公开(公告)号：AU2704601A

公开(公告)日：2001-07-31

申请号：AU2704601

申请日：2001-01-17

Applicant: SAGAMI CHEM RES ,  TOPPAN PRINTING CO LTD

Inventor： KATOH TADASHI ,  MIYATA FUSAE ,  YAMADA KAORU ,  YOSHIDA SADAMU

IPC: A61P35/02 ,  C07D498/04 ,  A61K31/5383 ,  A61P35/00 ,  C07D241/40 ,  C07D265/34

公开(公告)号：JPH10101678A

公开(公告)日：1998-04-21

申请号：JP25937296

申请日：1996-09-30

Applicant: SAGAMI CHEM RES

Inventor： KAMIMURA DAISUKE ,  YAMADA KAORU ,  TSUJI TOMOKO ,  YAMAGUCHI KOJI

IPC: C07D498/22 ,  A61K31/435 ,  A61P9/10 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new derivative capable of inhibiting the cell- adhering molecule production of human intravenous endothelial cells within a range not exhibiting cytotoxicity and useful as a metastasis control medicine, an antiinflammatory medicine, arteriosclerosis medicine, etc., by reducing a zoanthamine derivative. SOLUTION: A new reduction type zoanthamine derivative of formula I [R is H, methyl; R is a (substituted)alkyl, an alkoxycarbonyl, an aryloxycarbonyl, an alkenyloxycarbonyl, silyl, tetrahydropyranyl, an acyl; Me is methyl] or formula II. The derivative of formula I or II inhibits the production of a cell-adhering molecule (VCAM-1) with human intravenous endothelial cells, and is useful as a metastasis control medicine, an antiinflammatory medicine, and medicines for treating bronchial asthma, arteriosclerosis, transplant rejection, chronic rheumatoil arthritis, sarcoidosis, etc. The compound of formula I is obtained by reducing the 15 and 17-unsaturated carbonyl groups or 20- carbonyl group of the zoanthamine isolated from a coelenterate.

公开(公告)号：JPH1053589A

公开(公告)日：1998-02-24

申请号：JP30759296

申请日：1996-11-19

Applicant: SAGAMI CHEM RES

Inventor： TSUJI TOMOKO ,  YAMAGUCHI KOJI ,  YADA MIKA ,  KAMIMURA DAISUKE ,  YAMADA KAORU

IPC: A61K31/435 ,  A61P3/00 ,  A61P9/00 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07D498/22

Abstract: PROBLEM TO BE SOLVED: To obtain the subject production inhibitor containing a specific zoanthamine compound or its salt as an active ingredient, capable of inhibiting the production of interleukin-6 and useful for preventing and treating diseases caused by the interleukin-6, etc. SOLUTION: This interleukin-6 production inhibitor contains a zoanthamine compound of the formula (R is H, OH, or R forms a single bond together with R ; R is H, or R forms a single bond together with R or R ; R is H, or R forms a single bond together with R or methylene group together with R ; R is H, or R forms oxo group together with R ; R is OH, or R forms oxo group together with R ; R is H, methyl, hydroxymethyl; R is methyl, or R forms methylene group together with R ; R and R are combined with each other to form oxo group) or its pharmaceutically permissible salt as an active ingredient. The interleukin-6 inhibitor can inhibit the production of the interleukin-6, and thereby is useful for medicines for preventing and treating diseases caused by the interleukin-6, and further for bone resorption-inhibiting medicines, osteoporosis medicines, etc.

公开(公告)号：JPH09110689A

公开(公告)日：1997-04-28

申请号：JP27302495

申请日：1995-10-20

Applicant: SAGAMI CHEM RES

Inventor： KAMIMURA DAISUKE ,  YAMADA KAORU ,  TSUJI TOMOKO

IPC: C12P17/06 ,  A61K31/35 ,  A61K31/352 ,  A61P9/10 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07D311/92 ,  C12R1/01

Abstract: PROBLEM TO BE SOLVED: To obtain a new inhibiting agent containing a napyradiomycin compound represented by a specific formula as an active ingredient, capable of inhibiting the cell-adhesive molecule production of human venous endothelial cells within a range not expressing cytotoxicity, and useful as a cancer metastasis-inhibiting agent. SOLUTION: This agent for inhibiting the venous cell-adhesive molecule-1 production contains a napyradiomycin compound of formula I (R is Cl, H; R is H; R , R are each methyl, OH, or R , R form a ethylidene group together; R is Cl, Br), preferably napyradiomycin SC of formula II, as an active ingredient. The napyradiomycin compound is obtained e.g. by culturing Streptomyces cyaneus (FERM P-15233) in a liquid culture medium in culture conditions comprising 30-37 deg.C and a pH of 7-8 under an aerobic condition for 12hr to 10 days, extracting the microorganism culture product or the culture supernatant with an organic solvent and further separating the napyradiomycin compound by a chromatography.

公开(公告)号：JPH08245505A

公开(公告)日：1996-09-24

申请号：JP22896595

申请日：1995-09-06

Applicant: TOSOH CORP ,  SAGAMI CHEM RES

Inventor： KAMIMURA DAISUKE ,  YAMADA KAORU ,  TOKUHISA KENJI ,  WATANABE HIROYUKI

IPC: A61K31/215 ,  A61P35/00 ,  C07C67/14 ,  C07C67/28 ,  C07C69/33 ,  C07C271/34

Abstract: PURPOSE: To obtain a new compound useful as physiologically active substances including technical products of medicines and agrochemicals, their intermediates and antitumor agents. CONSTITUTION: This compound of formula I [R is H or a 1-20C acyloxy; R and R are each H or pivalyl and R and R are each H when R is H, on the other hand, R and R are each H, a 1-20C acyl, a (substituted)benzoyl, a (substituted)benzyl, trityl, etc., when A is the 1-20C acyloxy], e.g. 1,3- oxyingenol 20-trityl ether. The compound of formula I is obtained by reacting a compound of formula II [R is H or a 1-20C acyloxy; R is pivalyl when R is H, on the other hand, R is a 1-20C acyl, a (substituted)benzoyl, a (substituted)benzyl, trityl, etc., when R is a 1-20C acyloxy] with a halide of the formula R X [R is a 1-20C acyl, a (substituted)benzoyl, a (substituted) benzyl, trityl, etc.; X is a halogen].

公开(公告)号：JPH06797B2

公开(公告)日：1994-01-05

申请号：JP1815987

申请日：1987-01-30

Applicant: SAGAMI CHEM RES

Inventor： TERAJIMA ATSURO ,  MATSUDA FUYUHIKO ,  MATSUMOTO MITSUYO ,  SUZUKI MICHO ,  OOSAKI MASAKO ,  YAMADA KAORU

IPC: A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P35/00 ,  C07H15/252

公开(公告)号：JPH05247043A

公开(公告)日：1993-09-24

申请号：JP8138392

申请日：1992-03-04

Applicant: SAGAMI CHEM RES

Inventor： TERAJIMA ATSURO ,  HASHIMOTO MASARU ,  YAMADA KAORU

IPC: A61K31/40 ,  A61K31/396 ,  A61P35/00 ,  C07D207/20 ,  C07D487/04 ,  C07F7/18

Abstract: PURPOSE:To obtain a new compound useful as a carcinostatic agent having strong cell toxicity. CONSTITUTION:A compound of formula I (R and R are 1-5C alkyl or aralkyl) such as (S)-5-(t-butyldiphenylsilyloxy)methylpyrrolidine-2-thione. The compound of formula I is obtained by silylating (S) or (R)-5-hydroxymethylpyrrolidin-2-one of formula II as a starting substance, successively carrying out conversion of carbonyl group, reaction with a halogenomalonic diester and elimination of silyl group to give a compound of formula III, then sulfonylating the hydroxyl group of the compound of formula III and treating with a base (e.g. potassium hydroxide).

公开(公告)号：JPS63233986A

公开(公告)日：1988-09-29

申请号：JP6565787

申请日：1987-03-23

Applicant: SAGAMI CHEM RES

Inventor： SAKAI KUNIKAZU ,  YAMADA KAORU ,  ICHIKAWA TETSUYA ,  YAMASHITA MITSUO ,  KONDO SEI

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

Abstract: NEW MATERIAL:The compound of formula. USE:An antitumor agent. PREPARATION:Isothecium subdiversiforme is crushed in frozen state and extracted with ether. Ether is distilled out from the extract and the active component is purified by a combination of column chromatography and high- performance liquid chromatography (HPLC) using the in vitro proliferation inhibiting action against mouse lymphemia cell (P383) as an index.

公开(公告)号：JPS62228090A

公开(公告)日：1987-10-06

申请号：JP4168886

申请日：1986-02-28

Applicant: SAGAMI CHEM RES

Inventor： URATA HISAO ,  FUCHIGAMI TAKAMASA ,  TANAKA MARIKO ,  YAMADA KAORU ,  TOIDA NOBUKO

IPC: C07F15/00 ,  A61K31/505 ,  A61K31/555 ,  A61P35/00 ,  C07D239/54 ,  C07D239/553

Abstract: NEW MATERIAL:The compound of formula I (R and R are H, alkyl, alkenyl, aralkyl or O-containing heterocyclic group; M is Pd or Pt; X is halogen; L and L are unidentate ligand or together form a bidentate ligand). EXAMPLE:cis-( 2-Fluoro-3,5-dioxo-4, 6-dimethyl-4, 6-diaza-1-cyclohexenyl ) iodobis (triphenylphosphine)palladium. USE:An antitumor agent. PREPARATION:The objective compound can be produced e.g. according to the reaction formula by reacting the compound of formula II with the compound of formula III (n is 0-2 when L' is unidentate ligand and n is 0 or 1 when L' is bidentate ligand) in a solvent (usually benzene, etc.) at room temperature.

公开(公告)号：JPS62228069A

公开(公告)日：1987-10-06

申请号：JP11719686

申请日：1986-05-23

Applicant: SAGAMI CHEM RES

Inventor： FUCHIGAMI TAKAMASA ,  TANAKA MARIKO ,  YAMADA KAORU ,  TOIDA NOBUKO

IPC: C07D239/553 ,  A61K31/505 ,  A61P35/00 ,  C07D239/54

Abstract: NEW MATERIAL:A 1,3-disubstituted-5-fluoro-6-iodouracil derivative expressed by formula I (R and R are alkyl, alkenyl, aralkyl or oxygen-containing heterocyclic group). EXAMPLE:1,3-Dimethyl-5-fluoro-6-iodouracil. USE:An antitumor agent having improved toxicity of 5-fluorouracil and higher inhibition ratio of malignant tumor than that of 6-chloro derivatives. PREPARATION:A compound expressed by formula II is reacted in the presence of a base, e.g. butyllithium, lithium diisopropylamide, etc., preferably in an ether based solvent, e.g. diethyl ether, tetrahydrofuran, etc., to give a compound expressed by formula III, which is then reacted with an iodinating agent, e.g. iodine monochloride, iodine, etc., preferably in the above-mentioned solvent to afford the aimed compound expressed by formula I.