公开(公告)号：CA2017678A1

公开(公告)日：1990-11-30

申请号：CA2017678

申请日：1990-05-28

Applicant: UBE INDUSTRIES

Inventor： KODA AKIHIDE ,  KITA JUN ICHIRO ,  KAKU YOSHIO ,  HORIMI IICHIRO ,  SAKAMOTO OSAMI

IPC: C07D239/54 ,  C07D239/553 ,  C07H19/06 ,  C07H19/067 ,  A61K31/505 ,  A61K31/70

Abstract: : 5-Fluorouracil derivative There are diclosed a 5-fluorouracil derivative represented by the formula (1): (1) wherein A represents a group represented by or wherein R1 represents a hydrogen atom or OR5 group, R2, R3 and R5 may be the same or different and each represents a hydrogen atom or a group represented by the following formula (2): (2) wherein R6 represents an acyl group, R7 represents a hydrogen atom, a straight or branched alkyl group, a cycloalkyl group, an aralkyl group, a lower alkenyl group or a phenyl group, and n is an integer of 0 to 6, provided that at least one of R2, R3 and R5 is a group represented by the formula (2), and the case wherein R2 and R5 are both hydrogen atoms is excluded, R4 represents a group represented by the formula (2), and X represents an alkylene group or a cycloalkylene group, and an antitumor agent containing the same as an active ingredient.

公开(公告)号：JPS62158298A

公开(公告)日：1987-07-14

申请号：JP19286

申请日：1986-01-07

Applicant: ARAI TADASHI ,  UBE INDUSTRIES

Inventor： ARAI TADASHI ,  HORIMI IICHIRO ,  IWAYAMA AKIRA ,  NAKAMURA KAZUYOSHI ,  IWAMOTO YOSHITADA

IPC: C07G11/00 ,  A61K35/74 ,  A61P31/04 ,  C12P1/06 ,  C12R1/55

Abstract: NEW MATERIAL:An antibiotic neocopiamycin B having following physicochemical properties; Melting point: 124-126 deg.C (decomposition). Neutral white powdery substance. Molecular formula; C53H91O17N3. Solubility; Soluble in a lower alcohol such as methanol, ethanol and n-butanol, pyridine, dimethylformamide (DMF) and glacial acetic acid and hardly soluble or insoluble in acetone, dioxane, chloroform, carbon tetrachloride, ethyl acetate, butyl acetate, ethyl ether, petroleum ether, benzene, methyl isobutyl ketone and water. Initially pinked and then browned with conc. sulfuric acid and decoloring KMnO4 and bromine liquid. Negative to biuret reaction, ninhydrin reaction, Molisch's reaction, Fehling's solution, ferric chloride, etc., and positive to Dragendorff test and iodo-platinic acid reaction, etc. USE:An antimicrobial agent. PREPARATION:A bacterium strain of the genus Streptomyces, e.g. Streptomyces hygroscopicus IFM 1136, etc., is cultivated.

公开(公告)号：JPH0338573A

公开(公告)日：1991-02-19

申请号：JP17312289

申请日：1989-07-06

Applicant: UBE INDUSTRIES

Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  KAKU YOSHIO ,  HORIMI IICHIRO

IPC: C07D239/553 ,  A61K31/505 ,  A61P35/00

Abstract: NEW MATERIAL:A 1-carbamoyl-5-fluorouracil derivative expressed by formula I [x is 4-12C alkylene or cycloalkylene: R1 is acyl; R2 is H, 1-13C alkyl, aralkyl, (halogen-substituted)-lower-alkenyl or phenyl which may have a substituent group (lower alkyl, lower alkenyl or halogen); (n) is 0-8]. EXAMPLE:1-[6-[N-(2-n-Propyl-n-pentanoyl)glycyl]amino-n hexylcarbamoyl]-5- fluorouracil. USE:An antitumor agent reduced in side effects and having strong antitumor activity. PREPARATION:5-Fluorouracil is reacted with phosgene to give 1-chlorocarbonyl 5-fluorouracil expressed by formula II, which is then reacted with a compound expressed by formula V and obtained by subjecting a compound expressed by formula III to condensation through dehydration with a compound expressed by formula IV to provide the compound expressed by formula I.