Kaneka Corporation

Pfizer Corporation

Tatsuyoshi Tanaka

Masaru Mitsuda

Kazumi Okuro

Hiroyuki Ogino

Mitsuji Akazawa

Masaya Mizutani

Kenji Inoue

Yoshihiko Yasohara

Akira Nishiyama

Nobuo Nagashima

Tatsuya Honda

Akio Fujii

Masanobu Sugawara

Hirofumi Maeda

Naohiro Imai

It is an object of the present invention to provide a formulation comprising ethyl cellulose, an active pharmaceutical ingredient, and a solvent, which is a stable formulation in which generation of impurities is suppressed even during the long-term storage. According to the present invention, provided is a formulation comprising (a) an active pharmaceutical ingredient, (b) ethyl cellulose, (c) 2-mercaptobenzimidazole, and (d) 0.1 part by weight or more of solvent with respect to 1 part by weight of the ethyl cellulose.

Formulation comprising active pharmaceutical ingredient

It is an object of the present invention to provide a patch having practical adhesive force and cohesive force as a pharmaceutical product, and also exhibiting a fast-acting anesthetic action. The present invention provides a patch formed from an adhesive layer comprising 5% by weight or more and less than 20% by weight of a mixture of lidocaine and another local anesthetic, wherein the adhesive layer comprises at least a rubber-based pressure-sensitive adhesive and liquid paraffin and a content of a tackifier in the adhesive layer is 10% by weight or less.

Patch

The present invention aims to provide a novel type I natural ceramide derivative having a structure more similar to that of a type I natural ceramide composed of sphingosine and an &#x3c9;-acyloxy long-chain carboxylic acid; and a method for producing the same. The derivative is provided by reacting an &#x3c9;-acyloxy long-chain fatty acid derivative with dihydrosphingosine or a salt thereof. The thus produced novel type I natural ceramide derivative, when combined with other ceramides, can significantly improve the compatibility of ceramides, which facilitates preparation of a composition containing ceramides, such as a moisturizer or a cosmetic, and also increases the storage stability of the composition.

Type I natural ceramide derivative and method for producing same

It is an objective of the present invention to produce an anti-form of an optically active &#x3b2;-hydroxy-&#x3b1;-aminocarboxylic acid ester efficiently, simply and industrially advantageously. The objective can be accomplished by directly and selectively producing the anti-form of the optically active &#x3b2;-hydroxy-&#x3b1;-aminocarboxylic acid ester by asymmetric reduction of a &#x3b2;-keto-&#x3b1;-aminocarboxylic acid ester using an optically active amine complex as a catalyst. Further, the &#x3b2;-keto-&#x3b1;-aminocarboxylic acid ester as a raw material can be produced at a high yield by reacting a glycine derivative with a carboxylic acid derivative.

Process for producing optically active beta-hydroxy-alpha-aminocarboxylic acid ester

The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxy alcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active &#x3b1;-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.

Optically active halohydrin derivative and process for producing optically active epoxy alcohol derivative from the same

The present invention provides a method for easily producing an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative useful for an intermediate for pharmaceutical products, particularly an inhibitor of a cholesteryl ester transfer protein (CETP) from easily available raw materials. In the present invention, (S)-N-[4-(trifluoromethyl)phenyl]-3-hydroxypentanoic acid amide prepared from easily available raw materials leads a production of (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone to give (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide. Furthermore, (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone is reacted with a carbamic acid ester to give an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative.

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Takasago, Japan

Tatsuyoshi Tanaka