Astellas Pharma Gmbh

Kotobuki Pharmaceutical Co Ltd

Kotobuki Pharmaceuticals Co., Ltd.

Takashi Sugane

Takahiro Ishii

Takeshi Murakami

Yoshinori Kobayashi

Atsushi Noda

Kentaro Sato

Jun Maeda

Hiroshi Tomiyama

Ryota Shiraki

Kazuhiro Ikegai

Masakazu Imamura

Kyoichi Maeno

Takatoshi Kanayama

Akio Kakefuda

Takahiko Tobe

Chikashi Saitoh

Tatsuhisa Takahashi

Fumiyoshi Iwasaki

Eiji Kurosaki

Kayoko Kitta

Jotaro Suzuki

Fumie Narazaki

Chisato Kanai

Daisuke Yamashita

Hartmut Greiner

Hiroyuki Moritomo

Itsuro Shimada

Wataru Hamaguchi

Norio Asai

Junji Miyata

Takeshi Suzuki

Naomi Hosogai

Tetsuya Kimizuka

Atsuyuki Kohara

Takuma Morita

Michael Arlt

Satoshi Aoki

Noriyuki Kawano

Keizo Sugasawa

Takafumi Shimizu

Yasuhiro Yonetoku

Ryosuke Munakata

Takuya Makino

Hisashi Mihara

Kiyohiro Samizu

Daisuke Tanabe

Ryo Mizoguchi

Yuji Awamura

Noritaka Hamada

Kazuhiko Osoda

Kuniyuki Sano

Takaaki Sakaida

Yu Iwakawa

Hiromasa Oka

Ryota Astellas Pharma Inc Shiraki

[Problem] To provide a compound useful as an MCreceptor agonist. [Means for Solution] The present inventors studied MCreceptor agonists, and have found that a piperazine derivative has an MCreceptor agonistic action, thereby completing the present invention. The piperazine derivative of the present invention has an MCreceptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.

Piperazine derivative

To provide a compound which can be used as an MCreceptor agonist. The present inventors have investigated MCreceptor agonists, and have found that a piperazine derivative has an action related to the agonists, thereby completing the present invention. That is, the piperazine derivative of the present invention has an MCreceptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.

Object Provided are &#x3b2;-form crystal, &#x3b3;-form crystal, and &#x3b1;-form crystal of a benzoxadiazole derivative, wherein a uniform crystal having sufficient qualities can be obtained with high reproducibility, and they can be anytime supplied as crystals of drug substance for use in producing pharmaceuticals, are particularly suitable for mass synthesis in industrial production, hardly exhibit hygroscopicity and have particularly excellent photo-resistance. Means for Resolution A solving means includes &#x3b2;-form crystal of 4-[3-isopropyl-5-(6-phenyl-3-pyridyl)-4H-1,2,4-triazol-4-yl]-2,1,3-benzoxadiazole, which shows an endothermic peak at 145 to 150&#xb0; C. according to a differential scanning calorimeter analysis (DSC analysis) and shows X-ray powder diffraction peaks at 9.8, 11.1, 12.8, 13.3, 17.1, 20.2, 21.2 and 22.3 in 2&#x3b8;(&#xb0;), and the like.

Crystals of benzoxadiazole derivative

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

The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via &#x2014;X&#x2014; and A ring is directly bonded to the glucose residue, and it is usable as a Na-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

C-glycoside derivatives and salts thereof

A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound

To provide a compound usable for treatment of diseases associated with fatty acid amide hydrolase (FAAH), especially for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain. We have found that a novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative and its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivative of the present invention has an excellent effect for increasing an effective bladder capacity, an excellent effect for relieving urinary frequency and an excellent anti-allodynia effect, and is therefore usable for treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

A novel pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound or its pharmaceutically acceptable salt has a potent FAAH-inhibitory activity. Further, the pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate compound of the present disclosure is also useful in the treatment of urinary frequency and urinary incontinence, overactive bladder and/or pain.

The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.

Triazole derivative

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Tokyo, Japan

Takashi Sugane