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1. 发明专利

JPS59144754A Prostaglandin-mimic compound 失效
标题翻译： PROSTAGLANDIN-MIMIC化合物
公开(公告)号：JPS59144754A
公开(公告)日：1984-08-18
申请号：JP844484
申请日：1984-01-23
申请人： Ono Pharmaceut Co Ltd
发明人： HAYASHI MASAKI , KOORI SEIJI , ARAI YOSHINOBU , OKADA TADANORI , KONISHI YOSHITAKA
IPC分类号： A61K31/557 , A61K31/5575 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D309/12 , C08B37/00
CPC分类号： C08B37/0015 , C07C405/00 , C07D309/12
摘要： NEW MATERIAL:The compound of formula I (X is cis or trans-vinylene or ethylene; R
1 is H or 1W12C alkyl; R
3 is 1W10C alkyl; the double bond between 3- and 4-C atoms is trans or cis, or their mixture; the wavy line has α- or β-configuration).
EXAMPLE: 9-Oxo-11α,15α-dihydroxy-16,16-dimethylprosta-trans- and cis-3-trans-13- dienoic acid methyl ester [16,16-dimethyl-trans- and cis-Δ
3 -PGE
1 methyl ester].
USE: Useful as oxytocic, abortifacient, fertility improver, estrus regulative, contraceptive, emmenagogue, etc.
PREPARATION: The compound of formula I (X is Y and R
1 is R
7 ) can be prepared by hydrolyzing the OR
8 group of the compound of formula II (Y is cis- vinylene or ethylene; R
7 is 1W4C alkyl; R
8 is 2-tetrahydropyranyl) to hydroxyl group.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I化合物（X为顺式或反式亚乙烯基或亚乙基; R 1为H或1-12C烷基; R 3为1-10C烷基; 3-和4- C原子是反式或顺式或它们的混合物;波浪线具有α或β构型）。实施例：9-氧代-11α，15α-二羟基-16,16-二甲基丙基 - 反式和顺式-3-反式-13-二烯酸甲酯[16,16-二甲基 - 反式和顺式-Δt3 -3] PGE1甲酯]。用途：用作催产素，流产，生殖改善剂，发情调节剂，避孕药，止痛药等。制剂：式I化合物（X为Y和R 1为R 7）可以通过水解OR （Y为顺式 - 亚乙烯基或亚乙基; R 7为1-4 C烷基; R 8为2-四氢吡喃基）的化合物为羟基。

2. 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。

3. 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。

4. 发明专利

JPS5756464A Imidazole derivative ahd inhibitor for biosyntesis of thromboxane a2 失效
标题翻译：咪唑衍生物AHD抑制剂
公开(公告)号：JPS5756464A
公开(公告)日：1982-04-05
申请号：JP13064380
申请日：1980-09-22
申请人： Kissei Pharmaceut Co Ltd , Ono Pharmaceut Co Ltd
发明人： TAUCHI TADAO , KAWAMURA MASANORI , OKADA TADANORI , HAYASHI MASAKI
IPC分类号： A61K31/415 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P29/00 , A61P43/00 , C07C45/41 , C07D233/56 , C07D233/58 , C07D233/60 , C07D521/00
CPC分类号： C07D231/12 , C07C45/41 , C07C255/00 , C07D233/56 , C07D249/08 , C07C47/14
摘要： NEW MATERIAL:A compound shown by the formulaI[n is 4W9; R
1 is H or 1W2C alkyl; one of R
2 and R
3 is H and the other is halogen, phenyl, or R
2 and R
3 form -(CH
2 )
n -(n is 4W6), or show -CH
2 ]or its pharmaceutically acceptable nontoxic salt.
EXAMPLE: 1-(7-Carboxy-7-phenylheptyl)imidazole hydrochloride.
USE: An inhibitor for biosynthesis of thromboxane A
2 . Useful as a remedy for an inflammation, cerebral apoplexy, myocardial infarction, acute malum cordis, breast pang, thrombois, etc. caused by TXA
2 . An oral dosage is preferably 10mgW1g.
PROCESS: A metal salt of imidazole is reacted with a halogen compound shown by the formula II (X is halogen) in a reaction solvent at from room temperature to the reflux temperature of the solvent, to give a compound shown by the formulaIwherein one of R
2 and R
3 is H and the other is phenyl.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：由式I [n为4-9; R 1是H或1-2C烷基; R 2和R 3中的一个是H，另一个是卤素，苯基或R 2和R 3形式 - （CH 2）n - （n是4-6），或者表示-CH 2 ]或其药学上可接受的无毒盐。实施例：1-（7-羧基-7-苯基庚基）咪唑盐酸盐。用途：血栓素A2生物合成抑制剂。可用作TXA2引起的炎症，脑中风，心肌梗塞，急性脐带血，乳房肿胀，血栓形成等的补救措施。口服剂量优选为10mg-1g。方法：在室温至溶剂的回流温度下，在反应溶剂中使咪唑的金属盐与式II所示的卤素化合物（X为卤素）反应，得到式I化合物，其中R 2和R 3是H，另一个是苯基。

5. 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。

6. 发明专利

JPS5754167A Pyroglutamic acid derivative and its preparation 失效
标题翻译：空值
公开(公告)号：JPS5754167A
公开(公告)日：1982-03-31
申请号：JP12923780
申请日：1980-09-19
申请人： Ono Pharmaceut Co Ltd
发明人： TODA MASAAKI , IMAKI KATSUHIRO , SAKUYAMA SHIGERU , OKADA TADANORI , HAYASHI MASAKI
IPC分类号： C07D207/28
摘要： NEW MATERIAL:The pyroglutamic acid derivative of formula I (R
1 is H or lower alkyl).
EXAMPLE: N-Acryl-L-pyroglutamic acid.
USE: An intermediate for the preparation of the pyroglutamic acid derivative of formula II useful as a hypotensor having very strong angiotensinase-inhibiting activity.
PROCESS: The objective compound is prepared by reacting an active derivative of the acid of formula III with pyroglutamic acid in the presence of a base. The compound of formula I can be converted to (2S)-alkyl derivative stereoselectively, in extremely high selectivity, by reacting with thioacetic acid.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式Ⅰ的焦谷氨酸衍生物（R 1是H或低级烷基）。实施例：N-丙烯酰-L-焦谷氨酸。用途：用于制备具有非常强的血管紧张素酶抑制活性的低血压的式II的焦谷氨酸衍生物的中间体。方法：目标化合物通过在碱存在下使式III的酸的活性衍生物与焦谷氨酸反应来制备。通过与硫代乙酸反应，式I化合物可以以极高的选择性立体选择性地转化为（2S） - 烷基衍生物。

7. 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。

8. 发明专利

JPS5724359A Preparation of cyclic imide 失效
标题翻译：循环流化合物的制备
公开(公告)号：JPS5724359A
公开(公告)日：1982-02-08
申请号：JP9692080
申请日：1980-07-17
申请人： Ono Pharmaceut Co Ltd
发明人： TODA MASAAKI , IMAKI KATSUHIRO , SAKUYAMA SHIGERU , OKADA TADANORI , HAYASHI MASAKI
IPC分类号： C07D277/14 , A61K31/40 , A61K31/4015 , A61P9/12 , C07D207/277 , C07D207/28 , C07D263/16 , C07D263/18
摘要： PURPOSE: To obtain the titled compound useful as an intermediate for an antihypertensive agent easily and inexpensively, by reacting a compound, e.g., L- pyroglutamic acid, etc. with an active derivative of an acid, e.g., 3-acetylthio- 2(RS)-methylpropanoyl chloride, etc. in the presence of a base.
CONSTITUTION: A compound shown by the formula I (X is methylene, O, or S) is reacted with an active derivative of an acid shown by the formula II (R
1 is H or lower alkyl; R
2 is lower alkanoyl or benozoyl) in the presence of a base (e.g., sodium hydroxide, potassium hydroxide, sodium carbonate), to give a cyclic imide [e.g., (2S)-1-[3-acetylthio-2(RS)-methylpropanoyl]pyroglutamic acid, etc.] shown by the formula III.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：目的：通过使例如L-焦谷氨酸等化合物与酸的活性衍生物（例如3-乙酰硫基-2（RS））反应，可以容易且廉价地获得用作抗高血压药的中间体的标题化合物） - 甲基丙酰氯等。构成：由式I表示的化合物（X是亚甲基，O或S）与式II所示的酸的活性衍生物反应（R 1是H或低级烷基; R 2是较低的（例如，（2S）-1- [3-乙酰硫基-2（RS） - 甲基丙酰基]焦谷氨酰胺（例如（2S）-1- [3-乙酰硫基-2（RS） - 甲基丙酰基]焦谷氨酸酸等]，由式III表示。

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