Asahi Glass Company, Limited

The Green Cross Corporation

Agc Inc.

Other

Seikagaku Corporation

Nippon Zoki Pharmaceutical Co., Ltd.

Dainippon Pharmaceutical Company, Limited

Seikagaku Kogyo Co. Ltd.

Yutaka Mizushima, Asahi Glass Company Ltd.

Arata Yasuda

Takashi Okazoe

Yoshitomi Morizawa

Yoshihisa Inoue

Norifumi Nakamura

Hajime Ebisu

Jun Sasaki

Naomichi Ishida

Yasushi Matsumura

Yutaka Mizushima

Mitsugu Kasagawa

Buichi Fujitani

Tomoyuki Asai

Toshihide Inomata

Satoshi Kawaguchi

Yusuke Tomiyori

Keiichi Uchida

Yu Onozaki

Toshiaki Kadokawa

Kanoo Hosoki

Hiroyoshi Nanba

Naonobu Hatano

Kazuyoshi Sawada

Naoki Ichinokawa

Shuzhong Wang

Yoshitomo Morizawa

Taku Yamamoto

Kazuki Taguchi

Takashi Akiya

Tomoko Ito

The present invention provides a production method of &#x3b1;-fluoroacrylate ester, a composition containing a highly-pure fluorocyclopropane derivative and a composition containing highly-pure &#x3b1;-fluoroacrylate ester. The present invention relates to a method of producing a compound represented by the following formula (F), including subjecting a composition containing a compound represented by the following formula (A) to a purification treatment in the order of distillation and washing with an aqueous alkali solution to give a purified product containing a compound represented by the following formula (A), and subjecting the purified product to a thermal decomposition reaction, a composition containing a highly-pure compound represented by the following formula (A), and a composition containing a highly-pure compound represented by the following formula (F), wherein R may be the same or different and is a monovalent hydrocarbon group, and X is a halogen atom: 

Method for producing &#x3b1;-fluoro acrylic acid ester, and composition containing highly-pure fluorocyclopropane derivative, and composition containing highly-pure &#x3b1;-fluoro acrylic acid ester

The present invention relates to a novel prostaglandin derivative having an alkynyl group on &#x3c9;-chain, particularly, a novel prostaglandin derivative having a double bond at the 2-position and an alkynyl group on the &#x3c9;-chain and a medicament containing the compound as an active ingredient. According to the present invention, a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof; 

Prostaglandin derivative

To provide a novel method for producing a halogenated acrylic acid derivative. A compound represented by the formula (1): (wherein each of Rand Rwhich are independent of each other, is a hydrogen atom or a monovalent group essentially containing a carbon atom, or Rand Rtogether form a ring, Ris a monovalent group capable of being desorbed by ROH removal reaction, and each of Rand Rwhich are independent of each other, is a hydrogen atom or a monovalent group essentially containing a carbon atom) and having a boiling point of at most 500&#xb0; C., is subjected to ROH removal reaction in a vapor phase in the presence of a solid catalyst to obtain an ethene derivative represented by the formula (2): the ethene derivative represented by the formula (2) and a halogenated methane represented by the formula (3):CHXYZ&#x2003;&#x2003;(3)(wherein each of X, Y and Z which are independent of one another, is a halogen atom) are reacted in the presence of a basic compound and a phase transfer catalyst, to obtain a cyclopropane derivative represented by the formula (4): and the cyclopropane derivative represented by the formula (4) is reacted by heating in a liquid phase or in a vapor phase to obtain a halogenated acrylic acid ester derivative represented by the formula (5): 

Method for producing halogenated acrylic acid derivative

Quinolin-2-yl benzoic acid compounds which are useful as intermediates of quinoline compounds having angiotensin II antagonist activity prepared by decarboxylating 2-(carboxyphenyl)-4-quinolinecarboxylic acid compounds in which a carboxyl group bonded to a phenyl group may be esterified, while a carboxyl group bonded to a quinoline ring is not esterified, and both rings may have one or more substituents inert to the decarboxylation reaction.

Process for producing 2-(carboxyphenyl)-4-quinolinecarboxylic acid

A quinoline compound represented by the formula (1) or a salt thereof: ##STR1## wherein the definition of each substituents are described in the specification, which have angiotensin II antagonism and hypotensive action and are useful as an agent for the prevention and treatment of cardiovascular system diseases such as hypertension, heart failure and the like.

Quinoline compounds

Prostaglandin I.sub.2 derivatives

An isoindazole compound of the formula (1) or a salt thereof; a method for the production thereof; and pharmaceutical use of the compound and a salt thereof, particularly as an angiotensin II antagonist and as an agent for the prophylaxis and treatment of circulatory diseases (particularly hypertension and heart failure); ##STR1## wherein Q is a heterocyclic derivative of the formula (2) or (3) ##STR2## wherein other symbols of the above formulas are as defined in the Specification. The compound and its salt show superior angiotensin II antagonism and are low toxic. Accordingly, they are useful as angiotensin II antagonists for the treatment or prophylaxis of angiotensin II-mediated diseases such as circulatory diseases of hypertension (e.g. essential hypertension, renal hypertension) and heart failure.

Isoindazole compound

An emulsion of lipid containing a prostaglandin analogue of the formula (1): ##STR1## wherein R.sup.1 is an alkanoyl group, R.sup.2 is a hydrogen atom or an alkyl group, each of R.sup.3 and R.sup.4 is a hydrogen atom or a protective group for an alcohol, R.sup.5 is an alkyl group which may have a substitutent, and  is a single bond or a double bond.

Emulsion of lipid containing a prostaglandin analogue

An emulsion of lipid containing a prostaglandin analogue of the formula (1): ##STR1## wherein R.sup.1 is an alkanoyl group, R.sup.2 is a hydrogen atom or an alkyl group, each of R.sup.3 and R.sup.4 is a hydrogen atom or a protective group for an alcohol, R.sup.5 is an alkyl group which may have a substituent, and is a single bond or a double bond.

A 6-fluoroprostaglandin having the formula: ##STR1## wherein A is a carbonyl group or a hydroxymethylene group, R.sup.1 is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl group or a substituted or unsubstituted 5- or 6-membered cycloalkyl group, R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group, each of R.sup.3 and R.sup.4 which may be the same or different is a hydrogen atom or a protecting group, R.sup.5 is a hydrogen atom or a hydroxyl group, and is a single bond or a double bond, and its salt when R.sup.2 is a hydrogen atom.

6-fluoroprostaglandins

Growing community of inventors

Yokohama, Japan

Arata Yasuda