Fujisawa Pharmaceutical Company, Ltd.

Nippon Zoki Pharmaceutical Co., Ltd.

Takashi Ogino

Kunihiko Higashiura

Takao Takaya

Takashi Masugi

Kiyoshi Tsuji

Kazuhito Furukawa

Masaaki Matsuo

Taizo Ito

Hisashi Takasugi

Hiroshi Matsuda

Hideaki Yamanaka

Keiji Matsuda

Nobukiyo Konishi

Kenji Murano

David Barrett

Hachiro Seno

Kyoichi Shimomura

Takahiro Matsuya

Norihiro Igari

Takeshi Kato

Mitsuru Naiki

Katsuya Nakamura

Hidenori Ohki

Kazuo Okumura

Tadashi Terasaka

Hiroaki Mizuno

Takashi Tojo

Norio Hashimoto

Hirofumi Yamamoto

Taisuke Hasegawa

Atsushi Kanda

Ayako Toda

Masaharu Ichihara

Nobuyuki Shiraishi

Kazuyoshi Sawada

Atsushi Ohigashi

Tomoyuki Okada

Koji Kunimasu

Yuriko Yamazaki

Yuka Noda

Hiroyuki Iwatsuki

Yukari Konishi

A novel coumarin derivative or a pharmaceutically acceptable salt thereof and also to provide a pharmaceutical agent containing such a compound as an active ingredient is provided. The coumarin derivative or a pharmaceutically acceptable salt thereof exhibits an excellent suppressive action to the destruction of cartilage and suppressive action to the proliferation of synovial cells in a pharmacological test where the release of sulfated glycosaminoglycans (sGAG) and the proliferation of synovial cells are used as indicators whereby it is very useful as an active ingredient of a pharmaceutical composition such as a preventive or therapeutic agent for arthropathy such as osteoarthritis or chronic rheumatoid arthritis.

Coumarin derivative

An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, Rand R, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; Rand R, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.

Aminopropylidene derivative

Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.

Process for producing thiabenzoazulene-propionic acid derivative

The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.

Piperidine derivative

The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low intracerebral migration even when a mouse that is orally administered with the compound is subjected to an intracerebral receptor binding test, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The oxepin derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.

Oxepin derivative

Disclosed is a novel benzyloxypropylamine derivative having an excellent tachykinin receptor antagonistic effect. This compound shows a good transfer into the blood and a long blood half-life in the blood kinetic test using a guinea pig orally administered with the compound and is stable in an animal plasma. The compound also shows a high transfer to the central nervous system when it is orally administered to a guinea pig at a certain dose. Accordingly, the benzyloxypropylamine derivative is quite useful as a novel anti-tachykinin agent.

Benzyloxypropylamine derivative

A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof:wherein each of Xand Xis oxygen or two hydrogen atoms, XO, NH, NCH, or CH, n is an integer of 0 or 1, Ris hydrogen or lower alkyl and Ris hydrogen, cyano, tetrazolyl, aminotriazolyl , mesyl, t-butoxycarbonyl, or a lower alkyl which may be optionally substituted, Ris hydrogen, halogen, lower alkyl or lower alkoxy, each of Rand Ris hydrogen, lower alkoxy or trifluoromethyl, and a broken line indicates a single or double bond. The derivative may be used as a tachykinin antagonist in the treatment of diseases of the digestive system, nervous system and respiratory system, inflammation, allergy, carcinoid syndrome, chronic pain, headache, Crohn disease, depression and vomiting.

2-phenylpiperazine derivatives

This invention relates to new polypeptide compound represented by the general formula (I) wherein R, R, R, R, Rand Rare as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on &#x3b2;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases includinginfection (e.g.pneumonia) in a human being or an animal.

Cyclic hexapeptide derivatives

This invention relates to new polypeptide compound represented by general formula (I), wherein R, R, R, R, Rand Rare as defined in the description or a salt thereof which has antimicrobial activities (especially, antifungal activities), inhibitory activity on &#x3b2;-1,3-glucan synthase, to process for preparation thereof, to a pharmaceutical composition comprising the same, and to a method for prophylactic and/or therapeutic treatment of infectious diseases includinginfection (e.g.pneumonia) in a human being or an animal.

Cyclic hexapeptides having antibiotic activity

1,5-diphenylpyrazole derivatives

Compounds which exhibit excellent bronchodilating action with low side effects and are 7-amino-1-phenylpyrido&lsqb;2,3-d&rsqb;pyrimidine-2,4-dione derivatives represented by the formula (I) or a pharmaceutically acceptable salt or hydrate thereof:

7-aminopyrido&lsqb;2,3-D&rsqb;pyrimidine derivatives

The present invention relates to new pyrazole derivatives represented by the following general formula (I) ##STR1## wherein R.sup.1 is aryl which is substituted with substituent(s) selected from the group consisting of lower alkylthio, cyclo(lower)alkyl, hydroxy, hydroxy(lower) alkyl, cyano, lower alkylenedioxy, acyl, acyloxy, aryloxy and lower alkoxy optionally substituted with acyl or lower alkoxy,

Pyrazole derivatives, processes for preparation thereof and

The present invention relates to new pyrazole derivatives represented by the following general formula (I) ##STR1## wherein R.sup.1 is aryl which is substituted with substituent(s) selected from the group consisting of lower alkylthio, cyclo(lower)alkyl, hydroxy, hydroxy(lower)alkyl, cyano, lower alkylenedioxy, acyl, acyloxy, aryloxy and lower alkoxy optionally substituted with acyl or lower alkoxy, R.sup.2 is halogen, halo(lower)alkyl, cyano or acyl, and R.sup.3 is aryl substituted with nitro, hydroxy, lower alkoxy, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, provided that when R.sup.3 is aryl substituted with nitro, hydroxy or lower alkoxy, then R.sup.1 is aryl substituted with lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl, and pharmaceutically acceptable salts thereof.

Compounds of the formula: ##STR1## wherein A is S, SO, or SO.sub.2, R.sup.1 is H or acyl, R.sup.2 is H, alkyl, hydroxyalkyl, halogen or carboxy, and R.sup.3 is pyridyl are claimed. The compounds are useful as therapeutic agents for the treatment of e.g. rheumatism, nephritis and thrombocytopenia.

Thiazole derivatives, processes for production thereof and

Compounds of the formula: ##STR1## wherein A is S, SO, or SO2, R1 is H or acyl, R2 is H, alkyl, hydroxyalkyl, halogen or carboxy, and R3 is pyridyl are claimed. The compounds are useful as therapeutic agents for the treatment of e.g. rheumatism, nephritis and thrombocytopenia.

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Kato, Japan

Takashi Ogino