Astellas Pharma Gmbh

Comentis, Inc.

Ryosuke Munakata

Kiyohiro Samizu

Makoto Inoue

Noriyuki Kawano

Shingo Yamasaki

Hisao Hamaguchi

Lin Hong

Hiroaki Tominaga

Satoshi Aoki

Junji Sato

Seiji Yoshimura

Koichi Yonezawa

Takanori Koike

Takahiro Ishii

Hideyuki Watanabe

Akio Kamikawa

Takashi Sugane

Hirokazu Kubota

Nobuyuki Shiraishi

Masakatsu Kawakami

Toru Asano

Yasuhiro Shiina

Daisuke Sasuga

Yohei Koganemaru

Kayoko Mihara

Kazuyuki Hattori

Hiroaki Hoshii

Tetsuo Kiso

Hiroki Fukudome

Takahiro Kuramochi

Tomoaki Kawano

Junko Maeda

Yasuhiro Shina

Hiromasa Oka

Ryoji Hirabayashi

The present invention provides a hydrate of N-[(4S)-2-amino-2',2&#x2032;-dimethyldispiro[1,3-oxazole-4,4&#x2032;-chromene-3&#x2032;,3&#x2033;-oxetan]-6&#x2032;-yl]-5-chloropyridine-2-carboxamide which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by &#x3b2;-secretase activity, hydrolysis of a &#x3b2;-secretase site of a &#x3b2;-amyloid precursor protein, and/or &#x3b2;-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.

Chromane compounds

The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by &#x3b2;-secretase activity, hydrolysis of a &#x3b2;-secretase site of a &#x3b2;-amyloid precursor protein, and/or &#x3b2;-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.

[Problem] A compound, which can be used for preventing or treating diseases, in which 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with &#x2014;O&#x2014; (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11&#x3b2;-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.

Triazole derivative or salt thereof

A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.

Azole compound

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

Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.

Triarylcarboxylic acid derivative

Growing community of inventors

Tokyo, Japan

Ryosuke Munakata