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    • 52. 发明申请
    • 3-SUBSTITUTED PYRIDO[4',3':4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE
    • 3-取代的吡啶并[4”,3' :4,5]噻吩并[2,3-d]嘧啶DERIV ATE,其生产和使用
    • WO1998011110A1
    • 1998-03-19
    • PCT/EP1997004593
    • 1997-08-22
    • BASF AKTIENGESELLSCHAFTSTEINER, GerdLUBISCH, WilfriedBACH, AlfredEMLING, FranzWICKE, KarstenTESCHENDORF, Hans-JürgenBEHL, BertholdKERRRIGAN, FrankCHEETHAM, Sharon
    • BASF AKTIENGESELLSCHAFT
    • C07D495/14
    • C07D495/14
    • The invention concerns 3-substituted 3,4,5,6,7,8-hexahydro-pyrido[4,3':4,5]thieno-[2,3-d]pyrimidine derivatives of formula (I) in which: R designates a hydrogen atom, a C1-C4 alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 group - the aromatic optionally being substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups - a naphthylalkyl C1-C3 group, a phenylalkanone C2-C3 group or a phenylcarbamoylalkyl C2 group, wherein the phenyl group can be substituted by halogen; R designates a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which can optionally be mono-, di- or tri-substituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and can optionally be anellated with a benzene nucleus, which can optionally be mono- or di-substituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and can optionally contain 1 nitrogen atom, or with a 5- or 6-member ring which can contain between 1 and 2 oxygen atoms, or can be substituted by a phenyl-C1-C2 alkyl or alkoxy group, wherein the phenyl group can be substituted by halogen, a methyl, trifluoromethyl or methoxy group; A designates NH or an oxygen atom; B designates hydrogen or methyl; C designates hydrogen, methyl or hydroxy; X designates a nitrogen atom; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z designates a nitrogen atom, a carbon atom or CH, wherein the bond between Y and Z can also be a double bond; and n is the number 2, 3 or 4, and their physiologically compatible salts. These compounds are suitable as medicaments for treating diseases in which the serotonin concentration is reduced and in which the activity of the presynaptic receptors 5-HT1B, 5-HT1A, 5HT1D is to be blocked within a therapeutic context without greatly influencing other receptors. Such diseases include, for example, depression.
    • 3-取代的3,4,5,6,7,8 - 六氢吡啶并[4”,3' :4,5]噻吩并[2,3-D]式的嘧啶衍生物(I),其中R < 1>是一个氢原子,一个C1-C4烷基,乙酰基或苯甲酰基,苯基烷基C1-C4烷基,与芳族任选被卤素取代的,C1-C4烷基,三氟甲基,羟基,C1-C4烷氧基 ,氨基,氰基或硝基,一个萘基烷基C1-C3烷基,一个phenylalkanone C2-C3烷基,或C2 Phenylcarbamoylalkyl基团,其中所述苯基可以被卤素取代,R <2>是任选由 卤原子,C1-C4烷基,三氟甲基,三氟甲氧基,羟基,C1-C4烷氧基,氨基,单甲基,二甲基氨基,氰基或硝基,单 - ,二 - 或三 - 取代的苯基,吡啶基,嘧啶基 表示或吡嗪基任选地被一个苯核,任选地被卤素原子,C1-C4烷基,羟基,三氟甲基取代的被取代的,C1-C4烷氧基,氨基,氰基或硝基单声道 - - 可能是或二取代,并且可以含有1个氮原子,在适当情况下,或者可以与5或6元环,该环可含有1-2个氧原子,或由苯基C1-C2烷基或烷氧基是稠合的 基团可以被取代,其中卤素基团苯基,甲基,三氟甲基或甲氧基可被取代,A表示氧原子或NH,B代表氢或代表甲基,C是氢,甲基或羟基,X表示氮原子, ÿCH2,CH2-CH2,CH2-CH2-CH2或CH2-CH,Z表示氮原子,碳原子或CH,其中Y和Z之间的键也可以是双键,且n是数字2,3或4; 以及它们的生理学可接受的盐。 这些化合物作为药物的疾病状态,其中所述血清素浓度降低,并且其中一个治疗靶向突触前受体5-HT1B,5-HT1A的活动的一个部分,想阻断5-HT 1D没有其他受体的治疗有用 强烈影响。 这样的疾病状态,例如抑郁症。