Pfizer Corporation

Raqualia Pharma Inc.

Warner-Lambert Company

Xuanzhu Pharma Co., Ltd.

Kiyoshi Kawamura

Mikio Morita

Chikara Uchida

Tatsuya Yamagishi

Tomoki Kato

Yuji Shishido

Kazuo Ando

Sachiko Mihara

Seiji Nukui

Rodney W Stevens

Shinichi Koizumi

Kaoru Shimada

Yasuhiro Iwata

Yoshimasa Arano

Nobuyuki Takahashi

Masaki Sudo

Masashi Ohmi

Ryuichi Yamaguchi

Makiko Kuroda

Keiko Obata

Hiroaki Ito

Hengmiao Cheng

Alan Stobie

Brian S Bronk

Kazunari Nakao

Subas Man Sakya

Geoffrey E Gymer

Tadashi Inoue

Jin Li

Kristin M Lundy

Martha L Minich

Hiroki Sone

Norikazu Gaja

Kasumari Nakao

Shinya Fujiwara

Asako Ishibashi

The present invention relates to heterocyclic derivatives which have blocking activities of voltage gated sodium channels as the Nav1.7 and Nav1.8 channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

Heterocyclic derivatives as Nav1.7 and Nav1.8 blockers

The present invention relates to biaryloxy derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channel is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. 

Biaryloxy derivatives as TTX-S blockers

The present invention relates to pyrazolopyridine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. 

Pyrazolopyridine derivatives as TTX-S blockers

The present invention relates to novel compounds of a formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, pharmaceutical compositions comprising them and their use in therapy, for example as modulators of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR-1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor. 

Tetrahydropyrazolopyridine derivatives as ghrelin receptor agonists

The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example as modulators of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor. 

Serine derivatives as ghrelin receptor agonists

The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. 

Amide derivatives as TTX-S blockers

The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. 

Arylamide derivatives as TTX-S blockers

The present invention relates to pyrrolopyridinone derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. 

Pyrrolopyridinone derivatives as TTX-S blockers

The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPMb8 receptor. 

Sulfamoyl benzoic acid heterobicyclic derivatives as TRPM8 antagonists

This invention provides a compound of formula (I): wherein Rrepresents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, Rrepresents an alkyl group having from 1 to 4 carbon atoms, Rrepresents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula &#x2014;C(R)(R)&#x2014; (in which Rrepresents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and Rrepresents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HTreceptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. 

1-isopropyl-2-oxo-1,2-dihydropyridine-3-carboxamide derivatives having 5-HT4 receptor agonistic activity

Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HTreceptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HTreceptor. 

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This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents &#x3b1;; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; Rrepresents an isopropyl group, a n-propyl group or a cyclopentyl group; Rrepresents a methyl group, a fluorine atom or a chlorine atom; Rindependently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HTreceptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. 

This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R, R, R, A and m are each as described herein and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HTagonistic activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.

Indazole derivatives

This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein:A, R, R, R, Rand Rare each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HTagonistic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.

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Aichi, Japan

Kiyoshi Kawamura