PHENYL Compound, use of said Compound for the preparation of a Medicine Compound isotopically marked, Diagnostic agent, Pharmaceutical composition, Process for Preparation of said compound and Compound for exclusive use in this procedure

摘要

A phenyl compound according to formula (1) in which each of m and n is independently an integer of 0û3 and one or more of the hydrogens of said alkylene chain may be optionally substituted with any of C1-6 alkyl, C1 alkoxy -6 or hydroxy or one more of the methylene groups can be optionally substituted with a heteroatom such as O, N or S; R1 is selected from hydrogen, a C1-6 alkyl, C2-6 alkenyl, straight or branched C3-8 cycloalkyl, (C4-8 alkyl-cycloalkyl), where alkyl is C1-2 alkyl and cycloalkyl is C3-6 cycloalkyl, R2 is selected from any of (i) hydrogen; (ii) a C1-6 alkyl,1. Alquenilo c2-6 plasma c2-6, straight or scattered (III) [(CH2) q-arilo]; (IV) [(CH2) r-heterogeneities, heterogeneities have 5 to 10 atoms, heterogeneities are selected from any atom; Here, arilo and heretics can be optional, independently replaced by one or two alternatives, each of which is defined below, in addition, each of which is a whole 0-3; (V) c3-10 cyclododecene, 1. It can choose to contain one or more unhealthy parts, and can choose to be replaced by one or more heteromorphic parts. The heteromorphic part has 5 to 10 atoms, and the heteromorphic part is selected from any heteromorphic part;Here, arilo and heterosexuality can be optional and can be replaced by one or two alternatives. Here, the definition of each alternative and heterosexuality is as follows: (VI) selective and independent arilo C6-10, which is replaced by one or more heteromorphic (s) with 5 to 10 atoms, selected from any heteromorphic, N and O; heteromorphic atoms can be replaced by one or two substitutes, each of which is defined as follows; (VII) heteromorphism of 5 to 10 atoms, and heteromorphism selected from any one s, N and O;Among them, arilo and heretics can be optional, independently replaced by one or two alternatives, and each alternative and the alternatives defined below: or R1 and R2 can arbitrarily form an aperiodic ring, which can include optional saturation or unsaturated; R3 can be selected from any one of (I) hydrogen compounds; and (II) a tar. C1-6, alquenilo c2-6, rectum or branch c2-6, or c2-6 tar (III) arilalquilo C6-10, wherein arilo can be replaced by one or more 5 to 10 atom heteroatoms selected from any s, N, and O;Aries and non Aries may be replaced by one or two substitutes, and each substitute and non Aries (c5-10 tar) shall be replaced as defined in (IV) of the following definitions,Among them, heteromorphic atoms are 5 to 10, and heteromorphic atoms are selected from any s, N and O; negative and heteromorphic atoms can be optional and independently replaced by one or two substitutes, Each of them (V) c3-10 cyclododecane, as defined below, contains one or more unhealthy substances, which can be replaced by one or more heteromorphic atoms of 5 to 10 atoms. Heteromorphic atoms can be selected from any s, N and o. arilo and heteromorphic atoms can be selected independently. Replace with one or two substitutes, and in each case and as defined below; (VI) [cycloquilo C3-6 - (CH2) q],where q is an integer from 1 to 3; R4 is selected from (i) hydrogen; (ii) a C1-6 alkyl, C2-6 alkenyl or straight or branched C2-6 alkynyl, (iii) C6-10 aralkyl where the aryl may be optionally substituted with one or more heteroaryl (s) of 5 to 10 atoms and where the heteroatom is selected from any of S, N and O; and where aryl and heteroaryl may be optionally and independently substituted with 1 or 2 Y substituents, where each Y is as defined below; (iv) heteroaryl (C5-10 alkyl),1. Heteromorphism has 5 to 10 atoms. Heteromorphism atoms are selected from any s, N and o. arilo and heteromorphism atoms can be optional and independently replaced by 1 or 2 substitutes, each substitute and the substitute defined below; (v) C3-10 cyclododecane, optionally containing one or more unhealthy substances, may be replaced by one or more heteroatoms of 5 to 10 atoms, which may be selected from any one s, N and O, in which case arilo and heteroatoms may optionally or independently be replaced by one or two substitutes, in which case 1. Each as defined below;(VI) selective and independent arilo C6-10, which is replaced by one or more heteromorphic (s) with 5 to 10 atoms, selected from any heteromorphic, N and O; heteromorphic atoms can be replaced by one or two substitutes, each of which is defined as follows; (VII) heteromorphism of 5 to 10 atoms, selected from any s, N and O; arilo and heteromorphism can be optional, independently replaced by 1 or 2 substitutes, each of which and the substitutes defined below; R5 selected from (I) hydrogen; (II) C1-6 alquenilo c2-6 coke oil;C2-6 alkenyl or straight or branched C2-6 alkynyl, (iii) arylalkyl C6-10, where the aryl may optionally be substituted with one or more heteroaryl (s) of 5 to 10 atoms and where the heteroatom is selected from any of S, N and O; and where aryl and heteroaryl may be optionally and independently substituted with 1 or 2 Y substituents, where each Y is as defined below; (iv) heteroaryl (C5-10 alkyl),where the heteroaryl has from 5 to 10 atoms and where the heteroatom is selected from any of S, N and O and where aryl and heteroaryl can be optionally and independently substituted with 1 or 2 substituents Y, where each Y is as defined later. (v) C3-10 cycloalkyl, which optionally contains one or more unsaturations and is optionally substituted with one or more heteroaryl (s) of 5 to 10 atoms and where the heteroatom is selected from any of S, N and O; and where aryl and heteroaryl may be optionally and independently substituted with 1 or 2 Y substituents, where each Y is as defined below; (vi) aryl C5-10,optionally and independently substituted with one or more heteroaryl (s) having from 5 to 10 atoms and where the heteroatom or atoms are selected from any of S, N and O; and where heteroaryl may be optionally and independently substituted with 1 or 2 Y substituents where each Y is as defined below; (vii) heteroaryl of 5 to 10 atoms and where the heteroatom is selected from any of S, N and O and where aryl and heteroaryl may be optionally and independently substituted with 1 or 2 Y substituents, where each Y is as defined later; (viii) structures (2) or (3) where each of R7, R8, R9,R10 and R11 are selected independently from (a) hydrogen; (b) C1-6 alquenilo c2-6 tar or c2-6 straight tar or branch; (c) arilalquilo C 6-10; (c) arilalquilo C6-10, where arilo can be replaced by one or more 5 to 10 atom heteromorphisms selected from any s, N and O; arilo and Heretics can be optional and can be replaced independently by one or two alternatives, in which case each alternative is defined below; (d) heretics (c5-10 tar)Where there are 5 to 10 atoms in heteromorphism, heteromorphism atoms are selected from any s, N and o. arilo and heteromorphism atoms can be optional and independently replaced by one or two substitutes, where each of them is (E) cycloquilo c3-10, It can selectively contain one or more unhealthy substances, which can be replaced by one or more heteromorphic atoms of 5 to 10 atoms. Heteromorphic atoms can be selected from any s, N and O. cathode and heteromorphic atoms can be replaced by one or two substitutes, which can be replaced independently, There, each as defined below;(f) C6-10 aryl optionally and independently substituted with one or more heteroaryl (s) having from 5 to 10 atoms and where the heteroatom (s) are selected from any of S, N and O and where the heteroaryl may be optional and independently substituted with 1 or 2 Y substituents, where each Y is as defined below; (ix) structure (4) or R4 and R5 can optionally form a heterocyclic ring that can be optionally saturated or unsaturated. Each Y is independently selected from hydrogen, CH3; - (CH2) p1CF3 halogen, alkoxy, C1-3; hydroxy; -NO2; -OCF3; -CONRaRb, -COORa, -CORa, - (CH2) p2NraRbû (CH2) p3CH3, (CH2) p4SORaRb, - (CH2) p5SO2Ra,C4-8 (alkyl-cycloalkyl) where alkyl is C1-2 alkyl and cycloalkyl is C3-6 cycloalkyl, where 1 or 2 heteroaryls have 5 to 10 atoms and the heteroatom is selected from S, N and O, as well as oxides such as N-oxides or sulfoxides and where Ra and Rb is independently selected from hydrogen, a branched or straight C1-6 alkyl, C1-6 alkenyl or C3-8 cycloalkyl, and where each of p1, p2, p3, p4, p5, and p6 is independently 0.1 or 2, as well as the pharmaceutically acceptable salts of the compounds of formula 1 and also the isomers, hydrates, isoforms and prodrugs thereof; its use for the manufacture of a medicine, diagnostic agent,It contains its pharmaceutical ingredients, preparation process, intermediate compounds, and its sole use is in the preparation of Formula 1 compounds and treatment methods. These compounds contribute to the treatment of, in particular, various painful disorders, such as chronic pain, acute pain, cancer-related pain, and induced pain.