Pfizer Corporation

Raqualia Pharma Inc.

Warner-lambert Company

Requalia Pharma Inc.

Pfizer Japan, Inc.

Kazunari Nakao

Yoshiyuki Okumura

Seiji Nukui

Tatsuya Yamagishi

Satoshi Nagayama

Misato Hirano

Hirotaka Tanaka

Rodney W Stevens

Tadashi Inoue

Yuji Shishido

Akiyoshi Kawai

Tomoki Kato

Takeshi Hanazawa

Yoshinobu Hashizume

Kana Taniguchi

Miyako Matsumizu

Katsuhiro Shinjyo

Yoriko Miyake

Naomi Ueno

Hiroki Koike

Takashi Mano

Yukari Matsumoto

Kiyoshi Kawamura

Chikara Uchida

Satoru Iguchi

Kana Kon-I

Tadashi Kawashima

Shigeo Hayashi

Kana Kon-i

Naomi Uneo

Satoshi Nahayama

This invention provides a compound of the formula (I): And their use for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound. 

Substituted N-bicyclicalkyl bicycliccarboxyamide compounds

This invention provides a compound of the formula (I): 

Substituted methyl aryl or heteroaryl amide compounds

This invention provides a compound of the formula (I): wherein A and B are independently CRor N; D and E are each independently CRor N; Rrepresents (C-C)alkyl; Rrepresents hydrogen, halogen, hydroxy, (C-C) alkyl, halo(C-C) alkyl, hydroxy(C-C) alkyl, (C-C)alkoxy or (C-C)alkoxy-(C-C)alkyl; R, R, R, R, Rand Reach independently represent hydrogen, halogen, (C-C)alkyl, halo(C-C)alkyl, (C-C)alkoxy, hydroxy(C-C)alkyl or (C-C)alkoxy-(C-C)alkyl; or Rand Rare taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; Rand Reach independently represent hydrogen, halogen, (C-C)alkyl, halo(C-C)alkyl, hydroxy(C-C)alkyl, (C-C)alkoxy, hydroxy(C-C)alkoxy, (C-C)alkoxy-(C-C)alkyl, (C-C)alkoxy-(C-C)alkoxy, (C-C)alkylthio, (C-C)alkylsulfinyl, (C-C)alkylsulfonyl, NH, [(C-C)alkyl]NH&#x2014;, [(C-C)alkyl]N&#x2014;, HN&#x2014;(C-C)alkoxy, (C-C)alkyl-NH&#x2014;(C-C)alkoxy, [(C-C)alkyl]N(C-C)alkoxy; HN&#x2014;(C-C)alkoxy-(C-C)alkyl, (C-C)alkyl-NH&#x2014;(C-C)alkoxy-(C-C)alkyl, [(C-C)alkyl]N(C-C)alkoxy-(C-C)alkyl or 5- or 6- membered heterocyclic ring containing at least one nitrogen atom; Rrepresents halogen, (C-C)alkyl, halo(C-C)alkyl, hydroxy(C-C)alkyl, (C-C)alkoxy, hydroxy(C-C)alkoxy, (C-C)alkoxy-(C-C)alkyl, (C-C)alkoxy-(C-C)alkoxy, halo(C-C)alkylsulfonyl, halo(C-C)alkylsulfinyl, halo(C-C)alkoxy, halo(C-C)alkylthio, [(C-C)alkyl]NH&#x2014; or [(C-C)alkyl]N&#x2014;; or Rand R, when E is CR, are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C-C)alkyl, (C-C)alkoxy and hydroxy(C-C)alkyl; and Rrepresents hydrogen, halogen, (C-C)alkyl or hydroxy(C-C)alkyl; or a pharmaceutically acceptable salt or solvate thereof.

Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists

This invention provides a compound of the formula (I): wherein, variables A, B, D, E, and Rto Rare as defined in the specification.

This invention provides compounds of the formula (I) useful for the treatment of disease conditions caused by over activation of Vr1 receptors such as pain or the like in mammals as well as compositions comprising them.

Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists

This invention provides a compound of the formula (I): wherein

This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y, Y, Yand Yare independently selected from N, CH, etc.; Ris H, Calkyl, etc.; Qis a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is Calkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; Ris H, Calkyl, etc.; Z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, Calkyl, etc.; m is 0, 1 or 2; Rand Rare independently selected from H and Calkyl ; Ris H, Calkyl, etc.; Qis a 5-12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamadin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; Rand Rindependently represent a hydrogen atom or the like: Rand Rindependently represent a hydrogen atom or the like: Rrepresents &#x2014;COH or the like: Rrepresents an alkyl group having from 1 to 6 carbon atoms or the like: X represents a methylene group or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

Aryl or heteroaryl amide compounds

This invention provides a compound of the formula (I): wherein Rrepresents a (C&#x2013;C)alkyl group; Rrepresents a hydrogen atom, a halogen atom, a hydroxy group, a (C&#x2013;C)alkyl group or a (C&#x2013;C)alkoxy group; R, R, Rand Reach independently represents a hydrogen atom, a (C&#x2013;C)alkyl, or a halogen atom; Rrepresents a hydrogen atom, a halogen atom, a hydroxy group, a (C&#x2013;C)alkyl group optionally substituted with a piperidino group, a (C&#x2013;C)alkoxy group optionally substituted with a 3&#x2013;7 membered cycloalkyl ring, a hydroxy(C&#x2013;C)alkoxy group, a (C&#x2013;C)alkoxy-(C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy-(C&#x2013;C)alkoxy group, a halo (C&#x2013;C)alkyl group, a (C&#x2013;C)alkylthio group, a (C&#x2013;C)alkylsulfinyl group or a (C&#x2013;C)alkylsulfonyl group; Rrepresents a (C&#x2013;C)alkyl group, a halo(C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy group, a hydroxy(C&#x2013;C)alkoxy group, a (C&#x2013;C)alkoxy-(C&#x2013;C)alkyl group or a (C&#x2013;C)alkoxy-(C&#x2013;C)alkoxy group; or Rand R, when adjacent to each other, taken together with the carbon atoms to which they are attached form a 5&#x2013;8 membered carbocyclic or heterocyclic ring, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents selected from the group consisting of a hydroxy group, a (C&#x2013;C)alkyl group, a (C&#x2013;C)alkoxy group and a hydroxy(C&#x2013;C)alkyl group; and Rrepresents a hydrogen atom or a halogen atom; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor, such as pain or the like in mammalian. The present invention also provides a pharmaceutical composition comprising the compound of formula(I).

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This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof, wherein Y, Y, Yand Yare independently selected from N, CH, etc.; Ris H, Calkyl, etc.; Qis a 5&#x2013;12 membered monocyclic or bicyclic aromatic ring optionally containing up to 4 heteroatoms selected from O, N and S, etc.; A is a 5&#x2013;6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; B is Calkylene optionally substituted with an oxo group, etc.; W is NH, O, etc.; Ris H, Calkyl, etc.; Z is a 5&#x2013;12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc.; L is halo, Calkyl, etc.; m is 0, 1 or 2; Rand Rare independently selected from H and Calkyl; Ris H, Calkyl, etc.; Qis a 5&#x2013;12 membered monocyclic or bicyclic aromatic ring or tricyclic ring optionally containing up to 3 heteroatoms selected from O, N and S, etc. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.

This invention provides a compound of the formula (I):wherein:

Pyrazole compounds as anti-inflammatory and analgesic agents

This invention provides a compound of the formula (I):wherein: These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.

Imidazole compounds as anti-inflammatory and analgesic agents

This invention provides a compound of the following formula:

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Aichi-ken, Japan

Kazunari Nakao