Nk-2 antagonist basic linear compounds and formulations containing them

1) Compounds of general formula (I):

• wherein:
• X1 is a —NR6-CO—, —CO—, —NR6-CS— group;
• R1 is an aryl group selected from pyridine, thiophene, benzene, naphthalene, diphenyl, phenylthiophene, benzothiophene, benzofuran, N-indole substituted by an R7 group, where said aryl group may also be substituted by one or more independent groups selected from halogen, C1-C6 alkyl optionally substituted by not more than three fluorine atoms (i.e. trifluoromethyl group), C1-C6 alkyloxyl, optionally substituted by not more than three fluorine atoms (i.e. trifluoromethyloxyl group), —OH, —NHR7, —N(R7)2, —SR7, —CONHR7, —COR7, —COOR7, —R8COOR7, —OR8COOR7, —R8COR7, —CONHR7, —R8CONHR7, —NHCOR7, -nitro, where R7 is hydrogen or C1-C6 alkyl with a linear or branched chain, and R8 is a C1-C6 alkylene group with a linear or branched chain;
• R6 is selected from a group consisting of hydrogen or a C1-C6 alkyl with a linear or branched chain;
• the broken line indicates a possible double bond and n and m may independently be 0, 1, 2;
• R9 and R10 are selected independently in the hydrogen, C1-C6 alkyl group or may be connected to form an aromatic group selected in a phenyl group;
• X2 is selected in the group formed of —(CH2)p-, —(CH2)q-CO—, —(CH2)s-O—(CH2)q-, —CH═CH—, —CH═CH—CO—, CH═CH—O—(CH2)q- where p may be 2, 3, 4;
• q may be 2, 3, 4:
• and s may be 1, 2;
• R2 is selected from a group consisting of an aryl-alkyl or aryl radical where the aryl part is selected in a group consisting of benzothiophene, indole, pyridine, pyrrol, benzofuran, thiophene, benzene, naphthalene, imadazole, diphenyl, and may optionally be substituted by one or more substituents selected independently from halogen, C1-C6 alkyl optionally substituted by not more than three fluorine atoms (i.e. trifluoromethyl group), C1-C6 alkyloxyl, optionally substituted by not more than three fluorine atoms (i.e. trifluoromethyloxyl group), —OH, —NHR7, —N(R7)2, —SR7, —CONHR7, —COR7, —COOR7, —R8COOR7, —OR8COOR7, —R8COR7, —CONHR7, —R8CONHR7, —NHCOR7, —nitro, where R7 is hydrogen or C1-C6 alkyl with a linear or branched chain, and R8 is a C1-C6 alkylene group with a linear or branched chain;
• R3 contains at least a basic amino group and is selected from a group with general formula:
• —R4—X3—R5
• where R4 is selected from a group consisting of:
• an —NR6- amino group;
• an aliphatic heterocycle containing one or two heteroatoms selected from N, S and O, and optionally substituted by one or two C1-C6 alkyl groups;
• X3 can be a simple bond or is selected in the group consisting of (CH2)t-, —CO—, —O—(CH2)t-, —O—, —NH—CO—CH2-, —NH—CO— where t can be 1, 2, 3;
• R5 is:
• an aliphatic heterocycle, selected in the group consisting of pyrrolidine, piperidine, morpholine, tetrahydropyran, 1,4-dioxa-8-azaspiro[4,5]decane, dioxane, optionally substituted by one or more C1-C6 alkyl, hydroxymethyl, —OH, cyanomethyl and C1-C6 alkyloxy groups;
• a group selected from —NR11R12, —OR11 where R11, R12 are independently selected in the group:
• hydrogen, C1-C6 alkyl;
• an aryl selected from thiophene, pyridine, furane or phenyl optionally substituted by one or more halogen, C1-C6 alkyl, C1-C6 alkyloxy and OH groups;
• the pharmaceutically acceptable salts of compounds of formula (I) with organic and inorganic acids selected in the group:
• hydrochloric, sulphuric, phosphoric, acetic, trifluoroacetic, oxalic, malonic, maleic, fumaric, succinic, tartaric and citric acids;
• the possible optical isomers in the form of enantiomers or diastereoisomers, pure or in the form of racemic or non-racemic mixtures of said isomers;
• the “retro-inverted” compounds, that is, compounds having the structure of general formula (I), but wherein one or two amide bonds are reversed.