Pfizer Corporation

Warner-lambert Company

Chikara Uchida

Kiyoshi Kawamura

Hiroki Sone

Hirohide Noguchi

Satoru Iguchi

Mikio Morita

Koji Ando

Tomoki Kato

Toyoharu Numata

Noriaki Murase

Yoshinori Murata

Yasuhiro Katsu

Tatsuo Ueki

Alan Stobie

Seiji Nukui

Rodney W Stevens

Geoffrey E Gymer

Kana Kon-I

Sachiko Mihara

Hengmiao Cheng

Kazunari Nakao

Subas Man Sakya

Jin Li

Kristin M Lundy

Martha L Minich

Nobuaki Waizumi

Saturu Iguchi

Takashi Kojima

David Fenwick

Kasumari Nakao

Shinya Fujiwara

Isao Sakurada

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

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

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. 

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This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for 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. 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.

Benzimidazolone compounds having 5-HT4 receptor agonistic activity

This invention relates to compounds of the formula (I): wherein R, R, R, A and m are each as described herein or a pharmaceutically acceptable salt or solvate 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 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.

Benzimidazolone carboxylic acid 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.

Oxyindole derivatives

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.

This invention provides compounds of the formula (I) and (II):or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein Ris hydrogen or halo; Rand Rare independently hydrogen or Calkyl; Rand Rare independently hydrogen or Calkyl; Ris hydrogen, Calkyl, Calkoxy (C)alkyl or Calkyl substituted by up to 3 substituents selected from the groups consisting of Ccycloalkyl, aryl, heteroaryl and heterocyclic; Rand Rare hydrogen or taken together may form alkylene chain having one or two carbon atoms; Ris Calkyl or Ccycloalkyl; Ris Calkyl or NRR; L is (CRR)or NR; M is NRor (CRR); Rand Rare independently hydrogen or Calkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and Calkyl; with the proviso that when Ris Calkyl, L is not NR. These compounds have 5-HTreceptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators

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

Pyrazoloquinolinone derivatives as protein kinase C inhibitors

Imidazopyridine compounds as 5-HT4 receptor modulators

Heterocyclo-alkylsulfonyl pyrazole derivatives as anti-inflammatory/analgesic agents

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Chita-gun, Japan

Chikara Uchida