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1. 发明专利

JPS59110663A Novel glycerol derivative, its preparation and drug containing the same 失效
标题翻译：新型甘油衍生物，其制备和含有其的药物
公开(公告)号：JPS59110663A
公开(公告)日：1984-06-26
申请号：JP21920682
申请日：1982-12-16
申请人： Ono Pharmaceut Co Ltd
发明人： ITOU HIROYUKI , OKADA TADANORI , MIYAMOTO TSUMORU
IPC分类号： C07C271/08 , A61K31/13 , A61K31/16 , A61K31/165 , A61P7/02 , A61P9/12 , A61P11/00 , A61P29/00 , A61P35/00 , A61P37/08 , C07C67/00 , C07C239/00
摘要： NEW MATERIAL:A compound of formula I (R
1 is 8W22C straight or branched chain alkyl; R
2 is 1W6C straight or branched chain alkyl, phenyl; R
3 is 1W8C straight or branched chain alkylene; R
4 is amino, formula: -NHR
5 , -NHCOR
5 where R
5 is 1W4C straight or branched chain alkyl) and its acid adduct.
EXAMPLE: (2RS)-1-O-Hexadecyl-2-(N-methylamino)carbonyl-3-O-[4-(N,N-dimethylamino)butyl]glycerol.
USE: Blood platelet coagulation-inhibiting agent, antiasthma, antiallergic, anti- inflammatory, hypotensor or antitumor agent.
PREPARATION: A novel compound of formula II is subjected to acylation reaction to give a compound of formula I where R
4 is -NHCOR
5 , -NHCOϕ. The compound of formula II is obtained by hydrolysis of a compound of formula III.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I化合物（R 1为8-22C直链或支链烷基; R 2为1-6C直链或支链烷基，苯基; R 3为1-8C直链或支链链烷基; R 4是氨基，式：-NHR 5，-NHCOR 5，其中R 5是1-4C直链或支链烷基）及其酸加合物。实施例：（2RS）-1-O-十六烷基-2-（N-甲基氨基）羰基-3-O- [4-（N，N-二甲基氨基）丁基]甘油。用途：血小板凝血抑制剂，抗哮喘药，抗过敏药，抗炎药，低血压药或抗肿瘤剂。制备：将式II的新化合物进行酰化反应，得到其中R 4为-NHCOR 5，-NHCOF的式I化合物。式II化合物通过式Ⅲ化合物的水解得到。

2. 发明专利

JPS5920255A Novel glycerol derivative, its preparation and pharmaceutical containing said derivative 失效
标题翻译：新型甘油衍生物，其制备和药物含有衍生物
公开(公告)号：JPS5920255A
公开(公告)日：1984-02-01
申请号：JP12666482
申请日：1982-07-22
申请人： Ono Pharmaceut Co Ltd
发明人： ITOU HIROYUKI , OKADA TADANORI , MIYAMOTO TSUMORU
IPC分类号： A61K31/21 , A61P7/02 , A61P35/00 , A61P43/00 , C07C67/00 , C07C227/00 , C07C227/08 , C07C227/16 , C07C227/18 , C07C227/20 , C07C229/10 , C07C231/00 , C07C231/08 , C07C231/12 , C07C233/83
CPC分类号： Y02P20/55
摘要： NEW MATERIAL:The compound of formula I (R
1 is 8W22C alkyl or phenyl-substituted 1W5C alkyl; R
2 is H, 2W5C acyl, benzoyl, etc.; R
3 is 1W6C alkylene; R
4 is amino, benzoylamino etc.) and its acid addition salt.
EXAMPLE: 1-0-Octadecyl-2-RS-0-acetyl-3-0-(3-aminopropionyl)glycerol acetate.
USE: Blood platelet coagulation inhibiting agent,antiphlogistic agent, antitumor agent, etc. It has antagonistic activity to blood platelet activation factor, proliferation suppressing action or differentiation inducing action to tumor cells, etc.
PROCESS: The compound of formula III (R
7 is H or 1W4C alkyl) can be prepared by removing the protecting group (Z-group) of the amino group of the compound of formula II (Z is t-tuboxycarbonyl, etc.) by hydrolysis.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式Ⅰ化合物（R 1是8-22C烷基或苯基取代的1-5C烷基; R 2是H，2-5C酰基，苯甲酰基等; R 3是1 -6C亚烷基; R4是氨基，苯甲酰基氨基等）及其酸加成盐。实施例：1-0-十八烷基-2-RS-O-乙酰基-3-0-（3-氨基丙酰基）甘油乙酸酯。用途：血小板凝血抑制剂，消炎剂，抗肿瘤剂等，对血小板活化因子具有拮抗作用，对肿瘤细胞增殖抑制作用或分化诱导作用等。方法：式III化合物（R 7 >是H或1-4C烷基）可以通过水解除去式II化合物（Z是叔丁氧基羰基等）的氨基的保护基（Z-基团）来制备。

3. 发明专利

JPS59112961A Glycerol derivative, its preparation and drug containing said derivative 失效
标题翻译：甘油衍生物，其制剂和含有衍生物的药物
公开(公告)号：JPS59112961A
公开(公告)日：1984-06-29
申请号：JP22469982
申请日：1982-12-21
申请人： Ono Pharmaceut Co Ltd
发明人： ITOU HIROYUKI , OKADA TADANORI , MIYAMOTO TSUMORU
IPC分类号： C07C319/08 , A61K31/13 , A61K31/16 , A61K31/165 , A61P7/02 , A61P9/12 , A61P11/00 , A61P29/00 , A61P35/00 , A61P37/08 , C07C67/00 , C07C313/00 , C07C319/14 , C07C323/12 , C07C325/00 , C07C329/16
摘要： NEW MATERIAL:The compound of formula I [R
1 is 8W22C alkyl, or phenyl- substituted 2W5C alkyl; R
2 is H, 1W6C alkyl, group of formula II (R
5 is H, halogen, methoxy, etc.) etc.; R
3 is 1W8C alkylene; R
4 is amino, -NHCOR
7 (R
7 is 1W4C alkyl), NHR
7 , etc.] and its salt.
EXAMPLE: ( 2RS )-1-O-Hexadecyl-2-dehydroxy-2-methylthio-3-O-[4-(dimethylamino)- butyl]glycerol.
USE: A blood platelet coagulation inhibitor, antiasthmatic agent, anti-allergic agent, anti-inflammatory agent, hypotensor, or antitumor agent.
PROCESS: The compound of formula V (R
2a is 1W6C alkyl, etc.) is prepared by reacting the compound of formula III [R
8 is alkylsulfonyl or (substituted) arylsulfonyl; R
4a is -NHCOR
7 , -N(R
7 )
2 , etc.] with the compound of formula HS-R
9 (R
9 is 1W6C alkyl) or formula IV.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新物质：式I化合物[R 1]为8-22 C烷基或苯基取代的2-5C烷基; R 2是H，1-6C烷基，式II基团（R 5是H，卤素，甲氧基等）等; R 3是1-8C亚烷基; R 4是氨基，-NHCOR 7（R 7是1-4 C烷基），NHR 7等]及其盐。实施例（2RS）-1-O-十六烷基-2-脱羟基-2-甲硫基-3-O- [4-（二甲基氨基） - 丁基]甘油。用途：血小板凝血抑制剂，止喘药，抗过敏剂，抗炎药，低血压药或抗肿瘤剂。方法：式Ⅴ化合物（R 2a为1-6C烷基等）通过式Ⅲ化合物[R 8为烷基磺酰基或（取代的）芳基磺酰基; 式R-R 9的化合物（R 9是1-6C烷基）或式IV化合物，其中R 4a是-NHCOR 7，-N（R 7）2等。

4. 发明专利

JPS5931738A Glycerol derivative, preparation thereof and drug containing said derivative 失效
标题翻译：甘氨酸衍生物，其制剂和含有所述衍生物的药物
公开(公告)号：JPS5931738A
公开(公告)日：1984-02-20
申请号：JP14175582
申请日：1982-08-17
申请人： Ono Pharmaceut Co Ltd
发明人： ARAI YOSHINOBU , ITOU HIROYUKI , MIYAMOTO TSUMORU
IPC分类号： C07C271/20 , C07C67/00 , C07C213/00 , C07C217/28 , C07C231/00 , C07C231/02 , C07C231/12 , C07C235/10 , C07C239/00
摘要： NEW MATERIAL:A compound of formula I [A is imino or carbonylamino; R
1 is 8W22C alkyl or 1W5C alkyl substituted by phenyl group; R
2 is H or group of formula II (R
5 is H, halogen, OCH
3 , etc.), and further COR
6 or CONHR
6 (R
6 is alkyl or phenyl) when A is carbonylamino; R
3 is alkylene; R
4 is amino, NHCOR
7 (R
7 is R
6 ), etc.] or an acid addition salt thereof.
EXAMPLE: (2RS)-1-O-hexadecyl-2-O-benzyl-3-[ 4-(N, N-dimethylamino)butylamino ]- 1,2-propanediol.
USE: An inhibitor for blood platelet agglutination, antiasthmatic agent, antiallergic agent, anti-inflammatory agent, hypotensive agent and antitumor agent.
PROCESS: A compound of formula III (R
9 is alkyl- or arylsulfonyl) is reacted with a compound of formula IV to give the corresponding compound of formula I .
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I化合物[A为亚氨基或羰基氨基; R 1是8-22个碳原子的烷基或1-5个被苯基取代的烷基; R 2是H或式II的基团（R 5是H，卤素，OCH 3等），并且当A（R 5）是C 1 -C 4烷基或苯基时，R 6或CONHR 6 是羰基氨基; R 3是亚烷基; R 4为氨基，NHCOR 7（R 7为R 6）等]或其酸加成盐。实施例：（2RS）-1-O-十六烷基-2-O-苄基-3- [4-（N，N-二甲基氨基）丁基氨基] -1,2-丙二醇。用途：血小板凝集抑制剂，止喘药，抗过敏药，抗炎剂，降血压药和抗肿瘤剂。方法：将式III化合物（R 9是烷基 - 或芳基磺酰基）与式IV化合物反应，得到相应的式I化合物。

5. 发明专利

JPS58198445A Novel glycerol derivative, its preparation and pharmaceutical containing said derivative 失效
标题翻译：新型甘油衍生物，其制备和药物含有衍生物
公开(公告)号：JPS58198445A
公开(公告)日：1983-11-18
申请号：JP7917982
申请日：1982-05-13
申请人： Ono Pharmaceut Co Ltd
发明人： ITOU HIROYUKI , OKADA TADANORI , MIYAMOTO TSUMORU
IPC分类号： A61K31/215 , A61K31/16 , A61K31/165 , A61K31/22 , A61P7/02 , A61P29/00 , C07C67/00 , C07C209/00 , C07C209/08 , C07C209/12 , C07C209/62 , C07C211/03 , C07C231/00 , C07C231/02 , C07C231/12 , C07C231/14 , C07C233/18 , C07C233/68 , C07C239/00 , C07C275/10
摘要： NEW MATERIAL:The compound of formula I [R
1 is alkyl; R
2 is H, acyl, benzoyl or group of formula II (R
5 is H, halogen, methoxy or alkyl); R
3 is alkylene; R
4 is NH
2 , NHR
6 (R
6 is acyl or benzoyl), NHR
7 (R
7 is alkyl), N(R
7 )
2 , group of formula III (Y is anion of acid) or NHCONHR
7 ], or its acid addition salt when R
4 is NH
2 .
EXAMPLE: (2RS)-1-O-Hexadecyl-3-O-(4-aminobutyl)glycerol.
USE: Blood platelet coagulation inhibitor, antiasthmatic agent, antiallergic agent, antiphlogistic agent, hypotensor and antitumor agent.
PROCESS: The compound of formula I wherein R
2 is group of fomrula II and R
4 is NHR
7 , N(R
7 )
2 or group of formula III can be prepared by reacting the compound of formula IV (Tr is trityl) with R
5 -substituted benzyl halide, reacting the resultant compound of formula V with the compound of formula R
10 -O-R
3 - Cl to obtain the compound of formula VI, and finally reacting the product with the compound of formula NH
2 R
7 , NH(R
7 )
2 or N(R
7 )
3 .
COPYRIGHT: (C)1983,JPO&Japio
摘要翻译：新材料：式I化合物[R 1]是烷基; R 2是H，酰基，苯甲酰基或式II的基团（R 5是H，卤素，甲氧基或烷基）; R 3是亚烷基; R 4是NH 2，NHR 6（R 6是酰基或苯甲酰基），NHR 7（R 7是烷基），N（R 7）2，式III（Y 是酸的阴离子）或NHCONHR 7]或其酸加成盐，当R 4是NH 2时。实施例：（2RS）-1-O-十六烷基-3-O-（4-氨基丁基）甘油。用途：血小板凝固抑制剂，止喘药，抗过敏药，消炎药，低血压药和抗肿瘤药。方法：其中R 2是式II和R 4的基团的式I化合物是NHR 7，N（R 7）2或式III的基团可以通过使式 IV（Tr是三苯甲基）与R 5取代的苄基卤反应，使得到的式V化合物与式R 10 -OR 3 Cl的化合物反应，得到式VI化合物，最后使具有式NH 2 R 7，NH（R 7）2或N（R 7）3的化合物的产物。

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