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1. 发明专利

JPS59179092A 3(2-substituted-oxazol-5-yl)indole, its salt and their preparation 失效
标题翻译： 3（2-替代 - 奥沙唑-5-基）吲哚及其制备方法
公开(公告)号：JPS59179092A
公开(公告)日：1984-10-11
申请号：JP5495283
申请日：1983-03-29
申请人： Fujisawa Pharmaceut Co Ltd
发明人： UMEHARA KAZUYOSHI , YOSHIDA KEIZOU , KOUSAKA MASANOBU , IMANAKA HIROSHI
IPC分类号： C12P17/16 , A61K31/42 , A61P7/02 , C07D413/04
摘要： PURPOSE: A newly isolated microorganism in Streptoverticillium is cultured to produce the titled novel substance with an activity of inhibiting blood platelet coagulation.
CONSTITUTION: A novel strain, Streptoveticillium waxmanii No.30581 (FERM- 7013) has been isolated. The cultivation of the strain in a usual culture medium at 25W30°C for 50W100hr gives a novel compound, 3(2-substituted-oxazol-5-yl)indole or its salt. In the formula, R is propyl or butyl. The products have an action of inhibiting blood platelet coagulation.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：培养链霉菌新分离的微生物，制备具有抑制血小板凝血活性的标题新型物质。构成：已经分离了一种新型菌株，蜡状链霉菌（Streptoveticillium waxmanii）No.30581（FERM-7013）。在通常的培养基中在25-30℃下培养菌株50-100小时，得到新的化合物3（2-取代 - 恶唑-5-基）吲哚或其盐。在该式中，R是丙基或丁基。该产品具有抑制血小板凝血的作用。

2. 发明专利

JPS5973519A Preparation of swainsonine and immuno-regulating agent containing the same 失效
标题翻译：含有其的氨基磺酸和免疫调节剂的制备
公开(公告)号：JPS5973519A
公开(公告)日：1984-04-25
申请号：JP16116583
申请日：1983-08-31
申请人： Fujisawa Pharmaceut Co Ltd
发明人： HINO SUKEHIRO , NAKAHARA KUNIO , TERANO HIROSHI , HOSODA JIYUNJI , KOUSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI
IPC分类号： A61K31/435 , A61K36/06 , A61P37/00 , C07D471/04
CPC分类号： C07D471/04 , A61K31/435
摘要： PURPOSE: To obtain swainsonine useful as an immuno-regulating agent, by culturing a bacterial strain belonging to Metarhizium genus and capable of producing swainsonine (including novel bacterial strain), and separating the objective compound from the cultured product.
CONSTITUTION: A swainsonine-producing strain belonging to Metarhizium genus [including novel Metarhizium anisopliae F-3622 (FERM-P 7193) and sp F-3600 (FERM-P 7192)] is cultured in a nutrient liquid medium preferably under aerobic condition. Swainsonine of formula [chemical name; (1S, 2R, 8R, 8aR)-1,2,8-trihydroxyoctahydroindolidine] is separated from the cultured product by conventional means. It has been found that the known compound of formula and its salt have immuno-regulating activity. Accordingly, the compound of formula is useful as an immuno-regulating agent for the remedy of immuno-insufficiency (e.g. tumor, infectious diseases, autoimmune diseases, etc.).
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：获得可用作免疫调节剂的丝氨酸，通过培养属于Metarhizium属的细菌菌株并能够生产swainsonine（包括新菌株），并从培养产物中分离出目的化合物。构成：优选在需氧条件下，在营养液体培养基中培养属于Metarhizium属（包括新型Metarhizium anisopliae F-3622（FERM-P 7193）和sp F-3600（FERM-P 7192）]的产生swainsonine的菌株。化学名称：（1S，2R，8R，8aR）-1,2,8-三羟基辛烷二氢化茚]通过常规方法与培养产物分离。已经发现，已知的式及其盐的化合物具有免疫调节活性。因此，式的化合物可用作免疫功能不全（例如肿瘤，感染性疾病，自身免疫性疾病等）的补救的免疫调节剂。

3. 发明专利

JPS5753495A Fr-900201 substance, its preparation, and its use 失效
标题翻译： FR-900201物质，其制备及其用途
公开(公告)号：JPS5753495A
公开(公告)日：1982-03-30
申请号：JP12960080
申请日：1980-09-17
申请人： Fujisawa Pharmaceut Co Ltd
发明人： KOMORI TADAAKI , KOUSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI
IPC分类号： C12N1/20 , A61K35/74 , A61P31/04 , C07G11/00 , C12P1/06 , C12R1/465
摘要： NEW MATERIAL:The FR-900201 substance (and its salt) having the following physicochemical properties: elemental analysis (%) (hydrochloride), C 43.39, H 7.44, N 17.44, Cl 9.15, H
2 O 4.43; Molecular weight MW=666 [M+1=667 (FD mass spectrum method)]; molecular formula, C
28 H
46 N
10 O
9 ; melting point (hydrochloride), slowly decomposes at or above 205°C; [α]D
21 =-47.4° (C=0.4, water); solubility, easily soluble in water, soluble in methanol, etc., insoluble in acetone, chloroform, etc.; color reactions, positive to KMnO
4 , ninhydrin, Molish reactions, etc., negative to Tollens reagent, etc.; amphoteric substance; etc.
USE: Preventive and remedy for bacteriosis.
PROCESS: The compound is prepared by culturing Streptomyces lavendulae subsp. brasilicus No.1446 (FERM-P No.5649), if necessary in the presence of a defoaming agent, pref. at 30°C for 50W100hrs.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：具有以下物理化学性质的FR-900201物质（及其盐）：元素分析（％）（盐酸盐），C 43.39，H 7.44，N 17.44，Cl 9.15，H 2 O 4.43; 分子量MW = 666 [M + 1 = 667（FD质谱法）]; 分子式，C28H46N10O9; 熔点（盐酸盐），在205℃以上缓慢分解; αD 21 = - 47.4度（C = 0.4，水）; 溶解性好，易溶于水，溶于甲醇等，不溶于丙酮，氯仿等; 颜色反应，对KMnO4，茚三酮，莫利希反应等均呈阳性，对Tollens试剂为阴性等; 两性物质用途：预防和补救细菌病。方法：该化合物通过培养链霉菌（Streptomyces lavendulae subsp。）制备。如有必要，在消泡剂存在的情况下，首选的是Brasilicus No.1446（FERM-P No.5649）。在30℃下搅拌50-100小时。

4. 发明专利

JPS58212787A Substance ws6049, its preparation and anticancer agent containing the same as active constituent 失效
标题翻译：物质WS6049，其制备和含有相同活性成分的反应剂
公开(公告)号：JPS58212787A
公开(公告)日：1983-12-10
申请号：JP8900783
申请日：1983-05-19
申请人： Fujisawa Pharmaceut Co Ltd
发明人： KIYOTOO SUMIO , NISHIKAWA MOTOAKI , ISHIMI MORITA , TERANO HIROSHI , KOUSAKA MASANOBU , IMANAKA HIROSHI
IPC分类号： C07G11/00 , A61K35/74 , A61P31/04 , A61P35/00 , C12N1/20 , C12P1/04 , C12P1/06 , C12P13/00 , C12R1/03
CPC分类号： C12R1/03 , C12P1/06 , Y10S435/825
摘要： PURPOSE:To prepare novel substances WS6049-A and WS6049-B exhibiting the antimicrobial activity against various pathogenic germs and antitumor activity, by cultivating a microorganism belonging to the genus Actinomadura. CONSTITUTION:A microorganism, e.g. Actinomadura pulveraceus sp. nov. No. 6049 (ATCC39100), belonging to the genus Actinomadura, and having the ability to produce a substance WS6049-A or WS6049-B is inoculated into a culture medium and cultivated at 20-40 deg.C, preferably 25-30 deg.C, under aerobic conditions for about 50-100hr to collect the aimed substance WS6049-A or WS6049-B mainly from the resultant cultivated microbial cells.
摘要翻译：目的：通过培养属于Actinomadura属的微生物，制备出具有抗各种致病菌和抗肿瘤活性的抗微生物活性的新物质WS6049-A和WS6049-B。构成：微生物，例如放线菌 nov。属于Actinomadura属，并具有制备物质WS6049-A或WS6049-B的能力的第6049号（ATCC39100）接种到培养基中并在20-40℃，优选25-30度下培养。 C，在需氧条件下约50-100hr，主要从所得培养的微生物细胞中收集目标物质WS6049-A或WS6049-B。

5. 发明专利

JPS54147933A Anti-microbial agent 失效
标题翻译：抗生素代理
公开(公告)号：JPS54147933A
公开(公告)日：1979-11-19
申请号：JP1456879
申请日：1979-02-09
申请人： Fujisawa Pharmaceut Co Ltd
发明人： IMANAKA HIROSHI , NISHIDA MINORU
IPC分类号： C07D499/44 , A61K31/395 , A61K31/43 , A61K31/545 , A61K31/66 , A61P31/04 , C07F9/38
CPC分类号： A61K31/66 , C07F9/3808 , A61K31/395 , A61K31/43 , A61K31/545 , A61K33/42
摘要： PURPOSE: To provide an anti-microbial agent, containing a phosphonic acid derivative and a β-lactam antibiotic substance, and having a synergistic anti-microbial activity to various pathogenic microbials, even to the microbials to which separate application of the antibiotic substance is not efective.
CONSTITUTION: A composition containing (A) a phosphonic acid derivative of formula (R is lower alkanoyl; n is an integer of 2W5), e.g. 3-(N-formyl-N-hydroxyamino)-propyl phosphonic acid, and (B) a β-lactam antibiotic substance, such as penicillin-type, cepalosporin-type antibiotics, e.g. nocardin A. The weight ratio of (A) to (B) is 1:4 W 4:1, pref. 1:2 W 2:1. Application rate: 5W200 mg/kg/day, pref. 10W100 mg/kg/day.
COPYRIGHT: (C)1979,JPO&Japio
摘要翻译：目的：提供含有膦酸衍生物和β-内酰胺抗生素物质的抗微生物剂，并且对各种致病微生物具有协同的抗微生物活性，甚至是分离施用抗生素物质的微生物有效的构成：含有（A）膦酸衍生物（R为低级烷酰基; n为2-5的整数）的组合物，例如 3-（N-甲酰基-N-羟基氨基） - 丙基膦酸，和（B）β-内酰胺抗生素物质，例如青霉素型，头孢菌素型抗生素，例如。诺卡因A（A）与（B）的重量比为1:4〜4:1。 1：2 - 2：1。适用率：5-200 mg / kg / day， 10-100 mg / kg /天。

6. 发明专利

JPS59175891A 4-(2-formylaminovinyl)phenol, its salt and its preparation 失效
标题翻译： 4-（2-甲基氨基乙基）苯酚及其制备方法
公开(公告)号：JPS59175891A
公开(公告)日：1984-10-04
申请号：JP5325083
申请日：1983-03-28
申请人： Fujisawa Pharmaceut Co Ltd
发明人： UMEHARA KAZUYOSHI , YOSHIDA KEIZOU , KOUSAKA MASANOBU , IMANAKA HIROSHI
IPC分类号： C12P7/24 , A61K31/135 , A61K31/165 , A61P7/02 , C07C67/00 , C07C231/00 , C07C233/18
摘要： NEW MATERIAL:4-(2-Formylaminovinyl)phenol or a salt with it and an organic or inorganic base.
EXAMPLE: 4-(2-Formylaminovinyl)phenol.
USE: Useful as an inhibitor of blood platelet aggregation.
PREPARATION: A fungus such as Aspergillus fumigatus Fresenius No.5239 (FERM- P 6993) belonging to the genus Aspergillus, capable of producing 4-(2- formylaminovinyl)phenol at about 25W30°C for about 50W100hr, and 4-(2-formylaminovinyl)phenol or its salt is collected from its culture solution.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：4-（2-甲酰氨基乙烯基）苯酚或其盐与有机或无机碱。实施例：4-（2- Formylaminovinyl）苯酚。用途：可用作血小板聚集抑制剂。制备：一种真菌，例如属于曲霉属的烟曲霉Fresenius No.5239（FERM-P 6993），能够在约25-30℃下生产约50-100小时的4-（2-甲酰氨基乙烯基）苯酚，以及从其培养液中收集4-（2-甲酰基氨基乙烯基）苯酚或其盐。

7. 发明专利

JPS59152366A Novel nitroaliphatic compound, its preparation and use 失效
标题翻译：新型硝基化合物，其制备和使用
公开(公告)号：JPS59152366A
公开(公告)日：1984-08-31
申请号：JP25252083
申请日：1983-12-27
申请人： Fujisawa Pharmaceut Co Ltd
发明人： OKAMOTO MASANORI , ISHIMI MORITA , TAKASE SHIGEHIRO , UCHIDA ITSUROU , UMEHARA KAZUYOSHI , KOUSAKA MASANOBU , IMANAKA HIROSHI
IPC分类号： C07D207/416 , A61K31/15 , A61K31/16 , A61K31/215 , A61K31/26 , A61K31/445 , A61K31/495 , A61P7/02 , A61P9/08 , A61P9/12 , C07C43/23 , C07C45/41 , C07C57/03 , C07C205/51 , C07C233/02 , C07C233/09 , C07C233/20 , C07C233/49 , C07C235/28 , C07C249/04 , C07C251/32 , C07C251/38 , C07C251/40 , C07C251/60 , C07C255/10 , C07C255/19 , C07C255/23 , C07C255/64 , C07C291/12 , C07D207/40 , C07D207/404 , C07D295/18 , C07D295/185
CPC分类号： C07D207/404 , C07C43/23 , C07C45/41 , C07C57/03 , C07C205/44 , C07C205/51 , C07C255/00 , C07D295/185 , C07C47/21
摘要： NEW MATERIAL:The compound of formula I [R
1 is H, lower alkyl or lower alkoxyphenyl; R
2 and R
6 are H or lower alkyl; R
3 and R
5 are H or together form a single bond; R
4 is lower alkyl; R
7 is H, hydroxyiminomethyl, cyano, etc.; R
10 is H or lower alkyl which may have (esterified)carboxyl group] or its salt.
EXAMPLE: (E,E)-N-n-Butyl-4-ethyl-2,4-hexadienamide.
USE: Useful as a vasodilator, hypotensor, and antithrombic agent. It has muscle relaxing activity to smooth muscles resulting in the cardiovascular dilating and hypotensive activities, etc., and is effective to inhibit the coagulation of blood platelet.
PREPARATION: The compound of formula I
a can be prepared by reacting the compound of formula II or its salt with dinitrogen trioxide in the presence of an acid such as hydrochloric acid.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I化合物[R 1]为H，低级烷基或低级烷氧基苯基; R 2和R 6是H或低级烷基; R 3和R 5是H或一起形成单键; R 4是低级烷基; R 7是H，羟基亚氨基甲基，氰基等; R 10为H或可具有（酯化）羧基的低级烷基）或其盐。实施例：（E，E）-N-正丁基-4-乙基-2,4- hexadienamide。用途：作为血管扩张剂，低血压药和抗血栓药物有用。它具有平滑肌肉的肌肉松弛活性，导致心血管扩张和降血压活性等，并且有效抑制血小板的凝血。制备：式Ⅰa化合物可以通过式Ⅱ化合物或其盐与三氧化二氮在酸如盐酸的存在下反应来制备。

8. 发明专利

JPS5916884A Novel furans 失效
标题翻译：新的粉丝
公开(公告)号：JPS5916884A
公开(公告)日：1984-01-28
申请号：JP12659982
申请日：1982-07-19
申请人： Fujisawa Pharmaceut Co Ltd
发明人： OKAMOTO MASANORI , UCHIDA ITSUROU , UMEHARA KAZUYOSHI , KOUSAKA MASANOBU , IMANAKA HIROSHI
IPC分类号： A61K31/34 , A61K31/341 , A61P27/02 , A61P27/12 , C07C43/166 , C07D303/22 , C07D307/33 , C07D307/42 , C07D307/52 , C07D307/54 , C07D307/58 , C07D307/60 , C07D309/12 , C12P17/04
CPC分类号： C07D303/22 , C07C43/166 , C07D307/33 , C07D307/58 , C07D307/60 , C07D309/12 , C12P17/04 , C12R1/645 , Y02P20/55
摘要： NEW MATERIAL:A furan of formula I [A is lower alkylene; R
1 is carboxy, hydroxy, lower alkoxycarbonyl, lower alkoxycarbonylamino, lower alkanoyloxy; R
2 is H, halogen, halo-lower-alkyl; R
3 is H, halogen; R
4 is H, hydroxy, carboxy, lower alkoxy, lower alkanoyloxy; R
5 is H, halogen, or R
4 and R
5 incorporate to form =CH
2 ; F is number of double bonds, 0 or 1, n is 0 in case of F=1] or its salt.
EXAMPLE: 5-(3-Benzyloxypropyl)-2-oxo-4-phenyltetrahydro-3-furancarboxylic acid.
USE: A remedy of diabetic cataract.
PREPARATION: For example, the reaction of a compound of formula II (R
1
a is hydroxy-protecting group) with malonic acid in the presence of a base gives a compound of formula I .
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I的呋喃[A为低级亚烷基; R 1是羧基，羟基，低级烷氧基羰基，低级烷氧基羰基氨基，低级烷酰氧基; R 2是H，卤素，卤代低级烷基; R 3是H，卤素; R 4是H，羟基，羧基，低级烷氧基，低级烷酰氧基; R 5是H，卤素或R 4和R 5并入以形成= CH 2; F是双键数，0或1，在F = 1]的情况下n为0或其盐。实施例5-（3-苄氧基丙基）-2-氧代-4-苯基四氢-3-呋喃羧酸。用途：糖尿病性白内障的补救措施。制备：例如，式II化合物（R 1a是羟基保护基）与丙二酸在碱的存在下的反应得到式I化合物。

9. 发明专利

JPS5746917A Antibacterial agent 失效
标题翻译：抗菌剂
公开(公告)号：JPS5746917A
公开(公告)日：1982-03-17
申请号：JP12281280
申请日：1980-09-03
申请人： Fujisawa Pharmaceut Co Ltd
发明人： IMANAKA HIROSHI , NISHIDA MINORU
IPC分类号： A61K31/47 , A61K31/505 , A61K31/63 , A61K31/65 , A61K31/66 , A61K31/685 , A61P31/04
摘要： PURPOSE: An antibacterial agent having synergistic actions on bacteria, effective for preventing and remedying infections diseases, having low toxicity, obtained by blending an antibacterial substance with a phosphonic acid derivative.
CONSTITUTION: The titled agent comprising a phosphonic acid derivative [e.g., 3-(N-formyl-N-hydroxyamino)propylphosphonic acid] shown by the formula (R is lower alkanoyl; n is 2W5) or its pharmaceutically accetable salt and an antibacterial substance selected from the group consisting of nalidixic acid, tetracycline, trimethorium, and sulfamethoxazole or its pharmaceutically acceptable salt. The blending ratio of the phosphonic acid derivative to the antibacterial substance is preferably 4:1W1:4 by weight, and it is sufficiently 1:1 in common cases. The agenst is also effective against bacteria on which the antibacterial substances alone have no effect or only a little effect. A dose is in a range of 5W200mg/kg/day, preferably 10W 100mg/kg/day.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：目的：通过将抗菌物质与膦酸衍生物混合而获得的，对细菌具有协同作用的抗菌剂，其有效预防和治疗感染性疾病，毒性低。构成：由式（R为低级烷酰基; n为2-5）表示的膦酸衍生物[例如3-（N-甲酰基-N-羟基氨基）丙基膦酸]或其药学上可食用的盐和选自萘啶酸，四环素，三甲基铵和磺胺甲恶唑或其药学上可接受的盐的抗菌物质。膦酸衍生物与抗菌物质的配合比例优选为4:1〜1:4，通常情况下为1：1。对于单独使用抗菌物质没有影响或仅有一点影响的细菌，其效果也是有效的。剂量范围为5-200mg / kg /天，优选为10〜100mg / kg /天。

10. 发明专利

JPS59148745A Novel acylglutamyl lysine derivative 失效
标题翻译：新型ACYLGLUTAMYL LYSINE DERIVATIVE
公开(公告)号：JPS59148745A
公开(公告)日：1984-08-25
申请号：JP2040883
申请日：1983-02-08
申请人： Fujisawa Pharmaceut Co Ltd
发明人： KURODA YOSHIO , IGUCHI HIDEKO , KOUSAKA MASANOBU , AOKI HATSUO , IMANAKA HIROSHI , KITAURA YOSHIHIKO , NAKAGUCHI OSAMU , HENMI KEIJI , ARAYA MATSUHIKO , TAKENO SHIYUUICHI , OKADA TATSU , TANAKA HIROKAZU , HASHIMOTO SHINJI
IPC分类号： A61K38/00 , A61P31/04 , A61P37/04 , C07K5/02
摘要： NEW MATERIAL:An acylglutamyl lysine derivative shown by the formula I (R
1 is palmitoyl, or behenoyl; R
2 is H, or benzyl; R
3 is H, or benzyloxycarbonyl) and its salt.
EXAMPLE: Behenoyl-γ-D-Glu(α-OH)-L-Lys-D-AlaOH.
USE: Having improved preventing effect on infectious diseases and useful as a drug. Useful as a remedy for infectious diseases caused by pathogenic bacteria, especially by Gram-negative, Gram-positive bacteria and molds.
PREPARATION: A compound shown by the formula II is directly reacted with a compound shown by the formula III in the presence of a condensation agent such as N,N-dicyclohexylcarbodiimide, etc., to give a compound shown by the formula I . The compound shown by the formula II and the compound shown by the formula III are novel compounds, the compound shown by the formula II is synthesized from a compound shown by the formula IV and a compound shown by the formula V, and the compound shown by the formula III from the compound shown by the formula IV and a compound shown by the formula VI.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新物质：由式I表示的酰基谷氨酰赖氨酸衍生物（R 1为棕榈酰基或山嵛酰基; R 2为H或苄基; R 3为H或苄氧基羰基）及其盐。实施例：山嵛酰-γ-D-GLU（α-OH）-L-赖氨酸D-AlaOH。用途：改善对传染病的预防作用，有益于药物。可用作病原菌引起的感染性疾病的补救措施，特别是革兰氏阴性，革兰氏阳性菌和霉菌。制备：式II化合物在缩合剂例如N，N-二环己基碳二亚胺等存在下，与式Ⅲ化合物直接反应，得到式Ⅰ所示的化合物。由式II表示的化合物和由式III表示的化合物是新化合物，由式IV所示的化合物和式V所示的化合物合成式II所示的化合物，由式IV表示的化合物的式III化合物和式VI所示的化合物。

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