Pfizer Corporation

Warner-lambert Company

Sachiko Mihara

Kiyoshi Kawamura

Hiroki Koike

Seiji Nukui

Mikio Morita

Chikara Uchida

Yoshinobu Hashizume

Yukari Matsumoto

Masako Hirota

Hiroshi Nakamura

Alan Stobie

Tomoki Kato

Geoffrey E Gymer

Asako Ishibashi

Hisoshi Nakamura

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 provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein Rand Rindependently represent a hydrogen atom or the like; Rrepresents a hydrogen atom, or the like; Rrepresents a hydrogen atom or the like; represents one of the following or the like; Rrepresents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

Alpha aryl or heteroaryl methyl beta piperidino propanamide compounds as ORL1-receptor antagonists

This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein Rand Rindependently represent a hydrogen atom or the like; These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

Alpha aryl or heteroaryl methyl beta piperidino propanoic acid compounds as ORL1-receptor antagonists

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

Pyrazoloquinolinone derivatives as protein kinase C inhibitors

Growing community of inventors

Aichi-ken, Japan

Sachiko Mihara