Sankyo Company, Limited

Daiichi Sankyo Company, Limited

Toshiyuki Konosu

Sadao Oida

Takuya Uchida

Takeo Miyaoka

Yawara Tajima

Makoto Mori

Yoshiko Kagoshima

Hiroshi Yasuda

Yasushi Takahashi

Teruo Tanaka

Noriko Takeda

Tsuyoshi Soneda

Atsushi Somada

Nobuhisa Masuda

Yuko Yamamoto

Satoshi Ohya

Hiroshi Takeshita

Junichi Kuroyanagi

Tetsunori Fujisawa

Issei Achiwa

Aki Yokomizo

Akihiko Nakagawa

Takafumi Hosokawa

Tetsuji Noguchi

Kazuo Sato

Naoki Tanaka

Tetsuya Suzuki

Tomio Kimura

Hideo Takeshiba

Atsuhiro Sugidachi

Hisaki Kajino

Junzo Tobitsuka

Yukiyoshi Takahi

Makoto Yamaoka

Jitendra Anant Sattigeri

Hiroshi Ohta

Hiroyuki Itoh

Manoj Kumar Khera

Tarun Mathur

Ryo Itooka

Takahiro Shibayama

Jitendra A Sattigeri

Problem to be Solved There is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use. Solution to the Problem As a result of intensive research, the present inventors have found that a compound represented by general formula (I), 

Hydroxyalkyl thiadiazole derivatives

To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.

Imidazole carbonyl compound

An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.

A compound having the general formula (I) wherein Rrepresents C1-C6 alkyl, etc., Rrepresents hydrogen, C2-C7 alkanoyl, C7-C11 arylcarbonyl, the formula R&#x2014;(CH)&#x2014;, etc., Rrepresents C6-C10 aryl, etc., X, X, X, Xand Xeach independently represents hydrogen, halogen, etc., and n represents an integer of 0 to 2, pharmacologically acceptable salts thereof or prodrugs thereof. They have excellent inhibition of platelet activation, etc. and are useful as a prophylactic or therapeutic agents for diseases related to thrombus or embolus formation.

Cyclic amine derivative having heteroaryl ring

A triazole compound of the formula (I) or a pharmacologically salt thereof: wherein X represents a group of formula X&#x2014;OH which has antifungal activity, L represents an -(adjacently substituted C-Caryl)-CHgroup and R represents a &#x2014;P(&#x2550;O)(OH)group.

Water-soluble triazole fungicide

Amide-type triazole compounds

Triazole derivatives having antifungal activity

Triazole antifungal agent

A triazole compound having the formula: ##STR1## wherein Ar.sup.1 represents an optionally substituted phenyl, Ar.sup.2 represents an optionally substituted phenyl, R.sup.0 represents a hydrogen atom or a lower alkyl; R.sup.1 represents a lower alkyl; R.sup.2 to R.sup.5 represent a hydrogen atom or an unsubstituted or halo substituted alkyl, n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; and A represents a 1,3-dioxan-5-yl. The triazole compound of the present invention exhibits an excellent antifungal activity.

Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; is R.sup.1 is alkyl; R.sup.2 is substituted alkyl, substituted cycloalkyl R.sup.2 or optionally substituted heterocyclic; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.

Anti-fungal triazole derivatives, their uses

Compounds of formula (I): ##STR1## in which: Ar is optionally substituted phenyl; R.sup.1 is alkyl; R.sup.2 is substituted alkyl or substituted cycloalkyl; and n is 0, 1 or 2; and pharmaceutically acceptable salts and esters thereof have valuable anti-fungal properties and can be used for pharmaceutical and veterinary treatment. Methods of preparing these compounds are also provided.

Anti-fungal triazole derivatives

Compounds of formula (I): ##STR1## [in which: R.sup.1 and R.sup.2 are hydrogen or alkyl, or together are cycloalkyl; R.sup.3 and R.sup.4 are hydrogen, alkyl or phenyl, or together are cycloalkyl; or R.sup.1 and R.sup.3 together are cycloalkyl fused to the oxetane ring; Ar is phenyl substituted by R.sup.5, R.sup.6 and R.sup.7, where R.sup.5, R.sup.6 and R.sup.7 are hydrogen, halogen, alkyl, alkoxy, halogenated alkyl or halogenated alkoxy; and R.sup.8 and R.sup.9 are hydrogen or alkyl] and salts thereof have valuable agricultural and pharmaceutical anti-fungal or fungicidal activity. They may be prepared by a variety of processes.

Oxetane derivatives and their use as anti-fungal or fungicidal agents

Growing community of inventors

Kanagawa, Japan

Toshiyuki Konosu