Pfizer Corporation

Raqualia Pharma Inc.

Warner-lambert Company

Xuanzhu Pharma Co., Ltd.

Yuji Shishido

Tadashi Inoue

Satoshi Nagayama

Hirotaka Tanaka

Kiyoshi Kawamura

Tatsuya Yamagishi

Kazunari Nakao

Mikio Morita

Hiroaki Wakabayashi

Masashi Ohmi

Misato Hirano

Takeshi Hanazawa

Ryuichi Yamaguchi

Kunio Satake

Takafumi Ikeda

Noriaki Murase

Mitsuhiro Kawamura

Norikazu Gaja

Hiroaki Ito

Seiji Nukui

Kazuo Ando

Yoshiyuki Okumura

Masami Nakane

Tomoki Kato

Kaoru Shimada

Masaya Ikunaka

Makoto Kawai

Tadashi Kawashima

Yasuhiro Katsu

Makato Kawai

Satoshi Nahayama

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 amide 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. 

Amide 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 azaspiro 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 TRPM8 receptor. 

Azaspiro derivatives as TRPM8 antagonists

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

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 relates to novel substituted pyridylmethyl bicyclocarboxamide compounds and to their use in therapy. These compounds are particularly useful as modulators of the VR1 (Type I Vanilloid) receptor, and are thus useful for the treatment of pain, neuralgia, neuropathies, nerve injury, burns, migraine, carpal tunnel syndrome, fibromyalgia, neuritis, sciatica, pelvic hypersensitivity, bladder disease, inflammation, or the like in mammals, especially humans.

Substituted pyridylmethyl bicycliccarboxyamide 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

Compounds of the general formula (I): pharmaceutical compositions comprising a compound of general formula (I); and methods of treating disease conditions caused by overactivation of the VR1 receptor by administering a compound of general formula (I) to a subject.

Substituted aryloxymethyl bicyclicmethyl acetamide compounds

1,4-dihydropyridine compounds as bradykinin antagonists

Substituted benzylaminopiperidine compounds

5-membered heteroaryl substituted 1,4-dihydropyridine compounds as bradykinin antagonists

The invention provides a substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by,or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.

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Aichi-ken, Japan

Yuji Shishido