Daiichi Sankyo Company, Limited

Daiichi Pharmaceutical Co., Ltd.

Hiroyuki Naito

Toshiharu Ohta

Syozo Kobayashi

Kenji Yoshikawa

Hideyuki Kanno

Tsutomu Nagata

Kouichi Uoto

Satoshi Komoriya

Makoto Ono

Toshiharu Yoshino

Yumi Nakamoto

Noriyasu Haginoya

Akiyoshi Mochizuki

Makoto Takemura

Hisashi Takahashi

Rie Miyauchi

Yasunori Ono

Hiroaki Inagaki

Masatoshi Nagamochi

Yasuhiro Nakagami

Takashi Ohnuki

Mayumi Iizuka

Kayoko Masuda

Emiko Hatano

Kazuhiro Yoshida

Yuji Kasuya

Haruhiko Horino

Kenichi Yoshida

Masayuki Ito

Tatsuya Inoue

Takayasu Nagahara

Atsunobu Sakamoto

Masako Minami

Masaru Iwasaki

Yoko Murakami

Masanori Suzuki

Kiyoshi Nakayama

Takahiro Kitamura

Yasuyuki Takeda

Junichi Kuroyanagi

Taisaku Tanaka

Takashi Odagiri

Toshifumi Tsuda

Kazuo Kanai

Toshihiro Kiho

Tatsuya Yano

It is an object of the present invention to provide a new compound capable of efficiently inducing differentiation from pluripotent stem cells into insulin-producing cells. The object of the present invention is achieved by a compound represented by formula (I): 

Dihydroindolizinone derivative

The present invention relates to a terpenoid derivative that has the ability to activate the Keap1/Nrf2/ARE signaling pathway and is excellent in anti-inflammatory action and cytoprotective action, and a sustained-release pharmaceutical composition effective for the treatment and prevention of a posterior eye disease caused by oxidative stress, comprising the terpenoid derivative as an active ingredient. The present invention provides a local administration-type sustained-release pharmaceutical composition for the treatment or prevention of a posterior eye disease, comprising the terpenoid derivative of the present invention as an active ingredient, wherein the sustained-release pharmaceutical composition maintains a pharmacological action thereof for 1 week or longer by the sustained release of the terpenoid derivative under physiological conditions and has a base material administrable to the vitreous body and a form administrable to the vitreous body.

Sustained-release pharmaceutical composition for treatment and prevention of eye disease

It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway. The present invention provides terpenoid derivative A represented by the following formula (I): 

Terpenoid derivatives

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 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): 

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

A compound represented by formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q&#x2003;&#x2003;(1)[wherein Rand Rare hydrogen atoms or the like; Qis a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Qis a single bond or the like; Qrepresents the following group: (wherein Qis an alkylene group having 1 to 8 carbon atoms, or the like); and Tand Tare carbonyl groups or the like], a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after artificial valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

Diamine derivatives

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): 

A compound represented by the general formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q&#x2003;&#x2003;(1)wherein Rand Rare hydrogen atoms or the like; Qis a saturated or unsaturated, 5- or 6-membered cyclic hydrocarbon group which may be substituted, or the like; Qis a single bond or the like; Qis a group in which Qis an alkylene group having 1 to 8 carbon atoms, or the like; and Tand Tare carbonyl groups or the like; a salt thereof, a solvate thereof, or an N-oxide thereof. The compound is useful as an agent for preventing and/or treating cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.

Sulfonyl derivatives

Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: &lsqb;wherein R is hydrogen, hydroxyl, nitro or the like; R and R are each independently hydrogen, halogeno or the like; R and R are each dependently hydrogen, halogeno or the like; Q is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q is a single bond, oxygen or the like; Q is, e.g., a group represented by formula (a): T is carbonyl or the like; and X and X are each independently methylidyne or nitrogen&rsqb;. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.

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Tokyo, Japan

Satoshi Komoriya