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    • 1. 发明授权
    • Stilbene derivatives
    • 二苯乙烯衍生物
    • US5250562A
    • 1993-10-05
    • US829666
    • 1992-02-03
    • Michael KlausPeter MohrEkkehard Weiss
    • Michael KlausPeter MohrEkkehard Weiss
    • C07C211/10C07C317/18C07C323/12C07C323/25C07D295/092C07D295/13A61K31/40C07D207/06
    • C07D295/088C07C211/10C07C317/18C07C323/12C07C323/25C07D295/13C07C2102/08C07C2102/10
    • Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.
    • 式Ⅰ的化合物,其中R 1和R 2各自独立地为低级烷基; 或一起是直链中具有3-5个C原子的亚烷基; 残基R3和R4之一是氢,另一个是氢或低级烷基; R6和R7是氢或低级烷基; R5和R8是氢,低级烷基,低级烷氧基或卤素; X表示-O - , - S - , - SO - , - SO 2 - 或-NR 9; R9是氢,低级烷基或酰基; Y是-S(O)m R 10或-NHet,且其中X是-NR 9 - , - S - , - SO-或-SO 2 - ,以及-N(R 11)2或-OR 12; R10为低级烷基; R 11和R 12是氢,低级烷基或酰基; -NHet是通过N-原子连接的5-8元饱和或不饱和的单环杂环; n为2,3或4,m为0,1或2。 式I的化合物可用作治疗诸如赘生物,皮肤病或皮肤老化的病症的药剂。
    • 3. 发明授权
    • Tetrahydronaphthalene and indane derivatives
    • 四氢萘和茚满衍生物
    • US4876349A
    • 1989-10-24
    • US72075
    • 1987-07-10
    • Michael KlausEkkehard Weiss
    • Michael KlausEkkehard Weiss
    • A61K31/33A61K31/425A61K31/426A61K31/44A61K31/4402A61K31/4406A61K31/4409A61K31/4418A61K31/496A61K31/505A61P17/00A61P29/00A61P35/00A61P37/08C07D213/16C07D233/58C07D233/64C07D239/26C07D261/08C07D263/32C07D277/22C07D307/36C07D333/08
    • C07D213/16C07D239/26C07D307/36C07D333/08
    • The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >Co, >CR.sup.8 OR.sup.7 , --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.8 can be the same or different from one another.are useful for the treatment of neoplasms and dermatoses in mammals. The compounds can be manufactured from a corresponding bicyclic component and a heterocyclic component containing the residue R.sup.1 by a Wittig, Horner or Grignard reaction and the optional subsequent transformation of reactive groups.
    • 下式的化合物其中X和Y独立地是-CH 2 - 或> C(CH 3)2; Z是-CHR8-,> Co,> CR8 OR7,-CHR8-CHR8 + 13,-CHOR7-CH2-,-CO-CHOR7或-CHOR7-CHOR7-R1是5-或6-元单环杂环基,其中 任选地可以被卤素,低级烷基,低级烷氧基,酰氧基,硝基,羟基,氨基,低级烷基氨基或二 - 低级 - 烷基氨基和/或可以被低级烷基氨基取代的环-NH-基团上C -烷基; R2和R3独立地是氢,低级烷基,三氟甲基或卤素,R2和R3之一总是三氟甲基或低级烷基; R4和R5独立地是氢,烷基,烷氧基或卤素; R6是氢,低级烷基或-OR7; R7是氢,低级烷基或酰基; R8是氢或低级烷基; 并且R 7和R 8可以相同或不同。 可用于治疗哺乳动物的肿瘤和皮肤病。 化合物可以由对应的双环组分和含有残基R1的杂环组分通过Wittig,Horner或Grignard反应和任选的随后的反应性基团的转化来制备。
    • 7. 发明授权
    • Tetrahydronaphthalene and indane derivatives
    • 四氢萘和茚满衍生物
    • US5084476A
    • 1992-01-28
    • US395005
    • 1989-08-17
    • Michael KlausEkkehard Weiss
    • Michael KlausEkkehard Weiss
    • C07D213/16C07D239/26C07D307/36C07D333/08
    • C07D213/16C07D239/26C07D307/36C07D333/08
    • The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >CO, >CR.sup.8 OR.sup.7, --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --; R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.8 can be the same or different from one another,are useful for the treatment of neoplasms and dermatoses in mammals. The compounds can be manufactured from a corresponding bicyclic component and a heterocyclic component containing the residue R.sup.1 by a Wittig, Horner or Grignard reaction and the optional subsequent transformation of reactive groups.
    • 下式的化合物其中X和Y独立地是-CH 2 - 或> C(CH 3)2; Z是-CHR8-,> CO,> CR8OR7,-CHR8-CHR8-,-CHOR7-CH2-,-CO-CHOR7或-CHOR7-CHOR7-; R 1是任选地可以被卤素,低级烷基,低级烷氧基,酰氧基,硝基,羟基,氨基,低级烷基氨基或二低级烷基氨基和/或低级烷基氨基取代的5-或6-元单环杂环基, 或者可以被低级烷基取代在环-NH-基上; R2和R3独立地是氢,低级烷基,三氟甲基或卤素,R2和R3之一总是三氟甲基或低级烷基; R4和R5独立地是氢,烷基,烷氧基或卤素; R6是氢,低级烷基或-OR7; R7是氢,低级烷基或酰基; R8是氢或低级烷基; 并且R7和R8可以相同或不同,可用于治疗哺乳动物的肿瘤和皮肤病。 化合物可以由对应的双环组分和含有残基R1的杂环组分通过Wittig,Horner或Grignard反应和任选的随后的反应性基团的转化来制备。
    • 10. 发明授权
    • Stilbene derivatives
    • 二苯乙烯衍生物
    • US5378705A
    • 1995-01-03
    • US102609
    • 1993-08-05
    • Michael KlausPeter MohrEkkehard Weiss
    • Michael KlausPeter MohrEkkehard Weiss
    • C07C211/10C07C317/18C07C323/12C07C323/25C07D295/092C07D295/13A61K31/38C07D279/12
    • C07D295/088C07C211/10C07C317/18C07C323/12C07C323/25C07D295/13C07C2102/08C07C2102/10
    • Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.
    • 式Ⅰ的化合物,其中R 1和R 2各自独立地为低级烷基; 或一起是直链中具有3-5个C原子的亚烷基; 残基R3和R4之一是氢,另一个是氢或低级烷基; R6和R7是氢或低级烷基; R5和R8是氢,低级烷基,低级烷氧基或卤素; X表示-O - , - S - , - SO - , - SO 2 - 或-NR 9; R9是氢,低级烷基或酰基; Y是-S(O)m R 10或-NHet,且其中X是-NR 9 - , - S - , - SO-或-SO 2 - ,以及-N(R 11)2或-OR 12; R10为低级烷基; R 11和R 12是氢,低级烷基或酰基; -NHet是通过N-原子连接的5-8元饱和或不饱和的单环杂环; n为2,3或4,m为0,1或2。 式I的化合物可用作治疗诸如赘生物,皮肤病或皮肤老化的病症的药剂。