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    • 2. 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
    • 3-Amino-4-phenyl-1H-pyrazolo[3,4-b]pyridines and salts thereof
    • 3-氨基-4-苯基-1H-吡唑并[3,4-b]吡啶及其盐
    • US4182887A
    • 1980-01-08
    • US834114
    • 1977-09-19
    • Josef RochErich MullerBerthold NarrJosef NicklWalter Haarmann
    • Josef RochErich MullerBerthold NarrJosef NicklWalter Haarmann
    • A61K31/435A61P7/02A61P29/00C07D213/85C07D471/04
    • C07D471/04C07D213/85Y10S514/822
    • Compounds of the formula ##STR1## wherein R.sub.1 is mono- or di-substituted amino, where the substituents are selected from the group consisting of alkyl of 1 to 6 carbon atoms, cyclohexyl, allyl and benzyl; unsubstituted, mono-substituted or di-substituted pyrrolidino, piperidino, hexamethyleneimino, morpholino, piperazino, thiomorpholino, 1-oxido-thiomorpholino or 1,1-dioxido-thiomorpholino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl; 1,2,5,6-tetrahydropyridino; 1,2,3,4-tetrahydroisoquinolino; indolino; or 3,6-ethylene-hexamethyleneimino;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.
    • 其中R 1是单取代或二取代的氨基,其中取代基选自1至6个碳原子的烷基,环己基,烯丙基和苄基; 未取代的单取代或二取代的吡咯烷子基,哌啶子基,六亚甲基亚氨基,吗啉代,哌嗪子基,硫代吗啉代,1-氧代硫代吗啉代或1,1-二氧化硫代吗啉代,其中取代基选自甲基,羟甲基,羟基 ,苯基和苄基; 1,2,5,6-四氢吡啶子; 1,2,3,4-四氢异喹啉; indolino; 或3,6-亚乙基 - 六亚甲基亚氨基; R2是氢,甲基或苄基; R3为氢,卤素,1〜3个碳原子的烷基或1〜3个碳原子的烷氧基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用作消炎和抗血栓形成。