Pharmaceutical formulation, pyrazines, uses of these compounds for the manufacture of medicinal products, processes for the preparation of these compounds and Intermediate compounds

摘要

1. Pyrethroids using formula (1): conr3, nr3co, so2n3, nr3so2, ch2n3, nr3ch2, nr3conr3, C1-6 tar, CH2CO, coch2, ch = ch, och2 or CH2O; X is ch or N; P is phenyl or 5 or 6 aromatic rings, containing one or more heteroprotons selected from n, O or s, or phenyl or phenyl rings, or aromatic rings 5 or 6 members may optionally be combined with a saturated, partially saturated or unsaturated ring consisting of 5 or 6 members containing atoms selected from C, n or s; q is phenyl, or heteroaromatic rings containing 5 or 6 members selected from n, or at least one atom of nitrogen; R1 is halogen,nitro, C0-6CN alkyl, C0-6OR8 alkyl, fluormethyl, difluoromethyl, trifluoromethyl, C0-6 alkyl NR8R9, C0-6 alkyl CONR8R9, C0-6 alkyl NR8 (CO) R9, NR8 (CO) OR9, C0-6 alkyl O (CO) R8, C0-6 alkyl SO2R8, C0-6 alkyl SOR8, C0-6 alkyl COR8, C0-6 alkyl (CO) OR8, C1-6 alkyl CO2R8, O C0-6 alkyl SO2R8, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C0-6 alkyl C3-6 cycloalkyl, C0-6 alkyl aryl or C0-6 alkyl heteroaryl, wherein any C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, alkyl C0-6 C3-6 cycloalkyl, C0-6 alkyl aryl or C0-6 alkyl heteroaryl may optionally be substituted with one or more A; R2 is halo, nitro, CHO, C0-6 alkyl CN, OR C1-6 alkyl CN, C0-6 alkyl OR4,Or C1-6alkyl OR4, Fluoromethyl, Difluoromethyl, Trifluoromethyl, Fluoromethoxy, Difluoromethoxy, Trifluoromethoxy, C0-6alkyl NR4R5, O C1-6alkyl NR4R5, O C1-6alkyl Or C1-6alkyl NR4R5, NR4OR5, C0-6alkyl CO2R4, OR C1-6 alkyl CO2R4, C0-6 alkyl CONR4R5, OR C1-6 alkyl CONR4R5, OR C1-6 alkyl NR4 (CO) R5, C0-6 alkyl NR4 (CO) R5, O (CO) NR4R5, NR4 (CO) OR5, NR4 (CO) NR4R5, O (CO) OR4, O (CO) R4, OR C1-6 alkyl COR4, NR4 (CO) (CO) R4, NR4 (CO) / CO) NR4R5, SR4, C0-6 alkyl (SO2) NR4R5, OR C1-6 alkyl NR4 (SO2) R5, OR C0-6 alkyl (SO2) NR4R5, C0-6 (SO) alkyl NR4R5, OR C1-6 alkyl (SO) NR4R5, SO3R4 , C1-6 alkyl NR4 (SO2) NR4R5, C0-6NR4 (SO) R5 alkyl, OR C0-6 alkyl NR4 (SO) R5, O C0-6 SO2R4 alkyl, C0-6 SO2R4 alkyl, C0-6 SOR4 alkyl,C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C0-6 alkyl C3-6 cycloalkyl, C0-6 alkyl aryl or C0-6 alkyl heteroaryl, wherein any C1-6 alkyl, C2-6 alkenyl, alkynyl C2-6, C0-6 alkyl C3-6 cycloalkyl, C0-6 alkyl aryl or C0-6 alkyl heteroaryl may optionally be substituted with one or more A; m is 0, 1, 2, 3 or 4; n is 0, 1, 3, 4, or 5; R3 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C0-6alkyl C3-6cycloalkyl, C1-6alkyl NR6R7 or C1-6alkyl CONR6R7; R4 and R5 are independently selected from hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C0-6 alkyl C3-6 cycloalkyl, C0-6 alkyl aryl, C0-6 alkyl heteroaryl and C1-6 alkyl NR6R7 ;R4 and R5 may together form a 5- or 6-membered heterocyclic ring containing one or more heteroatoms selected from N, O, or S, wherein said heterocyclic ring may be optionally substituted with A; R6 and R7 are independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl and C0-6alkyl C3-6cycloalkyl; R6 and R7 may together form a 5- or 6-membered heterocyclic ring containing one or more heteroatoms selected from N, O, or S, wherein said heterocyclic ring may be optionally substituted with A; R8 and R9 are independently selected from hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl,C0-6 alkyl aryl, C0-6 alkyl heteroaryl and C0-6 alkyl C3-6 cycloalkyl; R8 and R9 may together form a 5- or 6-membered heterocyclic ring containing one or more heteroatoms selected from N, O, or S, wherein said heterocyclic ring may be optionally substituted with A; R14 is hydrogen, methyl, fluorine, chlorine, or bromine; wherein any C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C0-6 alkyl C3-6 cycloalkyl, C0-6 alkyl aryl, C0-6 alkyl heteroaryl defined under R3 to R9 may be substituted with one or more TO; A is halo nitro, CHO, CN, OR4, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C0-6 alkyl, C3-6 cycloalkyl; fluormethyl, difluoromethyl,Trifluoromethane, fluoromethyl, difluoroethane, trifluoromethy, c0-6 nr4r5 tar, C1-6 nr4r5, nr4r5, co2r8, conr4r5, Nr4 (CO) R4, O (CO) R4, cor4, Sr4, so) nr4r5, so) nr4r5, so 3r4, so2r4 or SO4, as free radicals or drug acceptable salts, However, if both P and Q are phenyle, P is methylpyridine, and Q is phenyl, then the substance is not methylene; drug formula, the use of these compounds in drug manufacturing, and the preparation process of these compounds,And intermediate compounds. These compounds are included in drugs for neurodegenerative and schizophrenic diseases, diabetes and diabetic neuropathy, and hair loss.