FUSED Heterocyclic compounds containing pyrrole and pyrazole, useful in the treatment of diseases mediated by serotonin, Pharmaceutical compositions containing them, Methods of Preparation and uses

摘要

Compound heterocyclic compounds containing pyridine and pyrazole, used for the treatment of serotonin transmitted diseases, pharmaceutical components containing such substances, preparation methods and uses. Item 1: a compound that has modulating activity from the formula serotonin receptor (1),(2) Or (3), where m is 0, 1 or 2, n is 1, 2 or 3; P is 1, 2 or 3, but M is 1, P is not 1, M + n is less than or equal to 4; m + P is less than or equal to 4; q is 0 or 1, R is 0, 1, 2, 3, 4 or 5; R3 is C1-4 tar, optional olefin, allyl or benzene, each with c1-3 halogen-3 substitute; AR is an arilo or heterosexual ring selected from a group consisting of A9 phenylReplace - oalquileno c1-4o in adjacent C - or RR or di- (CH2) 2-3NH-,- (CH2) 1-2NH (CH2) --(CH2) 2-3n (C1-4 tar) - O - (CH2) 1-2n (C1-4 tar) (CH2) -;RR is selected from a group consisting of - Oh, C1-6, oal quilo C1-6, alquenilo c2-6, oal quenilo C3-6, aquinio c2-6, oal quinilo C3-6, CN, NO2, n (ry) RZ (where ry and RZ are selected independently of H or C1-6 cypress reservoirs),- (C = O) N (Ry) Rz, - (N-Rt) CORt, - (N-Rt) SO2 C1-6 alkyl (where Rt is H or C1-6 alkyl), - (C = O) C1 alkyl -6, - (S = (O) n) - C1-6 alkyl (where n is selected from 0, 1 or 2),-So2n (ry) RZ -, ScF3, Halo -, CF3 -, ocf3 -, COOH and coo tar C1-6; and (b) polyphenylene or pyridine, to synthesize two carbon elements of cyclic carbon, adjacent to the other three carbon elements, forming five carbon aromatic rings, and the rest is replaced by carbon atoms; O, s, NH n (C1-4 tar), the rest It even has an extra carbon atom called - n=Optional simplex merging ringDi-o tri - is replaced by RR; (c) phenyl merges with two adjacent members of the ring to form a combined aromatic ring composed of six members, and the rest contains one or two carbon atoms, consisting of - n =,The combined ring can become a monkeyChange di-o tri to RR; d.nafilo, monomer can be selected-Di-o tri replaced with RR; (E) a monoric aromatic hydrocarbon compound, there are 5 atoms on the ring, there is a polymerization point of atom and carbon on the ring, which is replaced by carbon atom; O, gt, s, gt, NH O gt, n (C1-4 tar),It even has an extra carbon atom instead of - n =,In the alternative monomer or binary compounds, RR and benzodiazepine fusion or pyridiene fusion are used to replace the two adjacent carbon atoms, and the rest benzodiazepine fusion or pyridiene fusion,Whatever you want, monkeySay...(f) A single cycle aromatic hydrocarbon group with six atoms in the ring and one or two carbon atoms from - n=In the alternative monomer or binary compounds, RR and benzodiazepine fusion or pyridiene fusion are used to replace the two adjacent carbon atoms, and the rest benzodiazepine fusion or pyridiene fusion,The substitute is mono-odi, which is replaced by RR; (g) phenyl or pyridine, which is replaced by the substitute selected from a group of substances such as phenyl, pyridine, thiophosphor, oxazolilo and tetrazolidine. The resulting substitute is:There's no choice but monkeysDd-o tri - is replaced by RR; ALK is a c1-8 derivative or non derivative tar, alkn C2-8, C2-8 tar or C3-8 cyclopentadiene, optionally in monomer form,Say...O tri - replaced by a selected alternative independent of: Oh, - oal quilo C1-6, - or C3-6, - CN, - NO2, - n (RA) Rb (where R and Rb are selected independent of H, C1-6 tar or alquenilo c2-6),-(C = O) n (RA) Rb, - (n-rc) CORC, - (n-rc) SO2 C1-6 tar (RC is h or C1-6 tar),-(C = O) C 1-6 tar, - (s = (o) d) - C1-6 tar (D is selected from 0, 1 or 2);-So2n (RA) Rb -, ScF3, Halo -, CF3 -, ocf3 -, COOH and coo tar C1-6; CYC is h, or carbon ring, heterocycle, arilo or heterocycle selected from the following groups:Replace - oalquileno c1-4o in adjacent carbon - or RQ or di- (CH2) 2-3NH-,- (CH2) 1-2NH (CH2) --(CH2) 2-3n (C1-4 tar) - O - (CH2) 1-2n (C1-4 tar) (CH2) -;RQ is selected from a group consisting of - Oh, C1-6, oal quilo C1-6, cycloquilo C3-6, cycloquilo C3-6, fenilo, ofenio, bencilo, obencio, CN, NO2, n (RA) Rb (in this group, RA and Rb can be selected separately with n as h, C1-6 or alquenilo c2-6, or RA and Rb as carbonate rings). In contrast, C-ring has 5 to 7 members, with optional carbon replaced by or, = nU. NH O n (C1-4 tar)Choose a carbon replacement - Oh, and an optional one or two unsaturated links in the ring,-(C = O) n (RA) Rb, - (n-rc) CORC, - (n-rc) SO2 C1-6 tar (in the same substitute, RC is h or C1-6 tar or 2 RC), which can be combined with Amida to form a carbonated water / flow crystal with 4-6 members,-N - (SO2 C1-6) 2, - (C = O) C1-6 tar, - (s = (o) d) - C1-6 tar (d selected from 0, 1 or 2),-So2n (RA) Rb -, ScF3, Halo -, CF3 -, ocf3 -, COOH and coo tar C1-6; two carbon members are composed of three carbon atoms, forming five carbon aromatic rings, the rest is replaced by carbon atoms; O, s, NH N (C1-4 tar) and other residues up to one additional carbon atom, optionally from - n=Optional simplex merging ringDi-o tri - is replaced by RQ; triphenyl, combined with other carbides of 4 members, becomes two carbon members of cyclic carbon, forming a combined aromatic ring of 6 members, and the rest part contains one or two carbon atoms, composed of - n =,Optional simplex merging ringChange di-o tri - to RQ; IV) naftyl, and select monomer -,Di-o tri replaced with RQ; V) a single cycle aromatic hydrocarbon compound with five atoms on the ring, the carbon atom of which is the polymerization point, replaced by the carbon atom; O, gt, s, gt, NH gt, n (C1-4 tar),It even has an extra C atom that is - n=The optional monomer or di form, which is replaced by RQ and benzodiazepine fusion or pyridan, is optionally combined in two adjacent C atoms, and the rest benzodiazepine fusion or pyridiene fusion,Whatever you want, monkeySay...O tri -- replace with RQ; VI) a single cycle aromatic compound, in which there are six atoms in the ring, and the carbon atom is the polymerization point, replaced by - n =;The optional monomer or di form, which is replaced by RQ and benzodiazepine fusion or pyridan, is optionally combined in two adjacent C atoms, and the rest benzodiazepine fusion or pyridiene fusion,optionally, mono- or di-substituted with Rq; vii) a 3-8 membered non-aromatic carbocyclic or heterocyclic ring, said ring having 0, 1 or 2 non-adjacent heteroatomic members selected from O, S, -N =,NRQ, which has 0, 1 or 2 unsaturated links, 0, 1 or 2 carbonated carbide members, and optionally 1 to 5 carbonated bridge members, can selectively convert 0 to 5 RQ and benzo fusion or Pyr polycondensation into two adjacent C atoms, and the rest benzo diazepine fusion or Pyr polycondensation It has 0, 12 or 3 RQ substitutes; and (8) a 4-7 member aromatic free carbon ring or heterocyclic ring, from O, s, n=NQ, with 0, 1 or 2 unsaturated links, with 0, 1 or 2 carbonated carbon members, as an option, with a carbonated member forming a bridge, Forming a saturated link in two adjacent C atoms, or forming a C and N atoms, or forming a saturated link, with a carbon ring or heterocyclic ring of 4-7 members, with 0 or 1 possible additional heteroatom member, not in the cyclic alliance, from O, s, n =, NH or NRq, having 0, 1 or 2 unsaturated bonds, having 0, 1 or 2 carbon members that are a carbonyl and having the fused rings 0 to 5 substituents Rq; R1 is selected from the group consisting of H, C1-7 alkyl, C2-7 alkenyl, C2-7 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-7 alkyl, C3-7 cycloalkenyl, C3-7 cycloalkenyl-C1 alkyl -7 and C4-7benzo-fused cycloalkyl, each optionally mono-,Say...O tri - is changed to RP; RP is selected from a group consisting of - oh-oalkilo c1-6-cyclopropyllo C3-6 - or cyclopropyllo c3-6-cn-n2-phenyl, pyridine, Tianjin, furan, pyridyllio-n (RS) Ru (in which RS and Ru are independently selected from H or C1-6 tar, or can be combined with n as a whole carbonate compound). Convection change, ring has 5 to 7 members, optional carbon is replaced by or, = n,U. S. NH O n (C1-4 tar), optionally with one or two unsaturated links in the ring,-(C = O) n (RS) Ru, - (n-rv) CorV, - (n-rv) SO 2 C1-6 tar (RV is h or C1-6 tar or 2 RV in the same substitute), which can be used together with alliance amide to form a carbonated water exchange carnivorous ring with 4-6 members,-(C = O) C 1-6 tar, - (s = (o) n) - C1-6 tar (select 0, 1 or 2 from it),-So2n (RS) Ru -, ScF3, Halo -, CF3 -, ocf3 -, COOH and cooquilo C1-6, in which the above alternatives of phenyl, pyridine, Tianjin, furan and pyrrolene are in form.