Pfizer Corporation

Raqualia Pharma Inc.

Asahi Kasei Pharma Corporation

Hirohide Noguchi

Yoshimasa Arano

Chikara Uchida

Fumitaka Ito

Mikio Morita

Hiroshi Kondo

Kazuo Ando

Tadashi Inoue

Yasuhiro Katsu

Kana Kon-I

Nobuaki Waizumi

Yoriko Ohashi

Toshihiko Sone

Kazuki Toyoshima

Takashi Kojima

Alan Stobie

Tatsuya Yamagishi

Geoffrey E Gymer

Kaoru Shimada

Yasuhiro Iwata

Satoru Iguchi

Toyoharu Numata

Nobuyuki Takahashi

Masaki Sudo

Masashi Ohmi

Koki Matsubara

Madoka Jinno

Isao Sakurada

Toshinori Yamamoto

Hirohisa Shimokawa

David Fenwick

The present invention relates to tetrahydroquinoline derivatives of the present invention 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 P2X7 receptor.

Tetrahydroquinoline derivatives as P2X7 receptor antagonists

This invention relates to 4-{[4-({([4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]-oxy}methyl)piperidin-1-yl]methyl}tetrahydro-2H-pyran-4-carboxylic acid for use in therapeutic treatment of the human body. In particular, it relates to the compound having selective 5-HT4 receptor agonism, which is useful for treating gastroparesis, or preventing or delaying the onset or the progression of gastroparesis.

5-HT4 receptor agonist for gastroparesis

The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.

Polymorph form of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid

The present invention relates to picolinamide 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.

Picolinamide derivatives as TTX-S blockers

This invention relates to compounds of the formula (I): wherein A, B, R, R, m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HTreceptor 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 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.

Benzisoxazole derivatives

The present invention relates to novel oxyindole derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the motilin receptor (GPR38). 

Oxyindole derivatives with motilin receptor agonistic activity

This invention provides a compound of the formula (I):or a pharmaceutically acceptable salt thereof, wherein These compounds have 5-HTreceptor binding 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 also provides a pharmaceutical composition comprising the above compound.

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This invention provides a compound of the formula (I):or a pharmaceutically acceptable salt, amide or ester thereof, wherein Rrepresents a hydrogen atom or a halogen atom; Rrepresents a hydrogen atom, etc.; Rrepresents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of Ris substituted by at least one substituent selected from the group consisting of substituents &#x3b1;; said substituents &#x3b1; is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents &#x3b1;, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms These compounds have 5-HTreceptor binding 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 also provides a pharmaceutical composition comprising the above compound.

N-substituted piperidinyl-imidazopyridine compounds as 5-HT4 receptor modulators

A compound of the formula:or a pharmaceutically acceptable salt thereof, wherein Ris unsubstituted, mono-, di- or tri-substituted (C-C)cycloalkyl or (C-C)cycloalkenyl or the like, A is unsubstituted (C-C)alkyl or (C-C)alkenyl, hydroxy-(C-C)alkyl, (C-C)alkoxy-(C&#x2550;O), or unsubstituted, mono-, di- or tri-substituted aryl, or aromatic-heterocyclic or the like, M is a covalent bond O, S, NH or the like, Y is 4- to 12-membered bicyclic-carbocyclic rings or 4- to 12-membered bicyclic-heterocyclic rings, or 5- to 17 membered spirocarbocyclic rings or 5- to 17-membered spiroheterocyclic rings or the like, Z, Z, Zand Zare hydrogen or the like, is disclosed. These compounds have ORL-receptor agonist activity, and are thus useful as analgesics or the like in mammalian subjects.

Benzimidazole compounds as ORL1-receptor agonists

Imidazopyridine compounds as 5-HT4 receptor modulators

4-(2-keto-1-benzimidazolinyl)piperidine compounds as ORL1-receptor agonists

2-substituted-1-piperidyl benzimidazole compounds as ORL1-receptor agonists

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Aichi, Japan

Hirohide Noguchi