Banyu Pharmaceutical Co. Ltd

Msd K.k.

Norikazu Otake

Yoshio Ogino

Akio Kanatani

Susumu Nakagawa

Kenji Matsuda

Ryosuke Ushijima

Kazuhito Noguchi

Akira Naya

Tomoshige Numazawa

Koji Yamada

Yuji Haga

Fumio Nakano

Toshifumi Kimura

Takehiro Fukami

Akira Asai

Satoru Kuroyanagi

Ryuji Mitomo

Minoru Moriya

Yoshiharu Tanaka

Hideki Kurihara

Yufu Sagara

Yoshikazu Nagae

Moriaki Ishikawa

Toru Fujikawa

Tomoharu Iino

Masanori Asai

Takeru Yamakawa

Makoto Jitsuoka

Akio Ohno

Takuya Suga

Minaho Uchiyama

Toshihiro Sakamoto

Takashi Hayama

Masaru Nishikibe

Kenji Ohwaki

Sayaka Mizutani

Makoto Ando

Shigemitsu Okada

Toshihiko Saeki

Hideaki Imamura

Masayuki Ogawa

Hideki Jona

Hideo Kiyonaga

Ryosuke Ushizima

Yuki Iwahori

Seita Koito

Mitsuru Miyaji

Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; Rrepresents a group of a formula: (wherein Rand Reach independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.;Rrepresents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).

Heteroaryl quinazoline derivatives

Heteroaryloxy quinazoline derivative

A compound represented by the formula (I) is contained as an active ingredient: wherein Rand Rindependently represent a hydrogen atom, a lower alkyl group or the like, or Rtogether with a nitrogen atom to which L, Zand Rare attached may form an aliphatic nitrogenated heterocyclic group and Rand Rtogether with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents &#x2014;CH&#x2014;O&#x2014;, &#x2014;CH&#x2550;CH&#x2014; or the like; Zrepresents a single bond, a Calkylene group or the like; Zrepresents a single bond or a Calkylene group; L represents a methylene group, a Ccycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.

Phenylpyridone derivative

The present invention relates to compounds of Formula (I) wherein A, B and C are independently methine, said methine being optionally substituted; D is nitrogen; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted and least two of T, U, V and W are said methine groups; X is &#x2014;N(SOR)&#x2014;, N(COR)&#x2014; or &#x2014;CO&#x2014;; Y is C(R)(R)&#x2014;, &#x2014;O&#x2014; or &#x2014;N(R) and a pharmaceutically acceptable salt, ester or N-oxide derivative thereof.

Benzimidazole derivatives

The invention provides pyridone derivatives represented by a general formula (I) 

Pyridone derivative

The present invention relates to compounds of the general formula (I):   The compounds of the present invention are useful as an agent for the treatment of a variety of diseases related to NPY.

Sulfonamide derivatives

The present invention relates to a compound of the formula (I): (wherein A,,and D are independently nitrogen or optionally substituted methine; E is nitrogen, methine or hydroxy substituted methine; n is 0 or 1; T, U, V and W are independently nitrogen or optionally substituted methine; X is &#x2014;N(SOR)&#x2014;, &#x2014;N(COR)&#x2014; or &#x2014;CO&#x2014;; Y is &#x2014;C(R)(R)&#x2014;, &#x2014;O&#x2014; or &#x2014;N(R)&#x2014;, provided that the compound (I) when E is nitrogen, n is 0, X is &#x2014;CO&#x2014;, and Y is &#x2014;O&#x2014; is excluded) and the like, which are useful as an agent for the treatment of various diseases related to NPY.

The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, wherein a methine may be optionally substituted by a substituent, and at least two of T, U, V and W are methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastro-intestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

Azole derivatives

This invention relates to compounds which exhibit selective muscarinic Mreceptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I);  [in which A signifies a group expressed by a formula (a) or (b); Ar signifies optionally substituted aryl or heteroaryl; Band Bsignify aliphatic hydrocarbon; Rsignifies fluorine-substituted cycloalkyl; R, Rand Rsignify lower alkyl, single bond or alkylene bonded to B, or Rand Rare united to signify alkylene; Rand Rsignify hydrogen, lower alkyl, or a single bond or alkylene bonded to B; Rsignifies hydrogen, lower alkyl or a group expressed as &#x2014;N(R)R; and Xsignifies an anion].

Ester derivatives

This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [a] or [b]  The compounds of the invention exhibit selective antagonism to muscarinic Mreceptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

Amide derivatives

The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

This invention relates to compounds which exhibit selective muscarinic Mreceptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I);  Ar signifies optionally substituted aryl or heteroaryl; Band Bsignify aliphatic hydrocarbon; Rsignifies fluorine-substituted cycloalkyl; R, Rand Rsignify lower alkyl, single bond or alkylene bonded to B, or Rand Rare united to signify alkylene; Rand Rsignify hydrogen, lower alkyl, or a single bond or alkylene bonded to B; Rsignifies hydrogen, lower alkyl or a group expressed as &#x2014;N(R)R; and Xsignifies an anion].

This invention relates to benzimidazolone derivatives, represented by compounds of a general formula [I]  The benzimidazolone derivatives of the invention exhibit antagonism to muscarinic acetylcholine receptors, and are useful as treating agent and/or prophylactic of Parkinson's disease, drug-induced parkinsonism, dystonia, akinesia, pancreatitis, bilestone/cholecystitis, biliary dyskinesia, achalasia, pain, itch, cholinergic urticaria, irritable bowel syndrome, vomiting, nausea, dizziness, Meniere's disease, motion sickness and urinary disturbance.

Benzimidazolone derivatives

The present invention relates to novel benzimidazole derivatives which are useful as neuropeptide Y receptor antagonists.

This invention relates to compounds which exhibit selective muscarinic Mreceptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I);

Growing community of inventors

Tsukuba, Japan

Norikazu Otake