分享好友 知识库首页 频道列表

HETEROCYCLIC ANTAGONISTS WITH CONNECTION N OF THE RECEIVER P2Y1, EQUIPMENT IN THE TREATMENT OF AFFE

2025-06-18 19:194320下载
文件类型:PDF文档
文件大小:5458K
A compound of Formulates (1) : or a estereoisomero, tautomer, salt or pharmaceutically acceptable solvate of the same, in which : the ring To is C6-10 seed coat replaced with 0-5 R1, or heterociclo of 5 to 10 members that include/understand : carbon atoms and 1-4 heteroatoms selected between N, NR11, Or and S (Or) p, in which said heterociclo this replaced with 0-5 R1; ring B is C6-10 seed coat replaced with 0-4 R7 or heteroarilo of 5 10 members that include/understand : carbon atoms and 1-4 heteroatoms in the ring selected between N, NR11, N→O, S (Or) p and Or, in which said heteroarilo this replaced with 0-4 R7; replaced ring D this with 0-5 R6a and is selected between : 107 in that D1 is carbociclo of 5 to 7 members or heterociclo of 5-6 members that include/understand : carbon atoms and 0-3 heteroatoms in the ring selected between N, NR11, Or and S (Or) p, and 0-2 groups carbonilo and 0-3 double bonds; NR18 W is, Or, S, - NHCOCH=CH-, - NHCO2CH2-, - NHCON (Me) -, - NHCOCH2NH-, - NHCOCH (Me) -, - NHCOCH2CONH-, - NHCH2-, - NHCH2CH2CH2-, - NHSO2-, - NHSO2NH-, - NHSO2CH2-, - NHSO2CH=CH-, - NHCONHNHCO-, - CH2CONH-, R1 are, independently in each appearance, =O F, CL, Br, I, CF3, - CF2CF3, OCF3, - OCF2CF2H, - OCF2CF3, SiMe3, - (CRfRf) rORc, SRc, Cnn, NO2, - (CRfRf) rNR12R13, - (CRfRf) rC (Or) Rc, - (CRfRf) rCO2Rc, - (CRfRf) rC (Or) NR12R13, - C (Or) NR14 (CRfRf) tN12R13, - (CRfRf) rOC (Or) NR12R13, - (CRfRf) rNR14C (Or) NR12R13, - (CRfRf) rNR14C (Or) Rd - (CRfRf) rNR14C (Or) ORh, - NR14 (CRfRf) nC (Or) Rd, - NR14CO (CRfRf) nORc, - (CH2) rCR13 (=NORc), - (CH2) rC (NH2) (=NORc), - S (Or) pNR12R13, - (CRfRf) rNR14S (Or) pNR12R13, - NR14SO2CF3, - NR14S (Or) pRd, - S (Or) 2CF3, - S (Or) Rd, - S (Or) 2Rd, - OP (U) (OEt) 2, - (CH2) 2OP (U) (OEt) 2, - N (C1-4 alkyl) 3 +Cl -, 4, 4, 5, 5-tetrametil-1, 3, 2-dioxaborolanilo, C1-8 alkyl replaced with 0-2 Ra, alquenilo C2-8 replaced with 0-2 R8, alquinilo C2-8 replaced with 0-2 Ra, - (CRfRf) r-carbociclo C3-13 replaced with 0-5 Rb or - (CRfRf) r-heterociclo of 5 10 members that include/understand : carbon atoms and 1-4 heteroatoms selected between N, NR11, Or and S (Or) p, in which said heterociclo this replaced with 0-5 Rb; like alternative, two R1 in two adjacent carbon atoms are combined with the carbon atoms to which they estan united, form carbociclo or heterociclo of 5 to 10 members that include/understand : carbon atoms and 0-3 selected heteroatoms but between N, NR11, Or and S (Or) p and 0-2 groups carbonilo, in which said carbociclo or heterociclo this replaced with 0-4 Rb; R6a is, independently in each appearance, =O, F, CL, Br, I, - (CRiRi) r-ORc, SRc, Cnn, NO2, CF3, OCF3, - CF2CF3, - OCF2CF2H, - OCF2CF3, - (CRfRf) r-NR12R13, - C (Or) Rc, - (CRfRf) rC (Or) ORc, - (CRfRf) rC (Or) NR12R13, - (CRfRf) r-NR14C (Or) Rd, - S (Or) pNR12R13, - S (Or) Rd, - S (Or) 2Rd, If (Me) 3, If (C1-4 alkyl) 3, haloalquilo C1-4, haloalquiloxi C1-4-, alquiloxi C1-4-, alquiltio C1-4-, alquil C1-C4-C (Or) -, alquil C1-4-O-C (Or) -, alquil C1-4-C (Or) NH-, C1-8 alkyl replaced with 0-1 Ra, alquenilo C2-8 replaced with 0-1 Ra, alquinilo C2-8 replaced with 0-1 Ra, - (CRfRf) r-carbociclo C3-10 replaced with 0-2 Re or - (CRfRf) r-heterociclo of 5 10 members that include/understand : carbon atoms and 1-4 heteroatoms selected between N, NR11, Or and S (Or) p, in which said heterociclo this replaced with 0-2 Re; like alternative, when two R6a groups estan united to the same atom of carbon or silicon atom, along with the atom of carbon or silicon atom to which they estan united, form a carbociclico or heterocyclic ring of 3 to 7 members that include/understand : carbon atoms and 0-3 heteroatoms selected between N, NR11, Or, If and S (Or) p, 0-1 carbonilo and 0-3 double bonds of the ring, in which this carbociclico ring or heterocyclic this replaced with 0-3 Rb; like alternative, when two R6a groups estan united to adjacent atoms, along with the atoms to which they estan united form a carbociclico or heterocyclic ring of 5 to 7 members that include/understand : carbon atoms and 0-2 heteroatoms selected between N, NR11, Or, If and S (Or) p, 0-1 carbonilo and 0-3 double bonds of the ring, in which this carbociclico ring or heterocyclic this replaced with 0-3 Rb; R7 is, independently in each appearance, H, =O F, CL, Br, I, OCF3, CF3, ORc, SRc, Cnn, NO2, - NR12R13, - C (U) Rc, - C (Or) ORc, - C (Or) NR12R13, - NR14C (Or) Rd, - S (Or) pNR12R13, - S (Or) Rd, - S (Or) 2Rd, C1-8 alkyl replaced with 0-2 Ra, alquenilo C2-8 replaced with 0-2 Ra, alquinilo C2-8 replaced with 0-2 Ra, - (CRfRf) r-carbociclo C3-10 replaced with 0-3 Rb or - (CRfRf) r-heterociclo of 5 to 10 members that include/understand : carbon atoms and 1-4 heteroatoms selected between N, NR7b, Or and S (Or) p, in which said heterociclo this replaced with 0-3 Rb; like alternative, two R7 in two adjacent carbon atoms form a carbociclico or heterocyclic ring of 5 to 7 members that include/understand : carbon atoms and 0-3 heteroatoms in the ring selected enter Or, N, NR7b and S (Or) p, in which this carbociclico ring or heterocyclic this replaced with 0-2 R7c; R7b is H, C1-4 alkyl, - C (U) (C1-4 alkyl), - C (Or) phenyl, - C (Or) bencilo or bencilo; R7c is, independently in each appearance, H, F, CL, Br, I, OCF3, CF3, ORc, SRc, Cnn, NO2, - NR12R13, - C (Or) Rc, - C (Or) ORc, - C (Or) NR12R13; - NR14C (Or) Rd. - S (Or) pNR12R13, - S (Or) Rd, - S (Or) 2Rd, C1-4 alkyl, phenyl replaced with 0-3 Rb or bencilo replaced with 0-3 Rb; R11 is, independently in each appearance, H, alcoxi C1-4, C1-6 alkyl replaced with 1-5 fluorine, - (CRfRf) rC (Or) NR12R13, C1-8 alkyl replaced with 0-2 Ra, alquenilo C2-4 replaced with 0-1 Ra, alquinilo C2-4 replaced with 0-1 Ra, - C (U) (C1-6 alkyl), - C (O) (CH2) n (cicloalquilo C3-6), - C (O) (CH2) n (C6-10 seed coat), - C (O) (CH2) n (heteroarilo of 5 to 10 members), - C (Or) Or (C1-8 alkyl), - C (Or) Or(CH2) n (cicloalquilo C3-6), - C (Or) O (CH2) n (C6-10 seed coat), - C (Or) O (CH2) n (heteroarilo of 5 to 10 members), - C (Or) O (CH2) 2-4 (C1-4 alkyl), - C (Or) NH (C1-8 alkyl), - C (Or) NH (CH2) n (cicloalquilo C3-6), - C (Or) NH (CH2) n (C6-10 seed coat), - C (Or) NH (CH2) n (heteroarilo of 5 to 10 members), - S(Or) 2 (C1-8 alkyl), - S (Or) (2 CH2) n (cicloalquilo C3-6), - S (Or) (2 CH2) n (C6-10 seed coat), - S (Or) (2 CH2) n (heteroarilo of 5 to 10 members), - (CRfRf) r-carbociclo C3-10 or - (CRfRf) r-heterociclo of 5 to 10 members; in that this alkyl, cicloalquilo, seed coat and carbociclo estan replaced with 0-2 Rb, and said heteroarilo and heterociclo they estan replaced with 0-2 Rb and they include/understand : carbon atoms and 1-4 heteroatoms selected between N, NRf, Or and S (Or) p; R12 is, independently in each appearance, H, C1-6 alkyl replaced with 1-5 fluorine, - (CRfRf) rC (Or) NRfRf, C1-6 alkyl, - C (U) (C1-6 alkyl), - C (O) (CH2) n (C6-10 seed coat), - C (O) (CH2) n (heteroarilo of 5 to 10 members), - C (Or) Or (C1-4 alkyl), - C (Or) OCH2 (C6-10 seed coat), - (CH2) nC (Or) OCH2 (heteroarilo of 5 to 10 members), - (CH2) NOC (U) (C1-4 alkyl), - (CH2) NOC (U) (C6-10 seed coat), - (CH2) NOC (U) (heteroarilo of to 10 members), - (CH2) nC (Or) Or (C1-4 alkyl), - (5 CH2) nC (Or) Or (C6-10 seed coat), - (CH2) nC (Or) Or (heteroarilo of 5 to 10 members), - (CH2) nC (Or) NH (C1-6 alkyl), - (CH2) nC (Or) NH (C6-10 seed coat), - (CH2) nC (Or) NH (heteroarilo of 5 to 10 members), - (CH2) tOC (Or) NH (C1-6 alkyl), - (CH2) tOC (Or) NH (C6-10 seed coat), - (CH2) tOC (Or) NH (heteroarilo of 5 to 10 members), - S (Or) 2 (c1-6 alkyl), - S (Or) (2 CH2) n (C6-10 seed coat), - S (Or) (2 CH2) n (heteroarilo of to 10 members), - (CRfRf) n (C6-10 seed coat), or - (5 CRfRf) nheteroarilo of 5 to 10 members; in that this alkyl and seed coat estan replaced with 0-2 Rg; and said heteroarilo this replaced with 0-2 Rg and it includes/understands : carbon atoms and 1-4 heteroatoms selected between N, NR11, Or and S (Or) p; R13 is, independently in each appearance, H, C1-6 alkyl; or - (CH2) n-phenyl; like alternative, R12 and R13, when they estan united to the same nitrogen, are combined to form a heterocyclic ring of 5 to 10 members that include/understand : carbon atoms and 1-2 selected heteroatoms but between N, NR11, Or and S (Or) p; R14 is, independently in each appearance, H, C1-6 alkyl replaced with 0-2 R14a, alquenilo C2-6 replaced with 0-2 R14a, alquinilo C2-6 replaced with 0-2 R14a, - (CH2) rcarbociclo C3-10 replaced with 0-3 Rg, or - (CH2) rheterociclo of 5 to 10 members that include/understand : carbon atoms and 1-4 heteroatoms selected between N, NR11, Or and S (Or) p, in which said heterociclo this replaced with 0-3 Rg; R14a is, independently in each appearance, H, C1-4 alkyl, ORf CL, F, Br, I, =O, CF3, Cnn, NO2, NR12R13, - C (U) RF - C (Or) ORf, - C (Or) NR12R13 or - S (Or) pRf; R16 is, independently in each appearance, H, F, C1-6 alkyl replaced with 0-2 Ra, alquenilo C2-6 replaced with 0-2 Ra, alquinilo C2-6 replaced with 0-2 Ra or - (CH2) r-phenyl replaced with 0-2 Rb; R17 is, independently in each appearance, H, OH, C1-6 alkyl or - (CH2) n-phenyl; like alternative, R16 and R17 in the same carbon atom are combined to form a carbociclico or heterocyclic ring of 3 to 7 members that include/understand : carbon atoms and 0-2 heteroatoms selected between N, NR11, Or and S (Or) p, 0-1 carbonilo and 0-3 double bonds, in which this carbociclico ring or heterocyclic this replaced with 0-2 Rb; like alternative, two R16 groups in the adjacent atoms are combined to form a carbociclico or heterocyclic ring of 3 to 7 members that include/understand : carbon atoms and 0-2 heteroatoms selected between N, NR11, Or and S (Or) p, 0-1 carbonilo and 0-3 double bonds, in which this carbociclico ring or heterocyclic this replaced with 0-2 Rb; R18 is H, C1-6 alkyl replaced with 0-2 Ra, alquenilo C2-6 replaced with 0-2 Ra, alquinilo C2-6 replaced with 02 Ra, - C (Or) Rc, - C (Or) ORc, - C (Or) NR12R13, - S (Or) 2Rh, - S (Or) 2NR12R13, - (CH2) r-carbociclo C3-10 replaced with 0-3 Rb or - (CH2) r-heterociclo of 5 10 members that include/understand : carbon atoms and 1-4 heteroatoms selected between N, Or and S (Or) p and replaced with 0-3 Rb; Ra is, independently in each appearance, H, =O, F, OCF3, CF3, - (CRfRf) rORc, - (CRfRf) rSRc, Cnn, - (CRfRf) rNR12R13, - (CRfRt) rC (Or) Rc, - (CRfRf) rC (Or) ORc, - (CRfRf) rC (Or) NR12R13, - (CRfRf) rNR14C (Or) Rd, - (CRfRf) RS (Or) pNR12R13, - (CRfRf) RS (Or) Rd, - (CRfRf) RS (Or) 2Rd, C1-4 alkyl replaced with 1


请登录查看


反对 0
举报 0
收藏 0
打赏 0
评论 0