Pfizer Corporation

Raqualia Pharma Inc.

Asahi Kasei Pharma Corporation

Kazuo Ando

Tomoki Kato

Akiyoshi Kawai

Tomomi Nonomura

Kiyoshi Kawamura

Masashi Ohmi

Masami Nakane

Kunio Satake

Hirohide Noguchi

Takashi Mano

Yoshimasa Arano

Kazuki Toyoshima

Toshihiko Sone

Ryohei Magara

Fumitaka Ito

Hengmiao Cheng

Rodney W Stevens

Yuji Shishido

Tatsuya Yamagishi

Brian S Bronk

Subas Man Sakya

Hiroaki Wakabayashi

Makoto Kawai

Yasuhiro Iwata

Tsutomu Masuda

Takafumi Ikeda

Jin Li

Kaoru Shimada

Kristin M Lundy

Martha L Minich

Kana Kon-I

Koki Matsubara

Ryuichi Yamaguchi

Nobuko Asai

Mikito Takefuji

Hirofumi Omura

Yutaka Fukumoto

Takeshi Matsushita

Yohei Yuki

The present invention relates to 3-hydroxyoxindole derivatives which have antagonistic activities against CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR2 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 CRHR2 is involved.

3-hydroxyoxindole derivatives as CRHR2 antagonist

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

The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 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 CRHR1 and/or CRHR2 is involved.

Fused cyclic urea derivatives as CRHR2 antagonist

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

This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R, R, R, R, R, R, R, k, m, n, p, q, r and s are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity. 

N-substituted saturated heterocyclic sulfone compounds with CB2 receptor agonistic activity

This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R, Rand Rare each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or bronchitis. 

Benzimidazolone derivatives as CB2 receptor ligands

This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R, R, R, R, R, m and n are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, GERD, constipation, diarrhea, functional gastrointestinal disorders, irritable bowel syndrome, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, COPD, cryptogenic fibrosing alveolitis and bronchitis. 

Sulfonyl benzimidazole derivatives

This invention relates to a compound of the formula:or a pharmaceutically acceptable salt thereof, wherein A and Rare each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; Ris NH; Rand Rare each hydrogen, halo, (C-C)alkyl optionally substituted with halo and the like; and Xto Xare each hydrogen, halo, hydroxy, (C-C)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.

Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents

This invention provides a compound of the formula:or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; Ris optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, Ris heteroaryl; Ris Calkyl; halo-substituted Calkyl, Calkylamino, Cdialkylamino or amino; R, Rand Rare independently hydrogen, halo, Calkyl, halo-substituted Calkyl or the like; or two of R, Rand Rare taken together with atoms to which they are attached and form a 4-7 membered ring. Rand Rare independently hydrogen, halo, Calkyl, halo-substituted Calkyl, Calkoxy, Calkylthio, Calkylamino or N,N-di Calkylamino; and m and n are independently 1, 2, 3 or 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.

Sulfonylbenzene compounds as anti-inflammatory/analgesic agents

Heteroaryl phenyl pyrazole compounds as anti-inflammatory/analgesic agents

Sulfamoylheleroaryl pyrazole compounds as anti-inflammatory/analgesic agents

This invention provides a compound of the formula:

Growing community of inventors

Aichi-ken, Japan

Kazuo Ando