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    • 86. 发明申请
    • DINUCLEOTIDE AND OLIGONUCLEOTIDE ANALOGUES
    • 胆固醇和寡核苷酸类似物
    • WO1997035869A1
    • 1997-10-02
    • PCT/GB1997000651
    • 1997-03-11
    • NOVARTIS AGBAXTER, Anthony, DavidBAYLIS, Eric, KeithCOLLINGWOOD, Stephen, PaulFAIRHURST, Robin, AlecTAYLOR, Roger, John
    • NOVARTIS AG
    • C07H21/00
    • C07H19/06C07H21/00Y02P20/55
    • A compound which is a dinucleotide analogue of formula (I) or a salt thereof, where B an B are each independently a monovalent nucleoside base radical, R is hydrogen or Y , R and R are each independently hydrogen, halogen, hydroxy or -OY , R is hydrogen, halogen, hydroxy, -OY or R , R is hydrogen, halogen or R , R is hydrogen, Y or a phosphoramidyl group, Z is a group of formula (II), (III) or (IV), where R is hydrogen, halogen, hydroxy, -OY or R , R is hydrogen, halogen or R , R is hydroxy, R or -OR where R is a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C10 aromatic group or a C7 to C13 araliphatic group, and R is hydrogen, R a or -OCOR a where R a is C1 to C10 aliphatic, a C3 to C8 cycloaliphatic group, a C6 to C10 aromatic group or a C7 to C13 araliphatic group, Y , Y , Y , Y , and Y are each independently a hydroxy-protecting group, and R , R , R , R are each independently a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C10 aromatic group or a C7 to C13 araliphatic group.
    • 作为式(I)的二核苷酸类似物或其盐的化合物,其中B 1和B 2各自独立地为一价核苷碱基,R 1为氢或Y 1, 2>和R 3各自独立地为氢,卤素,羟基或-OY 2,R 4为氢,卤素,羟基,-OY 3或R 7,R 5为氢 ,卤素或R 8,R 6为氢,Y 4或亚磷酰基,Z为式(II),(III)或(IV)的基团,其中R 9为氢, 卤素,羟基,-OY 5或R 13,R 10是氢,卤素或R 14,R 11是羟基,R 15或-OR 15,其中R 15 >为C1至C10脂族基团,C3至C8脂环族基团,C6至C10芳族基团或C7至C13芳脂族基团,R12为氢,R12a或-OCOR12 其中R 12是C 1至C 10脂族基,C 3至C 8脂环族基团,C 6至C 10芳族基团或C 7至C 13芳脂基基团,Y 1,Y 2,Y 3, 4>和Y 5各自独立地为羟基保护基,R 7,R 8,R 13,R 14,Ar 各自独立地为C1至C10脂族基团,C3至C8脂环族基团,C6至C10芳族基团或C7至C13芳脂肪族基团。
    • 89. 发明申请
    • PYRIMIDIN-4-ONE DERIVATIVES AS PESTICIDE
    • PYRIMIDIN-4-ONE衍生物作为杀菌剂
    • WO1997033890A1
    • 1997-09-18
    • PCT/EP1997001056
    • 1997-03-03
    • NOVARTIS AGWALTER, Harald
    • NOVARTIS AG
    • C07D495/04
    • C07D487/04A01N43/90C07D491/04C07D495/04C07D513/04
    • Novel pyrimidin-4-one derivatives of formula (I), wherein: R1=C1-C8alkyl, C2-C8alkenyl, C2-C8alkynyl, C3-C6cycloalkyl, each of which is unsubstituted or substituted by halogen, O-C1-C4alkyl, O-C1-C4haloalky, O-C1-C4alkoxy, S-C1-C4alkyl, SO-C1-C4alkyl, SO2-C1-C4alkyl, CO-C1C4alkyl, N=C1-C4alkyl, NH-C1-C4alkyl, N(C1-C4alkyl)2, COO-C1-C4alkyl, COO-aryl, cyano, nitro, Si-(C1-C4alkyl)3, phenyl, halophenyl, phenoxyphenyl, halophenoxyphenyl, naphthyl; R2=OR5, SR6, NR7R8; R3 and R4 are each independently of the other hydrogen, halogen, C1-C4alkyl, C1-C4haloalkyl, C2-C4alkenyl, C2-C4haloalkenyl, C2-C4alkynyl, C2-C4haloalkynyl, Si-(C1-C6alkyl)3, COO-C1-C4alkyl, COO-aryl, COOH, CH=N-C1-C4alkyl, C(CH3)=N-C1-C4alkyl, SO-C1-C4alkyl, SO2-C1-C4alkyl, OR5, SR6, NR7R8, COR9; R9=hydrogen, C1-C4alkyl, phenyl, benzyl; R5 and R6 are each independently of the other C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, each of which is unsubstituted or substituted by halogen, O-C1-C4alkyl, O-C1-C4haloalkyl, O-C1-C4alkoxy, S-C1-C4alkyl, SO-C1-C4alkyl, SO2-C1-C4alkyl, CO-C1-C4alkyl, N=C1-C4alkyl, NH-C1-C4alkyl, N(C1-C4alkyl)2, COO-C1-C4alkyl, COO-aryl, cyano, nitro, Si-(C1-C4alkyl)3, phenyl, halophenyl, phenoxyphenyl, halophenoxyphenyl, naphthyl; R7 and R8 are each independently of the other C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, each of which is unsubstituted or substituted by halogen, O-C1-C4alkyl, O-C1-C4haloalkyl, O-C1-C4alkoxy, S-C1-C4alkyl, SO-C1-C4alkyl, SO2-C1-C4alkyl, CO-C1-C4-alkyl, N=C1-C4alkyl, NH-C1-C4alkyl, N(C1-C4alkyl)2, COO-C1-C4alkyl, COO-aryl, cyano, nitro, Si-(C1-C4alkyl)3, phenyl, halophenyl, phenoxyphenyl, halophenoxyphenyl, naphthyl; A = is a 5-membered heterocyclic ring which may be saturated or unsaturated, aromatic or non-aromatic and which may contain one or two hetero atoms O, S and/or N, each in the free form or in salt form. The novel compounds have plant-protective properties and are suitable for protecting plants against infestation by phytopathogenic micro-organisms, in particular fungi.
    • 式(I)的新型嘧啶-4-酮衍生物,其中:R1 = C1-C8烷基,C2-C8链烯基,C2-C8炔基,C3-C6环烷基,其各自为未取代或被卤素,O-C1-C4烷基,O C 1 -C 4卤代烷基,O-C 1 -C 4烷氧基,S-C 1 -C 4烷基,SO-C 1 -C 4烷基,SO 2 -C 1 -C 4烷基,CO-C 1 -C 4烷基,N = C 1 -C 4烷基,NH-C 1 -C 4烷基, )2,COO-C 1 -C 4烷基,COO-芳基,氰基,硝基,Si-(C 1 -C 4烷基)3,苯基,卤代苯基,苯氧基苯基,卤代苯氧基苯基, R2 = OR5,SR6,NR7R8; R3和R4分别独立地为氢,卤素,C1-C4烷基,C1-C4卤代烷基,C2-C4链烯基,C2-C4卤代烯基,C2-C4炔基,C2-C4卤代炔基,Si-(C1-C6烷基)3,COO-C1- C4烷基,COO-芳基,COOH,CH = N-C1-C4烷基,C(CH3)= N-C1-C4烷基,SO-C1-C4烷基,SO2-C1-C4烷基,OR5,SR6,NR7R8,COR9; R9 =氢,C1-C4烷基,苯基,苄基; R 5和R 6各自独立地为C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 3 -C 6环烷基,其各自未被取代或被卤素,O-C 1 -C 4烷基,O-C 1 -C 4卤代烷基,O-C 1 C 1-4烷氧基,S-C 1 -C 4烷基,SO-C 1 -C 4烷基,SO 2 -C 1 -C 4烷基,CO-C 1 -C 4烷基,N = C 1 -C 4烷基,NH-C 1 -C 4烷基,N(C 1 -C 4烷基)2,COO- -C 1-4烷基,COO-芳基,氰基,硝基,Si-(C 1 -C 4烷基)3,苯基,卤代苯基,苯氧基苯基,卤代苯氧基苯基,萘基; R 1和R 2各自独立地为C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 3 -C 6环烷基,其各自未被取代或被卤素,O-C 1 -C 4烷基,O-C 1 -C 4卤代烷基,O-C 1 C 1-4烷氧基,S-C 1 -C 4烷基,SO-C 1 -C 4烷基,SO 2 -C 1 -C 4烷基,CO-C 1 -C 4烷基,N = C 1 -C 4烷基,NH-C 1 -C 4烷基,N(C 1 -C 4烷基)2,COO C 1 -C 4烷基,COO-芳基,氰基,硝基,Si-(C 1 -C 4烷基)3,苯基,卤代苯基,苯氧基苯基,卤代苯氧基苯基,萘基; A =是可以是饱和或不饱和的,芳族或非芳族的5元杂环,并且可以含有一个或两个以游离形式或盐形式的一个或两个杂原子O,S和/或N。 新化合物具有植物保护性质,并且适合于保护植物免受植物病原微生物特别是真菌的侵袭。