Shionogi Company Limited

Purdue Pharma L.p.

Shionogi & Co., Ltd.

Tatsuhiko Ueno

Naoki Tsuno

Shinji Suzuki

Yuuji Kooriyama

Shuji Yonezawa

Chiaki Fujikoshi

Sae Matsumoto

Xiaoming Zhou

Yukio Tada

Yuusuke Tamura

Akira Yukimasa

Hiroki Yamaguchi

Akihiro Hori

Kazuya Okamoto

Motohiro Fujiu

Takatsugu Inoue

Terukazu Kato

Yoshio Hato

Yusuke Ichihashi

Jeffrey Michael Marra

Hiromi Kudo

Shohei Majima

Takashi Toyota

Yuusuke Satou

Toshikazu Hakogi

The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity. In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof. 

Stereoselective process for preparing substituted polycyclic pyridone derivatives

The present invention is related to a compound represented by formula (I) wherein &#x2014;X&#x2014; is &#x2014;NH&#x2014; or &#x2014;S&#x2014;; &#x2014;Z&#x2014; is &#x2014;O&#x2014; or &#x2014;S&#x2014;; R, Rand Rare each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like; Ris a cyano, substituted or unsubstituted amino, or the like; Ris each independently a halogen; b is 0 or 1; or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.

Aromatic heterocyclylamine derivative having TRPV4-inhibiting activity

The following compound is provided as an agent for treating a disease induced by production, secretion and/or deposition of amyloid &#x3b2; protein, for example, 

Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity

The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R, R, Q, Y, Z, A, B, Q, E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.

Cyclic urea- or lactam-substituted quinoxaline-type piperidines as ORL-1 modulators

The present disclosure relates to Oxime-Substituted Quinoxaline-Type Piperidine Compounds, such as those of Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, R, Q, Y, Z, A, B, and a are as defined herein; compositions comprising an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an Oxime-Substituted Quinoxaline-Type Piperidine Compound.

Oxime-substituted-quinoxaline-type piperidine compounds as ORL-1 modulators

This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; Ris optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; Rand Rare each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R, R, Rand Rare each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.;a pharmaceutically acceptable salt or solvate thereof,which is useful for treating diseases induced by production, secretion and/or deposition of amyloid &#x3b2; protein.

Aminodihydrothiazine derivatives substituted with a cyclic group

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Osaka, Japan

Tatsuhiko Ueno