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    • 5. 发明申请
    • SUBSTITUTED CYCLOALKANECARBOXYLIC ACID DERIVATIVES, THEIR PREPARATION AND USE AS ENDOTHELIN ANTAGONISTS
    • 取代环烷酸衍生物,生产与应用,内皮素拮抗剂
    • WO1995015944A1
    • 1995-06-15
    • PCT/EP1994003914
    • 1994-11-26
    • BASF AKTIENGESELLSCHAFTALBRECHT, Hans-PeterBÖHM, Hans-JoachimRASCHACK, ManfredUNGER, LilianeWERNET, Wolfgang
    • BASF AKTIENGESELLSCHAFT
    • C07D209/18
    • C07C205/56C07C62/06C07C62/18C07C62/38C07C69/757C07C229/46C07C229/50C07C235/34C07C2602/28C07D209/18
    • The invention describes compounds of formula (I), where A is an oxygen atom or a NH group; B is the radical -Zm-(CHQ)p-(CH=CH)q-(CH2)r-P, where Z is a -CO- group or -SO2-group, m is 0 or 1, p is 0, 1 or 2, q is 0, 1 or 2, r is 0, 1 or 2, Q is a hydrogen atom, a C1-4 alkyl radical, a carboxyl-, carboxamido- or carboxy-C1-4 alkyl group, and P is a hydrogen atom, an indolyl radical, or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkyl groups, and/or a C1-2 alkylenedioxy group; D is an amino-, hydroxy-, C1-4 alkoxy, C1-4 alkylamino-, aryl-C1-4 alkylenoxy- or aryl-C1-4 alkyleneamino, where the aryl radicals represent a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group; X is a C1-4 alkyl radical or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group; Y is a hydrogen atom, a C1-4 alkyl radical or a phenyl radical possibly substituted by 1-3-C1-4 alkyl radicals, halogen atoms, trifluoromethyl-, hydroxy-, C1-4 alkoxy-, C1-4 acyloxy-, amino-, C1-5 acylamino-, sulfonamido-, nitro-, C1-5 acyl-, carboxyl- or thio-C1-4 alkylene groups and/or a C1-2 alkylenedioxy group, or X and Y together represent a -(CH2)s group, where s is 3, 4 or 5, and 1 or 2 hydrogen atoms can be replaced by methyl groups, and n is 0 or 1, and possibly their salts with physiologically tolerable acids and bases. The compounds can be used to combat diseases.
    • 有式(I),其中A是氧原子或NH基团的发明中,B是基团-Zm-(CHQ)对 - (CH = CH)Q(CH 2)RP,其中Z是-CO - 或-SO 2基团,m是0或1,p是阿尔0,1或2,q为0,1或2,r是0,1或2,Q是氢原子,C 1-4 烷基,羧基,甲酰氨基,或羧基-C 1-4 - 烷基且P为氢原子或任选地被1-3个C 1-4烷基,卤素原子,三氟甲基,羟基,C 1-4烷氧基,C 1 -C 4-酰氧基,氨基,C 1-5酰氨基,磺酰氨基,硝基,C 1-5酰基,羧基或硫代C 1-4 - 烷基基团和/或C1-2亚烷基二氧基取代的苯基或 代表吲哚基团,D是氨基,羟基,C 1-4 - 烷氧基,C 1-4 - 烷基氨基,芳基-C 1-4 - 亚烷基或芳基-C 1-4亚烷基氨基,其中所述芳基任选被取代的1- 3个C 1-4烷基,卤素原子,三氟甲基,羟基,C 1-4 - 烷氧基,C 1-4 - 酰氧基,氨基,C 1-5酰氨基,磺 namido-,硝基,C 1-5酰基,羧基或硫代C1-4亚烷基基团和/或C 1-2 - 亚烷基二氧基取代的苯基,X表示C 1-4 - 烷基或任选被1个 -3 C 1-4烷基,卤素,三氟甲基,羟基,C 1-4烷氧基,C 1-4酰氧基,氨基,C 1-5酰氨基,磺酰氨基,硝基,C1-5- 亚烷基硫基-C 1-4 - 酰基,羧基或和/或亚烷基二C1-2取代的苯基基团,Y表示氢原子,C 1-4烷基或任选地被1-3 C 1-4烷基的基团,卤原子 甲基,三氟甲基,羟基,C 1-4 - 烷氧基,C 1-4 - 酰氧基,氨基,C 1-5酰氨基,磺酰氨基,硝基,C 1-5酰基,羧基或硫代C1 -4 - 亚烷基和/或C 1-2 - 亚烷基二氧基取代的苯基基团,或X和Y一起形成 - (CH 2)平均的小组,其中s是在其通过甲基基团1个或2个氢原子的数目3,4或5个 可以被替换,并且n为数字0或1, 和任选其盐与生理上可接受的酸或碱。 所述化合物适于防治疾病。