BISETHERS OF 1-OXA, AZA AND THIANAPHTHALEN-2-ONES AS PHOSPHOLAMBAN INHIBITORS
    1.
    发明公开
    BISETHERS OF 1-OXA, AZA AND THIANAPHTHALEN-2-ONES AS PHOSPHOLAMBAN INHIBITORS 审中-公开
    二醚1-氧杂,氮杂和噻萘-2-酮AS PHOSPHOLAMBANHEMMER

    公开(公告)号:EP1017691A1

    公开(公告)日:2000-07-12

    申请号:EP98946482.1

    申请日:1998-09-24

    摘要: Therapeutically active compounds of formula (I) or (II), in which R1 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy, COR10, CONR10R11, OR10, S(O)mR10, NR10COR11 or NR10R11, where R10 is hydrogen, alkyl, alkenyl, aryl, arylalkyl, hydroxyalkyl, halogenalkyl, alkoxy or hydroxy and R11 is hydrogen, alkyl, aryl, arylalkyl, alkoxy, aryloxy, hydroxy or acyl, or in case where X is NR11, R1 can also be carboxylalkyl; R6 is hydrogen, alkyl, alkenyl, aryl, arylalkyl; R2 and R7 mean hydrogen, alkyl, aryl, arylalkyl, alkenyl, COR10, CONR10R11, halogen, trifluoromethyl, nitro or cyano, where R10 and R11 are defined as above; R3 is hydrogen, alkyl, aryl or arylalkyl; A means alkyl or substituted alkyl, m is 0-2 and n is 1-3; Y means O, NR11 or S, where R11 is the same as above; X means O, NR11 or S, where R11 is the same as above, R4, R5, R8 and R9 mean independently one of the following groups (a), (b), (c), (d), (e), (f), (g), or in case where X is NR11, R4, R5, R8 and R9 can also independently mean HOOC-, R12OOC-, H2NCO- or HOHNCO-, wherein R12 means alkyl, arylalkyl or aryl, and wherein each aryl residue defined above by itself or as part of another group may be substituted, and pharmaceutically acceptable salts and esters thereof. The compounds have phospholamban inhibiting activity and are useful for treating heart failure.

    Aminoterminal propeptide of type I procollagen, antibody thereto and assay method using it
    3.
    发明公开
    Aminoterminal propeptide of type I procollagen, antibody thereto and assay method using it 失效
    Typ I Prokollagen aminoterminales Propeptid,dessenAntikörperund Testverfahren unter Verwendung davon

    公开(公告)号:EP0738735A2

    公开(公告)日:1996-10-23

    申请号:EP96302639.8

    申请日:1996-04-16

    申请人: ORION-YHTYMA OY

    IPC分类号: C07K14/78 C07K16/18 G01N33/68

    摘要: Aminoterminal propeptide of type I procollagen exists in serum in two forms: classical type I procollagen which is a heterotrimer containing two pro α1-chains and one pro α2-chain of type I procollagen, and an α1-homotrimer type I procollagen containing three identical pro α1-chains. These intact, trimeric aminoterminal propeptides may be isolated without the use of proteolytic enzymes and the resultant propeptides may be used to prepare antibodies specific for the intact trimeric propeptide, having no affinity for the monomeric form of the propeptide. Such antibodies are useful in methods of assaying intact trimeric aminoterminal propeptide of type I procollagen in serum, without false information resulting from inadvertent assay of the monomeric form of the propeptide.

    摘要翻译: I型原胶原的氨基末端前肽以两种形式存在于血清中:经典I型原胶原,其是含有两个前α1链和一个前α胶原的一个前α2链的异源三聚体,以及含有1个前胶原的α1-均三聚体I型前胶原 三个相同的proα1链。 可以分离这些完整的三聚体氨基末端前肽而不使用蛋白水解酶,并且所得前肽可用于制备对前体肽的单体形式没有亲和力的完整三聚体前肽特异性的抗体。 这样的抗体可用于测定血清中I型原胶原的完整三聚体氨基末端前肽的方法,而不会由于前体单体形式的无意识测定而导致的错误信息。

    Paired polypeptides
    4.
    发明公开
    Paired polypeptides 失效
    配对多糖

    公开(公告)号:EP0447133A3

    公开(公告)日:1992-12-09

    申请号:EP91301927.9

    申请日:1991-03-07

    申请人: ORION-YHTYMA OY

    发明人: Krupey, John

    摘要: The invention provides a binding assay reagent comprising a backbone polypeptide comprising glutamic acid residues and lysine residues is proportions such that the backbone polypeptide has a net positive charge, said backbone polypeptide having a molecular mass of ≧ 2.0 x 10⁵ Daltons; an optical dye label covalently bound to the backbone polypeptide, a specific binding molecule covalently bound to the backbone polypeptide, and an enhancing peptide associated with the backbone polypeptide, said enhancing peptide being comprised of a mixture of a) acidic and basic amino acid monomer residues having opposite stereochemical configurations or b) mixtures of homopolymers of acidic amino acids and basic amino acids wherein the homopolymers may be of the same or different stereochemical configurations, and wherein said enhancing peptide is electrically neutral or has a net negative charge. The binding assay reagents exhibit enhanced binding activity over that of the dye labelled polypeptides alone and also enhance the sensitivity of the binding assay by providing increased amounts of optical label.

    A METHOD FOR THE PREPARATION OF NANOPARTICLES
    5.
    发明公开
    A METHOD FOR THE PREPARATION OF NANOPARTICLES 有权
    用于生产纳米粒子

    公开(公告)号:EP1351666A1

    公开(公告)日:2003-10-15

    申请号:EP02710900.8

    申请日:2002-01-18

    IPC分类号: A61K9/14 A61K9/12 A61J3/02

    摘要: The invention relates to free nano-sized particles of active agents e.g. therapeutic, cosmetic or diagnostic agents, and to a method for the preparation of such particles. The method comprises providing a liquid feed stock comprising an active agent or combination of two or more active agents, atomising the liquid feed stock, suspending the droplets in a carrier gas, and passing the carrier gas and droplets through a heated tube flow reactor under predetermined residence time and temperature history, and collecting the particles produced. Nano-sized crystalline spherical uncharged particles with narrow aerodynamic particle size distribution and rough surfaces, are obtained. The particles show improved dissolution rate in-vitro and bioavailability in-vivo, dispersibility and stability.

    Aminoterminal propeptide of type I procollagen, antibody thereto and assay method using it
    6.
    发明公开
    Aminoterminal propeptide of type I procollagen, antibody thereto and assay method using it 失效
    I型前胶原氨基端前肽,抗体和测定方法,使用它

    公开(公告)号:EP0738735A3

    公开(公告)日:1999-01-20

    申请号:EP96302639.8

    申请日:1996-04-16

    申请人: ORION-YHTYMA OY

    IPC分类号: C07K14/78 C07K16/18 G01N33/68

    摘要: Aminoterminal propeptide of type I procollagen exists in serum in two forms: classical type I procollagen which is a heterotrimer containing two pro α1-chains and one pro α2-chain of type I procollagen, and an α1-homotrimer type I procollagen containing three identical pro α1-chains. These intact, trimeric aminoterminal propeptides may be isolated without the use of proteolytic enzymes and the resultant propeptides may be used to prepare antibodies specific for the intact trimeric propeptide, having no affinity for the monomeric form of the propeptide. Such antibodies are useful in methods of assaying intact trimeric aminoterminal propeptide of type I procollagen in serum, without false information resulting from inadvertent assay of the monomeric form of the propeptide.