Shionogi Company Limited

Sumitomo Chemical Company, Limited

Sumitomo Chem.co., Ltd.

Moriyasu Masui

Kazuya Okamoto

Yukihito Sumino

Hiroyuki Kai

Akira Takase

Kuniyoshi Nishida

Fumiya Ikarashi

Daisuke Yamada

Hidenori Mikamiyama

Toshiyuki Akiyama

Akihiro Hori

Naoki Tsuno

Michio Masuko

Akihiko Nakamura

Norihiko Tanimoto

Toshikazu Ohtsuka

Akira Matsumura

Yujiro Kiyoshima

Mikio Sasaki

Katuhisa Masumoto

Katsuaki Ohba

Takami Takeda

Diasuke Yamada

Kazuo Ueda

Makoto Adachi

Noriyuki Kurose

Yasunori Mitsuoka

Kosuke Anan

Genta Tadano

Naohiro Onodera

Tsuneo Iwakawa

Ken-ichi Kusakabe

Syuhei Yoshida

Kayoko Hata

A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Ris an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein Ris hydrogen, halogen, or the like; Ris hydrogen, a lower alkyl optionally substituted with substituent E, or the like; Ris a lower alkyl optionally substituted with substituent E, or the like; and Ris a lower alkyl group optionally substituted with substituent group E, or the like].

Crystalline methyl (4R,12aS)-7-(benzyloxy)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2&#x2032;:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxylate

A crystalline methyl (4R,12aS)-7-(benzyloxy)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2&#x2032;:4,5] pyrazino[2,1-b][1,3]oxazine-9-carboxylate of the formula (U2): 

A crystalline dimethyl 2-(benzyloxy)-1-(2,2-diethoxy-ethyl)-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate of the formula (U1): 

Crystalline dimethyl 3-(benzyloxy)-1-(2,2-dimethoxyethyl)-4-oxo-1,4-dihydropyridine-2,5-dicarboxylate

A process for preparing a compound shown by formula (W6): wherein each Hal is independently chloro or bromo, using a novel process for preparing a pyridine derivative represented by formula (W2), wherein Ris as defined herein.

Method of producing (3S,11aR)-6,8-dihalo-3-methyl-2,3,11,11a-tetrahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-5,7-diones

A process for preparing a compound shown by formula (W5): wherein each Hal is independently chloro or bromo, using a novel process for preparing a pyridine derivative represented by formula (W2), wherein Ris as defined herein.

Method of producing (4R,12aS)-7,9-dihalo-4-methyl-3,4,12,12a-tetrahydro-2H-pyrido[1',2&#x2032;:4,5]pyrazino[2,1-b][1,3]oxazine-6,8-diones

The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-&#x3b2; proteins. A compound of the formula (I): wherein R, R, R, R, R, R, ring A and the dashed lines are defined in the specification,its pharmaceutically acceptable salt or a solvate thereof.

Oxazine derivatives

A process for preparing a compound represented by formula (Y1) or (Y2) wherein Ris an optionally substituted carbocyclyl lower alkyl, or the like or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) wherein R, R, and Rare as defined herein.

Methods of producing substituted (3S,11aR)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-Hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamides

The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.

Method of producing pyrone and pyridone derivatives

Methods of producing substituted (4R,12AS)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12A-hexahydro-2H-pyrido[1',2&#x2032;:4,5]pyrazino[2,1-B][1,3]oxazine-9-carboxamides

Method for producing pyrone and pyridone derivatives

The present invention provides, for example, the following compound: 

Fused aminodihydropyrimidine derivative

The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain. 

Acrylamide compounds and the use thereof

The present invention provides a compound of formula (I): wherein

Oxazine derivatives and a pharmaceutical composition for inhibiting BACE1 containing them

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Osaka, Japan

Moriyasu Masui