专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明专利

JPS5931797A Novel 1-substituted imidazole nucleoside and its preparation 失效
标题翻译：新一代取代的咪唑烷核苷及其制备
公开(公告)号：JPS5931797A
公开(公告)日：1984-02-20
申请号：JP14316282
申请日：1982-08-18
申请人： Sumitomo Chem Co Ltd
发明人： TARUMI YUUZOU , ATAMI TOSHIO , YOSHIDA NOBORU
IPC分类号： C07H19/052 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61P17/16 , A61P37/06 , C07H19/04
摘要： NEW MATERIAL:The compound of formula I (R is β-D-glucopyranosyl, β-D- galactopyranosyl, 2-acetamido-2-deoxy-β-D-glucopyranosyl, α-L-rhamnopyranosyl, β-D-ribopyranosyl, β-D-arabinofuranosyl, etc.).
EXAMPLE: 4- Carbamoyl-1-( 2,3,4,6- tetra-O- acetyl-β-D- galactopyranosyl)-imidazolium- 5-olate (I:R=2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl).
USE: Immunosuppressive agent and antitumor agent.
PROCESS: The 4-carbamoylimidazolium-5-olate of formula II or its trimethylsilyl derivative is made to react with the glycose derivative of formula R'-Z (R' is β-D-glucopyranosyl, β-D-mannopyranosyl, etc.; Z is halogen, lower alkoxy, etc.) in the presence of stannic chloride and a condensation agent to obtain the compound of formula III, which is if necessary deacylated under basic condition.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新物质：式I化合物（R为β-D-吡喃葡萄糖基，β-D-吡喃半乳糖基，2-乙酰氨基-2-脱氧-β-D-吡喃葡萄糖基，α-L-鼠李糖吡喃糖基，β-D-吡喃半乳糖基，β D-阿拉伯呋喃糖基等）。实施例：4-氨甲酰基-1-（2,3,4,6-四-O-乙酰基-β-D-吡喃半乳糖基） - 咪唑鎓-5-醇酸酯（I：R = 2,3,4,6-四 - -O-乙酰基-β-D-吡喃半乳糖基）。用途：免疫抑制剂和抗肿瘤剂。方法：使式II的4-氨基甲酰基咪唑鎓-5-醇酸酯或其三甲基甲硅烷基衍生物与式R'-Z（R'是β-D-吡喃葡萄糖基，β-D-吡喃甘露糖基等）的糖苷衍生物反应。 Z是卤素，低级烷氧基等）在氯化锡和缩合剂的存在下，得到式III化合物，如果需要，在碱性条件下脱酰基。

2. 发明专利

JPS58203974A Optically active imidazolylpropanediol derivative and its preparation 失效
标题翻译：光学有效的咪唑并吡喃衍生物及其制备
公开(公告)号：JPS58203974A
公开(公告)日：1983-11-28
申请号：JP5332783
申请日：1983-03-28
申请人： Sumitomo Chem Co Ltd
发明人： SAJI KITAROU , SATOU RENZOU , AONO SHIYUNJI , ICHINOSE KATSUAKI , OKUDA TAKAO , ATAMI TOSHIO
IPC分类号： C07D233/60 , A61K31/415 , A61P31/04 , A61P31/10
摘要： NEW MATERIAL:(R)-2-(2,4-Dichlorophenyl)-1-(imidazol-1-yl)-2,3-propanediol of formula I .
USE: A synthetic intermediate of optically active imidazolylalkylthiopropanol derivative having strong mycostatic activity.
PROCESS: The optically active diol derivative of formula I can be prepared e.g. by (1) reacting the racemic imidazolyldiol derivative of formula II with an optically active carboxylic acid or its reactive derivative, preferably the optically active carboxylic acid of formula III to obtain the 1:1 mixture of two kinds of diastereomer esters, (2) separating the objective ester from the diastereomer mixture by chromatography, fractional recrystallization, etc., and (3) hydrolyzing the resultant ester.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I的（R）-2-（2,4-二氯苯基）-1-（咪唑-1-基）-2,3-丙二醇。用途：具有很强的静电活性的光学活性咪唑基烷基硫代丙醇衍生物的合成中间体。方法：式I的光学活性二醇衍生物可以例如制备。通过（1）使式II的外消旋咪唑烷二醇衍生物与光学活性羧酸或其反应性衍生物，优选式III的光学活性羧酸反应，得到两种非对映体酯的1:1混合物，（2）分离通过色谱法，分级重结晶等来自非对映异构体混合物的目标酯，和（3）水解所得酯。

3. 发明专利

JPS57120577A Novel imidazole derivative 失效
标题翻译：新咪唑衍生物
公开(公告)号：JPS57120577A
公开(公告)日：1982-07-27
申请号：JP758281
申请日：1981-01-20
申请人： Sumitomo Chem Co Ltd
发明人： TANAKA YOSHIHIRO , ATAMI TOSHIO , YOSHIDA NOBORU
IPC分类号： C07D233/90 , A61K31/415 , A61P35/00 , A61P37/06 , A61P37/08
摘要： NEW MATERIAL:A compound of formulaI[R is formula II (R
1 , R
2 are alkyl, phenyl), formula III (n is 0W3), formula IV (X is imino, alkyl-substituted imino, O); Y is O, S]and its acid adduct.
EXAMPLE: 5-Carbamoyl-1H-imidazol-4-yl dimethylcarbamate.
USE: Carcinostatic agent.
PREPARATION: The reaction between 4-carbamoyl-imidazolium-5-oleate or its reactive derivative and a carboxylic or thiocarboxylic acid of formula V or its reactive derivative gives the compound of formulaI. The reaction temperature is preferably -60W60°C.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式Ⅰ化合物[R为式Ⅱ（R1，R2为烷基，苯基），式Ⅲ（n为0-3），式Ⅳ（X为亚氨基，烷基取代的亚氨基，O） Y为O，S]及其酸加成物。实施例：5-氨基甲酰基-1H-咪唑-4-基二甲基氨基甲酸酯。用途：致癌剂。制备：4-氨基甲酰基 - 咪唑鎓-5-油酸酯或其反应性衍生物与式V的羧酸或硫代羧酸或其反应性衍生物之间的反应得到式I化合物。反应温度优选为-60-60℃。

4. 发明专利

JPS5925390A Novel 1-substituted imidazole-4-carboxamide 失效
标题翻译：新一代取代的咪唑-4-羧酰胺
公开(公告)号：JPS5925390A
公开(公告)日：1984-02-09
申请号：JP13545582
申请日：1982-08-02
申请人： Sumitomo Chem Co Ltd
发明人： TARUMI YUUZOU , ATAMI TOSHIO , YOSHIDA NOBORU , FUKUI MASARU
IPC分类号： C07D409/04 , A61K31/415 , A61P31/12 , A61P35/00 , A61P37/06 , C07D405/04
摘要： NEW MATERIAL:A Compound of formula I (A is O, S, sulfinyl or sulfonyl; B is lower alkylene; R is H, hydroxymethyl, acyloxymethyl, alkoxycarbonyl or carboxyl).
EXAMPLE: 4-Carbamoyl-1-tetrahydrofurylimidazolium-5-oleate.
USE: Useful as an antitumor agent having powerful inhibitory action on the multiplication of tumorous cells with very low toxicity, and orally administrable.
PROCESS: 4-Carbamoylimidazolium-5-oleate (or a reactive derivative thereof) is reacted with a compound of formula II (R' is H, acyloxymethyl or alkoxycarbonyl; Y is halogen, lower alkoxyl, trimethylsilyloxy or aroyloxy, etc.) if necessary in the presence of a condensing agent, e.g. trimethylsilyl trifluoromethanesulfonate, and if necessary further hydrolyzed.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I化合物（A为O，S，亚磺酰基或磺酰基; B为低级亚烷基; R为H，羟甲基，酰氧基甲基，烷氧基羰基或羧基）。实施例：4-氨基甲酰基-1- tetrahydrofurylimidazolium-5油酸酯。用途：作为具有非常低毒性的肿瘤细胞增殖具有强大抑制作用的抗肿瘤剂，可口服给药。方法：如果需要，将4-氨基甲酰基咪唑鎓-5-油酸酯（或其活性衍生物）与式II化合物（R'是H，酰氧基甲基或烷氧基羰基; Y是卤素，低级烷氧基，三甲基甲硅烷氧基或芳酰氧基等）在冷凝剂的存在下，例如三氟甲磺酸三甲基甲硅烷基酯，如果需要，进一步水解。

5. 发明专利

JPS5748971A Novel alkylimidazole derivative 失效
标题翻译：新的阿基咪唑衍生物
公开(公告)号：JPS5748971A
公开(公告)日：1982-03-20
申请号：JP12497480
申请日：1980-09-08
申请人： Sumitomo Chem Co Ltd
发明人： ATAMI TOSHIO , TARUMI YUUZOU
IPC分类号： C07D233/90 , A61K31/415 , A61P29/00
摘要： NEW MATERIAL:An imidazole derivative shown by the formula I(R
1 is lower alkyl or aralkyl; R
2 and R
3 are H, lower alkyl or aralkyl) and its salt.
EXAMPLE: 5-Carbamoyl-1-methylimidazolium-4-oleate.
USE: An anti-inflammatory agent. Having improved inhibiting actions on calabar swelling.
PROCESS: An amine shown by the formula R
1 -NH
2 is reacted with α-bromomalonamide shown by the formula II to give an α-aminomalonamide derivative shown by the formula III, which is reacted with an ortho-formate in the presence or absence of a catalyst to give a compound shown by the formula IV. If, necessary, this compound is reacted with an alkylating agent to give a compound shown by the formula V(R'
2 is lower alkyl or aralkyl), and optionally treated with an alkali to give a rearranged reaction product shown by the formula VI.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：由式I表示的咪唑衍生物（R1为低级烷基或芳烷基; R2和R3为H，低级烷基或芳烷基）及其盐。实施例：5-氨基甲酰基-1-甲基咪唑-4-油酸酯。用途：抗炎剂。改善对颅骨肿胀的抑制作用。方法：式R 1 -NH 2所示的胺与由式II表示的α-溴代马来酰胺反应，得到式III表示的α-氨基马来酰亚胺衍生物，其与原甲酸酯反应，在存在或不存在下催化剂，得到式IV所示的化合物。如果必要的话，该化合物与烷基化剂反应，得到式V所示的化合物（R'2是低级烷基或芳烷基），任选地用碱处理，得到式VI所示重排的反应产物。

6. 发明专利

JPS60193997A New cyanoimidazole ribonucleoside derivative and its preparation 失效
标题翻译：新的氰基亚胺唑酮衍生物及其制备
公开(公告)号：JPS60193997A
公开(公告)日：1985-10-02
申请号：JP4956384
申请日：1984-03-14
申请人： Sumitomo Chem Co Ltd
发明人： TARUMI YUUZOU , ATAMI TOSHIO , FUKUI MASARU
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61P35/00 , C07H19/052
CPC分类号： C07H19/052 , Y02P20/55
摘要： NEW MATERIAL:A compound of formula I (R
1 , R
2 , R
3 are H, protecting groups for hydroxyls) and its salt.
EXAMPLE: 4-Cyano-1-β-D-ribofuranosylimodazolium-5-oleate.
USE: A carcinostatic agent.
PREPARATION: The deprotection of a compound of formula II (R is protecting group for hydroxyl) such as 4-carbamoyl-1-(2,3,5-tri-O-acetyl)-β-D-ribofuranosyl)- imidazolium-5-oleate is carried out using phosphorus oxychloride, preferably by about 2mol amount to the compound for 2W3hr to give the compound of completely or partially deprotection.
COPYRIGHT: (C)1985,JPO&Japio
摘要翻译：新材料：式Ⅰ化合物（R1，R2，R3为H，羟基保护基）及其盐。实施例：4-氰基-1-β-D-呋喃核糖基咪唑鎓-5-油酸酯。使用：制癌剂。制备：式II化合物（R是羟基保护基）如4-氨基甲酰基-1-（2,3,5-三-O-乙酰基）-β-D-呋喃核糖基） - 咪唑鎓-5 - 油酸酯使用磷酰氯进行，优选用约2mol量的化合物进行2-3小时，得到完全或部分去保护的化合物。

7. 发明专利

JPS5936695A Novel imidazole nucleoside and its preparation 失效
标题翻译：新型咪唑烷核苷及其制备方法
公开(公告)号：JPS5936695A
公开(公告)日：1984-02-28
申请号：JP14531482
申请日：1982-08-20
申请人： Sumitomo Chem Co Ltd
发明人： TARUMI YUUZOU , ATAMI TOSHIO , YOSHIDA NOBORU
IPC分类号： C07H19/052 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7056 , A61P35/00 , A61P37/06 , C07H19/04
摘要： NEW MATERIAL:An imidazole nucleoside shown by the formula I [R
1 is group shown by the formula II (one of R
3 and R
4 is OH, acyloxy, or acetamide, and the other is H; one of R
5 and R
6 , and R
7 and R
8 is OH, acyloxy, and the other is H; one of R
9 and R
10 is H, CH
3 , CH
2 OH, acyloxymethyl, and the other is H), the formula III (one of R
11 and R
12 , and R
13 and R
14 is OH, acyloxy, and the other is H; one of R
15 and R
16 is CH
2 OH' or acyloxymethyl, and the other is H); R
2 is H, or R
1 ].
EXAMPLE: 5-Carbamoyl-1-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl) imidazolium-4-olate.
USE: A water-soluble carcinostatic agent, immunosuppressive agent.
PROCESS: For example, a compound shown by the formula IV is reacted with a saccharide derivative shown by the formula V (R'
3 WR'
8 are groups R
3 WR
8 other than OH; R'
9 WR'
10 are groups R
9 and R
10 other than CH
2 OH; R
17 is halogen, etc.) in the presence of a condensation agent, and if necessary, deacylated, to give a compound shown by the formula I (with the proviso that R
1 = group shown by the formula II).
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：由式I表示的咪唑核苷[R1为式Ⅱ所示的基团（R3和R4之一为OH，酰氧基或乙酰胺，另一个为H; R5和R6之一，R7和R8 是OH，酰氧基，另一个是H; R 9和R 10之一是H，CH 3，CH 2 OH，酰氧基甲基，另一个是H），式III（R 11和R 12之一，R 13和R 14是OH，酰氧基，另一个为H; R 15和R 16中的一个为CH 2 OH或酰氧基甲基，另一个为H）; R2是H或R1]。实施例：5-氨基甲酰基-1-（2,3,5-三-O-乙酰基-β-D-呋喃核糖基）咪唑鎓-4-醇酸酯。用途：水溶性制剂，免疫抑制剂。方法：例如，式IV所示的化合物与式V所示的糖衍生物（R'3-R'8是不同于OH的R3-R8基团; R'9-R'10是基团R9 和R 10，除了CH 2 OH; R 17是卤素等），并且如果需要，进行脱酰基化，得到式I所示的化合物（条件是R1 =式II所示的基团）。

8. 发明专利

JPS58203988A Optically active imidazolylmethyloxirane derivative and its preparation 失效
标题翻译：光学活性的咪唑啉衍生物衍生物及其制备
公开(公告)号：JPS58203988A
公开(公告)日：1983-11-28
申请号：JP5332683
申请日：1983-03-28
申请人： Sumitomo Chem Co Ltd
发明人： SAJI KITAROU , SATOU RENZOU , AONO SHIYUNJI , ICHINOSE KATSUAKI , OKUDA TAKAO , ATAMI TOSHIO
IPC分类号： C07C57/58 , C07B31/00 , C07B57/00 , C07C51/00 , C07C67/00 , C07D405/06
摘要： NEW MATERIAL:(R)-2-(2,4-Dichlorophenyl)-2-(imidazol-1-yl)methyloxirane of formula I .
USE: A synthetic intermediate of optically active imidazolylalkylthiopropanol derivative having strong antifungal activity.
PROCESS: The racemic isomer of the imidazolyldiol derivative of formula II is made to react with an optically active carboxylic acid (or its reactive derivative) (preferably the compound of formula III) to obtain two kinds of diastereomer esters, from which the objective ester is separated. The separated ester is hydrolyzed under alkaline condition, and the resultant optically active imidazolyldiol derivative of formula IV is methylated with methanesulfonyl chloride, and without isolating from the reaction system, treated with an alkali to obtain the objective compound of formula I .
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I的（R）-2-（2,4-二氯苯基）-2-（咪唑-1-基）甲基环氧乙烷。用途：具有强抗真菌活性的光学活性咪唑基烷基硫代丙醇衍生物的合成中间体。方法：使式II的咪唑烷二醇衍生物的外消旋异构体与光学活性羧酸（或其反应性衍生物）（优选式III化合物）反应，得到两种非对映异构体酯，其中目标酯为分开将分离的酯在碱性条件下水解，将得到的式Ⅳ的旋光性咪唑烷二醇衍生物用甲磺酰氯甲基化，不用从反应体系中分离，用碱处理，得到目的化合物Ⅰ。

9. 发明专利

JPS58203973A Optically active imidazolyl alcohol derivative and its preparation 失效
标题翻译：光学活性咪唑啉醇衍生物及其制备
公开(公告)号：JPS58203973A
公开(公告)日：1983-11-28
申请号：JP8853082
申请日：1982-05-24
申请人： Sumitomo Chem Co Ltd
发明人： SAJI KITAROU , SATOU RENZOU , AONO SHIYUNJI , ICHINOSE KATSUAKI , OKUDA TAKAO , ATAMI TOSHIO
IPC分类号： A61K31/415 , A61P31/04 , A61P31/10 , C07C55/07 , C07D233/60 , C07D521/00
CPC分类号： C07D231/12 , C07C55/07 , C07D233/56 , C07D249/08
摘要： NEW MATERIAL:The optically active imidazolyl alcohol derivative of formula I (n is 3 or 4; *C is asymmetric carbon atom) having (-) optical rotation in methanol solution, and its salt.
EXAMPLE: (-)-3-( n-Butylthio )-2-( 2,4-dichlorophenyl )-1-(imidazol-1-yl)-2-propanol hydrochloride.
USE: An antifungal agent. It has especially strong antifungal activity, and exhibits remarkable life-elongating effect in the life-elongation test using mouse.
PROCESS: The compound of formula I can be prepared by reacting the optically active epoxide derivative of formula II having (-)-optical rotation in methanol solution with an alkali metal salt of the thiol derivative of formula III (M is alkali metal) in a proper solvent at 0W30°C.
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：在甲醇溶液中具有（ - ）旋光性的式I的光学活性咪唑基醇衍生物（n为3或4; * C为不对称碳原子）及其盐。实施例：（ - ） - 3-（正丁硫基）-2-（2,4-二氯苯基）-1-（咪唑-1-基）-2-丙醇盐酸盐。用途：抗真菌剂。它具有特别强的抗真菌活性，并且在使用小鼠的寿命延长试验中显示出显着的寿命延长效果。方法：式I化合物可以通过在甲醇溶液中具有（ - ） - 旋光性的式II的光学活性环氧化物衍生物与式III的硫醇衍生物的碱金属盐（M是碱金属）反应来制备适当的溶剂在0-30℃。

10. 发明专利

JPS57120576A Novel imidazole ester 失效
标题翻译：新咪咪唑
公开(公告)号：JPS57120576A
公开(公告)日：1982-07-27
申请号：JP758181
申请日：1981-01-20
申请人： Sumitomo Chem Co Ltd
发明人： TANAKA YOSHIHIRO , ATAMI TOSHIO , YOSHIDA NOBORU
IPC分类号： C07D233/90 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P35/00 , A61P37/06 , A61P37/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： NEW MATERIAL:An imidazole derivative of formulaI(R
1 WR
3 are H, halogen, alkyl, alkenyl, cyano, formyl, halogenoalkyl, alkoxycarbonyl, aralkyloxycarbonyl, acetamide, substituted alkyl, alkoxycarbonyl-substituted alkenyl, alkoxy, heterocyclic ring) and its acid adduct.
EXAMPLE: 5-Carbamoyl-1H-imidazol-4-yl acrylate.
USE: Carcinostatic agent: it has effects to inhibit the propagation of tumor cells and prolong lives.
PREPARATION: The reaction between 4-carbamoyl-imidazolium-5-oleate or its reactive derivative and a carboxylic acid of formula II or its reactive derivative gives the compound of formulaI.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新物质：式I的咪唑衍生物（R1-R3为H，卤素，烷基，烯基，氰基，甲酰基，卤代烷基，烷氧基羰基，芳烷氧基羰基，乙酰胺，取代的烷基，烷氧基羰基取代的烯基，烷氧基，杂环）。实施例：5-氨基甲酰基-1H-咪唑-4-基丙烯酸酯。用途：致癌剂：具有抑制肿瘤细胞繁殖和延长寿命的作用。制备：4-氨基甲酰基 - 咪唑鎓-5-油酸酯或其活性衍生物与式II的羧酸或其反应性衍生物之间的反应得到式I化合物。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式