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61. 发明专利

JPH0148917B2 失效
公开(公告)号：JPH0148917B2
公开(公告)日：1989-10-20
申请号：JP13384381
申请日：1981-08-26
申请人： MITSUBISHI CHEM IND
发明人： NITSUTA KAZUMASA , FUJIMORI SHINICHIRO , HARUYAMA TOSHIO , INOE SHINYA
IPC分类号： C07J7/00 , C07J5/00

62. 发明专利

JPS6245878B2 失效
公开(公告)号：JPS6245878B2
公开(公告)日：1987-09-29
申请号：JP7980280
申请日：1980-06-13
申请人： MITSUBISHI CHEM IND
发明人： NITSUTA KAZUMASA , HARUYAMA TOSHIO
IPC分类号： C07J5/00

63. 发明专利

JPS6212237B2 失效
公开(公告)号：JPS6212237B2
公开(公告)日：1987-03-17
申请号：JP2958677
申请日：1977-03-17
申请人： MITSUBISHI CHEM IND
发明人： OKUJIMA HIROMI , NITSUTA KAZUMASA , FURUYA RIKIZO
IPC分类号： A61K31/57 , A61P7/10 , C07J31/00

64. 发明专利

JPS611698A NOVEL CORTICOID DERIVATIVE AND ITS PREPARATION 失效
公开(公告)号：JPS611698A
公开(公告)日：1986-01-07
申请号：JP12043984
申请日：1984-06-12
申请人： MITSUBISHI CHEM IND
发明人： NITSUTA KAZUMASA , MARUYAMA AKIRA , NAKAO KENICHIROU , MIYAKE KIYOSHI , UENO HIROAKI
IPC分类号： A61K31/57 , A61P5/38 , C07J5/00 , C07J7/00 , C07J21/00 , C07J31/00
摘要： NEW MATERIAL:A compound shown by the formula I [A is group shown by the formula II or formula III; X is H, or halogen; Y is H, oxo, halogen at alpha-position or beta-position, OH, 1-10C alkyl; n is 2-5; R is OH, halogen, -OSO2R (R is 1-10C alkyl, or halogenated alkyl), or -OCOR (R is as shown for R ); R is H, or 1-10C alkyl at alpha-position or beta-position; R is 1-10C alkyl; bond between C1-C2 is single - double bond]. EXAMPLE:4-Pregnen-11beta, 17alpha, 21-triol-3, 20-dione 17alpha-( beta-methoxycarbonylpropionate). USE:An anti-inflammatory drug, especially a local anti-inflammatory agent. Having weak side effect. PREPARATION:A compound shown by the formula IV is reacted with an orthoester shown by the formula V (R is R ) to give a corticoid 17alpha,21-orthoester derivative shown by the formula VI, which is hydrolyzed, to give a compound shown by the formula I (R is OH).

65. 发明专利

JPS60193978A Piperazine derivative and its acid adduct 失效
标题翻译：哌嗪衍生物及其添加剂
公开(公告)号：JPS60193978A
公开(公告)日：1985-10-02
申请号：JP4796584
申请日：1984-03-13
申请人： Mitsubishi Chem Ind Ltd
发明人： FUKAMI JIICHI , INOUE SHINYA , NITSUTA KAZUMASA , NAKAO KENICHIROU , KIKUMOTO RIYOUJI
IPC分类号： C07D295/08 , A61K31/495 , A61K31/625 , A61P9/12 , C07D213/74 , C07D295/10
摘要： NEW MATERIAL:A compound of formula I [R
1 is OR
3 , NR
3 R
4 (R
3 , R
4 are H, 1W3C alkyl); R
2 is H, 1W3C alkyl; X is -C(=O)-; Ar is pyridyl, phenyl which may be substituted with halogen or 1W3C alkyl; n is 3, 4, 5] and its acid adduct.
EXAMPLE: 5-[5-(4-Phenyl-1-piperazinyl)valeryl]salicylamide.
USE: Hypotensor: it develops satisfactory hypotensive effect with a small amount of administration, further its development is prompt and durative. Further, its high safety is suggested.
PREPARATION: The reaction of an ω-halogenoalkanoylbenzene of formula II (X is halogen) with a piperazine of formula III gives the compound of formula I . The stoichiometric relation between the two reactants is 1:1, but the use of excessive amount of piperazine helps the smooth progress of the reaction and so the piperazine is used by 1W10mol per mol of the compound of formula II.
COPYRIGHT: (C)1985,JPO&Japio
摘要翻译：新材料：式I化合物[R 1]为OR 3，NR 3 R 4（R 3，R 4为H，1-3C烷基）; R 2是H，1-3C烷基; X是-C（= O） - ; Ar是吡啶基，可被卤素或1-3C烷基取代的苯基; n为3,4,5]及其酸加合物。实施例：5- [5-（4-苯基-1-哌嗪基）戊酰基]水杨酰胺。用途：低血压药物：少量给药可以发挥令人满意的降压作用，进一步发展是及时和持续的。此外，建议其高安全性。制备：式II的ω-卤代烷酰基苯（X为卤素）与式III的哌嗪的反应得到式I化合物。两种反应物之间的化学计量关系为1:1，但使用过量的哌嗪有助于反应的顺利进行，因此哌嗪的用量为每摩尔式Ⅱ化合物1-10摩尔。

66. 发明专利

JPS59164716A Biosynthetic inhibitor for fatty acid 失效
标题翻译：脂肪酸的生物活性抑制剂
公开(公告)号：JPS59164716A
公开(公告)日：1984-09-17
申请号：JP3860383
申请日：1983-03-09
申请人： Mitsubishi Chem Ind Ltd
发明人： ENDOU AKIRA , NITSUTA KAZUMASA , MARUYAMA AKIRA
IPC分类号： A61K31/19 , A61P43/00 , C07C51/00 , C07C55/02 , C07C57/13 , C07C67/00 , C12N9/99
摘要： PURPOSE: A biosynthetic inhibitor for fatty acids, containing a specific dicarboxylic acid as an active constituent, and capable of inhibiting acetyl CoA carboxylase and treating obesity due to excess fat causing arteriosclerosis, diabetes, etc.
CONSTITUTION: A biosynthetic inhibitor for fatty acids containing a dicarboxylic acid of the formula (R is alkyl or alkenyl; n is 0 or an integer 1W6), anhydride or a salt thereof as an active constituent. The compound of the formula is capable of inhibiting acetyl CoA carboxylase which is a rate determining enzyme of a synthetic system for the fatty acids. Thus, the accumulation of excess fat which is a direct or indirect cause for arteriosclerosis, diabetes or gout, etc. having a tendency to cause complication is inhibited. The above-mentioned inhibitor can be orally or parenterally administered. The daily dose thereof is usually 0.1W2,000mg/kg. The compound of the formula can be produced by the well-known method.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：目的：一种脂肪酸的生物合成抑制剂，其含有特定的二羧酸作为活性成分，能够抑制乙酰辅酶A羧化酶和治疗由于过量脂肪引起的动脉硬化，糖尿病等引起的肥胖。构成：含有二羧酸（R是烷基或烯基; n是0或1-6的整数），酸酐或其盐作为活性成分。该化合物能够抑制作为脂肪酸合成体系的速率决定酶的乙酰辅酶A羧化酶。因此，抑制作为导致并发症的倾向的动脉硬化，糖尿病或痛风等的直接或间接原因的过量脂肪的积聚。上述抑制剂可以口服或肠胃外给药。其日剂量通常为0.1〜2,000mg / kg。式的化合物可以通过公知的方法制备。

67. 发明专利

JPS591277B2 JPS591277B2 - 失效
公开(公告)号：JPS591277B2
公开(公告)日：1984-01-11
申请号：JP6837675
申请日：1975-06-06
申请人： Mitsubishi Chem Ind
发明人： OKUJIMA HIROMI , NITSUTA KAZUMASA , FURUYA RIKIZO
IPC分类号： C07J1/00 , C07J21/00 , C07J31/00

68. 发明专利

JPS5821698A ACYLOXYSTEROID AND ITS PREPARATION 失效
公开(公告)号：JPS5821698A
公开(公告)日：1983-02-08
申请号：JP11834381
申请日：1981-07-28
申请人： MITSUBISHI CHEM IND
发明人： NITSUTA KAZUMASA , FUJIMORI SHINICHIROU , HARUYAMA TOSHIO , INOUE SHINYA
IPC分类号： C07J7/00
摘要： NEW MATERIAL:A 17beta-ethynyl-17alpha-acyloxysteroid of formulaI(the dotted line is single or double bond; X is acyloxy). EXAMPLE:17beta-Ethynyl-17alpha-acetoxyandrosta-1,4-dien-3-one. USE:An intermediate for preparing adrenocortical hormones, e.g. hydrocortisone and prednisolone. PROCESS:A 17beta-ethynyl-17alpha-hydroxysteroid, e.g. 17beta-ethynyl-17alpha-hydroxyandrosta- 1,4-dien-3-one, of formula II is reacted with an acid anhydride of a carboxylic acid or an acid halide, e.g. acetic anhydride, preferably in a molar amount of 5 times or more that of the compound of formula II at 100-135 deg.C.

69. 发明专利

JPS5818400A PREPARATION OF ACYLOXYSTEROID 失效
公开(公告)号：JPS5818400A
公开(公告)日：1983-02-02
申请号：JP11569181
申请日：1981-07-23
申请人： MITSUBISHI CHEM IND
发明人： NITSUTA KAZUMASA , FUJIMORI SHINICHIROU , HARUYAMA TOSHIO , INOUE SHINYA
IPC分类号： C07J7/00 , C07J5/00
摘要： PURPOSE:To prepare the titled compound useful as a synthetic intermediate of adrenocortical hormone, economically, by reacting a 17-halogenoacetyl-17-acyloxysteroid with a lower fatty acid salt in the presence of a crown ether. CONSTITUTION:A 17-halogenoacetyl-17-acyloxysteroid having a partial struture of formulaI(X is halogen; Y is acyloxy) os made to react with an alkali metal salt of a lower fatty acid in the presence of a crown ether to obtain the objective 17-acyloxyacetyl-17-acyloxysteroid. The amount of the crown ether is more than equimolar to the steroid used as the raw material, and the reaction is carried out usually in an aprotic solvent at 0-80 deg.C. The steroid used as the raw material can be synthesized e.g. by using an easily and exonomically available compound of formula II as the starting raw material.

70. 发明专利

JPS582223B2 失效
公开(公告)号：JPS582223B2
公开(公告)日：1983-01-14
申请号：JP7551874
申请日：1974-07-02
申请人： MITSUBISHI CHEM IND
发明人： OKUJIMA HIROMI , NITSUTA KAZUMASA , FURUYA RIKIZO
IPC分类号： C07C5/22 , B01D9/02 , B01J23/84 , C07B61/00 , C07C1/00 , C07C15/24 , C07C51/00 , C07C63/307 , C07C63/38 , C07C67/00

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