公开(公告)号：WO1996030346A1

公开(公告)日：1996-10-03

申请号：PCT/JP1996000828

申请日：1996-03-28

Applicant: TAIHO PHARMACEUTICAL CO., LTD. ,  YANO, Shingo ,  TADA, Yukio ,  KAZUNO Hideki ,  SATO, Tsutomu ,  YAMASHITA, Junichi ,  SUZUKI, Norihiko ,  EMURA, Tomohiro ,  FUKUSHIMA, Masakazu ,  ASAO, Tetsuji

Inventor： TAIHO PHARMACEUTICAL CO., LTD.

IPC: C07D239/54

CPC classification number: C07D239/54 ,  C07D231/12 ,  C07D233/56 ,  C07D239/553 ,  C07D249/08 ,  C07D403/06 ,  C07D403/12

Abstract: Uracil derivatives represented by general formula (1) or salts thereof, wherein R represents chloro, bromo, iodo, cyano or lower alkyl; and R represents a 4- to 8-membered heterocycle optionally substituted by lower alkyl, imino, hydroxy, hydroxymethyl, methanesulfonyloxy, amino or nitro and having one to three nitrogen atoms, amidinothio wherein hydrogen on nitrogen is optionally substituted by lower alkyl, guanidino wherein hydrogen on nitrogen is optionally substituted by lower alkyl or cyano, lower alkylamidino, amino wherein hydrogen on nitrogen is optionally substituted by lower alkyl, -CH2N(R )R (wherein R and R are the same or different and each represents hydrogen or lower alkyl, or R and R together with the nitrogen atom to which they are bonded may form pyrrolidine), -NH-(CH2)m-Z (wherein Z represents amino wherein hydrogen on nitrogen is optionally substituted by lower alkyl, or cyano; and m is an integer of 0 to 3), -NR (CH2)m-OH (wherein R represents hydrogen or lower alkyl; and n is a natural number of 1 to 4), -X-Y (wherein X represents S or NH; and Y represents 2-imidazolin-2-yl, 2-imidazolyl, 1-methylimidazol-2-yl, 1,2,4-triasol-3-yl, 2-pyrimidyl or 2-benzimidazolyl optionally substituted by lower alkyl), or ureido or thioureido wherein hydrogen on nitrogen is optionally substituted by lower alkyl; and drugs containing the same, such as antitumor effect potentiators and antitumor agents.

Abstract translation: 由通式（1）表示的尿嘧啶衍生物或其盐，其中R 1表示氯，溴，碘，氰基或低级烷基; 并且R 2表示任选被低级烷基，亚氨基，羟基，羟甲基，甲磺酰氧基，氨基或硝基取代且具有一至三个氮原子的4-至8-元杂环，其中氮上的氢任选被低级烷基取代 胍基，其中氮上的氢任选被低级烷基或氰基取代，低级烷基脒基，氨基，其中氮上的氢任选被低级烷基，-CH 2 N（R a）R b取代（其中R a和R b）相同或不同，各自表示氢或低级烷基，或R a和R b与它们所键合的氮原子一起形成吡咯烷），-NH-（CH2）mZ（其中 Z表示氨基，其中氮上的氢任选被低级烷基或氰基取代;且m为0至3的整数），-NR c（CH 2）m -OH（其中R c表示氢或低级烷基 ; n为1至4的自然数），-XY（其中X表示S或NH; Y表示2-咪唑啉-2-基 任选被低级烷基取代的2-嘧啶基或2-苯并咪唑基，或脲基或硫脲基，其中氮原子上的氢是任选的 被低级烷基取代; 和含有相同药物的药物，如抗肿瘤作用增强剂和抗肿瘤剂。

公开(公告)号：WO1990008784A1

公开(公告)日：1990-08-09

申请号：PCT/JP1990000141

申请日：1990-02-06

Applicant: TAIHO PHARMACEUTICAL CO., LTD. ,  KOTAI KASEI CO., LTD. ,  FAN, Hui-Zeng ,  YU, Song ,  YAMANAKA, Etsuji ,  NUMATA, Kazuhiro ,  OKA, Toshinori ,  SUZUKI, Norihiko ,  MURANAKA, Yoshiyuki

Inventor： TAIHO PHARMACEUTICAL CO., LTD. ,  KOTAI KASEI CO., LTD.

IPC: C08B37/00

CPC classification number: C08B37/0063

Abstract: This invention relates to a sulfated polysaccharide D-HG, prepared by depolymerizing FGAG (an extract from the parietes of a sea cucumber comprising a sulfated polysaccharide having a heparinlike action) or its salt and having the following physicochemical properties, pharmaceutically acceptable salts thereof, a method for preparing the same, and drugs for treating diffuse intravascular coagulation (DIC) and thrombosis containing the same as the active ingredient: (1) molecular weight: 3000 to 42000 according to HP GPC; (2) form: white, amorphous and highly hygroscopic powder; (3) solubility: soluble in water and insoluble in organic solvents such as ethanol and acetone; (4) specific rotation: (a); (5) color reaction: Elson-Morgan reaction (+); carbozole-sulfuric acid reaction (+); cysteine-sulfuric acid reaction (+); orcinol-hydrochloric acid reaction (+); azure A metachromasia reaction (+); (6) compositional analysis: galactosamine : glucuronic acid : fucose : sulfate radical = 1 : 0.8 ± 0.2 : 0.85 ± 0.15 : 3.4 ± 0.9.