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1. 发明专利

JP2000095781A LIPOPEPTIDE COMPOUND HAVING ANTITUMOR ACTIVITY 失效
公开(公告)号：JP2000095781A
公开(公告)日：2000-04-04
申请号：JP25473598
申请日：1998-09-09
申请人： SAGAMI CHEM RES
发明人： TSUJI TOMOKO , SHINOHARA TSUTOMU , YAMADA AKIKO , KAMIMURA DAISUKE , SUENAGA KIYOTAKE
IPC分类号： A61K31/55 , A61P35/00 , C07D413/12
摘要： PROBLEM TO BE SOLVED: To obtain a new compound manifesting a growth inhibitory activity against a cancer cell and useful as an antitumor agent. SOLUTION: This lipopeptide compound is a compound of the formula (R is H or methoxy), e.g. amamistatin A. The compound of the formula is obtained by extracting the cultured liquid of an Actinomyces [e.g. Actinomyces SCRC-A 2359 strain (FERM P16804)] with an organic solvent such as methanol, and then isolating with a chromatography such as a silica gel column chromatography, a reverse phase type high speed liquid chromatography, etc. Further, it has following physicochemical propeties. Color and state: a brown colored oily material; molecular formula: C37H55N5O11; Mass analysis value: EI mass spectrum m/z, 745(M), CI mass spectrum m/z, 746 (M+H), theoretical value of m/z, 746.3926 (calculated as C37H56N5O11); specific optical rotation: [α]D26, (-)9.8 deg. (c=0.606, methanol), etc.

2. 发明专利

JPH10279574A APOPTOSIS INDUCER, ANTITUMOR AGENT AND BASEMENT MEMBRANE INFILTRATION INHIBITOR 失效
公开(公告)号：JPH10279574A
公开(公告)日：1998-10-20
申请号：JP29436697
申请日：1997-10-27
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , YAMADA KAORU
IPC分类号： C07D307/92 , A61K31/365 , A61K36/47 , A61P35/00 , A61P37/00 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound, having actions on the induction of apoptosis in cells, suppressing action on cell proliferation, inhibiting actions, etc., on the infiltration into basement membranes and useful as an antitumor agent and an inhibitor of the basement membrane infiltration. SOLUTION: This compound is a jolkinolide D represented by the formula and capable of providing an active ingredient of an apoptosis inducer, an antitumor agent, an inhibitor of the basement membrane infiltration. The jolkinolide D represented by the formula can be obtained by separation and purification from Euphorbia jolkini Boiss. which is a plant of the family Euphorbiaceae. The daily dose of the active ingredient is usually about 1 μg to 500 mg and is preferably administered in one to divided several portions. Thereby, the compound can be used as a therapeutic agent for, e.g. malignant tumor, autoimmune diseases and inflammations.

3. 发明专利

JPH10204046A ANTIMICROBIAL AND ANTIFOULING AGENT AND BROMOACETAMIDE DERIVATIVE 失效
公开(公告)号：JPH10204046A
公开(公告)日：1998-08-04
申请号：JP1081897
申请日：1997-01-24
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , YAMADA AKIHIRO , YAZAWA KAZUYOSHI
IPC分类号： C07C233/04 , A01N37/18 , C07C233/05 , C07C233/06 , C07C233/07 , C07C233/13
摘要： PROBLEM TO BE SOLVED: To obtain a new compound, having in vitro growth inhibiting activities against bacteria, capable of manifesting antifouling activities in the field, having especially high antimicrobial activities against marine attached bacteria and useful as an antimicrobial and antifouling agent. SOLUTION: This new compound is represented by the formula (R and R are each H, an aralkyl, etc.; X is Br or H), e.g. N-2-[(4-nitrophenyl) ethyl]tribromoacetamide. In the case of the N-2-[(4-nitrophenyl) ethyl]tribromoacetamide as an example, the compound represented by the formula is synthesized by adding thionyl chloride and N,N-dimethylformamide to tribromoacetic acid, carrying out the refluxing for 5hr, concentrating the reactional mixture, adding a mixture solution prepared by adding triethylamine to a solution of a 2-(4-nitrophenyl)ethylamine hydrochloride converted into a free amine in dichloromethane thereto under cooling with ice, conducting reaction at ambient temperature for 17hr, then adding a 20% aqueous solution of Na2 CO3 thereto, stirring the mixture, subsequently extracting the mixture with ethyl acetate, concentrating and purifying the resultant extract.

4. 发明专利

JPH10101502A ANTIMICROBIAL AGENT 失效
公开(公告)号：JPH10101502A
公开(公告)日：1998-04-21
申请号：JP25294396
申请日：1996-09-25
申请人： CHICHIBU ONODA CEMENT CORP , SAGAMI CHEM RES
发明人： YAMAZAKI TAKESHI , TAKANO HIROYUKI , YAMADA AKIHIRO , KAMIMURA DAISUKE
IPC分类号： A01N37/06
摘要： PROBLEM TO BE SOLVED: To obtain an antimicrobial agent having an excellent antimicrobial effect to an adhering microorganism to ocean structural body, etc., and almost no toxicity to human and animal, by using palmitoleic acid as an active ingredient. SOLUTION: This antimicrobial agent contains palmitoleic acid as an active ingredient. Further, the acid is a 16C cis-lipophilic unsaturated fatty acid containing one double bond at the 9th carbon counting from a carboxylic terminal thereof, which is preferably obtained by e.g. culturing a diatom, preferably Navicula-sp. COCC9456 strain by using a mixture consisting of sea water and an inorganic compound as main components as a medium under approximately 20-25 deg.C temperature for several days to several weeks with an irradiation of visible rays, crushing the obtained cultured material with an added solvent such as ethanol and performing an extraction.

5. 发明专利

JPH09110835A 6-AZASPIRO(4,5)DECANE DERIVATIVE 失效
公开(公告)号：JPH09110835A
公开(公告)日：1997-04-28
申请号：JP27302395
申请日：1995-10-20
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , SHIYUU TOU , YAZAWA KAZUYOSHI , KANO MAYUMI , OOTANI YUIKO
IPC分类号： C07D221/20 , A61K31/445 , A61K35/56 , A61K35/618 , A61P29/00 , A61P43/00 , C07F7/10 , C07F7/18
摘要： PROBLEM TO BE SOLVED: To obtain a new 6-azaspiro[4,5]decane derivative, having inhibiting activities against cytoplasmic phospholipase A2 and useful as an antiinflammatory agent. SOLUTION: This 6-azaspiro[4,5]decane derivative is represented by formula I [R is H, a lower alkyl, a tri-lower alkylsilyl, an acyl or a sulfo-lower alkyl; R to R are each H, a lower alkyl, a tri-lower alkylsilyl or an acyl; X is a halogen; Y is O or NR (R is H, a lower alkyl, a tri-lower alkylsilyl or an acyl)], e.g. a compound represented by formula II. The compound represented by formula I is obtained by pulverizing and extracting a shucked shellfish which is shellfishes of the genus Pinna such as Pinna muricate Linnaeus in an organic solvent and further separating the extracted substance according to chromatography.

6. 发明专利

JPH08277219A CARCINOSTATIC AGENT AND HOMOCEREULIDE 失效
公开(公告)号：JPH08277219A
公开(公告)日：1996-10-22
申请号：JP31781195
申请日：1995-12-06
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , OU KIYOO , YAMADA KAORU , YAZAWA KAZUYOSHI
IPC分类号： C12P17/14 , A61K31/395 , A61P35/00 , C07D273/00 , C12R1/07
摘要： PURPOSE: To obtain a carcinostatic agent by using ingredients contained in a culture solution of a bacterium derived from the ocean, i.e., partially new cereulldes which are obtained from a culture solution of a microorganism belonging to the genus Bacillus as an active ingredient. CONSTITUTION: This carcinostatic agent contains cereulides of formula I (R is H or methyl) as an active ingredient. Homocereulide of formula II in the cereulides of formula I is especially a new compound. Since the cereulides of formula I have strong proliferating activities against a murine lymphocytic leukemic bacterium (P388) and a murine colonic cancer cell (Colon 26), a new type of the carcinostatic agent is obtained therefrom. The cereulides of formula I can simply be produced by using a microorganism. For example, Bacillus cereus SCRC-4h1-2 (deposited as FERM P-14746 with the National Institute of Bioscience and Human-Technology) is cited as the microorganism.

7. 发明专利

JPH07258168A 13-OXYINGENOL DERIVATIVE 失效
公开(公告)号：JPH07258168A
公开(公告)日：1995-10-09
申请号：JP7283994
申请日：1994-03-18
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , YAMADA KAORU
IPC分类号： A61K31/12 , A61P9/10 , A61P29/00 , A61P35/00 , C07C69/76
摘要： PURPOSE:To obtain a novel compound exhibiting a function to prevent production of a cell-binding molecule by human vein endothelial cell in a range without expressing cell toxicity and useful as a metastasis suppressing agent, and anti- inflammatory agent, a therapeutic medicine for arteriosclerosis, transplantation refusing reaction, chronic rheumatism, sarcoidosis, etc. CONSTITUTION:A compound of the formula I [R is a 2-18C acryl; R , R and R each is H or an aromatic acyl; R is H or a lower alkyl, with the proviso that at least one in R , R and R is an aromatic acyl], e.g. 13-O-dodecanoyl-3,20- di-O-benzoyl-13-oxyingenol. The compound of the formula I is obtained by hydrolyzing a 13-oxyingenol ester of the formula II and reacting the resultant 13-O- acyl-13-oxyingenol of the formula III with a halogenated aromatic acyl such as benzoyl chloride in the presence of a base such as 4-methylaminopyridine.

8. 发明专利

JPH07247291A OKADAIC ACID LACTONE DERIVATIVE 失效
公开(公告)号：JPH07247291A
公开(公告)日：1995-09-26
申请号：JP6441094
申请日：1994-03-09
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , YAMADA KAORU
IPC分类号： C07D519/00 , A61K31/365 , A61P35/00
摘要： PURPOSE:To provide a new okadaic acid derivative derived from okadaic acid, exhibiting an activity to inhibit the multiplication of a cancer cell P388 in vitro, expected as a masking substance for the highly poisonous okadaic acid, and useful as an antitumor agent, etc. CONSTITUTION:The new okadaic acid lactone derivative of formula I (R -R are H, a hydroxyl group-protecting group), having a multiplication-inhibiting activity against a murine lymphocytic leukemia cell P388 in vitro, useful as an antitumor agent, and having an use as a masking substance against highly poisonous okadaic acid. The compound is obtained by esterifying the carboxyl group of the okadaic acid of formula II (Me is methyl), treating the all secondary hydroxyl groups of the produced ester with a largely excessive silylating agent, treating the protected product with tetrabutylammonium chloride at a low temperature to remove the protecting group only on the 24-hydroxyl group, hydrolyzing the treated ester, subjecting the hydrolyzed groups to a Yamaguchi method to produce lactone groups, and subsequently removing the protecting groups.

9. 发明专利

JPH07228583A ABURATSUBOLACTAMS, ITS PRODUCTION MICROORGANISM, ITS PRODUCTION AND ANTI-INFLAMMATORY AGENT 失效
公开(公告)号：JPH07228583A
公开(公告)日：1995-08-29
申请号：JP27690194
申请日：1994-11-11
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , YAMADA KAORU , MASUZAWA YASUO , IJUIN YASUJI , KANO MAYUMI , YAZAWA KAZUYOSHI , TSUJI TOMOKO , PEI AKIYOSHI
IPC分类号： C12P17/18 , A61K31/40 , A61P29/00 , A61P35/00 , A61P43/00 , C07D487/08 , C12N1/20 , C12R1/465
摘要： PURPOSE:To obtain an aburatsubolactam substance having antitumor activity, activity to inhibit the O 2 production of human neutrophil, intracellular phospholipase A2 inhibiting action, action to inhibit the PAD production of human neutrophil, etc., and useful as medicines such as antitumor agent and antiinflammatory agent. CONSTITUTION:This aburatsubolactam substance is expressed by formula I to formula III (R and R ) are each independently H, a lower alkyl; R and R are each independently H, a hydroxyl-protecting group), e.g. aburatsubolactam A of formula IV, aburatsubolactam B of formula V and aburatsubolactam C of formula VI. The aburatsubolactam substances of formula I to formula III can be produced by culturing Streptomyces sp.SCRC-A20 preferably in a liquid medium under aerobic condition at preferably 25-45 deg.C) more preferably 30-7 deg.C) at pH6-9, preferably pH7-8 for 12hr to 10 days and extracting and purifying the cultured liquid. The microbial strain is a new strain obtained from Dolabella auricularia.

10. 发明专利

JPH06279489A NEW OKADAIC ACID DERIVATIVE 失效
公开(公告)号：JPH06279489A
公开(公告)日：1994-10-04
申请号：JP34570693
申请日：1993-12-22
申请人： SAGAMI CHEM RES
发明人： KAMIMURA DAISUKE , HAINO TAKEHARU , YAMADA KAORU
IPC分类号： A61K38/00 , A61P35/00 , A61P35/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/06
摘要： PURPOSE:To obtain the subject new derivative having anti-tumor activity, a strong in vitro proliferation inhibiting activity against mouse lymphatic leukemia cell and low toxicity and useful as a tumor treating agent, etc., by deriving from okadaic acid separated from a porifera. CONSTITUTION:The objective new okadaic acid derivative of formula II (R is amine residue of oligopeptide) having anti-tumor activity and low toxicity and useful as a tumor treating agent, etc., is obtained by derivatizing okadaic acid of formula I (Me is methyl) separated from Halichondria okada Kadota of a porifera to its p-nitrophenyl ester, adding glycylglycine, etc., to the ester, reacting the mixture under stirring in the presence of pyridine, triethylamine and water for 24 hours, subjecting the reaction solution to vacuum concentration after the completion of the reaction and purifying the concentrated product through silica gel chromatography.

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