Daiichi Pharmaceutical Co., Ltd.

Daiichi Sankyo Company, Limited

Rie Miyauchi

Makoto Takemura

Hisashi Takahashi

Katsuhiro Kawakami

Kenichi Kimura

Isao Hayakawa

Hitoshi Ohki

Satoshi Komoriya

Masatoshi Nagamochi

Toshiyuki Takeda

Hiroaki Inagaki

Kazuyuki Sugita

Junichi Kuroyanagi

Youichi Kimura

Masao Itoh

Shin Iimura

Sunanda Ghosh Dastidar

Ashwani Kumar Verma

Satoru Miyauchi

Masayuki Ishizaki

Punit Kumar Srivastava

Kumaragurubaran Nagaswamy

Sonali Nanasaheb Pansare

Pradip Balu Wagh

Rijwan Jaffer Momin

Pramod Raosaheb Markad

Aniruddha Mondal

Balkrishna Ramchandra Kale

Soma Ghosh

Yogesh Balasaheb Khairnar

Lalima Sharma

Takeshi Murata

Kenichi Yoshida

Tetsuya Suzuki

Kiyoshi Nakayama

Takahiro Kitamura

Yasuyuki Takeda

Takashi Odagiri

Toshifumi Tsuda

Kazuo Kanai

Tsuyoshi Ohtani

Kenji Namba

Mayumi Tanaka

Masayasu Sekiguchi

The present invention provides a heterocyclic compound of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof or a hydrate thereof, wherein A, A' B, D, R, Rand Rare as defined herein, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) useful for treating or preventing a disease, condition or disorder associated with protein kinases, preferably Janus Kinase family.

Heterocyclic compounds as protein kinase inhibitors

A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure. 

Fused substituted aminopyrrolidine derivative

An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.

Tri-, tetra-substituted-3-aminopyrrolidine derivative

A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I): 

Substituted pyrrolidine derivative

A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by formula (I): 

3-(1-Aminocycloalkyl)pyrrolidinyl-substituted-6-dehalodeno(hydrogen-substituted)quinolon carboxylic acid derivatives having specific substituents as represented by the following formula (I), its salts, and hydrates thereof exhibit a broad and potent antibacterial activity on gram-negative and gram-positive bacteria, in particular, resistant bacteria typified by gram-positive cocci, including MRSA, PRSP and VRE. Thus these compounds are usable as drugs. 

Dehalogeno-compounds

The present invention provides a method for effectively producing an optically active form of tetrasubstituted-5-azaspiro[2.4]heptane derivative, which serves as a useful production intermediate for quinolonecarboxylic acid antibacterial agents, and intermediates for the derivative. The present invention is directed to a method for producing a compound (VII) according to the following scheme. 

Process for preparation of tetrasubstituted 5-azaspiro[2.4]- heptane derivatives and optically active intermediates thereof

To provide a quinolone antibacterial drug and a therapeutic agent for infectious diseases, which exhibit potent antibacterial activity on Gram-positive and Gram-negative bacteria and which is highly safe. A compound represented by the following formula (1): (wherein Rrepresents a C3-C6 cycloalkyl group which may have a substituent or the like; Rrepresents a hydrogen atom or the like; Rand Reach independently represent a hydrogen atom or a C1-C6 alkyl group, or a substituted carboxyl group derived from an amino acid, a dipeptide, or a tripeptide, and, in the case where each of Rand Rrepresents a C1-C6 alkyl group, the alkyl group may be substituted by one or more atoms or groups selected from among a hydroxyl group, a halogen atom, a C1-C6 alkylthio group, and a C1-C6 alkoxy group; and n denotes an integer of 1 to 3), a salt thereof, and a hydrate of the compound or the salt. Also, antibacterial drugs and therapeutic agents for infectious diseases are prepared.

8-cyanoquinolonecarboxylic acid derivative

A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein Rand Rrepresent hydrogen atom, or the like; Rrepresents an alkyl group containing 1 to 6 carbon atoms, or the like; Rand Rindependently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that Rand Rdo not simultaneously represent hydrogen atom; or the substituents Rand Rtogether represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by Rand Rto form a spirocyclic structure with the pyrrolidine ring; Rand Rindependently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; Rrepresents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; Xrepresents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II): 

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

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Tokyo, Japan

Rie Miyauchi