首页> 外国专利> DERIVATIVES OF DIHYDROPIRROLO-1,2-AIINDOL AND TETRAHYDROPIRIDE -1,2-AIINDOL AS ANTAGONISTS OF PROSTAGLANDIN RECEPTORS D2.

DERIVATIVES OF DIHYDROPIRROLO-1,2-AIINDOL AND TETRAHYDROPIRIDE -1,2-AIINDOL AS ANTAGONISTS OF PROSTAGLANDIN RECEPTORS D2.

机译:作为前列腺素受体D2的拮抗剂的二氢吡咯烷-1,2-艾吲哚和四氢吡喃酯-1,2-艾吲哚的衍生物。

摘要

A compound having the ** formula ** and pharmaceutically acceptable salts and hydrates thereof, in which: R1, R2 and R3 are each independently selected from hydrogen and Rg; R4 is selected from H, CN, (C1-6) alkyl optionally substituted by one to six halogen, ORa and S (O) n ((C1-6) alkyl); R5 is selected from H and (C1.6) alkyl optionally substituted by one to six halogens; or R4 and R5 together represent an oxo; or R4 and R5 taken together form a 3 or 4 member ring containing 0 or 1 heteroatom selected from NRf, S and O optionally substituted by one or two groups selected from F, CF3 and CH3; R6 is selected from H and (C1.6) alkyl optionally substituted by one to six groups independently selected from ORa and halogen, Ar is aryl or heteroaryl each optionally substituted by one to four groups independently selected from Rg; A is (C1-3) alkyl optionally substituted by one to four halogen atoms, O (CH2) 1-2, S (CH2) 1-2; Q is selected from: (1) COOH, (2) CONRaRb, (3) C (O) NHSO2Rc, (4) SO2NHRa, (5) SO3H, (6) PO3H2 and (7) tetrazolyl, Y1 is ¿(CRdRe) a ¿X¿ (CRdRe) b¿, phenylene, cycloalkylidene (C3¿6) or cycloalkylene (C3¿6), a and b being whole numbers 0¿1 such that the sum of a and b is equal to 0, 1 or 2; X is a bond, O, S, NRa, C (O), OC (O), C (O) O, C (O) NRa, OC (O) NRa, NRaC (O), CRd = CRe or C = C; Y2 is CRdRe, CRdRe¿CRdRe or CRd = CRe.
机译:具有**式**的化合物及其药学上可接受的盐和水合物,其中:R 1,R 2和R 3各自独立地选自氢和R g; R4选自任选被1至6个卤素取代的H,CN,(C1-6)烷基,ORa和S(O)n((C1-6)烷基); R5选自H和任选被1至6个卤素取代的(C1.6)烷基;或R 4和R 5一起表示氧代;或者R4和R5一起形成3或4元环,其含有0或1个选自NRf,S和O的杂原子,所述杂原子任选地被选自F,CF3和CH3的一个或两个基团取代; R6选自H和(C1.6)烷基,其任选地被1-6个独立地选自ORa和卤素的基团取代; Ar是芳基或杂芳基,其各自任选地被1-4个独立地选自Rg的基团取代; A为任选被1-4个卤素原子取代的(C1-3)烷基,O(CH2)1-2,S(CH2)1-2; Q选自:(1)COOH,(2)CONRaRb,(3)C(O)NHSO2Rc,(4)SO2NHRa,(5)SO3H,(6)PO3H2和(7)四唑基,Y1为((CRdRe)) a'X'(CRdRe)b ?、亚苯基,亚环烷基(C3-6)或亚环烷基(C3-6),a和b为整数0?1,因此a和b的总和等于0、1或2; X是一个键,O,S,NRa,C(O),OC(O),C(O)O,C(O)NRa,OC(O)NRa,NRaC(O),CRd = CRe或C = C; Y2是CRdRe,CRdRe¿CRdRe或CRd = CRe。

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