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    • 1. 发明申请
    • ASIALOTRISACCHARIDE MORANOLINE DERIVATIVES AND DRUGS
    • ASIALOTRISACCHARIDE MORANOLINE DORIVATIVES AND DRUGS
    • WO1997048712A1
    • 1997-12-24
    • PCT/JP1997002069
    • 1997-06-16
    • NIPPON SHINYAKU CO., LTD.OHGI, TadaakiISHIYAMA, KouichiMORI, Kazuya
    • NIPPON SHINYAKU CO., LTD.
    • C07H17/02
    • C07H17/02
    • Novel asialotrisaccharide moranoline derivatives represented by general formula (I) which inhibit selectins and thus are useful in the treatment of diseases such as inflammation wherein R represents (a) or (b); one of R and R represents galactopyranosyl optionally substituted at all or some of the hydroxyl groups by -SO3H, -CH2COOH or (c) while another represents fucopyranosyl; A represents -(CH2)m-NR -CO-O-, -CO-O-, -(CH2)n-CO-O-, -C2H4(OC2H4)z-NR -CO-O-, -C2H4(OC2H4)y-OCH2-CO-O- or -(CH2)n-O-; R and R are the same or different and each represents a saturated or unsaturated hydrocarbon group or a saturated or unsaturated fatty acid residue; R and R are the same or different and each represents hydroxy, alkyl or alkoxy; and R represents H or alkyl.
    • 抑制选择素的由通式(I)表示的新型脱二羟基山梨醇衍生物衍生物,因此可用于治疗诸如炎症的疾病,其中R代表(a)或(b); R 1和R 2中的一个表示通过-SO 3 H,-CH 2 COOH或(c)任选地在所有或一些羟基上被取代的吡喃半乳糖基,而另一个代表fucopyranosyl; A表示 - (CH 2)m -NR 6 -CO-O-,-CO-O-, - (CH 2)n -CO-O-,-C 2 H 4(OC 2 H 4)z -NR NR -CO-O - , - C 2 H 4(OC 2 H 4)y -OCH 2 -CO-O-或 - (CH 2)n O-; R a和R b相同或不同,各自表示饱和或不饱和烃基或饱和或不饱和脂肪酸残基; R c和R d相同或不同,各自表示羟基,烷基或烷氧基; R e表示H或烷基。
    • 2. 发明申请
    • ISCHEMIC HEART MUSCLE PROTECTIVE AGENTS
    • ISCHEMIC HEART MUSCLE保护剂
    • WO1997025987A1
    • 1997-07-24
    • PCT/JP1997000071
    • 1997-01-17
    • NIPPON SHINYAKU CO., LTD.FUJIWARA, HisayoshiYOSHIKUNI, YoshiakiOCHI, Seishi
    • NIPPON SHINYAKU CO., LTD.
    • A61K31/445
    • C07D471/04A61K31/437C07C215/42C07C2601/14C07D211/46
    • Ischemic heart muscle protecting agents and remedies for angina pectoris containing as the active ingredient compounds represented by general formula (I), wherein R , R and R are the same or different and each represents hydrogen, acyl, cyclohexanecarbonyl, alkoxyacetyl, naphthylcarbonyl, phenylalkanoyl, cinnamoyl, pyridinecarbonyl, dihydropyridinecarbonyl, thiophenecarbonyl, furylcarbonyl or benzyl; and A represents CH or N; provided that when A represents CH, then R represents hydroxy, R represents alkylamino and R represents hydroxymethyl or acyloxymethyl; while when A represents N, then R represents hydrogen, R represents hydroxymethyl or acyloxy, R represents alkyl, aryloxyalkyl or arylalkenyl, or R and R are combined together so that general formula (I) is represented by general formula (II).
    • 缺血性心肌保护剂和含有作为由通式(I)表示的活性成分化合物的心绞痛的治疗剂,其中R 1,R 2和R 3相同或不同,各自表示氢,酰基 环己烷羰基,烷氧基乙酰基,萘基羰基,苯基烷酰基,肉桂酰基,吡啶羰基,二氢吡啶羰基,噻吩羰基,呋喃基羰基或苄基; A表示CH或N; 条件是当A表示CH时,R 4表示羟基,R 5表示烷基氨基,R 6表示羟甲基或酰氧基甲基; 而当A表示N时,R 6表示氢,R 4表示羟甲基或酰氧基,R 5表示烷基,芳氧基烷基或芳基烯基,或R 4和R 5组合在一起, 式(I)由通式(II)表示。
    • 6. 发明申请
    • GALACTOSYLMORANOLINE DERIVATIVE
    • 糖醇衍生物衍生物
    • WO1995006057A1
    • 1995-03-02
    • PCT/JP1994001371
    • 1994-08-19
    • NIPPON SHINYAKU CO., LTD.OHGI, TadaakiKYOTANI, YohsukeOGAWA, HirotsuguEZURE, Yohji
    • NIPPON SHINYAKU CO., LTD.
    • C07H17/02
    • C07H17/02
    • A novel galactosylmoranoline derivative represented by general formula [I], which is an intermediate for a sialyl-Lewis sugar chain derivative useful as a medicine, wherein R represents C1-C20 alkyl, C10 or lower alkenyl, C10 or lower alkynyl or C10 or lower aralkyl, each of which may be substituted by carboxy, lower alkoxycarbonyl, lower alkoxycarbonylaryloxy, lower alkoxycarbonylamino, amino, aroylamino, lower alkoxyamino, lower alkylamino, carbamoyl, lower alkylcarbamoyl, hydroxy, lower alkoxy, aroyl, aryloxycarbonyl, aralkyloxy, lower alkyl, lower cycloalkyl, epoxy or aryl; R represents hydroxy or acetamido; and R and R are different from each other and each represents hydroxy or 1-galactosyl.
    • 由通式[I]表示的新型半乳糖基吗啉衍生物衍生物,其是用作药物的唾液酸 - 路易斯糖链衍生物的中间体,其中R 1表示C1-C20烷基,C10或低级烯基,C10或低级炔基或 可以被羧基,低级烷氧基羰基,低级烷氧基羰基氧基,低级烷氧基羰基氨基,氨基,芳酰基氨基,低级烷氧基氨基,低级烷基氨基,氨基甲酰基,低级烷基氨基甲酰基,羟基,低级烷氧基,芳酰基,芳氧基羰基,芳烷氧基,低级 烷基,低级环烷基,环氧基或芳基; R 2表示羟基或乙酰氨基; R 3和R 4彼此不同,各自表示羟基或1-半乳糖基。