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    • 7. 发明授权
    • Glycopeptide derivatives, a process for their preparation and
pharmaceutical agents containing these compounds
    • 糖肽衍生物,其制备方法和含有这些化合物的药剂
    • US5556941A
    • 1996-09-17
    • US291729
    • 1994-08-16
    • Cenek KolarWerner Stuber
    • Cenek KolarWerner Stuber
    • A61K38/00A61P7/02C07K1/113C07K9/00C07K14/81A61K38/14C07K5/072
    • C07K9/003A61K38/00
    • Glycopeptide derivatives, a process for their preparation and pharmaceutical agents containing these compounds N-Glycopeptide derivatives of the formula I ##STR1## where aromatic is an unsubstituted or substituted benzene residue, naphthalene residue, chroman residue, chromene residue or coumarone residue,a is 0 to 5, b is 0 to 4, c is 0 or 1, d is 1 or 2R.sup.1 is (C.sub.1 -C.sub.3)-alkyl,R.sup.2 is (C.sub.1 -C.sub.3)-alkyl or (C.sub.1 -C.sub.3)-alkyloxy,R.sup.3 is H, OH, (C.sub.1 -C.sub.3)-alkyloxy, NH.sub.2, NH-(C.sub.1 -C.sub.6)-alkanoyl, NH-benzoyl, NH--SO.sub.3 H or NH-acyl radical of a natural N-acetylated amino acid,R.sup.4 is H, OH, or (C.sub.1 -C.sub.3)-alkyloxy,R.sup.5 is H, OH, (C.sub.1 -C.sub.3)-alkyloxy, fluorine, chlorine or bromine,R.sup.6 is H, CH.sub.3, CH.sub.2 OH, CH.sub.2 O--(C.sub.1 -C.sub.6), CH.sub.2 NHCOCH.sub.3 or CH.sub.2 NH--SO.sub.3 H,R.sup.5 and R.sup.6 are together O--CH.sub.2 --O--CH.sub.2, --O--CH(CH.sub.3)--O--CH.sub.2 or O--C(CH.sub.3).sub.2 --O--CH.sub.2,R.sup.7 is hydroxy-(C.sub.2 -C.sub.4)-alkyl or (C.sub.2 -C.sub.4)-alkyloxy-(C.sub.2 -C.sub.4)-alkyl,R.sup.8 is H or (C.sub.1 -C.sub.6)-alkyl orR.sup.7 -N-R.sup.8 are together a pyrrolidine ring or piperdine ring or morpholine ring, which can be substituted by HO, HOCH.sub.2, CH.sub.3 or COOH,W is --O--, --CONH-- or --C.sub.6 H.sub.4 --CONH andH-X is HCl, a (C.sub.1 -C.sub.7)-alkanoic acid or another pharmacologically tolerated inorganic or organic acid,are described, as are a process for their preparation and a pharmaceutical agent which contains these novel compounds. These pharmaceuticals can be used in particular for the therapy of thrombotic disorders.
    • 糖肽衍生物,其制备方法和含有这些化合物的药剂N-芳香族是未取代或取代的苯残基,萘残基,苯并二氢吡喃残基,色烯还原或香豆酮残基的式I的N-糖肽衍生物,a为0 (C 1 -C 3) - 烷基或(C 1 -C 3) - 烷氧基,R 3为H,C 1 -C 4烷基, OH,(C 1 -C 3) - 烷氧基,NH 2,NH-(C 1 -C 6) - 烷酰基,NH-苯甲酰基,NH-SO 3 H或NH-酰基自然的N-乙酰化氨基酸,R4is H,OH或( C1-C3) - 烷氧基,R5isH,OH,(C1-C3) - 烷氧基,氟,氯或溴,R6isH,CH3,CH2OH,CH2O-(C1-C6),CH2NHCOCH3或CH2NH-SO3H,R5和R6 在一起是O-CH 2 -O-CH 2,-O-CH(CH 3)-O-CH 2或OC(CH 3)2 -O-CH 2,R 7是羟基 - (C 2 -C 4) - 烷基或(C 2 -C 4) 烷氧基 - (C 2 -C 4) - 烷基,R 8是H或(C 1 -C 6) - 烷基或R 7 -N-R 8一起是可以被HO,HOCH 2,CH 3取代的吡咯烷环或哌啶环或吗啉环, COOH, W是-O - , - CONH - 或-C6H4-CONH,HX是HCl,(C1-C7) - 链烷酸或另一种药理学上耐受的无机或有机酸,以及其制备方法和药物 含有这些新化合物的试剂。 这些药物特别可用于治疗血栓形成障碍。
    • 8. 发明授权
    • Rhodomycins with a modified carbohydrate unit
    • 具有改性碳水化合物单位的罗红霉素
    • US5049549A
    • 1991-09-17
    • US451877
    • 1989-12-18
    • Cenek KolarHans P. KraemerKonrad Dehmel
    • Cenek KolarHans P. KraemerKonrad Dehmel
    • A61K31/35A61K31/351A61K31/70A61K31/7028A61K31/7034A61K31/704A61P31/04C07D309/12C07H15/252
    • C07H15/252Y02P20/55
    • 7-O-Glycosyl-rhodomycins which correspond to the general formula I below ##STR1## in which the radicals have the following meaning: R.sup.1 is a hydrogen atom or a hydroxyl group,R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group,R.sup.3 a hydroxyl group, an O-acyl protective group or the methyloxycarbonyl group,R.sup.4 is a hydrogen atom, an O-acyl protective group, an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group andR.sup.5 is an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group,where acyl protective group denotes an acetyl, mono-, di- or trihalogenoacetyl group with fluorine or chlorine as halogen or the p-nitrobenzoyl group, and a process for the preparation thereof and the use thereof as pharmaceuticals, are described.
    • 对应于以下通式I的7-O-糖基 - rhodomycins,其中基团具有以下含义:R 1是氢原子或羟基,R 2是氢原子或C 1 -C 4 - 烷基,R3为羟基,O-酰基保护基或甲氧基羰基,R4为氢原子,O-酰基保护基,叠氮基,氨基或三氟乙酰氨基,二C1-C4烷基氨基 或氰基甲基氨基,R 5为叠氮基,氨基或三氟乙酰氨基,二-C 1 -C 4 - 烷基氨基或氰基甲基氨基,其中酰基保护基表示具有氟或氯作为卤素的乙酰基,单 - ,二 - 或三卤代乙酰基 或对硝基苯甲酰基及其制备方法及其作为药物的用途。
    • 9. 发明授权
    • Glycopeptides, process for their preparation and their use
    • 糖肽,其制备方法及其用途
    • US4719289A
    • 1988-01-12
    • US776380
    • 1985-09-16
    • Cenek KolarFriedrich R. SeilerUrsula Knodler
    • Cenek KolarFriedrich R. SeilerUrsula Knodler
    • G01N33/53A61K38/00A61K39/00C07K1/113C07K9/00C07K16/00C07K17/02G01N33/543G01N33/574C07K5/06C07H5/04C07K5/08
    • C07K9/005G01N33/57469Y02P20/55
    • Compounds of the general formula I, II or IIIR.sup.1 --A.sup.1 --T--NH--R.sup.2 --COR.sup.3 IR.sup.1 --A.sup.1 --T--A.sup.2 --NH--R.sup.2 --COR.sup.3 IIR.sup.1 --A.sup.1 --T--A.sup.2 --A.sup.3 --T--A.sup.4 --NH--R.sup.2 --COR.sup.3 IIIare described, in whichR.sup.1 is a hydrogen atom, an alkoxycarbonyl or arylalkoxycarbonyl group conventionally used for protecting amino groups, or CH.sub.3 --(CH.sub.2).sub.m --CO, in which m=0-16,R.sup.2 is --(CH.sub.2).sub.n -- or --(CHOH).sub.n --, in which n=1-10,R.sup.3 is a hydroxyl group, an 0-alkyl or 0-arylalkyl protecting group, a group which activates carboxyl groups, a cephalin radical, an amino acid radical of oligopeptides, polypeptides or proteins which carries NH groups, or a carrier,A.sup.1, A.sup.2, A.sup.3 or A.sup.4 is a bonding dash or an amino acid radical present in glycophorin A, such as Ala, Val, Leu, Ile, Ser, Pro, Glu or Arg, in which, if appropriate, the reactive groups not forming part of the peptide bond are protected by protecting groups, and the radical T is ##STR1## in which R.sup.4 denotes a hydrogen atom or an acyl protecting group,R.sup.5 denotes a hydrogen atom, an acyl protecting group or the 2,3,4,6-tetra-0-acetyl-beta-D-galactopyranosyl or beta-D-galactopyranosyl radical,R.sup.6 denotes N.sub.3, NH.sub.2 or NHAc andR.sup.7 denotes H or CH.sub.3,together with a process for their preparation and their use, bound to a carrier, as artificial antigens, glycolipids or immunoadsorbents.
    • 通式I,II或III的化合物R1-A1-T-NH-R2-COR3I R1-A1-T-A2-NH-R2-COR3II R1-A1-T-A2-A3-T-A4-NH- 描述了其中R 1是氢原子,通常用于保护氨基的烷氧基羰基或芳基烷氧基羰基或其中m = 0-16的R 3 - (CH 2)m -CO,R 2是 - (CH 2) 正 - 或 - (CHOH)n - ,其中n = 1-10,R3是羟基,O-烷基或O-芳基烷基保护基,活化羧基的基团,头孢菌素基团,氨基酸基团 携带NH基团的载体,A1,A2,A3或A4的寡肽,多肽或蛋白质是血型糖蛋白A中存在的结合破伤或氨基酸,例如Ala,Val,Leu,Ile,Ser,Pro, Glu或Arg,其中如果合适的话,不形成肽键部分的反应性基团被保护基团保护,并且基团T是其中R 4表示氢原子或酰基保护基,R 5表示 氢原子,酰基保护基或2,3,4,6-四 a-O-乙酰基-β-D-吡喃半乳糖基或β-D-吡喃半乳糖基,R6表示N3,NH2或NHAc,R7表示H或CH3,以及其制备方法及其用途,结合载体,如 人造抗原,糖脂或免疫吸附剂。