The Green Cross Corporation

Senju Pharmaceutical Co., Ltd.

Zeria Pharmaceutical Co., Ltd.

Aska Pharmaceutical Co., Ltd.

Grelan Pharmaceutical Co., Ltd.

Hykes Laboratories LLC

Sapporo Breweries Limited

Aska Pharmaceuticals Co., Ltd.

Tomoji Aotsuka

Tetsuo Matsui

Yoshiyuki Nakamura

Kouki Ishitani

Hiromichi Ishikawa

Hashime Kanazawa

Hiroshi Hosono

Kentarou Kumazawa

Takashi Nose

Yoshiaki Tanaka

Naoyoshi Miura

Kuniyoshi Ogura

Nagatoshi Wagatsuma

Motoki Torizuka

Toshio Kurihara

Fujio Kobayashi

Naoki Nakata

Hisayoshi Kato

Takema Hase

Naoki Ashizawa

Mitsuo Soeda

Shinji Yokoyama

Takahiro Kumonaka

Makoto Okada

Koichi Hasumi

Heihachiro Arai

Naomi Kobayashi

Akihiro Okubo

Toshiyuki Nishio

Takahiro Nishimoto

Hideo Kato

Reijiro Arakawa

Hikari Morita

Maki Tsujita

Noaki Nakata

Hikaru Morita

Miwa Yoshida

Chikako Shimizu

Naoki Abe

A heterocyclic compound useful as an antiallergic agent is provided. A compound represented by the following formula (1) or a salt thereof: 

Heterocyclic compound and H1 receptor antagonist

The compound of the present invention is a novel compound which has a specific heterocycle skeleton, particularly a pyrazolonaphthyridine or pyrazoloquinoline skeleton having an organic group (e.g., a carbocycle and a heterocycle) bonding through an alkylene group at 3-position and a carbocycle bonding at 5-position and has a phosphodiesterase IV inhibitory activity. At least one of the ring (the carbocycle or the heterocycle) bonding at 3-position of the pyrazolonaphthyridine skeleton and the carbocycle bonding at 5-position may have a halogenated alkyl group and/or a halogenated alkoxy group as a substituent. Such a compound or a salt thereof is useful as a phosphodiesterase IV inhibitor and the like. According to the present invention, a novel compound having a high phosphodiesterase IV inhibitory effect can be provided.

Heterocycle compound, and production process and application thereof

A novel spiroquinone derivative having a high ABCA1 stabilization effect and being useful for prophylactic and/or therapeutic agents for various diseases developing hypo-high density lipoproteinemia is obtained. The novel spiroquinone derivative is a compound represented by the following formula: 

Spiroquinone compound and pharmaceutical composition

To provide a pharmaceutically effective prophylactic/preventive agent for low-HDL cholesterolemia, focusing on an HDL-generating mechanism. The ABCA1 stabilizer of the present invention contains a bisphenol-type compound selected form probucol spiroquinone, probucol diphenoquinone, and probucol bisphenol as an effective ingredient. The ABCA1 stabilizer can continuously and stably express ABCA1 by a mechanism quite different from that of conventional processes, and thus is useful as prophylactic/preventive agent for low-HDL cholesterolemia or arteriosclerosis.

ABCA1 stabilizer

The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): wherein A is phenyl, pyridyl, 1-oxypyridyl, or thienyl, which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of hydroxyl, halogen, cyano, nitro, lower alkyl, lower alkoxy, lower alkylcarbonyloxy, amino, carboxyl, lower alkoxycarbonyl, carboxy-lower alkylene, lower alkoxycarbonyl-lower alkylene, lower alkylsulfonyl, lower alkylsulfonylamino, and ureido; Ris a group selected from the group consisting of hydrogen, hydroxyl, halogen, cyano, nitro, lower alkoxy, amino, carboxyl, and lower alkoxycarbonyl; Ris hydrogen or lower alkyl; and m is an integer of 1 to 3; or a pharmaceutically acceptable salt thereof, possesses highly excellent PDE IV-specific inhibitory actions and is useful as an anti-asthmatic drug and/or a prophylactic/therapeutic drug for COPD with high safety.

Pyrazolonaphthyridine derivative

The purpose is to provide selective PDE IV inhibitors which have a potent anti-asthmatic profile with excellent safety. A compound of the formula (1): wherein A is methylene, lower alkylmethylene, carbonyl, etc., Y is a 5- or 6-membered heteroaryl group containing one or two heteroatoms selected from nitrogen, sulfur and oxygen, Z is i) a fused ring in which any of 5- or 6-membered heteroaryl groups is fused to a benzene ring, or ii) a phenyl group which may be unsubstituted or optionally substituted with one or more members selected from the group consisting of nitro, amino, an amino nitrogen-containing group, etc., provided that when A is methylene, Y is a 5- or 6-membered heteroaryl group selected from the group consisting of pyrrolyl, pyridyl, etc., and Z is a phenyl group which may be unsubstituted or substituted, the substituent on said phenyl group is amino, or an amino nitrogen-containing group; or a pharmaceutically acceptable salt thereof, possesses excellent PDE IV inhibition and is useful as a pharmaceutical drug, preferably an anti-asthmatic, etc.

PDE IV inhibitors

1,8-naphthyridin-2(1H)-one derivatives

Pyrazole derivatives and COX inhibitors containing them

Unique benzothiazole derivatives which exert superior aldose redactase inhibiting actions are unexpectedly and advantageously useful in the prophylactic and therapeutic treatment of diabetic complications. A benzothiazole derivative compound of the formula (1): ##STR1## wherein X is halogen, R.sup.1 and R.sup.2, which are the same or different, are each independently hydrogen or halogen, A is a methylene group or a sulfur atom, and --B--COOR.sup.3 is a group as defined in the specification; or a pharmaceutically acceptable salt and a pharmaceutical composition comprising the same which is a useful prophylactic or therapeutic agent for the treatment of diabetic complications.

2-substituted benzothiazole derivatives and prophylactic and therapeutic

A pyridothiazineacetic acid compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, production thereof, and a pharmaceutical composition, an aldose reductase inhibitor and a preparation for the prevention and treatment of the complications of diabetes, containing the same. The pyridothiazineacetic acid compound and a pharmaceutically acceptable salt thereof of the present invention have an aldose reductase inhibitory action and are superior in safety. Accordingly, they are useful as a preparation for the prevention and treatment of the complications of diabetes, such as faulty union of corneal injury, cataract, neurosis, retinopathy and nephropathy, particularly, cataract and neurosis. In addition, the production method of the present invention enables efficient production of said pyridothiazineacetic acid compound.

Pyridothiazineacetic acid compound, production thereof and use thereof

1,4-benzoxazine-2-acetic acid compound, method for production thereof

Quinoline-3-acetic acid derivative, process for production thereof and

Benzothiazole compound, production thereof and use thereof

1,4-Benzothiazine-2-acetic acid derivatives having an excellent aldose reductase inhibitory activity which are useful for the prevention and treatment of diabetic complications, such as diabetic cataract, retinopathy, nephropathy and neuropathy.

1,4-benzothiazine-2-acetic acid derivatives

Phenylalkanoylamine derivatives, process for preparing the same, and

Growing community of inventors

Hamura, Japan

Tomoji Aotsuka