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    • 33. 发明申请
    • METHOD FOR ANALYSIS OF SUBSTANCES IN TISSUE OR IN CELLS
    • 组织或细胞中物质分析方法
    • WO0165254A3
    • 2002-06-20
    • PCT/JP0101640
    • 2001-03-02
    • SUNTORY LTDYASUDA AKIKAZUYASUDA YOSHIMINAKAJIMA TERUMI
    • YASUDA AKIKAZUYASUDA YOSHIMINAKAJIMA TERUMI
    • G01N33/68
    • G01N33/6848G01N33/6818G01N33/6851
    • An improved method for directly identifying a chemical structure of a substance present in tissue or cells of organisms is disclosed. In particularly, the method for directly identifying a chemical structure of a substance present in tissue or cells of various kind of organisms comprises the following steps: (1) a step irradiating a laser to a certain intracellular region of a sample tissue slice or a cell, and analyzing the generating mass ions to obtain mass spectrum of the substance present at the cite, (2) a step analyzing the mass spectrum to obtain a mass profile of the substance existing at the intracellular region of the sample tissue slice or in cell, and(3) a step determining the chemical structure of the substance corresponding a certain molecular weight appeared in the mass profile. The method of this invention is conducted by utilizing the combined techniques of matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS), and on-line capillary reversed-phase HPLC/quadrupole orthogonal acceleration time-of-flight (Q-Tof)-MS, and molecular cloning, is disclosed.
    • 公开了用于直接鉴定存在于生物体的组织或细胞中的物质的化学结构的改进方法。 特别地,用于直接鉴定存在于各种生物体的组织或细胞中的物质的化学结构的方法包括以下步骤:(1)向样品组织切片或细胞的某个细胞内区域照射激光的步骤 并分析产生质量离子以获得存在于该引物上的物质的质谱,(2)分析质谱以获得存在于样品组织切片或细胞的细胞内区域的物质的质量分布的步骤, 和(3)确定质量分布中出现的对应于某一分子量的物质的化学结构的步骤。 本发明的方法是利用基质辅助激光解吸/电离飞行时间质谱(MALDI-TOF MS)和在线毛细管反相HPLC /四极正交加速时间的组合技术 (Q-Tof)-MS和分子克隆。
    • 34. 发明申请
    • PYRROLOTHIAZINE AND PYRROLOTHIAZEPINE COMPOUNDS HAVING SEROTONIN-2 RECEPTOR ANTAGONISTIC AND ALPHA1-BLOCKING ACTION
    • 具有SEROTONIN-2受体拮抗剂和ALPHA1阻断作用的吡罗昔康和吡咯烷酮化合物
    • WO9933840A2
    • 1999-07-08
    • PCT/JP9805954
    • 1998-12-25
    • SUNTORY LTDMIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • MIZUNO AKIRASHIBATA MAKOTOKAMEI TOMOEFUKAMI HARUKAZUINOMATA NORIO
    • A61K31/54A61K31/55A61P9/00A61P9/02A61P9/06A61P9/08A61P9/10A61P9/12A61P43/00C07D207/36C07D513/04
    • C07D513/04C07D207/36
    • A pyrrolesulfonamide derivative having formula (I) wherein the ring P represented by alpha is a pyrrole ring having structure beta or psi wherein R represents alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR1, in which R1 represents H, or alkyl, aralkyl or aryl; stands for 0 or 1; A represents alkylene, alkenylene or alkynylene; and Y represents a group delta in which W represents CH, C= or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C=; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group. The compound (I) has strong serotonin-2 receptor antagonistic action and low toxicity and less side effects, and is useful as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.
    • 具有式(I)的吡咯磺酰胺衍生物,其中由α表示的环P是具有β或psi结构的吡咯环,其中R表示烷基,环烷基,环烷基 - 烷基或芳烷基; 虚线表示存在或不存在键; 当存在键时,Z 2不存在,Z1表示H,但当不存在键时,Z1表示H,Z2表示OH或Z1,Z2组合在一起表示O或NOR1基团,其中R1表示 H或烷基,芳烷基或芳基; 代表0或1; A表示亚烷基,亚烯基或亚炔基; 并且Y表示其中W表示CH,C =或N的组δ; 当W为CH或N时,m代表0或1,当W为C =时,m代表1; B表示特定的二价基团; E1和E2各自独立地表示H或低级烷基; D表示芳族烃基或杂环基。 化合物(I)具有强的5-羟色胺-2受体拮抗作用,毒性低,副作用小,作为循环系统疾病如缺血性心脏病,脑血管障碍和周围循环障碍的治疗有用。