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公开(公告)号：JPS63115894A
公开(公告)日：1988-05-20
申请号：JP25830686
申请日：1986-10-31
Applicant: SAGAMI CHEM RES
Inventor： TERAJIMA ATSURO , MATSUDA FUYUHIKO , MATSUMOTO MITSUYO , SUZUKI MICHIYO , OSAKI MASAKO , YAMADA KAORU
IPC: C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00
Abstract: NEW MATERIAL:A compound expressed by formula I (R is H or trifluoroacetyl) and salt thereof. EXAMPLE:N-Trifluoroacetyl-14-fluoro-4-demethoxydaunorubicin. USE:A carcinostatic agent capable of exhibiting improved carcinostatic activity. PREPARATION:(R)-2-Acetyl-2,5,12-trihydroxy-1, 2, 3, 4-tetrahydroxynapht-hacene-6, 11-dione (7-deoxy-4-demethoxydaunomycinone) expressed by formula II is initially reacted with a brominating agent and the formed 2-bromoacetyl derivative is reacted with lithium fluoride, etc., to provide a compound expressed by formu la III, which is passed through an acetal derivative to give a compound expressed by formula IV. The resultant compound expressed by formula IV is then reacted with a daunosamine derivative expressed by formula V to afford an alpha-glycoside expressed by formula VI, which is deprotected.
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52.发明专利
公开(公告)号：JPS63115881A
公开(公告)日：1988-05-20
申请号：JP25830786
申请日：1986-10-31
Applicant: SAGAMI CHEM RES
Inventor： TERAJIMA ATSURO , KAWASAKI MOTOSHI , MATSUDA FUYUHIKO , YAMADA KAORU
IPC: C07D493/08 , A61K31/35 , A61P35/00 , C07H15/252 , C07H17/04
Abstract: NEW MATERIAL:A compound expressed by formula I (R is H or a protecting group of OH). EXAMPLE:(+)-(2R,3S,4R,5R,6R,13R)-3,5-Diacetoxy-4-dimethylamino-6-,13-d imethyl- 8,10,13-trihydroxy-3,4,5,6,11,12,13,14-octahydro-2H-naphthaceno[1,2-b] oxocin-9,16- dione. USE:A carcinostatic agent. PREPARATION:A cyclohexadienecarboxylic acid derivative expressed by formula II is oxidized to give a 3,4-epoxy-1-cyclohexenecarboxylic acid derivative, which is then reduced and subsequently oxidized to provide a 1-cyclohexenecarboxylic acid derivative expressed by formula III. The resultant derivative expressed by formula III is then treated with a base to form a trianion, which is protected with a silylating agent and subjected to the Diels-Alder reaction with a compound expressed by formula IV to cleave the silyl group which is a protecting group. The resultant compound is further oxidized with air to afford the aimed compound expressed by formula V.
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公开(公告)号：JPS62228094A
公开(公告)日：1987-10-06
申请号：JP6062086
申请日：1986-03-20
Applicant: SAGAMI CHEM RES
Inventor： TERAJIMA ATSURO , MATSUMOTO MITSUYO , KIMURA YOSHIICHI , SUZUKI MICHIYO , OSAKI MASAKO , YAMADA KAORU
IPC: C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00
Abstract: NEW MATERIAL:The compound of formula I (R is H or trifluoroacetyl) and its salt. EXAMPLE:3'-N-trifluoroacetyl-13-methyl-13-dihydrodaunorubicin. USE:A carcinostatic agent. PREPARATION:A compound of formula I wherein R is trifluoroacetyl can be produced by (1) protecting 7-OH group of daunomycin of formula II used as a starting raw material with silyl group, (2) reacting with a Grignard reagent such as methyl magnesium chloride, etc., to obtain the compound of formula III (R -R are alkyl), (3) reacting the compound with a daunosamine derivative of formula IV (R is acyl) in the presence of trimethylsilyl triflate and (4) deprotecting the resultant alpha-anomer glycoside of formula V in a solvent such as THF under dilute alkaline condition with NaOH, etc., at 0 deg.C - room temperature.
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公开(公告)号：JPS6277398A
公开(公告)日：1987-04-09
申请号：JP21477985
申请日：1985-09-30
Applicant: SAGAMI CHEM RES
Inventor： TERAJIMA ATSURO , MATSUMOTO MITSUYO , KIMURA YOSHIICHI , OSAKI MASAKO , SUZUKI MICHIYO , YAMADA KAORU , TOIDA NOBUKO
IPC: C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04
Abstract: NEW MATERIAL:The compound of formula I (R is 2-12C alkyl) or its salt. EXAMPLE:( 2S,4S )-(+)-4-O-alpha-L-daunosaminyl-2-nonanoyl-2,5,12-trihydroxy-1,2,3,4- tetrahydronaphthacene-6,11-dione hydrochloride. USE:A carcinostatic agent. PREPARATION:The compound of formula I can be produced e.g. by (1) reacting (R)-2,5,11-trihydroxy-1,2,3,4-tetrahydronaphthacene-6,11-dione-2-carbo xylic acid of formula II with a carbonyl compound of formula ACOA' (A and A' are azole residue), (2) reacting the reaction product with a Grignard reagent or formula RMgX (X is halogen) to obtain an acylated compound, (3) brominating and hydrolyzing the compound to introduce hydroxyl group at the 4-position, (4) reacting with an aglycone of formula III (Me is methyl; R1 is acyl) and (5) hydrolyzing the reaction product.
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公开(公告)号：JPS61145167A
公开(公告)日：1986-07-02
申请号：JP26548284
申请日：1984-12-18
Applicant: SAGAMI CHEM RES
Inventor： FUCHIGAMI TAKAMASA , YAMANOUCHI AKIKO , SAKAI KUNIKAZU , YAMADA KAORU
IPC: C07D405/04 , A61K31/505 , A61P35/00 , C07D239/00 , C07D239/54 , C07D239/553 , C07D307/00
Abstract: NEW MATERIAL:The compound of formula I (R and R are alkyl, alkenyl, aralkyl or oxygen-containing heterocyclic group). EXAMPLE:1-Methyl-3-benzyl-5-fluoro-6-chlorouracil. USE:An antitumor agent having decreased toxicity of 5-fluorouracil with lowering its activity to suppress the proliferation of malignant tumor. PREPARATION:The compound of formula I can be produced economically without using hazardous fluorine agent, by (1) reacting the compound of formula II with phosphorus oxychloride in the absence of solvent, preferably in the presence of a tert-amine such as dimethyl-aniline, at room temperature-150 deg.C, or (2) reacting the compound of formula IV with the compound of formula V (X is halogen) in an aprotic solvent, preferably in the presence of an acid acceptor under cooling or at
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Patent Agency Ranking
公开(公告)号：JPS61134358A
公开(公告)日：1986-06-21
申请号：JP25657084
申请日：1984-12-06
Applicant: Sagami Chem Res Center
Inventor： TERAJIMA ATSURO , KIMURA YOSHIICHI , SAKAI KUNIKAZU , MATSUMOTO MITSUYO , YAMADA KAORU , SUZUKI MICHIYO
IPC: A61K31/16 , A61K31/165 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/53 , A61P35/00 , C07C67/00 , C07C231/00 , C07C235/82 , C07D295/18
Abstract: NEW MATERIAL:A compound of formula I (R
1 , R
2 are H, alkyl, substituted alkyl or aralkyl; R
1 and R
2 incorporate to form polymethylene or heteroatom- containing polymethylene).
EXAMPLE: N-2,5,12-Trihydroxy-6,11-dioxo-1,2,3,4-tetrahydronapht-hacene-2-carbon yl)morpholin.
USE: Antitumor agent: It has a very simple structure with anthraquinone skeleton, free from aminosaccharides.
PREPARATION: The reaction of an acylimidazole of formula II with an amine of formula III is carried out in a solvent such as tetrahydrofuran at 0°C to room temperature to give the compound of formula I.
COPYRIGHT: (C)1986,JPO&JapioAbstract translation: 新材料：式I化合物（R 1，R 2）是H，烷基，取代的烷基或芳烷基; R 1和R 2并入以形成聚亚甲基或含杂原子的聚亚甲基）。 实施例：N-2,5,12-三羟基-6,11-二氧代-1,2,3,4-四氢萘并噻吩-2-碳基）吗啉。 用途：抗肿瘤剂：蒽醌骨架结构非常简单，无氨基糖。 制备：式II的酰基咪唑与式III的胺的反应在溶剂如四氢呋喃中，在0℃至室温下进行，得到式I的化合物。
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公开(公告)号：JPS59154993A
公开(公告)日：1984-09-04
申请号：JP2843283
申请日：1983-02-24
Applicant: Sagami Chem Res Center
Inventor： ICHIKAWA TETSUYA , YAMADA KAORU , SAKAI KUNIKAZU , KONDOU SEI
Abstract: NEW MATERIAL:The higher unsaturated fatty acid derivative of formula I (when Y is group a, R is 2,3-dihydroxypropyl, and when Y is group b, R is H).
EXAMPLE: 9(Z),12(Z),15(Z)-Octadecatrien-6-ynoic acid 2,3-dihydroxypropyl ester.
USE: It has antimicrobial activity against the pathogen of rice blast, Escherichia coli, beer yeast, Trichophyton, Bacillus subtilis and Pseudomonas aeruginosa, and is useful as an antimicrobial agent.
PREPARATION: Chopped KAMOJIGOKE (Dicranum scoparium Hedw., a kind of moss) is extracted with ether, methylene chloride, etc.
COPYRIGHT: (C)1984,JPO&JapioAbstract translation: 新材料：式I的高级不饱和脂肪酸衍生物（当Y为基团a时，R为2,3-二羟基丙基，当Y为B基团时，R为H）。 实施例：9（Z），12（Z），15（Z） - 十八碳烯-6-炔酸2,3-二羟丙基酯。 用途：对稻瘟病菌，大肠杆菌，啤酒酵母，毛癣菌，枯草芽孢杆菌和铜绿假单胞菌具有抗菌活性，可用作抗菌剂。 制备：用乙醚，二氯甲烷等萃取切碎的KAMOJIGOKE（Dicranum scoparium Hedw。，一种苔藓）
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公开(公告)号：JP2001213896A
公开(公告)日：2001-08-07
申请号：JP2000018637
申请日：2000-01-27
Applicant: SAGAMI CHEM RES
Inventor： KAMIMURA DAISUKE , ARIMOTO HIROICHI , YAMADA KAORU , YAZAWA KAZUYOSHI
Abstract: PROBLEM TO BE SOLVED: To provide a substance related to the control of a calcium concentra tion in cells. SOLUTION: An octapeptide represented by an amino acid sequence of the sequence number 1 in the specification. The octapeptide induces the increase in the concentration of calcium in cells, and has uses as new types of agrochemical, biochemical research reagent or the like.
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公开(公告)号：JP2001213875A
公开(公告)日：2001-08-07
申请号：JP2000018639
申请日：2000-01-27
Applicant: SAGAMI CHEM RES
Inventor： KAMIMURA DAISUKE , SUENAGA KIYOTAKE , YAMADA KAORU , TAKADA AKIRA , YAZAWA KAZUYOSHI
IPC: C07D319/02 , A61K31/357 , A61P35/00 , A61P35/02
Abstract: PROBLEM TO BE SOLVED: To provide a derivative of 3,6-dihydro-1,2-dioxin having a new structure and an antitumor agent. SOLUTION: This derivative is expressed by general formula (R1 and R2 are each H or combines to form a carbon-carbon double bond with each binding carbon atoms. R3 is H or a lower alkyl.), such as the derivative of 3, 6-dihydro-1, 2-dioxin and the antitumor agent includes the derivative of 3,6-dihydro-1,2-dioxin or its pharmaceutically permissible salt. The derivative has an antiproliferative activity to carcinoma cell such as leukemic cell or the like, and for example, has a use as a medicine for antitumor agent or the like.
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公开(公告)号：JP2000119292A
公开(公告)日：2000-04-25
申请号：JP28739998
申请日：1998-10-09
Applicant: SAGAMI CHEM RES
Inventor： YAZAWA KAZUYOSHI , SHINOHARA YUIKO , SHINOHARA TSUTOMU , KAMIMURA DAISUKE , SUENAGA KIYOTAKE , YAMADA KAORU
Abstract: PROBLEM TO BE SOLVED: To obtain an antiiflammatory agent or an antitumor agent and azalomycin SCs having a new structure. SOLUTION: Azalomycin SCs are represented by the following general formula (R1 to R11 denote each independently hydrogen atom, a lower alkyl group or an acyl group; and R12 denotes hydrogen atom or a lower alkyl group). The azalomycin SCs have an inhibiting activity for cytoplasmic phospholipase A2 and uses as a medicine, e.g. an antiinflammatory agent.
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