公开(公告)号：US3565559A

公开(公告)日：1971-02-23

申请号：US3565559D

申请日：1969-03-06

Applicant: SUMITOMO CHEMICAL CO

Inventor： SATO NOBUYASU ,  OISHI RYOTA ,  NAKAMURA TOSHIO

IPC: A61K9/50 ,  B01J13/08 ,  A61K9/04 ,  B01J13/02 ,  B44D1/02

CPC classification number: A61K9/5089 ,  B01J13/08 ,  Y10T428/2984 ,  Y10T428/2989

Abstract: PROCESS OF MAKING MICROCAPSULES OF ACTIVE CHEMICAL SUBSTANCES, FOR EXAMPLE, TO PREVENT VITAMIN A FROM AIROXIDATION, COATING PIGMENT PARTICLES IN CARBONLESS PAPER, ETC., WHICH CONSISTS OF (1) FORMING AN AQUEOUS EMULSION OR SUSPENSION OF THE ACTIVE CHEMICAL SUBSTANCE, (2) ADDING AN AQUEOUS SOLUTION OF A GELABLE HYDROPHILIC SUBSTANCE AND THEN SURFACE ACTIVE AGENT AND DISPERSING A LIQUID SOLVENT IMMISCIBLE WITH THE SAID EMULSION OR SUSPENSION OR (2'') DISPERSING A MIXTURE OF THE SURFACE ACTIVE AGENT AND THE LIQUID SOLVENT INTO THE AQUEOUS EMULSION OR SUSPENSION, TO FORM A DISPERSION AT A TEMPERATURE ABOVE A GELATIN POINT OF THE EMULSION OR SUSPENSION, (3'') RAISING THE DISPERSION TEMPERATURE TO AN INVERSION TEMPERATURE OR (3") IN CASE THE USED SURFACE ACTIVE AGENT IS MONO-VALENT METALLIC AND ADDING AN AQUEOUS SOLUTION CONTAINING MULTIVALENT METALLIC ION, TO INVERSE THE DISPERSION PHASE TO FORM DROPLETS, (4) STIRRING, (5) COOLING TO THE ABOVE SAID GELATION POINT TO CAUSE THE DROPLETS TO FORM MICROCAPSULES, (6) ADDING AN AQUEOUS ELECTROLYTE SOLUTION TO HARDEN THE MICROCAPSULES, (7) ADDING WATER-ABSORPTIVE SUBSTANCE TO COAT THE MICROCAPSULES OR (7'') WASHING AND DEHYDRATING THE MICROCAPSULES BY LOWER ALKYL ALCOHOLS, (8) FILTERING TO SEPARATE THE MICROCAPSULES, AND (9) DRYING THE MICROCAPSULES.

公开(公告)号：US3669987A

公开(公告)日：1972-06-13

申请号：US3669987D

申请日：1968-04-09

Applicant: SUMITOMO CHEMICAL CO

Inventor： SATO NOBUYASU ,  NAKAMURA TOSHIO ,  TAKENAKA HIROSHI

IPC: A61K9/02 ,  A61K9/06 ,  A61K31/00 ,  A61K31/405 ,  A61K33/12 ,  C07D209/04 ,  C07D209/26 ,  C07D209/28 ,  C07D27/56

CPC classification number: C07D209/04 ,  A61K9/02 ,  A61K9/06 ,  A61K31/00 ,  A61K31/405 ,  A61K33/12 ,  C07C243/00 ,  C07C251/72 ,  C07D209/26 ,  C07D209/28 ,  Y10S514/96 ,  A61K2300/00

Abstract: Alkali metal salts or organic amine molecular compounds of such 1-acyl-3-indolylaliphatic acid derivatives as 1-(pchlorobenzoyl)-2-methyl-5-methoxy-3-indolylacetic acid, 1cinnamoyl-2-methyl-5-methoxy-3-indolylacetic acid or 1nicotinoyl-2-methyl-5-methoxy-3-indolylacetic acid are prepared by dissolving about 1 mole of said 1-acyl-3-indolylaliphatic acid derivative in acetone or methanol, reacting in the presence of a small amount of water the resultant solution with about 0.5 mole of alkali metal carbonate, or about 1 mole of alkali metal bicarbonate or with about 1 mole of an organic amine and distilling off acetone or methanol and water from the reaction mixture to yield the alkali metal salt or organic amine molecular compound. Alkaline earth metal or aluminum salt or said 1-acyl-3indolylaliphatic acid derivative is prepared by reacting a soluble salt of alkaline earth metal or aluminum with an aqueous solution containing said alkali metal salt of 1-acyl-3indolylaliphatic acid derivative. These alkali metal salts or organic amine molecular compounds are enable to make solid injections for anti-inflammatory drugs.

Abstract translation: 这种1-酰基-3-吲哚脂肪酸衍生物的碱金属盐或有机胺分子化合物为1-（对氯苯甲酰基）-2-甲基-5-甲氧基-3-吲哚乙酸，1-肉桂酰基-2-甲基-5 - 甲氧基-3-吲哚乙酸或1-烟酰基-2-甲基-5-甲氧基-3-吲哚乙酸通过将约1摩尔所述1-酰基-3-吲哚基脂肪酸衍生物溶解在丙酮或甲醇中，在 用约0.5摩尔碱金属碳酸盐或约1摩尔碱金属碳酸氢盐或约1摩尔有机胺将所得溶液存在于少量水中，并从反应混合物中蒸除丙酮或甲醇和水，得到 碱金属盐或有机胺分子化合物。

公开(公告)号：US3592902A

公开(公告)日：1971-07-13

申请号：US3592902D

申请日：1968-04-09

Applicant: SUMITOMO CHEMICAL CO

Inventor： SATO NOBUYASU ,  NAKAMURA TOSHIO ,  TAKENAKA HIROSHI ,  WATABE EIKO

IPC: C07D209/28 ,  C07D27/38

CPC classification number: C07D209/28

Abstract: A STABLE INJECTION OF AN INDOLYLALIPHATIC ACID DERIVATIVE SUCH AS N-(P-CHLOROBENZOLY)-2-METHYL-5-METHOXY-3-INDOLYLACETIC ACID, N-CINNAMOLY-2-METHYL-5-METHOXY-3-INDOLYLACETIC ACID OR N-NICOTINOYL-2-METHYL-5-METHOXY-3INDOLYLACETIC ACID IS PREPARED BY DISSOLVING THE INDOLYLALIPHATIC ACID DERIVATIVE IN A NON-AQUEOUS ORGANIC SOLVENT FOR INJECTION AND ADDING AN AQUEOUS ORGANIC AMINE SOLUTION CONTAINING 0.6 TO 1 MOLE OF SAID ORGANIC AMINE PER 1 MOLE OF THE INDOLYLALIPHATIC ACID DERIVATIVE TO THE RESULTANT SOLUTION. THE THUS OBTAINED INJECTION IS USED AS AN ANTI-INFLAMMATORY DRUG.