Shionogi Company Limited

Purdue Pharma L.p.

Hidenori Mikamiyama

Yoshiyuki Taoda

Makoto Kawai

Toshiyuki Akiyama

Kenji Tomita

Naoyuki Suzuki

Kenji Morimoto

Moriyasu Masui

Naoki Tsuno

Kenji Takaya

Akira Matsumura

Kosuke Anan

Minako Mikamiyama

Bin Shao

Masahiro Fuji

Hitoshi Murai

Masayoshi Miyagawa

Chika Takahashi

Laykea Tafesse

Jiangchao Yao

Makoto Adachi

Chiyou Ni

Kayoko Hata

Chika Kageyama

Minamo Iwata

The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.

Substituted polycyclic carbamoyl pyridone derivative prodrug

This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.

Substituted polycyclic carbamolypyridone derivative

Substituted polycyclic carbamoylpyridone derivative

The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R-R, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate 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. 

Benzenesulfonamide compounds and the use thereof

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 invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SO; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. Rand Rare each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently &#x2550;O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate 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. 

Oxyimino compounds and the use thereof

The invention relates to oxycarbamoyl compounds of Formula I:  The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate 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.

Oxycarbamoyl compounds and the use thereof

The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R, R, m, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat 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. 

Tetrahydropyridinyl and dihydropyrrolyl compounds and the use thereof

It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR, Ais a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., Ais an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R, R, R, R, Rand Rare each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is &#x2014;(CRR)m-, &#x2014;CO(CRR)n-, &#x2014;CONR(CRR)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, Rand Rare each independently hydrogen, halogen, hydroxy etc., and Ris hydrogen or lower alkyl,or a pharmaceutically acceptable salt, or a solvate thereof.

Nitrogen-containing heterocycle derivatives substituted with cyclic group

A compound of the formula (I): wherein Z, Zand Zeach is independently carbon atom or nitrogen atom; Y is hydroxy, mercapto or amino; Ris a group of the formula: (wherein C ring is nitrogen-containing heteroaryl) has an inhibitory activity against integrase.

Nitrogen-containing heteroaryl compounds having inhibitory activity against HIV integrase

Compounds of Formula (1), pharmaceuticals containing the same, especially anti-HIV agents having anti viral activity, especially inhibitory activity against HIV integrase, wherein X represents either one of the following groups: (wherein, C ring is nitrogen-containing aromatic heterocyclic ring in which at least one atom in atoms neighboring the atom bound to the pyrimidine ring is unsubstituted nitrogen atom; Ris hydrogen or lower alkyl; D ring is aryl or heteroaryl) Zand Zeach is independently a single bond, O, S, S(&#x2550;O) or SO; Zis a single bond, lower alkylene or lower alkenylene; Ar is optionally substituted aryl or optionally substituted heteroaryl; Ris lower alkyl, substituted lower alkyl or the like; Ris a hydrogen atom or optionally substituted lower alkyl; or Rand Rmay form, together with an adjacent atom, an optionally substituted heterocyclic ring, a pharmaceutically acceptable salt or a solvate thereof.

Growing community of inventors

Osaka, Japan

Hidenori Mikamiyama