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    • 5. 发明申请
    • FACTOR VII-BINDING REAGENT
    • 因子VII结合试剂
    • WO1997049684A1
    • 1997-12-31
    • PCT/DK1997000275
    • 1997-06-23
    • NOVO NORDISK A/SPETERSEN, Lars, ChristianOLSEN, Ole, HvilstedRICHTER, Stefan, LutzJAKOBSEN, Palle
    • NOVO NORDISK A/S
    • C07D231/14
    • C07D241/52A61K31/16A61K31/415A61K31/4192A61K31/4439A61K31/4745A61K31/498A61K33/30C07D231/14A61K2300/00
    • Compounds of general formula (Ib) wherein X is a chain, aliphatic or comprising hetero atoms as chain members; and R1 is hydrogen, an amino group (optionally substituted with methyl), or a methyl group; and R2 is hydrogen, or a methyl group; or X, in combination with C2, R1, R2, N1, and C3, forms a carbocyclic or heterocyclic system; and wherein the distance between C1 and C3 is from about 0.37 nm to about 0.77, e.g. about 0.57 nm to about 0.67 nm; and pharmaceutically acceptable salts thereof; are zinc chelating agents. The compounds show anticoagulant properties due to an inhibitory interaction with factor VII and serum level Zn . The zinc chelating agents bind to factor VIIa and induces replacement of calcium ions with zinc ions in the serine protease domain of factor VIIa, thereby inhibiting the activity of factor VIIa or tissue factor-factor VIIa complex. The compounds are useful for the treatment of deficiencies of blood clotting factors or the effects of inhibitors to blood clotting factors. Methods for inhibiting clotting activity are disclosed.
    • 通式(Ib)的化合物,其中X是链,脂族或包含杂原子作为链成员; 和R 1是氢,氨基(任选被甲基取代)或甲基; 和R2是氢或甲基; 或X与C2,R1,R2,N1和C3组合形成碳环或杂环体系; 并且其中C1和C3之间的距离为约0.37nm至约0.77,例如 约0.57nm至约0.67nm; 及其药学上可接受的盐; 是锌螯合剂。 由于与因子VII和血清水平Zn 2+的抑制相互作用,化合物显示出抗凝血性质。 锌螯合剂与因子VIIa结合并诱导因子VIIa的丝氨酸蛋白酶结构域中的锌离子替代钙离子,从而抑制因子VIIa或组织因子因子VIIa复合物的活性。 该化合物可用于治疗凝血因子的缺陷或抑制剂对凝血因子的作用。 公开了抑制凝血活性的方法。
    • 10. 发明申请
    • A HUMAN KUNITZ-TYPE PROTEASE INHIBITOR VARIANT
    • 人类昆虫型蛋白酶抑制剂变种
    • WO1993014121A1
    • 1993-07-22
    • PCT/DK1993000004
    • 1993-01-07
    • NOVO NORDISK A/SNORRIS, FannyNORRIS, KjeldBJORN, Soren, ErikPETERSEN, Lars, ChristianOLSEN, Ole, Hvilsted
    • NOVO NORDISK A/S
    • C07K07/10
    • C07K14/8114A61K38/00
    • Variant of human Kunitz-type protease inhibitor domain II of tissue factor pathway inhibitor (TFPI), the variant comprising the following amino acid sequence X Asp Phe Cys Phe Leu Glu Glu Asp X Gly X Cys X X X X X X Tyr Phe Tyr Asn Asn Gln Thr Lys Gln Cys Glu Arg Phe X Tyr Gly Gly Cys X X X Met Asn Asn Phe X Thr Leu Glu Glu Cys Lys Asn Ile Cys Glu Asp X (SEQ ID No. 1), wherein X represents H or 1-5 naturally occurring amino acid residues except Cys, X -X each independently represents a naturally occurring amino acid residue, and X represents OH or 1-5 naturally occurring amino acid residues except Cys, with the proviso that at least one of the amino acid residues X -X is different from the corresponding amino acid residue of the native sequence.
    • 人类Kunitz型蛋白酶抑制剂结构域II的组织因子途径抑制剂(TFPI)的变体,包含以下氨基酸序列的变体X 1 Asp Phe Cys Phe Leu Glu Glu Asp X 2 Gly X 3 Cys X X 5 X 6 X 7 X 8 Tyr Phe Tyr Asn Asn Gln Thr Lys Gln Cys Glu Arg Phe X 10 Tyr Gly Gly Cys X 11 X < 12> X 13 Met Asn Asn Phe X 14 Thr Leu Glu Glu Cys Lys Asn Ile Cys Glu Asp X 15(SEQ ID No.1),其中X 1表示H或1-5天然存在 除Cys之外的氨基酸残基,X 2 -X 14各自独立地表示天然存在的氨基酸残基,X 15表示除Cys之外的OH或1-5个天然存在的氨基酸残基,条件是至少 氨基酸残基X 1 -X 15之一与天然序列的相应氨基酸残基不同。