A method of treating, preventing or inhibiting a disorder selected from the group consisting of cardiovascular or heart related diseases such as stroke, hypertension, tachycardia, and congestive heart failure, osteoporosis, premature birth, psychosocial dwarfism, stress-induced fever, ulcer, diarrhea, post-operative ileus, and colonic hypersensitivity associated with psychopathological disturbance and stress, comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of the formula ##STR1##or a pharmaceutically acceptable salt thereof, wherein A, B, D, E, Y, Z, R.sub.3, R.sub.4, and R.sub.5 are as defined herein.

Pfizer Inc

Corticotropin releasing factor antagonists

Provided is a compound useful as an N-type Ca.sup.2+ channel blocker. As a result of intensive studies of compounds having an action of blocking N-type Ca.sup.2+ channels, the present inventors found that a tetrahydroisoquinoline compound of the present invention having a substituent at the 1-position has an action of blocking the N-type Ca.sup.2+ channels, an antinociceptive pain action, an antineuropathic pain action, an abdominal pain-inhibitory action and an opioid-induced constipation-improving action, and the present invention has been completed based on these findings. The compound of the present invention can be used as a pharmaceutical composition for preventing and/or treating various pains such as neuropathic pain and nociceptive pain, headaches such as migraine and cluster headache, central nervous system diseases such as anxiety, depression, epilepsy, cerebral stroke and restless legs syndrome, abdominal symptoms such as abdominal pain and abdominal distension, stool abnormalities such as diarrhea and constipation, digestive system diseases such as irritable bowel syndrome, urinary system diseases such as overactive bladder and interstitial cystitis, etc.

Astellas Pharma Inc.

1-substituted tetrahydroisoquinoline compound

This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R.sup.1, R.sup.2 and R.sup.3 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 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. ##STR00001##

Pfizer Inc.

Benzimidazolone derivatives as CB2 receptor ligands

This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, 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. ##STR00001##

Sulfonyl benzimidazole derivatives

Fused-ring system N-alkylpiperidinyl-4-methyl carboxylic acid ester or amide derivs. and analogues (D, having formula (I-1)-(I-5), and their salts. The variables are defined herein. The compounds (I) are 5-HT4 receptor antagonists, and are useful for treatment or prophylaxis of gastrointestinal, cardiovascular or CNS disorders. Typically (I) are used for treatment of irritable bowel syndrome (including associated diarrhea and urinary incontinence); for treatment of the nausea and gastric symptoms of gastro-oesophageal reflux disease and dyspepsia; as antiemetics (e.g. against cytotoxin agent or radiation-induced emesis); for preventing atrial fibrillation and other atrial arrhythmias and reducing occurrence of stroke; as anxiolytics; and for treatment of migraine, schizophrenia, Parkinson's disease and Huntington's chorea.

diarrhea/stroke

Corticotropin releasing factor antagonists

1-substituted tetrahydroisoquinoline compound

Benzimidazolone derivatives as CB2 receptor ligands

Sulfonyl benzimidazole derivatives

N-alkylpiperidinyl-4-methyl carboxylic esters/amides of condensed ring systems as 5-HT4 receptor antagonists

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