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    • 7. 发明授权
    • Biphenylyl derivatives
    • 联苯衍生物
    • US3993683A
    • 1976-11-23
    • US577169
    • 1975-05-14
    • Josef NicklErich MullerBerthold NarrWalter HaarmannWolfgang SchroterRudolf Kadatz
    • Josef NicklErich MullerBerthold NarrWalter HaarmannWolfgang SchroterRudolf Kadatz
    • C07C67/00C07C69/76C07C313/00C07C315/04C07C317/10C07C317/18C07C317/24C07C317/44C07C323/16C07C323/45C07C323/52C07C323/60C07C323/65C07D213/30C07D295/185C07C149/40
    • C07D213/30C07C317/10C07C317/18C07C317/24C07C317/44C07C323/16C07C323/45C07C323/52C07C323/60C07C323/65C07D295/185Y10S514/822
    • Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, fluorine, bromine, methyl, methoxy, methylthio, nitro, cyano or, when A is other than methylene, R.sub.2 is hydrogen, R.sub.3 is carboxyl, m is 2 and n is 0, also chlorine;R.sub.2 is hydrogen or fluorine;R.sub.3 is hydrogen, methyl, hydroxymethyl, carboxyl, (alkoxy of 1 to 6 carbon atoms)-carbonyl, methoxy-(alkoxy of 1 to 6 carbon atoms)-carbonyl, (alkenyloxy of 2 to 6 carbon atoms)-carbonyl, (aralkoxy of 7 to 12 carbon atoms)-carbonyl, phenoxy-carbonyl, pyridylmethoxy-carbonyl, amino-carbonyl, (alkyl of 1 to 3 carbon atoms-amino)-carbonyl, (dialkyl of 1 to 3 carbon atoms-amino)-carbonyl, phenylamino-carbonyl, morpholino-carbonyl, piperidino-carbonyl, thiomorpholino-carbonyl, (1-oxidothiomorpholino)-carbonyl or (1,1-dioxido-thiomorpholino)-carbonyl;A is methylene, (alkyl of 1 to 3 carbon atoms)-methylene, di-(alkyl of 1 to 3 carbon atoms)-methylene, hydroxymethyl-methylene, hydroxymethylene or carbonyl;m is 1 or 2; andn is 0, 1, 2 or 3;And, when R.sub.3 is carboxyl, non-toxic salts thereof formed with an inorganic or organic base. The compounds as well as the salts are useful as antithrombotics, anticholesteremics and anticoagulants.
    • 式A的化合物是氢,氟,溴,甲基,甲氧基,甲硫基,硝基,氰基,或当A不是亚甲基时,R 2是氢,R 3是羧基,m是2,n是0,也是氯; R2是氢或氟; R 3是氢,甲基,羟甲基,羧基,(1至6个碳原子的烷氧基) - 羰基,甲氧基 - (1至6个碳原子的烷氧基) - 羰基,(2至6个碳原子的链烯氧基) - 羰基 7至12个碳原子的羰基,苯氧基 - 羰基,吡啶基甲氧羰基,氨基 - 羰基,(1至3个碳原子的烷基 - 氨基) - 羰基,(1至3个碳原子的二烷基 - 氨基) - 羰基, 苯基氨基羰基,吗啉代羰基,哌啶子基 - 羰基,硫代吗啉代羰基,(1-氧硫基吗啉代)羰基或(1,1-二氧化硫代吗啉代)羰基。 A是亚甲基,(1至3个碳原子的烷基) - 亚甲基,二(1至3个碳原子的烷基) - 亚甲基,羟甲基 - 亚甲基,羟基亚甲基或羰基; M IS 1 OR 2; 和N是0,1,2或3; 当R 3为羧基时,其无机盐与无机或有机碱形成。 化合物以及盐可用作抗血栓形成剂,抗胆固醇剂和抗凝剂。
    • 8. 发明授权
    • 2,4,5,6-Tetrasubstituted pyrimidines and salts thereof
    • 2,4,5,6-四取代嘧啶及其盐
    • US3975384A
    • 1976-08-17
    • US497459
    • 1974-08-14
    • Berthold NarrJosef RochErich MullerWalter Haarmann
    • Berthold NarrJosef RochErich MullerWalter Haarmann
    • C07D239/30C07D239/34C07D239/38C07D239/42C07D239/46C07D239/47C07D239/48C07D239/50C07D239/52C07D239/54C07D239/545C07D239/557C07D239/56C07D239/60C07D417/14
    • C07D239/30C07D239/34C07D239/38C07D239/42C07D239/47C07D239/48C07D239/50C07D239/52C07D239/545C07D239/557C07D239/56C07D239/60
    • Compounds of the formula ##SPC1##WhereinR.sub.1 is alkoxy of 1 to 3 carbon atoms, morpholino, thiomorpholino, 1-oxido-thiomorpholino, 1,1-dioxido-thiomorpholino, or ##EQU1## where A is hydrogen, alkanoyl of 1 to 4 carbon atoms, alkenoyl of 2 to 4 carbon atoms, methoxy-(alkanoyl of 1 to 4 carbon atoms), carboxyl-(alkanoyl of 1 to 4 carbon atoms), acetyl-(alkanoyl of 1 to 4 carbon atoms), methoxy-(alkenoyl of 2 to 4 carbon atoms), carboxyl-(alkenoyl of 2 to 4 carbon atoms), acetyl-(alkenoyl of 2 to 4 carbon atoms), aminocarbonyl, mono(alkyl of 1 to 4 carbon atoms)-aminocarbonyl, di-(alkyl of 1 to 4 carbon atoms)-aminocarbonyl, methoxymethylaminocarbonyl, pyridinoyl, salicyloyl, furanoyl, or (alkyl of 1 to 3 carbon atoms)-sulfonyl,R.sub.2 is morpholino, thiomorpholino, 1-oxido-thiomorpholino, 1,1-dioxido-thiomorpholino, piperazino or N'-[acetyl-(alkanoyl of 1 to 3 arbon atoms)]-piperazino,R.sub.3 is hydrogen, chlorine, bromine, nitro, cyano, formyl, acetyl or carbalkoxy of 2 to 4 carbon atoms, andR.sub.4 is hydrogen, chlorine, bromine, cyano, carbalkoxy of 2 to 4 carbon atoms, alkyl of 1 to 6 carbon atoms, mono(carbalkoxy of 2 to 4 carbon atoms)-alkyl of 1 to 6 carbon atoms, di(carbalkoxy of 2 to 4 carbon atoms)-alkyl of 1 to 6 carbon atoms, hydroxyl, allyloxy, alkoxy of 1 to 6 carbon atoms, mercapto, allylmercapto, (alkyl of 1 to 6 carbon atoms)-mercapto, 1-oxidothiomorpholino, or--NHBwhereB is hydrogen, alkyl of 1 to 3 carbon atoms, cyclohexyl, phenyl, chloro-phenyl, carboxy-phenyl, carbomethoxy-phenyl or pyridyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as the salts are useful as antithrombotics.
    • 式WHERE R1的化合物是1至3个碳原子的烷氧基,吗啉代,硫代吗啉代,1-氧代硫代吗啉代,1,1-二氧化硫代吗啉代或-NN-A,其中A是氢,1至4个碳原子的烷酰基 ,2至4个碳原子的烯酰基,1至4个碳原子的甲氧基 - (烷酰基),1至4个碳原子的羧基 - (烷酰基),1至4个碳原子的乙酰基 - (烷酰基),甲氧基 - 2至4个碳原子),羧基(2-4个碳原子的烯酰基),乙酰基(2至4个碳原子的烯酰基),氨基羰基,单(1-4个碳原子的烷基) - 氨基羰基,二 - (烷基 1至4个碳原子) - 氨基羰基,甲氧基甲基氨基羰基,哒嗪基,水杨酰基,呋喃酰基或(1至3个碳原子的烷基) - 磺酰基,R2是吗啉代,硫代吗啉代,1-氧代硫代吗啉代,1,1-二氧化硫代吗啉 ,哌嗪基或N' - [乙酰基(1至3个碳原子的烷酰基)] - 哌嗪基,R 3为氢,氯,溴,硝基,氰基,甲酰基,乙酰基或碳原子数2〜4的烷氧基,R4为氢 n,氯,溴,氰基,碳原子数为2〜4的烷氧基,碳原子数为1〜6的烷基,碳原子数2〜4的单(碳烷氧基) - 碳原子数为1〜6的烷基,二(碳数2〜4的烷氧基) 碳原子数1〜6的烷基,羟基,烯丙氧基,1〜6个碳原子的烷氧基,巯基,烯丙基巯基,(1〜6个碳原子的烷基) - 巯基,1-氧硫基吗啉代或-NHB,其中B为 氢,1至3个碳原子的烷基,环己基,苯基,氯 - 苯基,羧基 - 苯基,甲酯基 - 苯基或吡啶基,和非毒性,药理学上可接受的酸添加物; 化合物作为抗菌药物有用的方法。