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1. 发明授权

US3888843A 4-carbamoyl-1-' -d-ribofuranosylimidazolium-5-olate 失效
标题翻译： 4-羧基-1'-D-吡喃木糖基咪唑羧酸
公开(公告)号：US3888843A
公开(公告)日：1975-06-10
申请号：US36579473
申请日：1973-06-12
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , ANDO TAKUJI , TSUJINO MASATOSHI , TAKADA MASAKI , YOSHIZAWA MUNETOSHI , MATSUDA TETSUO , HAYASHI MITSUO
IPC分类号： C07H19/052 , C07D51/52
CPC分类号： C07H19/052 , Y10S435/911
摘要： Bredinin, which is 4-carbamoyl-1- Beta -Dribofuranosylimidazolium-5-olate, has immunosuppressive activity. For its production, microorganism Eupenicillium brefeldianum is cultivated in a nutrient medium and the immunosuppressive agent is isolated therefrom.

2. 发明专利

DE3875025D1 未知
公开(公告)号：DE3875025D1
公开(公告)日：1992-11-05
申请号：DE3875025
申请日：1988-07-22
申请人： TOYO JOZO KK
发明人： YAMAMOTO NAKAYUKI , SAKAKIBARA HIDEO , MIZUNO KIMIO
IPC分类号： A61K9/00 , A61K47/12 , A61K47/18 , A61K47/26 , A61K9/06 , A61K47/00
摘要： A nasal administration powder composition containing a physiologically active peptide as an active ingredient can be efficiently absorbed through nasal mucosa by the addition of a water-soluble organic acid as an absorption promoter. This composition may further contain a diluent. The water-soluble organic acid used as absorption promoter includes, for example, at least one of succinic acid, tartaric acid, citric acid, fumaric acid, maleic acid, malonic acid, glutaric acid, adipic acid, malic acid, L-glutamic acid, L-aspartic acid, gluconic acid and glucuronic acid.

3. 发明专利

CA1041446A ANTIBIOTICS ACULEACIN GROUP 未知
公开(公告)号：CA1041446A
公开(公告)日：1978-10-31
申请号：CA222766
申请日：1975-03-21
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , MATSUDA TETSUO , ASANO KATSUMI , YAGI AKIRA , TAKADA MASAKI , SAITO TETSU , TORIYA MINORU , MATSUURA KAZUO , SATOI SHUZO
IPC分类号： C12D9/00
摘要： A novel antibiotics ative against pathogenic yeasts and fungi designated Aculeacin group antibiotics -Aculeacin-A, -B, -C, -D, -E, -F, and -G --are producted from cultured broth of Asperqillus aculeatus FERM-P 2324.

4. 发明专利

DK138340B 未知
公开(公告)号：DK138340B
公开(公告)日：1978-08-14
申请号：DK83375
申请日：1975-03-03
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , MATSUDA TETSUO , ASANO KATSUMI , YAGI AKIRA , TAKADA MASAKI , TORIYA TETSU , TORIYA MINORU , MATSUURA KAZUO , SATOI SHUZO
IPC分类号： A61K36/06 , A01N63/04 , C07G11/00 , C12P1/02 , C12P21/00 , C12D9/04
摘要： 1495839 Aculeacin antibiotics TOYO JOZO KK 5 March 1975 [6 March 1974] 9118/75 Heading C3H The invention is directed to an antibiotic substance selected from the groups consisting of aculeacin-A, aculeacin-B, aculeacin-C, aculeacin-D, aculeacin-E, aculeacin-F and aculeacin-G. The aculeacins are characterized by the following physico-chemical properties (1) Elementary analysis (2) Molecular weight (3) Molecular formula (4) Melting point (5) Specific rotation [α] 24 (C= 1À0, methanol) D (6) Ultra violet spectrum in methanol or KOH-methanol as indicated in Figs. 1-4, 6-17 (these figures are not shown) (7) Infra-red absorption spectrum (KBr tablet) as indicated in Fig. 5 and 18-23 (these figures are not shown) (8) Nuclear magnetic resonance spectrum as indicated in Figs. 24-29 (these figures are not shown) (9) Colour reactions (10) Solubility Soluble in lower alcohols Slightly soluble in ethyl acetate and water Insoluble in acetone, chloroform, n-hexane and petroleum ether (11) Aculeacins are decomposed at an alkaline pH; they cannot be transferred from butanol to water at pH 2-9 (12) Colour: white crystalline powder (13) Rf value Carrier: silica gel sheet Solvent A: ethylacetate-isopropanol-water (10 : 2 : 1) B: chloroform-methanol (10 : 3) C: ethylacetate-methanol-water (20 : 4 : 1) D: ethylacetate-n-butanol (3 : 1) Developer: iodine Bioassay using Candida albicous (Aculeacin-A only) (14) Amino acid composition Aculeacins are hydrolysed with hydrochloric acid and the ninhydrin positive components are analysed, the results being indicated in Figs. 30 and 32 (these figures are not shown) and the table below V=violet (strong absorption at 570 mÁ), Y=yellow (strong absorption at 440 mÁ), UK=unknown amino acid, Thr=L-threonine, Pro=proline, + = positive peak, - =no peak, Tr=trace peak. The antibiotics are prepared by culturing in an appropriate medium a microorganism designated Aspergillus aculeatus M4214 FERM-P 2324.

5. 发明专利

DK134118B 未知
公开(公告)号：DK134118B
公开(公告)日：1976-09-13
申请号：DK263973
申请日：1973-05-14
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , ANDO TAKUJI , TAKADA MASAKI , HAYASHI MITSUO , TSUJINO MASATOSHI , YOSHIZAWA MUNETOSHI , MATSUDA TETSUO
IPC分类号： C12D13/00

6. 发明专利

CH595442A5 未知
公开(公告)号：CH595442A5
公开(公告)日：1978-02-15
申请号：CH286975
申请日：1975-03-06
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , MATSUDA TETSUO , ASANO KATSUMI , YAGI AKIRA , TAKADA MASAKI , SAITO TETSU , TORIYA MINORU , MATSUURA KAZUO , SATOI SHUZO
IPC分类号： A01N63/04 , A61K36/06 , C07G11/00 , C12P1/02 , C12P21/00 , C12D9/04
摘要： 1495839 Aculeacin antibiotics TOYO JOZO KK 5 March 1975 [6 March 1974] 9118/75 Heading C3H The invention is directed to an antibiotic substance selected from the groups consisting of aculeacin-A, aculeacin-B, aculeacin-C, aculeacin-D, aculeacin-E, aculeacin-F and aculeacin-G. The aculeacins are characterized by the following physico-chemical properties (1) Elementary analysis (2) Molecular weight (3) Molecular formula (4) Melting point (5) Specific rotation [α] 24 (C= 1À0, methanol) D (6) Ultra violet spectrum in methanol or KOH-methanol as indicated in Figs. 1-4, 6-17 (these figures are not shown) (7) Infra-red absorption spectrum (KBr tablet) as indicated in Fig. 5 and 18-23 (these figures are not shown) (8) Nuclear magnetic resonance spectrum as indicated in Figs. 24-29 (these figures are not shown) (9) Colour reactions (10) Solubility Soluble in lower alcohols Slightly soluble in ethyl acetate and water Insoluble in acetone, chloroform, n-hexane and petroleum ether (11) Aculeacins are decomposed at an alkaline pH; they cannot be transferred from butanol to water at pH 2-9 (12) Colour: white crystalline powder (13) Rf value Carrier: silica gel sheet Solvent A: ethylacetate-isopropanol-water (10 : 2 : 1) B: chloroform-methanol (10 : 3) C: ethylacetate-methanol-water (20 : 4 : 1) D: ethylacetate-n-butanol (3 : 1) Developer: iodine Bioassay using Candida albicous (Aculeacin-A only) (14) Amino acid composition Aculeacins are hydrolysed with hydrochloric acid and the ninhydrin positive components are analysed, the results being indicated in Figs. 30 and 32 (these figures are not shown) and the table below V=violet (strong absorption at 570 mÁ), Y=yellow (strong absorption at 440 mÁ), UK=unknown amino acid, Thr=L-threonine, Pro=proline, + = positive peak, - =no peak, Tr=trace peak. The antibiotics are prepared by culturing in an appropriate medium a microorganism designated Aspergillus aculeatus M4214 FERM-P 2324.

7. 发明专利

CA993390A IMMUNOSUPPRESSIVE AGENT FROM EUPENICILLIUM BREFELDIANUM 未知
公开(公告)号：CA993390A
公开(公告)日：1976-07-20
申请号：CA172325
申请日：1973-05-23
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , ANDO TAKUJI , TAKADA MASAKI , HAYASHI MITSUO , TSUJINO MASATOSHI , YOSHIZAWA MUNETOSHI , MATSUDA TETSUO

8. 发明专利

DE2509820A1 未知
公开(公告)号：DE2509820A1
公开(公告)日：1976-02-05
申请号：DE2509820
申请日：1975-03-06
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , MATSUDA TETSUO , ASANO KATSUMI , YAGI AKIRA , TAKADA MASAKI , SAITO TETSU , TORIYA MINORU , MATSUURA KAZUO , SATOI SHUZO
IPC分类号： A01N63/04 , A61K36/06 , C07G11/00 , C12P1/02 , C12P21/00 , C07H11/00
摘要： 1495839 Aculeacin antibiotics TOYO JOZO KK 5 March 1975 [6 March 1974] 9118/75 Heading C3H The invention is directed to an antibiotic substance selected from the groups consisting of aculeacin-A, aculeacin-B, aculeacin-C, aculeacin-D, aculeacin-E, aculeacin-F and aculeacin-G. The aculeacins are characterized by the following physico-chemical properties (1) Elementary analysis (2) Molecular weight (3) Molecular formula (4) Melting point (5) Specific rotation [α] 24 (C= 1À0, methanol) D (6) Ultra violet spectrum in methanol or KOH-methanol as indicated in Figs. 1-4, 6-17 (these figures are not shown) (7) Infra-red absorption spectrum (KBr tablet) as indicated in Fig. 5 and 18-23 (these figures are not shown) (8) Nuclear magnetic resonance spectrum as indicated in Figs. 24-29 (these figures are not shown) (9) Colour reactions (10) Solubility Soluble in lower alcohols Slightly soluble in ethyl acetate and water Insoluble in acetone, chloroform, n-hexane and petroleum ether (11) Aculeacins are decomposed at an alkaline pH; they cannot be transferred from butanol to water at pH 2-9 (12) Colour: white crystalline powder (13) Rf value Carrier: silica gel sheet Solvent A: ethylacetate-isopropanol-water (10 : 2 : 1) B: chloroform-methanol (10 : 3) C: ethylacetate-methanol-water (20 : 4 : 1) D: ethylacetate-n-butanol (3 : 1) Developer: iodine Bioassay using Candida albicous (Aculeacin-A only) (14) Amino acid composition Aculeacins are hydrolysed with hydrochloric acid and the ninhydrin positive components are analysed, the results being indicated in Figs. 30 and 32 (these figures are not shown) and the table below V=violet (strong absorption at 570 mÁ), Y=yellow (strong absorption at 440 mÁ), UK=unknown amino acid, Thr=L-threonine, Pro=proline, + = positive peak, - =no peak, Tr=trace peak. The antibiotics are prepared by culturing in an appropriate medium a microorganism designated Aspergillus aculeatus M4214 FERM-P 2324.

9. 发明专利

DE2326916A1 Bredinine - antiviral agent and immunosuppressant 未知
公开(公告)号：DE2326916A1
公开(公告)日：1974-12-19
申请号：DE2326916
申请日：1973-05-23
申请人： TOYO JOZO KK
发明人： MIZUNO KIMIO , ANDO TAKUJI , TAKADA MASAKI , HAYASHI MITSUO , TSUJINO MASATOSHI , YOSHIZAWA MUETOSHI , YOSHIZAWA MUNETOSHI , MATSUDA TETSUO
IPC分类号： C07H19/052 , C07D49/36
摘要： The compound of formula (I) is new: (I), called bredinine, is an immunosuppressive and antiviral agent of low toxicity. It also has weak anti-microbial activity (e.g. against Candida albicans) and antitumour activity. (I) is obtd. by culturing Eupenicillium brefeldianum NRRL 5734 most pref. under submerged, aerobic conditions. The nutrient medium is conventional, temp. is 26-30 degrees C and cultivation time typically 40-70 hrs. (I) is pref. recovered from the liquid phase by absorption on a strong basic ion-exchange resin, elution with acid and opt. further purification by treatment with Sephadex DEAE A-25.

10. 发明专利

JPH01157943A D-ALDOSTATIN AND PRODUCTION THEREOF 失效
公开(公告)号：JPH01157943A
公开(公告)日：1989-06-21
申请号：JP31564287
申请日：1987-12-14
申请人： TOYO JOZO KK
发明人： YAGINUMA SATOSHI , ASAHI TERU , MIZUNO KIMIO
IPC分类号： C07C231/00 , A61K31/195 , A61P3/08 , A61P3/10 , A61P13/02 , A61P15/00 , A61P25/00 , A61P27/02 , A61P27/12 , A61P43/00 , C07C67/00 , C07C231/02 , C07C233/47
摘要： NEW MATERIAL:D-aldostatin of formula I or its salt. USE:A medicine. It is an aldose reductase inhibiting substance having an activity twice as high as that of L-aldostatin and having excellent safety. It is useful as a preventive or remedy for cataract, retinopathy, neuropathy, rhinitis, circulatory disorder, etc., which are diabetic complicates. It can be used in the form of peroral drug, eye drop, nasal drop, suppository, etc., and is administered at a rate of 100gamma-500mg per dose. PREPARATION:The compound of formula I can be produced by reacting D- tyrosine of formula II with H2O2 and a peroxidase under alkaline condition and diformylating the resultant DD-bityrosine of formula III with a mixed formulation agent (e.g., formic acid-acetic anhydride) in a solvent or in the absence of solvent preferably at -20-+50 deg.C for 30min-5hr.

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