkyl), —S(═O)n-(C1-3alkyl), —CONRaRb (wherein Ra and Rb independently represent H or C1-3alkyl) or ═O;
• where there is a sulfur atom in the heterocyclic ring, said sulfur is optionally substituted by (═O)n, where n is 1 or 2;
• (3) Straight or branched C1-12 alkyl, optionally including one or more O, S(═O)n (where n is 0, 1 or 2) and N groups substituted within the alkyl chain, said alkyl opffonally substituted by one or more of the following groups, phenyl, halogen, hydroxy, C3-7 cycloalkyl or NRaRb wherein Ra and Rb independently represent hydrogen, C3-7 cycloalkyl or a C1-6 straight chain or branched alkyl optionally substituted by C3-7 cycloalkyl;
• (4) a fused bicyclic aromatic ring:
• 6
• wherein B represents a 5 or 6 membered heterocyclic aromatic group containing 1 or more O, N or S atoms, wherein the bicyclic ring is attached to the nitrogen atom of formula (I) via a ring atom of ring A and ring B is optionally substituted by —CO2 -(C1-3alkyl);
• (5) a phenyl group optionally substituted by one or more substituents selected from:
• -halogen, —SO3H, -(alk)nOH, -(alk)n -cyano, —(O)n -(C1-6)alkyl (optionally substituted by one or more halogens), - (alk)n -nitro, —(O)m -(alk)n—CO2Rc,
• -(alkn)- CONRcRd -(alk)n —CORc, -(alk)n —SORe, -(alk)n —SO2Re, -(alk)n- SO2NRcRd, -(alk)nORc, -(alk), —(CO)m- NHSO2Re, -(alk)m- NHCORc, -(alk)n- NRcRd wherein m and n are 0 or 1 and alk represents a C1-6alkylene group or C2-6 alkenyl group;
• (6) A phenyl group substituted by a 5 or 6 membered heterocyclic aromatic group, said heterocyclic aromatic group optionally being substituted by C1-3alkyl or NRcRd;
• Rc and Rd may each independently represent hydrogen, or C1-3 alkyl or when part of a group NRcRd, Rc and Rd together with the nitrogen atom may form a 5 or 6 membered heterocyclic ring optionally containing other heteroatoms, which heterocyclic ring may optionally be substituted further by one or more C1-3 alkyl groups;
• Re represents C1-3alkyl;
• N-(3-fluoro-4-hydroxyphenyl)-5′-O-methyl-adenosine,iand
• N-(4-hydroxyphenyl)-5′-O-methyl-adenosine;
• or a salt and/or solvate thereof.