JP-2022552373-A5 -

Dates

Publication Date

20230515

Application Date

20200624

Description

PCAN component 7a can be synthesized by a similar method.In one embodiment, for example, the following items are provided.(Item 1)formula[In the formula,CBNC is a cannabinoid conjugate component containing a therapeutic component that is covalently bound to a cannabinoid component either directly or via a linker.LccThis is a CBNC linker, but it may not always be present.B is a target-binding component, and the target-binding component is an antibody.LaThe active ingredient is a linker,A is the active ingredient,m is between 1 and 30, n is between 0 and 29, and the sum of m + n is between 1 and 30.CBNC is,(I) The therapeutic agent component is directly bound to the cannabinoid component, and the therapeutic agent component is(1)[# indicates the covalent binding site to the cannabinoid component.]A Michael acceptor component having a structure selected from,(2)[In the formula, Q is CO, CS, or CR6aR6bis], and(3) Structure[In the formula, R8and R9These are H and CH, independently.3, and CH2CH3[Selected from]Carbamate components havingSelected from,R is,(a) H,(b) (1) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(2) One, two, or three substituents independently selected from the substituents of group 1,C1-C8 linear or branched alkyl groups, which are substituted as needed.(c) Containing one, two, or three heteroatoms independently selected from O, N, and S,(1) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(2) One, two, or three substituents independently selected from the substituents of group 1,C1-C8 linear or branched heteroalkyl groups, which are substituted as needed.(d) (1)(i) 1, 2, 3, 4, 5, or 6 fluorine atoms, and/or(ii) One or two substituents independently selected from the substituents of group 2,C1-C6 linear or branched alkyl groups, which are substituted as needed, and(2) Containing one or two heteroatoms independently selected from O, N, and S,(i) 1, 2, 3, 4, 5, or 6 fluorine atoms, and/or(ii) One or two substituents independently selected from the substituents of group 1.C1-C6 linear or branched heteroalkyl groups, which are substituted as needed.Phenyl, independently selected from the group consisting of, optionally substituted with one, two, or three substituents.(e) (1) Phenyl,(2) Halides,(3) Cyano,(4) (i) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(ii) One, two, or three substituents independently selected from the substituents of group 2,C1-C6 linear or branched alkyl groups, which are substituted as needed, and(5) Containing one, two, or three atoms independently selected from O, N, and S,(i) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(ii) One, two, or three substituents independently selected from the substituents of group 2.C1-C6 linear or branched heteroalkyl groups, which are substituted as needed.A 6-10 member aromatic compound, independently selected from the group consisting of, optionally substituted with 1, 2, 3, or 4 substituents,(f) comprising 1, 2, 3, 4, 5, or 6 heteroatoms independently selected from O, N, and S,(1) Phenyl,(2) Halides,(3) Cyano,(4) Trifluoromethyl,(5) (i) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(ii) One, two, or three substituents independently selected from the substituents of group 2.C1-C6 linear or branched alkyl groups, which are substituted as needed, and(6) Containing one, two, or three atoms independently selected from O, N, and S,(i) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(ii) One, two, or three substituents independently selected from the substituents of group 2.C1-C6 linear or branched heteroalkyl groups, which are substituted as needed.A 5- to 10-membered heteroaromatic compound, independently selected from, optionally substituted with 1, 2, 3, or 4 substituents,(g) (1) (i) 1, 2, 3, 4, 5, or 6 fluorine atoms, and/or(ii) One, two, or three substituents independently selected from the substituents of group 2.C1-C6 linear or branched alkyl groups, which are substituted as needed.A molecule independently selected from the group consisting of, optionally substituted with one, two, or three substituents,(h) Having one, two, or three heteroatoms independently selected from O, N, and S,(1) (i) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(ii) One, two, or three substituents independently selected from the substituents of group 2.C1-C6 linear or branched alkyl groups, which are substituted as needed.(2) (i) 1, 2, 3, 4, 5, 6, 7, 8, or 9 fluorine atoms and/or(ii) One, two, or three substituents independently selected from the substituents of group 2.C1-C6 linear or branched heteroalkyl groups, which are substituted as needed.(3) Phenyl, which is optionally substituted with one, two, or three substituents independently selected from the substituents of group 2, and(4) 5- to 10-membered heteroaromatic compounds, optionally substituted with one, two, or three substituents independently selected from the substituents of group 2.A 3- to 9-membered cycloheteralkyl group, independently selected from the group consisting of