Astellas Pharma Gmbh

Tetsuo Kiso

Takahiro Kuramochi

Satoshi Miyamoto

Toshihiro Watanabe

Kazuhiro Ikegai

Hironori Harada

Norio Asai

Noriko Ishikawa

Shohei Shirakami

Seijiro Akamatsu

Koichi Yonezawa

Ryosuke Munakata

Yohei Koganemaru

Mina Tsukamoto

Ryoji Hirabayashi

[Problem] Provided is a pharmaceutical, in particular, a pharmaceutical composition which is useful for the treatment of pain. [Means for Solution] The present inventors have made extensive studies using model animals with pain for the purpose of providing a therapeutic agent for pain. As a result, they have found that 11&#x3b2;-hydroxydehydrogenase type 1 (11&#x3b2;-HSD1) inhibitor, in particular, a triazole compound having a cyclic group at the 3-position (or 5-position) of a triazole ring has a good effect of ameliorating chronic pain. That is, according to the present invention, a pharmaceutical composition comprising an 11&#x3b2;-HSD1 inhibitor, in particular, the triazole compound of the present invention, as an active ingredient, is useful for the treatment of pain (particularly, neuropathic pain or fibromyalgia).

Therapeutic agent for pain

To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation. The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

2-aminobenzamide derivatives

There is provided a compound having a capsaicin receptor VR1 inhibitory activity and useful as a therapeutic agent for various pains including inflammatory pain and neurogenic pain, migraine, cluster headache, bladder diseases including overactive bladder, and the like. A benzamide derivative or a salt thereof wherein a benzene ring is attached to a D ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring) through an amide bond, the benzene ring is directly bonded to an E ring (a monocyclic or bicyclic hydrocarbon ring or a monocyclic or bicyclic heteroaromatic ring), and the benzene ring is further bonded to A (an amino moiety, a monocyclic or bicyclic heterocycle) through L (a lower alkylene).

Benzamide derivative or salt thereof

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Tokyo, Japan

Tetsuo Kiso