公开(公告)号：KR820001543B1

公开(公告)日：1982-08-31

申请号：KR780002819

申请日：1978-09-16

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MATSUMURA KOICHI ,  MIYASHITA OSAMU ,  SIMATSU HIROSHI ,  HASHIMOTO NAOTO

IPC: A61K31/505 ,  C07D239/54

Abstract: Title compds. (I; R1 = lower alkyl; R4-CO- is residue of carboxylic acid; R2, R3 = phenyl, alkylidene, cycloalkylidene), having antivirus activity, were prepd. by reacting compd. (II) with compd. (III). Thus, anhydrous acetic acid 2.55 g and pyridine 10 ml were added in the soln. of acetone 6 ml and methyl-5-fluoro-6-hydroxy-1,2,3,4,5,6-hexa hydro-2,4-dioxopyrimidine-5-carboxylate 4.12 g, stirred for 12 hr and then cyclohexanone oxime 2.26 g was added. The reaction mixt. was stirred at room temp. for 2 hr and reacted at 65≦̸C for 3 hr to give methyl-5-fluoro-6-cyclohexylidene aminooxy-1,2,3,4,5,6-hexahydro-2,4-dioxopyrimidine-5-carboxylic acid 4.0 g.

公开(公告)号：PH14553A

公开(公告)日：1981-09-24

申请号：PH19603

申请日：1977-03-31

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  SHIMADZU HIROSHI ,  MATSUMURA KOICHI ,  HASHIMOTO NAOTO

IPC: A61K31/513 ,  A61P35/00 ,  C07C273/18 ,  C07C275/20 ,  C07C275/50 ,  C07D239/22 ,  C07D239/54 ,  C07D239/553 ,  C07D239/557 ,  C07D405/04 ,  C07F7/18 ,  A61K31/505 ,  C07D239/00

Abstract: New derivatives of the formula: (wherein X is O or NH; R1 is -OH which may optionally be etherified or esterified, etherified mercapto or -NH2 which may optionally be substituted; R2 and R3, respectively, mean H, lower alkyl or and Y is an esterified or amidated carboxyl group, or CN). These derivatives are produced, by fluorination of corresponding 1,2,3,4-tetrahydro-2,4-dioxopyrimidine compounds and can be converted into 5-fluorouracil derivatives under hydrolytic conditions. The new derivatives are able to prolong the lives of animals having carcinomas or have antiviral activity.

公开(公告)号：AU2371677A

公开(公告)日：1978-10-05

申请号：AU2371677

申请日：1977-03-29

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  MATSUMURA KOICHI ,  SHIMADZU HIROSHI ,  HASHIMOTO NAOTO

IPC: A61K31/513 ,  A61P35/00 ,  C07C273/18 ,  C07C275/20 ,  C07C275/50 ,  C07D239/22 ,  C07D239/54 ,  C07D239/553 ,  C07D239/557 ,  C07D405/04 ,  C07F7/18 ,  A61K31/505 ,  A61K31/535 ,  C07D239/46 ,  C07D239/48 ,  C07D239/56 ,  C07D239/60 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

公开(公告)号：CA1148489A

公开(公告)日：1983-06-21

申请号：CA357361

申请日：1980-07-30

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  AKIMOTO HIROSHI

IPC: A61K31/535 ,  A61P35/00 ,  C07D498/16 ,  C07D498/18 ,  C12P17/18

Abstract: Novel maytansinoid compounds of the formula: wherein X is H or C?, R1 is an alkyl group of 2 to 4 carbon atoms and R2 is a lower alkyl group or an unsubstituted or substituted phenyl or aralkyl group, have antimitotic, antitumor and antimicrobial activities

公开(公告)号：DE3061903D1

公开(公告)日：1983-03-17

申请号：DE3061903

申请日：1980-07-29

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  AKIMOTO HIROSHI HAMAKAOSHIEN-J

IPC: A61K31/535 ,  A61P35/00 ,  C07D498/16 ,  C07D498/18 ,  C12P17/18

Abstract: Novel maytansinoid compounds of the formula: wherein X is H or Cl, R1 is an alkyl group of 2 to 4 carbon atoms and R2 is a lower alkyl group or an unsubstituted or substituted phenyl or aralkyl group, have antimitotic, antitumor and antimicrobial activities.

公开(公告)号：CA1135262A

公开(公告)日：1982-11-09

申请号：CA353738

申请日：1980-06-10

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  AKIMOTO HIROSHI

IPC: A61K31/54 ,  A61P35/00 ,  C07D498/18

Abstract: Novel maytansinoids of the formula: wherein X is H or C?, and R is a hydrocarbon residue or an azaheterocyclic group, said R group having at least one of water-soluble substituents, have antimitotic, antitumor and antimicrobial activities.

公开(公告)号：CA1135260A

公开(公告)日：1982-11-09

申请号：CA353518

申请日：1980-06-06

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  AKIMOTO HIROSHI

IPC: A61K31/535 ,  A61P35/00 ,  C07D498/18 ,  C07D245/04

Abstract: Novel maytansinoids of the formula: wherein Y is H or Cl, and R is C2-15alkyl, phenyl-C1-4alkyl, pyridyl-C1-4alkyl, imidazolyl-C1-4alkyl, indolyl-C1-4alkyl, furyl-C1-4alkyl or thienyl-C1-4alkyl, any of said groups being substituted by hydroxyl, halogen or C1-5alkanoyloxy at its .alpha.- and/or .beta.-position, have antimitotic, antitumor and antimicrobial activities.

公开(公告)号：DE2714392A1

公开(公告)日：1977-12-22

申请号：DE2714392

申请日：1977-03-31

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  SHIMADZU HIROSHI SETTSU ,  MATSUMURA KOICHI ,  HASHIMOTO NAOTO

IPC: A61K31/513 ,  A61P35/00 ,  C07C273/18 ,  C07C275/20 ,  C07C275/50 ,  C07D239/22 ,  C07D239/54 ,  C07D239/553 ,  C07D239/557 ,  C07D405/04 ,  C07F7/18 ,  C07D405/00 ,  A61K31/495

Abstract: New derivatives of the formula: (wherein X is O or NH; R1 is -OH which may optionally be etherified or esterified, etherified mercapto or -NH2 which may optionally be substituted; R2 and R3, respectively, mean H, lower alkyl or and Y is an esterified or amidated carboxyl group, or CN). These derivatives are produced, by fluorination of corresponding 1,2,3,4-tetrahydro-2,4-dioxopyrimidine compounds and can be converted into 5-fluorouracil derivatives under hydrolytic conditions. The new derivatives are able to prolong the lives of animals having carcinomas or have antiviral activity.

公开(公告)号：DE3066482D1

公开(公告)日：1984-03-15

申请号：DE3066482

申请日：1980-06-06

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  AKIMOTO HIROSHI

IPC: A61K31/535 ,  A61P35/00 ,  C07D498/18

公开(公告)号：CA1147680A

公开(公告)日：1983-06-07

申请号：CA357234

申请日：1980-07-29

Applicant: TAKEDA CHEMICAL INDUSTRIES LTD

Inventor： MIYASHITA OSAMU ,  AKIMOTO HIROSHI

IPC: C07D498/18

Abstract: Novel maytansinoids of the formula: , wherein X is hydrogen or chlorine, R1 is C2-4 alkyl, R2 is C2-8 alkyl which may be substituted or methyl which is substituted, have antimicrobial, antimitotic and antitumor activities.