Daiichi Pharmaceutical Co., Ltd.

Daiichi Sankyo Company, Limited

Katsuhiro Kawakami

Makoto Takemura

Hisashi Takahashi

Rie Miyauchi

Hitoshi Ohki

Kenichi Kimura

Youichi Kimura

Isao Hayakawa

Toshiyuki Takeda

Tetsuya Suzuki

Kazumasa Aoki

Masao Itoh

Kazuki Yano

Shohgo Atarashi

Hiroshi Takeshita

Takao Horiuchi

Junichi Kuroyanagi

Syozo Kobayashi

Yoichi Kimura

Kentoku Gotanda

Yuichi Sugimoto

Issei Achiwa

Yusuke Yukimoto

Norikazu Matsuhashi

Kazuo Kanai

Tazuo Uemura

Keiji Uchiyama

Toshihiro Kiho

Atsushi Tengeiji

Tsuyoshi Ohtani

Haruko Kawato

Masayasu Sekiguchi

Mayumi Tanaka

Norimasa Mikata

Kenji Namba

Compounds or pharmacologically acceptable salts thereof for promoting osteogenesis, improving bone metabolism, preventing or treating bone fracture, preventing or treating a disease associated with bone metabolism, or in the field of orthopedics for the promotion of healing of bone fracture, a bone defect, and bone diseases such as osteoarthritis as well as in the field of dentistry for the treatment of periodontal disease and the stabilization of artificial tooth root. The compounds are represented by formula (I) or a pharmacologically acceptable salt thereof: 

Chromone derivative having osteogenesis promoting effect

A 1,6-&#x3b2;-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-&#x3b2;-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound. Concretely, provided is a compound of the following formula (I), its salt or hydrate, and a drug or antifungal containing, as the active ingredient, the compound, its salt or hydrate: 

Antifungal bicyclic hetero ring compounds

This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein Ris an optionally substituted aromatic group, a salt of the same or a hydrate of both.  In the formula, R, R: hydrogen atom, an alkyl group; R, R, R: hydrogen atom, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R, R: hydrogen atom, an alkyl group; R: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R:hydrogen atom, an alkylthio group; R: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X: halogen atom, a hydrogen atom; A: nitrogen atom, C&#x2014;X; X: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A, A:&#x3e;C&#x2550;C (&#x2014;A&#x2550;)&#x2014;N(&#x2014;R)&#x2014;, &#x3e;N&#x2014;C (&#x2014;A&#x3e;)&#x2550;C(&#x2014;R)&#x2014;; Rand Ror Rand Xmay be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.

Aminomethylpyrrolidine derivatives having aromatic substituents

An anti acid-fast bacterial agent containing, as an active ingredient, a pyridonecarboxylic acid derivative represented by the following general formula (1), a salt thereof, or a hydrate thereof, which shows excellent antibacterial activity againstand atypical acid-fast bacteria and exhibits good pharmacokinetics and safety 

Anti acid-fast bacterial agent containing pyridonecarboxylic acids as active ingredient

(&#x2212;)-7-[(7S)-7-Amino-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R, 2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid.1HCl.1HO and antibacterial compositions containing this compound. The compound of the present invention exhibits not only excellent antibacterial activity and safety, but also remarkable stability against light and humidity, and is thus useful as an antibacterial agent.

Quinolonecarboxylic acid derivative

Tricyclic amine derivatives

A quinolone derivative represented by formula (I):

Cycloalkylaminomethylpyrrolidine derivatives

A pyridobenzoxazine derivative having a bicyclic amine derivative as its substituent, represented by the formula (I):

Bicyclic amine derivative

Pyridonecarboxylic acid derivatives substituted by a bicyclic amino

A method for selectively obtaining any one of an anhydrate, a 1/2 hydrate, a 1 hydrate, and a 3/2 hydrate of 7-�(7-(S)-amino-5-azaspiro�2.4!heptan-5-yl!-8-chloro-6-fluoro-1-�(1R,2S)-2 -fluorocyclopropyl!-4-oxo-1,4-dihydroquinoline-3-carboxylic acid is disclosed, comprising treating the compound in an aqueous solvent or water or recrystallizing the compound from an aqueous solvent or water.

Crystals of antimicrobial compound

An optically active pyridobenzoxazine derivative represented by formula (I): ##STR1## wherein R.sup.1 and R.sup.2 wherein R.sup.1 and R.sup.2, which may be the same or different, each represent an alkyl group having from 1 to 6 carbon atoms, a halogenated alkyl group having from 1 to 6 carbon atoms, a hydroxyalkyl group having from 1 to 6 carbon atoms, or an alkoxymethyl group having from 2 to 7 carbon atoms; R.sup.3 represents a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, an acyl group having from 2 to 7 carbon atoms, a halogen-substituted or unsubstituted alkyloxycarbonyl group having from 2 to 7 carbon atoms, a phenylmethyloxycarbonyl group, or a phenylmethyloxycarbonyl group whose phenyl moiety is substituted with a halogen atom, a nitro group, or a methoxy group; R.sup.4 represents a methyl or fluoromethyl group which is in a .beta.-configuration; R.sup.5 represents a hydrogen atom, an amino group, a hydroxyl group, a methyl group, or a halogen atom; and X represents a fluorine atom or a chlorine atom, and a salt thereof are disclosed. These compounds exhibit potent antimicrobial activity with broad antimicrobial spectra and improved lipophilic properties.

Optically active pyridobenzoxazine derivatives

Growing community of inventors

Tokyo, Japan

Katsuhiro Kawakami